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(1E)-1-[(2E,6E,10E)-12-azido-3,7,11-trimethyldodeca-2,6,10-trien-1-ylidene]-2-oxodiphosphane + protein-cysteine
?
-
-
-
-
?
(2E,6E)-3,7-dimethyl-8-(2,3,5,6-tetrafluorophenoxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(2,3,5,6-tetrafluorophenoxy)-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-3,7-dimethyl-8-(phenylamino)octa-2,6-dien-1-yl diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-3,7-dimethyl-8-(phenylamino)octa-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-3,7-dimethyl-8-(phenylsulfanyl)octa-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-3,7-dimethyl-8-(phenylsulfanyl)octa-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-3,7-dimethyl-8-(prop-2-yn-1-yloxy)octa-2,6-dien-1-yl diphosphate + CCIQ
?
-
-
-
?
(2E,6E)-3,7-dimethyl-8-(prop-2-yn-1-yloxy)octa-2,6-dien-1-yl diphosphate + CGGDD
?
-
-
-
?
(2E,6E)-3,7-dimethyl-8-(prop-2-yn-1-yloxy)octa-2,6-dien-1-yl diphosphate + CSVL
?
-
-
-
?
(2E,6E)-3,7-dimethyl-8-(prop-2-yn-1-yloxy)octa-2,6-dien-1-yl diphosphate + CTIQ
?
-
-
-
?
(2E,6E)-3,7-dimethyl-8-(prop-2-yn-1-yloxy)octa-2,6-dien-1-yl diphosphate + CVIS
?
-
-
-
?
(2E,6E)-3,7-dimethyl-8-(prop-2-yn-1-yloxy)octa-2,6-dien-1-yl diphosphate + CVLL
?
-
-
-
?
(2E,6E)-3,7-dimethyl-8-(prop-2-yn-1-yloxy)octa-2,6-dien-1-yl diphosphate + CVLS
?
-
-
-
?
(2E,6E)-3,7-dimethyl-8-phenoxyocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-3,7-dimethyl-8-phenoxyocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-3,7-dimethyl-8-[(2-methylphenyl)amino]octa-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-3,7-dimethyl-8-[(2-methylphenyl)amino]octa-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-3,7-dimethyl-8-[(3,4,5-trimethoxybenzyl)oxy]octa-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-3,7-dimethyl-8-[(3,4,5-trimethoxybenzyl)oxy]octa-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-3,7-dimethyl-8-[(3-methylphenyl)amino]octa-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-3,7-dimethyl-8-[(3-methylphenyl)amino]octa-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-3,7-dimethyl-8-[(4-methylphenyl)amino]octa-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-3,7-dimethyl-8-[(4-methylphenyl)amino]octa-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-3,7-dimethyl-8-[(4-nitrophenyl)amino]octa-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-3,7-dimethyl-8-[(4-nitrophenyl)amino]octa-2,6-dien-1-y)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-3,7-dimethyl-8-[3-(1-methylethyl)phenoxy]octa-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-3,7-dimethyl-8-[3-(1-methylethyl)phenoxy]octa-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-3,7-dimethyl-8-[3-(trifluoromethoxy)phenoxy]octa-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-3,7-dimethyl-8-[3-(trifluoromethoxy)phenoxy]octa-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-3,7-dimethyl-8-[3-(trifluoromethyl)phenoxy]octa-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-3,7-dimethyl-8-[3-(trifluoromethyl)phenoxy]octa-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-3,7-dimethyl-8-[4-(1-methylethyl)phenoxy]octa-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-3,7-dimethyl-8-[4-(1-methylethyl)phenoxy]octa-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-3,7-dimethyl-8-[4-(trifluoromethoxy)phenoxy]octa-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-3,7-dimethyl-8-[4-(trifluoromethoxy)phenoxy]octa-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-3,7-dimethyl-8-[[2-(trifluoromethyl)phenyl]amino]octa-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-3,7-dimethyl-8-[[2-(trifluoromethyl)phenyl]amino]octa-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-3,7-dimethyl-8-[[3-(trifluoromethoxy)phenyl]amino]octa-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-3,7-dimethyl-8-[[3-(trifluoromethoxy)phenyl]amino]octa-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-3,7-dimethyl-8-[[4-(trifluoromethoxy)phenyl]amino]octa-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-3,7-dimethyl-8-[[4-(trifluoromethoxy)phenyl]amino]octa-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-3,7-dimethyl-9-phenylnona-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-3,7-dimethyl-9-phenylnona-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(2,3-difluorophenoxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(2,3-difluorophenoxy)-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(2,6-difluorophenoxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(2,6-difluorophenoxy)-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(2-bromophenoxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(2-bromophenoxy)-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(2-ethylphenoxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(2-ethylphenoxy)-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(2-fluorophenoxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(2-fluorophenoxy)-3,7-dimethylocta-2,6-dien-1-yll)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(2-iodophenoxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(2-iodophenoxy)-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(3,4-dichlorophenoxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(3,4-dichlorophenoxy)-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(3,4-difluorophenoxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(3,4-difluorophenoxy)-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(3,5-dichlorophenoxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(3,5-dichlorophenoxy)-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(3,5-difluorophenoxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(3,5-difluorophenoxy)-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(3-bromophenoxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(3-bromophenoxy)-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(3-cyanophenoxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(3-cyanophenoxy)-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(3-ethylphenoxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(3-ethylphenoxy)-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(3-fluorophenoxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(3-fluorophenoxy)-3,7-dimethylocta-2,6-dien-1-yll)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(3-iodophenoxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(3-iodophenoxy)-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(4-benzylphenoxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(4-benzylphenoxy)-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(4-bromophenoxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(4-bromophenoxy)-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(4-cyanophenoxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(4-cyanophenoxy)-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(4-ethylphenoxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(4-ethylphenoxy)-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(4-fluorophenoxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(4-fluorophenoxy)-3,7-dimethylocta-2,6-dien-1-yll)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(4-iodophenoxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(4-iodophenoxy)-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(4-nitrophenoxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(4-nitrophenoxy)-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(benzyloxy)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(benzyloxy)-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-(isoxazol-3-ylamino)-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-(isoxazol-3-ylamino)-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-[(2-ethylphenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-[(2-ethylphenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-[(2-fluorophenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-[(2-fluorophenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-[(2-methoxyphenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-[(2-methoxyphenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-[(3-bromophenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-[(3-bromophenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-[(3-cyanophenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-[(3-cyanophenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-[(3-ethylphenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-[(3-ethylphenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-[(3-fluorophenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-[(3-fluorophenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-[(3-iodophenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-[(3-iodophenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-[(3-methoxyphenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-[(3-methoxyphenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-[(4-bromophenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-[(4-bromophenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-[(4-cyanophenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-[(4-cyanophenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-[(4-fluorophenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-[(4-fluorophenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-[(4-iodophenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-[(4-iodophenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-[(4-methoxyphenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-[(4-methoxyphenyl)amino]-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-[3-(hydroxymethyl)phenoxy]-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-[3-(hydroxymethyl)phenoxy]-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-8-[4-(hydroxymethyl)phenoxy]-3,7-dimethylocta-2,6-dien-1-yl trihydrogen diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-8-[4-(hydroxymethyl)phenoxy]-3,7-dimethylocta-2,6-dien-1-yl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-farnesyl diphosphate + (protein)-L-cysteine
S-(2E,6E)-farnesyl protein + diphosphate
(2E,6E)-farnesyl diphosphate + CCIQ
S-(2E,6E)-farnesyl-CCIQ + diphosphate
-
-
-
?
(2E,6E)-farnesyl diphosphate + CGGDD
S-(2E,6E)-farnesyl-CGGDD + diphosphate
-
-
-
?
(2E,6E)-farnesyl diphosphate + CSVL
S-(2E,6E)-farnesyl-CSVL + diphosphate
-
-
-
?
(2E,6E)-farnesyl diphosphate + CTIQ
S-(2E,6E)-farnesyl-CTIQ + diphosphate
-
-
-
?
(2E,6E)-farnesyl diphosphate + CVIS
S-(2E,6E)-farnesyl-CVIS + diphosphate
-
-
-
?
(2E,6E)-farnesyl diphosphate + CVLL
S-(2E,6E)-farnesyl-CVLL + diphosphate
-
-
-
?
(2E,6E)-farnesyl diphosphate + CVLS
S-(2E,6E)-farnesyl-CVLS + diphosphate
-
-
-
?
(2E,6E)-farnesyl diphosphate + dansyl-CGVLS
dansyl-G-(S-(2E,6E)-farnesyl)CVLS
-
assay at pH 7.5, 37°C
-
-
?
(2E,6E)-farnesyl diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-farnesyl)CVLS + diphosphate
(2E,6E)-farnesyl diphosphate + K Ras-cysteine
S-(2E,6E)-farnesyl-[K Ras]-L-cysteine + diphosphate
-
-
-
?
(2E,6E)-farnesyl diphosphate + KGCVIM
S-(2E,6E)-farnesyl-KGCVIM + diphosphate
-
-
-
-
?
(2E,6E)-farnesyl diphosphate + KGCVVM
S-(2E,6E)-farnesyl-KGCVVM + diphosphate
-
-
-
-
?
(2E,6E)-farnesyl diphosphate + [H Ras]-L-cysteine
S-(2E,6E)-farnesyl-[H Ras]-L-cysteine + diphosphate
(2E,6E)-farnesyl diphosphate + [K Ras]-L-cysteine
S-(2E,6E)-farnesyl-[K Ras]-L-cysteine + diphosphate
(2E,6E)-farnesyl diphosphate + [N Ras]-L-cysteine
S-(2E,6E)-farnesyl-[N Ras]-L-cysteine + diphosphate
(2E,6E)-farnesyl diphosphate + [protein]-L-cysteine
S-(2E,6E)-farnesyl-[protein]-L-cysteine + diphosphate
(2E,6E)-farnesyl diphosphate + [protein]-L-cysteine
[protein]-S-((2E,6E)-farnesyl)-L-cysteine + diphosphate
-
assay at pH 7.5, 30°C
-
-
?
(2E,6E)-farnesyl diphosphate + [Rho]-L-cysteine
S-(2E,6E)-farnesyl-[Rho]-L-cysteine + diphosphate
(2E,6E,10E)-3,7,11-trimethyl-12-(prop-2-yn-1-yloxy)dodeca-2,6,10-trien-1-yl diphosphate + CCIQ
?
-
-
-
?
(2E,6E,10E)-3,7,11-trimethyl-12-(prop-2-yn-1-yloxy)dodeca-2,6,10-trien-1-yl diphosphate + CGGDD
?
-
-
-
?
(2E,6E,10E)-3,7,11-trimethyl-12-(prop-2-yn-1-yloxy)dodeca-2,6,10-trien-1-yl diphosphate + CSVL
?
-
-
-
?
(2E,6E,10E)-3,7,11-trimethyl-12-(prop-2-yn-1-yloxy)dodeca-2,6,10-trien-1-yl diphosphate + CTIQ
?
-
-
-
?
(2E,6E,10E)-3,7,11-trimethyl-12-(prop-2-yn-1-yloxy)dodeca-2,6,10-trien-1-yl diphosphate + CVIS
?
-
-
-
?
(2E,6E,10E)-3,7,11-trimethyl-12-(prop-2-yn-1-yloxy)dodeca-2,6,10-trien-1-yl diphosphate + CVLL
?
-
-
-
?
(2E,6E,10E)-3,7,11-trimethyl-12-(prop-2-yn-1-yloxy)dodeca-2,6,10-trien-1-yl diphosphate + CVLS
?
-
-
-
?
(2E,6Z)-3,11-dimethyl-7-(prop-2-yn-1-yl)dodeca-2,6,10-trien-1-yl diphosphate + CCIQ
?
-
-
-
?
(2E,6Z)-3,11-dimethyl-7-(prop-2-yn-1-yl)dodeca-2,6,10-trien-1-yl diphosphate + CGGDD
?
-
-
-
?
(2E,6Z)-3,11-dimethyl-7-(prop-2-yn-1-yl)dodeca-2,6,10-trien-1-yl diphosphate + CSVL
?
-
-
-
?
(2E,6Z)-3,11-dimethyl-7-(prop-2-yn-1-yl)dodeca-2,6,10-trien-1-yl diphosphate + CTIQ
?
-
-
-
?
(2E,6Z)-3,11-dimethyl-7-(prop-2-yn-1-yl)dodeca-2,6,10-trien-1-yl diphosphate + CVIS
?
-
-
-
?
(2E,6Z)-3,11-dimethyl-7-(prop-2-yn-1-yl)dodeca-2,6,10-trien-1-yl diphosphate + CVLL
?
-
-
-
?
(2E,6Z)-3,11-dimethyl-7-(prop-2-yn-1-yl)dodeca-2,6,10-trien-1-yl diphosphate + CVLS
?
-
-
-
?
(2E,6Z)-7-(but-3-yn-1-yl)-3,11-dimethyldodeca-2,6,10-trien-1-yl diphosphate + CCIQ
?
-
-
-
?
(2E,6Z)-7-(but-3-yn-1-yl)-3,11-dimethyldodeca-2,6,10-trien-1-yl diphosphate + CGGDD
?
-
-
-
?
(2E,6Z)-7-(but-3-yn-1-yl)-3,11-dimethyldodeca-2,6,10-trien-1-yl diphosphate + CSVL
?
-
-
-
?
(2E,6Z)-7-(but-3-yn-1-yl)-3,11-dimethyldodeca-2,6,10-trien-1-yl diphosphate + CTIQ
?
-
-
-
?
(2E,6Z)-7-(but-3-yn-1-yl)-3,11-dimethyldodeca-2,6,10-trien-1-yl diphosphate + CVIS
?
-
-
-
?
(2E,6Z)-7-(but-3-yn-1-yl)-3,11-dimethyldodeca-2,6,10-trien-1-yl diphosphate + CVLL
?
-
-
-
?
(2E,6Z)-7-(but-3-yn-1-yl)-3,11-dimethyldodeca-2,6,10-trien-1-yl diphosphate + CVLS
?
-
-
-
?
(2Z)-geranylgeranyl diphosphate + protein cysteine
diphosphate + S-(2Z)-geranylgeranylcysteinyl protein
-
-
-
-
?
10-benzyloxy-3-methyl-2-decen-1-ol-diphosphate + N-dansyl-Gly-Cys-Val-Leu-Ser
diphosphate + N-dansyl-Gly-S-(10-benzyloxy-3-methyl-2-decenyl)-Cys-Val-Leu-Ser
-
-
-
-
?
12-propargoxyfarnesyl diphosphate + N-dansyl-Gly-Cys-Val-Ile-Ala-OH
diphosphate + propargoxyfarnesyl N-dansyl-Gly-Cys-Val-Ile-Ala-OH
-
-
-
-
?
3-(3-methyl-2-butenyl)-7,11-dimethyldodeca-2(Z),6(E),10-triene 1-diphosphate + dansyl-Gly-Cys-Lys-Thr-Gln
? + diphosphate
-
-
-
-
?
3-(3-methyl-2-butenyl)-7,11-dimethyldodeca-2(Z),6(E),10-triene 1-diphosphate + dansyl-Gly-Cys-Lys-Val-Leu
? + diphosphate
-
-
-
-
?
3-(3-methyl-2-butenyl)-7,11-dimethyldodeca-2(Z),6(E),10-triene 1-diphosphate + dansyl-Gly-Cys-Val-Ile-Met
? + diphosphate
-
-
-
-
?
3-(3-methyl-2-butenyl)-7,11-dimethyldodeca-2(Z),6(E),10-triene 1-diphosphate + dansyl-Gly-Cys-Val-Leu-Ser
? + diphosphate
-
-
-
-
?
3-(azidomethyl)-N-[(2E,6E,8E)-2,6-dimethyl-8-(oxodiphosphanylidene)octa-2,6-dien-1-yl]aniline + protein-cysteine
?
-
-
-
-
?
3-(azidomethyl)-N-[(4E,8E,10E)-4,8-dimethyl-10-(oxodiphosphanylidene)deca-4,8-dien-1-yl]aniline + protein-cysteine
?
-
-
-
-
?
6-benzyloxy-3-methyl-2-hexen-1-ol-diphosphate + N-dansyl-Gly-Cys-Val-Leu-Ser
diphosphate + N-dansyl-Gly-S-(6-benzyloxy-3-methyl-2-hexenyl)-Cys-Val-Leu-Ser
-
-
-
-
?
7-benzyloxy-3-methyl-2-hepten-1-ol-diphosphate + N-dansyl-Gly-Cys-Val-Leu-Ser
diphosphate + N-dansyl-Gly-S-(7-benzyloxy-3-methyl-2-heptenyl)-Cys-Val-Leu-Ser
-
-
-
-
?
8-benzyloxy-3-methyl-2-octen-1-ol-diphosphate + N-dansyl-Gly-Cys-Val-Leu-Ser
diphosphate + N-dansyl-Gly-S-(8-benzyloxy-3-methyl-2-octenyl)-Cys-Val-Leu-Ser
-
-
-
-
?
9-benzyloxy-3-methyl-2-nonen-1-ol-diphosphate + N-dansyl-Gly-Cys-Val-Leu-Ser
diphosphate + N-dansyl-Gly-S-(9-benzyloxy-3-methyl-2-nonenyl)-Cys-Val-Leu-Ser
-
-
-
-
?
AAA-GPP + N-dansyl-GCVLS
?
-
-
-
-
?
APO-GPP + N-dansyl-GCVLS
?
-
-
-
-
?
CALQ + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CALQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CALV + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CALV + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CAVQ + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CAVQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CCIF + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CCIF + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CCIL + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CCIL + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CDVK + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CDVK + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CEIQ + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CEIQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CFLS + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CFLS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CFPS + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CFPS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CFTN + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CFTN + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CFVN + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CFVN + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CGIA + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CGIA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CGIM + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CGIM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CGLF + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CGLF + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CGLY + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CGLY + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CGVV + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CGVV + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CHIM + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CHIM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CHIQ + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CHIQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CHLM + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CHLM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CHLS + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CHLS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CHVM + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CHVM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CHVQ + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CHVQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CIVA + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CIVA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CKIF + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CKIF + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CKIS + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CKIS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CKIV + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CKIV + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CLIT + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CLIT + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CLLM + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CLLM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CLLV + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CLLV + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CLML + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CLML + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CLTS + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CLTS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CLVM + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CLVM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CNIM + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CNIM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CNLF + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CNLF + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CNLK + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CNLK + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CNLM + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CNLM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CNLQ + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CNLQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CQTA + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CQTA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CRIS + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CRIS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CSFM + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CSFM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CSIM + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CSIM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CSIS + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CSIS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CSLA + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CSLA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CSLC + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CSLC + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CSLG + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CSLG + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CSLH + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CSLH + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CSLM + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CSLM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CSVQ + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CSVQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CSVS + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CSVS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CTII + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CTII + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CTIV + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CTIV + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CTKF + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CTKF + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CTLA + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CTLA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CTLM + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CTLM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CTLQ + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CTLQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CTMS + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CTMS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CTTQ + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CTTQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CTVF + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CTVF + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CTVS + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CTVS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CTVV + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CTVV + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CVHF + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CVHF + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CVLA + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CVLA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CVLH + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CVLH + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CVLQ + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CVLQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CVQM + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CVQM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CVVT + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CVVT + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CYIS + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CYIS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CYLA + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CYLA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CYPD + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CYPD + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
CYVM + (2E,6E)-farnesyl diphosphate
S-(2E,6E)-farnesyl-CYVM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVAA + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVAA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVAM + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVAM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVAQ + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVAQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVAS + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVAS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVCA + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVCA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVCM + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVCM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVCQ + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVCQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVCS + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVCS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVDA + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVDA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVDM + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVDM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVDQ + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVDQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVDS + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVDS + diphosphate
dansyl-GCVEA + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVEA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVEM + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVEM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVEQ + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVEQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVES + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVES + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVFA + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVFA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVFM + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVFM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVFQ + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVFQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVFS + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVFS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVGA + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVGA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVGM + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVGM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVGQ + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVGQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVGS + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVGS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVHA + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVHA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVHM + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVHM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVHQ + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVHQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVHS + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVHS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVIA + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVIA + diphosphate
dansyl-GCVIA + 1-(4,5-dimethoxy-nitrophenyl)ethyl (2E,6E)-farnesyl diphosphate
?
-
7.6% enzyme activity, specific activity 0.058 microM/min
-
-
?
dansyl-GCVIA + 2-nitrophenyl (2E,6E)-farnesyl diphosphate
?
-
14% enzyme activity, specific activity 0.104 microM/min
-
-
?
dansyl-GCVIM + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVIM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVIQ + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVIQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVIS + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVIS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVKA + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVKA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVKLQ + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVLQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVKM + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVKM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVKQ + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVKQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVKS + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVKS + diphosphate
dansyl-GCVLA + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVLA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVLM + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVLM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVLS + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVLS + diphosphate
dansyl-GCVLS + (E)-[4-[(3,7-dimethylocta-2,6-dien-1-yl)oxy]phenyl]-methanyl diphosphate
dansyl-G-(S-(E)-[4-[(3,7-dimethylocta-2,6-dien-1-yl)oxy]phenyl]-methanyl)CVLS + diphosphate
-
-
-
-
?
dansyl-GCVLS + [3-[(3-phenoxyphenoxy)methyl]phenyl]-methanyl diphosphate
dansyl-G-(S-[3-[(3-phenoxyphenoxy)methyl]phenyl]-methanyl)CVLS + diphosphate
-
-
-
-
?
dansyl-GCVMA + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVMA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVMM + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVMM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVMQ + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVMQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVMS + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVMS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVNA + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVNA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVNM + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVNM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVNQ + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVNQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVNS + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVNS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVPA + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVPA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVPM + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVPM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVPQ + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVPQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVPS + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVPS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVQA + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVQA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVQM + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVQM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVQQ + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVQQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVQs + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVQS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVSA + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVSA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVSM + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVSM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVSQ + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVSQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVSS + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVSS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVTA + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVTA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVTM + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVTM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVTQ + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVTQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVTS + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVTS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVVA + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVVA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVVM + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVVM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVVQ + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVVQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVVS + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVVS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVWA + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVWA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVWM + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVWM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVWQ + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVWQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVWS + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVWS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVYA + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVYA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVYM + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVYM + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVYQ + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVYQ + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVYS + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVYS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
decadienyl azide diphosphate + protein-cysteine
?
-
-
-
-
?
farnesyl diphosphate + biotin-YRASNRSCAIM
diphosphate + biotin-YRASNRS-(S-farnesyl)CAIM
farnesyl diphosphate + dansyl-GCEV
diphosphate + farnesyl dansyl-GCEV
-
-
-
?
farnesyl diphosphate + dansyl-GCFT
diphosphate + farnesyl dansyl-GCFT
-
-
-
?
farnesyl diphosphate + dansyl-GCII
diphosphate + farnesyl dansyl-GCII
-
-
-
?
farnesyl diphosphate + dansyl-GCLL
diphosphate + farnesyl dansyl-GCLL
-
-
-
?
farnesyl diphosphate + dansyl-GCNV
diphosphate + farnesyl dansyl-GCNV
-
-
-
?
farnesyl diphosphate + dansyl-GCQL
diphosphate + farnesyl dansyl-GCQL
-
-
-
?
farnesyl diphosphate + dansyl-GCRL
diphosphate + farnesyl dansyl-GCRL
-
-
-
?
farnesyl diphosphate + dansyl-GCSV
diphosphate + farnesyl dansyl-GCSV
-
-
-
?
farnesyl diphosphate + dansyl-GCTV
diphosphate + farnesyl dansyl-GCTV
-
-
-
?
farnesyl diphosphate + dansyl-GCVL
diphosphate + farnesyl dansyl-GCVL
-
-
-
?
farnesyl diphosphate + dansyl-GCVLS
diphosphate + S-farnesyl dansyl-GCVLS
farnesyl diphosphate + dansyl-GCWI
diphosphate + farnesyl dansyl-GCWI
-
-
-
?
farnesyl diphosphate + dansyl-GCYL
diphosphate + farnesyl dansyl-GCYL
-
-
-
?
farnesyl diphosphate + dansyl-Gly-Cys-Lys-Thr-Gln
dansyl-Gly-S-farnesyl-Cys-Lys-Thr-Gln + diphosphate
-
-
-
-
?
farnesyl diphosphate + dansyl-Gly-Cys-Lys-Val-Leu
dansyl-Gly-S-farnesyl-Cys-Lys-Val-Leu + diphosphate
-
-
-
-
?
farnesyl diphosphate + dansyl-Gly-Cys-Val-Ile-Met
dansyl-Gly-S-farnesyl-Cys-Val-Ile-Met + diphosphate
-
-
-
-
?
farnesyl diphosphate + dansyl-Gly-Cys-Val-Leu-Ser
dansyl-Gly-S-farnesyl-Cys-Val-Leu-Ser + diphosphate
-
-
-
-
?
farnesyl diphosphate + Ds-GCVIA
diphosphate + ?
-
-
-
-
?
farnesyl diphosphate + GCVLS
Gly-S-farnesyl-Cys-Val-Leu-Ser + diphosphate
-
-
-
-
?
farnesyl diphosphate + GST-CIIL
diphosphate + S-farnesyl-GST-Cys-Ile-Ile-Ser
-
-
-
-
?
farnesyl diphosphate + GST-CIIS
?
-
GST-CIIS is glutathione S-transferase fused to the C-terminal 12 amino acids of yeast RAS2 protein
-
-
?
farnesyl diphosphate + human recombinant wild-type H-Ras-CVLS
diphosphate + ?
-
-
-
?
farnesyl diphosphate + mutant H-Ras-CVLL
diphosphate + ?
20fold less active than human recombinant wild-type H-Ras-CVLS
-
-
?
farnesyl diphosphate + N-dansyl-GCVLS
?
-
assay at pH 7.5, 30°C
-
-
?
farnesyl diphosphate + N-dansyl-GCVLS
S-farnesyl-N-dansyl-GCVLS + diphosphate
-
-
-
-
?
farnesyl diphosphate + N-dansyl-Gly-Cys-Val-Leu-Ser
diphosphate + N-dansyl-Gly-S-farnesyl-Cys-Val-Leu-Ser
-
the best substrate
-
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
farnesyl diphosphate + protein-cysteine
S-farnesyl protein + diphosphate
farnesyl diphosphate + Ras oncoprotein p21
diphosphate + Ras-S-farnesyl oncoprotein p21
-
-
-
-
?
farnesyl diphosphate + Ras protein
diphosphate + S-farnesyl Ras protein
-
-
-
-
?
farnesyl diphosphate + Ras-Cys-Val-Ile-Met
diphosphate + Ras-S-farnesyl-Cys-Val-Ile-Met
farnesyl diphosphate + Ras-Cys-Val-Leu-Met
diphosphate + Ras-S-farnesyl-Cys-Val-Leu-Met
-
-
-
-
?
farnesyl diphosphate + Thr-Lys-Cys-Val-Ile-Leu
Thr-Lys-S-farnesyl-Cys-Val-Ile-Leu + diphosphate
-
-
-
-
?
farnesyl diphosphate + Thr-Lys-Cys-Val-Ile-Met
Thr-Lys-S-farnesyl-Cys-Val-Ile-Met + diphosphate
-
-
-
-
?
farnesyl diphosphate + Thr-Lys-Cys-Val-Ile-Phe
Thr-Lys-S-farnesyl-Cys-Val-Ile-Phe + diphosphate
-
-
-
-
?
farnesyl diphosphate + Thr-Lys-Cys-Val-Ile-Ser
Thr-Lys-S-farnesyl-Cys-Val-Ile-Ser + diphosphate
-
-
-
-
?
farnesyl diphosphate + Thr-Lys-Cys-Val-Leu-Ala
Thr-Lys-S-farnesyl-Cys-Val-Leu-Ala + diphosphate
-
-
-
-
?
farnesyl diphosphate + Thr-Lys-Val-Ile-Phe
?
-
-
-
-
?
farnesyl diphosphate + [GST]-Cys-Ile-Ile-Ser
diphosphate + S-farnesyl-[GST]-Cys-Ile-Ile-Ser
-
-
-
-
?
farnesyl diphosphate + [protein]-L-cysteine
[protein]-S-((2E,6E)-farnesyl)-L-cysteine + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
farnesyl monophosphate + Gly-Cys-Val-Leu-Ser
phosphate + Gly-S-farnesyl-Cys-Val-Leu-Ser
-
-
-
-
?
farnesyl triphosphate + [Ras]-Cys-Val-Ile-Met
triphosphate + [Ras]-S-farnesyl-Cys-Val-Ile-Met
-
-
-
-
?
geranyl alkyne diphosphate + N-dansyl-GCVIA
N-dansyl-G-(alkyne geranyl)CVIA + diphosphate
-
-
-
-
ir
geranyl diphosphate + dansyl-GCVLS
dansyl-G-(S-geranyl)CVLS + diphosphate
-
-
-
-
?
geranylgeranyl diphosphate + N-dansyl-Gly-Cys-Val-Leu-Ser
diphosphate + N-dansyl-Gly-S-geranylgeranyl-Cys-Val-Leu-Ser
-
-
-
-
?
geranylgeranyl diphosphate + protein-cysteine
diphosphate + S-geranylgeranylcysteinyl protein
-
-
-
-
?
