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(4-methyl-7-[[(2S)-2-(4-[(1S)-1-(4-methylcyclohexyl)-1-[(thiophen-3-ylcarbonyl)amino]ethyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-2-oxo-2H-chromen-3-yl)acetic acid + H2O
?
-
-
-
-
?
(7-methoxycoumarin-4-yl)-acetyl-GRWHPMGAPWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
(7-methoxycoumarin-4-yl)-acetyl-GRWHPMG + APWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
specific substrate for CatS
-
-
?
(7-methoxycoumarin-4-yl)-acetyl-GRWPPMGLPWEK(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
(7-methoxycoumarin-4-yl)-acetyl-GRWPPMG + LPWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
specific substrate for CatS
-
-
?
(7-[[(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(phenylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-2H-chromen-3-yl)acetic acid + H2O
?
-
-
-
-
?
(7-[[(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(thiophen-3-ylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-2H-chromen-3-yl)acetic acid + H2O
?
-
-
-
-
?
(7-[[(2S)-2-(4-[(1S)-1-cyclohexyl-1-[(phenylcarbonyl)amino]ethyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-2H-chromen-3-yl)acetic acid + H2O
?
-
-
-
-
?
(7-[[(2S)-2-(4-[(1S)-1-cyclohexyl-1-[(thiophen-3-ylcarbonyl)amino]ethyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-2H-chromen-3-yl)acetic acid + H2O
?
-
-
-
-
?
(benzyloxycarbonyl-Phe-Arg)2-rhodamine 110 + H2O
?
-
-
-
-
?
10 kDa fragment of the lysosomal MHCII-bound invariant chain + H2O
class II associated invariant chain peptide fragments
-
li p10
-
-
?
Ac-His-Pro-Val-Lys-7-amido-3-carbamoylmethyl-4-methylcoumarin + H2O
Ac-His-Pro-Val-Lys + 7-amino-3-carbamoylmethyl-4-methylcoumarin
-
assay at pH 5.5, 37°C
-
-
?
Arg-7-amido-4-methylcoumarin + H2O
Arg + 7-amino-4-methylcoumarin
arresten + H2O
?
-
degradation, recombinant enzyme
-
-
?
benzoyl-Phe-Val-Arg-7-amido-4-methylcoumarin + H2O
benzoyl-Phe-Val-Arg + 7-amino-4-methylcoumarin
benzyloxycarbonyl-L-Val-L-Val-L-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-L-Val-L-Val-L-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Leu-Arg + 7-amino-4-methylcoumarin
benzyloxycarbonyl-Leu-Leu-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Leu-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Lys-4-nitrophenyl ester + H2O
benzyloxycarbonyl-Lys + 4-nitrophenol
-
-
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
benzyloxycarbonyl-Phe-Val-Arg-7-amido-4-methylcoumarin
benzyloxycarbonyl-Phe-Val-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Phe-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Val-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Val-Val-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
benzyloxycarbonyl-Val-Val-Arg-4-methyl-coumaryl-7-amide + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
?
-
-
-
-
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-L-Val-L-Val-L-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
Boc-Val-Leu-Lys-7-amido-4-methylcoumarin + H2O
Boc-Val-Leu-Lys + 7-amino-4-methylcoumarin
-
-
-
-
?
butyloxycarbonyl-L-Phe-L-Phe-L-Arg-7-amido-4-methylcoumarin + H2O
butyloxycarbonyl-L-Phe-L-Phe-L-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
butyloxycarbonyl-Val-Leu-Lys-7-amido-4-methylcoumarin + H2O
butyloxycarbonyl-Val-Leu-Lys + 7-amino-4-methylcoumarin
canstatin + H2O
?
-
degradation, recombinant enzyme
-
-
?
cathepsin K + H2O
?
cathepsin S cleaves cathepsin K (cathepsin cannibalism) which reduces the total elastin- and collagen-degradative activity in the multiple cathepsin system
-
-
?
CBZ-Val-Val-Arg- 7-amino-4-trifluoromethyl coumarin + H2O
?
-
-
-
?
Cbz-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
Cbz-Val-Val-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
CX3CL1 + H2O
?
cathepsin S is able to cleave membrane-anchored CX3CL1, releasing a 55-kDa fragment to the medium
-
-
?
elastin + H2O
elastin fragments
-
-
catS generates soluble elastin peptides
-
?
fractalkine + H2O
?
-
-
-
-
?
GRWH-norleucine-VGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWH-norleucine-VG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHDVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHDVG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHFVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHFVG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHGVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHGVG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHIVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHIVGL + RWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHKFSVRWE + H2O
?
-
-
-
?
GRWHKISVRWE + H2O
?
-
-
-
?
GRWHKLSVRWE + H2O
?
-
-
-
?
GRWHKVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHKVG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHKVSVRWE + H2O
GRWHKVS + VRWE
-
-
-
?
GRWHPVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHPVG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHT-norleucine-GLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHT-norleucine-G + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTDGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTDG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTFGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTFG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTGGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTGG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTIGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTIG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTKGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTKG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTMGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTMG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTPGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTPG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTTGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTTG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTV-norleucine-LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTV-norleucine + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVDLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVD + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVFLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVF + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVG-citrulline-RWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + citrulline-RWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVG-norleucine-RWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + norleucine-RWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVGFRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + FRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVGIRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + IRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVGKRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + KRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVGLDWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LDWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVGLFWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LFWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVGLHWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LHWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVGLIWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LIWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVGLKWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LKWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVGLPWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LPWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVGLQWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LQWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVGLRDE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LRDE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVGLRFE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LRFE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVGLRGE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LRGE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVGLRHE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LRHE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVGLRIE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LRIE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVGLRKE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LRKE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVGLRRE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LRRE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
GRWHTVG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
specific substrate for CatS
-
-
?
GRWHTVGRRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + RRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVGVRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + VRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVILRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVI + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVKLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVK + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVPLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVP + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVQLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVQ + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHTVTLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVT + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
GRWHVVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHVVG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
-
-
-
?
haemoglobin + H2O
?
-
-
-
-
?
Ii protein + H2O
Ii fragments
Ii-p10 + H2O
?
-
i.e. MHC classe-associated invariant chain, cathepsin S is the only human cysteine protease able to efficiently degrade the Ii-p10 fragment in epithelial cells
-
-
?
invariant chain + H2O
?
-
invariant chain li is degraded by CatS to the class II-associated invariant chain peptide which dissociates from the MHC-II molecule by forming a complex with the human leucocyte antigen-DM
-
-
?
L-Leu-Leu-Arg-7-amido-4-methylcoumarin + H2O
L-Leu-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
?
laminin alpha5-chain + H2O
?
the laminin-alpha5-chain is cleaved by CatS specifically at the Ser-Val bond
-
-
?
laminin-5 + H2O
laminin-5 gamma-2 fragments
leupeptin-induced peptide LIP10 + H2O
?
-
-
-
-
?
MHC class II-associated invariant chain Ii + H2O
?
MHCII-class assosciated invariant chain li + H2O
class II invariant chain peptide fragments
-
-
-
-
?
myelin basic protein + H2O
?
N-benzyloxycarbonyl-L-Phe-Arg-7-amido-4-methylcoumarin + H2O
N-benzyloxycarbonyl-L-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
N-benzyloxycarbonyl-Phe-Arg-4-nitroanilide + H2O
N-benzyloxycarbonyl-Phe-Arg + 4-nitroaniline
-
-
-
?
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1,2-dimethylpropyl]benzamide + H2O
?
-
-
-
-
?
o-aminobenzoic acid-Ala-Thr-Pro-Leu-Leu-Met-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Ala-Thr-Pro-Leu-Leu + Met-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
-
80% cleavage site, 20% cleavage site: o-aminobenzoic acid-Ala-Thr-Pro-Leu-Leu-Met + Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
?
o-aminobenzoic acid-Gly-Arg-Leu-Asp-Lys-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Gly-Arg-Leu-Asp + Lys-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
-
-
-
?
o-aminobenzoic acid-Gly-Phe-Phe-Val-Thr-Thr-Pro-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Gly-Phe-Phe + Val-Thr-Thr-Pro-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
-
-
-
?
o-aminobenzoic acid-His-Leu-Val-Glu-Ala-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-His-Leu-Val-Glu + Ala-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
-
-
-
?
o-aminobenzoic acid-His-Leu-Val-Glu-Ala-Leu-Tyr-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-His-Leu-Val-Glu + Ala-Leu-Tyr-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
-
56% cleavage site, 44% cleavage site: o-aminobenzoic acid-His-Leu-Val-Glu-Ala-Leu + Tyr-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
?
o-aminobenzoic acid-Leu-Arg-Met-Lys-Leu-Pro-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Leu-Arg-Met-Lys + Leu-Pro-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
-
74% cleavage site, 26% cleavage site: o-aminobenzoic acid-Leu-Arg + Met-Lys-Leu-Pro-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
?
o-aminobenzoic acid-Leu-Gln-Leu-Glu-Asn-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Leu-Gln + Leu-Glu-Asn-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
-
57% cleavage site, 42% cleavage site: o-aminobenzoic acid-Leu-Gln-Leu-Glu + Asn-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
?
o-aminobenzoic acid-Leu-Glu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Leu-Glu + Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
-
-
-
?
o-aminobenzoic acid-Leu-Phe-Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine + H2O
o-aminobenzoic acid-Leu-Phe + Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
-
-
-
?
o-aminobenzoic acid-Leu-Tyr-Leu-Val-Cys-Gly-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Leu-Tyr-Leu + Val-Cys-Gly-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
-
70% cleavage site, 30% cleavage site: o-aminobenzoic acid-Leu-Tyr + Leu-Val-Cys-Gly-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
?
o-aminobenzoic acid-Lys-Pro-Pro-Val-Val-Leu-Leu-Pro-Asp-Gln-N-(2,4-dinitrophenyl)ethylendiamine + H2O
o-aminobenzoic acid-Lys-Pro-Pro-Val-Val-Leu + Leu-Pro-Asp-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
-
-
-
?
o-aminobenzoic acid-Lys-Pro-Val-Ser-Thr-Glu-Gln-Leu-Ala-Gln-N-(2,4-dinitrophenyl)ethylendiamine + H2O
o-aminobenzoic acid-Lys-Pro-Val-Ser + Thr-Glu-Gln-Leu-Ala-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
-
-
-
?
o-aminobenzoic acid-Phe-Val-Asn-Gln-His-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Phe-Val-Asn + Gln-His-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
-
69% cleavage site, 31% cleavage site: o-aminobenzoic acid-Glu-Val + Asn-Gln-His-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
?
o-aminobenzoic acid-Ser-Arg-His-Ser-Leu-Glu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Ser-Arg-His-Ser-Leu-Glu + Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
-
-
-
?
o-aminobenzoic acid-Val-Leu-Phe-Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine + H2O
o-aminobenzoic acid-Val-Leu-Phe + Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
-
-
-
?
o-aminobenzoic acid-Val-Leu-Phe-Glu-Lys-Lys-Val-Tyr-Leu-Gln-N-(2,4-dinitrophenyl)ethylendiamine + H2O
o-aminobenzoic acid-Val-Leu-Phe-Glu-Lys-Lys-Val-Tyr + Leu-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
-
-
-
?
Oxidized insulin B-chain + H2O
?
-
major cleavage sites: Glu13-Ala14, Leu17-Val18 and Phe25-Tyr26. Minor cleavage sites: Asn3-Gln4, Ser9-His10 and Leu15-Tyr16
-
-
?
plasminogen + H2O
?
-
-
cleavage occurs at the Leu469-Leu470 peptide bond resulting in 2 fragments: 60000 Da and 38000 Da
-
?
prion protein 94-233 + H2O
prion protein 135-233 + prion protein 117-233 + prion protein 114-233
-
in vitro, enzyme causes specific and limited N-terminal truncation of prion protein 94-233
major soluble fragments, the region of prion protein between S135 and N146 is a major target for selective cleavage cathepsins S
-
?
pro-dipeptidyl peptidase I + H2O
?
-
i.e. cathepsin C, less efficient activation than with cathepsin L
-
-
?
protease-activated receptor-2 + H2O
?
tert-butyloxycarbonyl-Phe-Leu-Arg-7-amido-4-methylcoumarin + H2O
tert-butyloxycarbonyl-Phe-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
tert-butyloxycarbonyl-Phe-Phe-Arg-7-amido-4-methylcoumarin + H2O
tert-butyloxycarbonyl-Phe-Phe-Arg + 7-amino-4-methylcoumarin
Val-Arg-coumarin + H2O
?
-
-
-
-
?
Val-Val-Arg + H2O
?
-
-
-
-
?
Z-Leu-Arg-7-amido-4-methylcoumarin + H2O
Z-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Z-Leu-Leu-Arg-7-amido-4-methylcoumarin + H2O
Z-Leu-Leu-Arg + 7-amino-4-methylcoumarin
Z-Phe-Arg-AMC + H2O
?
-
-
-
-
?
Z-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
Z-Val-Val-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Z-Val-Val-Arg-AMC + H2O
?
-
-
-
-
?
additional information
?
-
Albumin + H2O
?
-
-
-
-
?
Albumin + H2O
?
-
-
-
-
?
Albumin + H2O
?
-
degradation
-
-
?
Arg-7-amido-4-methylcoumarin + H2O
Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Arg-7-amido-4-methylcoumarin + H2O
Arg + 7-amino-4-methylcoumarin
-
no activity detected
-
-
?
azocasein + H2O
?
-
high activity in presence of urea at pH 5.5
-
-
?
azocasein + H2O
?
-
reaction only in presence of urea
-
-
?
benzoyl-Phe-Val-Arg-7-amido-4-methylcoumarin + H2O
benzoyl-Phe-Val-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzoyl-Phe-Val-Arg-7-amido-4-methylcoumarin + H2O
benzoyl-Phe-Val-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Val-Val-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Val-Val-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
-
-
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
73% of the activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
-
-
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
butyloxycarbonyl-Val-Leu-Lys-7-amido-4-methylcoumarin + H2O
butyloxycarbonyl-Val-Leu-Lys + 7-amino-4-methylcoumarin
-
-
-
-
?
butyloxycarbonyl-Val-Leu-Lys-7-amido-4-methylcoumarin + H2O
butyloxycarbonyl-Val-Leu-Lys + 7-amino-4-methylcoumarin
-
-
-
-
?
Collagen + H2O
?
-
-
-
-
?
Collagen + H2O
?
-
-
-
-
?
Collagen + H2O
?
-
degradation
-
-
?
Collagen + H2O
?
-
-
-
-
?
Collagen + H2O
?
-
alpha-chain
-
-
?
Collagen type I + H2O
?
-
degradation
-
-
?
Collagen type I + H2O
?
-
degradation in plasma membranes
-
-
?
Elastin + H2O
?
-
can hydrolyze insoluble elastin at acid and neutral pH
-
-
?
Elastin + H2O
?
-
-
-
-
?
Elastin + H2O
?
-
degradation
-
-
?
Elastin + H2O
?
-
degradation in plasma membranes
-
-
?
Elastin + H2O
?
-
elastolytic enzyme activity of cathepsin S in artherosclerotic lesions, degradation of aortic elastin contributing to atherosclerosis and diabetes
-
-
?
Elastin + H2O
?
-
degradation, elastolytic enzyme activity of cathepsin S
-
-
?
Elastin + H2O
?
-
the enzyme shows distinctive preferences in degrading elastins from bovine neck ligament, aorta, and lung
-
-
?
Gelatin + H2O
?
-
-
-
-
?
Gelatin + H2O
?
-
alpha-chain
-
-
?
Hemoglobin + H2O
?
-
-
-
-
?
Hemoglobin + H2O
?
-
degradation
-
-
?
Ii protein + H2O
Ii fragments
-
-
-
-
?
Ii protein + H2O
Ii fragments
-
degradation
-
-
?
Ii protein + H2O
Ii fragments
-
inhibition of Ii degradation in enzyme-deficient cells leads to accumulation of Ii degradation intermediates in endosomal/lysosomal compartments
-
-
?
Ii protein + H2O
Ii fragments
-
Ii invariant chain
-
-
?
Ii protein + H2O
Ii fragments
-
inhibition of Ii degradation in enzyme-deficient cells leads to accumulation of Ii degradation intermediates in endosomal/lysosomal compartments
-
-
?
Ii protein + H2O
Ii fragments
-
Ii invariant chain
-
-
?
insulin + H2O
?
-
-
-
-
?
insulin + H2O
?
-
degradation
-
-
?
laminin-5 + H2O
laminin-5 gamma-2 fragments
-
degradation
bioactive gamma2-fragments of 100 kDa, 80 kDa, and 50 kDa
-
?
laminin-5 + H2O
laminin-5 gamma-2 fragments
-
degradation
-
-
?
laminin-5 + H2O
laminin-5 gamma-2 fragments
-
degradation
-
-
?
MHC class II-associated invariant chain Ii + H2O
?
-
degradation
-
-
?
MHC class II-associated invariant chain Ii + H2O
?
-
degradation, cathepsin S and MHC class II-associated invariant chain Ii are responsible for in vivo control of endosomal size and multivesicular morphology
-
-
?
myelin basic protein + H2O
?
-
-
-
-
?
myelin basic protein + H2O
?
-
degradation
-
-
?
protease-activated receptor-2 + H2O
?
-
-
-
?
protease-activated receptor-2 + H2O
?
-
-
-
?
tert-butyloxycarbonyl-Phe-Phe-Arg-7-amido-4-methylcoumarin + H2O
tert-butyloxycarbonyl-Phe-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
tert-butyloxycarbonyl-Phe-Phe-Arg-7-amido-4-methylcoumarin + H2O
tert-butyloxycarbonyl-Phe-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Z-Leu-Leu-Arg-7-amido-4-methylcoumarin + H2O
Z-Leu-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Z-Leu-Leu-Arg-7-amido-4-methylcoumarin + H2O
Z-Leu-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
?
Z-Leu-Leu-Arg-7-amido-4-methylcoumarin + H2O
Z-Leu-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Z-Leu-Leu-Arg-7-amido-4-methylcoumarin + H2O
Z-Leu-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
?
additional information
?
-
-
the enzyme prefers small neutral amino acid residues in the subsites S2 and S3
-
-
?
additional information
?
-
-
cathepsin S catalyzes a key step in antigen presentation, detailed overview
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
key protease responsible for the removal of the invariant chain from MHC class II molecules, the enzyme plays a major role in antigen presentation
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
cathepsin S is considered crucial for normal presentation of major histocompatibility complex class II-restricted antigens by antigen presenting cells to CD4+ T cells. It is a key enzyme for the degradation of the class II-associated invariant chain, a process that is required for effective antigen loading of class II molecules
-
-
?
additional information
?
-
-
the enzyme may contribute to the contact-dependent elastase activity of live human alveolar macrophages
-
-
?
additional information
?
-
-
Cat S is involved in degradtion of extracellular matrix and smooth muscle cell invasion, but not in adhesion and migration, overview, the enzyme shows elastolytic and collagenolytic activities on smooth muscle cell plasma membranes, overview
-
-
?
additional information
?
-
-
cathepsin S catalyzes a key step in antigen presentation, detailed overview, Cat S might be involved in psoriasis induction due to an increased interferon gamma level in the epidermis, Cat S is increased in neurons of Alzheimer's disease and Down's syndrome patients, where Cat S facilitates the formation of amyloidbeta from its precursor protein, Cat S might also be involved in asthma, Sjörgren's syndrome, allergen-specific T-cell proliferation in autoimmune processes, and atherosclerosis, overview
-
-
?
additional information
?
-
-
cathepsin S controls angiogenesis and tumor growth via matrix-derived angiogenic factors, the enzyme is required for neoplastic progression, overview
-
-
?
additional information
?
-
-
serum cathepsin S is increased in patients with atherosclerosis and diabetes, the cystatin C level might play a role in disease development, overview
-
-
?
additional information
?
-
-
the enzyme is involved in obesity and development of adiposity, enzyme regulation in subcutaneous adipose tissue, cathepsin S is upregulated in obesity, overview
-
-
?
additional information
?
-
-
active Cat S co-localizes with integrins, e.g. integrin alphanubeta3
-
-
?
additional information
?
-
-
Cat S forms an alpha-beta-CLIP complex, unlike CatB or CatD, from an alpha-beta-Ii molecule in vitro
-
-
?
additional information
?
-
does not cleave GRWHKISVRWE
-
-
?
additional information
?
-
-
does not cleave GRWHKISVRWE
-
-
?
additional information
?
-
cathepsin S is putatively involved in the pathogenesis of COPD
-
-
?
additional information
?
