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(4R)-1-acetyl-N-[(2R)-1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-1-acetyl-N-[(2S)-1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxo-3-phenylpropan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(ethylsulfonyl)-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfanyl)-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfinyl)-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-phenoxy-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[(2-chlorophenyl)sulfonyl]-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[(4-fluorophenyl)sulfonyl]-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[[4-(1H-pyrazol-1-yl)phenyl]sulfonyl]-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxopropan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-3-methyl-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(2-methylpropanoyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(2-oxopropyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(3-chlorobenzoyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(3-methoxypropanoyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(4-chlorobenzoyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(biphenyl-4-ylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(cyclohexylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(methylsulfinyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-benzoyl-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-phenyl-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyridin-3-ylcarbonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyridin-4-ylcarbonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyrrolidin-1-ylcarbonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(trifluoroacetyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-propanoyl-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[2-(1,3-benzoxazol-2-yl)-2-oxoethyl]-1-(cyclohexylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide
-
2-cyano-4-(2-hydroxyethoxy)-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[(1,4-dioxaspiro[4.5]dec-8-ylmethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-4-[(2-cyclopentylethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-4-[(6,8-dioxaspiro[3.5]non-7-ylmethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-4-[(cyclohexylmethyl)(methyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-4-[[(4,4-difluorocyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[[(4,4-dimethylcyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[[1-(2-hydroxyethyl)piperidin-4-yl]methoxy]-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-N-(1-methyl-4-phenylpiperidin-4-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-(4,5-dimethoxybiphenyl-2-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-methyl-4-(piperidin-4-ylmethoxy)-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-N-methyl-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-N-methyl-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[4.5]dec-8-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-N-methyl-4-[(spiro[3.5]non-7-ylmethyl)amino]-6-[(2,2,6,6-tetramethylpiperidin-4-yl)oxy]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-N-methyl-4-[[1-(1-methylethyl)piperidin-4-yl]methoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-N-[(1-methyl-4-phenylpiperidin-4-yl)methyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-[(1R)-2-pyridin-2-yl-1-(pyrrolidin-1-ylmethyl)ethyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-[5-[(1-methylpiperidin-4-yl)oxy]biphenyl-2-yl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
4-morpholinecarbonyl-Phe-(S-benzyl)Cys-PSI(CHO)
-
4-[(1-acetylpiperidin-4-yl)methoxy]-2-cyano-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
-
5-bromo-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
-
N-(4-benzyl-1-methylpiperidin-4-yl)-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)oxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-benzyl-2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylpropyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-[(1S)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
(2R)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
(2R)-2-(2-cyclohexylethyl)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(2-cyclopentylethyl)-4-morpholin-4-yl-4-oxo-N-[(1S)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
(2R)-2-(2-cyclopentylethyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)butanamide
-
-
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)butyl]butanamide
-
-
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-phenyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]butanamide
-
-
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
(2R)-2-(cyclohexylmethyl)-N-[(1R)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(cyclohexylmethyl)-N-[(1R)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(cyclopentylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1S)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)butyl]butanamide
-
-
(2R)-2-(cyclopentylmethyl)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(cyclopentylmethyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)-2-phenylethanol
-
-
(2R)-2-benzyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-[4'-(1-azabicyclo[2.2.2]oct-4-yl)-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
-
IC50: 1991 nM
(2R)-2-[4'-(4-tert-butylpiperazin-1-yl)-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
-
IC50: 8340 nM
(2R)-2-[4'-[1-(2-amino-2-methylpropyl)piperidin-4-yl]-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
-
IC50: 1427 nM
(2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-N-(1-cyanocyclopropyl)-3-(methylsulfanyl)propanamide
-
-
(2R)-4-dimethyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-2-(2-morpholin-4-yl-2-oxoethyl)pentanamide
-
-
(2R)-4-morpholin-4-yl-4-oxo-2-(2-phenylethyl)-N-[(1S)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
(2R)-5-dimethyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-2-(2-morpholin-4-yl-2-oxoethyl)hexanamide
-
-
(2R)-N-(1-benzyl-4-cyanopiperidin-4-yl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-(1-cyanocyclopropyl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-(1-cyanocyclopropyl)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-(4-cyano-1-methylpiperidin-4-yl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-(cyanomethyl)-2-[4'-[4-(2-hydroxy-2-methylpropyl)-1-piperazinyl][1,1'-biphenyl]-3-yl]-4-methylpentanamide
-
IC50 above 0.01 mM
(2R)-N-(cyanomethyl)-2-[4'-[4-(2-hydroxyethyl)-1-piperazinyl][1,1'-biphenyl]-3-yl]-4-methylpentanamide
-
IC50: 609 nM
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)-[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 2010 nM
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1H-tetraazol-5-yl)-1,1'-biphenyl-3-yl]pentanamide
-
IC50 above 0.01 mM
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methyl-1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 3931 nM
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-pyrimidinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 1365 nM
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-[4-(2-oxopropyl)-piperazin-1-yl]-1,1'-biphenyl-3-yl]pentanamide
-
IC50: 2364 nM
(2R)-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(1R)-2-[(4-chlorobenzyl)oxy]-1-cyanoethyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-2-carboxamide
-
IC50: 658 nM
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
-
IC50: 18 nM
(2R)-N-[(1S)-1-cyano-3-phenylpropyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-2-(2-morpholin-4-yl-2-oxoethyl)-5-phenylpentanamide
-
-
(2R)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-(2-phenylethyl)butanamide
-
-
(2R)-N-[(3R)-1-benzyl-3-cyanopiperidin-4-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-(1-methylethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-(2-methylpropyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-(2-phenylethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-(cyclopropylmethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-(propan-2-yl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cycloheptylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cycloheptylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(2,3-dihydro-1H-inden-2-ylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(2,3-dihydro-1H-inden-2-ylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclopentylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(1-methylcyclohexyl)methyl]-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(1-methylcyclohexyl)methyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(4-methylcyclohexyl)methyl]-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(4-methylcyclohexyl)methyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-(morpholin-4-yl)-4-oxo-2-(1,2,3,4-tetrahydronaphthalen-2-ylmethyl)butanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-(morpholin-4-yl)-4-oxo-2-[(4-phenylcyclohexyl)methyl]butanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-morpholin-4-yl-4-oxo-2-(1,2,3,4-tetrahydronaphthalen-2-ylmethyl)butanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-morpholin-4-yl-4-oxo-2-[(4-phenylcyclohexyl)methyl]butanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclopentylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclopentylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-methylpiperidin-4-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-methylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-methylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3S)-1-benzyl-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3S)-3-cyano-1-(cyclohexylmethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-1-(4,4'-bipiperidin-1-yl)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
-
-
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxypropan-1-one
-
-
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(propan-2-ylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(propylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
(2S)-1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(1'-methyl-4,4'-bipiperidin-1-yl)propan-2-ol
-
-
(2S)-2-(4-chlorophenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-2-(4-fluorophenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-2-(4-methoxyphenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-2-(4-methylphenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-2-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-2-amino-N-[(1S)-2-(biphenyl-4-yl)-1-cyanoethyl]butanamide
-
-
(2S)-3-cyclohexyl-1-(morpholin-4-yl)-1-oxopropan-2-yl [(2S)-1-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)propan-2-yl]carbamate
-
-
(2S)-4-morpholin-4-yl-4-oxo-2-phenyl-N-[(1S)-1-phenyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]butanamide
-
-
(2S)-4-morpholin-4-yl-4-oxo-2-phenyl-N-[(1S)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
(2S)-4-morpholin-4-yl-4-oxo-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
-
IC50: 53 nM
(2S)-N-[(1S)-1-cyclopropyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-phenylbutanamide
-
-
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[2-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[3-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-[(2S)-3-methyl-1-[[4-(trifluoromethoxy)phenyl]amino]butan-2-yl]-4-(morpholin-4-yl)-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
(2Z)-3-(4-[[5-(3,5-dimethylisoxazol-4-yl)-1,2,4-oxadiazol-3-yl]methoxy]phenyl)-2-(methylsulfonyl)prop-2-enenitrile
-
-
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(furan-2-yl)methanone
-
-
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(pyridin-2-yl)methanone
-
-
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(tetrahydrofuran-2-yl)methanone
-
-
(3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]phenyl)acetic acid
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
(3R)-3-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(3R)-tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
-
IC50: 42 nM
(3S)-3-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(3S)-3-[(N-1,3-benzoxazol-2-yl-3-cyclohexyl-L-alanyl)amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoic acid
-
IC50: 12 nM
(3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoic acid
(3S)-N-[2-(1H-indol-3-yl)ethyl]-3-[[(4-methylphenyl)sulfonyl]amino]-2-oxo-4-phenylbutanamide
-
-
(3S)-tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
-
IC50: 49 nM
(4S)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]hexanamide
-
IC50 above 0.01 mM
(S)-[1-[1-cyano-pyrrolidin-3(R)-ylcarbamoyl]-3-methyl-butyl]-carbamic acid benzyl ester
-
-
(S)-[1-[1-cyano-pyrrolidin-3(S)-ylcarbamoyl]-3-methyl-butyl]-carbamic acid benzyl ester
-
-
1,1-bis(cyanomethyl)-3-[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]urea
-
-
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[(4-[[(2,2,2-trifluoroethyl)sulfonyl]amino]benzoyl)amino]propanoyl]amino)-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([2-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-3-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-4-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(thiophen-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[methyl(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(methylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(phenylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-([4-[(ethylsulfonyl)amino]benzoyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-([[4-([[(dimethylamino)methyl]sulfonyl]amino)phenyl]carbonyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[(4-[[(2,4-dimethyl-1,3-thiazol-5-yl)sulfonyl]amino]benzoyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose ammoniate (1:1)
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[(4-[[(3-fluorophenyl)sulfonyl]amino]benzoyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[(4-[[(3-methoxyphenyl)sulfonyl]amino]benzoyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([2-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-fluoro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([4-[(ethylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2,4-dimethyl-1,3-thiazol-5-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([3-[(methylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([4-[(methylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([4-[(phenylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([4-[(pyridin-4-ylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-(methylsulfamoyl)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-([[4-(1-methylethyl)-1,3-thiazol-2-yl]sulfonyl]amino)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-sulfamoylphenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methyl-1H-imidazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methylethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2,2,2-trifluoroethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2-methylphenyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methylpyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(5-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[4-(methylsulfamoyl)benzoyl]amino]propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[4-methyl-N-(thiophen-3-ylcarbonyl)-L-leucyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[4-methyl-N-(thiophen-3-ylcarbonyl)-L-leucyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-([4-[(cyclohexylsulfonyl)amino]benzoyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-([4-[(cyclopropylsulfonyl)amino]benzoyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([4-[(benzylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([4-[(butylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([4-[(cyclopropylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-chloropyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(3-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(4-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(cyclohexylmethyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1-(1'-[(2S)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]-4,4'-bipiperidin-1-yl)ethanone
-
-
1-(1-[(2R)-3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 350 nM
1-(1-[(2S)-3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 190 nM
1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 10 nM
1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 50 nM
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 50 nM
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 140 nM
1-(1-[3-[3-(4-chloro-3-methylphenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 60 nM
1-(1-[3-[3-[3-[(2-hydroxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)pyrrolidin-2-one
-
-
1-(1-[3-[5-(methylsulfonyl)-3-[3-[(2-phenoxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)pyrrolidin-2-one
-
-
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 80 nM
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5,6-dichloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 110 nM
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methoxy-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 140 nM
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 90 nM
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 120 nM
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-7-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 210 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 130 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-(2,2,2-trifluoroethyl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 90 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-butyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 140 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 310 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 500 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-tert-butyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 100 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 100 nM
1-(1-[3-[5-acetyl-3-(4-chlorophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 460 nM
1-(1-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 120 nM
1-(1-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-fluoro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 230 nM
1-(2-[[5-[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl]ethyl)piperidin-4-ol
-
-
1-(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)-2-hydroxyethanone
-
-
1-(4-cyclopropylpiperazin-1-yl)-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
-
-
1-(4-methylpiperazin-1-yl)-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
-
-
1-(ethenylideneamino)-3-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 100 nM
1-bromo-3-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1-bromo-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1-cyano-(3,4-didehydro)-Pro-Leu methyl ester
-
-
1-cyano-(D)-Pro-(D)-Leu methyl ester
-
-
1-cyano-(D)-Pro-Ala methyl ester
-
-
1-cyano-(D)-Pro-Leu benzyl ester
-
-
1-cyano-(D)-Pro-Leu benzylamide
-
-
1-cyano-(D)-Pro-Leu dimethylamide
-
-
1-cyano-(D)-Pro-Leu methyl ester
-
-
1-cyano-(trans-benzyloxy)prolylleucine methyl ester
-
-
1-cyano-(trans-hydroxy)-Pro-Leu methyl ester
-
-
1-cyano-Pro isoamylamide
-
-
1-cyano-Pro-(D)-Leu methyl ester
-
-
1-cyano-Pro-Ala methyl ester
-
-
1-cyano-Pro-Leu benzyl ester
-
-
1-cyano-Pro-Leu methyl ester
-
-
1-cyano-Pro-Leu-Gly ethyl ester
-
-
1-cyano-Pro-Leu-Leu-Leu methyl ester
-
-
1-cyano-Pro-Phe methyl ester
-
-
1-formyl-(D)-Pro-Leu benzyl ester
-
-
1-iminomethyl-(D)-Pro-Leu benzyl ester
-
-
1-methyl-6-[4-(piperidin-4-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-(piperidin-4-yloxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-(pyridin-2-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-(pyridin-3-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-(pyridin-4-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[(3-oxopiperazin-1-yl)oxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[2-(2-oxopyrrolidin-1-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[2-(6-methylpyridin-2-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[2-(piperidin-4-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[3-(pyrrolidin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-([[1-(4-fluorophenyl)-1-methylethoxy]sulfinyl]methyl)-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
-
-
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(2-methylpropoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
-
-
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(4-fluorophenoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
-
-
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
-
-
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
-
-
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
-
-
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)methyl]-4-fluorobenzene
-
-
1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 50 nM
1-[1-(3-[3-[3-([2-[benzyl(methyl)amino]ethyl]sulfanyl)-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(2-methylpyrrolidin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(3-hydroxypyrrolidin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-hydroxypiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-methylpiperazin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-methylpiperazin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-methylpiperidin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-methylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-tert-butylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(benzylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(dimethylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(methylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[3-hydroxy-2-oxo-3-(piperidin-4-yl)propyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(4-phenylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(octahydroisoquinolin-2(1H)-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(pyrrolidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-oxo-2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-oxo-2-(pyrrolidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 50 nM
1-[1-(3-[5-acetyl-3-[4-(trifluoromethoxy)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 130 nM
1-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 100 nM
1-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 110 nM
1-[1-[(2R)-3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl]-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 180 nM
1-[1-[(2S)-3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl]-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 200 nM
1-[2-(dimethylamino)ethyl]-6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-[3-(dimethylamino)propyl]-6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-[3-[3-[(2-aminoethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidine-4-carboxamide
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-(methylsulfanyl)ethanone
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxyethanone
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-methoxyethanone
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]ethanone
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]propan-1-one
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-methyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[3-[4-(2-cyanophenyl)piperazin-1-yl]-2-hydroxypropyl]-3-(4-iodophenyl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide
-
IC50: 50 nM
1-[3-[4-(5-methyl-1H-indol-3-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(morpholin-4-yl)propan-2-ol
-
-
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperazin-1-yl)propan-2-ol
-
-
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[4-(2-[[5-[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl]ethyl)piperazin-1-yl]ethanone
-
-
1-[4-(dimethylamino)piperidin-1-yl]-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
-
-
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(3,4-dichlorobenzyl)methanamine
-
-
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(4-methoxybenzyl)methanamine
-
-
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(4-methylbenzyl)methanamine
-
-
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-methylmethanamine
-
-
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(morpholin-4-yl)propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(propylamino)propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(pyrrolidin-1-yl)propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-[4-(pyridin-2-yl)piperidin-1-yl]propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-[4-(pyrrolidin-1-yl)piperidin-1-yl]propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(pyrrolidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
2,2'-[[3-(trifluoromethyl)phenyl]imino]bis[N-(4-methylphenyl)acetamide]
-
-
2,3,4,5,6-pentafluoro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 0.020 mM
2-(1,1'-biphenyl-3-yl)-N-(cyanomethyl)-4-methylpentanamide
-
IC50: 1578 nM
2-(1,1'-biphenyl-4-yl)-N-(cyanomethyl)-4-methylpentanamide
-
IC50: 3343 nM
2-(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)-2-oxoethyl acetate
-
-
2-(4-tert-butylphenyl)-5-[[2-(3,4-dimethoxyphenyl)ethyl]amino]-1,3-oxazole-4-carbonitrile
-
-
2-(4-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperazin-1-yl)benzonitrile
-
IC50: 120 nM
2-([5-[1-[2-hydroxy-3-[(3S)-3-methylmorpholin-4-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(3-methyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(piperidin-1-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(pyrrolidin-1-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-[(3R)-3-hydroxypyrrolidin-1-yl]ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-[(3S)-3-hydroxypyrrolidin-1-yl]ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyrrolidin-1-ylcarbonyl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([5-[1-[3-[4-(2-fluorophenyl)piperazin-1-yl]-2-hydroxypropyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)-1,3-thiazolidine
-
-