HOM-GPP + N-dansyl-GCVLS
?
-
-
-
-
?
TKCVIA + farnesyl diphosphate
TK-(S-farnesyl)CVIA + diphosphate
-
-
-
-
?
TKCVIC + farnesyl diphosphate
diphosphate + ?
-
-
-
-
?
TKCVID + farnesyl diphosphate
TK-(S-farnesyl)CVID + diphosphate
-
-
-
-
?
TKCVIF + farnesyl diphosphate
TK-(S-farnesyl)CVIF + diphosphate
-
-
-
-
?
TKCVII + farnesyl diphosphate
TK-(S-farnesyl)CVII + diphosphate
-
-
-
-
?
TKCVIL + farnesyl diphosphate
TK-(S-farnesyl)CVIL + diphosphate
-
-
-
-
?
TKCVIM + farnesyl diphosphate
TK-(S-farnesyl)CVIM + diphosphate
-
-
-
-
?
TKCVIN + farnesyl diphosphate
TK-(S-farnesyl)CVIN + diphosphate
-
-
-
-
?
TKCVIQ + farnesyl diphosphate
TK-(S-farnesyl)CVIQ + diphosphate
-
-
-
-
?
TKCVIR + farnesyl diphosphate
TK-(S-farnesyl)CVIR + diphosphate
-
-
-
-
?
TKCVIS + farnesyl diphosphate
TK-(S-farnesyl)CVIS + diphosphate
-
-
-
-
?
TKCVIT + farnesyl diphosphate
TK-(S-farnesyl)CVIT + diphosphate
-
-
-
-
?
TKCVIV + farnesyl diphosphate
TK-(S-farnesyl)CVIV + diphosphate
-
-
-
-
?
TKCVIY + farnesyl diphosphate
TK-(S-farnesyl)CVIY + diphosphate
-
-
-
-
?
YRASNRSCAIM + farnesyl diphosphate
YRASNRS-(S-farnesyl)CAIM + diphosphate
-
-
-
-
?
[(4E,8E,10E)-4,8-dimethyl-10-(oxodiphosphanylidene)deca-4,8-dien-1-yl]oxyacetonitrile + protein-cysteine
?
-
-
-
-
?
additional information
?
-
(2E,6E)-farnesyl diphosphate + (protein)-L-cysteine
S-(2E,6E)-farnesyl protein + diphosphate
-
-
-
?
(2E,6E)-farnesyl diphosphate + (protein)-L-cysteine
S-(2E,6E)-farnesyl protein + diphosphate
-
-
-
?
(2E,6E)-farnesyl diphosphate + (protein)-L-cysteine
S-(2E,6E)-farnesyl protein + diphosphate
-
-
-
?
(2E,6E)-farnesyl diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-farnesyl)CVLS + diphosphate
-
-
-
-
?
(2E,6E)-farnesyl diphosphate + dansyl-GCVLS
dansyl-G-(S-(2E,6E)-farnesyl)CVLS + diphosphate
-
assay at pH 7.5, 30°C
-
-
?
(2E,6E)-farnesyl diphosphate + [H Ras]-L-cysteine
S-(2E,6E)-farnesyl-[H Ras]-L-cysteine + diphosphate
-
-
-
?
(2E,6E)-farnesyl diphosphate + [H Ras]-L-cysteine
S-(2E,6E)-farnesyl-[H Ras]-L-cysteine + diphosphate
-
-
-
?
(2E,6E)-farnesyl diphosphate + [K Ras]-L-cysteine
S-(2E,6E)-farnesyl-[K Ras]-L-cysteine + diphosphate
-
-
-
?
(2E,6E)-farnesyl diphosphate + [K Ras]-L-cysteine
S-(2E,6E)-farnesyl-[K Ras]-L-cysteine + diphosphate
-
-
-
?
(2E,6E)-farnesyl diphosphate + [N Ras]-L-cysteine
S-(2E,6E)-farnesyl-[N Ras]-L-cysteine + diphosphate
-
-
-
?
(2E,6E)-farnesyl diphosphate + [N Ras]-L-cysteine
S-(2E,6E)-farnesyl-[N Ras]-L-cysteine + diphosphate
-
-
-
?
(2E,6E)-farnesyl diphosphate + [protein]-L-cysteine
S-(2E,6E)-farnesyl-[protein]-L-cysteine + diphosphate
-
-
-
-
?
(2E,6E)-farnesyl diphosphate + [protein]-L-cysteine
S-(2E,6E)-farnesyl-[protein]-L-cysteine + diphosphate
-
the reaction is catalyzed by protein farnesyltransferase on protein substrates bearing the C-terminal CaaX motif
-
-
?
(2E,6E)-farnesyl diphosphate + [protein]-L-cysteine
S-(2E,6E)-farnesyl-[protein]-L-cysteine + diphosphate
-
-
-
?
(2E,6E)-farnesyl diphosphate + [protein]-L-cysteine
S-(2E,6E)-farnesyl-[protein]-L-cysteine + diphosphate
-
-
-
-
?
(2E,6E)-farnesyl diphosphate + [protein]-L-cysteine
S-(2E,6E)-farnesyl-[protein]-L-cysteine + diphosphate
-
-
-
?
(2E,6E)-farnesyl diphosphate + [protein]-L-cysteine
S-(2E,6E)-farnesyl-[protein]-L-cysteine + diphosphate
-
-
-
?
(2E,6E)-farnesyl diphosphate + [protein]-L-cysteine
S-(2E,6E)-farnesyl-[protein]-L-cysteine + diphosphate
-
-
-
?
(2E,6E)-farnesyl diphosphate + [protein]-L-cysteine
S-(2E,6E)-farnesyl-[protein]-L-cysteine + diphosphate
-
-
-
-
?
(2E,6E)-farnesyl diphosphate + [Rho]-L-cysteine
S-(2E,6E)-farnesyl-[Rho]-L-cysteine + diphosphate
-
-
-
?
(2E,6E)-farnesyl diphosphate + [Rho]-L-cysteine
S-(2E,6E)-farnesyl-[Rho]-L-cysteine + diphosphate
-
-
-
?
dansyl-GCVDS + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVDS + diphosphate
-
poor substrate for wild-type
-
-
?
dansyl-GCVDS + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVDS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVIA + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVIA + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVIA + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVIA + diphosphate
-
100% enzyme activity, specific activity 0.765 microM/min
-
-
?
dansyl-GCVKS + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVKS + diphosphate
-
poor substrate for wild-type
-
-
?
dansyl-GCVKS + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVKS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
dansyl-GCVLS + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVLS + diphosphate
-
-
-
-
?
dansyl-GCVLS + (2E,6E)-farnesyl diphosphate
dansyl-G-(S-(2E,6E)-farnesyl)CVLS + diphosphate
-
assay at pH 7.8, 25°C
-
-
?
farnesyl diphosphate + biotin-YRASNRSCAIM
diphosphate + biotin-YRASNRS-(S-farnesyl)CAIM
-
-
-
-
?
farnesyl diphosphate + biotin-YRASNRSCAIM
diphosphate + biotin-YRASNRS-(S-farnesyl)CAIM
-
-
-
-
?
farnesyl diphosphate + dansyl-GCVLS
diphosphate + S-farnesyl dansyl-GCVLS
-
-
-
?
farnesyl diphosphate + dansyl-GCVLS
diphosphate + S-farnesyl dansyl-GCVLS
-
-
-
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
posttranslational lipid modification in which a 15-carbon farnesyl isoprenoid is linked via a thioether bond to specific cysteine residues of proteins, the reactive cysteine is located in the C-terminal Ca1a2X motif in which C is the modified cysteine, a1 and a2 are often an aliphatic residue, and X is Ser, Met, Ala or Gln
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
substrate: Ras-CVIM and GST-PEP
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
-
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
-
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
-
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
-
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
-
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
-
-
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
-
-
-
ir
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
Ftase has an autonomous recognition sequence, referred to as the CAAX box, where C is a cysteine, A is usually an aliphatic amino acid, and X can be a variety of amino acids
-
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
-
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
-
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
enzyme prefers Gln and Met at the X position but not Ser, Thr or Cys, which are good substrates for mammalian enzyme
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
-
-
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
-
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
posttranslational lipid modification in which a 15-carbon farnesyl isoprenoid is linked via a thioether bond to specific cysteine residues of proteins, the reactive cysteine is located in the C-terminal Ca1a2X motif in which C is the modified cysteine, a1 and a2 are often an aliphatic residue, and X is Ser, Met, Ala or Gln
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
prenylation, farnesylation, substrates are Ras, nuclear lamins, transducin gamma subunit, protein substrate motif: Cys-aliphatic-aliphatic-X, X: M, S, Q, A, F
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
-
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
-
-
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
-
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
-
-
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
posttranslational lipid modification in which a 15-carbon farnesyl isoprenoid is linked via a thioether bond to specific cysteine residues of proteins, the reactive cysteine is located in the C-terminal Ca1a2X motif in which C is the modified cysteine, a1 and a2 are often an aliphatic residue, and X is Ser, Met, Ala or Gln
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
posttranslational lipid modification in which a 15-carbon farnesyl isoprenoid is linked via a thioether bond to specific cysteine residues of proteins, the reactive cysteine is located in the C-terminal Ca1a2X motif in which C is the modified cysteine, a1 and a2 are often an aliphatic residue, and X is Ser, Met, Ala or Gln
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
posttranslational lipid modification in which a 15-carbon farnesyl isoprenoid is linked via a thioether bond to specific cysteine residues of proteins, the reactive cysteine is located in the C-terminal Ca1a2X motif in which C is the modified cysteine, a1 and a2 are often an aliphatic residue, and X is Ser, Met, Ala or Gln
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
posttranslational lipid modification in which a 15-carbon farnesyl isoprenoid is linked via a thioether bond to specific cysteine residues of proteins, the reactive cysteine is located in the C-terminal Ca1a2X motif in which C is the modified cysteine, a1 and a2 are often an aliphatic residue, and X is Ser, Met, Ala or Gln
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
posttranslational lipid modification in which a 15-carbon farnesyl isoprenoid is linked via a thioether bond to specific cysteine residues of proteins, the reactive cysteine is located in the C-terminal Ca1a2X motif in which C is the modified cysteine, a1 and a2 are often an aliphatic residue, and X is Ser, Met, Ala or Gln
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
posttranslational lipid modification in which a 15-carbon farnesyl isoprenoid is linked via a thioether bond to specific cysteine residues of proteins, the reactive cysteine is located in the C-terminal Ca1a2X motif in which C is the modified cysteine, a1 and a2 are often an aliphatic residue, and X is Ser, Met, Ala or Gln
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
posttranslational lipid modification in which a 15-carbon farnesyl isoprenoid is linked via a thioether bond to specific cysteine residues of proteins, the reactive cysteine is located in the C-terminal Ca1a2X motif in which C is the modified cysteine, a1 and a2 are often an aliphatic residue, and X is Ser, Met, Ala or Gln
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
Ha-Ras-CVLS, which is a good substrate for mammalian enzyme, not farnesylated by the parasite enzyme, only the mammalian enzyme substrate RAS1-CVIM farnesylated by parasite enzyme
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
substrate are: Ras superfamiliy and Ras-related proteins for example Rap, Rab, Rac and Ral, large G proteins, nuclear lamins, rhodopsin kinase and the retinal cGMP phosphodiesterase
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
substrate are: Ras superfamiliy and Ras-related proteins for example Rap, Rab, Rac and Ral, large G proteins, nuclear lamins, rhodopsin kinase and the retinal cGMP phosphodiesterase
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
enzyme prefers linear residues in the X position of the CaaX box over branched residues, enzyme prefers Gln, Met and Ser at the X position
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
substrates are cellular proteins such as Ras at a cysteine residue near their carboxy-terminus
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
prenylation, farnesylation, substrates are Ras, nuclear lamins, transducin gamma subunit, protein substrate motif: Cys-aliphatic-aliphatic-X, X: M, S, Q, A, F
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
prenylation, farnesylation, substrates are Ras, nuclear lamins, transducin gamma subunit, protein substrate motif: Cys-aliphatic-aliphatic-X, X: M, S, Q, A, F
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
prenylation, farnesylation, substrates are Ras, nuclear lamins, transducin gamma subunit, protein substrate motif: Cys-aliphatic-aliphatic-X, X: M, S, Q, A, F
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
prenylation, farnesylation, substrates are Ras, nuclear lamins, transducin gamma subunit, protein substrate motif: Cys-aliphatic-aliphatic-X, X: M, S, Q, A, F
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
prenylation, farnesylation, substrates are Ras, nuclear lamins, transducin gamma subunit, protein substrate motif: Cys-aliphatic-aliphatic-X, X: M, S, Q, A, F
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
prenylation, farnesylation, substrates are Ras, nuclear lamins, transducin gamma subunit, protein substrate motif: Cys-aliphatic-aliphatic-X, X: M, S, Q, A, F
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
prenylation, farnesylation, substrates are Ras, nuclear lamins, transducin gamma subunit, protein substrate motif: Cys-aliphatic-aliphatic-X, X: M, S, Q, A, F
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
prenylation, farnesylation, substrates are Ras, nuclear lamins, transducin gamma subunit, protein substrate motif: Cys-aliphatic-aliphatic-X, X: M, S, Q, A, F
-
ir
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
preferred CaaX-substrate: CAIM
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
-
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
-
-
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
prenylation, farnesylation, substrates are Ras, nuclear lamins, transducin gamma subunit, protein substrate motif: Cys-aliphatic-aliphatic-X, X: M, S, Q, A, F
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
prenylation, farnesylation, substrates are Ras, nuclear lamins, transducin gamma subunit, protein substrate motif: Cys-aliphatic-aliphatic-X, X: M, S, Q, A, F
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
preferred CaaX-substrate: CAIM
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
the specific CAQQ motif of the ANJ1 protein has a low affinity for enzyme in vitro, enzyme specifically farnesylated the RasB-CVIM peptide substrate
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
substrate: Biotin lamin-B protein
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
Ha-Ras-CVLS, which is a good substrate for mammalian enzyme, not farnesylated by the parasite enzyme, only the mammalian enzyme substrate RAS1-CVIM farnesylated by parasite enzyme
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
enzyme prefers Gln and Met at the X position but not Ser, Thr or Cys, which are good substrates for mammalian enzyme
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
enzyme prefers Gln and Met at the X position but not Ser, Thr or Cys, which are good substrates for mammalian enzyme
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
-
Ha-Ras-CVLS, which is a good substrate for mammalian enzyme, not farnesylated by the parasite enzyme, only the mammalian enzyme substrate RAS1-CVIM farnesylated by parasite enzyme
-
?
farnesyl diphosphate + protein-cysteine
diphosphate + S-farnesyl protein
enzyme prefers Gln and Met at the X position but not Ser, Thr or Cys, which are good substrates for mammalian enzyme
-
?
farnesyl diphosphate + protein-cysteine
S-farnesyl protein + diphosphate
-
-
-
-
?
farnesyl diphosphate + protein-cysteine
S-farnesyl protein + diphosphate
-
process required for the transforming activity of oncogenic variants of Ras, making enzyme a prime target for anticancer therapeutics
-
-
?
farnesyl diphosphate + protein-cysteine
S-farnesyl protein + diphosphate
-
process necessary for the subcellular localisation of substrate to the plasma membrane
-
-
?
farnesyl diphosphate + protein-cysteine
S-farnesyl protein + diphosphate
-
the enzyme catalyzes posttranslational modification of proteins, the farnesyl moieties attached to the substrates are direcly involved in protein-protein interactions as well as in protein-membrane interactions
-
-
?
farnesyl diphosphate + protein-cysteine
S-farnesyl protein + diphosphate
-
substrate motif: carboxy-terminal -Ca1a2X box
-
-
?
farnesyl diphosphate + protein-cysteine
S-farnesyl protein + diphosphate
-
protein farnesylation is essential for early embryonic proliferation but dispensable for postnatal development and adult homeostasis. Ablation of FTase during tumor progression results in significant tumor reduction
-
-
?
farnesyl diphosphate + protein-cysteine
S-farnesyl protein + diphosphate
-
potential role for plant enzyme in cell cycle regulation
-
-
?
farnesyl diphosphate + protein-cysteine
S-farnesyl protein + diphosphate
-
potential role for plant enzyme in cell cycle regulation
-
-
?
farnesyl diphosphate + protein-cysteine
S-farnesyl protein + diphosphate
-
potential role for cell cycle
-
-
?
farnesyl diphosphate + protein-cysteine
S-farnesyl protein + diphosphate
-
-
-
-
?
farnesyl diphosphate + protein-cysteine
S-farnesyl protein + diphosphate
-
process required for the transforming activity of oncogenic variants of Ras, making enzyme a prime target for anticancer therapeutics
-
-
?
farnesyl diphosphate + protein-cysteine
S-farnesyl protein + diphosphate
-
process necessary for the subcellular localisation of substrate to the plasma membrane
-
-
?
farnesyl diphosphate + protein-cysteine
S-farnesyl protein + diphosphate
-
enzyme responsible for catalysing isoprene lipid modifications
-
-
?
farnesyl diphosphate + protein-cysteine
S-farnesyl protein + diphosphate
-
A series of steps modifies the C-terminus of Ras. Enzyme catalyses the first of these steps by transferring the farnesyl group from farnesyl diphosphates to the cysteine side chain in the CAAX sequence motif at the C-terminus of Ras
-
-
?
farnesyl diphosphate + protein-cysteine
S-farnesyl protein + diphosphate
-
catalyzes the post-translational modification of many important cellular proteins
-
-
?
farnesyl diphosphate + protein-cysteine
S-farnesyl protein + diphosphate
-
-
-
-
?
farnesyl diphosphate + protein-cysteine
S-farnesyl protein + diphosphate
-
process required for the transforming activity of oncogenic variants of Ras, making enzyme a prime target for anticancer therapeutics
-
-
?
farnesyl diphosphate + protein-cysteine
S-farnesyl protein + diphosphate
-
process necessary for the subcellular localisation of substrate to the plasma membrane
-
-
?
farnesyl diphosphate + protein-cysteine
S-farnesyl protein + diphosphate
-
a possible role for the enzyme during fruit development
-
-
?
farnesyl diphosphate + protein-cysteine
S-farnesyl protein + diphosphate
-
enzyme responsible for catalysing isoprene lipid modifications
-
-
?
farnesyl diphosphate + Ras-Cys-Val-Ile-Met
diphosphate + Ras-S-farnesyl-Cys-Val-Ile-Met
-
-
-
-
?
farnesyl diphosphate + Ras-Cys-Val-Ile-Met
diphosphate + Ras-S-farnesyl-Cys-Val-Ile-Met
-
-
-
-
?
farnesyl diphosphate + Ras-Cys-Val-Ile-Met
diphosphate + Ras-S-farnesyl-Cys-Val-Ile-Met
-
-
-
-
?
farnesyl diphosphate + Ras-Cys-Val-Ile-Met
diphosphate + Ras-S-farnesyl-Cys-Val-Ile-Met
-
best substrate
-
-
?
farnesyl diphosphate + Ras-Cys-Val-Ile-Met
diphosphate + Ras-S-farnesyl-Cys-Val-Ile-Met
-
best substrate
-
-
?
farnesyl diphosphate + Ras-Cys-Val-Ile-Met
diphosphate + Ras-S-farnesyl-Cys-Val-Ile-Met
-
-
-
-
?
farnesyl diphosphate + Ras-Cys-Val-Ile-Met
diphosphate + Ras-S-farnesyl-Cys-Val-Ile-Met
-
-
-
-
?
additional information
?
-
protein farnesytransferase catalyzes the farnesylation of proteins with a C-terminal tetrapeptide sequence denoted as a Ca1a2X box, determination of substrate recognition sequences, and substrate specificity, screening of the CVa2X library with alkyne-functionalized isoprenoid substrates, detailed overview
-
-
?
additional information
?
-
-
biotin-GPP is not transferred to the peptide substrate to any measurable extent
-
-
?
additional information
?
-
FTase-I can transfer isoprenoids to intracellular proteins that contain CAAX motifs. The isoprenoid groups can be selectively recognized by GGTase-I. The 15-carbon isoprenoid geranylgeranyl from its donor farnesyldiphosphate (FPP) is specific to FTase-I. Residues Lysalpha164, Hisbeta248, Argbeta291 and Tyrbeta300 in FTase can form hydrogen bonds with farnesyl diphosphate. When FTase is inhibited by a FTI, N-Ras and K-Ras can be alternatively prenylated by GGTase-I, EC 2.5.1.59, but H-Ras cannot
-
-
?
additional information
?
-
FTase-I can transfer isoprenoids to intracellular proteins that contain CAAX motifs. The isoprenoid groups can be selectively recognized by GGTase-I. The 15-carbon isoprenoid geranylgeranyl from its donor farnesyldiphosphate (FPP) is specific to FTase-I. Residues Lysalpha164, Hisbeta248, Argbeta291 and Tyrbeta300 in FTase can form hydrogen bonds with farnesyl diphosphate. When FTase is inhibited by a FTI, N-Ras and K-Ras can be alternatively prenylated by GGTase-I, EC 2.5.1.59, but H-Ras cannot
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-
?
additional information
?
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-
enzyme-substrate interaction study using synthetic peptides as substrates, modelling of the enzyme interaction with substrate protein tyrosine phosphatase, protein-protein docking and molecular dynamics simulation, overview
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-
?
additional information
?
-
-
although farnesyl diphosphate and geranylgeranyl diphosphate bind competitively, the geranyl geranyl diphosphate is not transferred efficiently to the protein substrate by enzyme
-
-
?
additional information
?
-
-
not: geranylgeranyl diphosphate
-
-
?
additional information
?
-
-
not: geranylgeranyl diphosphate
-
-
?
additional information
?
-
-
steady-state kinetics for modification of peptide substrates shows that the multiple-turnover activity depends on the analogue structure. Analogues in which the first isoprene is replaced with a benzyl group and an analogue in which each isoprene is replaced with an aryl group are good substrates. The single-turnover rate constant for alkylation depends on the Ca1a2X peptide sequence. The isoprenoid transition-state conformation is preferred over the inactive E-FPP-Ca1a2X ternary complex conformation and the farnesyl binding site in the exit groove may be significantly more selective for the farnesyl diphosphate substrate than the active site binding pocket
-
-
?
additional information
?
-
ligand interaction analysis with FTase alpha subunit, mass spectrometry, overview. The enzyme alpha-subunit interacts with Vps4A protein in vitro and in vivo
-
-
?
additional information
?
-
analogues of farnesyl diphosphate alter CaaX substrate specificity and reactions rates of protein farnesyltransferase, reactivity of four alkyne-containing analogs of farnesyl diphosphate with purified protein farnesyltransferase and a small library of dansylated peptides using an in vitro continuous spectrofluorimetric assay, overview. Activity with CGGDD, CVLL, and CSVL peptides is low with farnesyl diphosphate as well as with its analogues
-
-
?
additional information
?
-
FTase-I can transfer isoprenoids to intracellular proteins that contain CAAX motifs. The isoprenoid groups can be selectively recognized by GGTase-I. The 15-carbon isoprenoid geranylgeranyl from its donor farnesyldiphosphate (FPP) is specific to FTase-I. Residues Lysalpha164, Hisbeta248, Argbeta291 and Tyrbeta300 in FTase can form hydrogen bonds with farnesyl diphosphate. When FTase is inhibited by a FTI, N-Ras and K-Ras can be alternatively prenylated by GGTase-I, EC 2.5.1.59, but H-Ras cannot
-
-
?
additional information
?
-
FTase-I can transfer isoprenoids to intracellular proteins that contain CAAX motifs. The isoprenoid groups can be selectively recognized by GGTase-I. The 15-carbon isoprenoid geranylgeranyl from its donor farnesyldiphosphate (FPP) is specific to FTase-I. Residues Lysalpha164, Hisbeta248, Argbeta291 and Tyrbeta300 in FTase can form hydrogen bonds with farnesyl diphosphate. When FTase is inhibited by a FTI, N-Ras and K-Ras can be alternatively prenylated by GGTase-I, EC 2.5.1.59, but H-Ras cannot
-
-
?
additional information
?
-
protein farnesytransferase catalyzes the farnesylation of proteins with a C-terminal tetrapeptide sequence denoted as a Ca1a2X box, determination of substrate recognition sequences, and substrate specificity, screening of the CVa2X library with alkyne-functionalized isoprenoid substrates, detailed overview
-
-
?
additional information
?
-
-
protein farnesytransferase catalyzes the farnesylation of proteins with a C-terminal tetrapeptide sequence denoted as a Ca1a2X box, determination of substrate recognition sequences, and substrate specificity, screening of the CVa2X library with alkyne-functionalized isoprenoid substrates, detailed overview
-
-
?
additional information
?
-
enzyme prefers farnesyl diphosphate over geranylgeranyl diphosphate, but catalyzes the reactions of both substrates, i.e. reactions of EC 2.5.1.58 and EC 2.5.1.59, respectively
-
-
-
additional information
?
-
ligand interaction analysis with FTase alpha subunit, mass spectrometry, overview. The enzyme alpha-subunit interacts with Vps4A protein in vitro and in vivo
-
-
?
additional information
?
-
protein farnesytransferase catalyzes the farnesylation of proteins with a C-terminal tetrapeptide sequence denoted as a Ca1a2X box, determination of substrate recognition sequences, and substrate specificity, screening of the CVa2X library with alkyne-functionalized isoprenoid substrates, detailed overview
-
-
?
additional information
?
-
-
protein farnesytransferase catalyzes the farnesylation of proteins with a C-terminal tetrapeptide sequence denoted as a Ca1a2X box, determination of substrate recognition sequences, and substrate specificity, screening of the CVa2X library with alkyne-functionalized isoprenoid substrates, detailed overview
-
-
?