-
-
cathepsin S is putatively involved in the pathogenesis of COPD
-
-
?
additional information
?
-
-
CatS is capable of degrading a range of extracellular matrix macromolecules
-
-
?
additional information
?
-
-
CatS is identified as a compound involved in MHC class II maturation and trafficking within antigen presentation pathways, as well as in the control of processing antigens and the formation of peptide-receptive class II dimers
-
-
?
additional information
?
-
-
CatS is one of the major proteases involved in antigen processing
-
-
?
additional information
?
-
CTSS is a cysteine protease that has a central role in remodeling the extracellular matrix and it is implicated in the etiology of cardiovascular disease
-
-
?
additional information
?
-
-
CTSS is a cysteine protease that has a central role in remodeling the extracellular matrix and it is implicated in the etiology of cardiovascular disease
-
-
?
additional information
?
-
-
enzyme mediates degradation of the MHC class II invariant chain and participates in antigen processing
-
-
?
additional information
?
-
in antigen presenting cells Cat S plays an essential role in the proteolytic events that lead to antigen presentation at the cells surface for recognition by T cells
-
-
?
additional information
?
-
-
in the case of atherosclerotic lesions, the local extracellular matrix is degraded either by CatS secreted by smooth muscle cells and macrophages or by circulating CatS produced by adipose tissue, this elastolytic activity of CatS causes the migration of blood monocytes and smooth muscle cells into the vascular wall which leads to the progression of atherosclerotic lesions
-
-
?
additional information
?
-
major role of Cat S in these cells is the processing of the major histocompatibility complex class II associated invariant chain, which is essential for the normal functioning of the immune system, Cat S is largely responsible for the last proteolytic cleavage step of the invariant chain that produces class II-associated leupeptin induced peptide
-
-
?
additional information
?
-
-
protease is implicated in the development of atherosclerotic lesions in both animal
-
-
?
additional information
?
-
-
the cysteine protease cathepsin S is involved in the pathogenesis of autoimmune disorders, atherosclerosis and obesity
-
-
?
additional information
?
-
-
the function of cathepsin S within antigen presenting cells relates to its pivotal role in major histocompatibility class II restricted antigen presentation to CD4+ T-lymphocytes, cathepsin S mediates the final proteolytic cleavage of the invariant chain chaperone molecule 2 thereby facilitating the subsequent presentation of MHC-II associated peptides to CD4+ T-cells
-
-
?
additional information
?
-
-
the major role of CAT S is the processing of the major histocompatibility complex (MHC) class II associated invariant chain, which is essential for the normal functioning of the immune system
-
-
?
additional information
?
-
this enzyme serves a crucial role in MHC class II mediated immune systems, resulting in CD4+ T cell activation
-
-
?
additional information
?
-
-
this enzyme serves a crucial role in MHC class II mediated immune systems, resulting in CD4+ T cell activation
-
-
?
additional information
?
-
cathepsin S-dependent activation of PAR-2 activation
-
-
?
additional information
?
-
-
cathepsin S-dependent activation of PAR-2 activation
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
cathepsin S is implicated as a key enzyme in the processing of major histocompatability complex class II molecules
-
-
?
additional information
?
-
-
cathepsin S catalyzes a key step in antigen presentation, detailed overview
-
-
?
additional information
?
-
-
cathepsin S controls angiogenesis and tumor growth via matrix-derived angiogenic factors, the enzyme is required for neoplastic progression, overview
-
-
?
additional information
?
-
-
cathepsin S in professional antigen-presenting cells, APC, controls MHC class II-mediated antigen presentation by epithelial cells in vivo, and plays a critical role in invariant chain degradation
-
-
?
additional information
?
-
-
cathepsin S is responsible for murine autoimmune myasthenia gravis pathogenesis, overview
-
-
?
additional information
?
-
-
cathepsin S, a cysteine protease, plays an important role in generating peptides for the vacuolar, TAP-independent MHC class I cross-presentation in vivo
-
-
?
additional information
?
-
-
Cat S forms an alpha-beta-CLIP complex, unlike CatB or CatD, from an alpha-beta-Ii molecule in vitro
-
-
?
additional information
?
-
-
cathepsin S is a potent regulator of both cell and matrix turnover in advanced atherosclerosis
-
-
?
additional information
?
-
-
cathepsin S is an elastolytic enzyme
-
-
?
additional information
?
-
-
cathepsins are primarily involved in general protein turnover, CATS belongs to the cathepsins with a distinct substrate specificity
-
-
?
additional information
?
-
-
catS has proinflammatory effects
-
-
?
additional information
?
-
-
catS is a potent elastolytic protease and accelerates calcification in atherosclerotic mice with chronic renal disease induced by 5/6 nephrectemy
-
-
?
additional information
?
-
-
CatS is implicated in the regulation of intracellular cholesterol metabolism
-
-
?
additional information
?
-
-
CATS participates in inflammatory processes accompanying aging and pathologies of the central nervous system
-
-
?
additional information
?
-
-
it degrades the invariant chain Ii, which is crucial to the immune response since it acts as an essential step in MHC class II antigen presentation
-
-
?
additional information
?
-
-
cathepsin S substrate Leu-Arg and a poly(ethylene glycol) chain in dendritic arms
-
-
?
additional information
?
-
-
cathepsin S controls angiogenesis and tumor growth via matrix-derived angiogenic factors, the enzyme is required for neoplastic progression, overview
-
-
?
additional information
?
-
-
cathepsin S in professional antigen-presenting cells, APC, controls MHC class II-mediated antigen presentation by epithelial cells in vivo, and plays a critical role in invariant chain degradation
-
-
?
additional information
?
-
-
cathepsin S is responsible for murine autoimmune myasthenia gravis pathogenesis, overview
-
-
?
additional information
?
-
-
no activity with benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin and benzoyl-Gly-Gly-7-amido-4-methylcoumarin
-
-
?
additional information
?
-
-
proteolysis of prion protein by cathepsin S generates a soluble-structured intermediate oligomeric form, with potential implications for neurotoxic mechanisms
-
-
?
additional information
?
-
-
cathepsin S is implicated as a key enzyme in the processing of major histocompatability complex class II molecules
-
-
?
additional information
?
-
-
primary role of the enzyme in heterophagocytosis of proteins from the ultrafiltrate
-
-
?
additional information
?
-
-
cathepsin S is possibly involved in thyroid hormone biosynthesis
-
-
?
additional information
?
-
-
cathepsin S catalyzes a key step in antigen presentation, detailed overview
-
-
?
additional information
?
-
-
CATS is an important player in the spinal mechanisms involved in chronic pain induction and maintenance
-
-
?
additional information
?
-
-
CATS is widely expressed in the brain and is implicated in several neurological conditions such as Alzheimer's disease, amyotrophic lateral sclerosis and age-related inflammation, CATS is also implicated in neuropathic hyperalgesia and allodynia
-
-
?
additional information
?
-
-
key protease responsible for the removal of the invariant chain from MHC class II molecules, the enzyme plays a major role in antigen presentation
-
-
?
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(2R)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
(2R)-2-(2-cyclohexylethyl)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(2-cyclopentylethyl)-4-morpholin-4-yl-4-oxo-N-[(1S)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
(2R)-2-(2-cyclopentylethyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)butanamide
-
-
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)butyl]butanamide
-
-
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-phenyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]butanamide
-
-
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
(2R)-2-(cyclohexylmethyl)-N-[(1R)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(cyclohexylmethyl)-N-[(1R)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(cyclopentylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1S)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)butyl]butanamide
-
-
(2R)-2-(cyclopentylmethyl)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(cyclopentylmethyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)-2-phenylethanol
-
-
(2R)-2-benzyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-[4'-(1-azabicyclo[2.2.2]oct-4-yl)-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
-
IC50: 1991 nM
(2R)-2-[4'-(4-tert-butylpiperazin-1-yl)-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
-
IC50: 8340 nM
(2R)-2-[4'-[1-(2-amino-2-methylpropyl)piperidin-4-yl]-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
-
IC50: 1427 nM
(2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-N-(1-cyanocyclopropyl)-3-(methylsulfanyl)propanamide
-
-
(2R)-4-dimethyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-2-(2-morpholin-4-yl-2-oxoethyl)pentanamide
-
-
(2R)-4-morpholin-4-yl-4-oxo-2-(2-phenylethyl)-N-[(1S)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
(2R)-5-dimethyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-2-(2-morpholin-4-yl-2-oxoethyl)hexanamide
-
-
(2R)-N-(1-benzyl-4-cyanopiperidin-4-yl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-(1-cyanocyclopropyl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-(1-cyanocyclopropyl)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-(4-cyano-1-methylpiperidin-4-yl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-(cyanomethyl)-2-[4'-[4-(2-hydroxy-2-methylpropyl)-1-piperazinyl][1,1'-biphenyl]-3-yl]-4-methylpentanamide
-
IC50 above 0.01 mM
(2R)-N-(cyanomethyl)-2-[4'-[4-(2-hydroxyethyl)-1-piperazinyl][1,1'-biphenyl]-3-yl]-4-methylpentanamide
-
IC50: 609 nM
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)-[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 2010 nM
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1H-tetraazol-5-yl)-1,1'-biphenyl-3-yl]pentanamide
-
IC50 above 0.01 mM
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methyl-1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 3931 nM
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-pyrimidinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 1365 nM
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-[4-(2-oxopropyl)-piperazin-1-yl]-1,1'-biphenyl-3-yl]pentanamide
-
IC50: 2364 nM
(2R)-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(1R)-2-[(4-chlorobenzyl)oxy]-1-cyanoethyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-2-carboxamide
-
IC50: 658 nM
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
(2R)-N-[(1S)-1-cyano-3-phenylpropyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-2-(2-morpholin-4-yl-2-oxoethyl)-5-phenylpentanamide
-
-
(2R)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-(2-phenylethyl)butanamide
-
-
(2R)-N-[(3R)-1-benzyl-3-cyanopiperidin-4-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-(1-methylethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-(2-methylpropyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-(2-phenylethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-(cyclopropylmethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-(propan-2-yl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cycloheptylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cycloheptylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(2,3-dihydro-1H-inden-2-ylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(2,3-dihydro-1H-inden-2-ylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclopentylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(1-methylcyclohexyl)methyl]-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(1-methylcyclohexyl)methyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(4-methylcyclohexyl)methyl]-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(4-methylcyclohexyl)methyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-(morpholin-4-yl)-4-oxo-2-(1,2,3,4-tetrahydronaphthalen-2-ylmethyl)butanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-(morpholin-4-yl)-4-oxo-2-[(4-phenylcyclohexyl)methyl]butanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-morpholin-4-yl-4-oxo-2-(1,2,3,4-tetrahydronaphthalen-2-ylmethyl)butanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-morpholin-4-yl-4-oxo-2-[(4-phenylcyclohexyl)methyl]butanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclopentylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclopentylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-methylpiperidin-4-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-methylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-methylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3S)-1-benzyl-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3S)-3-cyano-1-(cyclohexylmethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-1-(4,4'-bipiperidin-1-yl)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
-
-
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxypropan-1-one
-
-
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(propan-2-ylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(propylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
(2S)-1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(1'-methyl-4,4'-bipiperidin-1-yl)propan-2-ol
-
-
(2S)-2-(4-chlorophenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-2-(4-fluorophenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-2-(4-methoxyphenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-2-(4-methylphenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-2-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-2-amino-N-[(1S)-2-(biphenyl-4-yl)-1-cyanoethyl]butanamide
-
-
(2S)-3-cyclohexyl-1-(morpholin-4-yl)-1-oxopropan-2-yl [(2S)-1-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)propan-2-yl]carbamate
-
-
(2S)-4-morpholin-4-yl-4-oxo-2-phenyl-N-[(1S)-1-phenyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]butanamide
-
-
(2S)-4-morpholin-4-yl-4-oxo-2-phenyl-N-[(1S)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
(2S)-4-morpholin-4-yl-4-oxo-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-2-carboxamide
-
-
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
(2S)-N-[(1S)-1-cyclopropyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-phenylbutanamide
-
-
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[2-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[3-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-[(2S)-3-methyl-1-[[4-(trifluoromethoxy)phenyl]amino]butan-2-yl]-4-(morpholin-4-yl)-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
(2Z)-3-(4-[[5-(3,5-dimethylisoxazol-4-yl)-1,2,4-oxadiazol-3-yl]methoxy]phenyl)-2-(methylsulfonyl)prop-2-enenitrile
-
-
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(furan-2-yl)methanone
-
-
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(pyridin-2-yl)methanone
-
-
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(tetrahydrofuran-2-yl)methanone
-
-
(3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]phenyl)acetic acid
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
(3R)-3-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(3R)-tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
-
IC50: 42 nM
(3S)-3-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(3S)-3-[(N-1,3-benzoxazol-2-yl-3-cyclohexyl-L-alanyl)amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoic acid
-
IC50: 12 nM
(3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoic acid
(3S)-N-[2-(1H-indol-3-yl)ethyl]-3-[[(4-methylphenyl)sulfonyl]amino]-2-oxo-4-phenylbutanamide
-
-
(3S)-tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
-
IC50: 49 nM
(4R)-1-acetyl-N-[(2R)-1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-1-acetyl-N-[(2S)-1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxo-3-phenylpropan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(ethylsulfonyl)-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfanyl)-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfinyl)-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-phenoxy-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[(2-chlorophenyl)sulfonyl]-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[(4-fluorophenyl)sulfonyl]-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[[4-(1H-pyrazol-1-yl)phenyl]sulfonyl]-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxopropan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-3-methyl-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(2-methylpropanoyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(2-oxopropyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(3-chlorobenzoyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(3-methoxypropanoyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(4-chlorobenzoyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(biphenyl-4-ylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(cyclohexylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(methylsulfinyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-benzoyl-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-phenyl-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyridin-3-ylcarbonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyridin-4-ylcarbonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyrrolidin-1-ylcarbonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(trifluoroacetyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-propanoyl-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[2-(1,3-benzoxazol-2-yl)-2-oxoethyl]-1-(cyclohexylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4S)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]hexanamide
-
IC50 above 0.01 mM
(S)-[1-[1-cyano-pyrrolidin-3(R)-ylcarbamoyl]-3-methyl-butyl]-carbamic acid benzyl ester
-
-
(S)-[1-[1-cyano-pyrrolidin-3(S)-ylcarbamoyl]-3-methyl-butyl]-carbamic acid benzyl ester
-
-
1,1-bis(cyanomethyl)-3-[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]urea
-
-
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[(4-[[(2,2,2-trifluoroethyl)sulfonyl]amino]benzoyl)amino]propanoyl]amino)-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([2-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-3-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-4-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(thiophen-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[methyl(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(methylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(phenylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-([4-[(ethylsulfonyl)amino]benzoyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-([[4-([[(dimethylamino)methyl]sulfonyl]amino)phenyl]carbonyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[(4-[[(2,4-dimethyl-1,3-thiazol-5-yl)sulfonyl]amino]benzoyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose ammoniate (1:1)
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[(4-[[(3-fluorophenyl)sulfonyl]amino]benzoyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[(4-[[(3-methoxyphenyl)sulfonyl]amino]benzoyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([2-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-fluoro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([4-[(ethylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2,4-dimethyl-1,3-thiazol-5-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([3-[(methylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([4-[(methylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([4-[(phenylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([4-[(pyridin-4-ylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-(methylsulfamoyl)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-([[4-(1-methylethyl)-1,3-thiazol-2-yl]sulfonyl]amino)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-sulfamoylphenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methyl-1H-imidazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methylethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2,2,2-trifluoroethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2-methylphenyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methylpyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(5-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[4-(methylsulfamoyl)benzoyl]amino]propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[4-methyl-N-(thiophen-3-ylcarbonyl)-L-leucyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[4-methyl-N-(thiophen-3-ylcarbonyl)-L-leucyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-([4-[(cyclohexylsulfonyl)amino]benzoyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-([4-[(cyclopropylsulfonyl)amino]benzoyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([4-[(benzylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([4-[(butylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([4-[(cyclopropylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-chloropyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(3-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(4-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(cyclohexylmethyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1-(1'-[(2S)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]-4,4'-bipiperidin-1-yl)ethanone
-
-
1-(1-[(2R)-3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 350 nM
1-(1-[(2S)-3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 190 nM
1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 10 nM
1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 50 nM
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 50 nM
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 140 nM
1-(1-[3-[3-(4-chloro-3-methylphenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 60 nM
1-(1-[3-[3-[3-[(2-hydroxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)pyrrolidin-2-one
-
-
1-(1-[3-[5-(methylsulfonyl)-3-[3-[(2-phenoxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)pyrrolidin-2-one
-
-
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 80 nM
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5,6-dichloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 110 nM
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methoxy-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 140 nM
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 90 nM
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 120 nM
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-7-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 210 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 130 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-(2,2,2-trifluoroethyl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 90 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-butyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 140 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 310 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 500 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-tert-butyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 100 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 100 nM
1-(1-[3-[5-acetyl-3-(4-chlorophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 460 nM
1-(1-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 120 nM
1-(1-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-fluoro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 230 nM
1-(2-[[5-[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl]ethyl)piperidin-4-ol
-
-
1-(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)-2-hydroxyethanone
-
-
1-(4-cyclopropylpiperazin-1-yl)-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
-
-
1-(4-methylpiperazin-1-yl)-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
-
-
1-(ethenylideneamino)-3-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 100 nM
1-bromo-3-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
1-bromo-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
1-cyano-(3,4-didehydro)-Pro-Leu methyl ester
-
-
1-cyano-(D)-Pro-(D)-Leu methyl ester
-
-
1-cyano-(D)-Pro-Ala methyl ester
-
-
1-cyano-(D)-Pro-Leu benzyl ester
-
-
1-cyano-(D)-Pro-Leu benzylamide
-
-
1-cyano-(D)-Pro-Leu dimethylamide
-
-
1-cyano-(D)-Pro-Leu methyl ester
-
-
1-cyano-(trans-benzyloxy)prolylleucine methyl ester
-
-
1-cyano-(trans-hydroxy)-Pro-Leu methyl ester
-
-
1-cyano-Pro isoamylamide
-
-
1-cyano-Pro-(D)-Leu methyl ester
-
-
1-cyano-Pro-Ala methyl ester
-
-
1-cyano-Pro-Leu benzyl ester
-
-
1-cyano-Pro-Leu methyl ester
-
-
1-cyano-Pro-Leu-Gly ethyl ester
-
-
1-cyano-Pro-Leu-Leu-Leu methyl ester
-
-
1-cyano-Pro-Phe methyl ester
-
-
1-formyl-(D)-Pro-Leu benzyl ester
-
-
1-iminomethyl-(D)-Pro-Leu benzyl ester
-
-