2-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)-2,3-dihydro-1,3-benzothiazole
-
-
2-amino-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]ethanone
-
-
2-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 35 nM
2-cyano-4-(2-hydroxyethoxy)-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
-
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
-
2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
-
2-cyano-N-methyl-4-[(spiro[3.5]non-7-ylmethyl)amino]-6-[(2,2,6,6-tetramethylpiperidin-4-yl)oxy]pyrimidine-5-carboxamide
-
-
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
-
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
-
2-hydroxy-1-(1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)ethanone
-
-
2-hydroxy-1-(1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)ethanone
-
-
2-hydroxy-N'-[1H-indol-3-yl(oxo)acetyl]-2,2-diphenylacetohydrazide
-
-
2-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)sulfanyl]ethanol
-
-
2-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-1,3-difluorobenzene
-
-
2-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]biphenyl
-
-
2-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]benzonitrile
-
-
2-[3-(4-chloro-3-[4-[(4-chloro-benzylamino)-methyl]-phenylethynyl]-phenyl)-1-[3-(3-methyl-morpholin-4-yl)-propyl]-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-oxo-acetamide
-
-
2-[3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
-
-
2-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-oxoacetamide
-
-
2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9-(2-hydroxyethyl)-9H-purine-6-carbonitrile
-
-
2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9-ethyl-9H-purine-6-carbonitrile
-
-
2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
-
-
2-[4-methoxy-3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
-
-
2-[5-carbamoyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-1-[[4-(2-cyanophenyl)piperazin-1-yl]methyl]ethyl carbamate
-
IC50: 20 nM
2-[N-(3-chlorophenyl)-L-leucyl]tetrahydropyridazine-1(2H)-carbonitrile
-
-
2-[N-(4-cyanophenyl)-L-leucyl]pyrazolidine-1-carbonitrile
-
-
2-[N-(4-cyanophenyl)-L-phenylalanyl]pyrazolidine-1-carbonitrile
-
-
2-[N-(4-fluorophenyl)-L-valyl]tetrahydropyridazine-1(2H)-carbonitrile
-
-
2-[N-[3-(trifluoromethyl)phenyl]-L-isoleucyl]tetrahydropyridazine-1(2H)-carbonitrile
-
-
2-[[5-(1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(morpholin-4-yl)ethanone
-
-
2-[[5-(1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
-
-
2-[[5-(1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(morpholin-4-yl)ethanone
-
-
2-[[5-(1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
-
-
2-[[5-(5-acetyl-1-[2-hydroxy-3-[4-(2-hydroxypropan-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
-
-
2-[[5-(5-acetyl-1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(morpholin-4-yl)ethanone
-
-
2-[[5-(5-ethyl-1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
-
-
2-[[5-[5-acetyl-1-[2-hydroxy-3-(4-methylpiperidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
-
-
2-{[3-(4-chloro-5-hydroxy-2-methoxyphenyl)-4-oxo-3,4-dihydroquinazolin-2-yl]sulfanyl}-N-[(1S)-1-cyano-1,2-dimethylpropyl]acetamide
-
-
3'-[1-[[(cyanomethy)amino]carbonyl]-3-methylbutyl]-1,1'biphenyl-4-carboxamide
-
IC50: 1373 nM
3-(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)prop-2-yn-1-ol
-
-
3-(4-chloro-3-ethynylphenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-(4-chloro-3-[[2-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-(4-chloro-3-[[3-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-(4-chloro-3-[[4-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 33 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-(naphthalen-2-ylacetyl)-L-alaninamide
-
IC50: 5.0 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-([5-[3-(trifluoromethyl)phenyl]furan-2-yl]acetyl)-L-alaninamide
-
IC50: 3.3 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(3-phenoxyphenyl)acetyl]-L-alaninamide
-
IC50: 8.0 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(4-morpholin-4-ylphenyl)acetyl]-L-alaninamide
-
IC50: 4.0 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(4-phenoxyphenyl)acetyl]-L-alaninamide
-
IC50: 17 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(5-methyl-1-phenyl-1H-pyrazol-4-yl)acetyl]-L-alaninamide
-
IC50: 34 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[[4-(1H-1,2,4-triazol-1-yl)phenyl]acetyl]-L-alaninamide
-
IC50: 26 nM
3-cyclohexyl-N2-(5-fluoro-1,3-benzoxazol-2-yl)-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
-
IC50: 197 nM
3-cyclohexyl-N2-(6-fluoro-1,3-benzoxazol-2-yl)-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
-
IC50: 43 nM
3-cyclohexyl-N2-([4-[(4,6-dimethylpyrimidin-2-yl)amino]phenyl]acetyl)-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 2.0 nM
3-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,5-dimethyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 30 nM
3-[3-(benzylsulfanyl)-4-chlorophenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide
-
-
3-[4-chloro-3-(4-methylpent-1-yn-1-yl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(cyclohexylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(hept-1-yn-1-yl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(phenylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(propylsulfanyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(thiophen-2-ylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(thiophen-3-ylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(2-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(2-methoxyphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(2-methylphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(2-phenoxyethyl)sulfanyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(2-phenylethyl)sulfanyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(3,4-dichlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(3-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(4-methoxyphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(4-methylphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[[(2S)-2-[([3-acetyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
3-[[(2S)-2-[[(4-[[(4-aminophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]benzamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
4-(3-acetylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-bromophenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-chlorophenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-cyclobutylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-cyclopentylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-cyclopropylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-ethylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-methylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-tert-butylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(acetylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 123 nM
4-(dimethylamino)-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
-
-
4-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 16 nM
4-fluoro-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
-
-
4-hydroxy-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
-
-
4-phenyl-6-propylpyrimidine-2-carbonitrile
-
-
4-propyl-6-(3-propylphenyl)pyrimidine-2-carbonitrile
-
-
4-propyl-6-[2-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-propyl-6-[3-(trifluoromethoxy)phenyl]pyrimidine-2-carbonitrile
-
-
4-propyl-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-propyl-6-[4-(trifluoromethoxy)-3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-propyl-6-[4-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]aniline
-
-
4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzoic acid
-
-
4-[(4-[(E)-[(cyanoacetyl)hydrazono]methyl]phenoxy)methyl]benzoic acid
-
-
4-[1-(2-hydroxy-3-[3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(3-[3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(3-[5-tert-butoxy-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(3-[5-tert-butoxy-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[2-chloro-5-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[3,5-bis(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[3-(2-methylpropyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[3-(methylsulfonyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[3-(propan-2-yl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-[4-(propan-2-yloxy)-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[4-chloro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[4-ethoxy-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[4-fluoro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[4-methoxy-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[4-methyl-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]benzamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]benzoic acid
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-3-[3-[(2-phenoxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-(methylsulfonyl)-1-[3-[4-(1H-pyrrolo[3,2-c]pyridin-3-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-(piperidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-(pyrrolidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-[4-(pyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-chloro-3-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 150 nM
5-chloro-3-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 80 nM
6-(4-chlorobenzyl)-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-(2-cyclooctylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-(2-piperidine-1-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(3,3-dimethylbutyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-(4,4-dimethylpentyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-[2-(3-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-chloro-1-(1-[3-[3-(4-chloro-3-methylphenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 50 nM
6-chloro-1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 60 nM
6-chloro-1-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 30 nM
6-[3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
-
-
6-[4-(2-hydroxyethoxy)-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-(2-hydroxyethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
-
-
6-[4-(3-oxopropyl)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-(ethylamino)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-[2-(morpholin-4-yl)ethyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-[3-(morpholin-4-yl)propyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-ethoxy-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
-
-
6-[4-methoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-phenoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-[2-(2-oxopyrrolidin-1-yl)ethoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
-
-
6-[4-[2-(dimethylamino)ethoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-[3-(2-ethyl-1H-imidazol-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
-
-
6-[4-[3-(4-ethylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
-
-
6-[4-[3-(dimethylamino)propoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[[4-(1-acetyl-1,2,3,6-tetrahydropyridine-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
6-[[4-(1-acetylpiperidin-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(1-acetylpiperidine-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
6-[[4-(4-acetyl-1,4-diazepan-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)-3-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazine-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-(4-methoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2-cyclohexylethyl)-6-(naphthalen-1-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2-cyclohexylethyl)-6-[(pyridine-2-yloxy)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[(pyridine-2-ylsulfanyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[[methyl(phenyl)amino]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-tert-butyl-6-(4-chlorobenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
9-[3-(dimethylamino)propyl]-2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
-
-
APC-2848
-
irreversible vinyl-sulfone inhibitor
benzyl [(2S)-1-(2-cyanotetrahydropyridazin-1(2H)-yl)-3-methyl-1-oxopentan-2-yl]carbamate
-
-
benzyloxycarbonyl-Ala-Leu-COCHO
-
-
Benzyloxycarbonyl-Phe-Ala-CHN2
-
-
benzyloxycarbonyl-Phe-Ala-COCHO
-
-
Benzyloxycarbonyl-Phe-Arg
-
-
benzyloxycarbonyl-Phe-Arg-COCHO
-
-
benzyloxycarbonyl-Phe-Leu-COCHO
-
potent, reversible cathepsin S inhibitor, the inhibitor is 400fold more selective for cathepsin S than for cathepsin B
Benzyloxycarbonyl-Phe-Phe-CHN2
-
0.001 mM, 98% inhibition
benzyloxycarbonyl-Phe-Tyr(OBut)-COCHO
-
-
benzyloxycarbonyl-Tyr-Ala-CHN2
-
0.001 mM, 88% inhibition
benzyloxycarbonyl-Tyr-Tyr(O-butyl)-CHN2
-
1 mM, 78% inhibition
benzyloxycarbonyl-Val-Val-Lys-NHO-4-nitrobenzoyl
-
-
carbobishydrazide
-
irreversible cathepsin S inhibitor
cathepsin K propeptide
-
-
-
cathepsin L propeptide
-
-
-
cathepsin S propeptide
-
0.0002 mM, blocks gelatinase, collagenase and elastinase activities of mature cathepsin S
-
chimeric propeptide of cathepsin S and cathepsin L S1-54/L44-86
-
-
-
CLIK-066
-
0.01 mM, 28% inhibition
CLIK-088
-
0.01 mM, 64% inhibition
CLIK-112
-
0.01 mM, 77% inhibition
CLIK-121
-
0.01 mM, complete inhibition
CLIK-148
-
0.01 mM, complete inhibition
CLIK-181
-
0.01 mM, 80% inhibition
CLIK-195
-
0.01 mM, complete inhibition
cystatin
-
0.001 mM, complete inhibition
-
dipeptide-vinyl sulfone LHVS
-
irreversible cathepsin S inhibitor
epoxysuccinyl-Ala benzyl ester
-
-
epoxysuccinyl-Arg benzyl ester
-
-
epoxysuccinyl-D-Phe benzyl amide
-
-
epoxysuccinyl-D-Phe benzyl ester
-
-
epoxysuccinyl-Ile benzyl ester
-
-
epoxysuccinyl-Leu benzyl amide
-
-
epoxysuccinyl-Leu benzyl ester
-
-
epoxysuccinyl-Phe benzyl amide
-
-
epoxysuccinyl-Phe benzyl ester
-
-
epoxysuccinyl-Val benzyl ester
-
-
ethyl (3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoate
-
IC50: 71 nM
methyl (2R)-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)(phenyl)ethanoate
-
-
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-4-[(1S)-1-[(1R)-2-[(1-cyanocyclopropyl)amino]-1-(methoxysulfinyl)methyl]-2-oxoethyl]amino)-2,2,2-trifluoroethyl]-4'-fluorobiphenyl
-
-
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfenate
-
-
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfinate
-
-
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(3-fluorophenyl)ethyl]amino]propane-1-sulfinate
-
-
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfenate
-
-
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfinate
-
-
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propane-1-sulfinate
-
-
methyl (2S)-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)(phenyl)ethanoate
-
-
methyl (2Z)-4-[4-(dimethylamino)phenyl]-4-oxo-2-[(phenylcarbonyl)hydrazono]butanoate
-
-
methyl (3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(oxo)acetate
-
-
methyl (3R)-3-[[(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanoyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate
-
-
methyl (3S)-3-[[(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanoyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate
-
-
methyl 1-[2-hydroxy-3-(4-quinolin-4-ylpiperazin-1-yl)propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(2-oxo-2,3-dihydro-4,1-benzoxazepin-1(5H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidine-4-carboxylate
-
-
methyl 1-[3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(5-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(6-chloro-2,2-dioxido-3,4-dihydro-1H-2,1,3-benzothiadiazin-1-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 2-amino-4-([(1S)-2-(1-[(benzyloxy)methyl]-3-[(2-ethoxy-2-oxoethyl)amino]-2,3-dioxopropylamino)-1-(cyclohexylmethyl)-2-oxoethyl]aminocarbonyl)benzoate
-
-
methyl 2-[[(1S)-1-(cyclohexylmethyl)-2-([2-[(4-fluorophenyl)amino]ethyl]amino)-2-oxoethyl]amino]-1,3-benzoxazole-6-carboxylate
-
IC50: 43 nM
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(3,4-dihydroisoquinolin-2(1H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(5-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2,2-dioxido-3,4-dihydro-1H-2,1,3-benzothiadiazin-1-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 4'-[(1S)-1-([(1S)-1-[(1-cyanocyclopropyl)carbamoyl]pentyl]amino)-2,2,2-trifluoroethyl]biphenyl-4-sulfinate
-
-
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
-
-
methyl 4-[(E)-[[(3-[2-[(2-chlorobenzyl)oxy]phenyl]-1H-pyrazol-5-yl)carbonyl]hydrazono]methyl]benzoate
-
-
morpholine-4-carboxylic acid [1-[1S-(N-benzoyl-hydrazinomethyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
IC50: 565 mM
morpholine-4-carboxylic acid [1R-(1S-cyano-3-phenyl-propylcarbamoyl)-1,3-dimethyl-butyl]-amide
-
-
morpholine-4-carboxylic acid [1R-(1S-cyano-3-phenyl-propylcarbamoyl)-3-methylbutyl]amide
-
IC50: 0.011 mM
morpholine-4-carboxylic acid [1S-(1R-cyano-3-phenylpropylcarbamoyl)-3-methylbutyl]amide
-
IC50: 387 nM
morpholine-4-carboxylic acid [1S-(1S-cyano-2,2-dimethylpropylcarbamoyl)-3-methylbutyl]amide
-
IC50: 0.107 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-2-methyl-propylcarbamoyl)-3-methylbutyl]amide
-
IC50: 1400 nM
morpholine-4-carboxylic acid [1S-(1S-cyano-2-phenylethylcarbamoyl)-3-methylbutyl]amide
-
IC50: 130 nM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenyl-propylcarbamoyl)-1,3-dimethyl-butyl]-amide
-
IC50: 0.076 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-cyclohexyl-ethyl]-amide
-
IC50: 5 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-methyl-propyl]-amide
-
IC50: 0.006 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-phenyl-ethyl]-amide
-
IC50: 173 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-3,3-dimethyl-butyl]-amide
-
IC50: 23 nM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-cyclohexyl-R-methyl]-amide
-
IC50: 84 nM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-ethyl]-amide
-
IC50: 0.134 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-pentyl]-amide
-
IC50: 41 nM
morpholine-4-carboxylic acid [1S-(1S-cyanobutylcarbamoyl)-3-methylbutyl]amide
-
IC50: 82 nM
morpholine-4-carboxylic acid [1S-(1S-cyanobutylcarbamoyl)-3-methylpentyl]amide
-
IC50: 56 nM
morpholine-4-carboxylic acid [1S-(1S-cyanomethylcarbamoyl)-3-methylbutyl]amide
-
IC50: 142 nM
morpholine-4-carboxylic acid [1S-(2-benzyloxy-1R-cyano-ethylcarbamoyl)-3-methylbutyl]amide
-
IC50: 19 nM
morpholine-4-carboxylic acid [1S-(cyanomethylcarbamoyl)-3-methylbutyl]amide
-
IC50: 124 nM
morpholine-4-carboxylic acid [1S-[(1-cyano-1-methyl)ethylcarbamoyl]-3-methylbutyl]amide
-
IC50: 114 nM
morpholine-4-carboxylic acid [1S-[(cyano-phenyl-S-methyl)carbamoyl]-3-methylbutyl]amide
-
IC50: 51 nM
morpholine-4-carboxylic acid [1S-[1S-(benzoyl-hydrazonomethyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
IC50: 11 nM
morpholine-4-carboxylic acid [1S-[1S-cyano-2-(3,4-dichlorophenyl)ethylcarbamoyl]-3-methylbutyl]amide
-
IC50: 56 nM
morpholine-4-carboxylic acid [1S-[1S-[(2-hydroxy-benzoyl)-hydrazonomethyl]-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
IC50: 7 nM
morpholine-4-carboxylic acid [1S-[1S-[(4-hydroxybenzoyl)-hydrazonomethyl]-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
IC50: 35 nM
morpholine-4-carboxylic acid [1S-[2-(2-chlorobenzyloxy)-1R-cyanoethylcarbamoyl]-3-methylbutyl]amide
-
9 nM
morpholine-4-carboxylic acid [1S-[2-(3-chlorobenzyloxy)-1R-cyanoethylcarbamoyl]-3-methylbutyl]amide
-
9 nM
morpholine-4-carboxylic acid [1S-[2-(4-chlorobenzyloxy)-1R-cyanoethylcarbamoyl]-3-methylbutyl]amide
-
27 nM
morpholine-4-carboxylic acid [3-methyl-1S-(1-prop-2-ynylcarbamoyl)butyl]amide
-
IC50: 0.097 m
morpholine-4-carboxylic acid [3-methyl-1S-(1R-methyl-3-phenylpropylcarbamoyl)butyl]amide
-
IC50 above 0.339 mM
morpholine-4-carboxylic acid [3-methyl-1S-(3-phenyl-propylcarbamoyl)butyl]amide
-
IC50 above 0.028 mM
morpholineurea-leucyl-homophenylalanine-vinylsulfone phenyl
-
LHVS, CatS-specific inhibitor at a concentration of 10 nM, other cathepsins are not inhibited
N,N-dimethyl-2-([5-[5-(methylsulfonyl)-1-[3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)acetamide
-
-
N-(1-cyanocyclopropyl)-3-(methylsulfinyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-(4'-fluorobiphenyl-4-yl)ethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-phenylethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-[(3,4-dichlorophenyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-[(4-fluorobenzyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-phenylethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-[(4-fluorophenyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-[[2-(4-fluorophenyl)propan-2-yl]sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(4-chlorobenzyl)-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
-
-
N-(4-cyano-1-phenyl-1H-pyrazol-5-yl)-2-[(4-ethyl-5-thiophen-2-yl-4H-1,2,4-triazol-3-yl)sulfanyl]acetamide
-
-
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetamide
-
-
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]phenyl)acetamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]phenyl)propanamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
N-(cyanomethyl)-2-[3-(1H-indol-5-yl)phenyl]-4-methylpentanamide
-
IC50: 922 nM
N-(cyanomethyl)-2-[3-(1H-indol-6-yl)phenyl]-4-methylpentanamide
-
IC50: 1257 nM
N-(cyanomethyl)-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]-3-phenylpropanamide
-
IC50 above 0.01 mM
N-(cyanomethyl)-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]acetamide
-
IC50 above 0.01 mM
N-(cyanomethyl)-3-cyclobutyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]propanamide
-
IC50: 2310 nM
N-(cyanomethyl)-3-cyclopropyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]propanamide
-
IC50: 6597 nM
N-(cyanomethyl)-4-methyl-2-(2-phenyl-1,3-thiazol-4-yl)pentanamide
-
IC50 above 0.01 mM
N-(cyanomethyl)-4-methyl-2-(3'-piperazin-1-yl-1,1'-biphenyl-3-yl)pentanamide methanesulfonate
-
IC50 above 0.01 mM
N-(cyanomethyl)-4-methyl-2-(3-pyridin-3-ylphenyl)-pentanamide
-
IC50 above 0.01 nM
N-(cyanomethyl)-4-methyl-2-(3-pyridin-4-ylphenyl)-pentanamide trifluoroacetate
-
IC50: 1748 nM
N-(cyanomethyl)-4-methyl-2-(3-pyrimidin-5-ylphenyl)pentanamide
-
IC50 above 0.01 mM
N-(cyanomethyl)-4-methyl-2-(5-phenylpyridin-3-yl)-pentanamide trifluoroacetate
-
IC50 above 0.01 mM
N-(cyanomethyl)-4-methyl-2-[2'-(1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 521 nM
N-(cyanomethyl)-4-methyl-2-[2'-(4-morpholinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 3368 nM
N-(cyanomethyl)-4-methyl-2-[3'-(4-morpholinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50 above 0.01 mM
N-(cyanomethyl)-4-methyl-2-[4'-(1,2,3,6-tetrahydro-4-pyridinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 652 nM
N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 1245 nM
N-(cyanomethyl)-4-methyl-2-[4'-(4-methyl-1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 1695 nM
N-(cyanomethyl)-4-methyl-2-[4'-(4-morpholinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 9422 nM
N-(cyanomethyl)-4-methyl-2-[4'-(4-piperidinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 1421 nM
N-(cyanomethyl)-4-methyl-2-[4'-(methylsulfonyl)-1,1'-biphenyl-3-yl]pentanamide
-
IC50: 6623 nM
N-benzyl-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-methylmethanamine
-
-
N-benzyl-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
-
-
N-benzyl-2-([5-[5-(methylsulfonyl)-1-[3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)acetamide
-
-
N-methyl-2-([5-[5-(methylsulfonyl)-1-[3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)acetamide
-
-
N-morpholinurea-leucine-homophenylalanine-vinylsulfone-phenyl
N-morpholinurea-leucyl-homophenylalanyl-vinylsulfone-phenyl
-
i.e. LHVS, irreversible inhibition, the inhibitor binds covalently to the active site, in vitro and in vivo inhibition
N-morpholinurealeucine-homophenylalanine-vinylsulfone-phenyl
-
-
N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-norvalinamide
-
-
N-[(1R)-1-([2-[(1,3-benzoxazol-2-ylsulfanyl)acetyl]hydrazino]carbonyl)propyl]-2-[(phenylcarbonyl)amino]benzamide
-
-
N-[(1S)-1-(1H-indol-2-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
-
IC50: 29 nM
N-[(1S)-1-(biphenyl-4-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
-
IC50: 34 nM
N-[(1S)-1-(cyclohexylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
-
IC50: 62 nM
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-1-benzofuran-2-carboxamide
-
IC50: 17 nM
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-(3-fluorophenyl)furan-2-carboxamide
-
IC50: 34 nM
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-[3-(trifluoromethyl)phenyl]furan-2-carboxamide
-
IC50: 11 nM
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-2-carboxamide
-
IC50: 47 nM
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-3-carboxamide
-
IC50: 6 nM
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-3-carboxamide
-
IC50: 213 nM
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
-
IC50: 11 nM
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydro-2H-pyran-4-carboxamide
-
IC50: 12 nM
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-3-carboxamide
-
IC50: 21 nM
N-[(1S)-1-(furan-2-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
-
IC50: 0.020 mM
N-[(1S)-1-cyclohexyl-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
-
IC50: 23 nM
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1,2-dimethylpropyl]benzamide
-
-
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1,2-dimethylpropyl]thiophene-3-carboxamide
-
-
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-(4-methylcyclohexyl)ethyl]thiophene-3-carboxamide
-
-
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-(trans-4-methylcyclohexyl)ethyl]thiophene-3-carboxamide
-
-
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-cyclohexylethyl]benzamide
-
-
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-cyclohexylethyl]thiophene-3-carboxamide
-
-
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-1-(naphthalen-2-ylmethyl)-2-oxoethyl]-3-methylbenzamide
-
IC50: 16 nM
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(1,3-thiazol-5-ylmethyl)ethyl]-3-methylbenzamide
-
IC50: 0.065 mM