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(+)-6-(camphorquinone-10-sulfonamido)-hexanoic acid
-
-
(-)-6-(camphorquinone-10-sulfonamido)-hexanoic acid
-
-
(1aR,2S,3aS,6aR,7aR)-2,6-dimethyl-1a-[(1E)-3-oxobut-1-en-1-yl]octahydro-5H-oxireno[4,5]cyclohepta[1,2-b]furan-5-one
-
-
(1aR,2S,3aS,6aR,7aR)-2-methyl-6-methylidene-1a-[(1E)-3-oxobut-1-en-1-yl]octahydro-5H-oxireno[4,5]cyclohepta[1,2-b]furan-5-one
-
-
(1aS,2S,3aS,6aR,7aS)-2,6-dimethyl-1a-[(1E)-3-oxobut-1-en-1-yl]octahydro-5H-oxireno[4,5]cyclohepta[1,2-b]furan-5-one
-
-
(1aS,2S,3aS,6aR,7aS)-2-methyl-6-methylidene-1a-[(1E)-3-oxobut-1-en-1-yl]octahydro-5H-oxireno[4,5]cyclohepta[1,2-b]furan-5-one
-
-
(1R,4aR,5R,7S)-5-[[(1R,4aR,8aS)-8a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-6-methoxy-5,8-dioxo-1,4,4a,5,8,8a-hexahydronaphthalen-1-yl]methyl]-7-hydroxy-1,4a-dimethyl-6-methylidenedecahydronaphthalene-1-carbaldehyde
-
-
(1R,4aR,5R,7S)-5-[[(1R,4aR,8aS)-8a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-6-methoxy-5,8-dioxo-1,4,4a,5,8,8a-hexahydronaphthalen-1-yl]methyl]-7-hydroxy-1,4a-dimethyl-6-methylidenedecahydronaphthalene-1-carboxylic acid
-
-
(2-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-1-[2-(methylsulfanyl)ethyl]hydrazinyl)acetic acid
(2E)-2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ylidene]butanedioic acid
(2E)-3-[(3aR,7S,8aS)-3,7-dimethyl-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]-1-methylprop-2-en-1-yl acetate
-
-
(2E,4E,8E)-5,9,13-trimethyltetradeca-2,4,8,12-tetraenoic acid
(2Z)-3-(1H-imidazol-2-yl)-5-methylhexa-2,4-dienoic acid
-
8% inhibition at 0.001 M
(2Z)-5-methyl-3-(1-methyl-1H-imidazol-2-yl)hexa-2,4-dienoic acid
-
8% inhibition at 0.001 M
(2Z,4E)-5,9-dimethyl-3-(1-methyl-1H-imidazol-2-yl)deca-2,4,8-trienoic acid
-
-
(2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoic acid
(2Z,6E)-3-(3-methylbut-2-enyl)-7,11-dimethyldodeca-2,6,10-triene monophosphate
-
IC50: 16 nM
(2Z,6E)-3-allyl-7,11-dimethyldodeca-2,6,10-trien-1-yl 5-nitrofurfuryl N-methyl-N-(4-chlorobutyl)phosphoramidate
-
-
(2Z,6E)-3-allyl-7,11-dimethyldodeca-2,6,10-triene monophosphate
-
-
(2Z,6E)-3-tert-butyl-7,11-dimethyldodeca-2,6,10-trien-1-yl 5-nitrofurfuryl N-methyl-N-(4-chlorobutyl)phosphoramidate
-
-
(2Z,6E)-3-tert-butyl-7,11-dimethyldodeca-2,6,10-triene monophosphate
-
IC50: 13 nM
(2Z,6E,10E)-3-(3-methyl-1-but-2-enyl)-7,11-dimethyldodeca-2,6,10-trien-1-yl 5-nitrofurfuryl N-methyl-N-(4-chlorobutyl)phosphoramidate
-
-
(3aR,7S,8aS)-3,7-dimethyl-6-[(1E)-3-oxobut-1-en-1-yl]-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-2-one
-
-
(3aR,7S,8aS)-6-[(1E)-3-hydroxybut-1-en-1-yl]-3,7-dimethyl-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-2-one
-
-
(3aR,7S,8aS)-7-methyl-3-methylidene-6-[(1E)-3-oxobut-1-en-1-yl]-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-2-one
-
-
(3aR,8S,9aS)-6-acetyl-3,8-dimethyl-3,3a,4,8,9,9a-hexahydro-2H-cyclohepta[1,2-b:4,5-b']difuran-2-one
-
-
(3R,3aR,7S,8aS)-3,7-dimethyl-6-(3-oxobutyl)-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-2-one
-
-
(3R,3aR,7S,8aS)-6-(3-hydroxybutyl)-3,7-dimethyl-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-2-one
-
-
(4aS,5R,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-2-methoxy-5-[[(1S,3S,7S,8aS)-1,3,7-trihydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
-
-
(4aS,5R,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-2-methoxy-6-methyl-5-[[(1R,8aS)-5,5,8a-trimethyl-2-methylidene-3-oxodecahydronaphthalen-1-yl]methyl]-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
-
-
(4aS,5R,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-5-[[(1R,3S,5R,8aS)-3-hydroxy-5-(hydroxymethyl)-5,8a-dimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-2-methoxy-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
-
-
(4aS,5R,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-5-[[(1R,3S,7S,8aS)-3,7-dihydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-2-methoxy-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
-
-
(4aS,5R,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-5-[[(1R,3S,8aS)-3-hydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-2-methoxy-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
-
-
(4aS,5R,8aR)-4a-(5-hydroxy-7-methoxy-4-oxo-4H-chromen-2-yl)-2-methoxy-6-methyl-5-[[(1R,8aS)-5,5,8a-trimethyl-2-methylidene-3-oxodecahydronaphthalen-1-yl]methyl]-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
-
-
(4aS,5S,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-5-[[(1R,2R,7S,8aS)-2,7-dihydroxy-2,5,5,8a-tetramethyldecahydronaphthalen-1-yl]methyl]-6-hydroxy-2-methoxy-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
-
-
(4E)-5,9-dimethyl-3-(1-methyl-1H-imidazol-2-yl)deca-4,8-dienoic acid
-
-
(4E,8E)-2-(ethoxycarbonyl)-5,9,13-trimethyl-2-[3-(1-methyl-1H-imidazol-2-yl)propyl]tetradeca-4,8,12-trienoic acid
(4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-4,8,12-trienoic acid
(4E,8E)-5,9,13-trimethyl-N-(phenylsulfonyl)tetradeca-4,8,12-trienamide
(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienamide
-
-
(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoic acid
(4E,8E)-N-hydroxy-5,9,13-trimethyltetradeca-4,8,12-trienamide
-
-
(4S)-4-([[5-(butan-2-yl)-3-(4-chlorophenyl)-4-cyanothiophen-2-yl]carbonyl]amino)-5-tert-butoxy-5-oxopentanoic acid
(6E,10E)-7,11,15-trimethyl-3-oxohexadeca-6,10,14-trienoic acid
(7E,11E)-8,12,16-trimethyl-4-oxoheptadeca-7,11,15-trienoic acid
(E,E)-8-O-(3-benzoylbenzyl)-3,7-dimethyl-2,6-octadiene 1-diphosphate
-
-
(E,E)-8-O-(4-benzoylbenzyl)-3,7-dimethyl-2,6-octadiene 1-diphosphate
-
-
(S)-N-(4-(3,4-dichlorophenoxy)benzyl)-6-(1H-indol-3-yl)piperazine-2,5-dione
-
dual inhibitor for both farnesyl transferase and geranygeranyltransferase-I. Compound occupies both isoprenoid and peptide substrate binding sites
(S)-N-(4-(3-chlorophenoxy)benzyl)-6-(1H-indol-3-yl)piperazine-2,5-dione
-
dual inhibitor for both farnesyl transferase and geranygeranyltransferase-I
1,4,8,10-tetrahydroxy-6-[(1E)-3-[(3S,8aS)-3-hydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]-1-methylprop-1-en-1-yl]-5,6-dihydro-7H-benzo[c]xanthen-7-one
-
-
1,5-dimethyl-1H-imidazole-4-sulfonic acid (5-bromo-2-fluorobenzyl)-[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-amide
-
98% inhibition at 50 nM
1,5-dimethyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(4-ethanesulfonyl-benzyl)-amide
-
97% inhibition at 50 nM
1,5-dimethyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(4-methanesulfonyl-benzyl)-amide
-
92% inhibition at 50 nM
1-(1-[3,4-bis[(hydroxyacetyl)amino]phenyl]-4,4-dicyano-1-oxobut-3-en-2-yl)-3-(dimethylamino)pyridinium
-
-
1-(1H-imidazol-5-ylmethyl)-7-pyridin-4-yl-4-[[2-(trifluoromethoxy)phenyl]carbonyl]-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine
-
-
1-(2-chlorophenyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[4-(methylsulfonyl)benzyl]methanesulfonamide
-
99% inhibition at 50 nM
1-(4,4-dicyano-1-oxo-1-phenylbut-3-en-2-yl)-3-(dimethylamino)pyridinium
-
-
1-(4,4-dicyano-1-oxo-1-phenylbut-3-en-2-yl)-3-methylpyridinium
-
-
1-methyl-1H-imidazole-4-sulfonic acid (2-bromo-allyl)-[1-(3-methyl-3H-imidazol-4-ylmethyl)-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-amide
-
97% inhibition at 50 nM
1-methyl-1H-imidazole-4-sulfonic acid (2-bromo-allyl)-[6-cyano-1-(3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-amide
-
94% inhibition at 50 nM
1-methyl-1H-imidazole-4-sulfonic acid (4-benzenesulfonylbenzyl)-[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-amide
-
99% inhibition at 50 nM
1-methyl-1H-imidazole-4-sulfonic acid (4-methanesulfonylbenzyl)-[1-(3-methyl-3H-imidazol-4-ylmethyl)-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-amide
-
98% inhibition at 50 nM
1-methyl-1H-imidazole-4-sulfonic acid benzyl-[6-cyano-1-(3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-amide
-
93% inhibition at 50 nM
1-methyl-1H-imidazole-4-sulfonic acid ethyl-[1-(3-methyl-3H-imidazol-4-ylmethyl)-6-phenyl-1,2,3,4-tetrahydro-quinolin-3-yl]amide
-
86% inhibition at 50 nM
1-methyl-1H-imidazole-4-sulfonic acid [1-(3-methyl-3H-imidazol-4-ylmethyl)-6-phenyl-1,2,3,4-tetrahydro-quinolin-3-yl]-(2-pyrrol-1-yl-ethyl)-amide
-
90% inhibition at 50 nM
1-methyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-yl-methyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(3-methoxy-propyl)-amide
-
-
1-methyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(4,4-dioxo-3,4-dihydro-2H-4lambda6-benzo[1,4]oxathin-7-ylmethyl)-amide
-
99% inhibition at 50 nM
1-methyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(4-ethanesulfonyl-benzyl)-amide
-
complete inhibition at 50 nM
1-methyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(4-fluoro-benzyl)-amide
-
99% inhibition at 50 nM
1-methyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(4-methanesulfonyl-benzyl)-amide
-
complete inhibition at 50 nM
1-methyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(5-trifluoromethyl-furan-2-ylmethyl)-amide
-
97% inhibition at 50 nM
1-methyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-[2-(2-fluoro-phenyl)-ethyl]-amide
-
complete inhibition at 50 nM
1-methyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-[2-(2-oxo-pyrrolidin-1-yl)-ethyl]-amide
-
99% inhibition at 50 nM
1-methyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-[2-(4-fluoro-phenyl)-ethyl]-amide
-
complete inhibition at 50 nM
1-methyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-[4-(1,3-dioxo-1,3-dihydro-isoindol-2-yloxy)-butyl]-amide
-
99% inhibition at 50 nM
1-methyl-1H-pyrazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(2-fluoro-benzyl)-amide
-
94% inhibition at 50 nM
1-methyl-N-(2-methylbenzyl)-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-1H-imidazole-4-sulfonamide
-
46% inhibition at 50 nM
1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-1H-imidazole-4-sulfonamide
-
80% inhibition at 50 nM
1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-methylprop-2-en-1-yl)-1H-imidazole-4-sulfonamide
-
99% inhibition at 50 nM
1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N-prop-2-en-1-yl-1H-imidazole-4-sulfonamide
-
98% inhibition at 50 nM
1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N-prop-2-yn-1-yl-1H-imidazole-4-sulfonamide
-
95% inhibition at 50 nM
1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(5-methylisoxazol-4-yl)methyl]-1H-imidazole-4-sulfonamide
1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(methylsulfonyl)ethyl]-1H-imidazole-4-sulfonamide
-
99% inhibition at 50 nM
1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N-[[5-(trifluoromethyl)furan-2-yl]methyl]-1H-imidazole-4-sulfonamide
-
88% inhibition at 50 nM
1-methylethyl 4-[([1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate
1-methylethyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
-
97% inhibition at 50 nM
1-[(3aR,7S,8aS)-3,7-dimethyl-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]-3-(1-hydroxyethoxy)butyl acetate
-
-
1-[(3aR,7S,8aS)-3,7-dimethyl-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]butane-1,3-diyl diacetate
-
-
1-[(3aR,7S,8aS)-7-methyl-3-methylidene-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]-3-oxobutyl acetate
-
-
1-[(3aR,7S,8aS)-7-methyl-3-methylidene-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]butane-1,3-diyl diacetate
-
-
1-[(3Z)-1-(4-bromophenyl)-4-cyano-5,5-dihydroxy-1-oxohept-3-en-2-yl]-3-(dimethylamino)pyridinium
-
-
1-[(3Z)-1-(4-chlorophenyl)-4-cyano-5,5-dihydroxy-1-oxohept-3-en-2-yl]-3-(dimethylamino)pyridinium
-
-
1-[(3Z)-1-[3,4-bis[(hydroxyacetyl)amino]phenyl]-4-cyano-5,5-dihydroxy-1-oxohept-3-en-2-yl]-3-(dimethylamino)pyridinium
-
-
1-[(3Z)-4-cyano-1-(3,4-dimethoxyphenyl)-5,5-dihydroxy-1-oxohept-3-en-2-yl]-3-methoxypyridinium
-
-
1-[(3Z)-4-cyano-1-(4-cyanophenyl)-5,5-dihydroxy-1-oxohept-3-en-2-yl]-3-(dimethylamino)pyridinium
-
-
1-[(3Z)-4-cyano-1-(4-fluorophenyl)-5,5-dihydroxy-1-oxohept-3-en-2-yl]-3-(dimethylamino)pyridinium
-
-
1-[(3Z)-4-cyano-5,5-dihydroxy-1-(4-methoxyphenyl)-1-oxohept-3-en-2-yl]-2,4-dimethylpyridinium
-
-
1-[(3Z)-4-cyano-5,5-dihydroxy-1-(4-methoxyphenyl)-1-oxohept-3-en-2-yl]-3-(dimethylamino)pyridinium
-
-
1-[(3Z)-4-cyano-5,5-dihydroxy-1-(4-methoxyphenyl)-1-oxohept-3-en-2-yl]-3-methoxypyridinium
-
-
1-[(3Z)-4-cyano-5,5-dihydroxy-1-(4-methylphenyl)-1-oxohept-3-en-2-yl]-3-(dimethylamino)pyridinium
-
-
1-[(3Z)-4-cyano-5,5-dihydroxy-1-(4-nitrophenyl)-1-oxohept-3-en-2-yl]-3-(dimethylamino)pyridinium
-
-
1-[(3Z)-4-cyano-5,5-dihydroxy-1-oxo-1-(3,4,5-trimethoxyphenyl)hept-3-en-2-yl]-2,4-dimethylpyridinium
-
-
1-[(3Z)-4-cyano-5,5-dihydroxy-1-oxo-1-(3,4,5-trimethoxyphenyl)hept-3-en-2-yl]-3-(dimethylamino)pyridinium
-
-
1-[(3Z)-4-cyano-5,5-dihydroxy-1-oxo-1-phenylhept-3-en-2-yl]-3-(dimethylamino)pyridinium
-
-
1-[(3Z)-4-cyano-5,5-dihydroxy-1-oxo-1-phenylhept-3-en-2-yl]-3-methylpyridinium
-
-
1-[1-(4-bromophenyl)-4,4-dicyano-1-oxobut-3-en-2-yl]-3-(dimethylamino)pyridinium
-
-
1-[1-(4-chlorophenyl)-4,4-dicyano-1-oxobut-3-en-2-yl]-3-(dimethylamino)pyridinium
-
-
1-[4,4-dicyano-1-(3,4-dimethoxyphenyl)-1-oxobut-3-en-2-yl]-3-methoxypyridinium
-
-
1-[4,4-dicyano-1-(4-cyanophenyl)-1-oxobut-3-en-2-yl]-3-(dimethylamino)pyridinium
-
-
1-[4,4-dicyano-1-(4-fluorophenyl)-1-oxobut-3-en-2-yl]-3-(dimethylamino)pyridinium
-
-
1-[4,4-dicyano-1-(4-methoxyphenyl)-1-oxobut-3-en-2-yl]-2,4-dimethylpyridinium
-
-
1-[4,4-dicyano-1-(4-methoxyphenyl)-1-oxobut-3-en-2-yl]-3-(dimethylamino)pyridinium
-
-
1-[4,4-dicyano-1-(4-methoxyphenyl)-1-oxobut-3-en-2-yl]-3-methoxypyridinium
-
-
1-[4,4-dicyano-1-(4-methylphenyl)-1-oxobut-3-en-2-yl]-3-(dimethylamino)pyridinium
-
-
1-[4,4-dicyano-1-(4-nitrophenyl)-1-oxobut-3-en-2-yl]-3-(dimethylamino)pyridinium
-
-
1-[4,4-dicyano-1-oxo-1-(3,4,5-trimethoxyphenyl)but-3-en-2-yl]-2,4-dimethylpyridinium
-
-
1-[4,4-dicyano-1-oxo-1-(3,4,5-trimethoxyphenyl)but-3-en-2-yl]-3-(dimethylamino)pyridinium
-
-
10-desmethoxystreptonigrin
-
-
18-oxa-2,5,9,11-tetraazahexacyclo[17.6.2.22,5.113,17.07,11.022,26]triaconta-1(26),7,9,13(28),14,16,19,21,22,24,26-undecaene-16-carbonitrile
-
-
2,2,2-trifluoroethyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
-
91% inhibition at 50 nM
2-amino-3-[2-butyl-4-(naphthalen-1-ylcarbonyl)piperazin-1-yl]propane-1-thiol
-
-
2-methylpropyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate
-
98% inhibition at 50 nM
2-methylpropyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
2-[(2E)-3,7-dimethyl-1-(1-methyl-1H-imidazol-2-yl)octa-2,6-dien-1-yl]butanedioic acid
2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]butanedioic acid
2-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](2-fluorobenzyl)amino]-2-oxoethyl acetate
-
33% inhibition at 50 nM
29-oxo-18-oxa-2,6,9,11-tetraazahexacyclo[17.5.3.12,5.113,17.07,11.022,26]nonacosa-7,9,13(28),14,16,19,21,26-octaene-16-carbonitrile
-
-
3,4-dihydro-2H-benzo[b][1,4]dioxepine-7-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydroquinolin-3-yl]-(4-methanesulfonyl-benzyl)-amide
-
97% inhibition at 50 nM
3-(1H-imidazol-2-yl)-5-methylhex-4-enoic acid
-
21% inhibition at 0.001 M
3-(3-methyl-2-butenyl)-7,11-dimethyldodeca-2(Z),6(E),10-triene 1-diphosphate
-
farnesylation of dansyl-GCKVL, IC5=: 510 nM
3-(4-chlorophenyl)-4-cyano-1-methyl-5-[(1-methylethyl)sulfanyl]-1H-pyrrole-2-carboxylic acid
-
-
3-(4-chlorophenyl)-4-cyano-5-(cyclohexylsulfanyl)thiophene-2-carboxylic acid
-
-
3-(4-chlorophenyl)-4-cyano-5-(ethylsulfanyl)thiophene-2-carboxylic acid
-
-
3-(4-chlorophenyl)-4-cyano-5-(isopropylthio)thiophene-2-carboxylic acid
3-(4-chlorophenyl)-4-cyano-5-(methylsulfanyl)thiophene-2-carboxylic acid
-
-
3-(4-chlorophenyl)-4-cyano-5-(morpholin-4-ylsulfanyl)thiophene-2-carboxylic acid
-
-
3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)-N-adamantylthiophene-2-carboxamide
3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
3-(4-chlorophenyl)-4-cyano-5-[(1-methylethyl)sulfanyl]furan-2-carboxylic acid
-
-
3-(4-chlorophenyl)-4-cyano-5-[(1-methylethyl)sulfanyl]thiophene-2-carboxamide
-
-
3-(4-chlorophenyl)-4-cyano-5-[(1-methylethyl)sulfanyl]thiophene-2-carboxylic acid
-
-
3-(4-chlorophenyl)-4-cyano-5-[(1-methylpropyl)sulfanyl]thiophene-2-carboxylic acid
-
-
3-(4-chlorophenyl)-4-cyano-5-[(2-methylpropyl)sulfanyl]thiophene-2-carboxylic acid
-
-
3-(4-chlorophenyl)-4-cyano-N'-[2-(methylsulfanyl)ethyl]-5-(propan-2-ylsulfanyl)thiophene-2-carbohydrazide
3-(4-chlorophenyl)-4-cyano-N-(naphthalen-1-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxamide
3-(4-chlorophenyl)-4-cyano-N-cyclopropyl-5-[(1-methylethyl)sulfanyl]thiophene-2-carboxamide
-
-
3-(4-chlorophenyl)-4-cyano-N-[2-(methylsulfanyl)ethyl]-5-(propan-2-ylsulfanyl)thiophene-2-carboxamide
3-(4-chlorophenyl)-4-ethynyl-5-(2l5-triaz-1-en-2-yn-1-yl)thiophene-2-carboxylic acid
3-(4-chlorophenyl)-4-ethynyl-5-[(1H-imidazol-4-ylacetyl)amino]thiophene-2-carboxylic acid
3-(4-chlorophenyl)-5-([[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl][[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynylthiophene-2-carboxylic acid
3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
3-allylfarnesol
-
potent inhibitor
3-allylfarnesyl diphosphate
-
IC50: 189 nM
3-hydroxy-1-[(3aR,7S,8aS)-7-methyl-3-methylidene-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]butyl acetate
-
-
3-methyl-2-[2-oxo-2-(10H-phenothiazin-10-yl)ethyl]indeno[1,2-c]pyrazol-4(2H)-one
-
most potent in vitro cytostatic activity inhibiting the growth of HCT-116, LOX IMVI and SK-MEL-5 cell lines
3-methyl-3H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(4-methanesulfonyl-benzyl)-amide
-
complete inhibition at 50 nM
3-methyl-thiophene-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(4-methanesulfonyl-benzyl)-amide
-
97% inhibition at 50 nM
3-oxo-3-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanoic acid
3-tert-butylfarnesyl diphosphate
-
IC50: 31 nM
3-[(tert-butylcarbamoyl-methyl)-(1-methyl-1H-imidazol-4-sulfonyl)-amino]-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-6-carboxylic acid
-
80% inhibition at 50 nM
3-[(tert-butylcarbamoyl-methyl)-(1-methyl-1H-imidazol-4-sulfonyl)-amino]-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-6-carboxylic acid benzylamide
-
59% inhibition at 50 nM
3-[(tert-butylcarbamoyl-methyl)-(1-methyl-1H-imidazol-4-sulfonyl)-amino]-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-6-carboxylic acid tert-butylamide
-
25% inhibition at 50 nM
3-[3-[2-([2-[1-(tert-butoxycarbonyl)piperidin-4-yl]-1-([(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]methyl)ethyl]sulfamoyl)benzyl]phenyl]propanoic acid
3-[[2-(tert-butylamino)-2-oxoethyl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino]-1-[(1-methyl-1H-imidazol-5-yl)methyl]-N-(1-methylpropyl)-1,2,3,4-tetrahydroquinoline-6-carboxamide
-
35% inhibition at 50 nM
3-[[2-(tert-butylamino)-2-oxoethyl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino]-N,N-diethyl-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinoline-6-carboxamide
-
69% inhibition at 50 nM
3-[[2-(tert-butylamino)-2-oxoethyl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino]-N-(1-methylethyl)-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinoline-6-carboxamide
-
46% inhibition at 50 nM
3-[[2-(tert-butylamino)-2-oxoethyl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino]-N-cyclohexyl-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinoline-6-carboxamide
-
66% inhibition at 50 nM
3-[[2-(tert-butylamino)-2-oxoethyl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino]-N-methyl-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinoline-6-carboxamide
-
69% inhibition at 50 nM
4,4-(biphenyldiglyoxaldehyde)
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-(3-cyclohexylpropanoyl)-N-(pyridin-3-ylmethyl)piperazine-2-carboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-(4-oxopentanoyl)-N-(pyridin-3-ylmethyl)piperazine-2-carboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-(5-oxohexanoyl)-N-(pyridin-3-ylmethyl)piperazine-2-carboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-(6-oxoheptanoyl)-N-(pyridin-3-ylmethyl)piperazine-2-carboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-(cycloheptylcarbonyl)-N-(pyridin-3-ylmethyl)piperazine-2-carboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-(cyclopentylcarbonyl)-N-(pyridin-3-ylmethyl)piperazine-2-carboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-(ethoxyacetyl)-N-(pyridin-3-ylmethyl)piperazine-2-carboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-hexanoyl-N-(pyridin-3-ylmethyl)piperazine-2-carboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-pentanoyl-N-(pyridin-3-ylmethyl)piperazine-2-carboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-pentanoyl-N-pyrazin-2-ylpiperazine-2-carboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-pentanoyl-N-pyridin-3-ylpiperazine-2-carboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-[(3,3-dihydroxycyclobutyl)carbonyl]-N-(pyridin-3-ylmethyl)piperazine-2-carboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-[4-(dimethylamino)-4-oxobutanoyl]-N-(pyridin-3-ylmethyl)piperazine-2-carboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-N-(1-oxidopyridin-3-yl)-1-pentanoylpiperazine-2-carboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-N-(1H-imidazol-4-ylmethyl)-1-pentanoylpiperazine-2-carboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-N-(2,5-dihydro-1H-imidazol-5-ylmethyl)-1-pentanoylpiperazine-2-carboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-N-isoxazol-5-yl-1-pentanoylpiperazine-2-carboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-N-[2-(1H-imidazol-4-yl)ethyl]-1-pentanoylpiperazine-2-carboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-N1-(1-methylethyl)-N2-(pyridin-3-ylmethyl)piperazine-1,2-dicarboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-N1-(2-methylpropyl)-N2-(pyridin-3-ylmethyl)piperazine-1,2-dicarboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-N1-(cyclohexylmethyl)-N2-(pyridin-3-ylmethyl)piperazine-1,2-dicarboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-N1-butyl-N2-(pyridin-3-ylmethyl)piperazine-1,2-dicarboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-N1-cycloheptyl-N2-(pyridin-3-ylmethyl)piperazine-1,2-dicarboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-N1-cyclohexyl-N2-(pyridin-3-ylmethyl)piperazine-1,2-dicarboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-N1-cyclohexyl-N2-[(3,5-dimethylisoxazol-4-yl)methyl]piperazine-1,2-dicarboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-N1-cyclohexyl-N2-[2-(1-methyl-1H-imidazol-5-yl)ethyl]piperazine-1,2-dicarboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-N1-cyclohexyl-N2-[2-(1H-imidazol-4-yl)ethyl]piperazine-1,2-dicarboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-N1-cyclohexyl-N2-[2-(6-methylpyridin-3-yl)ethyl]piperazine-1,2-dicarboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-N1-cyclohexyl-N2-[3-(1H-imidazol-4-yl)propyl]piperazine-1,2-dicarboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-N1-cyclohexyl-N2-[3-(2-oxopyrrolidin-1-yl)propyl]piperazine-1,2-dicarboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-N1-cyclopentyl-N2-(pyridin-3-ylmethyl)piperazine-1,2-dicarboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-N1-cyclopropyl-N2-(pyridin-3-ylmethyl)piperazine-1,2-dicarboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-N1-propyl-N2-(pyridin-3-ylmethyl)piperazine-1,2-dicarboxamide
-
-
4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-N1-tert-butyl-N2-(pyridin-3-ylmethyl)piperazine-1,2-dicarboxamide
-
-
4-(3-{[(4-cyano-3-naphthalen-1-yl-phenyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-methyl}-phenyl)-pyridine-2-carbonitrile
-
IC50: 0.37 nM, selective inhibitor
4-(4-chlorophenyl)-2-[(1-methylethyl)sulfanyl]-1,3-thiazole-5-carboxylic acid
-
-
4-(4-chlorophenyl)-5-(hydroxyacetyl)-2-[(1-methylethyl)sulfanyl]thiophene-3-carbonitrile
-
-
4-(4-chlorophenyl)-5-(methoxyacetyl)-2-[(1-methylethyl)sulfanyl]thiophene-3-carbonitrile
-
-
4-([(2-carboxy-furan-5-sulfonyl)-[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-amino]-methyl)-piperidine-1-carboxylic acid methyl ester
-
89% inhibition at 50 nM
4-([(benzo[1,2,5]oxadiazole-4-sulfonyl)-[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-amino]-methyl)-piperidine-1-carboxylic acid methyl ester
-
99% inhibition at 50 nM
4-([(benzo[1,2,5]thiadiazole-4-sulfonyl)-[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-amino]-methyl)-piperidine-1-carboxylic acid methyl ester
-
98% inhibition at 50 nM
4-([[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-cyclopropanesulfonyl-amino]-methyl)-piperidine-1-carboxylic acid methyl ester
-
37% inhibition at 50 nM
4-([[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-ethanesulfonyl-amino]-methyl)-piperidine-1-carboxylic acid methyl ester
-
44% inhibition at 50 nM
4-([[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-methanesulfonylmethanesulfonyl-amino]-methyl)-piperidine-1-carboxylic acid methyl ester
-
15% inhibition at 50 nM
4-cyano-3-(3,4-dihydroxyphenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
4-cyano-3-(3-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
4-cyano-3-(4-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
4-cyano-3-(4-methoxyphenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
4-cyano-3-(dibenzo[b,d]furan-1-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
4-cyano-3-(dibenzo[b,d]furan-4-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
4-cyano-3-(naphthalen-2-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
4-cyano-3-[3-(methoxycarbonyl)phenyl]-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
4-cyano-5-(propan-2-ylsulfanyl)-3-(3,4,5-trihydroxyphenyl)thiophene-2-carboxylic acid
4-ethynyl-5-([[1-(4-nitrobenzyl)-1H-imidazol-5-yl]methyl]amino)-3-phenylthiophene-2-carboxylic acid
4-oxo-4-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]butanoic acid
4-[(3'-Chloro-biphenyl-3-ylmethyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile
-
IC50: 0.45 nM, selective inhibitor
4-[(3-cyano-benzyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile
-
IC50: 0.39 nM, selective inhibitor
4-[(3-Methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile
-
IC50: 31 nM
4-[(4-cyano-benzyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile
-
IC50: 1.5 nM, selective inhibitor
4-[(5-[[4-(10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-yl)azepan-1-yl]methyl]-1H-imidazol-1-yl)methyl]benzonitrile
-
-
4-[(5-[[4-(10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-yl)piperidin-1-yl]methyl]-1H-imidazol-1-yl)methyl]benzonitrile
-
-
4-[(5-[[4-(5-oxido-7-propyl-7,12-dihydrodibenzo[c,f][1,2,8]oxathiazocin-12-yl)azepan-1-yl]methyl]-1H-imidazol-1-yl)methyl]benzonitrile
-
-
4-[(5-[[4-(7-butyl-5-oxido-7,12-dihydrodibenzo[c,f][1,2,8]oxathiazocin-12-yl)azepan-1-yl]methyl]-1H-imidazol-1-yl)methyl]benzonitrile
-
-
4-[(5-[[4-(7-methyl-5-oxido-7,12-dihydrodibenzo[c,f][1,2,8]oxathiazocin-12-yl)azepan-1-yl]methyl]-1H-imidazol-1-yl)methyl]benzonitrile
-
-
4-[(5-[[4-(7-methyl-5-oxido-7,12-dihydrodibenzo[c,f][1,2,8]oxathiazocin-12-yl)piperidin-1-yl]methyl]-1H-imidazol-1-yl)methyl]benzonitrile
-
-
4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]benzoic acid
-
66% inhibition at 50 nM
4-[2-[4-(3-chlorophenyl)-3-oxopiperazin-1-yl]-2-(1H-imidazol-5-yl)ethyl]benzonitrile
binds into the CAAX peptide site and competes with the CAAX substrate of FTase; binds into the CAAX peptide site and competes with the CAAX substrate of FTase
4-[5-(4,6-dimethoxy-1,3,5-triazin-2-yl)-1,2-oxazol-3-yl]-N,N-dimethylaniline
in a model structure, the dimethylamine is in front of the zinc atom. The conformation is stabilized by two well-conserved hydrogen bond groups, one from the triazine to Arg 702
4-[Biphenyl-3-ylmethyl-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile
-
IC50: 1.5 nM
4-[Hexyl-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile
-
IC50: 1.9 nM
4-[Methyl-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile
-
IC50: 38 nM
4-[N, N -bis((1H-imidazol-4-yl)methyl)aminomethyl]-2-(1-(o-tolyl))benzoylmethionine trifluoroacetate
-
IC50: 1.7 nM
4-[N-(1-H-imidazol-4-yl)methylamino]-2-(2-methoxyphenyl)-benzoylmethionine
-
IC50: 9.5 nM
4-[N-(1-H-imidazol-4-yl)methylamino]-2-(2-methylphenyl)-benzoylmethionine
-
IC50: 2.8 nM
4-[N-(1H-imidazol-4-yl)methylamino]-2-phenylbenzoylmethionine
-
IC50: 28 nM
4-[[(6-cyano-1-pyridin-3-ylmethyl-1,2,3,4-tetrahydro-quinolin-3-yl)-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid methyl ester
-
35% inhibition at 50 nM
4-[[4-([[4-(4-chlorophenyl)-3-ethynylthiophen-2-yl]amino]methyl)-1H-imidazol-1-yl]methyl]benzonitrile
4-[[5-([4-[7-(3-morpholin-4-ylpropyl)-5-oxido-7,12-dihydrodibenzo[c,f][1,2,8]oxathiazocin-12-yl]azepan-1-yl]methyl)-1H-imidazol-1-yl]methyl]benzonitrile
-
-
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(1,5-dimethyl-1H-imidazole-4-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid methyl ester
