Literature summary for 3.4.22.15 extracted from

Falgueyret, J.P.; Oballa, R.M.; Okamoto, O.; Wesolowski, G.; Aubin, Y.; Rydzewski, R.M.; Prasit, P.; Riendeau, D.; Rodan, S.B.; Percival, M.D.
Novel, nonpeptidic cyanamides as potent and reversible inhibitors of human cathepsins K and L (2001), J. Med. Chem., 44, 94-104.

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Inhibitors

Inhibitors	Comment	Organism	Structure
1,3-dihydro-pyrrolo[3,4-b]quinoline-2-carbonitrile	IC50: 0.00045 mM	Homo sapiens
1-cyano-3-azetidinyl cyclohexylmethyl ether	IC50: 0.00001 mM	Homo sapiens
1-cyanoazetidine	IC50: 0.00043 mM	Homo sapiens
1-cyanopyrrolidine	IC50: 0.004 mM	Homo sapiens
3-(benzyloxy)-1-cyanoazetidine	IC50: 0.00001 mM	Homo sapiens
3-[(benzyloxy)methyl]-1-cyanopyrrolidine	IC50: 0.00015 mM	Homo sapiens
benzyl 1-cyano-3-pyrrolidinylcarbamate	IC50: 0.000054 mM	Homo sapiens
diethyl-cyanamide	IC50 is above 0.1 mM	Homo sapiens
N-(1-cyano-3-pyrrolidinyl)benzamide	IC50: 0.00175 mM	Homo sapiens
N-(1-cyano-3-pyrrolidinyl)benzenesulfonamide	IC50: 0.00008 mM	Homo sapiens
N-(1-cyano-3-pyrrolidinyl)[1,1'-biphenyl]-4-carboxamide	IC50: 0.00085 mM	Homo sapiens
N-[(1-cyano-2-pyrrolidinyl)methyl]benzamide	IC50: 0.023 mM	Homo sapiens
N-[(1-cyano-2-pyrrolidinyl)methyl]benzenesulfonamide	IC50: 0.0115 mM	Homo sapiens
N-[(1-cyano-3-azetidinyl)methyl]benzamide	IC50: 0.00065 mM	Homo sapiens
N-[(1-cyano-3-azetidinyl)methyl]benzenesulfonamide	IC50: 0.00005 mM	Homo sapiens
N-[(1-cyano-3-azetidinyl)methyl]cyclohexanecarboxamide	IC50: 0.000006 mM	Homo sapiens
N-[(1-cyano-3-pyrrolidinyl)methyl]benzenesulfonamide	IC50: 0.00035 mM	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Substrates and Products (Substrate)

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

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.000006	-	IC50: 0.000006 mM	Homo sapiens	N-[(1-cyano-3-azetidinyl)methyl]cyclohexanecarboxamide
0.00001	-	IC50: 0.00001 mM	Homo sapiens	3-(benzyloxy)-1-cyanoazetidine
0.00001	-	IC50: 0.00001 mM	Homo sapiens	1-cyano-3-azetidinyl cyclohexylmethyl ether
0.00005	-	IC50: 0.00005 mM	Homo sapiens	N-[(1-cyano-3-azetidinyl)methyl]benzenesulfonamide
0.000054	-	IC50: 0.000054 mM	Homo sapiens	benzyl 1-cyano-3-pyrrolidinylcarbamate
0.00008	-	IC50: 0.00008 mM	Homo sapiens	N-(1-cyano-3-pyrrolidinyl)benzenesulfonamide
0.00015	-	IC50: 0.00015 mM	Homo sapiens	3-[(benzyloxy)methyl]-1-cyanopyrrolidine
0.00035	-	IC50: 0.00035 mM	Homo sapiens	N-[(1-cyano-3-pyrrolidinyl)methyl]benzenesulfonamide
0.00043	-	IC50: 0.00043 mM	Homo sapiens	1-cyanoazetidine
0.00045	-	IC50: 0.00045 mM	Homo sapiens	1,3-dihydro-pyrrolo[3,4-b]quinoline-2-carbonitrile
0.00065	-	IC50: 0.00065 mM	Homo sapiens	N-[(1-cyano-3-azetidinyl)methyl]benzamide
0.00085	-	IC50: 0.00085 mM	Homo sapiens	N-(1-cyano-3-pyrrolidinyl)[1,1'-biphenyl]-4-carboxamide
0.00175	-	IC50: 0.00175 mM	Homo sapiens	N-(1-cyano-3-pyrrolidinyl)benzamide
0.004	-	IC50: 0.004 mM	Homo sapiens	1-cyanopyrrolidine
0.0115	-	IC50: 0.0115 mM	Homo sapiens	N-[(1-cyano-2-pyrrolidinyl)methyl]benzenesulfonamide
0.023	-	IC50: 0.023 mM	Homo sapiens	N-[(1-cyano-2-pyrrolidinyl)methyl]benzamide
0.1	-	IC50 is above 0.1 mM	Homo sapiens	diethyl-cyanamide

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Release 2023.1 (January 2023)