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Literature summary extracted from

  • Zhang, X.; Yang, X.; Wang, H.; Li, S.; Guo, K.; Jiang, D.; Xiao, J.; Liang, D.
    Design, synthesis, and structure-activity relationship study of epoxysuccinyl-peptide derivatives as cathepsin B inhibitors (2017), Biol. Pharm. Bull., 40, 1240-1246 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.22.1 CA-074
-
 Homo sapiens
3.4.22.1 E64d substituting ethyl(methyl) sulfane for 2-methylbutane (R2) of E64d improves the inhibitory activity and selectivity for cathepsin B inhibition Homo sapiens
3.4.22.1 ethyl (2S,3S)-3-(((S)-1-((3-fluorophenethyl)amino)-4-(methylthio)-1-oxobutan-2-yl)carbamoyl)oxirane-2-carboxylate
-
 Homo sapiens
3.4.22.1 ethyl (2S,3S)-3-(((S)-1-(hexylamino)-4-(methylthio)-1-oxobutan-2-yl)carbamoyl)oxirane-2-carboxylate
-
 Homo sapiens
3.4.22.1 ethyl (2S,3S)-3-(((S)-4-(methylthio)-1-oxo-1-((3-phenylpropyl)amino)butan-2-yl)carbamoyl)oxirane-2-carboxylate
-
 Homo sapiens
3.4.22.1 ethyl (2S,3S)-3-(((S)-4-(methylthio)-1-oxo-1-((4-phenylbutyl)-amino)butan-2-yl)carbamoyl)oxirane-2-carboxylate
-
 Homo sapiens
3.4.22.1 ethyl (2S,3S)-3-(((S)-4-(methylthio)-1-oxo-1-(pentan-3-ylamino)butan-2-yl)carbamoyl)oxirane-2-carboxylate
-
 Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.4.22.1 lysosome
-
 Homo sapiens 5764
-

Organism

EC Number Organism UniProt Comment Textmining
3.4.22.1 Homo sapiens P07858
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.22.1 Ac-Arg-Arg-7-amido-4-trifluoromethylcoumarin + H2O
-
 Homo sapiens ?
-
 ?

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.22.1 0.00000427
-
 37°C, pH not specified in the publication Homo sapiens ethyl (2S,3S)-3-(((S)-1-(hexylamino)-4-(methylthio)-1-oxobutan-2-yl)carbamoyl)oxirane-2-carboxylate
3.4.22.1 0.00000661
-
 37°C, pH not specified in the publication Homo sapiens CA-074
3.4.22.1 0.00000716
-
 37°C, pH not specified in the publication Homo sapiens ethyl (2S,3S)-3-(((S)-4-(methylthio)-1-oxo-1-((3-phenylpropyl)amino)butan-2-yl)carbamoyl)oxirane-2-carboxylate
3.4.22.1 0.00001203
-
 37°C, pH not specified in the publication Homo sapiens E64d
3.4.22.1 0.00002368
-
 37°C, pH not specified in the publication Homo sapiens ethyl (2S,3S)-3-(((S)-4-(methylthio)-1-oxo-1-((4-phenylbutyl)-amino)butan-2-yl)carbamoyl)oxirane-2-carboxylate
3.4.22.1 0.00002409
-
 37°C, pH not specified in the publication Homo sapiens ethyl (2S,3S)-3-(((S)-1-((3-fluorophenethyl)amino)-4-(methylthio)-1-oxobutan-2-yl)carbamoyl)oxirane-2-carboxylate
3.4.22.1 0.00007427
-
 37°C, pH not specified in the publication Homo sapiens ethyl (2S,3S)-3-(((S)-4-(methylthio)-1-oxo-1-(pentan-3-ylamino)butan-2-yl)carbamoyl)oxirane-2-carboxylate