-
complete inhibition at 50 nM
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(1,5-dimethyl-1H-imidazole-4-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid tert-butyl ester
-
98% inhibition at 50 nM
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(2-oxo-2H-chromene-6-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid methyl ester
-
68% inhibition at 50 nM
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(3,4-dihydro-2H-benzo[b][1,4]dioxepine-7-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid methyl ester
-
99% inhibition at 50 nM
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(3-methyl-3H-imidazole-4-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid methyl ester
-
99% inhibition at 50 nM
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid ethylamide
-
98% inhibition at 50 nM
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid isobutyl ester
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid methyl ester
4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]-N,N-dimethylpiperidine-1-carboxamide
-
complete inhibition at 50 nM
4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]-N-(1-methylethyl)piperidine-1-carboxamide
-
complete inhibition at 50 nM
4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]-N-ethylpiperidine-1-carboxamide
5,7-dihydroxy-2-[(5R)-1-hydroxy-5-[[(3S,8aS)-3-hydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-2-methoxy-6-methyl-4-oxo-1,5,8,8a-tetrahydronaphthalen-4a(4H)-yl]-4H-chromen-4-one
-
-
5,7-dihydroxy-2-[(5R)-1-hydroxy-5-[[(3S,8aS)-3-hydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-6-methyl-2-oxo-1,5,8,8a-tetrahydronaphthalen-4a(2H)-yl]-4H-chromen-4-one
-
-
5,9,13-trimethyl-8,12-tetradecadiene-2,3-dione
-
0.093 mM causes a 94% reduction in enzyme activity after 30 min
5,9-dimethyl-8-decene-2,3-dione
-
0.017 mM causes a 62% reduction in enzyme activity after 30 min
5-(4,6-dimethoxy-1,3,5-triazin-2-yl)-1-(4-methoxyphenyl)pyrrolidin-2-thione
in S-configuration, the compound binds rather low in the site of the enzyme, at the end of the farnesyldiphosphate far from the zinc. In R-configuration, there is a hydrogen bond between one the methoxy groups and Arg 702
5-(4,6-dimethoxy-1,3,5-triazin-2-yl)-1-[3-(trifluoromethyl)phenyl]pyrrolidine-2-thione
-
5-(butan-2-yl)-3-(4-chlorophenyl)-4-cyanothiophene-2-carboxylic acid
5-(butylsulfanyl)-3-(4-chlorophenyl)-4-cyanothiophene-2-carboxylic acid
-
-
5-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynyl-3-phenylthiophene-2-carboxylic acid
5-acetyl-4-(4-chlorophenyl)-2-[(1-methylethyl)sulfanyl]thiophene-3-carbonitrile
-
-
5-methyl-3-(1-methyl-1H-imidazol-2-yl)hex-4-enoic acid
-
25% inhibition at 0.001 M
5-oxo-5-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]pentanoic acid
5-[(3-cyano-benzyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2'-methyl-biphenyl-2-carbonitrile
-
IC50: 0.97 nM, selective inhibitor
5-[(4-cyano-benzyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2'-methyl-biphenyl-2-carbonitrile
-
IC50: 10 nM, selective inhibitor
5-[(tert-butoxycarbonyl)[[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylic acid
5-[(tert-butoxycarbonyl)[[1-(4-nitrobenzyl)-1H-imidazol-4-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylic acid
5-[(tert-butoxycarbonyl)[[1-(4-nitrobenzyl)-1H-imidazol-5-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylic acid
5-[4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-2-[(pyridin-3-ylmethyl)carbamoyl]piperazin-1-yl]-5-oxopentyl acetate
-
-
6-([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)hexanamide
-
98% inhibition at 50 nM
6-[(4-hydroxyphenyl)(1H-imidazol-1-yl)methyl]-4-phenyl-1,2-dihydroquinolin-2-ol
-
-
6-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]hexanamide
-
81% inhibition at 50 nM
6-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-pyridine-2-carboxylic acid methyl ester
-
96% inhibition at 50 nM
6-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]pyridine-2-carboxylic acid
-
97% inhibition at 50 nM
alphabeta-dehydrocurvularin
-
-
benzyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
-
98% inhibition at 50 nM
Biphenyl-3-carboxylic acid (4-cyano-3-naphthalen-1-yl-phenyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amide
-
IC50: 14 nM
Biphenyl-3-sulfonic acid (4-cyano-3-naphthalen-1-yl-phenyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amide
-
IC50: 18 nM
Cys-Val-Phe-aminohexanoate
-
-
dehydrascorbic acid 6-palmitate
-
-
di-tert-butyl 2-[(2E,6E,10E)-1,3,7-trimethyl-1-(1-methyl-1H-imidazol-2-yl)dodeca-2,6,10-trien-1-yl]butanedioate
ED5
-
i.e. N-(N-tert-butoxycarbonylpiperidin-4-ylmethyl), N-(2-[((4-cyanophenyl)-3-methyl-3H-imidazol-4-ylmethyl)-amino]-ethyl) 2-methylbenzenesulfonamide, an ethylenediamine-scaffold inhibitor
ethyl (2-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-1-[2-(methylsulfanyl)ethyl]hydrazinyl)acetate
ethyl 3-(2,5-dimethoxyphenyl)-1,2-oxazole-5-carboxylate
-
ethyl 3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylate
ethyl 3-(4-chlorophenyl)-4-cyano-5-[(1-methylethyl)sulfanyl]thiophene-2-carboxylate
-
-
ethyl 3-(4-chlorophenyl)-4-ethynyl-5-(2l5-triaz-1-en-2-yn-1-yl)thiophene-2-carboxylate
ethyl 3-(4-chlorophenyl)-4-ethynyl-5-[(1H-imidazol-4-ylacetyl)amino]thiophene-2-carboxylate
ethyl 3-(4-chlorophenyl)-5-([[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl]amino)-4-ethynylthiophene-2-carboxylate
-
-
ethyl 3-(4-chlorophenyl)-5-([[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl][[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynylthiophene-2-carboxylate
ethyl 3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylate
ethyl 4-cyano-3-(dibenzo[b,d]furan-4-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylate
ethyl 4-ethynyl-5-([[1-(4-nitrobenzyl)-1H-imidazol-5-yl]methyl]amino)-3-phenylthiophene-2-carboxylate
ethyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate
-
98% inhibition at 50 nM
ethyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
ethyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
ethyl 5-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynyl-3-phenylthiophene-2-carboxylate
ethyl 5-[(tert-butoxycarbonyl)[[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylate
-
-
ethyl 5-[(tert-butoxycarbonyl)[[1-(4-nitrobenzyl)-1H-imidazol-4-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylate
-
-
ethyl 5-[(tert-butoxycarbonyl)[[1-(4-nitrobenzyl)-1H-imidazol-5-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylate
ethyl N-(tert-butoxycarbonyl)-N-[2-(methylsulfanyl)ethyl]glycinate
ethyl N-(tert-butoxycarbonyl)glycinate
ethyl [[2-([[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]amino)ethyl]sulfanyl]acetate
farnesyl diphosphate inhibitor II
-
FPT-II
farnesyltransferase inhibitors I and II
-
peptidomimemtic inhibitors, inhibitor I: 50% inhibition at 270 nM, inhibitor II: 50% inhibition at 0.97 nM
-
L-Cys-L-Val-L-Leu-L-Ser
-
-
L-penicillamine-Ile-Ile-Met
-
-
L-penicillamine-Val-Ile-Ala
-
-
L-penicillamine-Val-Ile-aminohexanoate
-
-
L-penicillamine-Val-Ile-Cys
-
-
L-penicillamine-Val-Ile-Gln
-
-
L-penicillamine-Val-Ile-homoserine
-
-
L-penicillamine-Val-Ile-Met
-
-
L-penicillamine-Val-Ile-Phe
-
-
L-penicillamine-Val-Val-Met
-
-
Lys-Lys-Cys-Val-Ile-Met
-
50% inhibition at 0.0025 mM
methyl (2S)-2-([(2S)-2-[(2-[[(2R)-2-amino-3-sulfanylpropyl]amino]-3-methylpentyl)oxy]-3-phenylpropanoyl]amino)-4-(methylsulfonyl)butanoate
a selective peptidomimetic enzme inhibitor
methyl 2-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]pyridine-4-carboxylate
-
complete inhibition at 50 nM
methyl 4-[([(2-chlorophenyl)sulfonyl][6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]amino)methyl]piperidine-1-carboxylate
-
97% inhibition at 50 nM
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1,2-dimethyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate
-
complete inhibition at 50 nM
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-2-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate
-
96% inhibition at 50 nM
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]benzoate
-
62% inhibition at 50 nM
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate
-
97% inhibition at 50 nM
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-pyrazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate
-
complete inhibition at 50 nM
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(3-fluorophenyl)sulfonyl]amino)methyl]piperidine-1-carboxylate
-
93% inhibition at 50 nM
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(3-methylthiophen-2-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate
-
95% inhibition at 50 nM
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(4-methoxyphenyl)sulfonyl]amino)methyl]piperidine-1-carboxylate
-
98% inhibition at 50 nM
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(4-methylthiophen-2-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate
-
99% inhibition at 50 nM
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][[3-(methoxycarbonyl)thiophen-2-yl]sulfonyl]amino)methyl]piperidine-1-carboxylate
-
92% inhibition at 50 nM
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate
methyl 4-[([[4-(acetylamino)phenyl]sulfonyl][6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]amino)methyl]piperidine-1-carboxylate
-
65% inhibition at 50 nM
methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
-
98% inhibition at 50 nM; complete inhibition at 50 nM
methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](dimethylsulfamoyl)amino]methyl]piperidine-1-carboxylate
-
58% inhibition at 50 nM
methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](methylsulfonyl)amino]methyl]piperidine-1-carboxylate
-
66% inhibition at 50 nM
methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](naphthalen-1-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
-
88% inhibition at 50 nM
methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](phenylsulfonyl)amino]methyl]piperidine-1-carboxylate
-
98% inhibition at 50 nM
methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](propylsulfonyl)amino]methyl]piperidine-1-carboxylate
-
55% inhibition at 50 nM
methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-3-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
-
99% inhibition at 50 nM
methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](quinolin-8-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
-
95% inhibition at 50 nM
methyl 4-[[[6-cyano-1-[1-(1H-imidazol-5-yl)ethyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
-
69% inhibition at 50 nM
methyl N-(1-cysteinylpiperidin-4-yl)-N-(phenylcarbonyl)-L-methioninate
-
IC50: 22.8 nM
methyl N-(1-[[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl]piperidin-4-yl)-N-(phenylcarbonyl)-L-isoleucinate
-
IC50: 32.7 nM
methyl N-(1-[[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl]piperidin-4-yl)-N-(phenylcarbonyl)-L-methioninate
-
IC50: 4.6 nM
methyl N-(1-[[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl]piperidin-4-yl)-N-(phenylcarbonyl)-L-phenylalaninate
-
IC50: 22 nM
methyl N-(1-[[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]piperidin-4-yl)-N-(phenylcarbonyl)-L-phenylalaninate
-
-
methyl N-(phenylcarbonyl)-N-{1-([1-[4-(trifluoromethyl)benzyl]-1H-imidazol-4-yl]methyl)piperidin-4-yl}-L-methioninate
-
IC50: 43.9 nM
methyl N-([2-[(1E,6E,10E)-4,4-bis(ethoxycarbonyl)-7,11,15-trimethylhexadeca-1,6,10,14-tetraen-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methioninate
methyl N-([2-[(6E,10E)-4,4-bis(ethoxycarbonyl)-7,11,15-trimethylhexadeca-6,10,14-trien-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methioninate
methyl N-([2-[4-ethoxy-2-(ethoxycarbonyl)-4-oxobutyl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methioninate
-
-
methyl N-([2-[4-ethoxy-2-(ethoxycarbonyl)-4-oxobutyl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-Lisoleucyl-L-alaninate
-
-
methyl N-([2-[5-ethoxy-3-(methoxycarbonyl)-5-oxopentyl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-isoleucyl-L-alaninate
-
-
methyl N-([2-[5-ethoxy-3-(methoxycarbonyl)-5-oxopentyl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methioninate
-
-
methyl N-([2-[6-ethoxy-4-(ethoxycarbonyl)-6-oxohexyl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-isoleucyl-L-alaninate
-
-
methyl N-([2-[6-ethoxy-4-(ethoxycarbonyl)-6-oxohexyl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methioninate
-
-
methyl N-([3-[methyl(1-methylidene-2,3-disulfanylpropyl)amino]-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-1-yl]acetyl)methioninate
-
-
methyl N-([5-[(tert-butoxycarbonyl)[[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophen-2-yl]carbonyl)-L-methioninate
-
-
methyl N-benzyl-N-(1-[[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl]piperidin-4-yl)-L-methioninate
-
IC50: 2.35 nM
methyl N-[(6E)-2-benzyl-5-(1-methylethyl)-8-(sulfanylmethyl)dec-6-enoyl]methioninate
-
-
methyl N-[1-[(1-benzyl-1H-imidazol-4-yl)methyl]piperidin-4-yl]-N-(phenylcarbonyl)-L-methioninate
-
IC50: 397 nM
methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonothioyl]-D-methioninate
methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-D-methioninate
methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-isoleucyl-L-methioninate
methyl N-[[3-(4-chlorophenyl)-4-ethynyl-5-(2l5-triaz-1-en-2-yn-1-yl)thiophen-2-yl]carbonyl]-L-methioninate
methyl N-[[3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methioninate
methyl N-[[4-cyano-3-(3,4-dihydroxyphenyl)-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methioninate
methyl N-[[4-cyano-3-(dibenzo[b,d]furan-4-yl)-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methioninate
methyl N-[[4-cyano-5-(propan-2-ylsulfanyl)-3-(3,4,5-trihydroxyphenyl)thiophen-2-yl]carbonyl]-L-methioninate
methyl N-[[5-(butan-2-yl)-3-(4-chlorophenyl)-4-cyanothiophen-2-yl]carbonyl]-L-methioninate
methyl N-[[5-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynyl-3-phenylthiophen-2-yl]carbonyl]-L-methioninate
methyl [2-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]ethyl]carbamate
-
90% inhibition at 50 nM
methyl [3-([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)propyl]carbamate
-
complete inhibition at 50 nM
methyl [3-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]propyl]carbamate
-
96% inhibition at 50 nM
methyl [4-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]butyl]carbamate
-
99% inhibition at 50 nM
methyl [4-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]butyl]ethylcarbamate
-
89% inhibition at 50 nM
methyl [4-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]butyl]methylcarbamate
-
90% inhibition at 50 nM
methyl [6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](2-fluorobenzyl)carbamate
-
26% inhibition at 50 nM
N'-[(1Z)-1-(3-hydroxy-1-oxo-1H-inden-2-yl)ethylidene]-3-(10H-phenothiazin-10-yl)propanehydrazide
-
-
N,1-dimethyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-1H-imidazole-4-sulfonamide
-
88% inhibition at 50 nM
N-(1-benzyl-2-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl)-1-methyl-1H-imidazole-4-sulfonamide
N-(1-benzyl-2-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl)-2-methylbenzenesulfonamide
N-(1-bromoethenyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
N-(2,1,3-benzothiadiazol-4-ylmethyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
-
99% inhibition at 50 nM
N-(2,1,3-benzothiadiazol-4-ylmethyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
-
85% inhibition at 50 nM
N-(2,1,3-benzoxadiazol-5-ylmethyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
-
99% inhibition at 50 nM
N-(2-aminoethyl)-4-([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)butanamide
-
-
N-(2-aminoethyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
-
72% inhibition at 50 nM
N-(2-aminoethyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
-
65% inhibition at 50 nM
N-(2-chloroprop-2-en-1-yl)-1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-1H-imidazole-4-sulfonamide
-
97% inhibition at 50 nM
N-(2-fluorobenzyl)-1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-1H-imidazole-4-sulfonamide
-
98% inhibition at 50 nM
N-(3-aminopropyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
-
60% inhibition at 50 nM
N-(4-bromobenzyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
-
66% inhibition at 50 nM
N-(4-bromophenyl)-4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxamide
-
38% inhibition at 50 nM
N-(4-cyanobenzyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
-
96% inhibition at 50 nM
N-([1-[(4-chlorophenyl)carbonyl]piperidin-4-yl]methyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]pyridine-2-sulfonamide
-
26% inhibition at 50 nM
N-([2-[(1E,6E,10E)-4-carboxy-4-(ethoxycarbonyl)-7,11,15-trimethylhexadeca-1,6,10,14-tetraen-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methionine
N-([2-[(6E,10E)-4-carboxy-4-(ethoxycarbonyl)-7,11,15-trimethylhexadeca-6,10,14-trien-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methionine
N-([5-[(2R)-2,3-dihydro-1,4-benzodioxin-2-ylmethoxy]-2'-methoxybiphenyl-2-yl]carbonyl)-D-methionine
-
-
N-([5-[(2R)-2,3-dihydro-1,4-benzodioxin-2-ylmethoxy]-2'-methoxybiphenyl-2-yl]carbonyl)-L-methionine
-
-
N-([5-[(2R)-2,3-dihydro-1,4-benzodioxin-2-ylmethoxy]-2'-methylbiphenyl-2-yl]carbonyl)-D-methionine
-
-
N-([5-[(2R)-2,3-dihydro-1,4-benzodioxin-2-ylmethoxy]-2'-methylbiphenyl-2-yl]carbonyl)-L-methionine
-
-
N-([5-[(2S)-2,3-dihydro-1,4-benzodioxin-2-ylmethoxy]-2'-methoxybiphenyl-2-yl]carbonyl)-D-methionine
-
-
N-([5-[(2S)-2,3-dihydro-1,4-benzodioxin-2-ylmethoxy]-2'-methoxybiphenyl-2-yl]carbonyl)-L-methionine
-
-
N-([5-[(2S)-2,3-dihydro-1,4-benzodioxin-2-ylmethoxy]-2'-methylbiphenyl-2-yl]carbonyl)-D-methionine
-
-
N-([5-[(2S)-2,3-dihydro-1,4-benzodioxin-2-ylmethoxy]-2'-methylbiphenyl-2-yl]carbonyl)-L-methionine
-
-
N-benzyl-1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-1H-imidazole-4-sulfonamide
-
99% inhibition at 50 nM
N-benzyl-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
N-butyl-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
-
32% inhibition at 50 nM
N-tert-butyl-2-[(1-methyl-1H-imidazole-4-sulfonyl)-[1-(3-methyl-3H-imidazol-4-ylmethyl)-6-phenyl-1,2,3,4-tetrahydro-quinolin-3-yl]-amino]-acetamide
-
97% inhibition at 50 nM
N-tert-butyl-4-[[[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxamide
-
22% inhibition at 50 nM
N-tert-butyl-4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxamide
-
98% inhibition at 50 nM
N-tert-butyl-N2-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N2-(methylsulfonyl)glycinamide
-
2% inhibition at 50 nM
N-tert-butyl-N2-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N2-(phenylsulfonyl)glycinamide
-
8% inhibition at 50 nM
N-tert-butyl-N2-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N2-(pyridin-2-ylsulfonyl)glycinamide
-
11% inhibition at 50 nM
N-tert-butyl-N2-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N2-(thiophen-2-ylsulfonyl)glycinamide
-
10% inhibition at 50 nM
N-tert-butyl-N2-[6-cyano-1-(1-methyl-1H-imidazol-5-yl)-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide
N-tert-butyl-N2-[6-cyano-1-(1H-imidazol-4-yl)-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide
-
15% inhibition at 50 nM
N-tert-butyl-N2-[6-cyano-1-(2,4-dimethyl-1,3-thiazol-5-yl)-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide
-
3% inhibition at 5 nM
N-tert-butyl-N2-[6-cyano-1-(4-fluorophenyl)-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide
-
71% inhibition at 50 nM
N-tert-butyl-N2-[6-cyano-1-(5-methylisoxazol-4-yl)-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide
-
3% inhibition at 50 nM
N-tert-butyl-N2-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N2-(pyridin-2-ylsulfonyl)glycinamide
N-tert-butyl-N2-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N2-(pyridin-3-ylsulfonyl)glycinamide
N-tert-butyl-N2-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N2-(pyridin-4-ylsulfonyl)glycinamide
N-tert-butyl-N2-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide
N-tert-butyl-N2-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(4-fluorophenyl)sulfonyl]glycinamide
N-tert-butyl-N2-[6-cyano-1-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide
-
60% inhibition at 50 nM
N-[(1-acetylpiperidin-4-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]pyridine-2-sulfonamide
-
94% inhibition at 50 nM
N-[(1-acetylpiperidin-4-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
N-[(1-bromonaphthalen-2-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
N-[(1-bromonaphthalen-2-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
N-[(1-butanoylpiperidin-4-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]pyridine-2-sulfonamide
N-[(1-butanoylpiperidin-4-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
N-[(2E)-but-2-en-1-yl]-1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-1H-imidazole-4-sulfonamide
-
98% inhibition at 50 nM
N-[(3-bromonaphthalen-2-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
N-[(5-[[(2R)-2,3-dihydro-1,4-benzodioxin-2-ylmethyl]carbamoyl]-2'-methoxybiphenyl-2-yl)carbonyl]-D-methionine
-
-
N-[(5-[[(2R)-2,3-dihydro-1,4-benzodioxin-2-ylmethyl]carbamoyl]-2'-methoxybiphenyl-2-yl)carbonyl]-L-methionine
-
-
N-[(5-[[(2R)-2,3-dihydro-1,4-benzodioxin-2-ylmethyl]carbamoyl]-2'-methylbiphenyl-2-yl)carbonyl]-D-methionine
-
-
N-[(5-[[(2R)-2,3-dihydro-1,4-benzodioxin-2-ylmethyl]carbamoyl]-2'-methylbiphenyl-2-yl)carbonyl]-L-methionine
-
-
N-[(5-[[(2S)-2,3-dihydro-1,4-benzodioxin-2-ylmethyl]carbamoyl]-2'-methoxybiphenyl-2-yl)carbonyl]-D-methionine
-
-
N-[(5-[[(2S)-2,3-dihydro-1,4-benzodioxin-2-ylmethyl]carbamoyl]-2'-methoxybiphenyl-2-yl)carbonyl]-L-methionine
-
-
N-[(5-[[(2S)-2,3-dihydro-1,4-benzodioxin-2-ylmethyl]carbamoyl]-2'-methylbiphenyl-2-yl)carbonyl]-D-methionine
-
-
N-[(5-[[(2S)-2,3-dihydro-1,4-benzodioxin-2-ylmethyl]carbamoyl]-2'-methylbiphenyl-2-yl)carbonyl]-L-methionine
-
-
N-[(6-chloro-2,1,3-benzothiadiazol-5-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
-
90% inhibition at 50 nM
N-[(6-chloro-2,1,3-benzothiadiazol-5-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
N-[(6E)-2-benzyl-5-(1-methylethyl)-8-(sulfanylmethyl)dec-6-enoyl]methionine
-
-
N-[1-(tert-butylamino)ethenyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
N-[2-([2-[(2-amino-3-sulfanylpropyl)amino]-3-methylbutyl]amino)-3-phenylpropyl]methionine
-
-
N-[2-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]acetyl]amino)-3-methylpentyl]-N-(naphthalen-1-ylmethyl)glycylmethionine
-
-
N-[2-chloro-4-(methylsulfonyl)benzyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
-
99% inhibition at 50 nM
N-[4-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](2-fluorobenzyl)sulfamoyl]phenyl]acetamide
-
25% inhibition at 50 nM
N-[6-bromo-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
N-[6-cyano-1-(1,2,3-thiadiazol-5-ylmethyl)-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)-1-methyl-1H-imidazole-4-carboxamide
-
66% inhibition at 50 nM
N-[6-cyano-1-(1H-imidazol-5-ylmethyl)-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)-1-methyl-1H-imidazole-4-carboxamide
-
88% inhibition at 50 nM
N-[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-2-dimethylamino-N-(2-fluoro-benzyl)-acetamide
-
16% inhibition at 50 nM
N-[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-N-(2-fluoro-benzyl)-3-methylsulfanylpropionamide
-
52% inhibition at 50 nM
N-[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-N-(2-fluoro-benzyl)-4-methoxy-benzenesulfonamide
-
66% inhibition at 50 nM
N-[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-N-(4-methanesulfonyl-benzyl)-benzenesulfonamide
-
99% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-([1-[(1-methyl-1H-imidazol-4-yl)sulfonyl]piperidin-4-yl]methyl)pyridine-2-sulfonamide
-
92% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[(1-propanoylpiperidin-4-yl)methyl]pyridine-2-sulfonamide
-
99% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(2-methylacryloyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
-
complete inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(2-methylpropanoyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
-
98% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(3,3-dimethylbutanoyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(cyclopentylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
-
complete inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(cyclopropylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
-
complete inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(ethylsulfonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
-
96% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(furan-3-ylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
-
92% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(methylsulfonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
-
98% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(phenylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(piperidin-1-ylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
-
94% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(pyrrolidin-1-ylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
-
99% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(thiophen-3-ylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
-
99% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(1-methylethenyl)-1H-imidazole-4-sulfonamide
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(2-methylbenzyl)-1H-imidazole-4-sulfonamide
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(2-phenylethyl)-1H-imidazole-4-sulfonamide
-
97% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(2-piperidin-1-ylethyl)-1H-imidazole-4-sulfonamide
-
93% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(2-thiophen-3-ylethyl)-1H-imidazole-4-sulfonamide
-
complete inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(piperidin-4-ylmethyl)-1H-imidazole-4-sulfonamide
-
65% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(pyridin-2-ylmethyl)-1H-imidazole-4-sulfonamide
-
98% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(pyridin-3-ylmethyl)-1H-imidazole-4-sulfonamide
-
99% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(quinolin-7-ylmethyl)-1H-imidazole-4-sulfonamide
-
99% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(thiophen-3-ylmethyl)-1H-imidazole-4-sulfonamide
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[(5-phenyl-1,3-oxazol-4-yl)methyl]-1H-imidazole-4-sulfonamide
-
92% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[2-(1H-pyrrol-1-yl)ethyl]-1H-imidazole-4-sulfonamide
-
99% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[2-(trifluoromethyl)benzyl]-1H-imidazole-4-sulfonamide
-
99% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[2-[2-(trifluoromethyl)phenyl]ethyl]-1H-imidazole-4-sulfonamide
-
99% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[4-(1H-1,2,4-triazol-1-yl)benzyl]-1H-imidazole-4-sulfonamide
-
93% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[4-(1H-pyrazol-1-yl)benzyl]-1H-imidazole-4-sulfonamide
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[4-(1H-pyrrol-1-yl)benzyl]-1H-imidazole-4-sulfonamide
-
99% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[4-(methylsulfonyl)benzyl]-1H-pyrazole-4-sulfonamide
-
97% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[[5-(trifluoromethyl)furan-2-yl]methyl]-1H-imidazole-4-sulfonamide
-
97% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-3-fluoro-N-[4-(methylsulfonyl)benzyl]benzenesulfonamide
-
96% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-4-methoxy-N-[4-(methylsulfonyl)benzyl]benzenesulfonamide
-
97% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-ethoxybenzyl)-1-methyl-1H-imidazole-4-sulfonamide
-
11% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)-1-methyl-1H-imidazole-4-carboxamide
-
92% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)-1-methyl-1H-imidazole-4-sulfonamide
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)-2,1,3-benzothiadiazole-4-sulfonamide
-
74% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)-2-methoxyacetamide
-
56% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)-3-(methylsulfanyl)propanamide
-
52% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)-N',N'-dimethylsulfamide
-
62% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)acetamide
-
43% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)benzenesulfonamide
-
86% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)cyclopropanecarboxamide
-
33% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)ethanesulfonamide
-
61% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)methanesulfonamide
-
51% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)propane-1-sulfonamide
-
41% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)pyridine-2-sulfonamide
-