1-methyl-6-[4-(piperidin-4-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-(piperidin-4-yloxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-(pyridin-2-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-(pyridin-3-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-(pyridin-4-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[(3-oxopiperazin-1-yl)oxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[2-(2-oxopyrrolidin-1-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[2-(6-methylpyridin-2-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[2-(piperidin-4-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[3-(pyrrolidin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-([[1-(4-fluorophenyl)-1-methylethoxy]sulfinyl]methyl)-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
-
-
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(2-methylpropoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
-
-
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(4-fluorophenoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
-
-
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
1-[(3R)-4-(methylsulfonyl)-2-oxo-3-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]butyl]cyclopropanecarbonitrile
-
-
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
-
-
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)methyl]-4-fluorobenzene
-
-
1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 50 nM
1-[1-(3-[3-[3-([2-[benzyl(methyl)amino]ethyl]sulfanyl)-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(2-methylpyrrolidin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(3-hydroxypyrrolidin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-hydroxypiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-methylpiperazin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-methylpiperazin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-methylpiperidin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-methylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-tert-butylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(benzylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(dimethylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(methylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[3-hydroxy-2-oxo-3-(piperidin-4-yl)propyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(4-phenylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(octahydroisoquinolin-2(1H)-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(pyrrolidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-oxo-2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-oxo-2-(pyrrolidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 50 nM
1-[1-(3-[5-acetyl-3-[4-(trifluoromethoxy)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 130 nM
1-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 100 nM
1-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 110 nM
1-[1-[(2R)-3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl]-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 180 nM
1-[1-[(2S)-3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl]-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 200 nM
1-[2-(dimethylamino)ethyl]-6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-[3-(dimethylamino)propyl]-6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-[3-[3-[(2-aminoethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidine-4-carboxamide
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-(methylsulfanyl)ethanone
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxyethanone
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-methoxyethanone
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]ethanone
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]propan-1-one
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-methyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[3-[4-(2-cyanophenyl)piperazin-1-yl]-2-hydroxypropyl]-3-(4-iodophenyl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide
-
IC50: 50 nM
1-[3-[4-(5-methyl-1H-indol-3-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(morpholin-4-yl)propan-2-ol
-
-
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperazin-1-yl)propan-2-ol
-
-
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[4-(2-[[5-[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl]ethyl)piperazin-1-yl]ethanone
-
-
1-[4-(dimethylamino)piperidin-1-yl]-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
-
-
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(3,4-dichlorobenzyl)methanamine
-
-
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(4-methoxybenzyl)methanamine
-
-
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(4-methylbenzyl)methanamine
-
-
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-methylmethanamine
-
-
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(morpholin-4-yl)propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(propylamino)propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(pyrrolidin-1-yl)propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-[4-(pyridin-2-yl)piperidin-1-yl]propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-[4-(pyrrolidin-1-yl)piperidin-1-yl]propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(pyrrolidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
2,2'-[[3-(trifluoromethyl)phenyl]imino]bis[N-(4-methylphenyl)acetamide]
-
-
2,3,4,5,6-pentafluoro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 0.020 mM
2-(1,1'-biphenyl-3-yl)-N-(cyanomethyl)-4-methylpentanamide
-
IC50: 1578 nM
2-(1,1'-biphenyl-4-yl)-N-(cyanomethyl)-4-methylpentanamide
-
IC50: 3343 nM
2-(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)-2-oxoethyl acetate
-
-
2-(4-tert-butylphenyl)-5-[[2-(3,4-dimethoxyphenyl)ethyl]amino]-1,3-oxazole-4-carbonitrile
-
-
2-(4-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperazin-1-yl)benzonitrile
-
IC50: 120 nM
2-([5-[1-[2-hydroxy-3-[(3S)-3-methylmorpholin-4-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(3-methyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(piperidin-1-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(pyrrolidin-1-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-[(3R)-3-hydroxypyrrolidin-1-yl]ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-[(3S)-3-hydroxypyrrolidin-1-yl]ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyrrolidin-1-ylcarbonyl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([5-[1-[3-[4-(2-fluorophenyl)piperazin-1-yl]-2-hydroxypropyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)-1,3-thiazolidine
-
-
2-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)-2,3-dihydro-1,3-benzothiazole
-
-
2-amino-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]ethanone
-
-
2-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 35 nM
2-cyano-4-(2-hydroxyethoxy)-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide
2-cyano-4-[(1,4-dioxaspiro[4.5]dec-8-ylmethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-4-[(2-cyclopentylethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-4-[(6,8-dioxaspiro[3.5]non-7-ylmethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-4-[(cyclohexylmethyl)(methyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
2-cyano-4-[[(4,4-difluorocyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[[(4,4-dimethylcyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[[1-(2-hydroxyethyl)piperidin-4-yl]methoxy]-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-N-(1-methyl-4-phenylpiperidin-4-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
2-cyano-N-(4,5-dimethoxybiphenyl-2-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-methyl-4-(piperidin-4-ylmethoxy)-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-N-methyl-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-N-methyl-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[4.5]dec-8-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-N-methyl-4-[(spiro[3.5]non-7-ylmethyl)amino]-6-[(2,2,6,6-tetramethylpiperidin-4-yl)oxy]pyrimidine-5-carboxamide
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
2-cyano-N-methyl-4-[[1-(1-methylethyl)piperidin-4-yl]methoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-N-[(1-methyl-4-phenylpiperidin-4-yl)methyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-[(1R)-2-pyridin-2-yl-1-(pyrrolidin-1-ylmethyl)ethyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-[5-[(1-methylpiperidin-4-yl)oxy]biphenyl-2-yl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-hydroxy-1-(1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)ethanone
-
-
2-hydroxy-1-(1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)ethanone
-
-
2-hydroxy-N'-[1H-indol-3-yl(oxo)acetyl]-2,2-diphenylacetohydrazide
-
-
2-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)sulfanyl]ethanol
-
-
2-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-1,3-difluorobenzene
-
-
2-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]biphenyl
-
-
2-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]benzonitrile
-
-
2-[3-(4-chloro-3-[4-[(4-chloro-benzylamino)-methyl]-phenylethynyl]-phenyl)-1-[3-(3-methyl-morpholin-4-yl)-propyl]-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-oxo-acetamide
-
-
2-[3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
-
-
2-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-oxoacetamide
-
-
2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9-(2-hydroxyethyl)-9H-purine-6-carbonitrile
-
-
2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9-ethyl-9H-purine-6-carbonitrile
-
-
2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
-
-
2-[4-methoxy-3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
-
-
2-[5-carbamoyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-1-[[4-(2-cyanophenyl)piperazin-1-yl]methyl]ethyl carbamate
-
IC50: 20 nM
2-[N-(3-chlorophenyl)-L-leucyl]tetrahydropyridazine-1(2H)-carbonitrile
-
-
2-[N-(4-cyanophenyl)-L-leucyl]pyrazolidine-1-carbonitrile
-
-
2-[N-(4-cyanophenyl)-L-phenylalanyl]pyrazolidine-1-carbonitrile
-
-
2-[N-(4-fluorophenyl)-L-valyl]tetrahydropyridazine-1(2H)-carbonitrile
-
-
2-[N-[3-(trifluoromethyl)phenyl]-L-isoleucyl]tetrahydropyridazine-1(2H)-carbonitrile
-
-
2-[[5-(1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(morpholin-4-yl)ethanone
-
-
2-[[5-(1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
-
-
2-[[5-(1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(morpholin-4-yl)ethanone
-
-
2-[[5-(1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
-
-
2-[[5-(5-acetyl-1-[2-hydroxy-3-[4-(2-hydroxypropan-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
-
-
2-[[5-(5-acetyl-1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(morpholin-4-yl)ethanone
-
-
2-[[5-(5-ethyl-1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
-
-
2-[[5-[5-acetyl-1-[2-hydroxy-3-(4-methylpiperidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
-
-
2-{[3-(4-chloro-5-hydroxy-2-methoxyphenyl)-4-oxo-3,4-dihydroquinazolin-2-yl]sulfanyl}-N-[(1S)-1-cyano-1,2-dimethylpropyl]acetamide
-
-
3'-[1-[[(cyanomethy)amino]carbonyl]-3-methylbutyl]-1,1'biphenyl-4-carboxamide
-
IC50: 1373 nM
3-(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)prop-2-yn-1-ol
-
-
3-(4-chloro-3-ethynylphenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-(4-chloro-3-[[2-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-(4-chloro-3-[[3-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-(4-chloro-3-[[4-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 33 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-(naphthalen-2-ylacetyl)-L-alaninamide
-
IC50: 5.0 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-([5-[3-(trifluoromethyl)phenyl]furan-2-yl]acetyl)-L-alaninamide
-
IC50: 3.3 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(3-phenoxyphenyl)acetyl]-L-alaninamide
-
IC50: 8.0 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(4-morpholin-4-ylphenyl)acetyl]-L-alaninamide
-
IC50: 4.0 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(4-phenoxyphenyl)acetyl]-L-alaninamide
-
IC50: 17 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(5-methyl-1-phenyl-1H-pyrazol-4-yl)acetyl]-L-alaninamide
-
IC50: 34 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[[4-(1H-1,2,4-triazol-1-yl)phenyl]acetyl]-L-alaninamide
-
IC50: 26 nM
3-cyclohexyl-N2-(5-fluoro-1,3-benzoxazol-2-yl)-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
-
IC50: 197 nM
3-cyclohexyl-N2-(6-fluoro-1,3-benzoxazol-2-yl)-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
-
IC50: 43 nM
3-cyclohexyl-N2-([4-[(4,6-dimethylpyrimidin-2-yl)amino]phenyl]acetyl)-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 2.0 nM
3-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,5-dimethyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 30 nM
3-[3-(benzylsulfanyl)-4-chlorophenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide
-
-
3-[4-chloro-3-(4-methylpent-1-yn-1-yl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(cyclohexylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(hept-1-yn-1-yl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(phenylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(propylsulfanyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(thiophen-2-ylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(thiophen-3-ylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(2-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(2-methoxyphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(2-methylphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(2-phenoxyethyl)sulfanyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(2-phenylethyl)sulfanyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(3,4-dichlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(3-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
3-[4-chloro-3-[(4-methoxyphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(4-methylphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[[(2S)-2-[([3-acetyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
3-[[(2S)-2-[[(4-[[(4-aminophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]benzamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
4-(3-acetylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-bromophenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-chlorophenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-cyclobutylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-cyclopentylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-cyclopropylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-ethylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-methylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-tert-butylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(acetylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 123 nM
4-(dimethylamino)-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
-
-
4-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 16 nM
4-fluoro-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
-
-
4-hydroxy-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
-
-
4-methyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-N2-(morpholin-4-ylcarbonyl)-L-leucinamide
-
-
4-methyl-N2-(morpholin-4-ylcarbonyl)-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)-L-leucinamide
-
-
4-morpholinecarbonyl-Phe-(S-benzyl)Cys-PSI(CHO)
-
4-morpholinecarboxamide, N-[(1R)-2-[[(1S)-1-(2-benzoxazolylcarbonyl) propyl] amino]-1-[[(cyclopropylmethyl)-sulfonyl]methyl]-2-oxoethyl]
-
previously reported as 05141, ihbitor-dosed mice are protected against ozone-induced airway hyperresponsiveness
4-phenyl-6-propylpyrimidine-2-carbonitrile
-
-
4-propyl-6-(3-propylphenyl)pyrimidine-2-carbonitrile
-
-
4-propyl-6-[2-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-propyl-6-[3-(trifluoromethoxy)phenyl]pyrimidine-2-carbonitrile
-
-
4-propyl-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-propyl-6-[4-(trifluoromethoxy)-3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-propyl-6-[4-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-[(1-acetylpiperidin-4-yl)methoxy]-2-cyano-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]aniline
-
-
4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzoic acid
-
-
4-[(4-[(E)-[(cyanoacetyl)hydrazono]methyl]phenoxy)methyl]benzoic acid
-
-
4-[1-(2-hydroxy-3-[3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(3-[3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(3-[5-tert-butoxy-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(3-[5-tert-butoxy-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
-
4-[2-chloro-5-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[3,5-bis(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[3-(2-methylpropyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[3-(methylsulfonyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[3-(propan-2-yl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-[4-(propan-2-yloxy)-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[4-chloro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[4-ethoxy-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[4-fluoro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[4-methoxy-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[4-methyl-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]benzamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]benzoic acid
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-3-[3-[(2-phenoxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-(methylsulfonyl)-1-[3-[4-(1H-pyrrolo[3,2-c]pyridin-3-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-(piperidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-(pyrrolidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-[4-(pyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-bromo-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
-
5-chloro-3-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 150 nM
5-chloro-3-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 80 nM
6-(4-chlorobenzyl)-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-(2-cyclooctylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-(2-piperidine-1-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(3,3-dimethylbutyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-(4,4-dimethylpentyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-[2-(3-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-chloro-1-(1-[3-[3-(4-chloro-3-methylphenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 50 nM
6-chloro-1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 60 nM
6-chloro-1-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 30 nM
6-[3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
-
-
6-[4-(2-hydroxyethoxy)-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-(2-hydroxyethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
-
-
6-[4-(3-oxopropyl)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-(ethylamino)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-[2-(morpholin-4-yl)ethyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-[3-(morpholin-4-yl)propyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-ethoxy-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
-
-
6-[4-methoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-phenoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-[2-(2-oxopyrrolidin-1-yl)ethoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
-
-
6-[4-[2-(dimethylamino)ethoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-[3-(2-ethyl-1H-imidazol-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
-
-
6-[4-[3-(4-ethylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
-
-
6-[4-[3-(dimethylamino)propoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[[4-(1-acetyl-1,2,3,6-tetrahydropyridine-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
6-[[4-(1-acetylpiperidin-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(1-acetylpiperidine-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
6-[[4-(4-acetyl-1,4-diazepan-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-[[4-(4-acetylpiperazin-1-yl)-3-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazine-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-(4-methoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2-cyclohexylethyl)-6-(naphthalen-1-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2-cyclohexylethyl)-6-[(pyridine-2-yloxy)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[(pyridine-2-ylsulfanyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[[methyl(phenyl)amino]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-tert-butyl-6-(4-chlorobenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
9-[3-(dimethylamino)propyl]-2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
-
-
APC-2848
-
irreversible vinyl-sulfone inhibitor
benzoyl-Phe-Phe-CHN2
-
0.006 mM, 39% inhibition
benzyl [(2S)-1-(2-cyanotetrahydropyridazin-1(2H)-yl)-3-methyl-1-oxopentan-2-yl]carbamate
-
-
benzyloxycarbonyl Phe-Ala-CH2F
-
very potent time-dependent inhibitor, inhibits proteinase 30times more efficiently than it does cathepsin L and about 300times better than it does cathepsin B
benzyloxycarbonyl-((CH3)3C-CH(NH2)-COOH)-Tyr-CHN2
-
t1/2 at 0.1 mM is 1.6 min
benzyloxycarbonyl-((CH3)3C-CH2-CH(NH2)-COOH)-Leu-Tyr-CHN2
-
t1/2 at 0.0004 mM is 3.85 min
benzyloxycarbonyl-Ala-Leu-COCHO
-
-
benzyloxycarbonyl-Ile-Met-CHN2
-
t1/2 at 0.001 mM is 5.4 min
benzyloxycarbonyl-Ile-Trp-CHN2
-
t1/2 at 0.004 mM is 3.45 min
benzyloxycarbonyl-Leu-Ala-CHN2
-
t1/2 at 0.0001 mM is 5.5 min
benzyloxycarbonyl-Leu-Leu-CHN2
-
t1/2 at 0.00002 mM is 8.6 min
benzyloxycarbonyl-Leu-Leu-Nle-CHN2
-
t1/2 at 0.000001 mM is 1.25 min
benzyloxycarbonyl-Leu-Leu-Tyr-CHN2
-
t1/2 at 0.000001 mM is 5.5 min
benzyloxycarbonyl-Leu-Nle-CHN2
-
t1/2 at 0.00001 mM is 3.4 min
benzyloxycarbonyl-Leu-Nva-CHN2
-
t1/2 at 0.00001 mM is 4.5 min
benzyloxycarbonyl-Leu-Thr(tert-butyl)-CHN2
-
t1/2 at 0.001 mM is 3.5 min
benzyloxycarbonyl-Leu-Trp-CHN2
-
t1/2 at 0.0002 mM is 2.6 min
benzyloxycarbonyl-Phe-Ala-CH2F
-
-
Benzyloxycarbonyl-Phe-Ala-CHN2
-
-
benzyloxycarbonyl-Phe-Ala-COCHO
-
-
Benzyloxycarbonyl-Phe-Arg
-
-
benzyloxycarbonyl-Phe-Arg-COCHO
-
-
benzyloxycarbonyl-Phe-Leu-COCHO
-
potent, reversible cathepsin S inhibitor, the inhibitor is 400fold more selective for cathepsin S than for cathepsin B
benzyloxycarbonyl-Phe-Lys(benzyloxycarbonyl)-CH3
-
inhibition in the micromolar range, competitive
Benzyloxycarbonyl-Phe-Phe-CHN2
benzyloxycarbonyl-Phe-Tyr(OBut)-COCHO
-
-
benzyloxycarbonyl-Phe-Tyr(tert-butyl)CHN2
-
t1/2 at 0.02 mM is 19.25 min, about 10000times more effective against cathepsin L than against cathepsin S
benzyloxycarbonyl-Trp-Met-CHN2
-
t1/2 at 0.00001 mM is 3.0 min
benzyloxycarbonyl-Tyr-Ala-CHN2
-
0.001 mM, 88% inhibition
benzyloxycarbonyl-Tyr-Tyr(O-butyl)-CHN2
-
1 mM, 78% inhibition
benzyloxycarbonyl-Val-Met-CHN2
-
t1/2 at 0.0001 mM is 3.5 min
benzyloxycarbonyl-Val-Nle-CHN2
-
t1/2 at 0.00003 mM is 5.8 min
benzyloxycarbonyl-Val-Trp-Nle-CHN2
-
t1/2 at 0.00001 mM is 5.7 min
benzyloxycarbonyl-Val-Val-CHN2
-
t1/2 at 0.0001 mM is 47.0 min
benzyloxycarbonyl-Val-Val-Lys-NHO-4-nitrobenzoyl
-
-
benzyloxycarbonyl-Val-Val-Nle-CHN2
-
t1/2 at 0.000001 is 2.5 min, 300times more effective in inactivating cathepsin S than cathepsin L
benzyloxycarbonyl-Val-Val-Phe-CH3
-
inhibition in the micromolar range, competitive
benzyloxycarbonyl-Val-Val-Tyr-CHN2
-
t1/2 at 0.000005 mM is 6.75 min
BMV083
a near-infrared quenched activity-based probe (qABP) that selectively targets cathepsin S in immune cells
BMV109
a pan-reactive cysteine cathepsin qABP
BMV117
a near-infrared quenched activity-based probe (qABP) that selectively targets cathepsin S in immune cells
BMV157
a near-infrared quenched activity-based probe (qABP) that targets cathepsin S in immune cells
butyloxycarbonyl-Lys-Leu-Tyr-CHN2
-
t1/2 at 0.0001 mM is 2.9 min
carbobishydrazide
-
irreversible cathepsin S inhibitor
cathepsin K propeptide
-
-
-
cathepsin L propeptide
-
-
-
cathepsin S propeptide
-
0.0002 mM, blocks gelatinase, collagenase and elastinase activities of mature cathepsin S
-
chimeric propeptide of cathepsin S and cathepsin L S1-54/L44-86
-
-
-
CLIK-066
-
0.01 mM, 28% inhibition
CLIK-088
-
0.01 mM, 64% inhibition
CLIK-112
-
0.01 mM, 77% inhibition
CLIK-121
-
0.01 mM, complete inhibition
CLIK-148
-
0.01 mM, complete inhibition
CLIK-181
-
0.01 mM, 80% inhibition
CLIK-195
-
0.01 mM, complete inhibition
CLIK60
-
selective CatS inhibitor, CatS inhibition increases macrophage cholesterol accumulation and efflux
cystatin A
-
inhibition in the subnanomolar range
-
cystatin B
-
inhibition in the subnanomolar range
-
dipeptide-vinyl sulfone LHVS
-
irreversible cathepsin S inhibitor
EM053
a pan-reactive cysteine cathepsin qABP
Ep-475
-
0.01 mM, complete inhibition
epoxysuccinyl-Ala benzyl ester
-
-
epoxysuccinyl-Arg benzyl ester
-
-
epoxysuccinyl-D-Phe benzyl amide
-
-
epoxysuccinyl-D-Phe benzyl ester
-
-
epoxysuccinyl-Ile benzyl ester
-
-
epoxysuccinyl-Leu benzyl amide
-
-
epoxysuccinyl-Leu benzyl ester
-
-
epoxysuccinyl-Phe benzyl amide
-
-
epoxysuccinyl-Phe benzyl ester
-
-
epoxysuccinyl-Val benzyl ester
-
-
ethyl (3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoate
-
IC50: 71 nM
iodoacetic acid
-
1 mM, 92% inhibition
LO143
a near-infrared quenched activity-based probe (qABP) that targets cathepsin S in immune cells
LO219
a near-infrared quenched activity-based probe (qABP) that targets cathepsin S in immune cells