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(pyridin-3-ylmethyl)ethyl]-3-methylbenzamide
-
IC50: 3707 nM
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(pyridin-4-ylmethyl)ethyl]-3-methylbenzamide
-
IC50: 6769 nM
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-phenylethyl]-3-methylbenzamide
-
IC50: 285 nM
N-[(1S)-3-cyclohexyl-1-([2-[(4-methoxyphenyl)amino]ethyl]carbamoyl)propyl]-3-methylbenzamide
-
IC50: 38 nM
N-[(1S)-3-methyl-1-(((4S)-3-oxo-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl)carbamoyl)butyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
-
-
N-[(2S)-1-([4-cyano-1-[3-(morpholin-4-yl)propyl]piperidin-4-yl]amino)-5,5-dimethyl-1-oxoheptan-2-yl]morpholine-4-carboxamide
-
-
N-[(2S)-1-[[(1R)-2-(benzyloxy)-1-cyanoethyl]amino]-3-cyclohexyl-1-oxopropan-2-yl]morpholine-4-carboxamide
-
-
N-[(2S)-2-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-3-methylbutan-2-yl]thiophene-3-carboxamide
-
-
N-[(2S)-3-cyclohexyl-1-([2-[(4-methoxyphenyl)amino]ethyl]amino)-1-oxopropan-2-yl]-5-[3-(trifluoromethyl)phenyl]furan-2-carboxamide
-
-
N-[(2S)-3-cyclohexyl-1-[[(2S)-1-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)propan-2-yl]amino]-1-oxopropan-2-yl]morpholine-4-carboxamide
-
-
N-[(2S)-3-methyl-2-[1-[(2S)-1-oxohexan-2-yl]-1H-1,2,3-triazol-4-yl]butan-2-yl]thiophene-3-carboxamide
-
-
N-[(3S)-4-benzyloxy-(2S)-4-methyl-[[[2-[(9-oxo-9H-1-fluorenyl)carbonyl]amino]propaneyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[(2S)-2-[(3-amino-4-chlorobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[(2S)-2-[(3-[(tert-butoxycarbonyl)amino]-4-chlorobenzoyl amino)]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ester
-
-
N-[(3S)-4-benzyloxy-3-[[[1-[(4-morpholinylcarbonyl)-amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[((1-methylcyclopropyl)carbonyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
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
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[((5-nitro-2-thienyl)carbonyl)amino]cyclo-hexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
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
-
-
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
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[(2-(2-thienyl)acetyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[(2-chloro-5-(methylsulfanyl)benzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[(3-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[(4-chloro-3-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[(4-methoxybenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[(5-chloro-2-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[(5-methoxy-2-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[2-(1-methylethyl)phenyl]-Na-(phenoxycarbonyl)-L-tryptophanamide
-
-
N-[2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)ethyl]-N2-(3-methylbenzoyl)-L-leucinamide
-
-
N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]-2-phenylacetamide
-
-
N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
-
-
N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]piperidine-3-carboxamide
-
-
N-[2-oxo-2-[(2Z)-2-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)hydrazino]ethyl]-2-pyridin-2-yl-1H-benzimidazole-1-carboxamide
-
-
N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-N2-[(3-methylphenyl)carbonyl]-L-leucinamide
-
IC50: 46 nM
N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 27 nM
N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-(3-methylbenzoyl)-L-leucinamide
-
-
N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(3-methylphenyl)carbonyl]-L-leucinamide
-
IC50: 62 nM
N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-4-(trifluoromethyl)-L-phenylalaninamide
-
IC50: 19 nM
N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 29 nM
N-[2-[(4-methoxyphenyl)amino]ethyl]-O-methyl-Na-[(3-methylphenyl)carbonyl]-L-tyrosinamide
-
IC50: 66 nM
N-[4-(4-cyano-1H-imidazo[4,5-c]pyridin-6-yl)-2-(trifluoromethyl)phenyl]formamide
-
-
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]-1-phenylethanamine
-
-
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]-2-phenylethanamine
-
-
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]benzamide
-
-
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]benzenesulfonamide
-
-
N-[[(2S)-1-[[(1S)-1-cyano-3-phenylpropyl]amino]-3-cyclohexyl-1-oxopropan-2-yl]carbamoyl]morpholine-4-carboxamide
-
-
N2-(5-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
-
IC50: 173 nM
N2-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[(1S)-1-[(5-fluoro-2,3-dihydro-1H-indol-1-yl)methyl]-3-(methylsulfonyl)propyl]-L-alaninamide
-
IC50: 21 nM
N2-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[(1S)-2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
-
IC50: 151 nM
N2-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
-
IC50: 93 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-(1-methyl-2-[[3-(methylsulfonyl)phenyl]amino]ethyl)-L-alaninamide
-
IC50: 26 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-(1-methyl-2-[[4-(methylsulfonyl)phenyl]amino]ethyl)-L-alaninamide
-
IC50: 11 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[(2S)-1-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)propan-2-yl]-L-alaninamide
-
-
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-2,2-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
-
IC50: 15 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
-
IC50: 15 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-2-oxo-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
-
IC50: 12.3 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
-
IC50: 3 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
-
IC50: 19 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]-1-methylethyl]-L-alaninamide
-
IC50: 1 nM
N2-(biphenyl-3-ylacetyl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 2.9 nM
N2-(biphenyl-4-ylacetyl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 9.1 nM
N2-(morpholin-4-ylcarbonyl)-N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-leucinamide
-
-
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[(1S)-2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
-
IC50: 26 nM
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)ethyl]-L-alaninamide
-
IC50: 222 nM
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
-
IC50: 94 nM
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 29 nM
N2-1,3-benzoxazol-2-yl-N-[(1R)-2-(benzyloxy)-1-[(5-fluoro-2,3-dihydro-1H-indol-1-yl)methyl]ethyl]-3-cyclohexyl-L-alaninamide
-
IC50: 5 nM
N2-benzoyl-N1-(cyanomethyl)-L-leucinamide
-
IC50: 41 nM
N2-[(3'-chlorobiphenyl-4-yl)acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 7.4 nM
N2-[(5-chloro-1-benzofuran-2-yl)acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 9.4 nM
N2-[[1-(5-bromopyrimidin-2-yl)piperidin-3-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 49 nM
N2-[[1-(5-bromopyrimidin-2-yl)piperidin-4-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 107 nM
N2-[[5-(4-chlorophenyl)furan-2-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 7.1 nM
o-aminobenzoic acid-Leu-Phe-Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
-
o-aminobenzoic acid-Val-Leu-Phe-Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
-
paecilopeptin
-
i.e. acetyl-Leu-Val-CHO, IC50: 21 nM
Peptidyl(acyloxy)methyl ketones
-
extremely potent inactivator
-
propeptide1-98 of chimeric cathepsin S
-
-
-
squamous cell carcinoma antigen 1
-
99% inhibition at 1 mM, interacts with cathespin S at 1:1 stoichiometry, t1/2 of the cathepsin-squamous cell carcinoma antigen 1 complex is above 1155 min
-
tert-butyl (3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoate
-
IC50: 730 nM
tert-butyl 1'-[(2S)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]-4,4'-bipiperidine-1-carboxylate
-
-
tert-butyl 4-[3'-[1-[[(cyanomethyl)amino]carbonyl]-3-methylbutyl]-1,1'-biphenyl-4-yl]piperazine-1-carboxylate
-
IC50: 1298 nM
tert-butyl 4-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperazine-1-carboxylate
-
-
tert-butyl [(2S)-1-(2-cyanopyrazolidin-1-yl)-1-oxo-3-phenylpropan-2-yl]carbamate
-
-
tert-butyl [(2S)-1-(2-cyanopyrazolidin-1-yl)-3-methyl-1-oxobutan-2-yl]carbamate
-
-
tert-butyl [(2S)-1-(2-cyanopyrazolidin-1-yl)-4-methyl-1-oxopentan-2-yl]carbamate
-
-
tert-butyl [(2S)-1-(2-cyanotetrahydropyridazin-1(2H)-yl)-3-methyl-1-oxobutan-2-yl]carbamate
-
-
tetrahydro-2H-pyran-4-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
-
IC50: 12 nM
Tg1 domain of testican-1
-
-
-
[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]benzene
-
-
[(2',3',4'-trifluorobiphenyl-2-yl)oxy]acetaldehyde
-
-
[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl](pyrrolidin-1-yl)methanone
-
-
[1S-(1S-cyano-3-phenylpropylcarbamoyl)-3-methylbutyl]-amide
-
IC50: 42 nM
[1S-(2-cyano-1S-phenethyl-ethylcarbamoyl)-3-methylbutyl]amide
-
IC50 above 0.02 mM
[2-[[(4-chlorophenyl)sulfanyl]methyl]-4-hydroxy-6,7-dimethoxyquinazolin-3(4H)-yl]acetonitrile
-
-
[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl](1H-1,2,4-triazol-3-yl)methanone
-
-
[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl](pyrrolidin-1-yl)methanone
-
-
[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl](thiophen-2-yl)methanone
-
-
[[2',3'-difluoro-4'-(2-methylpropyl)biphenyl-2-yl]oxy]acetaldehyde
-
-
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
(3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoic acid
-
-
(3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoic acid
-
IC50: 27 nM
1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
-
1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 50 nM
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
7-(2-cyclohexylethyl)-6-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2-cyclohexylethyl)-6-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
cathespin S propeptide
-
-
-
cathespin S propeptide
-
tight binding/slow reacting inhibition
-
cathespin S propeptide
-
more selective for inhibition of cathepsin L than cathepsin S
-
CLIK-060
-
strong
CLIK-060
-
0.001 mM, complete inhibition
cystatin C
-
-
-
cystatin C
-
endogenous specific enzyme inhibitor, absence of cystatin C results in increased angiogene sis and tumor cell proliferation
-
cystatin C
-
endogenous specific inhibitor
-
cystatin C
-
specific endogenous inhibitor, potency against smooth muscle cell invasion, overview
-
E-64
-
-
E-64
-
irreversible inhibitor
E-64
-
0.001 mM, 96% inhibition
E64
-
-
E64
-
potency against smooth muscle cell invasion, overview
E64
-
cysteine protease inhibitor
JNJ 10329670
-
CAS: 400797-24-2, the inhibitor blocks the presentation of tetanus toxoid and giant ragweed by human PBMCs, the inhibitor is a candidate for immunosuppressive therapy of allergies and autoimmune diseases, completely reversible inhibition
JNJ 10329670
-
competitive, reversible inhibition, 4-(2-keto-1-benzimidazolinyl)-piperidin-1-yl derivative, IC50: 100 nM
leupeptin
-
-
N-morpholinurea-leucine-homophenylalanine-vinylsulfone-phenyl
-
specific inhibitor
N-morpholinurea-leucine-homophenylalanine-vinylsulfone-phenyl
-
i.e. LHVS, specific inhibitor, potency against smooth muscle cell invasion, overview
additional information
-
analysis of inhibition mechanisms and binding to the active site
-
additional information
-
design and synthesis of arylaminoethyl amides as noncovalent inhibitors of cathepsin S, overview
-
additional information
-
inhibitory potential in vivo on Ii degradation in JY cells
-
additional information
-
reversible inhibition by a dipeptide-nitrile inhibitor
-
additional information
-
synthesis and evaluation of heterocyclic arylaminoethyl amides as noncovalent inhibitors of cathepsin S, binding specificities of positions P1-P3 and of subsite S3, overview
-
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Acute Coronary Syndrome
Association of Circulating Cathepsin S and Cardiovascular Disease Among Patients With Type 2 Diabetes: A Cross-Sectional Community-Based Study.
Acute Coronary Syndrome
Relationship between plasma cathepsin S and cystatin C levels and coronary plaque morphology of mild to moderate lesions: an in vivo study using intravascular ultrasound.
Adenocarcinoma
Antibody-mediated inhibition of cathepsin S blocks colorectal tumor invasion and angiogenesis.
Albuminuria
Cathepsin S Cleavage of Protease-Activated Receptor-2 on Endothelial Cells Promotes Microvascular Diabetes Complications.
Albuminuria
Cathepsin S inhibition combines control of systemic and peripheral pathomechanisms of autoimmune tissue injury.
Alzheimer Disease
Cathepsin S increases tau oligomer formation through limited cleavage, but only IL-6, not cathespin S serum levels correlate with disease severity in the neurodegenerative tauopathy progressive supranuclear palsy.
Alzheimer Disease
Improvement of cathepsin S detection using a designed FRET peptide based on putative natural substrates.
Alzheimer Disease
Lysosomal processing of amyloid precursor protein to A beta peptides: a distinct role for cathepsin S.
Alzheimer Disease
The lysosomal cysteine protease, cathepsin S, is increased in Alzheimer's disease and Down syndrome brain. An immunocytochemical study.
Anemia
Digital Hemoglobinometers as Point-of-Care Testing Devices for Hemoglobin Estimation: A Validation Study from India.
Anemia
Integrated point-of-care testing (POCT) for HIV, syphilis, malaria and anaemia at antenatal facilities in western Kenya: a qualitative study exploring end-users' perspectives of appropriateness, acceptability and feasibility.
Aneurysm
Cysteine Protease Cathepsins in Atherosclerotic Cardiovascular Diseases.
Aneurysm
Insights from molecular modeling into the selective inhibition of cathepsin S by its inhibitor.
Angina, Stable
Association of Circulating Cathepsin S and Cardiovascular Disease Among Patients With Type 2 Diabetes: A Cross-Sectional Community-Based Study.
Angina, Stable
Clinical application of simultaneous detection of cystatin C, cathepsin S, and IL-1 in classification of coronary artery disease.
Angina, Stable
Interrelated Cathepsin S-Lowering and LDL Subclass Profile Improvements Induced by Atorvastatin in the Plasma of Stable Angina Patients.
Angina, Unstable
Clinical application of simultaneous detection of cystatin C, cathepsin S, and IL-1 in classification of coronary artery disease.
Angina, Unstable
Increased serum cathepsin S in patients with atherosclerosis and diabetes.
Aortic Aneurysm
Adenosine-to-inosine RNA editing controls cathepsin S expression in atherosclerosis by enabling HuR-mediated post-transcriptional regulation.
Aortic Aneurysm
Smad4 Deficiency in Smooth Muscle Cells Initiates the Formation of Aortic Aneurysm.
Aortic Aneurysm, Abdominal
Cathepsin S is associated with degradation of collagen I in abdominal aortic aneurysm.
Aortic Aneurysm, Abdominal
Combined Cathepsin S and hs-CRP predicting inflammation of abdominal aortic aneurysm.
Aortic Aneurysm, Abdominal
Deficiency of cathepsin S attenuates angiotensin II-induced abdominal aortic aneurysm formation in apolipoprotein E-deficient mice.
Aortic Aneurysm, Abdominal
Determination of cathepsin S abundance and activity in human plasma and implications for clinical investigation.
Aortic Aneurysm, Abdominal
Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm.
Aortic Aneurysm, Abdominal
Pharmacological Inhibition of Cathepsin S Suppresses Abdominal Aortic Aneurysm in Mice.
Aortic Aneurysm, Abdominal
Plasma cathepsin s and cystatin C levels and risk of abdominal aortic aneurysm: a randomized population-based study.
Aortic Aneurysm, Abdominal
Plasma Cathepsin S is Associated with High-density Lipoprotein Cholesterol and Bilirubin in Patients with Abdominal Aortic Aneurysms.
Aortic Diseases
Upregulation of elastase proteins results in aortic dilatation in mucopolysaccharidosis I mice.
Aortic Valve Disease
Apolipoprotein A-I proteolysis in aortic valve stenosis: role of cathepsin S.
Aortic Valve Stenosis
Apolipoprotein A-I proteolysis in aortic valve stenosis: role of cathepsin S.
Arteriosclerosis
Effects of intermittent exercise on biomarkers of cardiovascular risk in night shift workers.
Arteritis
Cathepsin S and Protease-Activated Receptor-2 Drive Alloimmunity and Immune Regulation in Kidney Allograft Rejection.
Arthritis
Cathepsin S inhibitors as novel immunomodulators.
Arthritis
Cathepsin S regulates renal fibrosis in mouse models of mild and severe hydronephrosis.
Arthritis
Cathepsin S: therapeutic, diagnostic, and prognostic potential.
Arthritis
Collagenolytic protease expression in cranial cruciate ligament and stifle synovial fluid in dogs with cranial cruciate ligament rupture.
Arthritis
Exploring fragment-based target-specific ranking protocol with machine learning on cathepsin S.
Arthritis
Molecular modeling assisted identification and biological evaluation of potent cathepsin S inhibitors.
Arthritis
Spinal cathepsin S and fractalkine contribute to chronic pain in collagen induced arthritis.
Arthritis
The P2X7 Receptor, Cathepsin S and Fractalkine in the Trigeminal Subnucleus Caudalis Signal Persistent Hypernociception in Temporomandibular Rat Joints.
Arthritis, Experimental
Impaired invariant chain degradation and antigen presentation and diminished collagen-induced arthritis in cathepsin S null mice.
Arthritis, Rheumatoid
Advances in cathepsin S inhibitor design.
Arthritis, Rheumatoid
An orally active reversible inhibitor of cathepsin S inhibits human trans vivo delayed-type hypersensitivity.
Arthritis, Rheumatoid
Cathepsin S and cathepsin L in serum and synovial fluid in rheumatoid arthritis with and without autoantibodies.
Arthritis, Rheumatoid
Cathepsin S inhibitors: WO2010070615.
Arthritis, Rheumatoid
Circulating plasma levels of cathepsin S and L are not associated with disease severity in patients with rheumatoid arthritis.
Arthritis, Rheumatoid
Serum cathepsin S and cystatin C: relationship to subclinical carotid atherosclerosis in rheumatoid arthritis.
Arthritis, Rheumatoid
The role of cathepsins in osteoporosis and arthritis: rationale for the design of new therapeutics.
Asthma
Association between SNPs in the promoter region in cathepsin S and risk of asthma in Chinese Han population.
Asthma
Binding of chondroitin 4-sulfate to cathepsin s regulates its enzymatic activity.
Asthma
Circadian and concentration profile of cathepsin S in sera from healthy subjects and asthmatic patients.
Asthma
Genetic and Pharmacological Evaluation of Cathepsin S in a Mouse Model of Asthma.
Asthma
Overexpression of cathepsin s induces chronic atopic dermatitis in mice.
Asthma
Single nucleotide polymorphisms of cathepsin S and the risks of asthma attack induced by acaroid mites.
Astrocytoma
Cathepsin S expression: An independent prognostic factor in glioblastoma tumours--A pilot study.
Astrocytoma
Detection of cathepsin S cysteine protease in human brain tumour microdialysates in vivo.
Astrocytoma
The clinical significance of cathepsin S expression in human astrocytomas.
Atherosclerosis
A novel approach for reliable detection of cathepsin S activities in mouse antigen presenting cells.
Atherosclerosis
Adenosine-to-inosine RNA editing controls cathepsin S expression in atherosclerosis by enabling HuR-mediated post-transcriptional regulation.
Atherosclerosis
Association of Circulating Cathepsin S and Cardiovascular Disease Among Patients With Type 2 Diabetes: A Cross-Sectional Community-Based Study.
Atherosclerosis
Binding of chondroitin 4-sulfate to cathepsin s regulates its enzymatic activity.
Atherosclerosis
Cathepsin S Activity Controls Injury-Related Vascular Repair in Mice via the TLR2-Mediated p38MAPK and PI3K-Akt/p-HDAC6 Signaling Pathway.
Atherosclerosis
Cathepsin S contributes to macrophage migration via degradation of elastic fibre integrity to facilitate vein graft neointimal hyperplasia.
Atherosclerosis
Cathepsin S generates soluble CX3CL1 (fractalkine) in vascular smooth muscle cells.
Atherosclerosis
Cathepsin S inhibitors as novel immunomodulators.
Atherosclerosis
Cathepsin S regulates renal fibrosis in mouse models of mild and severe hydronephrosis.
Atherosclerosis
Cathepsin S, a novel biomarker of adiposity: relevance to atherogenesis.
Atherosclerosis
Clinical application of simultaneous detection of cystatin C, cathepsin S, and IL-1 in classification of coronary artery disease.
Atherosclerosis
Correlation between serum cathepsin S and insulin resistance in type 2 diabetes.
Atherosclerosis
Correlation of cathepsin S with coronary stenosis degree, carotid thickness, blood pressure, glucose and lipid metabolism and vascular endothelial function in atherosclerosis.
Atherosclerosis
CTSS promoter -25G/A: not a risk factor for CHD in Chinese.
Atherosclerosis
Cystathionine ? Lyase Sulfhydrates the RNA Binding Protein HuR to Preserve Endothelial Cell Function and Delay Atherogenesis.
Atherosclerosis
Cysteine protease cathepsin S as a key step in antigen presentation.
Atherosclerosis
Deficiency of cathepsin S reduces atherosclerosis in LDL receptor-deficient mice.
Atherosclerosis
Determination of cathepsin S abundance and activity in human plasma and implications for clinical investigation.
Atherosclerosis
Discovery of novel cathepsin S inhibitors by pharmacophore-based virtual high-throughput screening.
Atherosclerosis
Elevated circulating cathepsin S levels are associated with metabolic syndrome in overweight and obese individuals.
Atherosclerosis
IFN regulatory factor-1 regulates IFN-gamma-dependent cathepsin S expression.
Atherosclerosis
Improvement of cathepsin S detection using a designed FRET peptide based on putative natural substrates.
Atherosclerosis
Increased serum cathepsin S in patients with atherosclerosis and diabetes.
Atherosclerosis
Leukocyte cathepsin S is a potent regulator of both cell and matrix turnover in advanced atherosclerosis.
Atherosclerosis
Long-term endurance training increases serum cathepsin S and decreases IL-6 and hsCRP levels.
Atherosclerosis
Lysosomal cysteine proteases in atherosclerosis.
Atherosclerosis
Multiple Statistical Methods for Assessing Differential Gene Expression in Microarray Data of Diabetic Model Rats to Predict the Molecular Mechanism of Atorvastatin on Anti-Atherogenesis.
Atherosclerosis
Overexpression of cathepsin s induces chronic atopic dermatitis in mice.
Atherosclerosis
Pharmacological Inhibition of Cathepsin S Decreases Atherosclerotic Lesions in Apoe-/- Mice.
Atherosclerosis
Plasma Cathepsin S is Associated with High-density Lipoprotein Cholesterol and Bilirubin in Patients with Abdominal Aortic Aneurysms.
Atherosclerosis
Relationship between plasma cathepsin S and cystatin C levels and coronary plaque morphology of mild to moderate lesions: an in vivo study using intravascular ultrasound.
Atherosclerosis
REPLY: Treatment with oxLDL antibody reduces cathepsin S expression in atherosclerosis via down-regulating ADAR1-mediated RNA editing.
Atherosclerosis
Selective Cathepsin S Inhibition Attenuates Atherosclerosis in Apolipoprotein E-Deficient Mice with Chronic Renal Disease.
Atherosclerosis
Serum cathepsin S is associated with serum C-reactive protein and interleukin-6 independently of obesity in elderly men.
Atherosclerosis
Toll-like receptor 7 deficiency protects apolipoprotein E-deficient mice from diet-induced atherosclerosis.
Atherosclerosis
Transfer of exosomal microRNA-203-3p from dendritic cells to bone marrow-derived macrophages reduces development of atherosclerosis by downregulating Ctss in mice.
Atherosclerosis
Treatment with a human recombinant monoclonal IgG antibody against oxidized LDL in atherosclerosis-prone pigs reduces cathepsin S in coronary lesions.
Atherosclerosis
Treatment with oxLDL antibody reduces cathepsin S expression in atherosclerosis via down-regulating ADAR1-mediated RNA editing.
Atherosclerosis
Weight loss reduces adipose tissue cathepsin S and its circulating levels in morbidly obese women.
Atherosclerosis
[Impact of olmesartan medoxomil on atherosclerosis lesions in apolipoprotein E knockout mice].
Autoimmune Diseases
A novel approach for reliable detection of cathepsin S activities in mouse antigen presenting cells.
Autoimmune Diseases
An orally active reversible inhibitor of cathepsin S inhibits human trans vivo delayed-type hypersensitivity.
Autoimmune Diseases
Aod1 controlling day 3 thymectomy-induced autoimmune ovarian dysgenesis in mice encompasses two linked quantitative trait loci with opposing allelic effects on disease susceptibility.
Autoimmune Diseases
Binding of chondroitin 4-sulfate to cathepsin s regulates its enzymatic activity.
Autoimmune Diseases
Cathepsin S inhibitor prevents autoantigen presentation and autoimmunity.
Autoimmune Diseases
Cathepsin S inhibitors: WO2010070615.
Autoimmune Diseases
Cloning, expression analysis and enzymatic characterization of cathepsin S from olive flounder (Paralichthys olivaceus).
Autoimmune Diseases
Cysteine protease cathepsin S as a key step in antigen presentation.
Autoimmune Diseases
Inhibition of Cathepsin S Reduces Allogeneic T Cell Priming but Not Graft-versus-Host Disease Against Minor Histocompatibility Antigens.
Autoimmune Diseases
Substrate activity screening: a fragment-based method for the rapid identification of nonpeptidic protease inhibitors.
Autoimmune Diseases
Synthesis of proline analogues as potent and selective cathepsin S inhibitors.
Autoimmune Diseases
Therapeutic dosing of an orally active, selective cathepsin S inhibitor suppresses disease in models of autoimmunity.
Autoimmune Diseases
[Virtual screening study of cathepsin S natural inhibitor].
Bacterial Infections
Cathepsin S of Sciaenops ocellatus: Identification, transcriptional expression and enzymatic activity.
Bacterial Infections
Expression profile analysis of two cathepsin S in channel catfish (Ictalurus punctatus) mucosal tissues following bacterial challenge.
Brain Injuries, Traumatic
Inhibition of cathepsin S produces neuroprotective effects after traumatic brain injury in mice.
Brain Neoplasms
Detection of cathepsin S cysteine protease in human brain tumour microdialysates in vivo.
Breast Neoplasms
A Novel Role for Cathepsin S as a Potential Biomarker in Triple Negative Breast Cancer.
Breast Neoplasms
Analysis of tumour- and stroma-supplied proteolytic networks reveals a brain-metastasis-promoting role for cathepsin S.