complete inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-methylbenzyl)pyridine-2-sulfonamide
-
98% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(3-methoxypropyl)pyridine-2-sulfonamide
-
93% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(5-methoxypentyl)pyridine-2-sulfonamide
-
96% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(pyridin-2-ylmethyl)pyridine-2-sulfonamide
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(pyridin-2-ylsulfonyl)glycine
-
81% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(pyridin-3-ylmethyl)pyridine-2-sulfonamide
-
15% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(quinolin-8-ylmethyl)pyridine-2-sulfonamide
-
88% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(1-methyl-1H-imidazol-4-yl)sulfonyl]glycine
-
97% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(2-phenyl-2H-1,2,3-triazol-4-yl)methyl]pyridine-2-sulfonamide
-
97% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(3,5-dimethylisoxazol-4-yl)methyl]-1-methyl-1H-imidazole-4-sulfonamide
-
complete inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(4-phenyl-1,3-oxazol-5-yl)methyl]pyridine-2-sulfonamide
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(5-methyl-3-phenylisoxazol-4-yl)methyl]pyridine-2-sulfonamide
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(5-methylisoxazol-3-yl)methyl]pyridine-2-sulfonamide
-
94% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(5-methylisoxazol-4-yl)methyl]pyridine-2-sulfonamide
-
96% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl]-1-methyl-1H-imidazole-4-sulfonamide
-
98% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl]pyridine-2-sulfonamide
-
96% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(1H-imidazol-1-yl)ethyl]pyridine-2-sulfonamide
-
95% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(1H-indol-3-yl)ethyl]-1-methyl-1H-imidazole-4-sulfonamide
-
97% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(1H-pyrrol-1-yl)ethyl]pyridine-2-sulfonamide
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(2,3-dihydro-1,4-benzodioxin-5-yloxy)ethyl]pyridine-2-sulfonamide
-
88% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(2,3-dihydro-1H-indol-1-yl)ethyl]pyridine-2-sulfonamide
-
98% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(2,5-dihydrothiophen-3-yl)ethyl]-1-methyl-1H-imidazole-4-sulfonamide
-
complete inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(2-fluorophenyl)ethyl]pyridine-2-sulfonamide
-
98% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(4-fluorophenyl)ethyl]pyridine-2-sulfonamide
-
96% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(5,5-dimethyl-1,3-dioxan-2-yl)ethyl]pyridine-2-sulfonamide
-
95% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(dimethylamino)ethyl]-1-methyl-1H-imidazole-4-sulfonamide
-
64% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(trifluoromethyl)benzyl]pyridine-2-sulfonamide
-
91% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[3-(1H-1,2,4-triazol-1-yl)benzyl]pyridine-2-sulfonamide
-
53% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[3-(1H-pyrazol-1-yl)benzyl]pyridine-2-sulfonamide
-
90% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[3-(1H-pyrrol-1-yl)benzyl]pyridine-2-sulfonamide
-
97% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[3-(dimethylamino)propyl]-1-methyl-1H-imidazole-4-sulfonamide
-
34% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)butyl]-1-methyl-1H-imidazole-4-sulfonamide
-
97% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)butyl]pyridine-2-sulfonamide
-
92% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[4-(3,4-dimethyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)butyl]pyridine-2-sulfonamide
-
90% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[4-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)oxy]butyl]-1-methyl-1H-imidazole-4-sulfonamide
-
99% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[4-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)oxy]butyl]pyridine-2-sulfonamide
-
84% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[[5-(trifluoromethyl)furan-2-yl]methyl]pyridine-2-sulfonamide
-
84% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[4-(methylsulfonyl)benzyl]-1H-imidazole-4-sulfonamide
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-N-[4-(methylsulfonyl)benzyl]pyridine-2-sulfonamide
-
91% inhibition at 500 nM
N-[[2-(2,3-dicarboxypropyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-L-isoleucyl-L-alanine
-
-
N-[[2-(2,3-dicarboxypropyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-L-phenylalanyl-L-methionine
-
-
N-[[2-(3,4-dicarboxybutyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-L-isoleucyl-L-alanine
-
-
N-[[2-(3,4-dicarboxybutyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-L-phenylalanyl-L-methionine
-
-
N-[[2-(4,5-dicarboxypentyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-L-phenylalanyl-L-methionine
-
-
N-[[2-(4,5-dicarboxypentyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-Lisoleucyl-L-alanine
-
-
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonothioyl]-D-methionine
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-D-methionine
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-isoleucyl-L-methionine
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methionine
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-N-methyl-D-methionine
N-[[3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methionine
N-[[4-cyano-3-(dibenzo[b,d]furan-4-yl)-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methionine
N-[[4-cyano-5-(propan-2-ylsulfanyl)-3-(3,4,5-trihydroxyphenyl)thiophen-2-yl]carbonyl]-L-methionine
N-[[5-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynyl-3-phenylthiophen-2-yl]carbonyl]-L-methionine
N-{6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl}-N-(3-methoxypropyl)-1-methyl-1H-imidazole-4-sulfonamide
-
-
N2-[1-(2-aminoethyl)-6-cyano-1,2,3,4-tetrahydroquinolin-3-yl]-N-tert-butyl-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide
-
11% inhibition at 50 nM
N2-[1-[2-(acetylamino)-4-methyl-1,3-thiazol-5-yl]-6-cyano-1,2,3,4-tetrahydroquinolin-3-yl]-N-tert-butyl-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide
-
11% inhibition at 50 nM
N2-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N2-(pyridin-2-ylsulfonyl)glycinamide
-
82% inhibition at 50 nM
N2-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-glutamine
Na-[(3S)-3-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-phenylbutanoyl]-L-phenylalaninamide
-
-
pyridine-2-sulfonic acid (1-benzenesulfonyl-piperidin-4-ylmethyl)-[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-amide
-
-
pyridine-2-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(1-methanesulfonyl-piperidin-4-ylmethyl)-amide
-
99% inhibition at 50 nM
pyridine-2-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(2-pyrazol-1-ylethyl)-amide
-
99% inhibition at 50 nM
pyridine-2-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(4-fluoro-benzyl)-amide
-
91% inhibition at 50 nM
pyridine-2-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(4-methanesulfonyl-benzyl)-amide
-
96% inhibition at 50 nM
pyridine-2-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-piperidin-4-ylmethylamide
-
18% inhibition at 50 nM
pyridine-2-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-[1-(2,2-dimethylpropionyl)-piperidin-4-ylmethyl]-amide
-
99% inhibition at 50 nM
pyridine-2-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-[1-(3,3,3-trifluoropropionyl)-piperidin-4-ylmethyl]-amide
-
98% inhibition at 50 nM
pyridine-2-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-[2-(2-trifluoromethyl-phenyl)-ethyl]-amide
-
95% inhibition at 50 nM
tert-butyl (2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoate
tert-butyl 2-[2-(methylsulfanyl)ethyl]hydrazinecarboxylate
tert-butyl 4-(3-bromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-2-[(pyridin-3-ylmethyl)carbamoyl]piperazine-1-carboxylate
-
-
tert-butyl 4-(3-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]-2-[[(1-methyl-1H-imidazol-4-yl)sulfonyl]amino]propyl)piperidine-1-carboxylate
-
tert-butyl 4-(3-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]-2-[[(2-methylphenyl)sulfonyl]amino]propyl)piperidine-1-carboxylate
tert-butyl 4-[([1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate
-
33% inhibition at 50 nM
tert-butyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate
tert-butyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
-
69% inhibition at 50 nM
tert-butyl N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(phenylcarbonyl)glycinate
-
-
tert-butyl N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(1-methyl-1H-imidazol-4-yl)carbonyl]glycinate
-
-
tert-butyl N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(1-methyl-1H-imidazol-4-yl)sulfonyl]glycinate
tert-butyl N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(5-methylisoxazol-3-yl)carbonyl]glycinate
-
-
tert-butyl [2-([1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)ethyl]carbamate
-
98% inhibition at 50 nM
tert-butyl [2-([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)ethyl]carbamate
-
99% inhibition at 50 nM
tert-butyl [2-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]ethyl]carbamate
-
91% inhibition at 50 nM
tert-butyl [3-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]propyl]carbamate
-
97% inhibition at 50 nM
tert-butyl [3-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]propyl]methylcarbamate
-
86% inhibition at 50 nM
tert-butyl [4-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]butyl]carbamate
-
97% inhibition at 50 nM
tert-butyl [4-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]butyl]ethylcarbamate
-
92% inhibition at 50 nM
tert-butyl [4-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]butyl]methylcarbamate
-
98% inhibition at 50 nM
Zn2+
inhibition of human farnesyltransferase by zinc complexation can be improved with triazine-isoxazole moieties. The replacement of the isoxazole unit by a pyrrolidin-2-one is detrimental to the inhibitory activity while the pyrrolidin-2-thione derivatives conserves the biological potential
[(1-methyl-1H-imidazole-4-sulfonyl)-[1-(3-methyl-3H-imidazol-4-ylmethyl)-6-phenyl-1,2,3,4-tetrahydro-quinolin-3-yl]-amino]-acetic acid methyl ester
-
99% inhibition at 50 nM
[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ylidene]propanedioic acid
[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
[(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]sulfamic acid
[2-(4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidin-1-yl)-2-oxo-ethyl]-carbamic acid tert-butyl ester
-
88% inhibition at 50 nM
[3-(1-methyl-1H-imidazol-2-yl)propyl][(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
[3-(4-chlorophenyl)-4-cyano-5-[(1-methylethyl)sulfanyl]thiophen-2-yl]methyl acetate
-
-
[3-[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-propyl]-methyl-carbamic acid methyl ester
-
95% inhibition at 50 nM
[[(2E,4E,8E)-5,9,13-trimethyltetradeca-2,4,8,12-tetraenoyl]amino]propanedioic acid
-
-
[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanedioic acid
[[(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]amino]propanedioic acid
[[1-(3-benzyl-3H-imidazol-4-ylmethyl)-6-cyano-1,2,3,4-tetrahydro-quinolin-3-yl]-(1-methyl-1H-imidazole-4-sulfonyl)-amino]-acetic acid tert-butyl ester
-
45% inhibition at 5 nM
[[2-([[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]amino)ethyl]sulfanyl]acetic acid
(2-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-1-[2-(methylsulfanyl)ethyl]hydrazinyl)acetic acid
-
-
(2-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-1-[2-(methylsulfanyl)ethyl]hydrazinyl)acetic acid
-
-
(2E)-2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ylidene]butanedioic acid
-
-
(2E)-2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ylidene]butanedioic acid
-
-
(2E,4E,8E)-5,9,13-trimethyltetradeca-2,4,8,12-tetraenoic acid
-
-
(2E,4E,8E)-5,9,13-trimethyltetradeca-2,4,8,12-tetraenoic acid
-
-
(2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoic acid
-
-
(2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoic acid
-
-
(4E,8E)-2-(ethoxycarbonyl)-5,9,13-trimethyl-2-[3-(1-methyl-1H-imidazol-2-yl)propyl]tetradeca-4,8,12-trienoic acid
-
-
(4E,8E)-2-(ethoxycarbonyl)-5,9,13-trimethyl-2-[3-(1-methyl-1H-imidazol-2-yl)propyl]tetradeca-4,8,12-trienoic acid
-
50% growth inhibition at 0.004 mM
(4E,8E)-2-(ethoxycarbonyl)-5,9,13-trimethyl-2-[3-(1-methyl-1H-imidazol-2-yl)propyl]tetradeca-4,8,12-trienoic acid
-
-
(4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-4,8,12-trienoic acid
-
-
(4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-4,8,12-trienoic acid
-
-
(4E,8E)-5,9,13-trimethyl-N-(phenylsulfonyl)tetradeca-4,8,12-trienamide
-
-
(4E,8E)-5,9,13-trimethyl-N-(phenylsulfonyl)tetradeca-4,8,12-trienamide
-
-
(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoic acid
-
-
(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoic acid
-
-
(4S)-4-([[5-(butan-2-yl)-3-(4-chlorophenyl)-4-cyanothiophen-2-yl]carbonyl]amino)-5-tert-butoxy-5-oxopentanoic acid
-
-
(4S)-4-([[5-(butan-2-yl)-3-(4-chlorophenyl)-4-cyanothiophen-2-yl]carbonyl]amino)-5-tert-butoxy-5-oxopentanoic acid
-
-
(6E,10E)-7,11,15-trimethyl-3-oxohexadeca-6,10,14-trienoic acid
-
-
(6E,10E)-7,11,15-trimethyl-3-oxohexadeca-6,10,14-trienoic acid
-
-
(7E,11E)-8,12,16-trimethyl-4-oxoheptadeca-7,11,15-trienoic acid
-
-
(7E,11E)-8,12,16-trimethyl-4-oxoheptadeca-7,11,15-trienoic acid
-
-
1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(5-methylisoxazol-4-yl)methyl]-1H-imidazole-4-sulfonamide
-
79% inhibition at 50 nM
1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(5-methylisoxazol-4-yl)methyl]-1H-imidazole-4-sulfonamide
-
-
1-methylethyl 4-[([1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate
-
32% inhibition at 50 nM
1-methylethyl 4-[([1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate
-
-
2-methylpropyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
-
-
2-methylpropyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
-
2-[(2E)-3,7-dimethyl-1-(1-methyl-1H-imidazol-2-yl)octa-2,6-dien-1-yl]butanedioic acid
-
-
2-[(2E)-3,7-dimethyl-1-(1-methyl-1H-imidazol-2-yl)octa-2,6-dien-1-yl]butanedioic acid
-
-
2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]butanedioic acid
-
-
2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]butanedioic acid
-
-
3-(4-chlorophenyl)-4-cyano-5-(isopropylthio)thiophene-2-carboxylic acid
-
-
3-(4-chlorophenyl)-4-cyano-5-(isopropylthio)thiophene-2-carboxylic acid
-
-
3-(4-chlorophenyl)-4-cyano-5-(isopropylthio)thiophene-2-carboxylic acid
-
-
3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)-N-adamantylthiophene-2-carboxamide
-
-
3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)-N-adamantylthiophene-2-carboxamide
-
-
3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
3-(4-chlorophenyl)-4-cyano-N'-[2-(methylsulfanyl)ethyl]-5-(propan-2-ylsulfanyl)thiophene-2-carbohydrazide
-
-
3-(4-chlorophenyl)-4-cyano-N'-[2-(methylsulfanyl)ethyl]-5-(propan-2-ylsulfanyl)thiophene-2-carbohydrazide
-
-
3-(4-chlorophenyl)-4-cyano-N-(naphthalen-1-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxamide
-
-
3-(4-chlorophenyl)-4-cyano-N-(naphthalen-1-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxamide
-
-
3-(4-chlorophenyl)-4-cyano-N-[2-(methylsulfanyl)ethyl]-5-(propan-2-ylsulfanyl)thiophene-2-carboxamide
-
-
3-(4-chlorophenyl)-4-cyano-N-[2-(methylsulfanyl)ethyl]-5-(propan-2-ylsulfanyl)thiophene-2-carboxamide
-
-
3-(4-chlorophenyl)-4-ethynyl-5-(2l5-triaz-1-en-2-yn-1-yl)thiophene-2-carboxylic acid
-
-
3-(4-chlorophenyl)-4-ethynyl-5-(2l5-triaz-1-en-2-yn-1-yl)thiophene-2-carboxylic acid
-
-
3-(4-chlorophenyl)-4-ethynyl-5-[(1H-imidazol-4-ylacetyl)amino]thiophene-2-carboxylic acid
-
-
3-(4-chlorophenyl)-4-ethynyl-5-[(1H-imidazol-4-ylacetyl)amino]thiophene-2-carboxylic acid
-
-
3-(4-chlorophenyl)-5-([[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl][[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynylthiophene-2-carboxylic acid
-
-
3-(4-chlorophenyl)-5-([[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl][[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynylthiophene-2-carboxylic acid
-
-
3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
3-oxo-3-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanoic acid
-
-
3-oxo-3-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanoic acid
-
-
3-[3-[2-([2-[1-(tert-butoxycarbonyl)piperidin-4-yl]-1-([(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]methyl)ethyl]sulfamoyl)benzyl]phenyl]propanoic acid
-
-
3-[3-[2-([2-[1-(tert-butoxycarbonyl)piperidin-4-yl]-1-([(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]methyl)ethyl]sulfamoyl)benzyl]phenyl]propanoic acid
-
-
4-cyano-3-(3,4-dihydroxyphenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
4-cyano-3-(3,4-dihydroxyphenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
4-cyano-3-(3-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
4-cyano-3-(3-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
4-cyano-3-(3-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
4-cyano-3-(4-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
4-cyano-3-(4-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
4-cyano-3-(4-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
4-cyano-3-(4-methoxyphenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
4-cyano-3-(4-methoxyphenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
4-cyano-3-(4-methoxyphenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
4-cyano-3-(dibenzo[b,d]furan-1-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
4-cyano-3-(dibenzo[b,d]furan-1-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
4-cyano-3-(dibenzo[b,d]furan-1-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
4-cyano-3-(dibenzo[b,d]furan-4-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
4-cyano-3-(dibenzo[b,d]furan-4-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
4-cyano-3-(naphthalen-2-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
4-cyano-3-(naphthalen-2-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
4-cyano-3-(naphthalen-2-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
4-cyano-3-[3-(methoxycarbonyl)phenyl]-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
4-cyano-3-[3-(methoxycarbonyl)phenyl]-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
4-cyano-3-[3-(methoxycarbonyl)phenyl]-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
-
4-cyano-5-(propan-2-ylsulfanyl)-3-(3,4,5-trihydroxyphenyl)thiophene-2-carboxylic acid
-
-
4-cyano-5-(propan-2-ylsulfanyl)-3-(3,4,5-trihydroxyphenyl)thiophene-2-carboxylic acid
-
-
4-ethynyl-5-([[1-(4-nitrobenzyl)-1H-imidazol-5-yl]methyl]amino)-3-phenylthiophene-2-carboxylic acid
-
-
4-ethynyl-5-([[1-(4-nitrobenzyl)-1H-imidazol-5-yl]methyl]amino)-3-phenylthiophene-2-carboxylic acid
-
-
4-oxo-4-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]butanoic acid
-
-
4-oxo-4-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]butanoic acid
-
-
4-[[4-([[4-(4-chlorophenyl)-3-ethynylthiophen-2-yl]amino]methyl)-1H-imidazol-1-yl]methyl]benzonitrile
-
-
4-[[4-([[4-(4-chlorophenyl)-3-ethynylthiophen-2-yl]amino]methyl)-1H-imidazol-1-yl]methyl]benzonitrile
-
-
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid isobutyl ester
-
complete inhibition at 50 nM
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid isobutyl ester
-
-
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid methyl ester
-
complete inhibition at 50 nM
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid methyl ester
-
-
4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]-N-ethylpiperidine-1-carboxamide
-
-
4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]-N-ethylpiperidine-1-carboxamide
-
5-(butan-2-yl)-3-(4-chlorophenyl)-4-cyanothiophene-2-carboxylic acid
-
-
5-(butan-2-yl)-3-(4-chlorophenyl)-4-cyanothiophene-2-carboxylic acid
-
-
5-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynyl-3-phenylthiophene-2-carboxylic acid
-
-
5-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynyl-3-phenylthiophene-2-carboxylic acid
-
-
5-oxo-5-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]pentanoic acid
-
-
5-oxo-5-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]pentanoic acid
-
-
5-[(tert-butoxycarbonyl)[[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylic acid
-
-
5-[(tert-butoxycarbonyl)[[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylic acid
-
-
5-[(tert-butoxycarbonyl)[[1-(4-nitrobenzyl)-1H-imidazol-4-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylic acid
-
-
5-[(tert-butoxycarbonyl)[[1-(4-nitrobenzyl)-1H-imidazol-4-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylic acid
-
-
5-[(tert-butoxycarbonyl)[[1-(4-nitrobenzyl)-1H-imidazol-5-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylic acid
-
-
5-[(tert-butoxycarbonyl)[[1-(4-nitrobenzyl)-1H-imidazol-5-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylic acid
-
-
acetylshikonin
-
inhibits FTPase activity in a dose-dependent manner
acetylshikonin
-
inhibits FTPase activity in a dose-dependent manner
BMS-214662
-
-
BMS-214662
bind into the CAAX peptide site and compete with the CAAX substrate of FTase; bind into the CAAX peptide site and compete with the CAAX substrate of FTase
BMS-214662
-
the commercial name is Zamestra
chaetomellic acid A
competitive inhibitor
deoxyshikonin
-
inhibits FTPase activity in a dose-dependent manner
deoxyshikonin
-
inhibits FTPase activity in a dose-dependent manner
di-tert-butyl 2-[(2E,6E,10E)-1,3,7-trimethyl-1-(1-methyl-1H-imidazol-2-yl)dodeca-2,6,10-trien-1-yl]butanedioate
-
-
di-tert-butyl 2-[(2E,6E,10E)-1,3,7-trimethyl-1-(1-methyl-1H-imidazol-2-yl)dodeca-2,6,10-trien-1-yl]butanedioate
-
50% growth inhibition at 0.03 mM
di-tert-butyl 2-[(2E,6E,10E)-1,3,7-trimethyl-1-(1-methyl-1H-imidazol-2-yl)dodeca-2,6,10-trien-1-yl]butanedioate
-
-
EDTA
-
-
ethyl (2-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-1-[2-(methylsulfanyl)ethyl]hydrazinyl)acetate
-
-
ethyl (2-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-1-[2-(methylsulfanyl)ethyl]hydrazinyl)acetate
-
-
ethyl 3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylate
-
-
ethyl 3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylate
-
-
ethyl 3-(4-chlorophenyl)-4-ethynyl-5-(2l5-triaz-1-en-2-yn-1-yl)thiophene-2-carboxylate
-
-
ethyl 3-(4-chlorophenyl)-4-ethynyl-5-(2l5-triaz-1-en-2-yn-1-yl)thiophene-2-carboxylate
-
-
ethyl 3-(4-chlorophenyl)-4-ethynyl-5-[(1H-imidazol-4-ylacetyl)amino]thiophene-2-carboxylate
-
-
ethyl 3-(4-chlorophenyl)-4-ethynyl-5-[(1H-imidazol-4-ylacetyl)amino]thiophene-2-carboxylate
-
-
ethyl 3-(4-chlorophenyl)-5-([[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl][[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynylthiophene-2-carboxylate
-
-
ethyl 3-(4-chlorophenyl)-5-([[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl][[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynylthiophene-2-carboxylate
-
-
ethyl 3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylate
-
-
ethyl 3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylate
-
-
ethyl 4-cyano-3-(dibenzo[b,d]furan-4-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylate
-
-
ethyl 4-cyano-3-(dibenzo[b,d]furan-4-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylate
-
-
ethyl 4-ethynyl-5-([[1-(4-nitrobenzyl)-1H-imidazol-5-yl]methyl]amino)-3-phenylthiophene-2-carboxylate
-
-
ethyl 4-ethynyl-5-([[1-(4-nitrobenzyl)-1H-imidazol-5-yl]methyl]amino)-3-phenylthiophene-2-carboxylate
-
-
ethyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
-
complete inhibition at 50 nM
ethyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
-
-
ethyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
-
-
ethyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
-
ethyl 5-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynyl-3-phenylthiophene-2-carboxylate
-
-
ethyl 5-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynyl-3-phenylthiophene-2-carboxylate
-
-
ethyl 5-[(tert-butoxycarbonyl)[[1-(4-nitrobenzyl)-1H-imidazol-5-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylate
-
-
ethyl 5-[(tert-butoxycarbonyl)[[1-(4-nitrobenzyl)-1H-imidazol-5-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylate
-
-
ethyl N-(tert-butoxycarbonyl)-N-[2-(methylsulfanyl)ethyl]glycinate
-
-
ethyl N-(tert-butoxycarbonyl)-N-[2-(methylsulfanyl)ethyl]glycinate
-
-
ethyl N-(tert-butoxycarbonyl)glycinate
-
-
ethyl N-(tert-butoxycarbonyl)glycinate
-
-
ethyl [[2-([[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]amino)ethyl]sulfanyl]acetate
-
-
ethyl [[2-([[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]amino)ethyl]sulfanyl]acetate
-
-
FTI-2148
-
IC50: 0.86 nM
FTI-276
-
-
FTI-276
-
about 2fold more potent on parasite enzyme than on mammalian enzyme
FTI-276
-
about 2fold more potent on parasite enzyme than on mammalian enzyme
FTI-277
-
-
FTI-277
-
inhibition with potencies 10fold higher on parasite enzyme than on mammalian enzyme, however growth of bloodstream Trypanosoma brucei completely inhibited with 0.001 mM
FTI-277
-
inhibition with potencies 10fold higher on parasite enzyme than on mammalian enzyme, however growth of bloodstream Trypanosoma brucei completely inhibited with 0.001 mM
GGTI-297
-
inhibition with potencies 10fold higher on parasite enzyme than on mammalian enzyme
GGTI-297
-
inhibition with potencies 10fold higher on parasite enzyme than on mammalian enzyme
GGTI-298
-
-
GGTI-298
-
inhibition with potencies 10fold higher on parasite enzyme than on mammalian enzyme, however growth of bloodstream Trypanosoma brucei cmpletely inhibited with 0.005 mM
GGTI-298
-
inhibition with potencies 10fold higher on parasite enzyme than on mammalian enzyme, however growth of bloodstream Trypanosoma brucei cmpletely inhibited with 0.005 mM
KTSCVAM
-
40% inhibition of farnesylation in Toxoplasma gondii, 100% inhibition of enzyme in HeLa cells
KTSCVAM
-
40% inhibition of farnesylation in Toxoplasma gondii, 100% inhibition of enzyme in HeLa cells
KTSCVFM
-
80% inhibition of farnesylation in Toxoplasma gondii and 80% inhibition of enzyme in HeLa cells
KTSCVFM
-
80% inhibition of farnesylation in Toxoplasma gondii and 80% inhibition of enzyme in HeLa cells
KTSCVIA
-
50% inhibition of farnesylation in Toxoplasma gondii and no inhibition of enzyme in HeLa cells
KTSCVIA
-
50% inhibition of farnesylation in Toxoplasma gondii and no inhibition of enzyme in HeLa cells
KTSCVIF
-
no inhibition of farnesylation in Toxoplasma gondii, 80% inhibition of enzyme in HeLa cells
KTSCVIF
-
no inhibition of farnesylation in Toxoplasma gondii, 80% inhibition of enzyme in HeLa cells
KTSSVIM
-
80% inhibition of farnesylation in Toxoplasma gondii, 100% inhibition of enzyme in HeLa cells
KTSSVIM
-
80% inhibition of farnesylation in Toxoplasma gondii, 100% inhibition of enzyme in HeLa cells
L-739,750
-
-
L-745,631
-
similarly potent on parasite enzyme and on mammalian enzyme
L-745,631
-
similarly potent on parasite enzyme and on mammalian enzyme
lonafarnib
-
SCH-66336
lonafarnib
active in Ras-dependent and -independent malignant tumors; active in Ras-dependent and -independent malignant tumors
manumycin
-
-
manumycin
-
inhibition at concentration as low as 0.0025 mM, inhibitor most likely to affect only the processes that involve protein isoprenylation
manumycin A
specific PFT inhibitor
manumycin A
-
notable growth inhibition, application disrupts Ras1 localization in vivo
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate
-
98% inhibition at 500 nM
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate
-
85% inhibition at 0.005 mM
methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
-
-
methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
-
methyl N-([2-[(1E,6E,10E)-4,4-bis(ethoxycarbonyl)-7,11,15-trimethylhexadeca-1,6,10,14-tetraen-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methioninate
-
50% growth inhibition at 0.0011 mM
methyl N-([2-[(1E,6E,10E)-4,4-bis(ethoxycarbonyl)-7,11,15-trimethylhexadeca-1,6,10,14-tetraen-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methioninate
-
-
methyl N-([2-[(6E,10E)-4,4-bis(ethoxycarbonyl)-7,11,15-trimethylhexadeca-6,10,14-trien-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methioninate
-
50% growth inhibition at 0.001 mM
methyl N-([2-[(6E,10E)-4,4-bis(ethoxycarbonyl)-7,11,15-trimethylhexadeca-6,10,14-trien-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methioninate
-
-
methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonothioyl]-D-methioninate
-
-
methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonothioyl]-D-methioninate
-
-
methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-D-methioninate
-
-
methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-D-methioninate
-
-
methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-isoleucyl-L-methioninate