methyl (2R)-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)(phenyl)ethanoate
-
-
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-4-[(1S)-1-[(1R)-2-[(1-cyanocyclopropyl)amino]-1-(methoxysulfinyl)methyl]-2-oxoethyl]amino)-2,2,2-trifluoroethyl]-4'-fluorobiphenyl
-
-
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfenate
-
-
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfinate
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(3-fluorophenyl)ethyl]amino]propane-1-sulfinate
-
-
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfenate
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfinate
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propane-1-sulfinate
-
-
methyl (2S)-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)(phenyl)ethanoate
-
-
methyl (2Z)-4-[4-(dimethylamino)phenyl]-4-oxo-2-[(phenylcarbonyl)hydrazono]butanoate
-
-
methyl (3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(oxo)acetate
-
-
methyl (3R)-3-[[(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanoyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate
-
-
methyl (3S)-3-[[(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanoyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate
-
-
methyl (3S)-3-[[3-cyclohexyl-N-(morpholin-4-ylcarbonyl)-L-alanyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate
-
-
methyl 1-[2-hydroxy-3-(4-quinolin-4-ylpiperazin-1-yl)propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(2-oxo-2,3-dihydro-4,1-benzoxazepin-1(5H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidine-4-carboxylate
-
-
methyl 1-[3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(5-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(6-chloro-2,2-dioxido-3,4-dihydro-1H-2,1,3-benzothiadiazin-1-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 2-amino-4-([(1S)-2-(1-[(benzyloxy)methyl]-3-[(2-ethoxy-2-oxoethyl)amino]-2,3-dioxopropylamino)-1-(cyclohexylmethyl)-2-oxoethyl]aminocarbonyl)benzoate
-
-
methyl 2-[[(1S)-1-(cyclohexylmethyl)-2-([2-[(4-fluorophenyl)amino]ethyl]amino)-2-oxoethyl]amino]-1,3-benzoxazole-6-carboxylate
-
IC50: 43 nM
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(3,4-dihydroisoquinolin-2(1H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(5-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2,2-dioxido-3,4-dihydro-1H-2,1,3-benzothiadiazin-1-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 4'-[(1S)-1-([(1S)-1-[(1-cyanocyclopropyl)carbamoyl]pentyl]amino)-2,2,2-trifluoroethyl]biphenyl-4-sulfinate
-
-
methyl 4-([(1S)-2-((1S)-1-[(benzyloxy)methyl]-3-[(2-ethoxy-2-oxoethyl)amino]-2,3-dioxopropyl amino)-1-(cyclohexylmethyl)-2-oxoethyl]aminocarbonyl)-2-[(tert-butoxycarbonyl)amino]benzoate
-
-
methyl 4-[(E)-[[(3-[2-[(2-chlorobenzyl)oxy]phenyl]-1H-pyrazol-5-yl)carbonyl]hydrazono]methyl]benzoate
-
-
morpholine-4-carboxylic acid [1-[1S-(N-benzoyl-hydrazinomethyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
IC50: 565 mM
morpholine-4-carboxylic acid [1R-(1S-cyano-3-phenyl-propylcarbamoyl)-1,3-dimethyl-butyl]-amide
-
-
morpholine-4-carboxylic acid [1R-(1S-cyano-3-phenyl-propylcarbamoyl)-3-methylbutyl]amide
-
IC50: 0.011 mM
morpholine-4-carboxylic acid [1S-(1R-cyano-3-phenylpropylcarbamoyl)-3-methylbutyl]amide
-
IC50: 387 nM
morpholine-4-carboxylic acid [1S-(1S-cyano-2,2-dimethylpropylcarbamoyl)-3-methylbutyl]amide
-
IC50: 0.107 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-2-methyl-propylcarbamoyl)-3-methylbutyl]amide
-
IC50: 1400 nM
morpholine-4-carboxylic acid [1S-(1S-cyano-2-phenylethylcarbamoyl)-3-methylbutyl]amide
-
IC50: 130 nM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenyl-propylcarbamoyl)-1,3-dimethyl-butyl]-amide
-
IC50: 0.076 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-cyclohexyl-ethyl]-amide
-
IC50: 5 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-methyl-propyl]-amide
-
IC50: 0.006 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-phenyl-ethyl]-amide
-
IC50: 173 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-3,3-dimethyl-butyl]-amide
-
IC50: 23 nM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-cyclohexyl-R-methyl]-amide
-
IC50: 84 nM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-ethyl]-amide
-
IC50: 0.134 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-pentyl]-amide
-
IC50: 41 nM
morpholine-4-carboxylic acid [1S-(1S-cyanobutylcarbamoyl)-3-methylbutyl]amide
-
IC50: 82 nM
morpholine-4-carboxylic acid [1S-(1S-cyanobutylcarbamoyl)-3-methylpentyl]amide
-
IC50: 56 nM
morpholine-4-carboxylic acid [1S-(1S-cyanomethylcarbamoyl)-3-methylbutyl]amide
-
IC50: 142 nM
morpholine-4-carboxylic acid [1S-(2-benzyloxy-1R-cyano-ethylcarbamoyl)-3-methylbutyl]amide
-
IC50: 19 nM
morpholine-4-carboxylic acid [1S-(cyanomethylcarbamoyl)-3-methylbutyl]amide
-
IC50: 124 nM
morpholine-4-carboxylic acid [1S-[(1-cyano-1-methyl)ethylcarbamoyl]-3-methylbutyl]amide
-
IC50: 114 nM
morpholine-4-carboxylic acid [1S-[(cyano-phenyl-S-methyl)carbamoyl]-3-methylbutyl]amide
-
IC50: 51 nM
morpholine-4-carboxylic acid [1S-[1S-(benzoyl-hydrazonomethyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
IC50: 11 nM
morpholine-4-carboxylic acid [1S-[1S-cyano-2-(3,4-dichlorophenyl)ethylcarbamoyl]-3-methylbutyl]amide
-
IC50: 56 nM
morpholine-4-carboxylic acid [1S-[1S-[(2-hydroxy-benzoyl)-hydrazonomethyl]-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
IC50: 7 nM
morpholine-4-carboxylic acid [1S-[1S-[(4-hydroxybenzoyl)-hydrazonomethyl]-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
IC50: 35 nM
morpholine-4-carboxylic acid [1S-[2-(2-chlorobenzyloxy)-1R-cyanoethylcarbamoyl]-3-methylbutyl]amide
-
9 nM
morpholine-4-carboxylic acid [1S-[2-(3-chlorobenzyloxy)-1R-cyanoethylcarbamoyl]-3-methylbutyl]amide
-
9 nM
morpholine-4-carboxylic acid [1S-[2-(4-chlorobenzyloxy)-1R-cyanoethylcarbamoyl]-3-methylbutyl]amide
-
27 nM
morpholine-4-carboxylic acid [3-methyl-1S-(1-prop-2-ynylcarbamoyl)butyl]amide
-
IC50: 0.097 m
morpholine-4-carboxylic acid [3-methyl-1S-(1R-methyl-3-phenylpropylcarbamoyl)butyl]amide
-
IC50 above 0.339 mM
morpholine-4-carboxylic acid [3-methyl-1S-(3-phenyl-propylcarbamoyl)butyl]amide
-
IC50 above 0.028 mM
morpholineurea-leucyl-homophenylalanine-vinylsulfone phenyl
-
LHVS, CatS-specific inhibitor at a concentration of 10 nM, other cathepsins are not inhibited
morpholinurea-leucine-homophenylalanine-vinyl sulfone-phenyl
-
irreversible inhibitor
morpholinurea-leucinehomophenylalanine-vinyl phenyl sulfone
-
irreversible CatS inhibitor
N,N-dimethyl-2-([5-[5-(methylsulfonyl)-1-[3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)acetamide
-
-
N-(1-cyanocyclopropyl)-3-(methylsulfinyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-(4'-fluorobiphenyl-4-yl)ethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-phenylethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-[(3,4-dichlorophenyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-[(4-fluorobenzyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-phenylethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-[(4-fluorophenyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-[[2-(4-fluorophenyl)propan-2-yl]sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(4-benzyl-1-methylpiperidin-4-yl)-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-(4-chlorobenzyl)-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
-
-
N-(4-cyano-1-phenyl-1H-pyrazol-5-yl)-2-[(4-ethyl-5-thiophen-2-yl-4H-1,2,4-triazol-3-yl)sulfanyl]acetamide
-
-
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetamide
-
-
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]phenyl)acetamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]phenyl)propanamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
N-(cyanomethyl)-2-[3-(1H-indol-5-yl)phenyl]-4-methylpentanamide
-
IC50: 922 nM
N-(cyanomethyl)-2-[3-(1H-indol-6-yl)phenyl]-4-methylpentanamide
-
IC50: 1257 nM
N-(cyanomethyl)-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]-3-phenylpropanamide
-
IC50 above 0.01 mM
N-(cyanomethyl)-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]acetamide
-
IC50 above 0.01 mM
N-(cyanomethyl)-3-cyclobutyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]propanamide
-
IC50: 2310 nM
N-(cyanomethyl)-3-cyclopropyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]propanamide
-
IC50: 6597 nM
N-(cyanomethyl)-4-methyl-2-(2-phenyl-1,3-thiazol-4-yl)pentanamide
-
IC50 above 0.01 mM
N-(cyanomethyl)-4-methyl-2-(3'-piperazin-1-yl-1,1'-biphenyl-3-yl)pentanamide methanesulfonate
-
IC50 above 0.01 mM
N-(cyanomethyl)-4-methyl-2-(3-pyridin-3-ylphenyl)-pentanamide
-
IC50 above 0.01 nM
N-(cyanomethyl)-4-methyl-2-(3-pyridin-4-ylphenyl)-pentanamide trifluoroacetate
-
IC50: 1748 nM
N-(cyanomethyl)-4-methyl-2-(3-pyrimidin-5-ylphenyl)pentanamide
-
IC50 above 0.01 mM
N-(cyanomethyl)-4-methyl-2-(5-phenylpyridin-3-yl)-pentanamide trifluoroacetate
-
IC50 above 0.01 mM
N-(cyanomethyl)-4-methyl-2-[2'-(1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 521 nM
N-(cyanomethyl)-4-methyl-2-[2'-(4-morpholinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 3368 nM
N-(cyanomethyl)-4-methyl-2-[3'-(4-morpholinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50 above 0.01 mM
N-(cyanomethyl)-4-methyl-2-[4'-(1,2,3,6-tetrahydro-4-pyridinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 652 nM
N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 1245 nM
N-(cyanomethyl)-4-methyl-2-[4'-(4-methyl-1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 1695 nM
N-(cyanomethyl)-4-methyl-2-[4'-(4-morpholinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 9422 nM
N-(cyanomethyl)-4-methyl-2-[4'-(4-piperidinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 1421 nM
N-(cyanomethyl)-4-methyl-2-[4'-(methylsulfonyl)-1,1'-biphenyl-3-yl]pentanamide
-
IC50: 6623 nM
N-(trans-epoxysuccinyl)-L-leucine 4-guanidinobutylamide
-
N-benzyl-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-methylmethanamine
-
-
N-benzyl-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
-
-
N-benzyl-2-([5-[5-(methylsulfonyl)-1-[3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)acetamide
-
-
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)oxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-benzyl-2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-methyl-2-([5-[5-(methylsulfonyl)-1-[3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)acetamide
-
-
N-morpholinurea-leucine-homophenylalanine-vinylsulfone-phenyl
N-morpholinurea-leucyl-homophenylalanyl-vinylsulfone-phenyl
N-morpholinurealeucine-homophenylalanine-vinylsulfone-phenyl
-
-
N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-norvalinamide
-
-
N-[(1R)-1-([2-[(1,3-benzoxazol-2-ylsulfanyl)acetyl]hydrazino]carbonyl)propyl]-2-[(phenylcarbonyl)amino]benzamide
-
-
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylpropyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-[(1S)-1-(1H-indol-2-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
-
IC50: 29 nM
N-[(1S)-1-(biphenyl-4-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
-
IC50: 34 nM
N-[(1S)-1-(cyclohexylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
-
IC50: 62 nM
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-1-benzofuran-2-carboxamide
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-(3-fluorophenyl)furan-2-carboxamide
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-[3-(trifluoromethyl)phenyl]furan-2-carboxamide
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-2-carboxamide
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-3-carboxamide
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]morpholine-4-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-3-carboxamide
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[[(1S)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]amino]ethyl]morpholine-4-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydro-2H-pyran-4-carboxamide
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-3-carboxamide
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-2-(5-fluoro-2,2-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-2-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
-
-
N-[(1S)-1-(cyclopentylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
-
-
N-[(1S)-1-(furan-2-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
-
IC50: 0.020 mM
N-[(1S)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-[(1S)-1-cyclohexyl-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
-
IC50: 23 nM
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1,2-dimethylpropyl]benzamide
-
-
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1,2-dimethylpropyl]thiophene-3-carboxamide
-
-
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-(4-methylcyclohexyl)ethyl]thiophene-3-carboxamide
-
-
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-(trans-4-methylcyclohexyl)ethyl]thiophene-3-carboxamide
-
-
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-cyclohexylethyl]benzamide
-
-
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-cyclohexylethyl]thiophene-3-carboxamide
-
-
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-1-(naphthalen-2-ylmethyl)-2-oxoethyl]-3-methylbenzamide
-
IC50: 16 nM
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(1,3-thiazol-5-ylmethyl)ethyl]-3-methylbenzamide
-
IC50: 0.065 mM
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(pyridin-3-ylmethyl)ethyl]-3-methylbenzamide
-
IC50: 3707 nM
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(pyridin-4-ylmethyl)ethyl]-3-methylbenzamide
-
IC50: 6769 nM
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-phenylethyl]-3-methylbenzamide
-
IC50: 285 nM
N-[(1S)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxo-1-[(2-phenylethyl)sulfanyl]ethyl]morpholine-4-carboxamide
-
-
N-[(1S)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxo-1-[(2-phenylethyl)sulfonyl]ethyl]morpholine-4-carboxamide
-
-
N-[(1S)-3-cyclohexyl-1-([2-[(4-methoxyphenyl)amino]ethyl]carbamoyl)propyl]-3-methylbenzamide
-
IC50: 38 nM
N-[(1S)-3-methyl-1-(((4S)-3-oxo-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl)carbamoyl)butyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
-
-
N-[(2S)-1-([4-cyano-1-[3-(morpholin-4-yl)propyl]piperidin-4-yl]amino)-5,5-dimethyl-1-oxoheptan-2-yl]morpholine-4-carboxamide
-
-
N-[(2S)-1-[[(1R)-2-(benzyloxy)-1-cyanoethyl]amino]-3-cyclohexyl-1-oxopropan-2-yl]morpholine-4-carboxamide
-
-
N-[(2S)-2-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-3-methylbutan-2-yl]thiophene-3-carboxamide
-
-
N-[(2S)-3-cyclohexyl-1-([2-[(4-methoxyphenyl)amino]ethyl]amino)-1-oxopropan-2-yl]-5-[3-(trifluoromethyl)phenyl]furan-2-carboxamide
-
-
N-[(2S)-3-cyclohexyl-1-[[(2S)-1-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)propan-2-yl]amino]-1-oxopropan-2-yl]morpholine-4-carboxamide
-
-
N-[(2S)-3-methyl-2-[1-[(2S)-1-oxohexan-2-yl]-1H-1,2,3-triazol-4-yl]butan-2-yl]thiophene-3-carboxamide
-
-
N-[(3S)-4-benzyloxy-(2S)-4-methyl-[[[2-[(9-oxo-9H-1-fluorenyl)carbonyl]amino]propaneyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[(2S)-2-[(3-amino-4-chlorobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[(2S)-2-[(3-[(tert-butoxycarbonyl)amino]-4-chlorobenzoyl amino)]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ester
-
-
N-[(3S)-4-benzyloxy-3-[[[1-[(4-morpholinylcarbonyl)-amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[((1-methylcyclopropyl)carbonyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[((2,2-dimethyl-4-oxo-3,4-dihydro-2H-6-pyranyl)carbonyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[((5-nitro-2-thienyl)carbonyl)amino]cyclo-hexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[((E)-3-(2,5-dimethoxyphenyl)-2-propenoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[(2,3-dioxo-3-(2-thienyl)propanoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[(2-(2-thienyl)acetyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[(2-chloro-5-(methylsulfanyl)benzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[(3-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[(4-chloro-3-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[(4-methoxybenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[(5-chloro-2-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[(5-methoxy-2-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[2-(1-methylethyl)phenyl]-Na-(phenoxycarbonyl)-L-tryptophanamide
-
-
N-[2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)ethyl]-N2-(3-methylbenzoyl)-L-leucinamide
-
-
N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]-2-phenylacetamide
-
-
N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
-
-
N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]piperidine-3-carboxamide
-
-
N-[2-oxo-2-[(2Z)-2-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)hydrazino]ethyl]-2-pyridin-2-yl-1H-benzimidazole-1-carboxamide
-
-
N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-N2-[(3-methylphenyl)carbonyl]-L-leucinamide
-
IC50: 46 nM
N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 27 nM
N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-(3-methylbenzoyl)-L-leucinamide
-
-
N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(3-methylphenyl)carbonyl]-L-leucinamide
-
IC50: 62 nM
N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-4-(trifluoromethyl)-L-phenylalaninamide
-
IC50: 19 nM
N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 29 nM
N-[2-[(4-methoxyphenyl)amino]ethyl]-O-methyl-Na-[(3-methylphenyl)carbonyl]-L-tyrosinamide
-
IC50: 66 nM
N-[4-(4-cyano-1H-imidazo[4,5-c]pyridin-6-yl)-2-(trifluoromethyl)phenyl]formamide
-
-
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]-1-phenylethanamine
-
-
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]-2-phenylethanamine
-
-
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]benzamide
-
-
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]benzenesulfonamide
-
-
N-[[(2S)-1-[[(1S)-1-cyano-3-phenylpropyl]amino]-3-cyclohexyl-1-oxopropan-2-yl]carbamoyl]morpholine-4-carboxamide
-
-
N2-(5-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
-
IC50: 173 nM
N2-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[(1S)-1-[(5-fluoro-2,3-dihydro-1H-indol-1-yl)methyl]-3-(methylsulfonyl)propyl]-L-alaninamide
-
IC50: 21 nM
N2-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[(1S)-2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
-
IC50: 151 nM
N2-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
-
IC50: 93 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-(1-methyl-2-[[3-(methylsulfonyl)phenyl]amino]ethyl)-L-alaninamide
-
IC50: 26 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-(1-methyl-2-[[4-(methylsulfonyl)phenyl]amino]ethyl)-L-alaninamide
-
IC50: 11 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[(2S)-1-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)propan-2-yl]-L-alaninamide
-
-
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-2,2-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
-
IC50: 15 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
-
IC50: 15 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-2-oxo-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
-
IC50: 12.3 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
-
IC50: 3 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
-
IC50: 19 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]-1-methylethyl]-L-alaninamide
-
IC50: 1 nM
N2-(biphenyl-3-ylacetyl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 2.9 nM
N2-(biphenyl-4-ylacetyl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 9.1 nM
N2-(morpholin-4-ylcarbonyl)-N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-leucinamide
-
-
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[(1S)-2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
-
IC50: 26 nM
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)ethyl]-L-alaninamide
-
IC50: 222 nM
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
-
IC50: 94 nM
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 29 nM
N2-1,3-benzoxazol-2-yl-N-[(1R)-2-(benzyloxy)-1-[(5-fluoro-2,3-dihydro-1H-indol-1-yl)methyl]ethyl]-3-cyclohexyl-L-alaninamide
-
IC50: 5 nM
N2-benzoyl-N1-(cyanomethyl)-L-leucinamide
-
IC50: 41 nM
N2-[(3'-chlorobiphenyl-4-yl)acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 7.4 nM
N2-[(5-chloro-1-benzofuran-2-yl)acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 9.4 nM
N2-[[1-(5-bromopyrimidin-2-yl)piperidin-3-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 49 nM
N2-[[1-(5-bromopyrimidin-2-yl)piperidin-4-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 107 nM
N2-[[5-(4-chlorophenyl)furan-2-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 7.1 nM
Na-(morpholin-4-ylcarbonyl)-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)-L-phenylalaninamide
-
-
NEM
-
1 mM, complete inhibition
o-aminobenzoic acid-Leu-Phe-Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
-
o-aminobenzoic acid-Val-Leu-Phe-Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
-
p-chloromercuriphenylsulfonic acid
-
1 mM, 96% inhibition
paecilopeptin
-
i.e. acetyl-Leu-Val-CHO, IC50: 21 nM
Peptidyl(acyloxy)methyl ketones
-
extremely potent inactivator
-
propeptide1-98 of chimeric cathepsin S
-
-
-
squamous cell carcinoma antigen 1
-
99% inhibition at 1 mM, interacts with cathespin S at 1:1 stoichiometry, t1/2 of the cathepsin-squamous cell carcinoma antigen 1 complex is above 1155 min
-
tert-butyl (3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoate
-
IC50: 730 nM
tert-butyl 1'-[(2S)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]-4,4'-bipiperidine-1-carboxylate
-
-
tert-butyl 4-[3'-[1-[[(cyanomethyl)amino]carbonyl]-3-methylbutyl]-1,1'-biphenyl-4-yl]piperazine-1-carboxylate
-
IC50: 1298 nM
tert-butyl 4-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperazine-1-carboxylate
-
-
tert-butyl [(2S)-1-(2-cyanopyrazolidin-1-yl)-1-oxo-3-phenylpropan-2-yl]carbamate
-
-
tert-butyl [(2S)-1-(2-cyanopyrazolidin-1-yl)-3-methyl-1-oxobutan-2-yl]carbamate
-
-
tert-butyl [(2S)-1-(2-cyanopyrazolidin-1-yl)-4-methyl-1-oxopentan-2-yl]carbamate
-
-
tert-butyl [(2S)-1-(2-cyanotetrahydropyridazin-1(2H)-yl)-3-methyl-1-oxobutan-2-yl]carbamate
-
-
tetrahydro-2H-pyran-4-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
-
-
Tg1 domain of testican-1
-
-
-
[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]benzene
-
-
[(2',3',4'-trifluorobiphenyl-2-yl)oxy]acetaldehyde
-
-
[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl](pyrrolidin-1-yl)methanone
-
-
[1S-(1S-cyano-3-phenylpropylcarbamoyl)-3-methylbutyl]-amide
-
IC50: 42 nM
[1S-(2-cyano-1S-phenethyl-ethylcarbamoyl)-3-methylbutyl]amide
-
IC50 above 0.02 mM
[2-[[(4-chlorophenyl)sulfanyl]methyl]-4-hydroxy-6,7-dimethoxyquinazolin-3(4H)-yl]acetonitrile
-
-
[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl](1H-1,2,4-triazol-3-yl)methanone
-
-
[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl](pyrrolidin-1-yl)methanone
-
-
[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl](thiophen-2-yl)methanone
-
-
[[2',3'-difluoro-4'-(2-methylpropyl)biphenyl-2-yl]oxy]acetaldehyde
-
-
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
-
IC50: 18 nM
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
-
-
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
-
IC50: 53 nM
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
-
-
(3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoic acid
-
IC50: 27 nM
(3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoic acid
-
-
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 50 nM
1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
-
1-bromo-3-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1-bromo-3-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1-bromo-3-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1-bromo-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1-bromo-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1-bromo-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
-
-
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
-
-
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
-
-
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
-
-
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
-
-
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
-
-
2-cyano-4-(2-hydroxyethoxy)-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-4-(2-hydroxyethoxy)-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
-
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
-
2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
-
2-cyano-N-methyl-4-[(spiro[3.5]non-7-ylmethyl)amino]-6-[(2,2,6,6-tetramethylpiperidin-4-yl)oxy]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-N-methyl-4-[(spiro[3.5]non-7-ylmethyl)amino]-6-[(2,2,6,6-tetramethylpiperidin-4-yl)oxy]pyrimidine-5-carboxamide
-
-
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
-
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
-
3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
7-(2-cyclohexylethyl)-6-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
Benzyloxycarbonyl-Phe-Phe-CHN2
-
0.0005 mM: 51-58% inhibition after 10 min. 0.005 mM: 86-90% inhibition after 10 min
Benzyloxycarbonyl-Phe-Phe-CHN2
-
t1/2 at 0.001 mM is 6.4 min
Benzyloxycarbonyl-Phe-Phe-CHN2
-
0.001 mM, 98% inhibition
Benzyloxycarbonyl-Phe-Phe-CHN2
-
-
cathespin S propeptide
-
-
-
cathespin S propeptide
-
tight binding/slow reacting inhibition
-
cathespin S propeptide
-
