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Literature summary for 3.4.22.1 extracted from

  • Edem, P.E.; Czorny, S.; Valliant, J.F.
    Synthesis and evaluation of radioiodinated acyloxymethyl ketones as activity-based probes for cathepsin B (2014), J. Med. Chem., 57, 9564-9577.
    View publication on PubMed
Search for more literature for 3.4.22.1

Inhibitors

Inhibitors Comment Organism Structure
(5S)-5-([N-[(benzyloxy)carbonyl]-L-phenylalanyl]amino)-7-[(2,6-dimethylbenzoyl)oxy]-6-oxoheptan-1-aminium trifluoroacetate
-
 Homo sapiens
(5S)-5-([N-[(benzyloxy)carbonyl]-L-phenylalany]amino)-6-oxo-7-[(2,4,6-trimethylbenzoyl)oxy]heptan-1-aminium trifluoroacetate
-
 Homo sapiens
(S)-18-[(S)-2-([(benzyloxy)carbonyl]amino)-3-phenylpropanamido]-1-(4-iodo-1H-1,2,3-triazol-1-yl)-12,19-dioxo-3,6,9-trioxa-13-azaicosan-20-yl 2,4,6-trimethylbenzoate
-
 Homo sapiens
(S)-20-[(S)-2-([(benzyloxy)carbonyl]amino)-3-phenylpropanamido]-1-(3-iodophenyl)-1,14,21-trioxo-5,8,11-trioxa-2,15-diazadocosan-22-yl 2,4,6-trimethylbenzoate
-
 Homo sapiens
(S)-20-[(S)-2-([(benzyloxy)carbonyl]amino)-3-phenylpropanamido]-1-(4-iodophenyl)-1,14,21-trioxo-5,8,11-trioxa-2,15-diazadocosan-22-yl 2,4,6-trimethylbenzoate
-
 Homo sapiens
(S)-3-[(S)-2-([(benzyloxy)carbonyl]amino)-3-phenylpropanamido]-7-(3-iodobenzamido)-2-oxoheptyl 2,4,6-trimethylbenzoate pH 6, 37°C, ki/Ki (sec-1M-1): 630 Homo sapiens
(S)-3-[(S)-2-([(benzyloxy)carbonyl]amino)-3-phenylpropanamido]-7-[3-(3-iodophenyl)ureido]-2-oxoheptyl 2,4,6-trimethylbenzoate pH 6, 37°C, ki/Ki (sec-1M-1): 0.013 Homo sapiens
(S)-3-[(S)-2-([(benzyloxy)carbonyl]amino)-3-phenylpropanamido]-7-[3-(4-iodophenyl)ureido]-2-oxoheptyl 2,4,6-trimethylbenzoate pH 6, 37°C, ki/Ki (sec-1M-1): 0.0035 Homo sapiens
(S)-3-[(S)-2-([(benzyloxy)carbonyl]amino)-3-phenylpropanamido]-7-[6-(3-iodobenzamido)hexanamido]-2-oxoheptyl 2,4,6-trimethylbenzoate pH 6, 37°C, ki/Ki (sec-1M-1): 280 Homo sapiens
(S)-3-[(S)-2-([(benzyloxy)carbonyl]amino)-3-phenylpropanamido]-7-[6-(4-iodo-1H-1,2,3-triazol-1-yl)hexanamido]-2-oxoheptyl 2,4,6-trimethylbenzoate
-
 Homo sapiens
(S)-3-[(S)-2-([(benzyloxy)carbonyl]amino)-3-phenylpropanamido]-7-[6-(4-iodobenzamido)hexanamido]-2-oxoheptyl 2,4,6-trimethylbenzoate pH 6, 37°C, ki/Ki (sec-1M-1): 310 Homo sapiens
(S)-3-[(S)-2-[(benzyloxycarbonyl)amino]-3-phenylpropanamido]-7-(6-[3-(3-iodophenyl)ureido]hexanamido)-2-oxoheptyl 2,4,6-trimethylbenzoate
-
 Homo sapiens
(S)-3-[(S)-2-[(benzyloxycarbonyl)amino]-3-phenylpropanamido]-7-(6-[3-(4-iodophenyl)ureido]hexanamido)-2-oxoheptyl 2,4,6-trimethylbenzoate
-
 Homo sapiens
N-alpha-[(benzyloxy)carbonyl]-N-[(3S)-1-[(2,6-dimethylbenzoyl)oxy]-7-[(6-[(2Z)-2-[(2E,4E)-5-(1-ethyl-3,3-dimethyl-5-sulfo-3H-indolium-2-yl)penta-2,4-dien-1-ylidene]-3,3-dimethyl-5-sulfo-2,3-dihydro-1H-indol-1-yl]hexanoyl)amino]-2-oxoheptan-3-yl]-L-phenylalaninamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P07858
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
CBZ-Arg-Arg-4-nitroanilide + H2O
-
 Homo sapiens CBZ-Arg-Arg + 4-nitroaniline
-
 ?