-
-
methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-isoleucyl-L-methioninate
-
-
methyl N-[[3-(4-chlorophenyl)-4-ethynyl-5-(2l5-triaz-1-en-2-yn-1-yl)thiophen-2-yl]carbonyl]-L-methioninate
-
-
methyl N-[[3-(4-chlorophenyl)-4-ethynyl-5-(2l5-triaz-1-en-2-yn-1-yl)thiophen-2-yl]carbonyl]-L-methioninate
-
-
methyl N-[[3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methioninate
-
-
methyl N-[[3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methioninate
-
-
methyl N-[[4-cyano-3-(3,4-dihydroxyphenyl)-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methioninate
-
-
methyl N-[[4-cyano-3-(3,4-dihydroxyphenyl)-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methioninate
-
-
methyl N-[[4-cyano-3-(dibenzo[b,d]furan-4-yl)-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methioninate
-
-
methyl N-[[4-cyano-3-(dibenzo[b,d]furan-4-yl)-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methioninate
-
-
methyl N-[[4-cyano-5-(propan-2-ylsulfanyl)-3-(3,4,5-trihydroxyphenyl)thiophen-2-yl]carbonyl]-L-methioninate
-
-
methyl N-[[4-cyano-5-(propan-2-ylsulfanyl)-3-(3,4,5-trihydroxyphenyl)thiophen-2-yl]carbonyl]-L-methioninate
-
-
methyl N-[[5-(butan-2-yl)-3-(4-chlorophenyl)-4-cyanothiophen-2-yl]carbonyl]-L-methioninate
-
-
methyl N-[[5-(butan-2-yl)-3-(4-chlorophenyl)-4-cyanothiophen-2-yl]carbonyl]-L-methioninate
-
-
methyl N-[[5-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynyl-3-phenylthiophen-2-yl]carbonyl]-L-methioninate
-
-
methyl N-[[5-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynyl-3-phenylthiophen-2-yl]carbonyl]-L-methioninate
-
-
N-(1-benzyl-2-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl)-1-methyl-1H-imidazole-4-sulfonamide
-
-
N-(1-benzyl-2-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl)-1-methyl-1H-imidazole-4-sulfonamide
-
-
N-(1-benzyl-2-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl)-2-methylbenzenesulfonamide
-
-
N-(1-benzyl-2-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl)-2-methylbenzenesulfonamide
-
-
N-(1-bromoethenyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
-
-
N-(1-bromoethenyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
-
N-([2-[(1E,6E,10E)-4-carboxy-4-(ethoxycarbonyl)-7,11,15-trimethylhexadeca-1,6,10,14-tetraen-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methionine
-
-
N-([2-[(1E,6E,10E)-4-carboxy-4-(ethoxycarbonyl)-7,11,15-trimethylhexadeca-1,6,10,14-tetraen-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methionine
-
50% growth inhibition at 0.0172 mM
N-([2-[(6E,10E)-4-carboxy-4-(ethoxycarbonyl)-7,11,15-trimethylhexadeca-6,10,14-trien-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methionine
-
-
N-([2-[(6E,10E)-4-carboxy-4-(ethoxycarbonyl)-7,11,15-trimethylhexadeca-6,10,14-trien-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methionine
-
50% growth inhibition at 0.0314 mM
N-benzyl-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
-
-
N-benzyl-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
-
N-tert-butyl-N2-[6-cyano-1-(1-methyl-1H-imidazol-5-yl)-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide
-
80% inhibition at 50 nM
N-tert-butyl-N2-[6-cyano-1-(1-methyl-1H-imidazol-5-yl)-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide
-
-
N-tert-butyl-N2-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N2-(pyridin-2-ylsulfonyl)glycinamide
-
-
N-tert-butyl-N2-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N2-(pyridin-2-ylsulfonyl)glycinamide
-
N-tert-butyl-N2-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N2-(pyridin-3-ylsulfonyl)glycinamide
-
-
N-tert-butyl-N2-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N2-(pyridin-3-ylsulfonyl)glycinamide
-
N-tert-butyl-N2-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N2-(pyridin-4-ylsulfonyl)glycinamide
-
-
N-tert-butyl-N2-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N2-(pyridin-4-ylsulfonyl)glycinamide
-
N-tert-butyl-N2-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide
-
-
N-tert-butyl-N2-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide
-
N-tert-butyl-N2-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(4-fluorophenyl)sulfonyl]glycinamide
-
-
N-tert-butyl-N2-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(4-fluorophenyl)sulfonyl]glycinamide
-
N-[(1-acetylpiperidin-4-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
-
-
N-[(1-acetylpiperidin-4-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
-
N-[(1-bromonaphthalen-2-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
-
69% inhibition at 50 nM
N-[(1-bromonaphthalen-2-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
-
-
N-[(1-bromonaphthalen-2-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
-
N-[(1-bromonaphthalen-2-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
-
-
N-[(1-bromonaphthalen-2-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
-
N-[(1-butanoylpiperidin-4-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]pyridine-2-sulfonamide
-
95% inhibition at 50 nM
N-[(1-butanoylpiperidin-4-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]pyridine-2-sulfonamide
-
-
N-[(1-butanoylpiperidin-4-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
-
-
N-[(1-butanoylpiperidin-4-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
-
N-[(3-bromonaphthalen-2-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
-
55% inhibition at 50 nM
N-[(3-bromonaphthalen-2-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
-
-
N-[(6-chloro-2,1,3-benzothiadiazol-5-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
-
53% inhibition at 50 nM
N-[(6-chloro-2,1,3-benzothiadiazol-5-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
-
-
N-[(6-chloro-2,1,3-benzothiadiazol-5-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
-
-
N-[(6-chloro-2,1,3-benzothiadiazol-5-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
-
N-[1-(tert-butylamino)ethenyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
-
-
N-[1-(tert-butylamino)ethenyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
-
N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
-
19% inhibition at 50 nM
N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
-
-
N-[6-bromo-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
-
74% inhibition at 500 nM
N-[6-bromo-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
-
51% inhibition at 0.005 mM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(3,3-dimethylbutanoyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
-
96% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(3,3-dimethylbutanoyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
-
-
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(phenylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
-
94% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(phenylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
-
-
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(1-methylethenyl)-1H-imidazole-4-sulfonamide
-
-
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(1-methylethenyl)-1H-imidazole-4-sulfonamide
-
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(2-methylbenzyl)-1H-imidazole-4-sulfonamide
-
complete inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(2-methylbenzyl)-1H-imidazole-4-sulfonamide
-
-
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(2-methylbenzyl)-1H-imidazole-4-sulfonamide
-
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(thiophen-3-ylmethyl)-1H-imidazole-4-sulfonamide
-
99% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(thiophen-3-ylmethyl)-1H-imidazole-4-sulfonamide
-
-
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(thiophen-3-ylmethyl)-1H-imidazole-4-sulfonamide
-
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[4-(1H-pyrazol-1-yl)benzyl]-1H-imidazole-4-sulfonamide
-
98% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[4-(1H-pyrazol-1-yl)benzyl]-1H-imidazole-4-sulfonamide
-
-
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)-1-methyl-1H-imidazole-4-sulfonamide
-
96% inhibition at 50 nM; complete inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)-1-methyl-1H-imidazole-4-sulfonamide
-
-
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(pyridin-2-ylmethyl)pyridine-2-sulfonamide
-
complete inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(pyridin-2-ylmethyl)pyridine-2-sulfonamide
-
-
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(pyridin-2-ylmethyl)pyridine-2-sulfonamide
-
-
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(pyridin-2-ylmethyl)pyridine-2-sulfonamide
-
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(4-phenyl-1,3-oxazol-5-yl)methyl]pyridine-2-sulfonamide
-
98% inhibition at 50 nM; complete inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(4-phenyl-1,3-oxazol-5-yl)methyl]pyridine-2-sulfonamide
-
-
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(5-methyl-3-phenylisoxazol-4-yl)methyl]pyridine-2-sulfonamide
-
-
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(5-methyl-3-phenylisoxazol-4-yl)methyl]pyridine-2-sulfonamide
-
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(1H-pyrrol-1-yl)ethyl]pyridine-2-sulfonamide
-
99% inhibition at 50 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(1H-pyrrol-1-yl)ethyl]pyridine-2-sulfonamide
-
-
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
-
94% inhibition at 500 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide
-
39% inhibition at 0.005 mM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[4-(methylsulfonyl)benzyl]-1H-imidazole-4-sulfonamide
-
99% inhibition at 500 nM
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[4-(methylsulfonyl)benzyl]-1H-imidazole-4-sulfonamide
-
47% inhibition at 0.005 mM
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonothioyl]-D-methionine
-
-
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonothioyl]-D-methionine
-
-
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-D-methionine
-
-
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-D-methionine
-
-
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-isoleucyl-L-methionine
-
-
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-isoleucyl-L-methionine
-
-
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methionine
-
-
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methionine
-
-
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-N-methyl-D-methionine
-
-
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-N-methyl-D-methionine
-
-
N-[[3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methionine
-
-
N-[[3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methionine
-
-
N-[[4-cyano-3-(dibenzo[b,d]furan-4-yl)-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methionine
-
-
N-[[4-cyano-3-(dibenzo[b,d]furan-4-yl)-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methionine
-
-
N-[[4-cyano-5-(propan-2-ylsulfanyl)-3-(3,4,5-trihydroxyphenyl)thiophen-2-yl]carbonyl]-L-methionine
-
-
N-[[4-cyano-5-(propan-2-ylsulfanyl)-3-(3,4,5-trihydroxyphenyl)thiophen-2-yl]carbonyl]-L-methionine
-
-
N-[[5-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynyl-3-phenylthiophen-2-yl]carbonyl]-L-methionine
-
-
N-[[5-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynyl-3-phenylthiophen-2-yl]carbonyl]-L-methionine
-
-
N2-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-glutamine
-
-
N2-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-glutamine
-
-
R-115777
-
-
R115777
-
-
R115777
-
tipifarnid, Zarnestra
R115777
-
IC50: 0.57 nM, selective inhibitor
SCH-44342
-
-
SCH-44342
-
2 orders of magnitude less potent on parasite enzyme than on mammalian enzyme
SCH-44342
-
2 orders of magnitude less potent on parasite enzyme than on mammalian enzyme
SCH-66336
-
lonafarnib, Sarasar
SCH66336
-
-
SCH66336
-
IC50: 7.8 nM, selective inhibitor
shikonine
-
inhibits FTPase activity in a dose-dependent manner
shikonine
-
inhibits FTPase activity in a dose-dependent manner
tert-butyl (2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoate
-
-
tert-butyl (2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoate
-
-
tert-butyl 2-[2-(methylsulfanyl)ethyl]hydrazinecarboxylate
-
-
tert-butyl 2-[2-(methylsulfanyl)ethyl]hydrazinecarboxylate
-
-
tert-butyl 4-(3-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]-2-[[(1-methyl-1H-imidazol-4-yl)sulfonyl]amino]propyl)piperidine-1-carboxylate
-
-
-
tert-butyl 4-(3-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]-2-[[(1-methyl-1H-imidazol-4-yl)sulfonyl]amino]propyl)piperidine-1-carboxylate
-
-
-
tert-butyl 4-(3-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]-2-[[(2-methylphenyl)sulfonyl]amino]propyl)piperidine-1-carboxylate
-
-
tert-butyl 4-(3-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]-2-[[(2-methylphenyl)sulfonyl]amino]propyl)piperidine-1-carboxylate
-
-
tert-butyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate
-
-
tert-butyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate
-
tert-butyl N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(1-methyl-1H-imidazol-4-yl)sulfonyl]glycinate
-
-
tert-butyl N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(1-methyl-1H-imidazol-4-yl)sulfonyl]glycinate
-
tetrahydroquinoline
-
-
tipifarnib
-
an ethylenediamine-scaffold inhibitor
tipifarnib
-
notable growth inhibition
[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ylidene]propanedioic acid
-
-
[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ylidene]propanedioic acid
-
-
[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
-
-
[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
-
-
[(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]sulfamic acid
-
-
[(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]sulfamic acid
-
-
[3-(1-methyl-1H-imidazol-2-yl)propyl][(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
-
-
[3-(1-methyl-1H-imidazol-2-yl)propyl][(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
-
-
[3-(1-methyl-1H-imidazol-2-yl)propyl][(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
-
-
[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanedioic acid
-
-
[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanedioic acid
-
-
[[(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]amino]propanedioic acid
-
-
[[(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]amino]propanedioic acid
-
-
[[2-([[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]amino)ethyl]sulfanyl]acetic acid
-
-
[[2-([[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]amino)ethyl]sulfanyl]acetic acid
-
-
additional information
-
inhibitor structure-function analysis for antifungal drug design, comparisons of enzyme-inhibitor complex crystal structures from Aspergillus fumigatus with structures from Homo sapiens (PDB IDs 1KZO and 1TN6) and Cryptococcus neoformans (PDB ID 3Q75), Peptide-induced conformational changes, overview. Binding groove widening is consistent with variations in steady-state enzyme kinetics
-
additional information
-
higher concentrations of the alpha-dicarbonyl compound results in more rapid and more extensive inactivation
-
additional information
-
not: KTSSVIM
-
additional information
-
synthesis of a family of 30 benzoylated N-ylides and evaluation for the inhibitory activity on human protein farnesyltransferase. Most of these novel compounds posses in vitro inhibition potencies in the micromolar range. The nature of the substituents on the pyridine and phenyl units proves to be important in determining inhibitory activity and generally, the replacement of the cyanoacrylonitrile function by a cyanoethylacrylate group decreases the biological potential on farnesyltransferase, structure-activity relationship, overview
-
additional information
inhibition mechanisms for FTase and GGTase-I, EC 2.5.1.59, are different. Two classes of FTase enzyme inhibitors, bisubstrate imidazole-containing derivatives linked by an acidic substituent and a peptidyl chain and peptidomimetic molecules, which can be divided into two groups, namely thiol and non-thiol compounds. Molecular modeling studies of FTase and protein-inhibitor interactions, overview; inhibition mechanisms for FTase and GGTase-I, EC 2.5.1.59, are different. Two classes of FTase enzyme inhibitors, bisubstrate imidazole-containing derivatives linked by an acidic substituent and a peptidyl chain and peptidomimetic molecules, which can be divided into two groups, namely thiol and non-thiol compounds. Molecular modeling studies of FTase and protein-inhibitor interactions, overview
-
additional information
inhibition mechanisms for FTase and GGTase-I, EC 2.5.1.59, are different. Two classes of FTase enzyme inhibitors, bisubstrate imidazole-containing derivatives linked by an acidic substituent and a peptidyl chain and peptidomimetic molecules, which can be divided into two groups, namely thiol and non-thiol compounds. Molecular modeling studies of FTase and protein-inhibitor interactions, overview; inhibition mechanisms for FTase and GGTase-I, EC 2.5.1.59, are different. Two classes of FTase enzyme inhibitors, bisubstrate imidazole-containing derivatives linked by an acidic substituent and a peptidyl chain and peptidomimetic molecules, which can be divided into two groups, namely thiol and non-thiol compounds. Molecular modeling studies of FTase and protein-inhibitor interactions, overview
-
additional information
-
introduction of an N-benzylimidazole moiety on protein farnesyltransferase inhibitors highly improves their antiparasitic activity against parasite cell proliferation, e.g. of Plasmodium falciparum, Leishmania donovani, Trypanosoma cruzi, and Trypanosoma brucei, overview. Generally compounds of the arylthiophene series are not very active on Plasmodium falciparum. No inhibition by ethyl 3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylate and methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methioninate
-
additional information
-
addition of a methionine residue at position 2 of 3-arylthiophenes greatly improves enzyme inhibition, antiparasitic effect of the compounds on proliferation of 4 protozoan parasites, i.e. Plasmodium falciparum, Trypanosoma brucei brucei, Trypanosoma cruzi and Leishmania donovani, overview. No inhibition by 3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)-N-(adamant-1-ylmethyl)thiophene-2-carboxamide, 3-(4-chlorophenyl)-4-cyano-N-(naphthalen-1-ylmethyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxamide, methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-N-methyl-D-methioninate, ethyl 3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylate, and methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methioninate
-
additional information
-
-
-
additional information
-
not inhibited by 4-[[[6-cyano-1-(3-methyl-3H-imidazole-4-sulfonyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid methyl ester
-
additional information
-
two primary modes of inhibition: blocking the peptide substrate site and blocking the exit groove
-
additional information
-
hexapeptide containing a switch of leucine for methionine at the COOH terminus or a switch of cysteine for serine at the prenylation site is essentially inactive in competing for enzyme activity
-
additional information
-
tetrapeptides with sequence L-penicillamine-Val-Ile-X and Cys-Val-Phe-X
-
additional information
-
enzyme inhibited by peptides containing the C-terminal CAAX sequence
-
additional information
-
enzyme inhibited by peptides containing the C-terminal CAAX sequence
-
additional information
-
not: KTSSVIM
-
additional information
-
introduction of an N-benzylimidazole moiety on protein farnesyltransferase inhibitors highly improves their antiparasitic activity against parasite cell proliferation, e.g. of Plasmodium falciparum, Leishmania donovani, Trypanosoma cruzi, and Trypanosoma brucei, overview. Generally compounds of the arylthiophene series are not very active on Plasmodium falciparum. No inhibition by ethyl 3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylate, methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methioninate, ethyl 3-(4-chlorophenyl)-5-([[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl]amino)-4-ethynylthiophene-2-carboxylate, ethyl 5-[(tert-butoxycarbonyl)[[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylate, methyl N-([5-[(tert-butoxycarbonyl)[[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophen-2-yl]carbonyl)-L-methioninate, and ethyl 5-[(tert-butoxycarbonyl)[[1-(4-nitrobenzyl)-1H-imidazol-4-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylate
-
additional information
-
addition of a methionine residue at position 2 of 3-arylthiophenes greatly improves enzyme inhibition, antiparasitic effect of the compounds on proliferation of 4 protozoan parasites, i.e. Plasmodium falciparum, Trypanosoma brucei brucei, Trypanosoma cruzi and Leishmania donovani, overview. No inhibition by 3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)-N-(adamant-1-ylmethyl)thiophene-2-carboxamide, 3-(4-chlorophenyl)-4-cyano-N-(naphthalen-1-ylmethyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxamide, methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-N-methyl-D-methioninate, ethyl 3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylate, and methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methioninate
-
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0.09
(1aR,2S,3aS,6aR,7aR)-2,6-dimethyl-1a-[(1E)-3-oxobut-1-en-1-yl]octahydro-5H-oxireno[4,5]cyclohepta[1,2-b]furan-5-one
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.1
(1aR,2S,3aS,6aR,7aR)-2-methyl-6-methylidene-1a-[(1E)-3-oxobut-1-en-1-yl]octahydro-5H-oxireno[4,5]cyclohepta[1,2-b]furan-5-one
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.066
(1aS,2S,3aS,6aR,7aS)-2,6-dimethyl-1a-[(1E)-3-oxobut-1-en-1-yl]octahydro-5H-oxireno[4,5]cyclohepta[1,2-b]furan-5-one
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.5
(1aS,2S,3aS,6aR,7aS)-2-methyl-6-methylidene-1a-[(1E)-3-oxobut-1-en-1-yl]octahydro-5H-oxireno[4,5]cyclohepta[1,2-b]furan-5-one
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.0018
(1R,4aR,5R,7S)-5-[[(1R,4aR,8aS)-8a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-6-methoxy-5,8-dioxo-1,4,4a,5,8,8a-hexahydronaphthalen-1-yl]methyl]-7-hydroxy-1,4a-dimethyl-6-methylidenedecahydronaphthalene-1-carbaldehyde
Rattus norvegicus
-
30°C, pH 7.5
0.04
(1R,4aR,5R,7S)-5-[[(1R,4aR,8aS)-8a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-6-methoxy-5,8-dioxo-1,4,4a,5,8,8a-hexahydronaphthalen-1-yl]methyl]-7-hydroxy-1,4a-dimethyl-6-methylidenedecahydronaphthalene-1-carboxylic acid
Rattus norvegicus
-
30°C, pH 7.5
0.00053
(2-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-1-[2-(methylsulfanyl)ethyl]hydrazinyl)acetic acid
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.0065 - 0.016
(2E)-2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ylidene]butanedioic acid
0.9
(2E)-3-[(3aR,7S,8aS)-3,7-dimethyl-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]-1-methylprop-2-en-1-yl acetate
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.04 - 0.13
(2E,4E,8E)-5,9,13-trimethyltetradeca-2,4,8,12-tetraenoic acid
0.012 - 0.175
(2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoic acid
0.000016
(2Z,6E)-3-(3-methylbut-2-enyl)-7,11-dimethyldodeca-2,6,10-triene monophosphate
Homo sapiens
-
IC50: 16 nM
0.000013
(2Z,6E)-3-tert-butyl-7,11-dimethyldodeca-2,6,10-triene monophosphate
Homo sapiens
-
IC50: 13 nM
0.21
(3aR,7S,8aS)-3,7-dimethyl-6-[(1E)-3-oxobut-1-en-1-yl]-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-2-one
Saccharomyces cerevisiae
-
30°C, pH 7.5
1
(3aR,7S,8aS)-6-[(1E)-3-hydroxybut-1-en-1-yl]-3,7-dimethyl-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-2-one
Saccharomyces cerevisiae
-
value above, 30°C, pH 7.5
0.1
(3aR,7S,8aS)-7-methyl-3-methylidene-6-[(1E)-3-oxobut-1-en-1-yl]-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-2-one
Saccharomyces cerevisiae
-
30°C, pH 7.5
1
(3aR,8S,9aS)-6-acetyl-3,8-dimethyl-3,3a,4,8,9,9a-hexahydro-2H-cyclohepta[1,2-b:4,5-b']difuran-2-one
Saccharomyces cerevisiae
-
value above, 330°C, pH 7.5
0.24
(3R,3aR,7S,8aS)-3,7-dimethyl-6-(3-oxobutyl)-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-2-one
Saccharomyces cerevisiae
-
30°C, pH 7.5
1
(3R,3aR,7S,8aS)-6-(3-hydroxybutyl)-3,7-dimethyl-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-2-one
Saccharomyces cerevisiae
-
value above, 30°C, pH 7.5
0.086
(4aS,5R,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-2-methoxy-5-[[(1S,3S,7S,8aS)-1,3,7-trihydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
Rattus norvegicus
-
30°C, pH 7.5
0.0032
(4aS,5R,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-2-methoxy-6-methyl-5-[[(1R,8aS)-5,5,8a-trimethyl-2-methylidene-3-oxodecahydronaphthalen-1-yl]methyl]-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
Rattus norvegicus
-
30°C, pH 7.5
0.01
(4aS,5R,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-5-[[(1R,3S,5R,8aS)-3-hydroxy-5-(hydroxymethyl)-5,8a-dimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-2-methoxy-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
Rattus norvegicus
-
30°C, pH 7.5
0.04
(4aS,5R,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-5-[[(1R,3S,7S,8aS)-3,7-dihydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-2-methoxy-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
Rattus norvegicus
-
30°C, pH 7.5
0.0057
(4aS,5R,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-5-[[(1R,3S,8aS)-3-hydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-2-methoxy-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
Rattus norvegicus
-
30°C, pH 7.5
0.003
(4aS,5R,8aR)-4a-(5-hydroxy-7-methoxy-4-oxo-4H-chromen-2-yl)-2-methoxy-6-methyl-5-[[(1R,8aS)-5,5,8a-trimethyl-2-methylidene-3-oxodecahydronaphthalen-1-yl]methyl]-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
Rattus norvegicus
-
30°C, pH 7.5
0.017
(4aS,5S,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-5-[[(1R,2R,7S,8aS)-2,7-dihydroxy-2,5,5,8a-tetramethyldecahydronaphthalen-1-yl]methyl]-6-hydroxy-2-methoxy-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
Rattus norvegicus
-
30°C, pH 7.5
0.5 - 0.7
(4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-4,8,12-trienoic acid
0.2
(4E,8E)-5,9,13-trimethyl-N-(phenylsulfonyl)tetradeca-4,8,12-trienamide
0.2
(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienamide
Homo sapiens
-
value above, 30°C, pH 7.5
0.042 - 0.17
(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoic acid
0.0104 - 0.029
(4S)-4-([[5-(butan-2-yl)-3-(4-chlorophenyl)-4-cyanothiophen-2-yl]carbonyl]amino)-5-tert-butoxy-5-oxopentanoic acid
0.08 - 0.2
(6E,10E)-7,11,15-trimethyl-3-oxohexadeca-6,10,14-trienoic acid
0.015 - 0.06
(7E,11E)-8,12,16-trimethyl-4-oxoheptadeca-7,11,15-trienoic acid
0.0131
(S)-N-(4-(3,4-dichlorophenoxy)benzyl)-6-(1H-indol-3-yl)piperazine-2,5-dione
Rattus norvegicus
-
pH 7.4, 30°C
0.0178
(S)-N-(4-(3-chlorophenoxy)benzyl)-6-(1H-indol-3-yl)piperazine-2,5-dione
Rattus norvegicus
-
pH 7.4, 30°C
0.037
1,4,8,10-tetrahydroxy-6-[(1E)-3-[(3S,8aS)-3-hydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]-1-methylprop-1-en-1-yl]-5,6-dihydro-7H-benzo[c]xanthen-7-one
Rattus norvegicus
-
30°C, pH 7.5
0.0259
1-(1-[3,4-bis[(hydroxyacetyl)amino]phenyl]-4,4-dicyano-1-oxobut-3-en-2-yl)-3-(dimethylamino)pyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.000024
1-(1H-imidazol-5-ylmethyl)-7-pyridin-4-yl-4-[[2-(trifluoromethoxy)phenyl]carbonyl]-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine
Homo sapiens
-
-
0.0462
1-(4,4-dicyano-1-oxo-1-phenylbut-3-en-2-yl)-3-(dimethylamino)pyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.0000075
1-methyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-yl-methyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(3-methoxy-propyl)-amide
Rattus norvegicus
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100
0.0000034
1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(5-methylisoxazol-4-yl)methyl]-1H-imidazole-4-sulfonamide
Rattus norvegicus
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100
0.0000048
1-methylethyl 4-[([1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate
Rattus norvegicus
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100
0.633
1-[(3aR,7S,8aS)-3,7-dimethyl-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]-3-(1-hydroxyethoxy)butyl acetate
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.04
1-[(3aR,7S,8aS)-3,7-dimethyl-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]butane-1,3-diyl diacetate
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.15
1-[(3aR,7S,8aS)-7-methyl-3-methylidene-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]-3-oxobutyl acetate
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.04
1-[(3aR,7S,8aS)-7-methyl-3-methylidene-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]butane-1,3-diyl diacetate