Breast Neoplasms
Differential cathepsin responses to inhibitor-induced feedback: E-64 and cystatin C elevate active cathepsin S and suppress active cathepsin L in breast cancer cells.
Breast Neoplasms
Discovery of novel cathepsin inhibitors with potent anti-metastatic effects in breast cancer cells.
Breast Neoplasms
Is There Any Role for Serum Cathepsin S and CRP Levels on Prognostic Information in Breast Cancer? The Swedish Mammography Cohort.
Breast Neoplasms
Long-term endurance training increases serum cathepsin S levels in healthy female subjects.
Breast Neoplasms
Recent advances in the field of anti-cancer immunotherapy.
Breast Neoplasms
Up-regulation of cathepsin S expression by HSP90 and 5-HT7 receptor-dependent serotonin signaling correlates with triple negativity of human breast cancer.
Carcinogenesis
Cathepsin S Controls Angiogenesis and Tumor Growth via Matrix-derived Angiogenic Factors.
Carcinogenesis
Cathepsin S is aberrantly overexpressed in human hepatocellular carcinoma.
Carcinogenesis
Inhibition of Cathepsin S by Fsn0503 enhances the efficacy of chemotherapy in colorectal carcinomas.
Carcinogenesis
Inhibition of cathepsin S induces autophagy and apoptosis in human glioblastoma cell lines through ROS-mediated PI3K/AKT/mTOR/p70S6K and JNK signaling pathways.
Carcinoma, Hepatocellular
Cathepsin S is aberrantly overexpressed in human hepatocellular carcinoma.
Carcinoma, Hepatocellular
Cathepsin S silencing induces apoptosis of human hepatocellular carcinoma cells.
Carcinoma, Hepatocellular
Melittin suppresses cathepsin S-induced invasion and angiogenesis via blocking of the VEGF-A/VEGFR-2/MEK1/ERK1/2 pathway in human hepatocellular carcinoma.
Carcinoma, Hepatocellular
Silencing cathepsin S gene expression inhibits growth, invasion and angiogenesis of human hepatocellular carcinoma in vitro.
Carcinoma, Hepatocellular
[Effects of up-regulation of cathepsin S by HBx gene on HepG2 cell].
Carcinoma, Non-Small-Cell Lung
Nidogen-1 Degraded by Cathepsin S can be Quantified in Serum and is Associated with Non-Small Cell Lung Cancer.
Cardiomegaly
Simvastatin inhibited cardiac hypertrophy and fibrosis in apolipoprotein E-deficient mice fed a "Western-style diet" by increasing PPAR ? and ? expression and reducing TC, MMP-9, and Cat S levels.
Cardiovascular Diseases
Acute phase serum cathepsin S level and cathepsin S/cystatin C ratio are the associated factors with cerebral infarction and their diagnostic value for cerebral infarction.
Cardiovascular Diseases
Association between serum cathepsin S and mortality in older adults.
Cardiovascular Diseases
Association of Circulating Cathepsin S and Cardiovascular Disease Among Patients With Type 2 Diabetes: A Cross-Sectional Community-Based Study.
Cardiovascular Diseases
Cathepsin S genotypes are associated with Apo-A1 and HDL-cholesterol in lean and obese French populations.
Cardiovascular Diseases
Cathepsin S: therapeutic, diagnostic, and prognostic potential.
Cardiovascular Diseases
Exploring fragment-based target-specific ranking protocol with machine learning on cathepsin S.
Cardiovascular Diseases
Point-of-care testing in primary care: A systematic review on implementation aspects addressed in test evaluations.
Cardiovascular Diseases
Serum cathepsin S and cystatin C: relationship to subclinical carotid atherosclerosis in rheumatoid arthritis.
Cardiovascular Diseases
Serum cathepsin S is associated with serum C-reactive protein and interleukin-6 independently of obesity in elderly men.
Cardiovascular Diseases
The genetic polymorphisms of cathepsin S were associated with metabolic disorders in a Chinese Han population.
Carotid Artery Diseases
Adenosine-to-inosine RNA editing controls cathepsin S expression in atherosclerosis by enabling HuR-mediated post-transcriptional regulation.
Carotid Artery Diseases
Serum cathepsin S and cystatin C: relationship to subclinical carotid atherosclerosis in rheumatoid arthritis.
cathepsin s deficiency
Arterial and aortic valve calcification abolished by elastolytic cathepsin S deficiency in chronic renal disease.
cathepsin s deficiency
Cathepsin S controls adipocytic and osteoblastic differentiation, bone turnover, and bone microarchitecture.
cathepsin s deficiency
Cathepsin S Controls Angiogenesis and Tumor Growth via Matrix-derived Angiogenic Factors.
cathepsin s deficiency
Cathepsin S deficiency confers protection from neonatal hyperoxia-induced lung injury.
cathepsin s deficiency
Cathepsin S Deficiency Mitigated Chronic Stress-Related Neointimal Hyperplasia in Mice.
cathepsin s deficiency
Cathepsin S deficiency results in abnormal accumulation of autophagosomes in macrophages and enhances Ang II-induced cardiac inflammation.
cathepsin s deficiency
Deficiency of cathepsin S attenuates angiotensin II-induced abdominal aortic aneurysm formation in apolipoprotein E-deficient mice.
cathepsin s deficiency
Effective suppression of donor specific antibody production by Cathepsin S inhibitors in a mouse transplantation model.
Cerebral Infarction
Acute phase serum cathepsin S level and cathepsin S/cystatin C ratio are the associated factors with cerebral infarction and their diagnostic value for cerebral infarction.
Cerebral Infarction
Association between CTSS gene polymorphism and the risk of acute atherosclerotic cerebral infarction in Chinese population: a case-control study.
Cholestasis
[The effect of Cathepsin S in primary biliary cholangitis].
Coinfection
Repurposing Saquinavir for Host-Directed Therapy to Control Mycobacterium Tuberculosis Infection.
Colitis
Cathepsin S is Activated During Colitis and Causes Visceral Hyperalgesia by a PAR2-dependent Mechanism in Mice.
Colitis
Demonstration of elevated levels of active cathepsin S in dextran sulfate sodium colitis using a new activatable probe.
Colitis
Protease-activated receptor-2 in endosomes signals persistent pain of irritable bowel syndrome.
Colorectal Neoplasms
Antibody targeting of Cathepsin S induces antibody-dependent cellular cytotoxicity.
Colorectal Neoplasms
Antibody-mediated inhibition of cathepsin S blocks colorectal tumor invasion and angiogenesis.
Colorectal Neoplasms
Cathepsin S from both tumor and tumor-associated cells promote cancer growth and neovascularization.
Colorectal Neoplasms
Evaluating the diagnostic and prognostic value of circulating cathepsin S in gastric cancer.
Colorectal Neoplasms
Inhibition of Cathepsin S by Fsn0503 enhances the efficacy of chemotherapy in colorectal carcinomas.
Colorectal Neoplasms
The role of Cathepsin S as a marker of prognosis and predictor of chemotherapy benefit in adjuvant CRC: a pilot study.
Colorectal Neoplasms
[Effect of jianpi-jiedu formula on tumor angiogenesis-relevant genes expression in colorectal cancer].
Communicable Diseases
Application of nanodiagnostics in point-of-care tests for infectious diseases.
Connective Tissue Diseases
Connective tissue diseases. Inhibiting cathepsin S to treat SLE and lupus nephritis.
Coronary Artery Disease
Adenosine-to-inosine RNA editing controls cathepsin S expression in atherosclerosis by enabling HuR-mediated post-transcriptional regulation.
Coronary Artery Disease
Clinical application of simultaneous detection of cystatin C, cathepsin S, and IL-1 in classification of coronary artery disease.
Coronary Artery Disease
Correlation of cathepsin S with coronary stenosis degree, carotid thickness, blood pressure, glucose and lipid metabolism and vascular endothelial function in atherosclerosis.
Coronary Artery Disease
Cysteine Protease Cathepsins in Atherosclerotic Cardiovascular Diseases.
Coronary Artery Disease
Increased plasma levels of CATS mRNA but not CATB mRNA in patients with coronary atherosclerosis.
Coronary Artery Disease
Optimisation of methods for quantifying plasma mRNA levels from genes responsible for coronary artery plaque development and destabilization.
Coronary Disease
Cathepsin B and S as markers for cardiovascular risk and all-cause mortality in patients with stable coronary heart disease during 10 years: a CLARICOR trial sub-study.
Coronary Disease
Correlation between serum cathepsin S and insulin resistance in type 2 diabetes.
Coronary Stenosis
Correlation of cathepsin S with coronary stenosis degree, carotid thickness, blood pressure, glucose and lipid metabolism and vascular endothelial function in atherosclerosis.
Cough
Introducing new point-of-care tests for common infections in publicly funded clinics in South Africa: a qualitative study with primary care clinicians.
COVID-19
COVID-19 Point-of-Care Diagnostics That Satisfy Global Target Product Profiles.
COVID-19
Performance of two rapid point of care SARS-COV-2 antibody assays against laboratory-based automated chemiluminescent immunoassays for SARS-COV-2 IG-G, IG-M and total antibodies.
COVID-19
Rapid community point-of-care testing for COVID-19 (RAPTOR-C19): protocol for a platform diagnostic study.
COVID-19
Rapid lateral flow tests for the detection of SARS-CoV-2 neutralizing antibodies.
COVID-19
The diagnostic accuracy of isothermal nucleic acid point-of-care tests for human coronaviruses: A systematic review and meta-analysis.
Cystic Fibrosis
A new player in the game: epithelial cathepsin S in early cystic fibrosis lung disease.
Cystic Fibrosis
Cathepsin S: therapeutic, diagnostic, and prognostic potential.
Cystic Fibrosis
miR-31 dysregulation in cystic fibrosis airways contributes to increased pulmonary cathepsin S production.
Cystic Fibrosis
Molecular modeling assisted identification and biological evaluation of potent cathepsin S inhibitors.
Cystic Fibrosis
Targeting of Cathepsin S Reduces Cystic Fibrosis-like Lung Disease.
Cystic Fibrosis
Therapeutic Inhibition of Cathepsin S Reduces Inflammation and Mucus Plugging in Adult ?ENaC-Tg Mice.
Dacryocystitis
Phenylephrine increases tear cathepsin S secretion in healthy murine lacrimal gland acinar cells through an alternative secretory pathway.
Dengue
Controlled peptide solvation in portion-mixing libraries of FRET peptides: improved specificity determination for Dengue 2 virus NS2B-NS3 protease and human cathepsin S.
Dermatitis
Cathepsin S, a new pruritus biomarker in clinical dandruff/seborrhoeic dermatitis evaluation.
Dermatitis, Atopic
Overexpression of cathepsin s induces chronic atopic dermatitis in mice.
Dermatitis, Atopic
Overexpression of Cathepsin S Induces Chronic Atopic Dermatitis in Mice.
Diabetes Complications
Cathepsin S Cleavage of Protease-Activated Receptor-2 on Endothelial Cells Promotes Microvascular Diabetes Complications.
Diabetes Mellitus
Long-term endurance training increases serum cathepsin S and decreases IL-6 and hsCRP levels.
Diabetes Mellitus, Type 2
Association of Circulating Cathepsin S and Cardiovascular Disease Among Patients With Type 2 Diabetes: A Cross-Sectional Community-Based Study.
Diabetes Mellitus, Type 2
Circulating cathepsin S improves glycaemic control in mice.
Diabetes Mellitus, Type 2
Correlation between serum cathepsin S and insulin resistance in type 2 diabetes.
Diabetes Mellitus, Type 2
Determination of cathepsin S abundance and activity in human plasma and implications for clinical investigation.
Diabetes Mellitus, Type 2
Usefulness of Cathepsin S to Predict Risk for Obstructive Sleep Apnea among Patients with Type 2 Diabetes.
Diabetic Nephropathies
Cathepsin S Cleavage of Protease-Activated Receptor-2 on Endothelial Cells Promotes Microvascular Diabetes Complications.
Diabetic Retinopathy
Cathepsin S Cleavage of Protease-Activated Receptor-2 on Endothelial Cells Promotes Microvascular Diabetes Complications.
Diphtheria
Common Reference-Based Tandem Mass Tag Multiplexing for the Relative Quantification of Peptides: Design and Application to Degradome Analysis of Diphtheria Toxoid.
Down Syndrome
The lysosomal cysteine protease, cathepsin S, is increased in Alzheimer's disease and Down syndrome brain. An immunocytochemical study.
Dry Eye Syndromes
Phenylephrine increases tear cathepsin S secretion in healthy murine lacrimal gland acinar cells through an alternative secretory pathway.
Dyslipidemias
Cholesterol Point-of-Care Testing for Community Pharmacies: A Review of the Current Literature.
Esophageal Neoplasms
Evaluating the diagnostic and prognostic value of circulating cathepsin S in gastric cancer.
Fatty Liver
Serum lipocalin-2, cathepsin S and chemerin levels and nonalcoholic fatty liver disease.
Fibromyalgia
High levels of cathepsin S and cystatin C in patients with fibromyalgia syndrome.
Gastrointestinal Neoplasms
Cathepsin S as a target in gastric cancer.
Gaucher Disease
Aberrant progranulin, YKL-40, cathepsin D and cathepsin S in Gaucher disease.
Glioblastoma
Cathepsin S expression: An independent prognostic factor in glioblastoma tumours--A pilot study.
Glioblastoma
Inhibition of cathepsin S induces autophagy and apoptosis in human glioblastoma cell lines through ROS-mediated PI3K/AKT/mTOR/p70S6K and JNK signaling pathways.
Glioblastoma
Inhibition of Cathepsin S Induces Mitochondrial Apoptosis in Glioblastoma Cell Lines Through Mitochondrial Stress and Autophagosome Accumulation.
Glioblastoma
Inhibition of Cathepsin S Restores TGF-?-induced Epithelial-to-mesenchymal Transition and Tight Junction Turnover in Glioblastoma Cells.
Glioblastoma
[Cathepsin S (CTSS) is highly expressed in temozolomide-resistant glioblastoma T98G cells and associated with poor prognosis].
Glomerulonephritis
Cathepsin S inhibition combines control of systemic and peripheral pathomechanisms of autoimmune tissue injury.
Glomerulonephritis, IGA
The Clinical Significance and Potential Role of Cathepsin S in IgA Nephropathy.
Graft vs Host Disease
Inhibition of Cathepsin S Reduces Allogeneic T Cell Priming but Not Graft-versus-Host Disease Against Minor Histocompatibility Antigens.
Graves Disease
Cathepsin S is not crucial to TSHR processing and presentation in a murine model of Graves' disease.
Heart Diseases
Correlation of cathepsin S with coronary stenosis degree, carotid thickness, blood pressure, glucose and lipid metabolism and vascular endothelial function in atherosclerosis.
Heart Failure
Soluble Glycoprotein 130 and Heat Shock Protein 27 as Novel Candidate Biomarkers of Chronic Heart Failure with Preserved Ejection Fraction.
Heart Failure
[Association between lososomal cysteine protease cathepsin's activation and left ventricular function and remodeling in hypertensive heart failure rats]
Heart Valve Diseases
Long-term endurance training increases serum cathepsin S and decreases IL-6 and hsCRP levels.
Hepatitis
Point-of-care testing and the control of infectious diseases.
Hepatitis B
Cathepsin S is aberrantly overexpressed in human hepatocellular carcinoma.
Hepatitis B
Performance of point of care assays for hepatitis B and C viruses in chronic kidney disease patients.
Hepatitis B
[Effects of up-regulation of cathepsin S by HBx gene on HepG2 cell].
Hepatitis C
Hepatitis C virus-mediated inhibition of cathepsin s increases invariant-chain expression on hepatocyte surface.
Hepatitis C
Performance of point of care assays for hepatitis B and C viruses in chronic kidney disease patients.
HIV Infections
Challenges of HIV diagnosis and management in the context of pre-exposure prophylaxis (PrEP), post-exposure prophylaxis (PEP), test and start and acute HIV infection: a scoping review.
Hydronephrosis
Cathepsin S regulates renal fibrosis in mouse models of mild and severe hydronephrosis.
Hyperalgesia
Cathepsin S causes inflammatory pain via biased agonism of PAR2 and TRPV4.
Hyperalgesia
Cathepsin S in the spinal microglia contributes to remifentanil-induced hyperalgesia in rats.
Hyperalgesia
Cathepsin S is Activated During Colitis and Causes Visceral Hyperalgesia by a PAR2-dependent Mechanism in Mice.
Hyperalgesia
Peripheral role of cathepsin S in Th1 cell-dependent transition of nerve injury-induced acute pain to a chronic pain state.
Hyperalgesia
Protease-activated receptor-2 in endosomes signals persistent pain of irritable bowel syndrome.
Hyperalgesia
Role of the cysteine protease cathepsin S in neuropathic hyperalgesia.
Hyperalgesia
Selective Cathepsin S Inhibition with MIV-247 Attenuates Mechanical Allodynia and Enhances the Antiallodynic Effects of Gabapentin and Pregabalin in a Mouse Model of Neuropathic Pain.
Hyperalgesia
Selective inhibition of peripheral cathepsin S reverses tactile allodynia following peripheral nerve injury in mouse.
Hypercholesterolemia
The genetic polymorphisms of cathepsin S were associated with metabolic disorders in a Chinese Han population.
Hypergammaglobulinemia
Cathepsin S inhibition combines control of systemic and peripheral pathomechanisms of autoimmune tissue injury.
Hyperglycemia
Impact of an inpatient multidisciplinary glucose control management program.
Hypersensitivity
An orally active reversible inhibitor of cathepsin S inhibits human trans vivo delayed-type hypersensitivity.
Hypersensitivity
Changes in vascular permeability in the spinal cord contribute to chemotherapy-induced neuropathic pain.
Hypertension
Cathepsin S promotes the development of pulmonary arterial hypertension.
Hypertension
Serum cathepsin S is associated with serum C-reactive protein and interleukin-6 independently of obesity in elderly men.
Hypertension
[Association between lososomal cysteine protease cathepsin's activation and left ventricular function and remodeling in hypertensive heart failure rats]
Hypertension, Pulmonary
Cathepsin S promotes the development of pulmonary arterial hypertension.
Infections
"It's not a time spent issue, it's a 'what have you spent your time doing?' issue
" A qualitative study of UK patient opinions and expectations for implementation of Point of Care Tests for sexually transmitted infections and antimicrobial resistance.
Infections
A novel electronic algorithm using host biomarker point-of-care tests for the management of febrile illnesses in Tanzanian children (e-POCT): A randomized, controlled non-inferiority trial.
Infections
An ideal test? A multi-country qualitative study of clinicians' and patients' views of point of care tests for lower respiratory tract infection in primary care.
Infections
Cathepsin L maturation and activity is impaired in macrophages harboring M. avium and M. tuberculosis.
Infections
Cathepsin S supports acid-independent infection by some reoviruses.
Infections
COVID-19 Point-of-Care Diagnostics That Satisfy Global Target Product Profiles.
Infections
COVID-19 point-of-care testing in care homes: what are the lessons for policy and practice?
Infections
Expression profile analysis of two cathepsin S in channel catfish (Ictalurus punctatus) mucosal tissues following bacterial challenge.
Infections
Genome-wide identification, expression signature and immune functional analysis of two cathepsin S (CTSS) genes in turbot (Scophthalmus maximus L.).
Infections
In-vitro diagnostic point-of-care tests in paediatric ambulatory care: A systematic review and meta-analysis.
Infections
Introducing new point-of-care tests for common infections in publicly funded clinics in South Africa: a qualitative study with primary care clinicians.
Infections
Molecular cloning, sequencing and characterization of channel catfish (Ictalurus punctatus, Rafinesque 1818) cathepsin S gene.
Infections
Mycobacterium bovis bacillus Calmette-Guérin secreting active cathepsin S stimulates expression of mature MHC class II molecules and antigen presentation in human macrophages.
Infections
Mycobacterium bovis BCG attenuates surface expression of mature class II molecules through IL-10-dependent inhibition of cathepsin S.
Infections
Performance of point-of-care tests for the detection of chlamydia trachomatis infections: A systematic review and meta-analysis.
Infections
Point of care tests for invasive fungal infections: a blueprint for increasing availability in Africa.
Infections
Point-of-care diagnostics: needs of African health care workers and their role combating global antimicrobial resistance.
Infections
Point-of-care testing for HCV infection: recent advances and implications for alternative screening.
Infections
Rapid community point-of-care testing for COVID-19 (RAPTOR-C19): protocol for a platform diagnostic study.
Infections
Role of Cathepsin S in Periodontal Inflammation and Infection.
Infections
Simultaneous Quantitative Detection of Helicobacter Pylori Based on a Rapid and Sensitive Testing Platform using Quantum Dots-Labeled Immunochromatiographic Test Strips.
Influenza, Human
Do point-of-care tests (POCTs) offer a new paradigm for the management of patients with influenza?
Influenza, Human
Emerging point of care tests for influenza: innovation or status quo.
Influenza, Human
Important role of cathepsin S in generating peptides for TAP-independent MHC class I crosspresentation in vivo.
Influenza, Human
Integrating molecular point-of-care testing for influenza into primary care: a mixed-methods feasibility study.
Influenza, Human
Point of care testing: diagnosis outside the virology laboratory.
Influenza, Human
The clinical utility of point-of-care tests for influenza in ambulatory care: A systematic review and meta-analysis.
Insulin Resistance
Correlation between serum cathepsin S and insulin resistance in type 2 diabetes.
Insulin Resistance
Elevated circulating cathepsin S levels are associated with metabolic syndrome in overweight and obese individuals.
Insulin Resistance
Influence of a prudent diet on circulating cathepsin S in humans.
Insulin Resistance
Long-term endurance training increases serum cathepsin S and decreases IL-6 and hsCRP levels.
Insulin Resistance
Serum Cathepsin S Is Associated With Decreased Insulin Sensitivity and the Development of Diabetes Type 2 in a Community-Based Cohort of Elderly Men.
Insulin Resistance
Serum lipocalin-2, cathepsin S and chemerin levels and nonalcoholic fatty liver disease.
Insulin Resistance
Vitamin D deficiency in childhood obesity is associated with high levels of circulating inflammatory mediators, and low insulin sensitivity.
Joint Diseases
The proinflammatory cytokines interleukin-1? and tumor necrosis factor ? promote the expression and secretion of proteolytically active cathepsin S from human chondrocytes.
Kidney Neoplasms
Inhibition of Cathepsin S Induces Mitochondrial ROS That Sensitizes TRAIL-Mediated Apoptosis Through p53-Mediated Downregulation of Bcl-2 and c-FLIP.