more selective for inhibition of cathepsin L than cathepsin S
-
CLIK-060
-
0.001 mM, complete inhibition
cystatin
-
0.001 mM, complete inhibition
-
cystatin
-
0.5 mg/ml, 82% inhibition
-
cystatin C
-
wild-type and mutant forms
-
cystatin C
-
inhibition in the picomolar range
-
cystatin C
-
specific endogenous inhibitor, potency against smooth muscle cell invasion, overview
-
cystatin C
-
endogenous specific inhibitor
-
cystatin C
-
endogenous specific enzyme inhibitor, absence of cystatin C results in increased angiogene sis and tumor cell proliferation
-
cystatin C
-
endogenous specific enzyme inhibitor, absence of cystatin C results in increased angiogenesis and tumor cell proliferation
-
E-64
-
0.001 mM, 96% inhibition
E-64
-
irreversible inhibitor
E-64
-
0.005 mM, 96% inhibition
E64
-
-
E64
-
potency against smooth muscle cell invasion, overview
E64
-
cysteine protease inhibitor
E64
-
general cathepsin inhibitor
egg white cystatin
-
-
-
JNJ 10329670
-
-
JNJ 10329670
-
CAS: 400797-24-2, the inhibitor blocks the presentation of tetanus toxoid and giant ragweed by human PBMCs, the inhibitor is a candidate for immunosuppressive therapy of allergies and autoimmune diseases, completely reversible inhibition
JNJ 10329670
-
competitive, reversible inhibition, 4-(2-keto-1-benzimidazolinyl)-piperidin-1-yl derivative, IC50: 100 nM
L-873724
-
-
leupeptin
-
5.2 nM
leupeptin
-
1 mM, complete inhibition
LHVS
-
-
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfinate
-
-
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfinate
-
-
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfinate
-
-
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfenate
-
-
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfenate
-
-
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfenate
-
-
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfinate
-
-
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfinate
-
-
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfinate
-
-
N-morpholinurea-leucine-homophenylalanine-vinylsulfone-phenyl
-
i.e. LHVS, specific inhibitor, potency against smooth muscle cell invasion, overview
N-morpholinurea-leucine-homophenylalanine-vinylsulfone-phenyl
-
specific inhibitor
N-morpholinurea-leucine-homophenylalanine-vinylsulfone-phenyl
-
specific inhibitor
N-morpholinurea-leucyl-homophenylalanyl-vinylsulfone-phenyl
-
i.e. LHVS, irreversible inhibition, the inhibitor binds covalently to the active site, in vitro and in vivo inhibition
N-morpholinurea-leucyl-homophenylalanyl-vinylsulfone-phenyl
-
i.e. LHVS, irreversible inhibition, the inhibitor binds covalently to the active site
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-1-benzofuran-2-carboxamide
-
IC50: 17 nM
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-1-benzofuran-2-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-(3-fluorophenyl)furan-2-carboxamide
-
IC50: 34 nM
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-(3-fluorophenyl)furan-2-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-[3-(trifluoromethyl)phenyl]furan-2-carboxamide
-
IC50: 11 nM
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-[3-(trifluoromethyl)phenyl]furan-2-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-2-carboxamide
-
IC50: 47 nM
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-2-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-3-carboxamide
-
IC50: 6 nM
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-3-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-3-carboxamide
-
IC50: 213 nM
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-3-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
-
IC50: 11 nM
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydro-2H-pyran-4-carboxamide
-
IC50: 12 nM
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydro-2H-pyran-4-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-3-carboxamide
-
IC50: 21 nM
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-3-carboxamide
-
-
RO5461111
-
RO5461111
inhibits Cat-S activity and reduces podocyte loss, proteinuria, glomerulosclerosis, and renal inflammation in T2D db/db mice
Stefin A
-
human stefin A
-
Stefin B
-
bovine stefin B, competitive
-
Stefin B
-
human and bovine stefin B
-
tetrahydro-2H-pyran-4-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
-
IC50: 12 nM
tetrahydro-2H-pyran-4-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
-
-
additional information
-
inhibitory potential in vivo on Ii degradation in JY cells
-
additional information
-
analysis of inhibition mechanisms and binding to the active site; design and synthesis of arylaminoethyl amides as noncovalent inhibitors of cathepsin S, overview
-
additional information
-
synthesis and evaluation of heterocyclic arylaminoethyl amides as noncovalent inhibitors of cathepsin S, binding specificities of positions P1-P3 and of subsite S3, overview
-
additional information
-
reversible inhibition by a dipeptide-nitrile inhibitor
-
additional information
-
diverse arylaminoethyl amides as noncovalent inhibitors of cathepsin S with IC50 in the nanomolar range, optimization of P1 and N-aryl, binding specificities of positions P1 and P2, and of subsite S1, overview
-
additional information
-
no inhibition by proteasome inhibitors
-
additional information
-
effect of cathepsin S inhibition on bronchoalveolar lavage fluid cytokines: inhibition reduces ozone-induced interleukin-6 levels at 3 h and 20-24 h and TNF-alpha levels are inhibited at 20-24 h
-
additional information
design and synthesis of a near-infrared quenched activity-based probes (qABP) that selectively target cathepsin S which is highly expressed in immune cells, green-fluorescent pan-reactive cysteine cathepsin qABP in dual color labeling studies in bone marrow-derived immune cells, and identification of vesicles containing exclusively cathepsin S activity, method optimization and evaluation, overview. The high degree of selectivity is retained both in vitro and in vivo
-
additional information
-
synthesis and inhibitory effects of diverse arylaminoethyl carbamate inhibitors possessing a substrate peptidomimetic scaffold, structue-activity relationship, pharmacokinetics, overview
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0.000095
(2R)-2-(2-cyclohexylethyl)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000002
(2R)-2-(2-cyclopentylethyl)-4-morpholin-4-yl-4-oxo-N-[(1S)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
0.000011
(2R)-2-(2-cyclopentylethyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000194
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)butanamide
-
-
0.000013
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)butyl]butanamide
-
-
0.000016
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
0.000062
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-phenyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]butanamide
-
-
0.000018
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
0.000028
(2R)-2-(cyclohexylmethyl)-N-[(1R)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000011
(2R)-2-(cyclohexylmethyl)-N-[(1R)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.1
(2R)-2-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
Ki above 0.1 mM
0.000012
(2R)-2-(cyclopentylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1S)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)butyl]butanamide
-
-
0.000031
(2R)-2-(cyclopentylmethyl)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000038
(2R)-2-(cyclopentylmethyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.024
(2R)-2-benzyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
Ki above 0.024 mM
0.000408
(2R)-4-dimethyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-2-(2-morpholin-4-yl-2-oxoethyl)pentanamide
-
-
0.00006
(2R)-4-morpholin-4-yl-4-oxo-2-(2-phenylethyl)-N-[(1S)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
0.00007
(2R)-5-dimethyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-2-(2-morpholin-4-yl-2-oxoethyl)hexanamide
-
-
0.000014
(2R)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-2-(2-morpholin-4-yl-2-oxoethyl)-5-phenylpentanamide
-
-
0.000027
(2R)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-(2-phenylethyl)butanamide
-
-
0.000021
(2S)-2-(4-chlorophenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000024
(2S)-2-(4-fluorophenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000105
(2S)-2-(4-methoxyphenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000134
(2S)-2-(4-methylphenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.001368
(2S)-2-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000019
(2S)-3-cyclohexyl-1-(morpholin-4-yl)-1-oxopropan-2-yl [(2S)-1-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)propan-2-yl]carbamate
-
-
0.000261
(2S)-4-morpholin-4-yl-4-oxo-2-phenyl-N-[(1S)-1-phenyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]butanamide
-
-
0.000037
(2S)-4-morpholin-4-yl-4-oxo-2-phenyl-N-[(1S)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
0.0156
(2S)-4-morpholin-4-yl-4-oxo-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
0.000616
(2S)-N-[(1S)-1-cyclopropyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
0.00159
(2S)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
0.000025
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-phenylbutanamide
-
-
0.1
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[2-(trifluoromethyl)phenyl]butanamide
-
Ki above 0.1 mM
0.01853
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[3-(trifluoromethyl)phenyl]butanamide
-
-
0.000043
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
0.000043
(2S)-N-[(2S)-3-methyl-1-[[4-(trifluoromethoxy)phenyl]amino]butan-2-yl]-4-(morpholin-4-yl)-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
0.00844
(2Z)-3-(4-[[5-(3,5-dimethylisoxazol-4-yl)-1,2,4-oxadiazol-3-yl]methoxy]phenyl)-2-(methylsulfonyl)prop-2-enenitrile
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.1
(3R)-3-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
Ki above 0.1 mM
0.001721
(3S)-3-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000071
(3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoic acid
-
-
0.00298
(3S)-N-[2-(1H-indol-3-yl)ethyl]-3-[[(4-methylphenyl)sulfonyl]amino]-2-oxo-4-phenylbutanamide
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.00031
(S)-[1-[1-cyano-pyrrolidin-3(R)-ylcarbamoyl]-3-methyl-butyl]-carbamic acid benzyl ester
-
pH 6.5, 23°C
0.00097
(S)-[1-[1-cyano-pyrrolidin-3(S)-ylcarbamoyl]-3-methyl-butyl]-carbamic acid benzyl ester
-
pH 6.5, 23°C
0.4377
1,1-bis(cyanomethyl)-3-[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]urea
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.0000083
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[(4-[[(2,2,2-trifluoroethyl)sulfonyl]amino]benzoyl)amino]propanoyl]amino)-L-erythro-hex-2-ulose
-
-
0.00003
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([2-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000049
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000004
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000012
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000026
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000008
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000023
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000021
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-3-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000027
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-4-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000023
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(thiophen-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00011
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[methyl(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000063
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(methylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000056
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(phenylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000019
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-([4-[(ethylsulfonyl)amino]benzoyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.0000053
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-([[4-([[(dimethylamino)methyl]sulfonyl]amino)phenyl]carbonyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000007
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[(4-[[(2,4-dimethyl-1,3-thiazol-5-yl)sulfonyl]amino]benzoyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose ammoniate (1:1)
-
-
0.0000034
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[(4-[[(3-fluorophenyl)sulfonyl]amino]benzoyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.000001
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[(4-[[(3-methoxyphenyl)sulfonyl]amino]benzoyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.00033
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([2-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000016
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-fluoro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000026
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000019
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([4-[(ethylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000007
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2,4-dimethyl-1,3-thiazol-5-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000038
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000034
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000001
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000002
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000033
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000012
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([3-[(methylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.0000026
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([4-[(methylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.0000008
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([4-[(phenylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.0000009
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([4-[(pyridin-4-ylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.00019
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-(methylsulfamoyl)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000057
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-([[4-(1-methylethyl)-1,3-thiazol-2-yl]sulfonyl]amino)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00014
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-sulfamoylphenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000045
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methyl-1H-imidazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000029
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methylethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000083
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2,2,2-trifluoroethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000039
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2-methylphenyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000013
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000009
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methylpyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000086
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(5-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00014
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[4-(methylsulfamoyl)benzoyl]amino]propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.000031
1,4-anhydro-3,5,6-trideoxy-3-[[4-methyl-N-(thiophen-3-ylcarbonyl)-L-leucyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00018
1,4-anhydro-3-[[(2S)-2-([4-[(cyclohexylsulfonyl)amino]benzoyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-erythro-hex-2-ulose
-
-
0.0000024
1,4-anhydro-3-[[(2S)-2-([4-[(cyclopropylsulfonyl)amino]benzoyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-erythro-hex-2-ulose
-
-
0.0000056
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000012
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000031
1,4-anhydro-3-[[(2S)-2-[([4-[(benzylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000034
1,4-anhydro-3-[[(2S)-2-[([4-[(butylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000024
1,4-anhydro-3-[[(2S)-2-[([4-[(cyclopropylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000059
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-chloropyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000008
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000006
1,4-anhydro-3-[[(2S)-2-[[(4-[[(3-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000011
1,4-anhydro-3-[[(2S)-2-[[(4-[[(4-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00018
1,4-anhydro-3-[[(2S)-2-[[(4-[[(cyclohexylmethyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000033
1-cyano-(3,4-didehydro)-Pro-Leu methyl ester
-
pH 6.5, 23°C
0.026
1-cyano-(D)-Pro-(D)-Leu methyl ester
-
pH 6.5, 23°C
0.054
1-cyano-(D)-Pro-Ala methyl ester
-
pH 6.5, 23°C
0.000012
1-cyano-(D)-Pro-Leu benzyl ester
-
pH 6.5, 23°C
0.03
1-cyano-(D)-Pro-Leu benzylamide
-
pH 6.5, 23°C
0.00015
1-cyano-(D)-Pro-Leu dimethylamide
-
pH 6.5, 23°C
0.00054
1-cyano-(D)-Pro-Leu methyl ester
-
pH 6.5, 23°C
0.00003
1-cyano-(trans-benzyloxy)prolylleucine methyl ester
-
pH 6.4, 25°C
0.000054
1-cyano-(trans-hydroxy)-Pro-Leu methyl ester
-
pH 6.5, 23°C
0.00028
1-cyano-Pro isoamylamide
-
pH 6.5, 23°C
0.0011
1-cyano-Pro-(D)-Leu methyl ester
-
pH 6.5, 23°C
0.00053
1-cyano-Pro-Ala methyl ester
-
pH 6.5, 23°C
0.000014
1-cyano-Pro-Leu benzyl ester
-
pH 6.5, 23°C
0.000052
1-cyano-Pro-Leu methyl ester
-
pH 6.5, 23°C
0.000035
1-cyano-Pro-Leu-Gly ethyl ester
-
pH 6.5, 23°C
0.0000067
1-cyano-Pro-Leu-Leu-Leu methyl ester
-
pH 6.5, 23°C
0.00024
1-cyano-Pro-Phe methyl ester
-
pH 6.5, 23°C
0.01458
2,2'-[[3-(trifluoromethyl)phenyl]imino]bis[N-(4-methylphenyl)acetamide]
-
in 0.5 M MES, 2 mM DTT at pH 6.0
146.3
2-(4-tert-butylphenyl)-5-[[2-(3,4-dimethoxyphenyl)ethyl]amino]-1,3-oxazole-4-carbonitrile
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.05686
2-hydroxy-N'-[1H-indol-3-yl(oxo)acetyl]-2,2-diphenylacetohydrazide
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.0109
2-[[3-(4-chloro-5-hydroxy-2-methoxyphenyl)-4-oxo-3,4-dihydroquinazolin-2-yl]sulfanyl]-N-[(1S)-1-cyano-1,2-dimethylpropyl]acetamide
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.000057
3-[[(2S)-2-[([3-acetyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000013
3-[[(2S)-2-[[(4-[[(4-aminophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00000064
4-morpholinecarboxamide, N-[(1R)-2-[[(1S)-1-(2-benzoxazolylcarbonyl) propyl] amino]-1-[[(cyclopropylmethyl)-sulfonyl]methyl]-2-oxoethyl]
-
excellent selectivity and activity for cathepsin S over the other cathepsin family members L, K and B
3.39
4-[(4-[(E)-[(cyanoacetyl)hydrazono]methyl]phenoxy)methyl]benzoic acid
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.000004
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
with Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as substrate
0.0027
benzyloxycarbonyl-Ala-Leu-COCHO
-
pH 6.4, 25°C
0.000018
benzyloxycarbonyl-Phe-Ala-CH2F
-
pH 6.5
0.00125
Benzyloxycarbonyl-Phe-Ala-CHN2
-
pH 6.5, 25°C
0.0000232
benzyloxycarbonyl-Phe-Ala-COCHO
-
pH 6.4, 25°C
0.0000024
Benzyloxycarbonyl-Phe-Arg
-
pH 6.4, 25°C
0.000000185
benzyloxycarbonyl-Phe-Leu-COCHO
-
pH 6.4, 25°C
0.0014
benzyloxycarbonyl-Phe-Lys(benzyloxycarbonyl)-CH3
-
pH 6.5
0.00000223
benzyloxycarbonyl-Phe-Tyr(OBut)-COCHO
-
pH 6.4, 25°C
0.0018
benzyloxycarbonyl-Val-Val-CH3
-
pH 6.5
0.00015
benzyloxycarbonyl-Val-Val-Lys-NHO-4-nitrobenzoyl
-
pH 6.5, 25°C
0.0000063
cathepsin K propeptide
-
-
-
0.000065
cathepsin L propeptide
-
-
-
0.00000005 - 0.0000076
cathepsin S propeptide
-
0.001
CLIK60
-
CatS activity in RAW264.7 cells or peritoneal macrophages from C57Bl/6 or LDLr-/-mice is completely repressed
0.00000001
cystatin C mutant L9W/W106G
-
pH 7.0, 37°C
-
0.000000011
cystatin C mutant V10F/W106G
-
pH 7.0, 37°C
-
0.0000015
cystatin C mutant V10R/W106G
-
pH 7.0, 37°C
-
0.00000019
cystatin C mutant V10W/W106G
-
pH 7.0, 37°C
-
0.00000011
cystatin C mutant W106G
-
pH 7.0, 37°C
-
0.000034 - 0.002364
JNJ 10329670
0.01663
methyl (2Z)-4-[4-(dimethylamino)phenyl]-4-oxo-2-[(phenylcarbonyl)hydrazono]butanoate
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.000005
methyl (3R)-3-[[(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanoyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate
-
-
0.000069
methyl (3S)-3-[[(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanoyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate
-
-
0.00278
methyl 4-[(E)-[[(3-[2-[(2-chlorobenzyl)oxy]phenyl]-1H-pyrazol-5-yl)carbonyl]hydrazono]methyl]benzoate
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.00005
morpholine-4-carboxylic acid [1S-[1S-(benzoyl-hydrazonomethyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
pH 4.5
0.000033
morpholine-4-carboxylic acid [1S-[1S-[(2-hydroxy-benzoyl)-hydrazonomethyl]-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
pH 4.5
0.00011
morpholine-4-carboxylic acid [1S-[1S-[(4-hydroxybenzoyl)-hydrazonomethyl]-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
pH 4.5
0.1982
N-(4-cyano-1-phenyl-1H-pyrazol-5-yl)-2-[(4-ethyl-5-thiophen-2-yl-4H-1,2,4-triazol-3-yl)sulfanyl]acetamide
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.0000055
N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-norvalinamide
-
-
0.00889
N-[(1R)-1-([2-[(1,3-benzoxazol-2-ylsulfanyl)acetyl]hydrazino]carbonyl)propyl]-2-[(phenylcarbonyl)amino]benzamide
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.0012
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1,2-dimethylpropyl]benzamide
-
-
0.00042
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1,2-dimethylpropyl]thiophene-3-carboxamide
-
-
0.000015
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-(4-methylcyclohexyl)ethyl]thiophene-3-carboxamide
-
-
0.000015
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-(trans-4-methylcyclohexyl)ethyl]thiophene-3-carboxamide
-
-
0.0002
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-cyclohexylethyl]benzamide
-
-
0.000018
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-cyclohexylethyl]thiophene-3-carboxamide
-
-
0.00042
N-[(2S)-2-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-3-methylbutan-2-yl]thiophene-3-carboxamide
-
-
0.000009
N-[(2S)-3-methyl-2-[1-[(2S)-1-oxohexan-2-yl]-1H-1,2,3-triazol-4-yl]butan-2-yl]thiophene-3-carboxamide
-
-
0.01948
N-[2-(1-methylethyl)phenyl]-Na-(phenoxycarbonyl)-L-tryptophanamide
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.01527
N-[2-oxo-2-[(2Z)-2-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)hydrazino]ethyl]-2-pyridin-2-yl-1H-benzimidazole-1-carboxamide
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.000068
N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-(3-methylbenzoyl)-L-leucinamide
-
-
0.000003
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[(2S)-1-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)propan-2-yl]-L-alaninamide
-
-
0.025
o-aminobenzoic acid-Leu-Phe-Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
substrate N-benzyloxycarbonyl-L-Phe-Arg-7-amido-4-methylcoumarin
0.02
o-aminobenzoic acid-Val-Leu-Phe-Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
substrate N-benzyloxycarbonyl-L-Phe-Arg-7-amido-4-methylcoumarin
0.00049
[(2',3',4'-trifluorobiphenyl-2-yl)oxy]acetaldehyde
-
-
0.02817
[2-[[(4-chlorophenyl)sulfanyl]methyl]-4-hydroxy-6,7-dimethoxyquinazolin-3(4H)-yl]acetonitrile
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.0000096
[[2',3'-difluoro-4'-(2-methylpropyl)biphenyl-2-yl]oxy]acetaldehyde
-
-
additional information
(2S)-2-amino-N-[(1S)-2-(biphenyl-4-yl)-1-cyanoethyl]butanamide
0.00000005
cathepsin S propeptide
-
wild-type enzyme
-
0.00000027
cathepsin S propeptide
-
pH 6.5, 37°C
-
0.0000003
cathepsin S propeptide
-
mutant enzyme E44A
-
0.0000013
cathepsin S propeptide
-
mutant enzyme R48A
-
0.0000025
cathepsin S propeptide
-
using benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin as a substrate
-
0.0000076
cathepsin S propeptide
-
-
-
0.000034
JNJ 10329670
-
pH 5.0
0.000124
JNJ 10329670
-
pH 5.0
0.000266
JNJ 10329670
-
pH 5.0
0.000411
JNJ 10329670
-
pH 5.0
0.002364
JNJ 10329670
-
pH 5.0
additional information
(2S)-2-amino-N-[(1S)-2-(biphenyl-4-yl)-1-cyanoethyl]butanamide
-
value above 0.01
additional information
additional information
-
Ki-value for wild-type cystatin C, and the mutant cystatins V10F, V10W, V10R, and L9W are below 0.01 nM
-
additional information
additional information
-
Ki-values above 0.15 mM: 1-iminomethyl-(D)-Pro-Leu benzyl ester, 1-formyl-(D)-Pro-Leu benzyl ester
-
additional information
N2-(morpholin-4-ylcarbonyl)-N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-leucinamide
-
value below 0.0000001
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
0.000395
(2R)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.0001
(2R)-2-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)-2-phenylethanol
Homo sapiens
-
-
0.001991
(2R)-2-[4'-(1-azabicyclo[2.2.2]oct-4-yl)-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
Homo sapiens
-
IC50: 1991 nM
0.00834