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.0364
1-[(3Z)-1-(4-bromophenyl)-4-cyano-5,5-dihydroxy-1-oxohept-3-en-2-yl]-3-(dimethylamino)pyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.0319
1-[(3Z)-1-(4-chlorophenyl)-4-cyano-5,5-dihydroxy-1-oxohept-3-en-2-yl]-3-(dimethylamino)pyridinium
Homo sapiens
-
pH and temperature not specified in the publication
55.22
1-[(3Z)-1-[3,4-bis[(hydroxyacetyl)amino]phenyl]-4-cyano-5,5-dihydroxy-1-oxohept-3-en-2-yl]-3-(dimethylamino)pyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.0208
1-[(3Z)-4-cyano-1-(3,4-dimethoxyphenyl)-5,5-dihydroxy-1-oxohept-3-en-2-yl]-3-methoxypyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.0239
1-[(3Z)-4-cyano-1-(4-cyanophenyl)-5,5-dihydroxy-1-oxohept-3-en-2-yl]-3-(dimethylamino)pyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.0623
1-[(3Z)-4-cyano-1-(4-fluorophenyl)-5,5-dihydroxy-1-oxohept-3-en-2-yl]-3-(dimethylamino)pyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.0627
1-[(3Z)-4-cyano-5,5-dihydroxy-1-(4-methoxyphenyl)-1-oxohept-3-en-2-yl]-3-(dimethylamino)pyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.0436
1-[(3Z)-4-cyano-5,5-dihydroxy-1-(4-methylphenyl)-1-oxohept-3-en-2-yl]-3-(dimethylamino)pyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.0435
1-[(3Z)-4-cyano-5,5-dihydroxy-1-oxo-1-(3,4,5-trimethoxyphenyl)hept-3-en-2-yl]-2,4-dimethylpyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.048
1-[(3Z)-4-cyano-5,5-dihydroxy-1-oxo-1-(3,4,5-trimethoxyphenyl)hept-3-en-2-yl]-3-(dimethylamino)pyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.0309
1-[(3Z)-4-cyano-5,5-dihydroxy-1-oxo-1-phenylhept-3-en-2-yl]-3-(dimethylamino)pyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.0197
1-[1-(4-bromophenyl)-4,4-dicyano-1-oxobut-3-en-2-yl]-3-(dimethylamino)pyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.0125
1-[1-(4-chlorophenyl)-4,4-dicyano-1-oxobut-3-en-2-yl]-3-(dimethylamino)pyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.0314
1-[4,4-dicyano-1-(3,4-dimethoxyphenyl)-1-oxobut-3-en-2-yl]-3-methoxypyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.0462
1-[4,4-dicyano-1-(4-cyanophenyl)-1-oxobut-3-en-2-yl]-3-(dimethylamino)pyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.0236
1-[4,4-dicyano-1-(4-fluorophenyl)-1-oxobut-3-en-2-yl]-3-(dimethylamino)pyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.0274
1-[4,4-dicyano-1-(4-methoxyphenyl)-1-oxobut-3-en-2-yl]-2,4-dimethylpyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.0222
1-[4,4-dicyano-1-(4-methoxyphenyl)-1-oxobut-3-en-2-yl]-3-(dimethylamino)pyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.0273
1-[4,4-dicyano-1-(4-methoxyphenyl)-1-oxobut-3-en-2-yl]-3-methoxypyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.0145
1-[4,4-dicyano-1-(4-methylphenyl)-1-oxobut-3-en-2-yl]-3-(dimethylamino)pyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.0282
1-[4,4-dicyano-1-(4-nitrophenyl)-1-oxobut-3-en-2-yl]-3-(dimethylamino)pyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.0201
1-[4,4-dicyano-1-oxo-1-(3,4,5-trimethoxyphenyl)but-3-en-2-yl]-2,4-dimethylpyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.0156
1-[4,4-dicyano-1-oxo-1-(3,4,5-trimethoxyphenyl)but-3-en-2-yl]-3-(dimethylamino)pyridinium
Homo sapiens
-
pH and temperature not specified in the publication
0.0000002
18-oxa-2,5,9,11-tetraazahexacyclo[17.6.2.22,5.113,17.07,11.022,26]triaconta-1(26),7,9,13(28),14,16,19,21,22,24,26-undecaene-16-carbonitrile
Homo sapiens
-
-
0.000001
2-amino-3-[2-butyl-4-(naphthalen-1-ylcarbonyl)piperazin-1-yl]propane-1-thiol
Homo sapiens
-
IC50 less than 0.000001 mM
0.59 - 0.85
2-[(2E)-3,7-dimethyl-1-(1-methyl-1H-imidazol-2-yl)octa-2,6-dien-1-yl]butanedioic acid
0.0025 - 0.0054
2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]butanedioic acid
0.000001
29-oxo-18-oxa-2,6,9,11-tetraazahexacyclo[17.5.3.12,5.113,17.07,11.022,26]nonacosa-7,9,13(28),14,16,19,21,26-octaene-16-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM
0.047
3-(4-chlorophenyl)-4-cyano-1-methyl-5-[(1-methylethyl)sulfanyl]-1H-pyrrole-2-carboxylic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.00145
3-(4-chlorophenyl)-4-cyano-5-(cyclohexylsulfanyl)thiophene-2-carboxylic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.000325
3-(4-chlorophenyl)-4-cyano-5-(ethylsulfanyl)thiophene-2-carboxylic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.00011 - 0.016
3-(4-chlorophenyl)-4-cyano-5-(isopropylthio)thiophene-2-carboxylic acid
0.00061
3-(4-chlorophenyl)-4-cyano-5-(methylsulfanyl)thiophene-2-carboxylic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.028
3-(4-chlorophenyl)-4-cyano-5-(morpholin-4-ylsulfanyl)thiophene-2-carboxylic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.05
3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)-N-adamantylthiophene-2-carboxamide
0.011 - 0.016
3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
0.002
3-(4-chlorophenyl)-4-cyano-5-[(1-methylethyl)sulfanyl]furan-2-carboxylic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.0011
3-(4-chlorophenyl)-4-cyano-5-[(1-methylethyl)sulfanyl]thiophene-2-carboxamide
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.00011
3-(4-chlorophenyl)-4-cyano-5-[(1-methylethyl)sulfanyl]thiophene-2-carboxylic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.000345
3-(4-chlorophenyl)-4-cyano-5-[(1-methylpropyl)sulfanyl]thiophene-2-carboxylic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.00089
3-(4-chlorophenyl)-4-cyano-5-[(2-methylpropyl)sulfanyl]thiophene-2-carboxylic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.0019
3-(4-chlorophenyl)-4-cyano-N'-[2-(methylsulfanyl)ethyl]-5-(propan-2-ylsulfanyl)thiophene-2-carbohydrazide
0.0216 - 0.05
3-(4-chlorophenyl)-4-cyano-N-(naphthalen-1-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxamide
0.022
3-(4-chlorophenyl)-4-cyano-N-cyclopropyl-5-[(1-methylethyl)sulfanyl]thiophene-2-carboxamide
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.024
3-(4-chlorophenyl)-4-cyano-N-[2-(methylsulfanyl)ethyl]-5-(propan-2-ylsulfanyl)thiophene-2-carboxamide
0.00094 - 0.0012
3-(4-chlorophenyl)-4-ethynyl-5-(2l5-triaz-1-en-2-yn-1-yl)thiophene-2-carboxylic acid
0.013 - 0.022
3-(4-chlorophenyl)-4-ethynyl-5-[(1H-imidazol-4-ylacetyl)amino]thiophene-2-carboxylic acid
0.00097 - 0.064
3-(4-chlorophenyl)-5-([[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl][[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynylthiophene-2-carboxylic acid
0.00064 - 0.0054
3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
0.000189
3-allylfarnesyl diphosphate
Homo sapiens
-
IC50: 189 nM
1
3-hydroxy-1-[(3aR,7S,8aS)-7-methyl-3-methylidene-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]butyl acetate
Saccharomyces cerevisiae
-
value above, 30°C, pH 7.5
0.00335
3-methyl-2-[2-oxo-2-(10H-phenothiazin-10-yl)ethyl]indeno[1,2-c]pyrazol-4(2H)-one
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.08 - 0.16
3-oxo-3-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanoic acid
0.000031
3-tert-butylfarnesyl diphosphate
Homo sapiens
-
IC50: 31 nM
0.00007 - 0.0008
3-[3-[2-([2-[1-(tert-butoxycarbonyl)piperidin-4-yl]-1-([(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]methyl)ethyl]sulfamoyl)benzyl]phenyl]propanoic acid
0.00000037
4-(3-{[(4-cyano-3-naphthalen-1-yl-phenyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-methyl}-phenyl)-pyridine-2-carbonitrile
Rattus norvegicus
-
IC50: 0.37 nM, selective inhibitor
0.051
4-(4-chlorophenyl)-2-[(1-methylethyl)sulfanyl]-1,3-thiazole-5-carboxylic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.0000075
4-(4-chlorophenyl)-5-(hydroxyacetyl)-2-[(1-methylethyl)sulfanyl]thiophene-3-carbonitrile
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.0057
4-(4-chlorophenyl)-5-(methoxyacetyl)-2-[(1-methylethyl)sulfanyl]thiophene-3-carbonitrile
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.00046 - 0.039
4-cyano-3-(3-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
0.00027 - 0.029
4-cyano-3-(4-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
0.00025 - 0.007
4-cyano-3-(4-methoxyphenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
0.001 - 0.015
4-cyano-3-(dibenzo[b,d]furan-1-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
0.00032 - 0.032
4-cyano-3-(naphthalen-2-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
0.00062 - 0.0097
4-cyano-3-[3-(methoxycarbonyl)phenyl]-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
0.00001 - 0.01
4-ethynyl-5-([[1-(4-nitrobenzyl)-1H-imidazol-5-yl]methyl]amino)-3-phenylthiophene-2-carboxylic acid
0.1 - 0.13
4-oxo-4-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]butanoic acid
0.00000045
4-[(3'-Chloro-biphenyl-3-ylmethyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile
Rattus norvegicus
-
IC50: 0.45 nM, selective inhibitor
0.000039
4-[(3-cyano-benzyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile
Rattus norvegicus
-
IC50: 0.39 nM, selective inhibitor
0.000031
4-[(3-Methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile
Rattus norvegicus
-
IC50: 31 nM
0.0000015
4-[(4-cyano-benzyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile
Rattus norvegicus
-
IC50: 1.5 nM, selective inhibitor
0.000285
4-[(5-[[4-(10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-yl)azepan-1-yl]methyl]-1H-imidazol-1-yl)methyl]benzonitrile
Homo sapiens
-
-
0.00031
4-[(5-[[4-(10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-yl)piperidin-1-yl]methyl]-1H-imidazol-1-yl)methyl]benzonitrile
Homo sapiens
-
-
0.0000465
4-[(5-[[4-(5-oxido-7-propyl-7,12-dihydrodibenzo[c,f][1,2,8]oxathiazocin-12-yl)azepan-1-yl]methyl]-1H-imidazol-1-yl)methyl]benzonitrile
Homo sapiens
-
-
0.000043
4-[(5-[[4-(7-butyl-5-oxido-7,12-dihydrodibenzo[c,f][1,2,8]oxathiazocin-12-yl)azepan-1-yl]methyl]-1H-imidazol-1-yl)methyl]benzonitrile
Homo sapiens
-
-
0.0000448
4-[(5-[[4-(7-methyl-5-oxido-7,12-dihydrodibenzo[c,f][1,2,8]oxathiazocin-12-yl)azepan-1-yl]methyl]-1H-imidazol-1-yl)methyl]benzonitrile
Homo sapiens
-
-
0.000045
4-[(5-[[4-(7-methyl-5-oxido-7,12-dihydrodibenzo[c,f][1,2,8]oxathiazocin-12-yl)piperidin-1-yl]methyl]-1H-imidazol-1-yl)methyl]benzonitrile
Homo sapiens
-
-
0.0373
4-[5-(4,6-dimethoxy-1,3,5-triazin-2-yl)-1,2-oxazol-3-yl]-N,N-dimethylaniline
Homo sapiens
pH 7.5, 30°C
0.0000015
4-[Biphenyl-3-ylmethyl-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile
Rattus norvegicus
-
IC50: 1.5 nM
0.0000019
4-[Hexyl-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile
Rattus norvegicus
-
IC50: 1.9 nM
0.000038
4-[Methyl-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile
Rattus norvegicus
-
IC50: 38 nM
0.0000017
4-[N, N -bis((1H-imidazol-4-yl)methyl)aminomethyl]-2-(1-(o-tolyl))benzoylmethionine trifluoroacetate
Mus musculus
-
IC50: 1.7 nM
0.0000095
4-[N-(1-H-imidazol-4-yl)methylamino]-2-(2-methoxyphenyl)-benzoylmethionine
Mus musculus
-
IC50: 9.5 nM
0.0000028
4-[N-(1-H-imidazol-4-yl)methylamino]-2-(2-methylphenyl)-benzoylmethionine
Mus musculus
-
IC50: 2.8 nM
0.000028
4-[N-(1H-imidazol-4-yl)methylamino]-2-phenylbenzoylmethionine
Mus musculus
-
IC50: 28 nM
0.0051
4-[[4-([[4-(4-chlorophenyl)-3-ethynylthiophen-2-yl]amino]methyl)-1H-imidazol-1-yl]methyl]benzonitrile
Homo sapiens
-
pH 7.5, 30°C
0.0000173
4-[[5-([4-[7-(3-morpholin-4-ylpropyl)-5-oxido-7,12-dihydrodibenzo[c,f][1,2,8]oxathiazocin-12-yl]azepan-1-yl]methyl)-1H-imidazol-1-yl]methyl]benzonitrile
Homo sapiens
-
-
0.00000065
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid ethylamide
Plasmodium falciparum
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.0000014 - 0.000025
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid isobutyl ester
0.00000058 - 0.0000032
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid methyl ester
0.025
5,7-dihydroxy-2-[(5R)-1-hydroxy-5-[[(3S,8aS)-3-hydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-2-methoxy-6-methyl-4-oxo-1,5,8,8a-tetrahydronaphthalen-4a(4H)-yl]-4H-chromen-4-one
Rattus norvegicus
-
30°C, pH 7.5
0.007
5,7-dihydroxy-2-[(5R)-1-hydroxy-5-[[(3S,8aS)-3-hydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-6-methyl-2-oxo-1,5,8,8a-tetrahydronaphthalen-4a(2H)-yl]-4H-chromen-4-one
Rattus norvegicus
-
30°C, pH 7.5
0.0038
5-(4,6-dimethoxy-1,3,5-triazin-2-yl)-1-(4-methoxyphenyl)pyrrolidin-2-thione
Homo sapiens
pH 7.5, 30°C
0.0411
5-(4,6-dimethoxy-1,3,5-triazin-2-yl)-1-[3-(trifluoromethyl)phenyl]pyrrolidine-2-thione
Homo sapiens
pH 7.5, 30°C
0.02
5-(butan-2-yl)-3-(4-chlorophenyl)-4-cyanothiophene-2-carboxylic acid
Homo sapiens
-
about, pH and temperature not specified in the publication
0.00124
5-(butylsulfanyl)-3-(4-chlorophenyl)-4-cyanothiophene-2-carboxylic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.00037 - 0.018
5-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynyl-3-phenylthiophene-2-carboxylic acid
0.00079
5-acetyl-4-(4-chlorophenyl)-2-[(1-methylethyl)sulfanyl]thiophene-3-carbonitrile
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.035 - 0.06
5-oxo-5-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]pentanoic acid
0.00000097
5-[(3-cyano-benzyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2'-methyl-biphenyl-2-carbonitrile
Rattus norvegicus
-
IC50: 0.97 nM, selective inhibitor
0.00001
5-[(4-cyano-benzyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2'-methyl-biphenyl-2-carbonitrile
Rattus norvegicus
-
IC50: 10 nM, selective inhibitor
0.00064 - 0.055
5-[(tert-butoxycarbonyl)[[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylic acid
0.00038 - 0.036
5-[(tert-butoxycarbonyl)[[1-(4-nitrobenzyl)-1H-imidazol-4-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylic acid
0.00098
5-[(tert-butoxycarbonyl)[[1-(4-nitrobenzyl)-1H-imidazol-5-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylic acid
Homo sapiens
-
pH 7.5, 30°C
0.00018
6-[(4-hydroxyphenyl)(1H-imidazol-1-yl)methyl]-4-phenyl-1,2-dihydroquinolin-2-ol
Homo sapiens
-
-
0.0044
acetylgliotoxin
Homo sapiens
-
-
0.0487
alphabeta-dehydrocurvularin
Homo sapiens
-
-
0.0249
andrastin A
Homo sapiens
-
-
0.0471
andrastin B
Homo sapiens
-
-
0.0133
andrastin C
Homo sapiens
-
-
0.000014
Biphenyl-3-carboxylic acid (4-cyano-3-naphthalen-1-yl-phenyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amide
Rattus norvegicus
-
IC50: 14 nM
0.000018
Biphenyl-3-sulfonic acid (4-cyano-3-naphthalen-1-yl-phenyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amide
Rattus norvegicus
-
IC50: 18 nM
0.0000014
BMS-214662
Homo sapiens
-
-
0.000175 - 0.00034
chaetomellic acid A
0.0168
citreohybridone A
Homo sapiens
-
-
0.0036
citreohybridone B
Homo sapiens
-
-
0.1
desloratadine
Rattus norvegicus
-
value above
0.7
di-tert-butyl 2-[(2E,6E,10E)-1,3,7-trimethyl-1-(1-methyl-1H-imidazol-2-yl)dodeca-2,6,10-trien-1-yl]butanedioate
Homo sapiens
-
30°C, pH 7.5
0.0233
econazole
Rattus norvegicus
-
-
0.000275
ED5
Aspergillus fumigatus
-
pH 7.5, 25°C
0.05
ethyl (2-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-1-[2-(methylsulfanyl)ethyl]hydrazinyl)acetate
Homo sapiens
-
pH and temperature not specified in the publication
0.0372
ethyl 3-(2,5-dimethoxyphenyl)-1,2-oxazole-5-carboxylate
Homo sapiens
pH 7.5, 30°C
0.021 - 0.031
ethyl 3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylate
0.0038
ethyl 3-(4-chlorophenyl)-4-cyano-5-[(1-methylethyl)sulfanyl]thiophene-2-carboxylate
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.001 - 0.0012
ethyl 3-(4-chlorophenyl)-4-ethynyl-5-(2l5-triaz-1-en-2-yn-1-yl)thiophene-2-carboxylate
0.014 - 0.1
ethyl 3-(4-chlorophenyl)-4-ethynyl-5-[(1H-imidazol-4-ylacetyl)amino]thiophene-2-carboxylate
0.034
ethyl 3-(4-chlorophenyl)-5-([[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl]amino)-4-ethynylthiophene-2-carboxylate
Homo sapiens
-
pH 7.5, 30°C
0.000013
ethyl 3-(4-chlorophenyl)-5-([[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl][[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynylthiophene-2-carboxylate
Homo sapiens
-
pH 7.5, 30°C
0.00019 - 0.0074
ethyl 4-ethynyl-5-([[1-(4-nitrobenzyl)-1H-imidazol-5-yl]methyl]amino)-3-phenylthiophene-2-carboxylate
0.0000005 - 0.0000055
ethyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
0.00013
ethyl 5-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynyl-3-phenylthiophene-2-carboxylate
Homo sapiens
-
pH 7.5, 30°C
0.00029
ethyl 5-[(tert-butoxycarbonyl)[[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylate
Homo sapiens
-
pH 7.5, 30°C
0.00033
ethyl 5-[(tert-butoxycarbonyl)[[1-(4-nitrobenzyl)-1H-imidazol-4-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylate
Homo sapiens
-
pH 7.5, 30°C
0.0021
ethyl 5-[(tert-butoxycarbonyl)[[1-(4-nitrobenzyl)-1H-imidazol-5-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylate
Homo sapiens
-
pH 7.5, 30°C
0.0093 - 0.022
ethyl [[2-([[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]amino)ethyl]sulfanyl]acetate
0.00000086
FTI-2148
Mus musculus
-
IC50: 0.86 nM
0.0000006 - 0.000015
FTI-276
0.0011
gliotoxin
Homo sapiens
-
-
0.0473
granaticin A
Homo sapiens
-
-
0.0448
granaticin B
Homo sapiens
-
-
0.058
kurasoin A
Homo sapiens
-
-
0.065
kurasoin B
Homo sapiens
-
-
0.0000018
L-739,750
Homo sapiens
-
-
0.000002
L-788,123
Homo sapiens
-
-
0.0066
L-Cys-L-Val-L-Leu-L-Ser
Homo sapiens
-
-
0.0133
loratadine
Rattus norvegicus
-
-
0.00024
methyl (2S)-2-([(2S)-2-[(2-[[(2R)-2-amino-3-sulfanylpropyl]amino]-3-methylpentyl)oxy]-3-phenylpropanoyl]amino)-4-(methylsulfonyl)butanoate
Homo sapiens
pH and temperature not specified in the publication
0.00000029 - 0.0000027
methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
0.0000228
methyl N-(1-cysteinylpiperidin-4-yl)-N-(phenylcarbonyl)-L-methioninate
Rattus norvegicus
-
IC50: 22.8 nM
0.0000327
methyl N-(1-[[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl]piperidin-4-yl)-N-(phenylcarbonyl)-L-isoleucinate
Rattus norvegicus
-
IC50: 32.7 nM
0.0000046
methyl N-(1-[[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl]piperidin-4-yl)-N-(phenylcarbonyl)-L-methioninate
Rattus norvegicus
-
IC50: 4.6 nM
0.000022
methyl N-(1-[[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl]piperidin-4-yl)-N-(phenylcarbonyl)-L-phenylalaninate
Rattus norvegicus
-
IC50: 22 nM
0.000022
methyl N-(1-[[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]piperidin-4-yl)-N-(phenylcarbonyl)-L-phenylalaninate
Homo sapiens
-
-
0.0000439
methyl N-(phenylcarbonyl)-N-{1-([1-[4-(trifluoromethyl)benzyl]-1H-imidazol-4-yl]methyl)piperidin-4-yl}-L-methioninate
Rattus norvegicus
-
IC50: 43.9 nM
1
methyl N-([2-[4-ethoxy-2-(ethoxycarbonyl)-4-oxobutyl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methioninate
Saccharomyces cerevisiae
-
IC50 above 1 mM, in 5.8 mM dithiothreitol, 12 mM MgCl2, 0.012 mM ZnCl2 and 0.09% (w/v) CHAPS, 53 mM Tris-HCl, at pH 7.5 and 30°C
1
methyl N-([2-[5-ethoxy-3-(methoxycarbonyl)-5-oxopentyl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-isoleucyl-L-alaninate
Saccharomyces cerevisiae
-
IC50 above 1 mM, in 5.8 mM dithiothreitol, 12 mM MgCl2, 0.012 mM ZnCl2 and 0.09% (w/v) CHAPS, 53 mM Tris-HCl, at pH 7.5 and 30°C
0.19
methyl N-([2-[5-ethoxy-3-(methoxycarbonyl)-5-oxopentyl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methioninate
Saccharomyces cerevisiae
-
in 5.8 mM dithiothreitol, 12 mM MgCl2, 0.012 mM ZnCl2 and 0.09% (w/v) CHAPS, 53 mM Tris-HCl, at pH 7.5 and 30°C
0.34
methyl N-([2-[6-ethoxy-4-(ethoxycarbonyl)-6-oxohexyl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-isoleucyl-L-alaninate
Saccharomyces cerevisiae
-
in 5.8 mM dithiothreitol, 12 mM MgCl2, 0.012 mM ZnCl2 and 0.09% (w/v) CHAPS, 53 mM Tris-HCl, at pH 7.5 and 30°C
0.035
methyl N-([2-[6-ethoxy-4-(ethoxycarbonyl)-6-oxohexyl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methioninate
Saccharomyces cerevisiae
-
in 5.8 mM dithiothreitol, 12 mM MgCl2, 0.012 mM ZnCl2 and 0.09% (w/v) CHAPS, 53 mM Tris-HCl, at pH 7.5 and 30°C
0.00068
methyl N-([5-[(tert-butoxycarbonyl)[[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophen-2-yl]carbonyl)-L-methioninate
Homo sapiens
-
pH 7.5, 30°C
0.00000235
methyl N-benzyl-N-(1-[[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl]piperidin-4-yl)-L-methioninate
Rattus norvegicus
-
IC50: 2.35 nM
0.000397
methyl N-[1-[(1-benzyl-1H-imidazol-4-yl)methyl]piperidin-4-yl]-N-(phenylcarbonyl)-L-methioninate
Rattus norvegicus
-
IC50: 397 nM
0.00046 - 0.0082
methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonothioyl]-D-methioninate
0.0028 - 0.05
methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-D-methioninate
0.05
methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-isoleucyl-L-methioninate
0.0017 - 0.0046
methyl N-[[3-(4-chlorophenyl)-4-ethynyl-5-(2l5-triaz-1-en-2-yn-1-yl)thiophen-2-yl]carbonyl]-L-methioninate
0.019 - 0.023
methyl N-[[3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methioninate
0.0047 - 0.0053
methyl N-[[4-cyano-3-(3,4-dihydroxyphenyl)-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methioninate
0.05
methyl N-[[4-cyano-3-(dibenzo[b,d]furan-4-yl)-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methioninate
0.0036 - 0.0056
methyl N-[[4-cyano-5-(propan-2-ylsulfanyl)-3-(3,4,5-trihydroxyphenyl)thiophen-2-yl]carbonyl]-L-methioninate
0.05
methyl N-[[5-(butan-2-yl)-3-(4-chlorophenyl)-4-cyanothiophen-2-yl]carbonyl]-L-methioninate
0.00015 - 0.015
methyl N-[[5-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynyl-3-phenylthiophen-2-yl]carbonyl]-L-methioninate
0.0189
miconazole
Rattus norvegicus
-
-
0.00373
N'-[(1Z)-1-(3-hydroxy-1-oxo-1H-inden-2-yl)ethylidene]-3-(10H-phenothiazin-10-yl)propanehydrazide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000005 - 0.000056
N-(1-benzyl-2-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl)-1-methyl-1H-imidazole-4-sulfonamide
0.000005 - 0.00016
N-(1-benzyl-2-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl)-2-methylbenzenesulfonamide
0.0009
N-([1-[(4-chlorophenyl)carbonyl]piperidin-4-yl]methyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]pyridine-2-sulfonamide
Plasmodium falciparum
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.00064
N-([2-[(1E,6E,10E)-4-carboxy-4-(ethoxycarbonyl)-7,11,15-trimethylhexadeca-1,6,10,14-tetraen-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methionine
Homo sapiens
-
30°C, pH 7.5
0.00024
N-([2-[(6E,10E)-4-carboxy-4-(ethoxycarbonyl)-7,11,15-trimethylhexadeca-6,10,14-trien-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methionine
Homo sapiens
-
30°C, pH 7.5
0.000112
N-([5-[(2R)-2,3-dihydro-1,4-benzodioxin-2-ylmethoxy]-2'-methoxybiphenyl-2-yl]carbonyl)-L-methionine
Homo sapiens
-
-
0.000075
N-([5-[(2R)-2,3-dihydro-1,4-benzodioxin-2-ylmethoxy]-2'-methylbiphenyl-2-yl]carbonyl)-D-methionine
Homo sapiens
-
-
0.000053
N-([5-[(2R)-2,3-dihydro-1,4-benzodioxin-2-ylmethoxy]-2'-methylbiphenyl-2-yl]carbonyl)-L-methionine
Homo sapiens
-
-
0.000053
N-([5-[(2S)-2,3-dihydro-1,4-benzodioxin-2-ylmethoxy]-2'-methoxybiphenyl-2-yl]carbonyl)-D-methionine
Homo sapiens
-
-
0.000055
N-([5-[(2S)-2,3-dihydro-1,4-benzodioxin-2-ylmethoxy]-2'-methoxybiphenyl-2-yl]carbonyl)-L-methionine
Homo sapiens
-
-
0.00005
N-([5-[(2S)-2,3-dihydro-1,4-benzodioxin-2-ylmethoxy]-2'-methylbiphenyl-2-yl]carbonyl)-D-methionine
Homo sapiens
-
-
0.000045
N-([5-[(2S)-2,3-dihydro-1,4-benzodioxin-2-ylmethoxy]-2'-methylbiphenyl-2-yl]carbonyl)-L-methionine
Homo sapiens
-
-
0.000005 - 0.000008
N-tert-butyl-N2-[6-cyano-1-(1-methyl-1H-imidazol-5-yl)-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide
0.0008
N-tert-butyl-N2-[6-cyano-1-(1H-imidazol-4-yl)-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide
Plasmodium falciparum
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.000042
N-tert-butyl-N2-[6-cyano-1-(4-fluorophenyl)-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide
Plasmodium falciparum
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.0000024
N-[(1-acetylpiperidin-4-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]pyridine-2-sulfonamide
Plasmodium falciparum
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.000003 - 0.0000065
N-[(1-butanoylpiperidin-4-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]pyridine-2-sulfonamide
0.00044
N-[(3-bromonaphthalen-2-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
Rattus norvegicus
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100
0.843
N-[(5-[[(2R)-2,3-dihydro-1,4-benzodioxin-2-ylmethyl]carbamoyl]-2'-methoxybiphenyl-2-yl)carbonyl]-D-methionine
Homo sapiens
-
-
0.302
N-[(5-[[(2S)-2,3-dihydro-1,4-benzodioxin-2-ylmethyl]carbamoyl]-2'-methoxybiphenyl-2-yl)carbonyl]-D-methionine
Homo sapiens
-
-
0.151
N-[(5-[[(2S)-2,3-dihydro-1,4-benzodioxin-2-ylmethyl]carbamoyl]-2'-methoxybiphenyl-2-yl)carbonyl]-L-methionine
Homo sapiens
-
-
0.012
N-[(5-[[(2S)-2,3-dihydro-1,4-benzodioxin-2-ylmethyl]carbamoyl]-2'-methylbiphenyl-2-yl)carbonyl]-D-methionine
Homo sapiens
-
-
0.016
N-[(5-[[(2S)-2,3-dihydro-1,4-benzodioxin-2-ylmethyl]carbamoyl]-2'-methylbiphenyl-2-yl)carbonyl]-L-methionine
Homo sapiens
-
-
0.00001
N-[(6-chloro-2,1,3-benzothiadiazol-5-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
Rattus norvegicus
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100
0.000105
N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
Rattus norvegicus
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100
0.0000021
N-[2-([2-[(2-amino-3-sulfanylpropyl)amino]-3-methylbutyl]amino)-3-phenylpropyl]methionine
Homo sapiens
-
-
0.00000015
N-[2-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]acetyl]amino)-3-methylpentyl]-N-(naphthalen-1-ylmethyl)glycylmethionine
Homo sapiens
-
-
0.0000008
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[(1-propanoylpiperidin-4-yl)methyl]pyridine-2-sulfonamide
Plasmodium falciparum
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.0000006
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(2-methylpropanoyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
Plasmodium falciparum
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.0000006 - 0.0000078
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(3,3-dimethylbutanoyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
0.00000075
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(cyclopropylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
Plasmodium falciparum
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.000007 - 0.000016
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(phenylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
0.000005
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[4-(1H-1,2,4-triazol-1-yl)benzyl]-1H-imidazole-4-sulfonamide
Plasmodium falciparum
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.0000005 - 0.0000026
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[4-(1H-pyrazol-1-yl)benzyl]-1H-imidazole-4-sulfonamide
0.001
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)-1-methyl-1H-imidazole-4-sulfonamide
Rattus norvegicus
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100
0.0000038
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(pyridin-2-ylmethyl)pyridine-2-sulfonamide
Rattus norvegicus
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100
0.000003
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(4-phenyl-1,3-oxazol-5-yl)methyl]pyridine-2-sulfonamide
Rattus norvegicus
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100
0.0000017
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(1H-pyrrol-1-yl)ethyl]pyridine-2-sulfonamide
Rattus norvegicus
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100
0.27
N-[[2-(2,3-dicarboxypropyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-L-isoleucyl-L-alanine
Saccharomyces cerevisiae
-
in 5.8 mM dithiothreitol, 12 mM MgCl2, 0.012 mM ZnCl2 and 0.09% (w/v) CHAPS, 53 mM Tris-HCl, at pH 7.5 and 30°C
0.15
N-[[2-(2,3-dicarboxypropyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-L-phenylalanyl-L-methionine
Saccharomyces cerevisiae
-
in 5.8 mM dithiothreitol, 12 mM MgCl2, 0.012 mM ZnCl2 and 0.09% (w/v) CHAPS, 53 mM Tris-HCl, at pH 7.5 and 30°C
0.08
N-[[2-(3,4-dicarboxybutyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-L-isoleucyl-L-alanine
Saccharomyces cerevisiae
-
in 5.8 mM dithiothreitol, 12 mM MgCl2, 0.012 mM ZnCl2 and 0.09% (w/v) CHAPS, 53 mM Tris-HCl, at pH 7.5 and 30°C
0.4
N-[[2-(3,4-dicarboxybutyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-L-phenylalanyl-L-methionine
Saccharomyces cerevisiae
-
in 5.8 mM dithiothreitol, 12 mM MgCl2, 0.012 mM ZnCl2 and 0.09% (w/v) CHAPS, 53 mM Tris-HCl, at pH 7.5 and 30°C
0.08
N-[[2-(4,5-dicarboxypentyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-L-phenylalanyl-L-methionine
Saccharomyces cerevisiae
-
in 5.8 mM dithiothreitol, 12 mM MgCl2, 0.012 mM ZnCl2 and 0.09% (w/v) CHAPS, 53 mM Tris-HCl, at pH 7.5 and 30°C
0.18
N-[[2-(4,5-dicarboxypentyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-Lisoleucyl-L-alanine
Saccharomyces cerevisiae
-
in 5.8 mM dithiothreitol, 12 mM MgCl2, 0.012 mM ZnCl2 and 0.09% (w/v) CHAPS, 53 mM Tris-HCl, at pH 7.5 and 30°C