Liver Diseases
Plasma signature of neurological disease in the monogenetic disorder niemann-pick type C.
Liver Diseases
Point-of-Care Testing in Liver Disease and Liver Surgery.
Liver Diseases
Serum lipocalin-2, cathepsin S and chemerin levels and nonalcoholic fatty liver disease.
Liver Neoplasms
Evaluating the diagnostic and prognostic value of circulating cathepsin S in gastric cancer.
Lung Diseases
A new player in the game: epithelial cathepsin S in early cystic fibrosis lung disease.
Lung Diseases
Cathepsin S: investigating an old player in lung disease pathogenesis, comorbidities, and potential therapeutics.
Lung Diseases
Targeting of Cathepsin S Reduces Cystic Fibrosis-like Lung Disease.
Lung Diseases
Therapeutic Inhibition of Cathepsin S Reduces Inflammation and Mucus Plugging in Adult ?ENaC-Tg Mice.
Lung Diseases, Interstitial
Cathepsin S, a new serum biomarker of sarcoidosis discovered by transcriptome analysis of alveolar macrophages.
Lung Diseases, Interstitial
Decreased serum cathepsin S levels in patients with systemic sclerosis-associated interstitial lung disease.
Lung Injury
Cathepsin S deficiency confers protection from neonatal hyperoxia-induced lung injury.
Lung Neoplasms
Cathepsin S in tumours, regional lymph nodes and sera of patients with lung cancer: relation to prognosis.
Lung Neoplasms
Evaluating the diagnostic and prognostic value of circulating cathepsin S in gastric cancer.
Lung Neoplasms
Nidogen-1 Degraded by Cathepsin S can be Quantified in Serum and is Associated with Non-Small Cell Lung Cancer.
Lung Neoplasms
The effect of catalase on migration and invasion of lung cancer cells by regulating the activities of cathepsin S, L, and K.
Lupus Erythematosus, Systemic
Cathepsin S inhibition suppresses systemic lupus erythematosus and lupus nephritis because cathepsin S is essential for MHC class II-mediated CD4 T cell and B cell priming.
Lupus Erythematosus, Systemic
Global Proteomics Deciphered Novel-Function of Osthole Against Pulmonary Arterial Hypertension.
Lupus Nephritis
Cathepsin S inhibition combines control of systemic and peripheral pathomechanisms of autoimmune tissue injury.
Lupus Nephritis
Cathepsin S inhibition suppresses systemic lupus erythematosus and lupus nephritis because cathepsin S is essential for MHC class II-mediated CD4 T cell and B cell priming.
Lupus Nephritis
Connective tissue diseases. Inhibiting cathepsin S to treat SLE and lupus nephritis.
Lymphoma, B-Cell
Aptamer based proteomic pilot study reveals a urine signature indicative of pediatric urinary tract infections.
Lymphoma, B-Cell
Novel urine biomarkers to distinguish UTI from culture-negative pyuria.
Lymphoma, Follicular
Cathepsin S Alterations Induce a Tumor-Promoting Immune Microenvironment in Follicular Lymphoma.
Lymphoma, Follicular
Cathepsin S Regulates Antigen Processing and T Cell Activity in Non-Hodgkin Lymphoma.
Lymphoma, Non-Hodgkin
Cathepsin S Protease Mediates T-Cell Response in Non-Hodgkin Lymphoma.
Lymphoma, Non-Hodgkin
Cathepsin S Regulates Antigen Processing and T Cell Activity in Non-Hodgkin Lymphoma.
Malaria
In-vitro diagnostic point-of-care tests in paediatric ambulatory care: A systematic review and meta-analysis.
Malaria
Integrated point-of-care testing (POCT) for HIV, syphilis, malaria and anaemia at antenatal facilities in western Kenya: a qualitative study exploring end-users' perspectives of appropriateness, acceptability and feasibility.
Malaria
Point-of-care tests for syphilis and yaws in a low-income setting - A qualitative study of healthcare worker and patient experiences.
Measles
Investigation of a measles outbreak in Zimbabwe, 2010: potential of a point of care test to replace laboratory confirmation of suspected cases.
Melanoma
Cathepsin S and its inhibitor cystatin C: imbalance in uveal melanoma.
Metabolic Syndrome
Elevated circulating cathepsin S levels are associated with metabolic syndrome in overweight and obese individuals.
Metabolic Syndrome
Proportional correlates of adipolin and cathepsin S in metabolic syndrome patients with and without prediabetes.
Metabolic Syndrome
The genetic polymorphisms of cathepsin S were associated with metabolic disorders in a Chinese Han population.
Mouth Neoplasms
Inhibition of cathepsin S confers sensitivity to methyl protodioscin in oral cancer cells via activation of p38 MAPK/JNK signaling pathways.
Mouth Neoplasms
Sulforaphane suppresses oral cancer cell migration by regulating cathepsin S expression.
Multiple Sclerosis
A novel approach for reliable detection of cathepsin S activities in mouse antigen presenting cells.
Multiple Sclerosis
Advances in cathepsin S inhibitor design.
Multiple Sclerosis
An orally active reversible inhibitor of cathepsin S inhibits human trans vivo delayed-type hypersensitivity.
Multiple Sclerosis
Cathepsins and their endogenous inhibitors Cystatins: Expression and Modulation in Multiple Sclerosis.
Multiple Sclerosis
Overcoming hERG issues for brain-penetrating cathepsin S inhibitors: 2-cyanopyrimidines. Part 2.
Muscular Dystrophies
Cathepsin S contributes to the pathogenesis of muscular dystrophy in mice.
Myasthenia Gravis
Cathepsin S is required for murine autoimmune myasthenia gravis pathogenesis.
Myasthenia Gravis, Autoimmune, Experimental
Cathepsin S is not crucial to TSHR processing and presentation in a murine model of Graves' disease.
Myocardial Infarction
Cathepsin S degrades arresten and canstatin in infarcted area after myocardial infarction in rats.
Myocardial Infarction
Increased plasma cathepsin S and trombospondin-1 in patients with acute ST segment elevation myocardial infarction.
Myocardial Infarction
Increased serum cathepsin S in patients with atherosclerosis and diabetes.
Myositis
Antigen processing and presentation in human muscle: cathepsin S is critical for MHC class II expression and upregulated in inflammatory myopathies.
Nasopharyngeal Neoplasms
Evaluating the diagnostic and prognostic value of circulating cathepsin S in gastric cancer.
Neoplasm Metastasis
Analysis of tumour- and stroma-supplied proteolytic networks reveals a brain-metastasis-promoting role for cathepsin S.
Neoplasm Metastasis
Cathepsin S as a target in gastric cancer.
Neoplasm Metastasis
Cathepsin S is aberrantly overexpressed in human hepatocellular carcinoma.
Neoplasm Metastasis
Design and synthesis of alpha-ketoamides as cathepsin S inhibitors with potential applications against tumor invasion and angiogenesis.
Neoplasm Metastasis
Discovery of novel cathepsin inhibitors with potent anti-metastatic effects in breast cancer cells.
Neoplasm Metastasis
Down-regulation of cathepsin S and matrix metalloproteinase-9 via Src, a non-receptor tyrosine kinase, suppresses triple-negative breast cancer growth and metastasis.
Neoplasm Metastasis
Evaluating the diagnostic and prognostic value of circulating cathepsin S in gastric cancer.
Neoplasm Metastasis
Hispolon suppresses metastasis via autophagic degradation of cathepsin S in cervical cancer cells.
Neoplasm Metastasis
Increased levels of macrophage-secreted cathepsin S during prostate cancer progression in TRAMP mice and patients.
Neoplasm Metastasis
Leading the invasion: The role of Cathepsin S in the tumour microenvironment.
Neoplasm Metastasis
Lysosomal cysteine protease cathepsin S is involved in cancer cell motility by regulating store-operated Ca2+ entry.
Neoplasm Metastasis
Regulating BRCA1 protein stability by cathepsin S-mediated ubiquitin degradation.
Neoplasm Metastasis
Silencing cathepsin S gene expression inhibits growth, invasion and angiogenesis of human hepatocellular carcinoma in vitro.
Neoplasm Metastasis
Targeting cathepsin S induces tumor cell autophagy via the EGFR-ERK signaling pathway.
Neoplasms
A bioavailable cathepsin S nitrile inhibitor abrogates tumor development.
Neoplasms
A Chitosan-PLGA based catechin hydrate nanoparticles used in targeting of lungs and cancer treatment.
Neoplasms
A novel approach for reliable detection of cathepsin S activities in mouse antigen presenting cells.
Neoplasms
A Novel Role for Cathepsin S as a Potential Biomarker in Triple Negative Breast Cancer.
Neoplasms
Analysis of tumour- and stroma-supplied proteolytic networks reveals a brain-metastasis-promoting role for cathepsin S.
Neoplasms
Antibody targeting of Cathepsin S induces antibody-dependent cellular cytotoxicity.
Neoplasms
Antibody targeting of cathepsin S inhibits angiogenesis and synergistically enhances anti-VEGF.
Neoplasms
Antibody-mediated inhibition of cathepsin S blocks colorectal tumor invasion and angiogenesis.
Neoplasms
Association between serum cathepsin S and mortality in older adults.
Neoplasms
Autophagy-Regulated ROS from Xanthine Oxidase Acts as an Early Effector for Triggering Late Mitochondria-Dependent Apoptosis in Cathepsin S-Targeted Tumor Cells.
Neoplasms
Binding of chondroitin 4-sulfate to cathepsin s regulates its enzymatic activity.
Neoplasms
Cathepsin S and its inhibitor cystatin C: imbalance in uveal melanoma.
Neoplasms
Cathepsin S as a target in gastric cancer.
Neoplasms
Cathepsin S attenuates endosomal EGFR signalling: A mechanical rationale for the combination of cathepsin S and EGFR tyrosine kinase inhibitors.
Neoplasms
Cathepsin S Controls Angiogenesis and Tumor Growth via Matrix-derived Angiogenic Factors.
Neoplasms
Cathepsin S from both tumor and tumor-associated cells promote cancer growth and neovascularization.
Neoplasms
Cathepsin S in tumours, regional lymph nodes and sera of patients with lung cancer: relation to prognosis.
Neoplasms
Cathepsin S is aberrantly overexpressed in human hepatocellular carcinoma.
Neoplasms
Cathepsin S regulates renal fibrosis in mouse models of mild and severe hydronephrosis.
Neoplasms
Cathepsin S, a novel biomarker of adiposity: relevance to atherogenesis.
Neoplasms
Cathepsin S-cleavable, multi-block HPMA copolymers for improved SPECT/CT imaging of pancreatic cancer.
Neoplasms
Cathepsin S: therapeutic, diagnostic, and prognostic potential.
Neoplasms
Chlorella powder inhibits the activities of peptidase cathepsin S, PLA2, cyclooxygenase-2, thromboxane synthase, tyrosine phosphatases, tumor necrosis factor-alpha converting enzyme, calpain and kinases.
Neoplasms
Correlation between serum cathepsin S and insulin resistance in type 2 diabetes.
Neoplasms
Design and synthesis of alpha-ketoamides as cathepsin S inhibitors with potential applications against tumor invasion and angiogenesis.
Neoplasms
Detection of cathepsin S cysteine protease in human brain tumour microdialysates in vivo.
Neoplasms
Differential gene signatures in rat mammary tumors induced by DMBA and those induced by fractionated gamma radiation.
Neoplasms
DOTAM-Based, Targeted, Activatable Fluorescent Probes for the Highly Sensitive and Selective Detection of Cancer Cells.
Neoplasms
Dynamic Model of Protease State and Inhibitor Trafficking to Predict Protease Activity in Breast Cancer Cells.
Neoplasms
Effects of novel human cathepsin S inhibitors on cell migration in human cancer cells.
Neoplasms
Endothelial Dysfunction in Tristetraprolin-deficient Mice is not caused by Enhanced TNF-? Expression.
Neoplasms
Evaluating the diagnostic and prognostic value of circulating cathepsin S in gastric cancer.
Neoplasms
Exploring fragment-based target-specific ranking protocol with machine learning on cathepsin S.
Neoplasms
Fat cell-derived modulators of vascular cell pathophysiology: the list keeps growing.
Neoplasms
Fsn0503h antibody-mediated blockade of cathepsin S as a potential therapeutic strategy for the treatment of solid tumors.
Neoplasms
Glioblastoma and endothelial cells cross-talk, mediated by SDF-1, enhances tumour invasion and endothelial proliferation by increasing expression of cathepsins B, S, and MMP-9.
Neoplasms
Hispolon suppresses metastasis via autophagic degradation of cathepsin S in cervical cancer cells.
Neoplasms
IL-18 and IL-12 synergy induces matrix degrading enzymes in the lung.
Neoplasms
In vivo imaging of mouse tumors by a lipidated cathepsin S substrate.
Neoplasms
Increased levels of macrophage-secreted cathepsin S during prostate cancer progression in TRAMP mice and patients.
Neoplasms
Influence of a prudent diet on circulating cathepsin S in humans.
Neoplasms
Inhibition of Cathepsin S by Fsn0503 enhances the efficacy of chemotherapy in colorectal carcinomas.
Neoplasms
Inhibition of cathepsin S induces autophagy and apoptosis in human glioblastoma cell lines through ROS-mediated PI3K/AKT/mTOR/p70S6K and JNK signaling pathways.
Neoplasms
Inhibition of Cathepsin S Induces Mitochondrial Apoptosis in Glioblastoma Cell Lines Through Mitochondrial Stress and Autophagosome Accumulation.
Neoplasms
Inhibition of Cathepsin S Induces Mitochondrial ROS That Sensitizes TRAIL-Mediated Apoptosis Through p53-Mediated Downregulation of Bcl-2 and c-FLIP.
Neoplasms
Is There Any Role for Serum Cathepsin S and CRP Levels on Prognostic Information in Breast Cancer? The Swedish Mammography Cohort.
Neoplasms
Leading the invasion: The role of Cathepsin S in the tumour microenvironment.
Neoplasms
Long-term endurance training increases serum cathepsin S and decreases IL-6 and hsCRP levels.
Neoplasms
Lysosomal cysteine protease cathepsin S is involved in cancer cell motility by regulating store-operated Ca2+ entry.
Neoplasms
Molecular modeling assisted identification and biological evaluation of potent cathepsin S inhibitors.
Neoplasms
Novel Opportunities for Cathepsin S Inhibitors in Cancer Immunotherapy by Nanocarrier-Mediated Delivery.
Neoplasms
Plasminogen hydrolysis by cathepsin S and identification of derived peptides as selective substrate for cathepsin V and cathepsin L inhibitor.
Neoplasms
Pro-inflammatory cytokines induce expression of matrix-metabolizing enzymes in human cervical smooth muscle cells.
Neoplasms
Radiation-induced cathepsin S is involved in radioresistance.
Neoplasms
Recent advances in the field of anti-cancer immunotherapy.
Neoplasms
Recombinant cathepsin S propeptide attenuates cell invasion by inhibition of cathepsin L-like proteases in tumor microenvironment.
Neoplasms
Regulating BRCA1 protein stability by cathepsin S-mediated ubiquitin degradation.
Neoplasms
Silencing cathepsin S gene expression inhibits growth, invasion and angiogenesis of human hepatocellular carcinoma in vitro.
Neoplasms
Targeting cathepsin S induces tumor cell autophagy via the EGFR-ERK signaling pathway.
Neoplasms
The clinical significance of cathepsin S expression in human astrocytomas.
Neoplasms
The proinflammatory cytokines interleukin-1? and tumor necrosis factor ? promote the expression and secretion of proteolytically active cathepsin S from human chondrocytes.
Neoplasms
The Role of Affordable, Point-of-Care Technologies for Cancer Care in Low- and Middle-Income Countries: A Review and Commentary.
Neoplasms
Up-regulation of cathepsin S expression by HSP90 and 5-HT7 receptor-dependent serotonin signaling correlates with triple negativity of human breast cancer.
Neoplasms
Z-FL-COCHO, a cathepsin S inhibitor, enhances oxaliplatin-mediated apoptosis through the induction of endoplasmic reticulum stress.
Neoplasms
[Effects of up-regulation of cathepsin S by HBx gene on HepG2 cell].
Nephritis
Connective tissue diseases. Inhibiting cathepsin S to treat SLE and lupus nephritis.
Neuralgia
Cathepsin S release from primary cultured microglia is regulated by the P2X7 receptor.
Neuralgia
Differential expression of Cathepsin S and X in the spinal cord of a rat neuropathic pain model.
Neuralgia
Discovery of orally bioavailable cathepsin S inhibitors for the reversal of neuropathic pain.
Neuralgia
Inhibition of spinal microglial cathepsin S for the reversal of neuropathic pain.
Neuralgia
Microglial signalling mechanisms: Cathepsin S and Fractalkine.
Neuralgia
Overcoming hERG issues for brain-penetrating cathepsin S inhibitors: 2-cyanopyrimidines. Part 2.
Neuralgia
Recent advances in the design of cathepsin S inhibitors.
Neuralgia
Selective Cathepsin S Inhibition with MIV-247 Attenuates Mechanical Allodynia and Enhances the Antiallodynic Effects of Gabapentin and Pregabalin in a Mouse Model of Neuropathic Pain.
Neuroinflammatory Diseases
Hydrogen sulfide inhibits ATP-induced neuroinflammation and A?1-42 synthesis by suppressing the activation of STAT3 and cathepsin S.
Niemann-Pick Diseases
Cathepsin S contributes to microglia-mediated olfactory dysfunction through the regulation of Cx3cl1-Cx3cr1 axis in a Niemann-Pick disease type C1 model.
Non-alcoholic Fatty Liver Disease
Serum lipocalin-2, cathepsin S and chemerin levels and nonalcoholic fatty liver disease.
Obesity
Cathepsin S controls adipocytic and osteoblastic differentiation, bone turnover, and bone microarchitecture.
Obesity
Cathepsin s promotes human preadipocyte differentiation: possible involvement of fibronectin degradation.
Obesity
Cathepsin S, a novel biomarker of adiposity: relevance to atherogenesis.
Obesity
Cathepsins in human obesity: changes in energy balance predominantly affect cathepsin s in adipose tissue and in circulation.
Obesity
Circulating cathepsin S improves glycaemic control in mice.
Obesity
Determination of cathepsin S abundance and activity in human plasma and implications for clinical investigation.
Obesity
Discovery of novel cathepsin S inhibitors by pharmacophore-based virtual high-throughput screening.
Obesity
Emerging role of cathepsin S in obesity and its associated diseases.
Obesity
Improvement of cathepsin S detection using a designed FRET peptide based on putative natural substrates.
Obesity
Molecular modeling assisted identification and biological evaluation of potent cathepsin S inhibitors.
Obesity
Serum cathepsin S is associated with serum C-reactive protein and interleukin-6 independently of obesity in elderly men.
Obesity
Vitamin D deficiency in childhood obesity is associated with high levels of circulating inflammatory mediators, and low insulin sensitivity.
Obesity, Abdominal
Elevated circulating cathepsin S levels are associated with metabolic syndrome in overweight and obese individuals.
Obstetric Labor, Premature
Omega-3 Polyunsaturated Fatty Acids Reduce Preterm Labor by Inhibiting Trophoblast Cathepsin S and Inflammasome Activation.
Osteoporosis
Potency and selectivity of inhibition of cathepsin K, L and S by their respective propeptides.
Osteoporosis
The role of cathepsins in osteoporosis and arthritis: rationale for the design of new therapeutics.
Ovarian Neoplasms
CTD-2020K17.1, a Novel Long Non-Coding RNA, Promotes Migration, Invasion, and Proliferation of Serous Ovarian Cancer Cells In Vitro.
Ovarian Neoplasms
Long Noncoding RNA CTD-2589M5.4 Inhibits Ovarian Cancer Cell Proliferation, Migration, and Invasion Via Downregulation of the Extracellular Matrix-Receptor Interaction Pathway.
Ovarian Neoplasms
Two SPRi biosensors for the determination of cathepsin S in blood plasma.
Overweight
Elevated circulating cathepsin S levels are associated with metabolic syndrome in overweight and obese individuals.
Pancreatic Neoplasms
The influence of linker length on the properties of cathepsin S cleavable (177)Lu-labeled HPMA copolymers for pancreatic cancer imaging.
Pancreatitis
Active Cathepsins B, L and S in Murine and Human Pancreatitis.
Papilloma, Inverted
Expression of cathepsin S and its inhibitor stefin A in sinonasal inverted papilloma.
Paralysis
Cathepsin S increases tau oligomer formation through limited cleavage, but only IL-6, not cathespin S serum levels correlate with disease severity in the neurodegenerative tauopathy progressive supranuclear palsy.
Pediatric Obesity
Vitamin D deficiency in childhood obesity is associated with high levels of circulating inflammatory mediators, and low insulin sensitivity.
Periodontal Diseases
Role of Cathepsin S in Periodontal Inflammation and Infection.
Periodontitis
Role of Cathepsin S in Periodontal Inflammation and Infection.
Peripheral Arterial Disease
Cysteine Protease Cathepsins in Atherosclerotic Cardiovascular Diseases.
Peripheral Nerve Injuries
Peripheral role of cathepsin S in Th1 cell-dependent transition of nerve injury-induced acute pain to a chronic pain state.
Peripheral Nerve Injuries
Role of the cysteine protease cathepsin S in neuropathic hyperalgesia.
Peripheral Nerve Injuries
Selective inhibition of peripheral cathepsin S reverses tactile allodynia following peripheral nerve injury in mouse.
Peripheral Nervous System Diseases
Targeting lysosomal cysteine protease cathepsin S reveals immunomodulatory therapeutic strategy for oxaliplatin-induced peripheral neuropathy.
Pneumoconiosis
Cathepsin S, a new serum biomarker of sarcoidosis discovered by transcriptome analysis of alveolar macrophages.
Pneumonia
Genetic and Pharmacological Evaluation of Cathepsin S in a Mouse Model of Asthma.
Pneumonia
Point-of-care testing for community-acquired pneumonia: do we have all the answers?
Prediabetic State
Proportional correlates of adipolin and cathepsin S in metabolic syndrome patients with and without prediabetes.
Prostatic Neoplasms
Increased levels of macrophage-secreted cathepsin S during prostate cancer progression in TRAMP mice and patients.
Proteinuria
Cathepsin S inhibition combines control of systemic and peripheral pathomechanisms of autoimmune tissue injury.
Pruritus
Cathepsin S, a new pruritus biomarker in clinical dandruff/seborrhoeic dermatitis evaluation.