(2R)-2-[4'-(4-tert-butylpiperazin-1-yl)-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
Homo sapiens
-
IC50: 8340 nM
0.001427
(2R)-2-[4'-[1-(2-amino-2-methylpropyl)piperidin-4-yl]-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
Homo sapiens
-
IC50: 1427 nM
0.00008
(2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-N-(1-cyanocyclopropyl)-3-(methylsulfanyl)propanamide
Homo sapiens
-
-
0.000135
(2R)-N-(1-cyanocyclopropyl)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.01
(2R)-N-(cyanomethyl)-2-[4'-[4-(2-hydroxy-2-methylpropyl)-1-piperazinyl][1,1'-biphenyl]-3-yl]-4-methylpentanamide
Homo sapiens
-
IC50 above 0.01 mM
0.000609
(2R)-N-(cyanomethyl)-2-[4'-[4-(2-hydroxyethyl)-1-piperazinyl][1,1'-biphenyl]-3-yl]-4-methylpentanamide
Homo sapiens
-
IC50: 609 nM
0.00201
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)-[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 2010 nM
0.01
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1H-tetraazol-5-yl)-1,1'-biphenyl-3-yl]pentanamide
Homo sapiens
-
IC50 above 0.01 mM
0.003931
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methyl-1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 3931 nM
0.001365
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-pyrimidinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 1365 nM
0.002364
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-[4-(2-oxopropyl)-piperazin-1-yl]-1,1'-biphenyl-3-yl]pentanamide
Homo sapiens
-
IC50: 2364 nM
0.000037
(2R)-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000062
(2R)-N-[(1R)-2-[(4-chlorobenzyl)oxy]-1-cyanoethyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000658
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-2-carboxamide
Homo sapiens
-
IC50: 658 nM
0.000018 - 0.000053
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
0.000171
(2R)-N-[(1S)-1-cyano-3-phenylpropyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000207
(2R)-N-[(3R)-1-benzyl-3-cyanopiperidin-4-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000066
(2R)-N-[(3R)-3-cyano-1-(1-methylethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000039
(2R)-N-[(3R)-3-cyano-1-(2-methylpropyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000022
(2R)-N-[(3R)-3-cyano-1-(2-phenylethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000022
(2R)-N-[(3R)-3-cyano-1-(cyclopropylmethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000023
(2R)-N-[(3R)-3-cyano-1-cycloheptylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000042
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(2,3-dihydro-1H-inden-2-ylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
-
0.000042
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(2,3-dihydro-1H-inden-2-ylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000023
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000063
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclopentylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000047
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(1-methylcyclohexyl)methyl]-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000014
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(4-methylcyclohexyl)methyl]-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.0000019
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-(morpholin-4-yl)-4-oxo-2-(1,2,3,4-tetrahydronaphthalen-2-ylmethyl)butanamide
Homo sapiens
-
-
0.003136
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-(morpholin-4-yl)-4-oxo-2-[(4-phenylcyclohexyl)methyl]butanamide
Homo sapiens
-
-
0.0000019
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-morpholin-4-yl-4-oxo-2-(1,2,3,4-tetrahydronaphthalen-2-ylmethyl)butanamide
Homo sapiens
-
-
0.003136
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-morpholin-4-yl-4-oxo-2-[(4-phenylcyclohexyl)methyl]butanamide
Homo sapiens
-
-
0.000075
(2R)-N-[(3R)-3-cyano-1-cyclopentylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000251
(2R)-N-[(3R)-3-cyano-1-methylpiperidin-4-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000155
(2R)-N-[(3R)-3-cyano-1-methylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000141
(2R)-N-[(3R)-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
-
0.000141
(2R)-N-[(3R)-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000029
(2R)-N-[(3S)-1-benzyl-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000041
(2R)-N-[(3S)-3-cyano-1-(cyclohexylmethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.00003
(2S)-1-(4,4'-bipiperidin-1-yl)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
Homo sapiens
-
-
0.000245
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxypropan-1-one
Homo sapiens
-
-
0.000058
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.00035
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(propan-2-ylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.0003
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(propylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.00001
(2S)-1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(1'-methyl-4,4'-bipiperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.000658
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-2-carboxamide
Rattus norvegicus
-
-
0.000018 - 0.000053
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
0.00033
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(furan-2-yl)methanone
Homo sapiens
-
-
0.00014
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(pyridin-2-yl)methanone
Homo sapiens
-
-
0.00031
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(tetrahydrofuran-2-yl)methanone
Homo sapiens
-
-
0.000006
(3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]phenyl)acetic acid
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000042
(3R)-tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
Homo sapiens
-
IC50: 42 nM
0.000012
(3S)-3-[(N-1,3-benzoxazol-2-yl-3-cyclohexyl-L-alanyl)amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoic acid
Homo sapiens
-
IC50: 12 nM
0.000027
(3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoic acid
Homo sapiens
-
IC50: 27 nM
0.000049
(3S)-tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
Homo sapiens
-
IC50: 49 nM
0.0000043
(4R)-1-acetyl-N-[(2R)-1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000033
(4R)-1-acetyl-N-[(2S)-1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0001
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxo-3-phenylpropan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0001
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(ethylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000207
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfanyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000837
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfinyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000033
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.001
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-phenoxy-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000023
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[(2-chlorophenyl)sulfonyl]-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000032
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[(4-fluorophenyl)sulfonyl]-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000032
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[[4-(1H-pyrazol-1-yl)phenyl]sulfonyl]-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000181
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxopropan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000246
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-3-methyl-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000024
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(2-methylpropanoyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000454
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(2-oxopropyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000011
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(3-chlorobenzoyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000033
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(3-methoxypropanoyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.000002
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(4-chlorobenzoyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000041
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(biphenyl-4-ylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000033
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(cyclohexylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000035
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(methylsulfinyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.000003
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-benzoyl-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000124
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-phenyl-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000035
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyridin-3-ylcarbonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000033
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyridin-4-ylcarbonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000037
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyrrolidin-1-ylcarbonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000027
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(trifluoroacetyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000031
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-propanoyl-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.000156
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000366
(4R)-N-[2-(1,3-benzoxazol-2-yl)-2-oxoethyl]-1-(cyclohexylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.01
(4S)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]hexanamide
Homo sapiens
-
IC50 above 0.01 mM
0.0000002
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)benzene
Homo sapiens
-
-
0.0000002 - 0.000015
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
0.0017
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
Homo sapiens
-
effect of R1 substituent on the Ii p10 cell assay at 37°C
0.00012
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
Homo sapiens
-
effect of R1 substituent on the Ii p10 cell assay at 37°C
0.00031
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2,4-dimethyl-1,3-thiazol-5-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
Homo sapiens
-
effect of R1 substituent on the Ii p10 cell assay at 37°C
0.00015
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
Homo sapiens
-
effect of R1 substituent on the Ii p10 cell assay at 37°C
0.000062
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
Homo sapiens
-
effect of R1 substituent on the Ii p10 cell assay at 37°C
0.0014
1,4-anhydro-3-[[(2S)-2-[[(4-[[(3-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
Homo sapiens
-
effect of R1 substituent on the Ii p10 cell assay at 37°C
0.00001
1-(1'-[(2S)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]-4,4'-bipiperidin-1-yl)ethanone
Homo sapiens
-
-
0.00035
1-(1-[(2R)-3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 350 nM
0.00019
1-(1-[(2S)-3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 190 nM
0.00001
1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 10 nM
0.00005
1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 50 nM
0.00005
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 50 nM
0.00005
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 50 nM
0.00014
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 140 nM
0.00006
1-(1-[3-[3-(4-chloro-3-methylphenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 60 nM
0.0002
1-(1-[3-[3-[3-[(2-hydroxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)pyrrolidin-2-one
Homo sapiens
-
-
0.00022
1-(1-[3-[5-(methylsulfonyl)-3-[3-[(2-phenoxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)pyrrolidin-2-one
Homo sapiens
-
-
0.00008
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 80 nM
0.00011
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5,6-dichloro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 110 nM
0.00014
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methoxy-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 140 nM
0.00009
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 90 nM
0.00012
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 120 nM
0.00021
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-7-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 210 nM
0.00013
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 130 nM
0.00009
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-(2,2,2-trifluoroethyl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 90 nM
0.00014
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-butyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 140 nM
0.00031
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 310 nM
0.0005
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 500 nM
0.0001
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-tert-butyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 100 nM
0.0001
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 100 nM
0.00046
1-(1-[3-[5-acetyl-3-(4-chlorophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 460 nM
0.00012
1-(1-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 120 nM
0.00023
1-(1-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-fluoro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 230 nM
0.000565
1-(2-[[5-[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl]ethyl)piperidin-4-ol
Homo sapiens
-
-
0.00022
1-(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)-2-hydroxyethanone
Homo sapiens
-
-
0.00029
1-(4-cyclopropylpiperazin-1-yl)-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
Homo sapiens
-
-
0.00115
1-(4-methylpiperazin-1-yl)-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
Homo sapiens
-
-
0.0001
1-(ethenylideneamino)-3-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 100 nM
0.0000002 - 0.000044
1-bromo-3-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
0.0000002 - 0.000066
1-bromo-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
0.0000141
1-methyl-6-[4-(piperidin-4-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000316
1-methyl-6-[4-(piperidin-4-yloxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00002
1-methyl-6-[4-(pyridin-2-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000126
1-methyl-6-[4-(pyridin-3-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00001
1-methyl-6-[4-(pyridin-4-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000078
1-methyl-6-[4-[(3-oxopiperazin-1-yl)oxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000078
1-methyl-6-[4-[2-(2-oxopyrrolidin-1-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000011
1-methyl-6-[4-[2-(6-methylpyridin-2-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000083
1-methyl-6-[4-[2-(piperidin-4-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000095
1-methyl-6-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000028
1-methyl-6-[4-[3-(pyrrolidin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000627
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-([[1-(4-fluorophenyl)-1-methylethoxy]sulfinyl]methyl)-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
Homo sapiens
-
-
0.0000004
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(2-methylpropoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
Homo sapiens
-
-
0.0000004
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(4-fluorophenoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
Homo sapiens
-
-
0.0000005 - 0.000759
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
0.0000003 - 0.000021
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
0.0000003
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
Homo sapiens
-
-
0.0000005
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)methyl]-4-fluorobenzene
Homo sapiens
-
-
0.00004
1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00005
1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 50 nM
0.00201
1-[1-(3-[3-[3-([2-[benzyl(methyl)amino]ethyl]sulfanyl)-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.0001
1-[1-(3-[3-[3-[[2-(2-methylpyrrolidin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00009
1-[1-(3-[3-[3-[[2-(3-hydroxypyrrolidin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00034
1-[1-(3-[3-[3-[[2-(4-hydroxypiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00074
1-[1-(3-[3-[3-[[2-(4-methylpiperazin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00106
1-[1-(3-[3-[3-[[2-(4-methylpiperazin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00021
1-[1-(3-[3-[3-[[2-(4-methylpiperidin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00011
1-[1-(3-[3-[3-[[2-(4-methylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00016
1-[1-(3-[3-[3-[[2-(4-tert-butylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.0007
1-[1-(3-[3-[3-[[2-(benzylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00128
1-[1-(3-[3-[3-[[2-(dimethylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.0008
1-[1-(3-[3-[3-[[2-(methylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00012
1-[1-(3-[3-[3-[[3-hydroxy-2-oxo-3-(piperidin-4-yl)propyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.0002
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(4-phenylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00002
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00027
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.000055
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(octahydroisoquinolin-2(1H)-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00017
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00041
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(pyrrolidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00007
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-oxo-2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00006
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-oxo-2-(pyrrolidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00005
1-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 50 nM
0.00013
1-[1-(3-[5-acetyl-3-[4-(trifluoromethoxy)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 130 nM
0.0001
1-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 100 nM
0.00011
1-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 110 nM
0.00018
1-[1-[(2R)-3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl]-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 180 nM
0.0002
1-[1-[(2S)-3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl]-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 200 nM
0.000032
1-[2-(dimethylamino)ethyl]-6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000027
1-[3-(dimethylamino)propyl]-6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00113
1-[3-[3-[(2-aminoethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.00011
1-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidine-4-carboxamide
Homo sapiens
-
-
0.00031
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-(methylsulfanyl)ethanone
Homo sapiens
-
-
0.000235
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxyethanone
Homo sapiens
-
-
0.00047
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-methoxyethanone
Homo sapiens
-
-
0.000385
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]ethanone
Homo sapiens
-
-
0.00069
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]propan-1-one
Homo sapiens
-
-
0.0096
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.000149
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.009
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-methyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.00005
1-[3-[4-(2-cyanophenyl)piperazin-1-yl]-2-hydroxypropyl]-3-(4-iodophenyl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide
Homo sapiens
-
IC50: 50 nM
0.000058
1-[3-[4-(5-methyl-1H-indol-3-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00014
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(morpholin-4-yl)propan-2-ol
Homo sapiens
-
-
0.00038
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperazin-1-yl)propan-2-ol
Homo sapiens
-
-
0.00008
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.001035
1-[4-(2-[[5-[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl]ethyl)piperazin-1-yl]ethanone
Homo sapiens
-
-
0.00071
1-[4-(dimethylamino)piperidin-1-yl]-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
Homo sapiens
-
-
0.00008
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(3,4-dichlorobenzyl)methanamine
Homo sapiens
-
-
0.00023
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(4-methoxybenzyl)methanamine
Homo sapiens
-
-
0.00035
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(4-methylbenzyl)methanamine
Homo sapiens
-
-
0.0013
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-methylmethanamine
Homo sapiens
-
-
0.00049
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
Homo sapiens
-
-
0.00042
1-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.000325
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(morpholin-4-yl)propan-2-ol
Homo sapiens
-
-
0.000204
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.000595
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(propylamino)propan-2-ol
Homo sapiens
-
-
0.000335
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(pyrrolidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.00001
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-[4-(pyridin-2-yl)piperidin-1-yl]propan-2-ol
Homo sapiens
-
-
0.000218
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-[4-(pyrrolidin-1-yl)piperidin-1-yl]propan-2-ol
Homo sapiens
-
-
0.000712
1-[5-(methylsulfonyl)-3-[3-[[2-(pyrrolidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.02
2,3,4,5,6-pentafluoro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
Homo sapiens
-
IC50: 0.020 mM
0.001578
2-(1,1'-biphenyl-3-yl)-N-(cyanomethyl)-4-methylpentanamide
Homo sapiens
-
IC50: 1578 nM
0.003343
2-(1,1'-biphenyl-4-yl)-N-(cyanomethyl)-4-methylpentanamide
Homo sapiens
-
IC50: 3343 nM
0.00028
2-(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)-2-oxoethyl acetate
Homo sapiens
-
-
0.00012
2-(4-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperazin-1-yl)benzonitrile
Homo sapiens
-
IC50: 120 nM
0.0003
2-([5-[1-[2-hydroxy-3-[(3S)-3-methylmorpholin-4-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00001
2-([5-[1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00002
2-([5-[1-[2-hydroxy-3-[4-(3-methyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00001
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00001
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(piperidin-1-yl)ethanone
Homo sapiens
-
-
0.000001
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(pyrrolidin-1-yl)ethanone
Homo sapiens
-
-
0.000007
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-[(3R)-3-hydroxypyrrolidin-1-yl]ethanone
Homo sapiens
-
-
0.000007
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-[(3S)-3-hydroxypyrrolidin-1-yl]ethanone
Homo sapiens
-
-
0.00004
2-([5-[1-[2-hydroxy-3-[4-(pyrrolidin-1-ylcarbonyl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00001
2-([5-[1-[3-[4-(2-fluorophenyl)piperazin-1-yl]-2-hydroxypropyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.000005
2-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)-1,3-thiazolidine
Homo sapiens
-
-
0.0000013
2-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)-2,3-dihydro-1,3-benzothiazole
Homo sapiens
-
-
0.00081
2-amino-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]ethanone
Homo sapiens
-
-
0.000035
2-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
Homo sapiens
-
IC50: 35 nM
0.000006
2-cyano-4-(2-hydroxyethoxy)-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
0.00013
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
0.000014
2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide
0.000031
2-cyano-4-[(1,4-dioxaspiro[4.5]dec-8-ylmethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000026
2-cyano-4-[(2-cyclopentylethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000032
2-cyano-4-[(cyclohexylmethyl)(methyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000022
2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
0.000022
2-cyano-4-[[(4,4-difluorocyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000093
2-cyano-4-[[(4,4-dimethylcyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000003
2-cyano-4-[[1-(2-hydroxyethyl)piperidin-4-yl]methoxy]-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000007
2-cyano-N-(1-methyl-4-phenylpiperidin-4-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000015
2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
0.000024
2-cyano-N-(4,5-dimethoxybiphenyl-2-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000005
2-cyano-N-methyl-4-(piperidin-4-ylmethoxy)-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000003
2-cyano-N-methyl-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000003
2-cyano-N-methyl-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[4.5]dec-8-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000005
2-cyano-N-methyl-4-[(spiro[3.5]non-7-ylmethyl)amino]-6-[(2,2,6,6-tetramethylpiperidin-4-yl)oxy]pyrimidine-5-carboxamide
0.000002
