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Literature summary for 3.4.22.27 extracted from

  • Chen, J.C.; Uang, B.J.; Lyu, P.C.; Chang, J.Y.; Liu, K.J.; Kuo, C.C.; Hsieh, H.P.; Wang, H.C.; Cheng, C.S.; Chang, Y.H.; Chang, M.D.; Chang, W.S.; Lin, C.C.
    Design and synthesis of alpha-ketoamides as cathepsin S inhibitors with potential applications against tumor invasion and angiogenesis (2010), J. Med. Chem., 53, 4545-4549.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
His-tagged version expressed in Escherichia coli Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
methyl 2-amino-4-([(1S)-2-(1-[(benzyloxy)methyl]-3-[(2-ethoxy-2-oxoethyl)amino]-2,3-dioxopropylamino)-1-(cyclohexylmethyl)-2-oxoethyl]aminocarbonyl)benzoate
-
Homo sapiens
methyl 4-([(1S)-2-((1S)-1-[(benzyloxy)methyl]-3-[(2-ethoxy-2-oxoethyl)amino]-2,3-dioxopropyl amino)-1-(cyclohexylmethyl)-2-oxoethyl]aminocarbonyl)-2-[(tert-butoxycarbonyl)amino]benzoate
-
Homo sapiens
N-[(2S)-1-[[(1R)-2-(benzyloxy)-1-cyanoethyl]amino]-3-cyclohexyl-1-oxopropan-2-yl]morpholine-4-carboxamide
-
Homo sapiens
N-[(3S)-4-benzyloxy-(2S)-4-methyl-[[[2-[(9-oxo-9H-1-fluorenyl)carbonyl]amino]propaneyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
Homo sapiens
N-[(3S)-4-benzyloxy-3-[[[(2S)-2-[(3-amino-4-chlorobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
Homo sapiens
N-[(3S)-4-benzyloxy-3-[[[(2S)-2-[(3-[(tert-butoxycarbonyl)amino]-4-chlorobenzoyl amino)]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ester
-
Homo sapiens
N-[(3S)-4-benzyloxy-3-[[[1-[(4-morpholinylcarbonyl)-amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
Homo sapiens
N-[(3S)-4-benzyloxy-3-[[[2-[((1-methylcyclopropyl)carbonyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
Homo sapiens
N-[(3S)-4-benzyloxy-3-[[[2-[((2,2-dimethyl-4-oxo-3,4-dihydro-2H-6-pyranyl)carbonyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
Homo sapiens
N-[(3S)-4-benzyloxy-3-[[[2-[((5-nitro-2-thienyl)carbonyl)amino]cyclo-hexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
Homo sapiens
N-[(3S)-4-benzyloxy-3-[[[2-[((E)-3-(2,5-dimethoxyphenyl)-2-propenoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
Homo sapiens
N-[(3S)-4-benzyloxy-3-[[[2-[(2,3-dioxo-3-(2-thienyl)propanoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
Homo sapiens
N-[(3S)-4-benzyloxy-3-[[[2-[(2-(2-thienyl)acetyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
Homo sapiens
N-[(3S)-4-benzyloxy-3-[[[2-[(2-chloro-5-(methylsulfanyl)benzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
Homo sapiens
N-[(3S)-4-benzyloxy-3-[[[2-[(3-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
Homo sapiens
N-[(3S)-4-benzyloxy-3-[[[2-[(4-chloro-3-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
Homo sapiens
N-[(3S)-4-benzyloxy-3-[[[2-[(4-methoxybenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
Homo sapiens
N-[(3S)-4-benzyloxy-3-[[[2-[(5-chloro-2-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
Homo sapiens
N-[(3S)-4-benzyloxy-3-[[[2-[(5-methoxy-2-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens

Renatured (Commentary)

Renatured (Comment) Organism
-
Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
-
Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
cathepsin S
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000019
-
pH 6.5, 37°C Homo sapiens N-[(3S)-4-benzyloxy-3-[[[2-[(3-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
0.0000044
-
pH 6.5, 37°C Homo sapiens N-[(3S)-4-benzyloxy-3-[[[1-[(4-morpholinylcarbonyl)-amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
0.0000055
-
pH 6.5, 37°C Homo sapiens N-[(2S)-1-[[(1R)-2-(benzyloxy)-1-cyanoethyl]amino]-3-cyclohexyl-1-oxopropan-2-yl]morpholine-4-carboxamide