Pruritus
Skullcapflavone II Suppresses TNF-?/IFN-?-Induced TARC, MDC, and CTSS Production in HaCaT Cells.
Psoriasis
A novel approach for reliable detection of cathepsin S activities in mouse antigen presenting cells.
Psoriasis
Advances in cathepsin S inhibitor design.
Psoriasis
Cathepsin S is the major activator of the psoriasis-associated proinflammatory cytokine IL-36?.
Psoriasis
Differential effects of specific cathepsin S inhibition in biocompartments from patients with primary Sjögren syndrome.
Pulmonary Arterial Hypertension
Cathepsin S promotes the development of pulmonary arterial hypertension.
Pulmonary Disease, Chronic Obstructive
A highly significant association between Cathepsin S gene polymorphisms rs12068264 and chronic obstructive pulmonary disease susceptibility in Han Chinese population.
Pulmonary Disease, Chronic Obstructive
Cathepsin S inhibitors as novel immunomodulators.
Pulmonary Disease, Chronic Obstructive
Cigarette smoke induces overexpression of active human cathepsin S in lungs from current smokers with or without COPD.
Pulmonary Disease, Chronic Obstructive
Common functional polymorphisms in the cathepsin S promoter in Japanese subjects: possible contribution to pulmonary emphysema.
Pulmonary Disease, Chronic Obstructive
Plasma Cathepsin S and Cathepsin S/Cystatin C Ratios Are Potential Biomarkers for COPD.
Pulmonary Disease, Chronic Obstructive
Protein Phosphatase 2A Reduces Cigarette Smoke-Induced Cathepsin S and Loss of Lung Function.
Pulmonary Disease, Chronic Obstructive
Secretory leucocyte protease inhibitor inhibits interferon-gamma-induced cathepsin S expression.
Pulmonary Disease, Chronic Obstructive
Therapeutic Inhibition of Cathepsin S Reduces Inflammation and Mucus Plugging in Adult ?ENaC-Tg Mice.
Pulmonary Disease, Chronic Obstructive
[The association between Cathepsin S and pulmonary function and CT phenotypes in patients with chronic obstructive pulmonary disease].
Pulmonary Emphysema
Common functional polymorphisms in the cathepsin S promoter in Japanese subjects: possible contribution to pulmonary emphysema.
Pulmonary Eosinophilia
Genetic and Pharmacological Evaluation of Cathepsin S in a Mouse Model of Asthma.
Renal Insufficiency, Chronic
Arterial and aortic valve calcification abolished by elastolytic cathepsin S deficiency in chronic renal disease.
Renal Insufficiency, Chronic
Cathepsin S As an Inhibitor of Cardiovascular Inflammation and Calcification in Chronic Kidney Disease.
Renal Insufficiency, Chronic
Performance of point of care assays for hepatitis B and C viruses in chronic kidney disease patients.
Renal Insufficiency, Chronic
Selective Cathepsin S Inhibition Attenuates Atherosclerosis in Apolipoprotein E-Deficient Mice with Chronic Renal Disease.
Respiratory Tract Infections
An ideal test? A multi-country qualitative study of clinicians' and patients' views of point of care tests for lower respiratory tract infection in primary care.
Respiratory Tract Infections
Assessing the potential of upper respiratory tract point-of-care testing: a systematic review of the prognostic significance of upper respiratory tract microbes.
Respiratory Tract Infections
COVID-19 point-of-care testing in care homes: what are the lessons for policy and practice?
Respiratory Tract Infections
In-vitro diagnostic point-of-care tests in paediatric ambulatory care: A systematic review and meta-analysis.
Sarcoidosis
Cathepsin S, a new serum biomarker of sarcoidosis discovered by transcriptome analysis of alveolar macrophages.
Scleroderma, Systemic
Decreased serum cathepsin S levels in patients with systemic sclerosis-associated interstitial lung disease.
Scrub Typhus
Scrub typhus point-of-care testing: A systematic review and meta-analysis.
Seizures
Increased expression of the lysosomal protease cathepsin S in hippocampal microglia following kainate-induced seizures.
Sepsis
Systemic inflammation and protease profile of Afro-Caribbean patients with sepsis.
Sexually Transmitted Diseases
"It's not a time spent issue, it's a 'what have you spent your time doing?' issue
" A qualitative study of UK patient opinions and expectations for implementation of Point of Care Tests for sexually transmitted infections and antimicrobial resistance.
Sexually Transmitted Diseases
Advancing point of care diagnostics for the control and prevention of STIs: the way forward.
Sexually Transmitted Diseases
Patterns of point-of-care test use among obstetricians and gynaecologists in the US.
Sexually Transmitted Diseases
Perceptions of an ideal point-of-care test for sexually transmitted infections--a qualitative study of focus group discussions with medical providers.
Sexually Transmitted Diseases
Point-of-care diagnostics: needs of African health care workers and their role combating global antimicrobial resistance.
Sexually Transmitted Diseases
Point-of-care testing for HCV infection: recent advances and implications for alternative screening.
signal peptidase ii deficiency
B cell survival, surface BCR and BAFFR expression, CD74 metabolism, and CD8- dendritic cells require the intramembrane endopeptidase SPPL2A.
Sjogren's Syndrome
Insights into the roles of cathepsins in antigen processing and presentation revealed by specific inhibitors.
Sleep Apnea, Obstructive
Usefulness of Cathepsin S to Predict Risk for Obstructive Sleep Apnea among Patients with Type 2 Diabetes.
Speech Disorders
The Communication Attitude Test (CAT-S): normative values for 220 Swedish children.
ST Elevation Myocardial Infarction
Increased plasma cathepsin S and trombospondin-1 in patients with acute ST segment elevation myocardial infarction.
Stomach Diseases
Evaluating the diagnostic and prognostic value of circulating cathepsin S in gastric cancer.
Stomach Neoplasms
Cathepsin S as a target in gastric cancer.
Stomach Neoplasms
Cathepsin S mediates gastric cancer cell migration and invasion via a putative network of metastasis-associated proteins.
Stomach Neoplasms
Cathepsin S Mediates Gastric Cancer Cell Migration and Invasion via a Putative Network of Metastasis-Associated Proteins.
Stomach Neoplasms
Evaluating the diagnostic and prognostic value of circulating cathepsin S in gastric cancer.
Stroke
Point-of-Care-Testing in Acute Stroke Management: An Unmet Need Ripe for Technological Harvest.
Supranuclear Palsy, Progressive
Cathepsin S increases tau oligomer formation through limited cleavage, but only IL-6, not cathespin S serum levels correlate with disease severity in the neurodegenerative tauopathy progressive supranuclear palsy.
Synovitis
Detecting cathepsin activity in human osteoarthritis via activity-based probes.
Syphilis
Estimating the uptake of maternal syphilis screening and other antenatal interventions before and after national rollout of syphilis point-of-care testing in Ghana.
Syphilis
Factors associated with failure to screen for syphilis during antenatal care in Ghana: a case control study.
Syphilis
Field evaluation of two point-of-care tests for syphilis among men who have sex with men, Verona, Italy.
Syphilis
Integrated point-of-care testing (POCT) for HIV, syphilis, malaria and anaemia at antenatal facilities in western Kenya: a qualitative study exploring end-users' perspectives of appropriateness, acceptability and feasibility.
Syphilis
Patterns of point-of-care test use among obstetricians and gynaecologists in the US.
Syphilis
Point-of-care diagnostics: needs of African health care workers and their role combating global antimicrobial resistance.
Syphilis
Rollout of rapid point of care tests for antenatal syphilis screening in Ghana: healthcare provider perspectives and experiences.
Syphilis
Standardised protocol for a prospective cross-sectional multicentre clinic-based evaluation of two dual point-of-care tests for the screening of HIV and syphilis in men who have sex with men, sex workers and pregnant women.
Syphilis
The impact of antenatal syphilis point of care testing on pregnancy outcomes: A systematic review.
Tauopathies
Cathepsin S increases tau oligomer formation through limited cleavage, but only IL-6, not cathespin S serum levels correlate with disease severity in the neurodegenerative tauopathy progressive supranuclear palsy.
Thrombophilia
Point-of-Care Testing in Liver Disease and Liver Surgery.
Thrombosis
Cathepsin S is aberrantly overexpressed in human hepatocellular carcinoma.
Thrombosis
Insights from molecular modeling into the selective inhibition of cathepsin S by its inhibitor.
Thrombosis
Point-of-Care Testing in Liver Disease and Liver Surgery.
Triple Negative Breast Neoplasms
A Novel Role for Cathepsin S as a Potential Biomarker in Triple Negative Breast Cancer.
Triple Negative Breast Neoplasms
Down-regulation of cathepsin S and matrix metalloproteinase-9 via Src, a non-receptor tyrosine kinase, suppresses triple-negative breast cancer growth and metastasis.
Tuberculosis
Cathepsin L maturation and activity is impaired in macrophages harboring M. avium and M. tuberculosis.
Urinary Bladder Neoplasms
Cathepsin S inhibition changes regulatory T-cell activity in regulating bladder cancer and immune cell proliferation and apoptosis.
Uterine Cervical Neoplasms
Hispolon suppresses metastasis via autophagic degradation of cathepsin S in cervical cancer cells.
Uterine Cervical Neoplasms
Phloretin suppresses metastasis by targeting protease and inhibits cancer stemness and angiogenesis in human cervical cancer cells.
Vascular Diseases
Adenosine-to-inosine RNA editing controls cathepsin S expression in atherosclerosis by enabling HuR-mediated post-transcriptional regulation.
Vascular Diseases
Fat cell-derived modulators of vascular cell pathophysiology: the list keeps growing.
Vascular System Injuries
Fat cell-derived modulators of vascular cell pathophysiology: the list keeps growing.
Venous Thromboembolism
Point-of-care testing in primary care: A systematic review on implementation aspects addressed in test evaluations.
Virus Diseases
Point of care testing: diagnosis outside the virology laboratory.
Vitreoretinopathy, Proliferative
Melatonin attenuates epidermal growth factor-induced cathepsin S expression in ARPE-19 cells: Implications for proliferative vitreoretinopathy.
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0.000095
(2R)-2-(2-cyclohexylethyl)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000002
(2R)-2-(2-cyclopentylethyl)-4-morpholin-4-yl-4-oxo-N-[(1S)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
0.000011
(2R)-2-(2-cyclopentylethyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000194
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)butanamide
-
-
0.000013
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)butyl]butanamide
-
-
0.000016
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
0.000062
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-phenyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]butanamide
-
-
0.000018
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
0.000028
(2R)-2-(cyclohexylmethyl)-N-[(1R)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000011
(2R)-2-(cyclohexylmethyl)-N-[(1R)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.1
(2R)-2-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
Ki above 0.1 mM
0.000012
(2R)-2-(cyclopentylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1S)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)butyl]butanamide
-
-
0.000031
(2R)-2-(cyclopentylmethyl)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000038
(2R)-2-(cyclopentylmethyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.024
(2R)-2-benzyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
Ki above 0.024 mM
0.000408
(2R)-4-dimethyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-2-(2-morpholin-4-yl-2-oxoethyl)pentanamide
-
-
0.00006
(2R)-4-morpholin-4-yl-4-oxo-2-(2-phenylethyl)-N-[(1S)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
0.00007
(2R)-5-dimethyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-2-(2-morpholin-4-yl-2-oxoethyl)hexanamide
-
-
0.000014
(2R)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-2-(2-morpholin-4-yl-2-oxoethyl)-5-phenylpentanamide
-
-
0.000027
(2R)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-(2-phenylethyl)butanamide
-
-
0.000021
(2S)-2-(4-chlorophenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000024
(2S)-2-(4-fluorophenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000105
(2S)-2-(4-methoxyphenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000134
(2S)-2-(4-methylphenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.001368
(2S)-2-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000019
(2S)-3-cyclohexyl-1-(morpholin-4-yl)-1-oxopropan-2-yl [(2S)-1-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)propan-2-yl]carbamate
-
-
0.000261
(2S)-4-morpholin-4-yl-4-oxo-2-phenyl-N-[(1S)-1-phenyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]butanamide
-
-
0.000037
(2S)-4-morpholin-4-yl-4-oxo-2-phenyl-N-[(1S)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
0.0156
(2S)-4-morpholin-4-yl-4-oxo-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
0.000616
(2S)-N-[(1S)-1-cyclopropyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
0.00159
(2S)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
0.000025
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-phenylbutanamide
-
-
0.1
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[2-(trifluoromethyl)phenyl]butanamide
-
Ki above 0.1 mM
0.01853
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[3-(trifluoromethyl)phenyl]butanamide
-
-
0.000043
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
0.000043
(2S)-N-[(2S)-3-methyl-1-[[4-(trifluoromethoxy)phenyl]amino]butan-2-yl]-4-(morpholin-4-yl)-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
0.00844
(2Z)-3-(4-[[5-(3,5-dimethylisoxazol-4-yl)-1,2,4-oxadiazol-3-yl]methoxy]phenyl)-2-(methylsulfonyl)prop-2-enenitrile
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.1
(3R)-3-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
Ki above 0.1 mM
0.001721
(3S)-3-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000071
(3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoic acid
-
-
0.00298
(3S)-N-[2-(1H-indol-3-yl)ethyl]-3-[[(4-methylphenyl)sulfonyl]amino]-2-oxo-4-phenylbutanamide
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.00031
(S)-[1-[1-cyano-pyrrolidin-3(R)-ylcarbamoyl]-3-methyl-butyl]-carbamic acid benzyl ester
-
pH 6.5, 23°C
0.00097
(S)-[1-[1-cyano-pyrrolidin-3(S)-ylcarbamoyl]-3-methyl-butyl]-carbamic acid benzyl ester
-
pH 6.5, 23°C
0.4377
1,1-bis(cyanomethyl)-3-[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]urea
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.0000083
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[(4-[[(2,2,2-trifluoroethyl)sulfonyl]amino]benzoyl)amino]propanoyl]amino)-L-erythro-hex-2-ulose
-
-
0.00003
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([2-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000049
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000004
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000012
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000026
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000008
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000023
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000021
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-3-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000027
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-4-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000023
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(thiophen-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00011
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[methyl(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000063
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(methylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000056
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(phenylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000019
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-([4-[(ethylsulfonyl)amino]benzoyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.0000053
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-([[4-([[(dimethylamino)methyl]sulfonyl]amino)phenyl]carbonyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000007
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[(4-[[(2,4-dimethyl-1,3-thiazol-5-yl)sulfonyl]amino]benzoyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose ammoniate (1:1)
-
-
0.0000034
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[(4-[[(3-fluorophenyl)sulfonyl]amino]benzoyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.000001
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[(4-[[(3-methoxyphenyl)sulfonyl]amino]benzoyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.00033
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([2-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000016
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-fluoro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000026
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000019
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([4-[(ethylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000007
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2,4-dimethyl-1,3-thiazol-5-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000038
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000034
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000001
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000002
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000033
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000012
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([3-[(methylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.0000026
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([4-[(methylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.0000008
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([4-[(phenylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.0000009
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([4-[(pyridin-4-ylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.00019
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-(methylsulfamoyl)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000057
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-([[4-(1-methylethyl)-1,3-thiazol-2-yl]sulfonyl]amino)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00014
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-sulfamoylphenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000045
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methyl-1H-imidazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000029
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methylethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000083
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2,2,2-trifluoroethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000039
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2-methylphenyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000013
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000009
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methylpyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000086
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(5-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00014
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[4-(methylsulfamoyl)benzoyl]amino]propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.000031
1,4-anhydro-3,5,6-trideoxy-3-[[4-methyl-N-(thiophen-3-ylcarbonyl)-L-leucyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00018
1,4-anhydro-3-[[(2S)-2-([4-[(cyclohexylsulfonyl)amino]benzoyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-erythro-hex-2-ulose
-
-
0.0000024
1,4-anhydro-3-[[(2S)-2-([4-[(cyclopropylsulfonyl)amino]benzoyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-erythro-hex-2-ulose
-
-
0.0000056
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000012
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000031
1,4-anhydro-3-[[(2S)-2-[([4-[(benzylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000034
1,4-anhydro-3-[[(2S)-2-[([4-[(butylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000024
1,4-anhydro-3-[[(2S)-2-[([4-[(cyclopropylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000059
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-chloropyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000008
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000006
1,4-anhydro-3-[[(2S)-2-[[(4-[[(3-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000011
1,4-anhydro-3-[[(2S)-2-[[(4-[[(4-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00018
1,4-anhydro-3-[[(2S)-2-[[(4-[[(cyclohexylmethyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000033
1-cyano-(3,4-didehydro)-Pro-Leu methyl ester
-
pH 6.5, 23°C
0.026
1-cyano-(D)-Pro-(D)-Leu methyl ester
-
pH 6.5, 23°C
0.054
1-cyano-(D)-Pro-Ala methyl ester
-
pH 6.5, 23°C
0.000012
1-cyano-(D)-Pro-Leu benzyl ester
-
pH 6.5, 23°C
0.03
1-cyano-(D)-Pro-Leu benzylamide
-
pH 6.5, 23°C
0.00015
1-cyano-(D)-Pro-Leu dimethylamide
-
pH 6.5, 23°C
0.00054
1-cyano-(D)-Pro-Leu methyl ester
-
pH 6.5, 23°C
0.00003
1-cyano-(trans-benzyloxy)prolylleucine methyl ester
-
pH 6.4, 25°C
0.000054
1-cyano-(trans-hydroxy)-Pro-Leu methyl ester
-
pH 6.5, 23°C
0.00028
1-cyano-Pro isoamylamide
-
pH 6.5, 23°C
0.0011
1-cyano-Pro-(D)-Leu methyl ester
-
pH 6.5, 23°C
0.00053
1-cyano-Pro-Ala methyl ester
-
pH 6.5, 23°C
0.000014
1-cyano-Pro-Leu benzyl ester
-
pH 6.5, 23°C
0.000052
1-cyano-Pro-Leu methyl ester
-
pH 6.5, 23°C
0.000035
1-cyano-Pro-Leu-Gly ethyl ester
-
pH 6.5, 23°C
0.0000067
1-cyano-Pro-Leu-Leu-Leu methyl ester
-
pH 6.5, 23°C
0.00024
1-cyano-Pro-Phe methyl ester
-
pH 6.5, 23°C
0.01458
2,2'-[[3-(trifluoromethyl)phenyl]imino]bis[N-(4-methylphenyl)acetamide]
-
in 0.5 M MES, 2 mM DTT at pH 6.0
146.3
2-(4-tert-butylphenyl)-5-[[2-(3,4-dimethoxyphenyl)ethyl]amino]-1,3-oxazole-4-carbonitrile
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.05686
2-hydroxy-N'-[1H-indol-3-yl(oxo)acetyl]-2,2-diphenylacetohydrazide
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.0109
2-[[3-(4-chloro-5-hydroxy-2-methoxyphenyl)-4-oxo-3,4-dihydroquinazolin-2-yl]sulfanyl]-N-[(1S)-1-cyano-1,2-dimethylpropyl]acetamide
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.000057
3-[[(2S)-2-[([3-acetyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000013
3-[[(2S)-2-[[(4-[[(4-aminophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
3.39
4-[(4-[(E)-[(cyanoacetyl)hydrazono]methyl]phenoxy)methyl]benzoic acid
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.000004
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
with Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as substrate
0.0027
benzyloxycarbonyl-Ala-Leu-COCHO
-
pH 6.4, 25°C
0.00125
Benzyloxycarbonyl-Phe-Ala-CHN2
-
pH 6.5, 25°C
0.0000232
benzyloxycarbonyl-Phe-Ala-COCHO
-
pH 6.4, 25°C
0.0000024
Benzyloxycarbonyl-Phe-Arg
-
pH 6.4, 25°C
0.000000185
benzyloxycarbonyl-Phe-Leu-COCHO
-
pH 6.4, 25°C
0.00000223
benzyloxycarbonyl-Phe-Tyr(OBut)-COCHO
-
pH 6.4, 25°C
0.00015
benzyloxycarbonyl-Val-Val-Lys-NHO-4-nitrobenzoyl
-
pH 6.5, 25°C
0.0000063
cathepsin K propeptide
-
-
-
0.000065
cathepsin L propeptide
-
-
-
0.00000005 - 0.0000076
cathepsin S propeptide
-
0.000034
JNJ 10329670
-
pH 5.0
0.01663
methyl (2Z)-4-[4-(dimethylamino)phenyl]-4-oxo-2-[(phenylcarbonyl)hydrazono]butanoate
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.000005
methyl (3R)-3-[[(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanoyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate
-
-
0.000069
methyl (3S)-3-[[(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanoyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate
-
-
0.00278
methyl 4-[(E)-[[(3-[2-[(2-chlorobenzyl)oxy]phenyl]-1H-pyrazol-5-yl)carbonyl]hydrazono]methyl]benzoate
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.00005
morpholine-4-carboxylic acid [1S-[1S-(benzoyl-hydrazonomethyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
pH 4.5
0.000033
morpholine-4-carboxylic acid [1S-[1S-[(2-hydroxy-benzoyl)-hydrazonomethyl]-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
pH 4.5
0.00011
morpholine-4-carboxylic acid [1S-[1S-[(4-hydroxybenzoyl)-hydrazonomethyl]-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
pH 4.5
0.1982
N-(4-cyano-1-phenyl-1H-pyrazol-5-yl)-2-[(4-ethyl-5-thiophen-2-yl-4H-1,2,4-triazol-3-yl)sulfanyl]acetamide
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.0000055
N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-norvalinamide
-
-
0.00889
N-[(1R)-1-([2-[(1,3-benzoxazol-2-ylsulfanyl)acetyl]hydrazino]carbonyl)propyl]-2-[(phenylcarbonyl)amino]benzamide
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.0012
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1,2-dimethylpropyl]benzamide
-
-
0.00042
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1,2-dimethylpropyl]thiophene-3-carboxamide
-
-
0.000015
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-(4-methylcyclohexyl)ethyl]thiophene-3-carboxamide
-
-
0.000015
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-(trans-4-methylcyclohexyl)ethyl]thiophene-3-carboxamide
-
-
0.0002
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-cyclohexylethyl]benzamide
-
-
0.000018
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-cyclohexylethyl]thiophene-3-carboxamide
-
-
0.00042
N-[(2S)-2-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-3-methylbutan-2-yl]thiophene-3-carboxamide
-
-
0.000009
N-[(2S)-3-methyl-2-[1-[(2S)-1-oxohexan-2-yl]-1H-1,2,3-triazol-4-yl]butan-2-yl]thiophene-3-carboxamide
-
-
0.01948
N-[2-(1-methylethyl)phenyl]-Na-(phenoxycarbonyl)-L-tryptophanamide
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.01527
N-[2-oxo-2-[(2Z)-2-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)hydrazino]ethyl]-2-pyridin-2-yl-1H-benzimidazole-1-carboxamide
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.000068
N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-(3-methylbenzoyl)-L-leucinamide
-
-
0.000003
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[(2S)-1-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)propan-2-yl]-L-alaninamide
-
-
0.025
o-aminobenzoic acid-Leu-Phe-Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
substrate N-benzyloxycarbonyl-L-Phe-Arg-7-amido-4-methylcoumarin
0.02
o-aminobenzoic acid-Val-Leu-Phe-Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
substrate N-benzyloxycarbonyl-L-Phe-Arg-7-amido-4-methylcoumarin
0.00049
[(2',3',4'-trifluorobiphenyl-2-yl)oxy]acetaldehyde
-
-
0.02817
[2-[[(4-chlorophenyl)sulfanyl]methyl]-4-hydroxy-6,7-dimethoxyquinazolin-3(4H)-yl]acetonitrile
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.0000096
[[2',3'-difluoro-4'-(2-methylpropyl)biphenyl-2-yl]oxy]acetaldehyde
-
-
additional information
(2S)-2-amino-N-[(1S)-2-(biphenyl-4-yl)-1-cyanoethyl]butanamide
0.00000005
cathepsin S propeptide
-
wild-type enzyme
-
0.00000027
cathepsin S propeptide
-
pH 6.5, 37°C
-
0.0000003
cathepsin S propeptide
-
mutant enzyme E44A
-
0.0000013
cathepsin S propeptide
-
mutant enzyme R48A
-
0.0000025
cathepsin S propeptide
-
using benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin as a substrate
-
0.0000076
cathepsin S propeptide
-
-
-
additional information
(2S)-2-amino-N-[(1S)-2-(biphenyl-4-yl)-1-cyanoethyl]butanamide
-
value above 0.01
additional information
additional information
-
Ki-values above 0.15 mM: 1-iminomethyl-(D)-Pro-Leu benzyl ester, 1-formyl-(D)-Pro-Leu benzyl ester
-
additional information
N2-(morpholin-4-ylcarbonyl)-N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-leucinamide
-
value below 0.0000001
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
0.0000043
(4R)-1-acetyl-N-[(2R)-1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000033
(4R)-1-acetyl-N-[(2S)-1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0001
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxo-3-phenylpropan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0001
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(ethylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000207
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfanyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000837
