Literature summary for 3.4.22.38 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-cyano-3-azetidinyl cyclohexylmethyl ether	IC 50: 20 nM	Homo sapiens
3-(benzyloxy)-1-cyanoazetidine	IC 50: 40 nM	Homo sapiens
3-[(benzyloxy)methyl]-1-cyanopyrrolidine	IC 50: 100 nM	Homo sapiens
benzyl 1-cyano-3-pyrrolidinylcarbamate	IC 50: 40 nM	Homo sapiens
N-(1-cyano-3-pyrrolidinyl)benzamide	IC 50: 370 nM	Homo sapiens
N-(1-cyano-3-pyrrolidinyl)[1,1'-biphenyl]-4-carboxamide	IC 50: 290 nM	Homo sapiens
N-(1-cyano-3pyrrolidinyl)benzenesulfonamide	IC 50: 50 nM	Homo sapiens
N-[(1-cyano-2-pyrrolidinyl)methyl]benzamide	IC 50: 0.013 mM	Homo sapiens
N-[(1-cyano-2-pyrrolidinyl)methyl]benzenesulfonamide	IC 50: 0.012 mM	Homo sapiens
N-[(1-cyano-3-azetidinyl)methyl]benzamide	IC 50: 70 nM	Homo sapiens
N-[(1-cyano-3-azetidinyl)methyl]benzenesulfonamide	IC 50: 20 nM	Homo sapiens
N-[(1-cyano-3-azetidinyl)methyl]cyclohexanecarboxamide	IC 50: 5 nM	Homo sapiens
N-[(1-cyano-3pyrrolidinyl)methyl]benzenesulfonamide	IC 50: 200 nM	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.00002	-	N-[(1-cyano-3-azetidinyl)methyl]benzenesulfonamide	pH 5.5, room temperature	Homo sapiens
0.00009	-	N-(1-cyano-3pyrrolidinyl)benzenesulfonamide	pH 5.5, room temperature	Homo sapiens
0.00014	-	benzyl 1-cyano-3-pyrrolidinylcarbamate	pH 5.5, room temperature	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.000005	-	IC 50: 5 nM	Homo sapiens	N-[(1-cyano-3-azetidinyl)methyl]cyclohexanecarboxamide
0.00002	-	IC 50: 20 nM	Homo sapiens	N-[(1-cyano-3-azetidinyl)methyl]benzenesulfonamide
0.00002	-	IC 50: 20 nM	Homo sapiens	1-cyano-3-azetidinyl cyclohexylmethyl ether
0.00004	-	IC 50: 40 nM	Homo sapiens	benzyl 1-cyano-3-pyrrolidinylcarbamate
0.00004	-	IC 50: 40 nM	Homo sapiens	3-(benzyloxy)-1-cyanoazetidine
0.00005	-	IC 50: 50 nM	Homo sapiens	N-(1-cyano-3pyrrolidinyl)benzenesulfonamide
0.00007	-	IC 50: 70 nM	Homo sapiens	N-[(1-cyano-3-azetidinyl)methyl]benzamide
0.0001	-	IC 50: 100 nM	Homo sapiens	3-[(benzyloxy)methyl]-1-cyanopyrrolidine
0.0002	-	IC 50: 200 nM	Homo sapiens	N-[(1-cyano-3pyrrolidinyl)methyl]benzenesulfonamide
0.00029	-	IC 50: 290 nM	Homo sapiens	N-(1-cyano-3-pyrrolidinyl)[1,1'-biphenyl]-4-carboxamide
0.00037	-	IC 50: 370 nM	Homo sapiens	N-(1-cyano-3-pyrrolidinyl)benzamide
0.012	-	IC 50: 0.012 mM	Homo sapiens	N-[(1-cyano-2-pyrrolidinyl)methyl]benzenesulfonamide
0.013	-	IC 50: 0.013 mM	Homo sapiens	N-[(1-cyano-2-pyrrolidinyl)methyl]benzamide

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Release 2023.1 (January 2023)