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
0.000004
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
0.000003
2-cyano-N-methyl-4-[[1-(1-methylethyl)piperidin-4-yl]methoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000006
2-cyano-N-[(1-methyl-4-phenylpiperidin-4-yl)methyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000004
2-cyano-N-[(1R)-2-pyridin-2-yl-1-(pyrrolidin-1-ylmethyl)ethyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000003
2-cyano-N-[5-[(1-methylpiperidin-4-yl)oxy]biphenyl-2-yl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.00001
2-hydroxy-1-(1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)ethanone
Homo sapiens
-
-
0.00001
2-hydroxy-1-(1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)ethanone
Homo sapiens
-
-
0.00096
2-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)sulfanyl]ethanol
Homo sapiens
-
-
0.0000007
2-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-1,3-difluorobenzene
Homo sapiens
-
-
0.0000018
2-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]biphenyl
Homo sapiens
-
-
0.00001
2-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]benzonitrile
Homo sapiens
-
-
0.00006
2-[3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00007
2-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-oxoacetamide
Homo sapiens
-
-
0.0000045
2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9-(2-hydroxyethyl)-9H-purine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000072
2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9-ethyl-9H-purine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000039
2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000023
2-[4-methoxy-3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00002
2-[5-carbamoyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-1-[[4-(2-cyanophenyl)piperazin-1-yl]methyl]ethyl carbamate
Homo sapiens
-
IC50: 20 nM
0.000016
2-[N-(3-chlorophenyl)-L-leucyl]tetrahydropyridazine-1(2H)-carbonitrile
Homo sapiens
-
-
0.000013
2-[N-(4-cyanophenyl)-L-leucyl]pyrazolidine-1-carbonitrile
Homo sapiens
-
-
0.000033
2-[N-(4-cyanophenyl)-L-phenylalanyl]pyrazolidine-1-carbonitrile
Homo sapiens
-
-
0.000035
2-[N-(4-fluorophenyl)-L-valyl]tetrahydropyridazine-1(2H)-carbonitrile
Homo sapiens
-
-
0.000019
2-[N-[3-(trifluoromethyl)phenyl]-L-isoleucyl]tetrahydropyridazine-1(2H)-carbonitrile
Homo sapiens
-
-
0.00019
2-[[5-(1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00006
2-[[5-(1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
Homo sapiens
-
-
0.00011
2-[[5-(1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00006
2-[[5-(1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
Homo sapiens
-
-
0.00015
2-[[5-(5-acetyl-1-[2-hydroxy-3-[4-(2-hydroxypropan-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
Homo sapiens
-
-
0.00002
2-[[5-(5-acetyl-1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00025
2-[[5-(5-ethyl-1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
Homo sapiens
-
-
0.00018
2-[[5-[5-acetyl-1-[2-hydroxy-3-(4-methylpiperidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
Homo sapiens
-
-
0.001373
3'-[1-[[(cyanomethy)amino]carbonyl]-3-methylbutyl]-1,1'biphenyl-4-carboxamide
Homo sapiens
-
IC50: 1373 nM
0.0079
3-(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)prop-2-yn-1-ol
Homo sapiens
-
-
0.0074
3-(4-chloro-3-ethynylphenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00087
3-(4-chloro-3-[[2-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0015
3-(4-chloro-3-[[3-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00028
3-(4-chloro-3-[[4-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.000033
3-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
Homo sapiens
-
IC50: 33 nM
0.000005
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-(naphthalen-2-ylacetyl)-L-alaninamide
Homo sapiens
-
IC50: 5.0 nM
0.0000033
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-([5-[3-(trifluoromethyl)phenyl]furan-2-yl]acetyl)-L-alaninamide
Homo sapiens
-
IC50: 3.3 nM
0.000008
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(3-phenoxyphenyl)acetyl]-L-alaninamide
Homo sapiens
-
IC50: 8.0 nM
0.000004
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(4-morpholin-4-ylphenyl)acetyl]-L-alaninamide
Homo sapiens
-
IC50: 4.0 nM
0.000017
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(4-phenoxyphenyl)acetyl]-L-alaninamide
Homo sapiens
-
IC50: 17 nM
0.000034
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(5-methyl-1-phenyl-1H-pyrazol-4-yl)acetyl]-L-alaninamide
Homo sapiens
-
IC50: 34 nM
0.000026
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[[4-(1H-1,2,4-triazol-1-yl)phenyl]acetyl]-L-alaninamide
Homo sapiens
-
IC50: 26 nM
0.000197
3-cyclohexyl-N2-(5-fluoro-1,3-benzoxazol-2-yl)-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 197 nM
0.000043
3-cyclohexyl-N2-(6-fluoro-1,3-benzoxazol-2-yl)-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 43 nM
0.000002
3-cyclohexyl-N2-([4-[(4,6-dimethylpyrimidin-2-yl)amino]phenyl]acetyl)-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 2.0 nM
0.00003
3-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,5-dimethyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 30 nM
0.00165
3-[3-(benzylsulfanyl)-4-chlorophenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.000235
3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide
Homo sapiens
-
-
0.0083
3-[4-chloro-3-(4-methylpent-1-yn-1-yl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0067
3-[4-chloro-3-(cyclohexylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.011
3-[4-chloro-3-(hept-1-yn-1-yl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00061
3-[4-chloro-3-(phenylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0036
3-[4-chloro-3-(propylsulfanyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00079
3-[4-chloro-3-(thiophen-2-ylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0015
3-[4-chloro-3-(thiophen-3-ylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00072
3-[4-chloro-3-[(2-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00055
3-[4-chloro-3-[(2-methoxyphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0011
3-[4-chloro-3-[(2-methylphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0006
3-[4-chloro-3-[(2-phenoxyethyl)sulfanyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00147
3-[4-chloro-3-[(2-phenylethyl)sulfanyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00032
3-[4-chloro-3-[(3,4-dichlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0007
3-[4-chloro-3-[(3-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0002 - 0.00069
3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.00048
3-[4-chloro-3-[(4-methoxyphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00028
3-[4-chloro-3-[(4-methylphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.000007
3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]benzamide
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000447
4-(3-acetylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000174
4-(3-bromophenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000148
4-(3-chlorophenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000063
4-(3-cyclobutylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000155
4-(3-cyclopentylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0002
4-(3-cyclopropylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000083
4-(3-ethylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00095
4-(3-methylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000191
4-(3-tert-butylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000123
4-(acetylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
Homo sapiens
-
IC50: 123 nM
0.00053
4-(dimethylamino)-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
Homo sapiens
-
-
0.000016
4-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
Homo sapiens
-
IC50: 16 nM
0.00036
4-fluoro-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
Homo sapiens
-
-
0.00039
4-hydroxy-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
Homo sapiens
-
-
0.000093
4-methyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-N2-(morpholin-4-ylcarbonyl)-L-leucinamide
Rattus norvegicus
-
-
0.00022
4-methyl-N2-(morpholin-4-ylcarbonyl)-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)-L-leucinamide
Rattus norvegicus
-
-
0.01
4-phenyl-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00041
4-propyl-6-(3-propylphenyl)pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.01
4-propyl-6-[2-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000115
4-propyl-6-[3-(trifluoromethoxy)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000041
4-propyl-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000032
4-propyl-6-[4-(trifluoromethoxy)-3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.001259
4-propyl-6-[4-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00001
4-[(1-acetylpiperidin-4-yl)methoxy]-2-cyano-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00043
4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]aniline
Homo sapiens
-
-
0.00051
4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzoic acid
Homo sapiens
-
-
0.001925
4-[1-(2-hydroxy-3-[3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.00001
4-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.0018
4-[1-(3-[3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.00003
4-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.00012
4-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.0001
4-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.000826
4-[1-(3-[5-tert-butoxy-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.0009
4-[1-(3-[5-tert-butoxy-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.000022
4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.001047
4-[2-chloro-5-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000051
4-[3,5-bis(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000224
4-[3-(2-methylpropyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000093
4-[3-(methylsulfonyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000195
4-[3-(propan-2-yl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000045
4-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000058
4-[4-(propan-2-yloxy)-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000028
4-[4-chloro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000006
4-[4-ethoxy-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000013
4-[4-fluoro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000015
4-[4-methoxy-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00001
4-[4-methyl-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000013
4-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000016
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzoic acid
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000002
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]benzamide
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00074
5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-3-[3-[(2-phenoxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00081
5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.000058
5-(methylsulfonyl)-1-[3-[4-(1H-pyrrolo[3,2-c]pyridin-3-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00038
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-(piperidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00052
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-(pyrrolidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00056
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-[4-(pyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.000002
5-bromo-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.00015
5-chloro-3-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 150 nM
0.00008
5-chloro-3-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 80 nM
0.00045
6-(4-chlorobenzyl)-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000033
6-(4-chlorobenzyl)-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000021
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000099
6-(4-chlorobenzyl)-7-(2-cyclooctylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000007
6-(4-chlorobenzyl)-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000064
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000002
6-(4-chlorobenzyl)-7-(3,3-dimethylbutyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00015
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.00032
6-(4-chlorobenzyl)-7-(4,4-dimethylpentyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00011
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.00019
6-(4-chlorobenzyl)-7-[2-(3-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000019
6-(4-chlorobenzyl)-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, pyrrolopyrimidine inhibitor by modification of the P2 moieties
0.00005
6-chloro-1-(1-[3-[3-(4-chloro-3-methylphenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 50 nM
0.00006
6-chloro-1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 60 nM
0.00003
6-chloro-1-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 30 nM
0.001047
6-[3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.002884
6-[3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000071
6-[4-(2-hydroxyethoxy)-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000145
6-[4-(2-hydroxyethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000024
6-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000063
6-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000155
6-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0002
6-[4-(3-oxopropyl)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000105
6-[4-(ethylamino)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00004
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000037
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-[2-(morpholin-4-yl)ethyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000035
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-[3-(morpholin-4-yl)propyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000025
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00166
6-[4-ethoxy-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000339
6-[4-methoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000676
6-[4-phenoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000029
6-[4-[2-(2-oxopyrrolidin-1-yl)ethoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000209
6-[4-[2-(dimethylamino)ethoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000031
6-[4-[3-(2-ethyl-1H-imidazol-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000072
6-[4-[3-(4-ethylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000058
6-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000041
6-[4-[3-(dimethylamino)propoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000013
6-[[4-(1-acetyl-1,2,3,6-tetrahydropyridine-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000015
6-[[4-(1-acetylpiperidin-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000015
6-[[4-(1-acetylpiperidine-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000012 - 0.000014
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.00005
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000009 - 0.00001
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000005
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00001 - 0.000028
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000017
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000009
6-[[4-(4-acetylpiperazine-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00011
7-(2-cyclohexylethyl)-6-(4-methoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00014
7-(2-cyclohexylethyl)-6-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.00044
7-(2-cyclohexylethyl)-6-(naphthalen-1-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00001
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000024
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000011
7-(2-cyclohexylethyl)-6-[(pyridine-2-yloxy)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000006
7-(2-cyclohexylethyl)-6-[(pyridine-2-ylsulfanyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000052
7-(2-cyclohexylethyl)-6-[[methyl(phenyl)amino]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00046
7-tert-butyl-6-(4-chlorobenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000069
9-[3-(dimethylamino)propyl]-2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00004
benzyl [(2S)-1-(2-cyanotetrahydropyridazin-1(2H)-yl)-3-methyl-1-oxopentan-2-yl]carbamate
Homo sapiens
-
-
42
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
Homo sapiens
at pH 6.5 and 37°C
0.000071
ethyl (3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoate
Homo sapiens
-
IC50: 71 nM
0.0001
JNJ 10329670
Homo sapiens
-
competitive, reversible inhibition, 4-(2-keto-1-benzimidazolinyl)-piperidin-1-yl derivative, IC50: 100 nM
0.000178 - 0.002441
L-873724
0.0000005 - 0.0000017
LHVS
0.0001
methyl (2R)-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)(phenyl)ethanoate
Homo sapiens
-
-
0.01
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-4-[(1S)-1-[(1R)-2-[(1-cyanocyclopropyl)amino]-1-(methoxysulfinyl)methyl]-2-oxoethyl]amino)-2,2,2-trifluoroethyl]-4'-fluorobiphenyl
Homo sapiens
-
-
0.002173
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfenate
Homo sapiens
-
-
0.00000016 - 0.001051
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfinate
0.0000064
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(3-fluorophenyl)ethyl]amino]propane-1-sulfinate
Homo sapiens
-
-
0.000096 - 0.01
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfenate
0.0000006 - 0.000426
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfinate
0.0000025
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propane-1-sulfinate
Homo sapiens
-
-
0.00012
methyl (2S)-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)(phenyl)ethanoate
Homo sapiens
-
-
0.00004
methyl (3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(oxo)acetate
Homo sapiens
-
-
0.000005
methyl (3S)-3-[[3-cyclohexyl-N-(morpholin-4-ylcarbonyl)-L-alanyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate
Rattus norvegicus
-
-
0.0017
methyl 1-[2-hydroxy-3-(4-quinolin-4-ylpiperazin-1-yl)propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000163
methyl 1-[2-hydroxy-3-[4-(2-oxo-2,3-dihydro-4,1-benzoxazepin-1(5H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000088
methyl 1-[2-hydroxy-3-[4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000048
methyl 1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000023
methyl 1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000028
methyl 1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.00008
methyl 1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.00002
methyl 1-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidine-4-carboxylate
Homo sapiens
-
-
0.000023
methyl 1-[3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000145
methyl 1-[3-[4-(5-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.00003
methyl 1-[3-[4-(6-chloro-2,2-dioxido-3,4-dihydro-1H-2,1,3-benzothiadiazin-1-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000018
methyl 1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000013
methyl 1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000016
methyl 1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.00013
methyl 1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000043
methyl 2-[[(1S)-1-(cyclohexylmethyl)-2-([2-[(4-fluorophenyl)amino]ethyl]amino)-2-oxoethyl]amino]-1,3-benzoxazole-6-carboxylate
Homo sapiens
-
IC50: 43 nM
0.000133
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000065
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000033
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000032
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000068
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.001775
methyl 3-(4-bromophenyl)-1-[3-[4-(3,4-dihydroisoquinolin-2(1H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000322
methyl 3-(4-bromophenyl)-1-[3-[4-(3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.00006
methyl 3-(4-bromophenyl)-1-[3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.0017
methyl 3-(4-bromophenyl)-1-[3-[4-(5-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000075
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2,2-dioxido-3,4-dihydro-1H-2,1,3-benzothiadiazin-1-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000033
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000018
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000048
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.00013
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000265
methyl 4'-[(1S)-1-([(1S)-1-[(1-cyanocyclopropyl)carbamoyl]pentyl]amino)-2,2,2-trifluoroethyl]biphenyl-4-sulfinate
Homo sapiens
-
-
565
morpholine-4-carboxylic acid [1-[1S-(N-benzoyl-hydrazinomethyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
Homo sapiens
-
IC50: 565 mM
0.011
morpholine-4-carboxylic acid [1R-(1S-cyano-3-phenyl-propylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 0.011 mM
0.000387
morpholine-4-carboxylic acid [1S-(1R-cyano-3-phenylpropylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 387 nM
0.107
morpholine-4-carboxylic acid [1S-(1S-cyano-2,2-dimethylpropylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 0.107 mM
0.0014
morpholine-4-carboxylic acid [1S-(1S-cyano-2-methyl-propylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 1400 nM
0.00013
morpholine-4-carboxylic acid [1S-(1S-cyano-2-phenylethylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 130 nM
0.076
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenyl-propylcarbamoyl)-1,3-dimethyl-butyl]-amide
Homo sapiens
-
IC50: 0.076 mM
5
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-cyclohexyl-ethyl]-amide
Homo sapiens
-
IC50: 5 mM
0.006
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-methyl-propyl]-amide
Homo sapiens
-
IC50: 0.006 mM
173
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-phenyl-ethyl]-amide
Homo sapiens
-
IC50: 173 mM
0.000023
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-3,3-dimethyl-butyl]-amide
Homo sapiens
-
IC50: 23 nM
0.000084
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-cyclohexyl-R-methyl]-amide
Homo sapiens
-
IC50: 84 nM
0.134
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-ethyl]-amide
Homo sapiens
-
IC50: 0.134 mM
0.000041
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-pentyl]-amide
Homo sapiens
-
IC50: 41 nM
0.000082
morpholine-4-carboxylic acid [1S-(1S-cyanobutylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 82 nM
0.000056
morpholine-4-carboxylic acid [1S-(1S-cyanobutylcarbamoyl)-3-methylpentyl]amide
Homo sapiens
-
IC50: 56 nM
0.000142
morpholine-4-carboxylic acid [1S-(1S-cyanomethylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 142 nM
0.000019
morpholine-4-carboxylic acid [1S-(2-benzyloxy-1R-cyano-ethylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 19 nM
0.000124
morpholine-4-carboxylic acid [1S-(cyanomethylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 124 nM
0.000114
morpholine-4-carboxylic acid [1S-[(1-cyano-1-methyl)ethylcarbamoyl]-3-methylbutyl]amide
Homo sapiens
-
IC50: 114 nM
0.000051
morpholine-4-carboxylic acid [1S-[(cyano-phenyl-S-methyl)carbamoyl]-3-methylbutyl]amide
Homo sapiens
-
IC50: 51 nM
0.000011
morpholine-4-carboxylic acid [1S-[1S-(benzoyl-hydrazonomethyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
Homo sapiens
-
IC50: 11 nM
0.000056
morpholine-4-carboxylic acid [1S-[1S-cyano-2-(3,4-dichlorophenyl)ethylcarbamoyl]-3-methylbutyl]amide
Homo sapiens
-
IC50: 56 nM
0.000007
morpholine-4-carboxylic acid [1S-[1S-[(2-hydroxy-benzoyl)-hydrazonomethyl]-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
Homo sapiens
-
IC50: 7 nM
0.000035
morpholine-4-carboxylic acid [1S-[1S-[(4-hydroxybenzoyl)-hydrazonomethyl]-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
Homo sapiens
-
IC50: 35 nM
0.097
morpholine-4-carboxylic acid [3-methyl-1S-(1-prop-2-ynylcarbamoyl)butyl]amide
Homo sapiens
-
IC50: 0.097 mM
0.339
morpholine-4-carboxylic acid [3-methyl-1S-(1R-methyl-3-phenylpropylcarbamoyl)butyl]amide
Homo sapiens
-
IC50 above 0.339 mM
0.028
morpholine-4-carboxylic acid [3-methyl-1S-(3-phenyl-propylcarbamoyl)butyl]amide
Homo sapiens
-
IC50 above 0.028 mM
0.00052
N,N-dimethyl-2-([5-[5-(methylsulfonyl)-1-[3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)acetamide
Homo sapiens
-
-
0.000729
N-(1-cyanocyclopropyl)-3-(methylsulfinyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
Homo sapiens
-
-
0.00001
N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-(4'-fluorobiphenyl-4-yl)ethyl]-L-alaninamide
Homo sapiens
-
-
0.0000018
N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
Homo sapiens
-
-
0.0000025
N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-phenylethyl]-L-alaninamide
Homo sapiens
-
-
0.0000002
N-(1-cyanocyclopropyl)-3-[(3,4-dichlorophenyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
Homo sapiens
-
-
0.0000005
N-(1-cyanocyclopropyl)-3-[(4-fluorobenzyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-phenylethyl]-L-alaninamide
Homo sapiens
-
-
0.0000004
N-(1-cyanocyclopropyl)-3-[(4-fluorophenyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
Homo sapiens
-
-