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfinyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000033
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.001
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-phenoxy-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000023
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[(2-chlorophenyl)sulfonyl]-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000032
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[(4-fluorophenyl)sulfonyl]-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000032
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[[4-(1H-pyrazol-1-yl)phenyl]sulfonyl]-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000181
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxopropan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000246
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-3-methyl-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000024
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(2-methylpropanoyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000454
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(2-oxopropyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000011
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(3-chlorobenzoyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000033
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(3-methoxypropanoyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.000002
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(4-chlorobenzoyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000041
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(biphenyl-4-ylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000033
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(cyclohexylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000035
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(methylsulfinyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.000003
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-benzoyl-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000124
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-phenyl-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000035
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyridin-3-ylcarbonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000033
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyridin-4-ylcarbonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000037
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyrrolidin-1-ylcarbonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000027
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(trifluoroacetyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000031
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-propanoyl-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.000156
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000366
(4R)-N-[2-(1,3-benzoxazol-2-yl)-2-oxoethyl]-1-(cyclohexylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.000006
2-cyano-4-(2-hydroxyethoxy)-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00013
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000014
2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000031
2-cyano-4-[(1,4-dioxaspiro[4.5]dec-8-ylmethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000026
2-cyano-4-[(2-cyclopentylethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000032
2-cyano-4-[(cyclohexylmethyl)(methyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000022
2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000022
2-cyano-4-[[(4,4-difluorocyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000093
2-cyano-4-[[(4,4-dimethylcyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000003
2-cyano-4-[[1-(2-hydroxyethyl)piperidin-4-yl]methoxy]-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000007
2-cyano-N-(1-methyl-4-phenylpiperidin-4-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000015
2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000024
2-cyano-N-(4,5-dimethoxybiphenyl-2-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000005
2-cyano-N-methyl-4-(piperidin-4-ylmethoxy)-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000003
2-cyano-N-methyl-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000003
2-cyano-N-methyl-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[4.5]dec-8-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000005
2-cyano-N-methyl-4-[(spiro[3.5]non-7-ylmethyl)amino]-6-[(2,2,6,6-tetramethylpiperidin-4-yl)oxy]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000002
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
0.000004
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000003
2-cyano-N-methyl-4-[[1-(1-methylethyl)piperidin-4-yl]methoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000006
2-cyano-N-[(1-methyl-4-phenylpiperidin-4-yl)methyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000004
2-cyano-N-[(1R)-2-pyridin-2-yl-1-(pyrrolidin-1-ylmethyl)ethyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000003
2-cyano-N-[5-[(1-methylpiperidin-4-yl)oxy]biphenyl-2-yl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.00001
4-[(1-acetylpiperidin-4-yl)methoxy]-2-cyano-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000022
4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000002
5-bromo-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
42
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
Homo sapiens
at pH 6.5 and 37°C
0.000002
N-(4-benzyl-1-methylpiperidin-4-yl)-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000001
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)oxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000021
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylpropyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000023
N-[(1S)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000395
(2R)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.0001
(2R)-2-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)-2-phenylethanol
Homo sapiens
-
-
0.001991
(2R)-2-[4'-(1-azabicyclo[2.2.2]oct-4-yl)-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
Homo sapiens
-
IC50: 1991 nM
0.00834
(2R)-2-[4'-(4-tert-butylpiperazin-1-yl)-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
Homo sapiens
-
IC50: 8340 nM
0.001427
(2R)-2-[4'-[1-(2-amino-2-methylpropyl)piperidin-4-yl]-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
Homo sapiens
-
IC50: 1427 nM
0.00008
(2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-N-(1-cyanocyclopropyl)-3-(methylsulfanyl)propanamide
Homo sapiens
-
-
0.000135
(2R)-N-(1-cyanocyclopropyl)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.01
(2R)-N-(cyanomethyl)-2-[4'-[4-(2-hydroxy-2-methylpropyl)-1-piperazinyl][1,1'-biphenyl]-3-yl]-4-methylpentanamide
Homo sapiens
-
IC50 above 0.01 mM
0.000609
(2R)-N-(cyanomethyl)-2-[4'-[4-(2-hydroxyethyl)-1-piperazinyl][1,1'-biphenyl]-3-yl]-4-methylpentanamide
Homo sapiens
-
IC50: 609 nM
0.00201
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)-[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 2010 nM
0.01
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1H-tetraazol-5-yl)-1,1'-biphenyl-3-yl]pentanamide
Homo sapiens
-
IC50 above 0.01 mM
0.003931
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methyl-1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 3931 nM
0.001365
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-pyrimidinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 1365 nM
0.002364
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-[4-(2-oxopropyl)-piperazin-1-yl]-1,1'-biphenyl-3-yl]pentanamide
Homo sapiens
-
IC50: 2364 nM
0.000037
(2R)-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000062
(2R)-N-[(1R)-2-[(4-chlorobenzyl)oxy]-1-cyanoethyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000658
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-2-carboxamide
Homo sapiens
-
IC50: 658 nM
0.000018
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
Homo sapiens
-
IC50: 18 nM
0.000171
(2R)-N-[(1S)-1-cyano-3-phenylpropyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000207
(2R)-N-[(3R)-1-benzyl-3-cyanopiperidin-4-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000066
(2R)-N-[(3R)-3-cyano-1-(1-methylethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000039
(2R)-N-[(3R)-3-cyano-1-(2-methylpropyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000022
(2R)-N-[(3R)-3-cyano-1-(2-phenylethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000022
(2R)-N-[(3R)-3-cyano-1-(cyclopropylmethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000023
(2R)-N-[(3R)-3-cyano-1-cycloheptylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000042
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(2,3-dihydro-1H-inden-2-ylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
-
0.000042
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(2,3-dihydro-1H-inden-2-ylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000023
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000063
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclopentylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000047
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(1-methylcyclohexyl)methyl]-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000014
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(4-methylcyclohexyl)methyl]-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.0000019
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-(morpholin-4-yl)-4-oxo-2-(1,2,3,4-tetrahydronaphthalen-2-ylmethyl)butanamide
Homo sapiens
-
-
0.003136
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-(morpholin-4-yl)-4-oxo-2-[(4-phenylcyclohexyl)methyl]butanamide
Homo sapiens
-
-
0.0000019
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-morpholin-4-yl-4-oxo-2-(1,2,3,4-tetrahydronaphthalen-2-ylmethyl)butanamide
Homo sapiens
-
-
0.003136
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-morpholin-4-yl-4-oxo-2-[(4-phenylcyclohexyl)methyl]butanamide
Homo sapiens
-
-
0.000075
(2R)-N-[(3R)-3-cyano-1-cyclopentylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000251
(2R)-N-[(3R)-3-cyano-1-methylpiperidin-4-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000155
(2R)-N-[(3R)-3-cyano-1-methylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000141
(2R)-N-[(3R)-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
-
0.000141
(2R)-N-[(3R)-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000029
(2R)-N-[(3S)-1-benzyl-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000041
(2R)-N-[(3S)-3-cyano-1-(cyclohexylmethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.00003
(2S)-1-(4,4'-bipiperidin-1-yl)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
Homo sapiens
-
-
0.000245
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxypropan-1-one
Homo sapiens
-
-
0.000058
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.00035
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(propan-2-ylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.0003
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(propylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.00001
(2S)-1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(1'-methyl-4,4'-bipiperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.000053
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
Homo sapiens
-
IC50: 53 nM
0.00033
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(furan-2-yl)methanone
Homo sapiens
-
-
0.00014
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(pyridin-2-yl)methanone
Homo sapiens
-
-
0.00031
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(tetrahydrofuran-2-yl)methanone
Homo sapiens
-
-
0.000006
(3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]phenyl)acetic acid
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000042
(3R)-tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
Homo sapiens
-
IC50: 42 nM
0.000012
(3S)-3-[(N-1,3-benzoxazol-2-yl-3-cyclohexyl-L-alanyl)amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoic acid
Homo sapiens
-
IC50: 12 nM
0.000027
(3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoic acid
Homo sapiens
-
IC50: 27 nM
0.000049
(3S)-tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
Homo sapiens
-
IC50: 49 nM
0.01
(4S)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]hexanamide
Homo sapiens
-
IC50 above 0.01 mM
0.0000002
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)benzene
Homo sapiens
-
-
0.0000002
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Homo sapiens
-
-
0.0017
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
Homo sapiens
-
effect of R1 substituent on the Ii p10 cell assay at 37°C
0.00012
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
Homo sapiens
-
effect of R1 substituent on the Ii p10 cell assay at 37°C
0.00031
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2,4-dimethyl-1,3-thiazol-5-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
Homo sapiens
-
effect of R1 substituent on the Ii p10 cell assay at 37°C
0.00015
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
Homo sapiens
-
effect of R1 substituent on the Ii p10 cell assay at 37°C
0.000062
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
Homo sapiens
-
effect of R1 substituent on the Ii p10 cell assay at 37°C
0.0014
1,4-anhydro-3-[[(2S)-2-[[(4-[[(3-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
Homo sapiens
-
effect of R1 substituent on the Ii p10 cell assay at 37°C
0.00001
1-(1'-[(2S)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]-4,4'-bipiperidin-1-yl)ethanone
Homo sapiens
-
-
0.00035
1-(1-[(2R)-3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 350 nM
0.00019
1-(1-[(2S)-3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 190 nM
0.00001
1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 10 nM
0.00005
1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 50 nM
0.00005
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 50 nM
0.00005
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 50 nM
0.00014
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 140 nM
0.00006
1-(1-[3-[3-(4-chloro-3-methylphenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 60 nM
0.0002
1-(1-[3-[3-[3-[(2-hydroxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)pyrrolidin-2-one
Homo sapiens
-
-
0.00022
1-(1-[3-[5-(methylsulfonyl)-3-[3-[(2-phenoxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)pyrrolidin-2-one
Homo sapiens
-
-
0.00008
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 80 nM
0.00011
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5,6-dichloro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 110 nM
0.00014
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methoxy-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 140 nM
0.00009
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 90 nM
0.00012
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 120 nM
0.00021
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-7-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 210 nM
0.00013
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 130 nM
0.00009
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-(2,2,2-trifluoroethyl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 90 nM
0.00014
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-butyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 140 nM
0.00031
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 310 nM
0.0005
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 500 nM
0.0001
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-tert-butyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 100 nM
0.0001
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 100 nM
0.00046
1-(1-[3-[5-acetyl-3-(4-chlorophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 460 nM
0.00012
1-(1-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 120 nM
0.00023
1-(1-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-fluoro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 230 nM
0.000565
1-(2-[[5-[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl]ethyl)piperidin-4-ol
Homo sapiens
-
-
0.00022
1-(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)-2-hydroxyethanone
Homo sapiens
-
-
0.00029
1-(4-cyclopropylpiperazin-1-yl)-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
Homo sapiens
-
-
0.00115
1-(4-methylpiperazin-1-yl)-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
Homo sapiens
-
-
0.0001
1-(ethenylideneamino)-3-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 100 nM
0.0000002
1-bromo-3-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Homo sapiens
-
-
0.0000003
1-bromo-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Homo sapiens
-
-
0.0000141
1-methyl-6-[4-(piperidin-4-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000316
1-methyl-6-[4-(piperidin-4-yloxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00002
1-methyl-6-[4-(pyridin-2-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000126
1-methyl-6-[4-(pyridin-3-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00001
1-methyl-6-[4-(pyridin-4-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000078
1-methyl-6-[4-[(3-oxopiperazin-1-yl)oxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000078
1-methyl-6-[4-[2-(2-oxopyrrolidin-1-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000011
1-methyl-6-[4-[2-(6-methylpyridin-2-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000083
1-methyl-6-[4-[2-(piperidin-4-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000095
1-methyl-6-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000028
1-methyl-6-[4-[3-(pyrrolidin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000627
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-([[1-(4-fluorophenyl)-1-methylethoxy]sulfinyl]methyl)-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
Homo sapiens
-
-
0.0000004
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(2-methylpropoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
Homo sapiens
-
-
0.0000004
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(4-fluorophenoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
Homo sapiens
-
-
0.0000005
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
Homo sapiens
-
-
0.0000003
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
Homo sapiens
-
-
0.0000003
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
Homo sapiens
-
-
0.0000005
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)methyl]-4-fluorobenzene
Homo sapiens
-
-
0.00004
1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00005
1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 50 nM
0.00201
1-[1-(3-[3-[3-([2-[benzyl(methyl)amino]ethyl]sulfanyl)-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.0001
1-[1-(3-[3-[3-[[2-(2-methylpyrrolidin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00009
1-[1-(3-[3-[3-[[2-(3-hydroxypyrrolidin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00034
1-[1-(3-[3-[3-[[2-(4-hydroxypiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00074
1-[1-(3-[3-[3-[[2-(4-methylpiperazin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00106
1-[1-(3-[3-[3-[[2-(4-methylpiperazin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00021
1-[1-(3-[3-[3-[[2-(4-methylpiperidin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00011
1-[1-(3-[3-[3-[[2-(4-methylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00016
1-[1-(3-[3-[3-[[2-(4-tert-butylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.0007
1-[1-(3-[3-[3-[[2-(benzylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00128
1-[1-(3-[3-[3-[[2-(dimethylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.0008
1-[1-(3-[3-[3-[[2-(methylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00012
1-[1-(3-[3-[3-[[3-hydroxy-2-oxo-3-(piperidin-4-yl)propyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.0002
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(4-phenylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00002
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00027
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.000055
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(octahydroisoquinolin-2(1H)-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00017
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00041
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(pyrrolidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00007
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-oxo-2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00006
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-oxo-2-(pyrrolidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00005
1-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 50 nM
0.00013
1-[1-(3-[5-acetyl-3-[4-(trifluoromethoxy)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 130 nM
0.0001
1-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 100 nM
0.00011
1-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 110 nM
0.00018
1-[1-[(2R)-3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl]-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 180 nM
0.0002
1-[1-[(2S)-3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl]-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 200 nM
0.000032
1-[2-(dimethylamino)ethyl]-6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000027
1-[3-(dimethylamino)propyl]-6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00113
1-[3-[3-[(2-aminoethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.00011
1-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidine-4-carboxamide
Homo sapiens
-
-
0.00031
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-(methylsulfanyl)ethanone
Homo sapiens
-
-
0.000235
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxyethanone
Homo sapiens
-
-
0.00047
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-methoxyethanone
Homo sapiens
-
-
0.000385
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]ethanone
Homo sapiens
-
-
0.00069
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]propan-1-one
Homo sapiens
-
-
0.0096
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.000149
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.009
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-methyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.00005
1-[3-[4-(2-cyanophenyl)piperazin-1-yl]-2-hydroxypropyl]-3-(4-iodophenyl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide
Homo sapiens
-
IC50: 50 nM
0.000058
1-[3-[4-(5-methyl-1H-indol-3-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00014
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(morpholin-4-yl)propan-2-ol
Homo sapiens
-
-
0.00038
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperazin-1-yl)propan-2-ol
Homo sapiens
-
-
0.00008
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.001035
1-[4-(2-[[5-[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl]ethyl)piperazin-1-yl]ethanone
Homo sapiens
-
-
0.00071
1-[4-(dimethylamino)piperidin-1-yl]-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
Homo sapiens
-
-
0.00008
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(3,4-dichlorobenzyl)methanamine
Homo sapiens
-
-
0.00023
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(4-methoxybenzyl)methanamine
Homo sapiens
-
-
0.00035
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(4-methylbenzyl)methanamine
Homo sapiens
-
-
0.0013
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-methylmethanamine
Homo sapiens
-
-
0.00049
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
Homo sapiens
-
-
0.00042
1-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.000325
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(morpholin-4-yl)propan-2-ol
Homo sapiens
-
-
0.000204
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.000595
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(propylamino)propan-2-ol
Homo sapiens
-
-
0.000335
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(pyrrolidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.00001
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-[4-(pyridin-2-yl)piperidin-1-yl]propan-2-ol
Homo sapiens
-
-
0.000218
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-[4-(pyrrolidin-1-yl)piperidin-1-yl]propan-2-ol
Homo sapiens
-
-
0.000712
1-[5-(methylsulfonyl)-3-[3-[[2-(pyrrolidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.02
2,3,4,5,6-pentafluoro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
Homo sapiens
-
IC50: 0.020 mM
0.001578
2-(1,1'-biphenyl-3-yl)-N-(cyanomethyl)-4-methylpentanamide
Homo sapiens
-
IC50: 1578 nM
0.003343
2-(1,1'-biphenyl-4-yl)-N-(cyanomethyl)-4-methylpentanamide
Homo sapiens
-
IC50: 3343 nM
0.00028
2-(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)-2-oxoethyl acetate
Homo sapiens
-
-
0.00012
2-(4-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperazin-1-yl)benzonitrile
Homo sapiens
-
IC50: 120 nM
0.0003
2-([5-[1-[2-hydroxy-3-[(3S)-3-methylmorpholin-4-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00001
2-([5-[1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00002
2-([5-[1-[2-hydroxy-3-[4-(3-methyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00001
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00001
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(piperidin-1-yl)ethanone
Homo sapiens
-
-
0.000001
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(pyrrolidin-1-yl)ethanone
Homo sapiens
-
-
0.000007
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-[(3R)-3-hydroxypyrrolidin-1-yl]ethanone
Homo sapiens
-
-
0.000007
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-[(3S)-3-hydroxypyrrolidin-1-yl]ethanone
Homo sapiens
-
-
0.00004
2-([5-[1-[2-hydroxy-3-[4-(pyrrolidin-1-ylcarbonyl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00001
2-([5-[1-[3-[4-(2-fluorophenyl)piperazin-1-yl]-2-hydroxypropyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.000005
2-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)-1,3-thiazolidine
Homo sapiens
-
-
0.0000013
2-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)-2,3-dihydro-1,3-benzothiazole
Homo sapiens
-
-
0.00081
2-amino-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]ethanone
Homo sapiens
-
-
0.000035
2-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
Homo sapiens
-
IC50: 35 nM
0.000006
2-cyano-4-(2-hydroxyethoxy)-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.00013
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000014
2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000022
2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000015
2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000005
2-cyano-N-methyl-4-[(spiro[3.5]non-7-ylmethyl)amino]-6-[(2,2,6,6-tetramethylpiperidin-4-yl)oxy]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000002
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000004
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.00001
2-hydroxy-1-(1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)ethanone
Homo sapiens
-
-
0.00001
2-hydroxy-1-(1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)ethanone
Homo sapiens
-
-
0.00096
2-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)sulfanyl]ethanol
Homo sapiens
-
-
0.0000007
2-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-1,3-difluorobenzene
Homo sapiens
-
-
0.0000018
2-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]biphenyl
Homo sapiens
-
-
0.00001
2-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]benzonitrile
Homo sapiens
-
-
0.00006
2-[3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00007
2-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-oxoacetamide
Homo sapiens
-
-
0.0000045
2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9-(2-hydroxyethyl)-9H-purine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000072
2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9-ethyl-9H-purine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000039
2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000023
2-[4-methoxy-3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00002
2-[5-carbamoyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-1-[[4-(2-cyanophenyl)piperazin-1-yl]methyl]ethyl carbamate
Homo sapiens
-
IC50: 20 nM
0.000016
2-[N-(3-chlorophenyl)-L-leucyl]tetrahydropyridazine-1(2H)-carbonitrile
Homo sapiens
-
-
0.000013
2-[N-(4-cyanophenyl)-L-leucyl]pyrazolidine-1-carbonitrile
Homo sapiens
-
-
