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Literature summary for 3.4.22.27 extracted from

  • Walker, B.; Lynas, J.F.; Meighan, M.A.; Bromme, D.
    Evaluation of dipeptide alpha-keto-beta-aldehydes as new inhibitors of cathepsin S (2000), Biochem. Biophys. Res. Commun., 275, 401-405.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
benzyloxycarbonyl-Ala-Leu-COCHO
-
Homo sapiens
benzyloxycarbonyl-Phe-Ala-COCHO
-
Homo sapiens
Benzyloxycarbonyl-Phe-Arg
-
Homo sapiens
benzyloxycarbonyl-Phe-Arg-COCHO
-
Homo sapiens
benzyloxycarbonyl-Phe-Leu-COCHO potent, reversible cathepsin S inhibitor, the inhibitor is 400fold more selective for cathepsin S than for cathepsin B Homo sapiens
benzyloxycarbonyl-Phe-Tyr(OBut)-COCHO
-
Homo sapiens
CLIK-060 0.001 mM, complete inhibition Homo sapiens
CLIK-066 0.01 mM, 28% inhibition Homo sapiens
CLIK-088 0.01 mM, 64% inhibition Homo sapiens
CLIK-112 0.01 mM, 77% inhibition Homo sapiens
CLIK-121 0.01 mM, complete inhibition Homo sapiens
CLIK-148 0.01 mM, complete inhibition Homo sapiens
CLIK-181 0.01 mM, 80% inhibition Homo sapiens
CLIK-195 0.01 mM, complete inhibition Homo sapiens

Localization

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

Organism

Organism UniProt Comment Textmining
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 benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000000185
-
benzyloxycarbonyl-Phe-Leu-COCHO pH 6.4, 25°C Homo sapiens
0.00000223
-
benzyloxycarbonyl-Phe-Tyr(OBut)-COCHO pH 6.4, 25°C Homo sapiens
0.0000024
-
Benzyloxycarbonyl-Phe-Arg pH 6.4, 25°C Homo sapiens
0.0000232
-
benzyloxycarbonyl-Phe-Ala-COCHO pH 6.4, 25°C Homo sapiens
0.0027
-
benzyloxycarbonyl-Ala-Leu-COCHO pH 6.4, 25°C Homo sapiens