0.000627
N-(1-cyanocyclopropyl)-3-[[2-(4-fluorophenyl)propan-2-yl]sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
Homo sapiens
-
-
0.000265
N-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Homo sapiens
-
-
0.000002
N-(4-benzyl-1-methylpiperidin-4-yl)-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.00014
N-(4-chlorobenzyl)-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
Homo sapiens
-
-
0.000008
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetamide
Homo sapiens
-
-
0.000008
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]phenyl)acetamide
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000012
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]phenyl)propanamide
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000922
N-(cyanomethyl)-2-[3-(1H-indol-5-yl)phenyl]-4-methylpentanamide
Homo sapiens
-
IC50: 922 nM
0.001257
N-(cyanomethyl)-2-[3-(1H-indol-6-yl)phenyl]-4-methylpentanamide
Homo sapiens
-
IC50: 1257 nM
0.01
N-(cyanomethyl)-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]-3-phenylpropanamide
Homo sapiens
-
IC50 above 0.01 mM
0.01
N-(cyanomethyl)-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]acetamide
Homo sapiens
-
IC50 above 0.01 mM
0.00231
N-(cyanomethyl)-3-cyclobutyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]propanamide
Homo sapiens
-
IC50: 2310 nM
0.006597
N-(cyanomethyl)-3-cyclopropyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]propanamide
Homo sapiens
-
IC50: 6597 nM
0.01
N-(cyanomethyl)-4-methyl-2-(2-phenyl-1,3-thiazol-4-yl)pentanamide
Homo sapiens
-
IC50 above 0.01 mM
0.01
N-(cyanomethyl)-4-methyl-2-(3'-piperazin-1-yl-1,1'-biphenyl-3-yl)pentanamide methanesulfonate
Homo sapiens
-
IC50 above 0.01 mM
0.00000001
N-(cyanomethyl)-4-methyl-2-(3-pyridin-3-ylphenyl)-pentanamide
Homo sapiens
-
IC50 above 0.01 nM
0.001748
N-(cyanomethyl)-4-methyl-2-(3-pyridin-4-ylphenyl)-pentanamide trifluoroacetate
Homo sapiens
-
IC50: 1748 nM
0.01
N-(cyanomethyl)-4-methyl-2-(3-pyrimidin-5-ylphenyl)pentanamide
Homo sapiens
-
IC50 above 0.01 mM
0.01
N-(cyanomethyl)-4-methyl-2-(5-phenylpyridin-3-yl)-pentanamide trifluoroacetate
Homo sapiens
-
IC50 above 0.01 mM
0.000521
N-(cyanomethyl)-4-methyl-2-[2'-(1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 521 nM
0.003368
N-(cyanomethyl)-4-methyl-2-[2'-(4-morpholinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 3368 nM
0.01
N-(cyanomethyl)-4-methyl-2-[3'-(4-morpholinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50 above 0.01 mM
0.000652
N-(cyanomethyl)-4-methyl-2-[4'-(1,2,3,6-tetrahydro-4-pyridinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 652 nM
0.001245
N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 1245 nM
0.001695
N-(cyanomethyl)-4-methyl-2-[4'-(4-methyl-1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 1695 nM
0.009422
N-(cyanomethyl)-4-methyl-2-[4'-(4-morpholinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 9422 nM
0.001421
N-(cyanomethyl)-4-methyl-2-[4'-(4-piperidinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 1421 nM
0.006623
N-(cyanomethyl)-4-methyl-2-[4'-(methylsulfonyl)-1,1'-biphenyl-3-yl]pentanamide
Homo sapiens
-
IC50: 6623 nM
0.0006
N-benzyl-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-methylmethanamine
Homo sapiens
-
-
0.00042
N-benzyl-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
Homo sapiens
-
-
0.00037
N-benzyl-2-([5-[5-(methylsulfonyl)-1-[3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)acetamide
Homo sapiens
-
-
0.000001
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)oxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.00115
N-methyl-2-([5-[5-(methylsulfonyl)-1-[3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)acetamide
Homo sapiens
-
-
0.000021
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylpropyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000029
N-[(1S)-1-(1H-indol-2-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 29 nM
0.000034
N-[(1S)-1-(biphenyl-4-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 34 nM
0.000062
N-[(1S)-1-(cyclohexylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 62 nM
0.000017
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-1-benzofuran-2-carboxamide
0.000034
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-(3-fluorophenyl)furan-2-carboxamide
0.000011
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-[3-(trifluoromethyl)phenyl]furan-2-carboxamide
0.000047
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-2-carboxamide
0.000006
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-3-carboxamide
0.000099
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000213
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-3-carboxamide
0.000011
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[[(1S)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]amino]ethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000011
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
0.000012
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydro-2H-pyran-4-carboxamide
0.000021
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-3-carboxamide
0.000111
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-2-(5-fluoro-2,2-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000087
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000011
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-2-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000049
N-[(1S)-1-(cyclopentylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.02
N-[(1S)-1-(furan-2-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 0.020 mM
0.000023
N-[(1S)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000023
N-[(1S)-1-cyclohexyl-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 23 nM
0.000016
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-1-(naphthalen-2-ylmethyl)-2-oxoethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 16 nM
0.065
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(1,3-thiazol-5-ylmethyl)ethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 0.065 mM
0.003707
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(pyridin-3-ylmethyl)ethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 3707 nM
0.006769
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(pyridin-4-ylmethyl)ethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 6769 nM
0.000285
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-phenylethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 285 nM
0.000012
N-[(1S)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxo-1-[(2-phenylethyl)sulfanyl]ethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000032
N-[(1S)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxo-1-[(2-phenylethyl)sulfonyl]ethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000038
N-[(1S)-3-cyclohexyl-1-([2-[(4-methoxyphenyl)amino]ethyl]carbamoyl)propyl]-3-methylbenzamide
Homo sapiens
-
IC50: 38 nM
0.0000055
N-[(2S)-1-[[(1R)-2-(benzyloxy)-1-cyanoethyl]amino]-3-cyclohexyl-1-oxopropan-2-yl]morpholine-4-carboxamide
Homo sapiens
-
pH 6.5, 37°C
0.0000044
N-[(3S)-4-benzyloxy-3-[[[1-[(4-morpholinylcarbonyl)-amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
Homo sapiens
-
pH 6.5, 37°C
0.0000019
N-[(3S)-4-benzyloxy-3-[[[2-[(3-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
Homo sapiens
-
pH 6.5, 37°C
0.00013
N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]-2-phenylacetamide
Homo sapiens
-
-
0.00038
N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
Homo sapiens
-
-
0.00042
N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]piperidine-3-carboxamide
Homo sapiens
-
-
0.000046
N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-N2-[(3-methylphenyl)carbonyl]-L-leucinamide
Homo sapiens
-
IC50: 46 nM
0.000027
N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
Homo sapiens
-
IC50: 27 nM
0.000062
N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(3-methylphenyl)carbonyl]-L-leucinamide
Homo sapiens
-
IC50: 62 nM
0.000019
N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-4-(trifluoromethyl)-L-phenylalaninamide
Homo sapiens
-
IC50: 19 nM
0.000029
N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
Homo sapiens
-
IC50: 29 nM
0.000066
N-[2-[(4-methoxyphenyl)amino]ethyl]-O-methyl-Na-[(3-methylphenyl)carbonyl]-L-tyrosinamide
Homo sapiens
-
IC50: 66 nM
0.003236
N-[4-(4-cyano-1H-imidazo[4,5-c]pyridin-6-yl)-2-(trifluoromethyl)phenyl]formamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00019
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]-1-phenylethanamine
Homo sapiens
-
-
0.00058
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]-2-phenylethanamine
Homo sapiens
-
-
0.00035
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]benzamide
Homo sapiens
-
-
0.00016
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]benzenesulfonamide
Homo sapiens
-
-
0.000173
N2-(5-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 173 nM
0.000021
N2-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[(1S)-1-[(5-fluoro-2,3-dihydro-1H-indol-1-yl)methyl]-3-(methylsulfonyl)propyl]-L-alaninamide
Homo sapiens
-
IC50: 21 nM
0.000151
N2-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[(1S)-2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
Homo sapiens
-
IC50: 151 nM
0.000093
N2-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 93 nM
0.000026
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-(1-methyl-2-[[3-(methylsulfonyl)phenyl]amino]ethyl)-L-alaninamide
Homo sapiens
-
IC50: 26 nM
0.000011
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-(1-methyl-2-[[4-(methylsulfonyl)phenyl]amino]ethyl)-L-alaninamide
Homo sapiens
-
IC50: 11 nM
0.000015
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-2,2-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
Homo sapiens
-
IC50: 15 nM
0.000015
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
Homo sapiens
-
IC50: 15 nM
0.0000123
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-2-oxo-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
Homo sapiens
-
IC50: 12.3 nM
0.000003
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
Homo sapiens
-
IC50: 3 nM
0.000019
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 19 nM
0.000001
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]-1-methylethyl]-L-alaninamide
Homo sapiens
-
IC50: 1 nM
0.0000029
N2-(biphenyl-3-ylacetyl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 2.9 nM
0.0000091
N2-(biphenyl-4-ylacetyl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 9.1 nM
0.000026
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[(1S)-2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
Homo sapiens
-
IC50: 26 nM
0.000222
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)ethyl]-L-alaninamide
Homo sapiens
-
IC50: 222 nM
0.000094
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 94 nM
0.000029
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 29 nM
0.000005
N2-1,3-benzoxazol-2-yl-N-[(1R)-2-(benzyloxy)-1-[(5-fluoro-2,3-dihydro-1H-indol-1-yl)methyl]ethyl]-3-cyclohexyl-L-alaninamide
Homo sapiens
-
IC50: 5 nM
0.000041
N2-benzoyl-N1-(cyanomethyl)-L-leucinamide
Homo sapiens
-
IC50: 41 nM
0.0000074
N2-[(3'-chlorobiphenyl-4-yl)acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 7.4 nM
0.0000094
N2-[(5-chloro-1-benzofuran-2-yl)acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 9.4 nM
0.000049
N2-[[1-(5-bromopyrimidin-2-yl)piperidin-3-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 49 nM
0.000107
N2-[[1-(5-bromopyrimidin-2-yl)piperidin-4-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 107 nM
0.0000071
N2-[[5-(4-chlorophenyl)furan-2-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 7.1 nM
0.0114
Na-(morpholin-4-ylcarbonyl)-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)-L-phenylalaninamide
Rattus norvegicus
-
-
0.000021
paecilopeptin
Homo sapiens
-
i.e. acetyl-Leu-Val-CHO, IC50: 21 nM
0.00073
tert-butyl (3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoate
Homo sapiens
-
IC50: 730 nM
0.00001
tert-butyl 1'-[(2S)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]-4,4'-bipiperidine-1-carboxylate
Homo sapiens
-
-
0.001298
tert-butyl 4-[3'-[1-[[(cyanomethyl)amino]carbonyl]-3-methylbutyl]-1,1'-biphenyl-4-yl]piperazine-1-carboxylate
Homo sapiens
-
IC50: 1298 nM
0.00015
tert-butyl 4-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperazine-1-carboxylate
Homo sapiens
-
-
0.000004
tert-butyl [(2S)-1-(2-cyanopyrazolidin-1-yl)-1-oxo-3-phenylpropan-2-yl]carbamate
Homo sapiens
-
-
0.000023
tert-butyl [(2S)-1-(2-cyanopyrazolidin-1-yl)-3-methyl-1-oxobutan-2-yl]carbamate
Homo sapiens
-
-
0.000003
tert-butyl [(2S)-1-(2-cyanopyrazolidin-1-yl)-4-methyl-1-oxopentan-2-yl]carbamate
Homo sapiens
-
-
0.000004
tert-butyl [(2S)-1-(2-cyanotetrahydropyridazin-1(2H)-yl)-3-methyl-1-oxobutan-2-yl]carbamate
Homo sapiens
-
-
0.000012
tetrahydro-2H-pyran-4-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
0.000042 - 0.000049
tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
0.0000006
[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]benzene
Homo sapiens
-
-
0.00009
[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl](pyrrolidin-1-yl)methanone
Homo sapiens
-
-
0.000042
[1S-(1S-cyano-3-phenylpropylcarbamoyl)-3-methylbutyl]-amide
Homo sapiens
-
IC50: 42 nM
0.02
[1S-(2-cyano-1S-phenethyl-ethylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50 above 0.02 mM
0.000205
[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl](1H-1,2,4-triazol-3-yl)methanone
Homo sapiens
-
-
0.00119
[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl](pyrrolidin-1-yl)methanone
Homo sapiens
-
-
0.000355
[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl](thiophen-2-yl)methanone
Homo sapiens
-
-
additional information
(2R)-N-(1-benzyl-4-cyanopiperidin-4-yl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
0.000018
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
Homo sapiens
-
IC50: 18 nM
0.000053
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
Rattus norvegicus
-
-
0.000018
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
Rattus norvegicus
-
-
0.000053
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
Homo sapiens
-
IC50: 53 nM
0.0000002
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Homo sapiens
-
-
0.0000002
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Mus musculus
-
IC50 less than 0.2 mM
0.000015
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Rattus norvegicus
-
IC50 less than 0.2 mM
0.0000002
1-bromo-3-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Homo sapiens
-
-
0.0000002
1-bromo-3-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Mus musculus
-
IC50 less than 0.2 mM
0.000044
1-bromo-3-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Rattus norvegicus
-
IC50 less than 0.2 mM
0.0000002
1-bromo-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Mus musculus
-
-
0.0000003
1-bromo-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Homo sapiens
-
-
0.000066
1-bromo-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Rattus norvegicus
-
-
0.0000005
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
Homo sapiens
-
-
0.0000009
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
Mus musculus
-
-
0.000759
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
Rattus norvegicus
-
-
0.0000003
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
Homo sapiens
-
-
0.0000008
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
Mus musculus
-
-
0.000021
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
Rattus norvegicus
-
-
0.000006
2-cyano-4-(2-hydroxyethoxy)-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000006
2-cyano-4-(2-hydroxyethoxy)-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00013
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
-
-
0.00013
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000014
2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000014
2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000022
2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000022
2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000015
2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000015
2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000005
2-cyano-N-methyl-4-[(spiro[3.5]non-7-ylmethyl)amino]-6-[(2,2,6,6-tetramethylpiperidin-4-yl)oxy]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000005
2-cyano-N-methyl-4-[(spiro[3.5]non-7-ylmethyl)amino]-6-[(2,2,6,6-tetramethylpiperidin-4-yl)oxy]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000002
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000002
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000002
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000004
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000004
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.0002
3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00069
3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Mus musculus
-
-
0.000021
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000021
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000064
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000064
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00015
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00015
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00011
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00011
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000012
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
rat Cat S, Z-Leu-Leu-Arg-7-amido-4-methylcumarin as substrate
0.000014
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Mus musculus
-
mus Cat S, Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as substrate
0.000009
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00001
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Mus musculus
-
mus Cat S, Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as substrate
0.00001
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
rat Cat S, Z-Leu-Leu-Arg-7-amido-4-methylcumarin as substrate
0.00001
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00002
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Mus musculus
-
mus Cat S, Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as substrate
0.000028
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
rat Cat S, Z-Leu-Leu-Arg-7-amido-4-methylcumarin as substrate
0.00014
7-(2-cyclohexylethyl)-6-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00014
7-(2-cyclohexylethyl)-6-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00001
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00001
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000024
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000024
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000178
L-873724
Homo sapiens
-
-
0.000254
L-873724
Mus musculus
-
-
0.002441
L-873724
Rattus norvegicus
-
-
0.0000005
LHVS
Mus musculus
-
-
0.0000012
LHVS
Homo sapiens
-
-
0.0000017
LHVS
Rattus norvegicus
-
-
0.00000016
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfinate
Mus musculus
-
-
0.000011
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfinate
Homo sapiens
-
-
0.001051
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfinate
Rattus norvegicus
-
-
0.000096
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfenate
Mus musculus
-
-
0.000729
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfenate
Homo sapiens
-
-
0.01
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfenate
Rattus norvegicus
-
IC50 above 0.01 mM
0.0000006
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfinate
Mus musculus
-
-
0.0000018
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfinate
Homo sapiens
-
-
0.000426
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfinate
Rattus norvegicus
-
-
0.000017
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-1-benzofuran-2-carboxamide
Rattus norvegicus
-
-
0.000017
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-1-benzofuran-2-carboxamide
Homo sapiens
-
IC50: 17 nM
0.000034
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-(3-fluorophenyl)furan-2-carboxamide
Rattus norvegicus
-
-
0.000034
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-(3-fluorophenyl)furan-2-carboxamide
Homo sapiens
-
IC50: 34 nM
0.000011
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-[3-(trifluoromethyl)phenyl]furan-2-carboxamide
Rattus norvegicus
-
-
0.000011
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-[3-(trifluoromethyl)phenyl]furan-2-carboxamide
Homo sapiens
-
IC50: 11 nM
0.000047
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-2-carboxamide
Rattus norvegicus
-
-
0.000047
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-2-carboxamide
Homo sapiens
-
IC50: 47 nM
0.000006
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-3-carboxamide
Rattus norvegicus
-
-
0.000006
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-3-carboxamide
Homo sapiens
-
IC50: 6 nM
0.000213
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-3-carboxamide
Rattus norvegicus
-
-
0.000213
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-3-carboxamide
Homo sapiens
-
IC50: 213 nM
0.000011
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000011
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
Homo sapiens
-
IC50: 11 nM
0.000012
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydro-2H-pyran-4-carboxamide
Rattus norvegicus
-
-
0.000012
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydro-2H-pyran-4-carboxamide
Homo sapiens
-
IC50: 12 nM
0.000021
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-3-carboxamide
Rattus norvegicus
-
-
0.000021
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-3-carboxamide
Homo sapiens
-
IC50: 21 nM
0.000012
tetrahydro-2H-pyran-4-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
Rattus norvegicus
-
-
0.000012
tetrahydro-2H-pyran-4-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
Homo sapiens
-
IC50: 12 nM
0.000042
tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
Rattus norvegicus
-
-
0.000049
tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
Rattus norvegicus
-
-
additional information
(2R)-N-(1-benzyl-4-cyanopiperidin-4-yl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 207 - 347 nM
additional information
(2R)-N-(1-cyanocyclopropyl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 135 - 154 nM
additional information
(2R)-N-(4-cyano-1-methylpiperidin-4-yl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 251 - 641 nM
additional information
(2R)-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 37 - 63 nM
additional information
(2R)-N-[(3R)-3-cyano-1-(propan-2-yl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 66 - 82 nM
additional information
(2R)-N-[(3R)-3-cyano-1-cycloheptylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 23 - 35 nM
additional information
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 23 - 49 nM
additional information
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(1-methylcyclohexyl)methyl]-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 47 - 62 nM
additional information
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(4-methylcyclohexyl)methyl]-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 14 - 17 nM
additional information
(2R)-N-[(3R)-3-cyano-1-cyclopentylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 75 -78 nM
additional information
(2R)-N-[(3R)-3-cyano-1-methylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 155 - 172 nM
additional information
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methylpyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
Homo sapiens
-
IC50 above 20 microM, effect of R1 substituent on the Ii p10 cell assay at 37°C
additional information
2-cyano-4-[(6,8-dioxaspiro[3.5]non-7-ylmethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
Homo sapiens
IC50 is above 0.001 mM, determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 is below 0.001 M, inhibition is determined by a fluorometric assay with recombinant Cat S
additional information
2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
-
IC50: below 1 nM
additional information
6-(4-chlorobenzyl)-7-(2-piperidine-1-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
rat mutant G137C Cat S, IC50 is above 0.01 mM, Z-Leu-Leu-Arg-7-amido-4-methylcumarin as substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
rat mutant G137C Cat S, IC50 is above 0.01 mM, Z-Leu-Leu-Arg-7-amido-4-methylcumarin as substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
rat mutant G137C Cat S, IC50 is above 0.01 mM, Z-Leu-Leu-Arg-7-amido-4-methylcumarin as substrate
additional information
Chlorella powder
Homo sapiens
-
chlorella powder inhibits peptidase cathepsin S in a dose-concentration manner with 50% inhibitory concentration of 3.46 mg/l
-
additional information
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 is below 0.001 M, inhibition is determined by a fluorometric assay with recombinant Cat S
additional information
N-benzyl-2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 is below 0.001 M, inhibition is determined by a fluorometric assay with recombinant Cat S
additional information
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 is below 0.001 M, inhibition is determined by a fluorometric assay with recombinant Cat S
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