Synonyms

Synonyms Comment Organism
cathepsin B
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
6
-
 assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000052
-
 (5S)-5-([N-[(benzyloxy)carbonyl]-L-phenylalanyl]amino)-7-[(2,6-dimethylbenzoyl)oxy]-6-oxoheptan-1-aminium trifluoroacetate pH 6, 37°C Homo sapiens
0.00008
-
 (5S)-5-([N-[(benzyloxy)carbonyl]-L-phenylalany]amino)-6-oxo-7-[(2,4,6-trimethylbenzoyl)oxy]heptan-1-aminium trifluoroacetate pH 6, 37°C Homo sapiens
0.00012
-
 N-alpha-[(benzyloxy)carbonyl]-N-[(3S)-1-[(2,6-dimethylbenzoyl)oxy]-7-[(6-[(2Z)-2-[(2E,4E)-5-(1-ethyl-3,3-dimethyl-5-sulfo-3H-indolium-2-yl)penta-2,4-dien-1-ylidene]-3,3-dimethyl-5-sulfo-2,3-dihydro-1H-indol-1-yl]hexanoyl)amino]-2-oxoheptan-3-yl]-L-phenylalaninamide pH 6, 37°C Homo sapiens
0.000181
-
 (S)-20-[(S)-2-([(benzyloxy)carbonyl]amino)-3-phenylpropanamido]-1-(4-iodophenyl)-1,14,21-trioxo-5,8,11-trioxa-2,15-diazadocosan-22-yl 2,4,6-trimethylbenzoate pH 6, 37°C Homo sapiens
0.00035
-
 (S)-18-[(S)-2-([(benzyloxy)carbonyl]amino)-3-phenylpropanamido]-1-(4-iodo-1H-1,2,3-triazol-1-yl)-12,19-dioxo-3,6,9-trioxa-13-azaicosan-20-yl 2,4,6-trimethylbenzoate pH 6, 37°C Homo sapiens
0.00037
-
 (S)-20-[(S)-2-([(benzyloxy)carbonyl]amino)-3-phenylpropanamido]-1-(3-iodophenyl)-1,14,21-trioxo-5,8,11-trioxa-2,15-diazadocosan-22-yl 2,4,6-trimethylbenzoate pH 6, 37°C Homo sapiens
0.001
-
 (S)-3-[(S)-2-([(benzyloxy)carbonyl]amino)-3-phenylpropanamido]-7-[6-(4-iodo-1H-1,2,3-triazol-1-yl)hexanamido]-2-oxoheptyl 2,4,6-trimethylbenzoate pH 6, 37°C Homo sapiens
0.002
-
 (S)-3-[(S)-2-([(benzyloxy)carbonyl]amino)-3-phenylpropanamido]-7-(3-iodobenzamido)-2-oxoheptyl 2,4,6-trimethylbenzoate pH 6, 37°C Homo sapiens