0.00023 - 0.0017
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonothioyl]-D-methionine
0.00045 - 0.0014
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-D-methionine
0.0019 - 0.0022
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-isoleucyl-L-methionine
0.000067 - 0.00012
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methionine
0.0018 - 0.0033
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-N-methyl-D-methionine
0.000042
N-[[3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methionine
0.00014 - 0.00019
N-[[4-cyano-3-(dibenzo[b,d]furan-4-yl)-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methionine
0.0048 - 0.0087
N-[[4-cyano-5-(propan-2-ylsulfanyl)-3-(3,4,5-trihydroxyphenyl)thiophen-2-yl]carbonyl]-L-methionine
0.0036 - 0.04
N-[[5-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynyl-3-phenylthiophen-2-yl]carbonyl]-L-methionine
0.000076 - 0.0012
N2-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-glutamine
0.0000285
Na-[(3S)-3-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-phenylbutanoyl]-L-phenylalaninamide
Homo sapiens
-
-
0.0237
O-methylthysanone
Homo sapiens
-
-
0.025
penicillic acid
Homo sapiens
-
-
0.00065
pepticinnamin A
Homo sapiens
-
-
-
0.0002
pepticinnamin B
Homo sapiens
-
-
-
0.0001
pepticinnamin C
Homo sapiens
-
-
-
0.001
pepticinnamin D
Homo sapiens
-
-
-
0.0003
pepticinnamin E
Homo sapiens
-
-
0.0005
pepticinnamin F
Homo sapiens
-
-
-
0.0000009
pyridine-2-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(1-methanesulfonyl-piperidin-4-ylmethyl)-amide
Plasmodium falciparum
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.0000012
pyridine-2-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-[1-(2,2-dimethylpropionyl)-piperidin-4-ylmethyl]-amide
Plasmodium falciparum
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.000002
pyridine-2-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-[1-(3,3,3-trifluoropropionyl)-piperidin-4-ylmethyl]-amide
Plasmodium falciparum
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.00000057 - 0.00000086
R115777
0.076
rupatadine
Rattus norvegicus
-
-
0.027
SCH-37370
Homo sapiens
-
-
0.00025
SCH-44342
Homo sapiens
-
-
0.0000019 - 0.0001
SCH-66336
0.0000078
SCH66336
Rattus norvegicus
-
IC50: 7.8 nM, selective inhibitor
0.0145
sclerotiorin
Homo sapiens
-
-
0.048
spiculisporic acid
Homo sapiens
-
-
0.3 - 0.6
tert-butyl (2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoate
0.0000012 - 0.0037
tert-butyl 4-(3-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]-2-[[(1-methyl-1H-imidazol-4-yl)sulfonyl]amino]propyl)piperidine-1-carboxylate
-
0.000003 - 0.00405
tert-butyl 4-(3-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]-2-[[(2-methylphenyl)sulfonyl]amino]propyl)piperidine-1-carboxylate
0.000007
tert-butyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
Rattus norvegicus
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100
0.00005
tert-butyl N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(phenylcarbonyl)glycinate
Plasmodium falciparum
-
IC50 above 0.00005 mM, at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.00005
tert-butyl N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(1-methyl-1H-imidazol-4-yl)carbonyl]glycinate
Plasmodium falciparum
-
IC50 above 0.00005 mM, at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.00005
tert-butyl N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(5-methylisoxazol-3-yl)carbonyl]glycinate
Plasmodium falciparum
-
IC50 above 0.00005 mM, at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.0122
thysanone
Homo sapiens
-
-
0.0024
tipifarnib
Aspergillus fumigatus
-
pH 7.5, 25°C
0.2
ubenimex
Rattus norvegicus
-
value above
0.0257
WS5995-C
Homo sapiens
-
-
0.0009
[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ylidene]propanedioic acid
Homo sapiens
-
30°C, pH 7.5
0.00088 - 0.004
[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
0.085 - 0.2
[(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]sulfamic acid
0.021
[3-(1-methyl-1H-imidazol-2-yl)propyl][(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
Homo sapiens
-
30°C, pH 7.5
0.045
[3-(4-chlorophenyl)-4-cyano-5-[(1-methylethyl)sulfanyl]thiophen-2-yl]methyl acetate
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.005 - 0.01
[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanedioic acid
0.06 - 0.2
[[(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]amino]propanedioic acid
0.0037 - 0.0089
[[2-([[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]amino)ethyl]sulfanyl]acetic acid
0.0065
(2E)-2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ylidene]butanedioic acid
Homo sapiens
-
30°C, pH 7.5
0.016
(2E)-2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ylidene]butanedioic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.04
(2E,4E,8E)-5,9,13-trimethyltetradeca-2,4,8,12-tetraenoic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.13
(2E,4E,8E)-5,9,13-trimethyltetradeca-2,4,8,12-tetraenoic acid
Homo sapiens
-
30°C, pH 7.5
0.012
(2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoic acid
Homo sapiens
-
30°C, pH 7.5
0.028
(2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.13
(2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.175
(2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoic acid
Homo sapiens
-
30°C, pH 7.5
0.5
(4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-4,8,12-trienoic acid
Homo sapiens
-
30°C, pH 7.5
0.7
(4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-4,8,12-trienoic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.2
(4E,8E)-5,9,13-trimethyl-N-(phenylsulfonyl)tetradeca-4,8,12-trienamide
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.2
(4E,8E)-5,9,13-trimethyl-N-(phenylsulfonyl)tetradeca-4,8,12-trienamide
Homo sapiens
-
value above, 30°C, pH 7.5
0.042
(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.17
(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoic acid
Homo sapiens
-
30°C, pH 7.5
0.0104
(4S)-4-([[5-(butan-2-yl)-3-(4-chlorophenyl)-4-cyanothiophen-2-yl]carbonyl]amino)-5-tert-butoxy-5-oxopentanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.029
(4S)-4-([[5-(butan-2-yl)-3-(4-chlorophenyl)-4-cyanothiophen-2-yl]carbonyl]amino)-5-tert-butoxy-5-oxopentanoic acid
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.08
(6E,10E)-7,11,15-trimethyl-3-oxohexadeca-6,10,14-trienoic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.2
(6E,10E)-7,11,15-trimethyl-3-oxohexadeca-6,10,14-trienoic acid
Homo sapiens
-
30°C, pH 7.5
0.015
(7E,11E)-8,12,16-trimethyl-4-oxoheptadeca-7,11,15-trienoic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.06
(7E,11E)-8,12,16-trimethyl-4-oxoheptadeca-7,11,15-trienoic acid
Homo sapiens
-
30°C, pH 7.5
0.59
2-[(2E)-3,7-dimethyl-1-(1-methyl-1H-imidazol-2-yl)octa-2,6-dien-1-yl]butanedioic acid
Homo sapiens
-
30°C, pH 7.5
0.85
2-[(2E)-3,7-dimethyl-1-(1-methyl-1H-imidazol-2-yl)octa-2,6-dien-1-yl]butanedioic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.0025
2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]butanedioic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.0054
2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]butanedioic acid
Homo sapiens
-
30°C, pH 7.5
0.00011
3-(4-chlorophenyl)-4-cyano-5-(isopropylthio)thiophene-2-carboxylic acid
Saccharomyces cerevisiae
-
pH 7.5, 30°C
0.0106
3-(4-chlorophenyl)-4-cyano-5-(isopropylthio)thiophene-2-carboxylic acid
Trypanosoma brucei
-
pH 7.5, 30°C
0.016
3-(4-chlorophenyl)-4-cyano-5-(isopropylthio)thiophene-2-carboxylic acid
Homo sapiens
-
pH 7.5, 30°C
0.05
3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)-N-adamantylthiophene-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.05
3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)-N-adamantylthiophene-2-carboxamide
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.011
3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Trypanosoma brucei
-
pH 7.5, 30°C
0.011
3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.016
3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Homo sapiens
-
pH 7.5, 30°C
0.016
3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0019
3-(4-chlorophenyl)-4-cyano-N'-[2-(methylsulfanyl)ethyl]-5-(propan-2-ylsulfanyl)thiophene-2-carbohydrazide
Homo sapiens
-
pH and temperature not specified in the publication
0.0019
3-(4-chlorophenyl)-4-cyano-N'-[2-(methylsulfanyl)ethyl]-5-(propan-2-ylsulfanyl)thiophene-2-carbohydrazide
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.0216
3-(4-chlorophenyl)-4-cyano-N-(naphthalen-1-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.05
3-(4-chlorophenyl)-4-cyano-N-(naphthalen-1-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxamide
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.024
3-(4-chlorophenyl)-4-cyano-N-[2-(methylsulfanyl)ethyl]-5-(propan-2-ylsulfanyl)thiophene-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.024
3-(4-chlorophenyl)-4-cyano-N-[2-(methylsulfanyl)ethyl]-5-(propan-2-ylsulfanyl)thiophene-2-carboxamide
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.00094
3-(4-chlorophenyl)-4-ethynyl-5-(2l5-triaz-1-en-2-yn-1-yl)thiophene-2-carboxylic acid
Trypanosoma brucei
-
pH 7.5, 30°C
0.0012
3-(4-chlorophenyl)-4-ethynyl-5-(2l5-triaz-1-en-2-yn-1-yl)thiophene-2-carboxylic acid
Homo sapiens
-
pH 7.5, 30°C
0.013
3-(4-chlorophenyl)-4-ethynyl-5-[(1H-imidazol-4-ylacetyl)amino]thiophene-2-carboxylic acid
Trypanosoma brucei
-
pH 7.5, 30°C
0.022
3-(4-chlorophenyl)-4-ethynyl-5-[(1H-imidazol-4-ylacetyl)amino]thiophene-2-carboxylic acid
Homo sapiens
-
pH 7.5, 30°C
0.00097
3-(4-chlorophenyl)-5-([[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl][[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynylthiophene-2-carboxylic acid
Homo sapiens
-
pH 7.5, 30°C
0.064
3-(4-chlorophenyl)-5-([[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl][[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynylthiophene-2-carboxylic acid
Trypanosoma brucei
-
pH 7.5, 30°C
0.00064
3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Saccharomyces cerevisiae
-
pH 7.5, 30°C
0.0033
3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Homo sapiens
-
pH 7.5, 30°C
0.0054
3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Trypanosoma brucei
-
pH 7.5, 30°C
0.08
3-oxo-3-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanoic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.16
3-oxo-3-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanoic acid
Homo sapiens
-
30°C, pH 7.5
0.00007
3-[3-[2-([2-[1-(tert-butoxycarbonyl)piperidin-4-yl]-1-([(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]methyl)ethyl]sulfamoyl)benzyl]phenyl]propanoic acid
Plasmodium falciparum
-
-
0.0008
3-[3-[2-([2-[1-(tert-butoxycarbonyl)piperidin-4-yl]-1-([(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]methyl)ethyl]sulfamoyl)benzyl]phenyl]propanoic acid
Homo sapiens
-
-
0.00046
4-cyano-3-(3-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Saccharomyces cerevisiae
-
pH 7.5, 30°C
0.0086
4-cyano-3-(3-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Trypanosoma brucei
-
pH 7.5, 30°C
0.039
4-cyano-3-(3-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Homo sapiens
-
pH 7.5, 30°C
0.00027
4-cyano-3-(4-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Saccharomyces cerevisiae
-
pH 7.5, 30°C
0.02
4-cyano-3-(4-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Homo sapiens
-
pH 7.5, 30°C
0.029
4-cyano-3-(4-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Trypanosoma brucei
-
pH 7.5, 30°C
0.00025
4-cyano-3-(4-methoxyphenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Saccharomyces cerevisiae
-
pH 7.5, 30°C
0.0069
4-cyano-3-(4-methoxyphenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Trypanosoma brucei
-
pH 7.5, 30°C
0.007
4-cyano-3-(4-methoxyphenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Homo sapiens
-
pH 7.5, 30°C
0.001
4-cyano-3-(dibenzo[b,d]furan-1-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Saccharomyces cerevisiae
-
pH 7.5, 30°C
0.0033
4-cyano-3-(dibenzo[b,d]furan-1-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Trypanosoma brucei
-
pH 7.5, 30°C
0.015
4-cyano-3-(dibenzo[b,d]furan-1-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Homo sapiens
-
pH 7.5, 30°C
0.00032
4-cyano-3-(naphthalen-2-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Saccharomyces cerevisiae
-
pH 7.5, 30°C
0.0055
4-cyano-3-(naphthalen-2-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Homo sapiens
-
pH 7.5, 30°C
0.032
4-cyano-3-(naphthalen-2-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Trypanosoma brucei
-
pH 7.5, 30°C
0.00062
4-cyano-3-[3-(methoxycarbonyl)phenyl]-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Saccharomyces cerevisiae
-
pH 7.5, 30°C
0.0048
4-cyano-3-[3-(methoxycarbonyl)phenyl]-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Homo sapiens
-
pH 7.5, 30°C
0.0097
4-cyano-3-[3-(methoxycarbonyl)phenyl]-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
Trypanosoma brucei
-
pH 7.5, 30°C
0.00001
4-ethynyl-5-([[1-(4-nitrobenzyl)-1H-imidazol-5-yl]methyl]amino)-3-phenylthiophene-2-carboxylic acid
Homo sapiens
-
pH 7.5, 30°C
0.01
4-ethynyl-5-([[1-(4-nitrobenzyl)-1H-imidazol-5-yl]methyl]amino)-3-phenylthiophene-2-carboxylic acid
Trypanosoma brucei
-
pH 7.5, 30°C
0.1
4-oxo-4-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]butanoic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.13
4-oxo-4-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]butanoic acid
Homo sapiens
-
30°C, pH 7.5
0.0000014
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid isobutyl ester
Plasmodium falciparum
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.000025
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid isobutyl ester
Rattus norvegicus
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100
0.00000058
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid methyl ester
Plasmodium falciparum
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.0000032
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid methyl ester
Rattus norvegicus
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100
0.00037
5-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynyl-3-phenylthiophene-2-carboxylic acid
Homo sapiens
-
pH 7.5, 30°C
0.018
5-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynyl-3-phenylthiophene-2-carboxylic acid
Trypanosoma brucei
-
pH 7.5, 30°C
0.035
5-oxo-5-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]pentanoic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.06
5-oxo-5-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]pentanoic acid
Homo sapiens
-
30°C, pH 7.5
0.00064
5-[(tert-butoxycarbonyl)[[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylic acid
Homo sapiens
-
pH 7.5, 30°C
0.055
5-[(tert-butoxycarbonyl)[[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylic acid
Trypanosoma brucei
-
pH 7.5, 30°C
0.00038
5-[(tert-butoxycarbonyl)[[1-(4-nitrobenzyl)-1H-imidazol-4-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylic acid
Homo sapiens
-
pH 7.5, 30°C
0.036
5-[(tert-butoxycarbonyl)[[1-(4-nitrobenzyl)-1H-imidazol-4-yl]methyl]amino]-3-(4-chlorophenyl)-4-ethynylthiophene-2-carboxylic acid
Trypanosoma brucei
-
pH 7.5, 30°C
0.000175
chaetomellic acid A
Homo sapiens
-
30°C, pH 7.5
0.00034
chaetomellic acid A
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.021
ethyl 3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylate
Homo sapiens
-
pH 7.5, 30°C
0.031
ethyl 3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylate
Trypanosoma brucei
-
pH 7.5, 30°C
0.001
ethyl 3-(4-chlorophenyl)-4-ethynyl-5-(2l5-triaz-1-en-2-yn-1-yl)thiophene-2-carboxylate
Trypanosoma brucei
-
pH 7.5, 30°C
0.0012
ethyl 3-(4-chlorophenyl)-4-ethynyl-5-(2l5-triaz-1-en-2-yn-1-yl)thiophene-2-carboxylate
Homo sapiens
-
pH 7.5, 30°C
0.014
ethyl 3-(4-chlorophenyl)-4-ethynyl-5-[(1H-imidazol-4-ylacetyl)amino]thiophene-2-carboxylate
Trypanosoma brucei
-
pH 7.5, 30°C
0.1
ethyl 3-(4-chlorophenyl)-4-ethynyl-5-[(1H-imidazol-4-ylacetyl)amino]thiophene-2-carboxylate
Homo sapiens
-
pH 7.5, 30°C
0.00019
ethyl 4-ethynyl-5-([[1-(4-nitrobenzyl)-1H-imidazol-5-yl]methyl]amino)-3-phenylthiophene-2-carboxylate
Homo sapiens
-
pH 7.5, 30°C
0.0074
ethyl 4-ethynyl-5-([[1-(4-nitrobenzyl)-1H-imidazol-5-yl]methyl]amino)-3-phenylthiophene-2-carboxylate
Trypanosoma brucei
-
pH 7.5, 30°C
0.0000005
ethyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
Plasmodium falciparum
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.0000055
ethyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
Rattus norvegicus
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100
0.0093
ethyl [[2-([[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]amino)ethyl]sulfanyl]acetate
Homo sapiens
-
pH and temperature not specified in the publication
0.022
ethyl [[2-([[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]amino)ethyl]sulfanyl]acetate
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.0000006
FTI-276
Homo sapiens
-
-
0.00000078
FTI-276
Saccharomyces cerevisiae
-
pH 7.5, 30°C
0.00001
FTI-276
Trypanosoma brucei
-
pH 7.5, 30°C
0.000015
FTI-276
Homo sapiens
-
pH 7.5, 30°C
0.00000029
methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
Plasmodium falciparum
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.0000027
methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
Plasmodium falciparum
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.00046
methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonothioyl]-D-methioninate
Homo sapiens
-
pH and temperature not specified in the publication
0.0082
methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonothioyl]-D-methioninate
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.0028
methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-D-methioninate
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.05
methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-D-methioninate
Homo sapiens
-
pH and temperature not specified in the publication
0.05
methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-isoleucyl-L-methioninate
Homo sapiens
-
pH and temperature not specified in the publication
0.05
methyl N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-isoleucyl-L-methioninate
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.0017
methyl N-[[3-(4-chlorophenyl)-4-ethynyl-5-(2l5-triaz-1-en-2-yn-1-yl)thiophen-2-yl]carbonyl]-L-methioninate
Trypanosoma brucei
-
pH 7.5, 30°C
0.0046
methyl N-[[3-(4-chlorophenyl)-4-ethynyl-5-(2l5-triaz-1-en-2-yn-1-yl)thiophen-2-yl]carbonyl]-L-methioninate
Homo sapiens
-
pH 7.5, 30°C
0.019
methyl N-[[3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methioninate
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.023
methyl N-[[3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methioninate
Homo sapiens
-
pH and temperature not specified in the publication
0.0047
methyl N-[[4-cyano-3-(3,4-dihydroxyphenyl)-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methioninate
Homo sapiens
-
pH and temperature not specified in the publication
0.0053
methyl N-[[4-cyano-3-(3,4-dihydroxyphenyl)-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methioninate
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.05
methyl N-[[4-cyano-3-(dibenzo[b,d]furan-4-yl)-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methioninate
Homo sapiens
-
pH and temperature not specified in the publication
0.05
methyl N-[[4-cyano-3-(dibenzo[b,d]furan-4-yl)-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methioninate
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.0036
methyl N-[[4-cyano-5-(propan-2-ylsulfanyl)-3-(3,4,5-trihydroxyphenyl)thiophen-2-yl]carbonyl]-L-methioninate
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.0056
methyl N-[[4-cyano-5-(propan-2-ylsulfanyl)-3-(3,4,5-trihydroxyphenyl)thiophen-2-yl]carbonyl]-L-methioninate
Homo sapiens
-
pH and temperature not specified in the publication
0.05
methyl N-[[5-(butan-2-yl)-3-(4-chlorophenyl)-4-cyanothiophen-2-yl]carbonyl]-L-methioninate
Homo sapiens
-
pH and temperature not specified in the publication
0.05
methyl N-[[5-(butan-2-yl)-3-(4-chlorophenyl)-4-cyanothiophen-2-yl]carbonyl]-L-methioninate
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.00015
methyl N-[[5-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynyl-3-phenylthiophen-2-yl]carbonyl]-L-methioninate
Homo sapiens
-
pH 7.5, 30°C
0.015
methyl N-[[5-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynyl-3-phenylthiophen-2-yl]carbonyl]-L-methioninate
Trypanosoma brucei
-
pH 7.5, 30°C
0.0000005
N-(1-benzyl-2-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl)-1-methyl-1H-imidazole-4-sulfonamide
Plasmodium falciparum
-
-
0.000056
N-(1-benzyl-2-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl)-1-methyl-1H-imidazole-4-sulfonamide
Homo sapiens
-
-
0.000005
N-(1-benzyl-2-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl)-2-methylbenzenesulfonamide
Plasmodium falciparum
-
-
0.00016
N-(1-benzyl-2-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl)-2-methylbenzenesulfonamide
Homo sapiens
-
-
0.000005
N-tert-butyl-N2-[6-cyano-1-(1-methyl-1H-imidazol-5-yl)-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide
Rattus norvegicus
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100
0.000008
N-tert-butyl-N2-[6-cyano-1-(1-methyl-1H-imidazol-5-yl)-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide
Plasmodium falciparum
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.000003
N-[(1-butanoylpiperidin-4-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]pyridine-2-sulfonamide
Plasmodium falciparum
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.0000065
N-[(1-butanoylpiperidin-4-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]pyridine-2-sulfonamide
Rattus norvegicus
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100
0.0000006
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(3,3-dimethylbutanoyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
Plasmodium falciparum
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.0000078
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(3,3-dimethylbutanoyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
Rattus norvegicus
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100
0.000007
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(phenylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
Plasmodium falciparum
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.000016
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(phenylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
Rattus norvegicus
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100
0.0000005
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[4-(1H-pyrazol-1-yl)benzyl]-1H-imidazole-4-sulfonamide
Plasmodium falciparum
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100
0.0000026
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[4-(1H-pyrazol-1-yl)benzyl]-1H-imidazole-4-sulfonamide
Rattus norvegicus
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100
0.00023
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonothioyl]-D-methionine
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.0017
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonothioyl]-D-methionine
Homo sapiens
-
pH and temperature not specified in the publication
0.00045
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-D-methionine
Homo sapiens
-
pH and temperature not specified in the publication
0.0014
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-D-methionine
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.0019
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-isoleucyl-L-methionine
Homo sapiens
-
pH and temperature not specified in the publication
0.0022
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-isoleucyl-L-methionine
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.000067
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methionine
Homo sapiens
-
pH and temperature not specified in the publication
0.000077
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methionine
Homo sapiens
-
pH 7.5, 30°C
0.000077
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methionine
Homo sapiens
-
pH and temperature not specified in the publication
0.000079
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methionine
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.00012
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methionine
Trypanosoma brucei
-
pH 7.5, 30°C
0.00012
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methionine
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.0018
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-N-methyl-D-methionine
Homo sapiens
-
pH and temperature not specified in the publication
0.0033
N-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-N-methyl-D-methionine
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.000042
N-[[3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methionine
Homo sapiens
-
pH and temperature not specified in the publication
0.000042
N-[[3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methionine
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.00014
N-[[4-cyano-3-(dibenzo[b,d]furan-4-yl)-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methionine
Homo sapiens
-
pH and temperature not specified in the publication
0.00019
N-[[4-cyano-3-(dibenzo[b,d]furan-4-yl)-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-methionine
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.0048
N-[[4-cyano-5-(propan-2-ylsulfanyl)-3-(3,4,5-trihydroxyphenyl)thiophen-2-yl]carbonyl]-L-methionine
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.0087
N-[[4-cyano-5-(propan-2-ylsulfanyl)-3-(3,4,5-trihydroxyphenyl)thiophen-2-yl]carbonyl]-L-methionine
Homo sapiens
-
pH and temperature not specified in the publication
0.0036
N-[[5-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynyl-3-phenylthiophen-2-yl]carbonyl]-L-methionine
Homo sapiens
-
pH 7.5, 30°C
0.04
N-[[5-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl]amino)-4-ethynyl-3-phenylthiophen-2-yl]carbonyl]-L-methionine
Trypanosoma brucei
-
pH 7.5, 30°C
0.000076
N2-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-glutamine
Homo sapiens
-
pH and temperature not specified in the publication
0.0012
N2-[[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]-L-glutamine
Trypanosoma brucei
-
pH and temperature not specified in the publication
0.00000057
R115777
Rattus norvegicus
-
IC50: 0.57 nM, selective inhibitor
0.00000086
R115777
Homo sapiens
-
-
0.0000019
SCH-66336
Homo sapiens
-
-
0.0001
SCH-66336
Rattus norvegicus
-
30°C, pH 7.5
0.3
tert-butyl (2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoate
Homo sapiens
-
30°C, pH 7.5
0.6
tert-butyl (2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoate
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.0000012
tert-butyl 4-(3-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]-2-[[(1-methyl-1H-imidazol-4-yl)sulfonyl]amino]propyl)piperidine-1-carboxylate
Plasmodium falciparum
-
-
-
0.0037
tert-butyl 4-(3-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]-2-[[(1-methyl-1H-imidazol-4-yl)sulfonyl]amino]propyl)piperidine-1-carboxylate
Homo sapiens
-
-
-
0.000003
tert-butyl 4-(3-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]-2-[[(2-methylphenyl)sulfonyl]amino]propyl)piperidine-1-carboxylate
Plasmodium falciparum
-
-
0.00405
tert-butyl 4-(3-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]-2-[[(2-methylphenyl)sulfonyl]amino]propyl)piperidine-1-carboxylate
Homo sapiens
-
-
0.00088
[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
Homo sapiens
-
30°C, pH 7.5
0.004
[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.085
[(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]sulfamic acid
Homo sapiens
-
30°C, pH 7.5
0.2
[(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]sulfamic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.005
[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanedioic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.01
[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanedioic acid
Homo sapiens
-
30°C, pH 7.5
0.06
[[(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]amino]propanedioic acid
Homo sapiens
-
30°C, pH 7.5
0.2
[[(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]amino]propanedioic acid
Saccharomyces cerevisiae
-
30°C, pH 7.5
0.0037
[[2-([[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]amino)ethyl]sulfanyl]acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0089
[[2-([[3-(4-chlorophenyl)-4-cyano-5-(propan-2-ylsulfanyl)thiophen-2-yl]carbonyl]amino)ethyl]sulfanyl]acetic acid
Trypanosoma brucei
-
pH and temperature not specified in the publication
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