0.000033
2-[N-(4-cyanophenyl)-L-phenylalanyl]pyrazolidine-1-carbonitrile
Homo sapiens
-
-
0.000035
2-[N-(4-fluorophenyl)-L-valyl]tetrahydropyridazine-1(2H)-carbonitrile
Homo sapiens
-
-
0.000019
2-[N-[3-(trifluoromethyl)phenyl]-L-isoleucyl]tetrahydropyridazine-1(2H)-carbonitrile
Homo sapiens
-
-
0.00019
2-[[5-(1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00006
2-[[5-(1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
Homo sapiens
-
-
0.00011
2-[[5-(1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00006
2-[[5-(1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
Homo sapiens
-
-
0.00015
2-[[5-(5-acetyl-1-[2-hydroxy-3-[4-(2-hydroxypropan-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
Homo sapiens
-
-
0.00002
2-[[5-(5-acetyl-1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00025
2-[[5-(5-ethyl-1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
Homo sapiens
-
-
0.00018
2-[[5-[5-acetyl-1-[2-hydroxy-3-(4-methylpiperidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
Homo sapiens
-
-
0.001373
3'-[1-[[(cyanomethy)amino]carbonyl]-3-methylbutyl]-1,1'biphenyl-4-carboxamide
Homo sapiens
-
IC50: 1373 nM
0.0079
3-(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)prop-2-yn-1-ol
Homo sapiens
-
-
0.0074
3-(4-chloro-3-ethynylphenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00087
3-(4-chloro-3-[[2-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0015
3-(4-chloro-3-[[3-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00028
3-(4-chloro-3-[[4-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.000033
3-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
Homo sapiens
-
IC50: 33 nM
0.000005
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-(naphthalen-2-ylacetyl)-L-alaninamide
Homo sapiens
-
IC50: 5.0 nM
0.0000033
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-([5-[3-(trifluoromethyl)phenyl]furan-2-yl]acetyl)-L-alaninamide
Homo sapiens
-
IC50: 3.3 nM
0.000008
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(3-phenoxyphenyl)acetyl]-L-alaninamide
Homo sapiens
-
IC50: 8.0 nM
0.000004
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(4-morpholin-4-ylphenyl)acetyl]-L-alaninamide
Homo sapiens
-
IC50: 4.0 nM
0.000017
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(4-phenoxyphenyl)acetyl]-L-alaninamide
Homo sapiens
-
IC50: 17 nM
0.000034
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(5-methyl-1-phenyl-1H-pyrazol-4-yl)acetyl]-L-alaninamide
Homo sapiens
-
IC50: 34 nM
0.000026
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[[4-(1H-1,2,4-triazol-1-yl)phenyl]acetyl]-L-alaninamide
Homo sapiens
-
IC50: 26 nM
0.000197
3-cyclohexyl-N2-(5-fluoro-1,3-benzoxazol-2-yl)-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 197 nM
0.000043
3-cyclohexyl-N2-(6-fluoro-1,3-benzoxazol-2-yl)-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 43 nM
0.000002
3-cyclohexyl-N2-([4-[(4,6-dimethylpyrimidin-2-yl)amino]phenyl]acetyl)-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 2.0 nM
0.00003
3-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,5-dimethyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 30 nM
0.00165
3-[3-(benzylsulfanyl)-4-chlorophenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.000235
3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide
Homo sapiens
-
-
0.0083
3-[4-chloro-3-(4-methylpent-1-yn-1-yl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0067
3-[4-chloro-3-(cyclohexylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.011
3-[4-chloro-3-(hept-1-yn-1-yl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00061
3-[4-chloro-3-(phenylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0036
3-[4-chloro-3-(propylsulfanyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00079
3-[4-chloro-3-(thiophen-2-ylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0015
3-[4-chloro-3-(thiophen-3-ylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00072
3-[4-chloro-3-[(2-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00055
3-[4-chloro-3-[(2-methoxyphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0011
3-[4-chloro-3-[(2-methylphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0006
3-[4-chloro-3-[(2-phenoxyethyl)sulfanyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00147
3-[4-chloro-3-[(2-phenylethyl)sulfanyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00032
3-[4-chloro-3-[(3,4-dichlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0007
3-[4-chloro-3-[(3-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0002
3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00048
3-[4-chloro-3-[(4-methoxyphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00028
3-[4-chloro-3-[(4-methylphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.000007
3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]benzamide
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000447
4-(3-acetylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000174
4-(3-bromophenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000148
4-(3-chlorophenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000063
4-(3-cyclobutylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000155
4-(3-cyclopentylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0002
4-(3-cyclopropylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000083
4-(3-ethylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00095
4-(3-methylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000191
4-(3-tert-butylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000123
4-(acetylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
Homo sapiens
-
IC50: 123 nM
0.00053
4-(dimethylamino)-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
Homo sapiens
-
-
0.000016
4-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
Homo sapiens
-
IC50: 16 nM
0.00036
4-fluoro-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
Homo sapiens
-
-
0.00039
4-hydroxy-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
Homo sapiens
-
-
0.01
4-phenyl-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00041
4-propyl-6-(3-propylphenyl)pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.01
4-propyl-6-[2-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000115
4-propyl-6-[3-(trifluoromethoxy)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000041
4-propyl-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000032
4-propyl-6-[4-(trifluoromethoxy)-3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.001259
4-propyl-6-[4-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00043
4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]aniline
Homo sapiens
-
-
0.00051
4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzoic acid
Homo sapiens
-
-
0.001925
4-[1-(2-hydroxy-3-[3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.00001
4-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.0018
4-[1-(3-[3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.00003
4-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.00012
4-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.0001
4-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.000826
4-[1-(3-[5-tert-butoxy-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.0009
4-[1-(3-[5-tert-butoxy-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.001047
4-[2-chloro-5-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000051
4-[3,5-bis(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000224
4-[3-(2-methylpropyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000093
4-[3-(methylsulfonyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000195
4-[3-(propan-2-yl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000045
4-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000058
4-[4-(propan-2-yloxy)-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000028
4-[4-chloro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000006
4-[4-ethoxy-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000013
4-[4-fluoro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000015
4-[4-methoxy-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00001
4-[4-methyl-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000013
4-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000016
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzoic acid
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000002
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]benzamide
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00074
5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-3-[3-[(2-phenoxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00081
5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.000058
5-(methylsulfonyl)-1-[3-[4-(1H-pyrrolo[3,2-c]pyridin-3-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00038
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-(piperidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00052
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-(pyrrolidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00056
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-[4-(pyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00015
5-chloro-3-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 150 nM
0.00008
5-chloro-3-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 80 nM
0.00045
6-(4-chlorobenzyl)-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000033
6-(4-chlorobenzyl)-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000021
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000099
6-(4-chlorobenzyl)-7-(2-cyclooctylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000007
6-(4-chlorobenzyl)-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000064
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000002
6-(4-chlorobenzyl)-7-(3,3-dimethylbutyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00015
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.00032
6-(4-chlorobenzyl)-7-(4,4-dimethylpentyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00011
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.00019
6-(4-chlorobenzyl)-7-[2-(3-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000019
6-(4-chlorobenzyl)-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, pyrrolopyrimidine inhibitor by modification of the P2 moieties
0.00005
6-chloro-1-(1-[3-[3-(4-chloro-3-methylphenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 50 nM
0.00006
6-chloro-1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 60 nM
0.00003
6-chloro-1-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 30 nM
0.001047
6-[3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.002884
6-[3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000071
6-[4-(2-hydroxyethoxy)-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000145
6-[4-(2-hydroxyethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000024
6-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000063
6-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000155
6-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0002
6-[4-(3-oxopropyl)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000105
6-[4-(ethylamino)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00004
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000037
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-[2-(morpholin-4-yl)ethyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000035
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-[3-(morpholin-4-yl)propyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000025
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00166
6-[4-ethoxy-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000339
6-[4-methoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000676
6-[4-phenoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000029
6-[4-[2-(2-oxopyrrolidin-1-yl)ethoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000209
6-[4-[2-(dimethylamino)ethoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000031
6-[4-[3-(2-ethyl-1H-imidazol-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000072
6-[4-[3-(4-ethylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000058
6-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000041
6-[4-[3-(dimethylamino)propoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000013
6-[[4-(1-acetyl-1,2,3,6-tetrahydropyridine-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000015
6-[[4-(1-acetylpiperidin-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000015
6-[[4-(1-acetylpiperidine-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00005
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000009
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000005
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00001
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000017
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000009
6-[[4-(4-acetylpiperazine-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00011
7-(2-cyclohexylethyl)-6-(4-methoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00014
7-(2-cyclohexylethyl)-6-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.00044
7-(2-cyclohexylethyl)-6-(naphthalen-1-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00001
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000024
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000011
7-(2-cyclohexylethyl)-6-[(pyridine-2-yloxy)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000006
7-(2-cyclohexylethyl)-6-[(pyridine-2-ylsulfanyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000052
7-(2-cyclohexylethyl)-6-[[methyl(phenyl)amino]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00046
7-tert-butyl-6-(4-chlorobenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000069
9-[3-(dimethylamino)propyl]-2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00004
benzyl [(2S)-1-(2-cyanotetrahydropyridazin-1(2H)-yl)-3-methyl-1-oxopentan-2-yl]carbamate
Homo sapiens
-
-
0.000071
ethyl (3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoate
Homo sapiens
-
IC50: 71 nM
0.0001
JNJ 10329670
Homo sapiens
-
competitive, reversible inhibition, 4-(2-keto-1-benzimidazolinyl)-piperidin-1-yl derivative, IC50: 100 nM
0.000178
L-873724
Homo sapiens
-
-
0.0000012
LHVS
Homo sapiens
-
-
0.0001
methyl (2R)-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)(phenyl)ethanoate
Homo sapiens
-
-
0.01
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-4-[(1S)-1-[(1R)-2-[(1-cyanocyclopropyl)amino]-1-(methoxysulfinyl)methyl]-2-oxoethyl]amino)-2,2,2-trifluoroethyl]-4'-fluorobiphenyl
Homo sapiens
-
-
0.002173
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfenate
Homo sapiens
-
-
0.000011
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfinate
Homo sapiens
-
-
0.0000064
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(3-fluorophenyl)ethyl]amino]propane-1-sulfinate
Homo sapiens
-
-
0.000729
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfenate
Homo sapiens
-
-
0.0000018
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfinate
Homo sapiens
-
-
0.0000025
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propane-1-sulfinate
Homo sapiens
-
-
0.00012
methyl (2S)-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)(phenyl)ethanoate
Homo sapiens
-
-
0.00004
methyl (3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(oxo)acetate
Homo sapiens
-
-
0.0017
methyl 1-[2-hydroxy-3-(4-quinolin-4-ylpiperazin-1-yl)propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000163
methyl 1-[2-hydroxy-3-[4-(2-oxo-2,3-dihydro-4,1-benzoxazepin-1(5H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000088
methyl 1-[2-hydroxy-3-[4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000048
methyl 1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000023
methyl 1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000028
methyl 1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.00008
methyl 1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.00002
methyl 1-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidine-4-carboxylate
Homo sapiens
-
-
0.000023
methyl 1-[3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000145
methyl 1-[3-[4-(5-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.00003
methyl 1-[3-[4-(6-chloro-2,2-dioxido-3,4-dihydro-1H-2,1,3-benzothiadiazin-1-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000018
methyl 1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000013
methyl 1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000016
methyl 1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.00013
methyl 1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000043
methyl 2-[[(1S)-1-(cyclohexylmethyl)-2-([2-[(4-fluorophenyl)amino]ethyl]amino)-2-oxoethyl]amino]-1,3-benzoxazole-6-carboxylate
Homo sapiens
-
IC50: 43 nM
0.000133
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000065
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000033
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000032
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000068
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.001775
methyl 3-(4-bromophenyl)-1-[3-[4-(3,4-dihydroisoquinolin-2(1H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000322
methyl 3-(4-bromophenyl)-1-[3-[4-(3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.00006
methyl 3-(4-bromophenyl)-1-[3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.0017
methyl 3-(4-bromophenyl)-1-[3-[4-(5-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000075
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2,2-dioxido-3,4-dihydro-1H-2,1,3-benzothiadiazin-1-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000033
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000018
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000048
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.00013
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000265
methyl 4'-[(1S)-1-([(1S)-1-[(1-cyanocyclopropyl)carbamoyl]pentyl]amino)-2,2,2-trifluoroethyl]biphenyl-4-sulfinate
Homo sapiens
-
-
565
morpholine-4-carboxylic acid [1-[1S-(N-benzoyl-hydrazinomethyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
Homo sapiens
-
IC50: 565 mM
0.011
morpholine-4-carboxylic acid [1R-(1S-cyano-3-phenyl-propylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 0.011 mM
0.000387
morpholine-4-carboxylic acid [1S-(1R-cyano-3-phenylpropylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 387 nM
0.107
morpholine-4-carboxylic acid [1S-(1S-cyano-2,2-dimethylpropylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 0.107 mM
0.0014
morpholine-4-carboxylic acid [1S-(1S-cyano-2-methyl-propylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 1400 nM
0.00013
morpholine-4-carboxylic acid [1S-(1S-cyano-2-phenylethylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 130 nM
0.076
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenyl-propylcarbamoyl)-1,3-dimethyl-butyl]-amide
Homo sapiens
-
IC50: 0.076 mM
5
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-cyclohexyl-ethyl]-amide
Homo sapiens
-
IC50: 5 mM
0.006
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-methyl-propyl]-amide
Homo sapiens
-
IC50: 0.006 mM
173
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-phenyl-ethyl]-amide
Homo sapiens
-
IC50: 173 mM
0.000023
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-3,3-dimethyl-butyl]-amide
Homo sapiens
-
IC50: 23 nM
0.000084
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-cyclohexyl-R-methyl]-amide
Homo sapiens
-
IC50: 84 nM
0.134
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-ethyl]-amide
Homo sapiens
-
IC50: 0.134 mM
0.000041
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-pentyl]-amide
Homo sapiens
-
IC50: 41 nM
0.000082
morpholine-4-carboxylic acid [1S-(1S-cyanobutylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 82 nM
0.000056
morpholine-4-carboxylic acid [1S-(1S-cyanobutylcarbamoyl)-3-methylpentyl]amide
Homo sapiens
-
IC50: 56 nM
0.000142
morpholine-4-carboxylic acid [1S-(1S-cyanomethylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 142 nM
0.000019
morpholine-4-carboxylic acid [1S-(2-benzyloxy-1R-cyano-ethylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 19 nM
0.000124
morpholine-4-carboxylic acid [1S-(cyanomethylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 124 nM
0.000114
morpholine-4-carboxylic acid [1S-[(1-cyano-1-methyl)ethylcarbamoyl]-3-methylbutyl]amide
Homo sapiens
-
IC50: 114 nM
0.000051
morpholine-4-carboxylic acid [1S-[(cyano-phenyl-S-methyl)carbamoyl]-3-methylbutyl]amide
Homo sapiens
-
IC50: 51 nM
0.000011
morpholine-4-carboxylic acid [1S-[1S-(benzoyl-hydrazonomethyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
Homo sapiens
-
IC50: 11 nM
0.000056
morpholine-4-carboxylic acid [1S-[1S-cyano-2-(3,4-dichlorophenyl)ethylcarbamoyl]-3-methylbutyl]amide
Homo sapiens
-
IC50: 56 nM
0.000007
morpholine-4-carboxylic acid [1S-[1S-[(2-hydroxy-benzoyl)-hydrazonomethyl]-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
Homo sapiens
-
IC50: 7 nM
0.000035
morpholine-4-carboxylic acid [1S-[1S-[(4-hydroxybenzoyl)-hydrazonomethyl]-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
Homo sapiens
-
IC50: 35 nM
0.097
morpholine-4-carboxylic acid [3-methyl-1S-(1-prop-2-ynylcarbamoyl)butyl]amide
Homo sapiens
-
IC50: 0.097 mM
0.339
morpholine-4-carboxylic acid [3-methyl-1S-(1R-methyl-3-phenylpropylcarbamoyl)butyl]amide
Homo sapiens
-
IC50 above 0.339 mM
0.028
morpholine-4-carboxylic acid [3-methyl-1S-(3-phenyl-propylcarbamoyl)butyl]amide
Homo sapiens
-
IC50 above 0.028 mM
0.00052
N,N-dimethyl-2-([5-[5-(methylsulfonyl)-1-[3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)acetamide
Homo sapiens
-
-
0.000729
N-(1-cyanocyclopropyl)-3-(methylsulfinyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
Homo sapiens
-
-
0.00001
N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-(4'-fluorobiphenyl-4-yl)ethyl]-L-alaninamide
Homo sapiens
-
-
0.0000018
N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
Homo sapiens
-
-
0.0000025
N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-phenylethyl]-L-alaninamide
Homo sapiens
-
-
0.0000002
N-(1-cyanocyclopropyl)-3-[(3,4-dichlorophenyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
Homo sapiens
-
-
0.0000005
N-(1-cyanocyclopropyl)-3-[(4-fluorobenzyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-phenylethyl]-L-alaninamide
Homo sapiens
-
-
0.0000004
N-(1-cyanocyclopropyl)-3-[(4-fluorophenyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
Homo sapiens
-
-
0.000627
N-(1-cyanocyclopropyl)-3-[[2-(4-fluorophenyl)propan-2-yl]sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
Homo sapiens
-
-
0.000265
N-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Homo sapiens
-
-
0.00014
N-(4-chlorobenzyl)-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
Homo sapiens
-
-
0.000008
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetamide
Homo sapiens
-
-
0.000008
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]phenyl)acetamide
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000012
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]phenyl)propanamide
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000922
N-(cyanomethyl)-2-[3-(1H-indol-5-yl)phenyl]-4-methylpentanamide
Homo sapiens
-
IC50: 922 nM
0.001257
N-(cyanomethyl)-2-[3-(1H-indol-6-yl)phenyl]-4-methylpentanamide
Homo sapiens
-
IC50: 1257 nM
0.01
N-(cyanomethyl)-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]-3-phenylpropanamide
Homo sapiens
-
IC50 above 0.01 mM
0.01
N-(cyanomethyl)-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]acetamide
Homo sapiens
-
IC50 above 0.01 mM
0.00231
N-(cyanomethyl)-3-cyclobutyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]propanamide
Homo sapiens
-
IC50: 2310 nM
0.006597
N-(cyanomethyl)-3-cyclopropyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]propanamide
Homo sapiens
-
IC50: 6597 nM
0.01
N-(cyanomethyl)-4-methyl-2-(2-phenyl-1,3-thiazol-4-yl)pentanamide
Homo sapiens
-
IC50 above 0.01 mM
0.01
N-(cyanomethyl)-4-methyl-2-(3'-piperazin-1-yl-1,1'-biphenyl-3-yl)pentanamide methanesulfonate
Homo sapiens
-
IC50 above 0.01 mM
0.00000001
N-(cyanomethyl)-4-methyl-2-(3-pyridin-3-ylphenyl)-pentanamide
Homo sapiens
-
IC50 above 0.01 nM
0.001748
N-(cyanomethyl)-4-methyl-2-(3-pyridin-4-ylphenyl)-pentanamide trifluoroacetate
Homo sapiens
-
IC50: 1748 nM
0.01
N-(cyanomethyl)-4-methyl-2-(3-pyrimidin-5-ylphenyl)pentanamide
Homo sapiens
-
IC50 above 0.01 mM
0.01
N-(cyanomethyl)-4-methyl-2-(5-phenylpyridin-3-yl)-pentanamide trifluoroacetate
Homo sapiens
-
IC50 above 0.01 mM
0.000521
N-(cyanomethyl)-4-methyl-2-[2'-(1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 521 nM
0.003368
N-(cyanomethyl)-4-methyl-2-[2'-(4-morpholinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 3368 nM
0.01
N-(cyanomethyl)-4-methyl-2-[3'-(4-morpholinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50 above 0.01 mM
0.000652
N-(cyanomethyl)-4-methyl-2-[4'-(1,2,3,6-tetrahydro-4-pyridinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 652 nM
0.001245
N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 1245 nM
0.001695
N-(cyanomethyl)-4-methyl-2-[4'-(4-methyl-1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 1695 nM
0.009422
N-(cyanomethyl)-4-methyl-2-[4'-(4-morpholinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 9422 nM
0.001421
N-(cyanomethyl)-4-methyl-2-[4'-(4-piperidinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 1421 nM
0.006623
N-(cyanomethyl)-4-methyl-2-[4'-(methylsulfonyl)-1,1'-biphenyl-3-yl]pentanamide
Homo sapiens
-
IC50: 6623 nM
0.0006
N-benzyl-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-methylmethanamine
Homo sapiens
-
-
0.00042
N-benzyl-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
Homo sapiens
-
-
0.00037
N-benzyl-2-([5-[5-(methylsulfonyl)-1-[3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)acetamide
Homo sapiens
-
-
0.00115
N-methyl-2-([5-[5-(methylsulfonyl)-1-[3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)acetamide
Homo sapiens
-
-
0.000029
N-[(1S)-1-(1H-indol-2-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 29 nM
0.000034
N-[(1S)-1-(biphenyl-4-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 34 nM
0.000062
N-[(1S)-1-(cyclohexylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 62 nM
0.000017
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-1-benzofuran-2-carboxamide
Homo sapiens
-
IC50: 17 nM
0.000034
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-(3-fluorophenyl)furan-2-carboxamide
Homo sapiens
-
IC50: 34 nM
0.000011
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-[3-(trifluoromethyl)phenyl]furan-2-carboxamide
Homo sapiens
-
IC50: 11 nM
0.000047
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-2-carboxamide
Homo sapiens
-
IC50: 47 nM
0.000006
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-3-carboxamide
Homo sapiens
-
IC50: 6 nM
0.000213
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-3-carboxamide
Homo sapiens
-
IC50: 213 nM
0.000011
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
Homo sapiens
-
IC50: 11 nM
0.000012
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydro-2H-pyran-4-carboxamide
Homo sapiens
-
IC50: 12 nM
0.000021
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-3-carboxamide
Homo sapiens
-
IC50: 21 nM
0.02
N-[(1S)-1-(furan-2-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 0.020 mM
0.000023
N-[(1S)-1-cyclohexyl-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 23 nM
0.000016
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-1-(naphthalen-2-ylmethyl)-2-oxoethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 16 nM
0.065
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(1,3-thiazol-5-ylmethyl)ethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 0.065 mM
0.003707
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(pyridin-3-ylmethyl)ethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 3707 nM
0.006769
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(pyridin-4-ylmethyl)ethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 6769 nM
0.000285
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-phenylethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 285 nM
0.000038
N-[(1S)-3-cyclohexyl-1-([2-[(4-methoxyphenyl)amino]ethyl]carbamoyl)propyl]-3-methylbenzamide
Homo sapiens
-
IC50: 38 nM
0.0000055
N-[(2S)-1-[[(1R)-2-(benzyloxy)-1-cyanoethyl]amino]-3-cyclohexyl-1-oxopropan-2-yl]morpholine-4-carboxamide
Homo sapiens
-
pH 6.5, 37°C
0.0000044
N-[(3S)-4-benzyloxy-3-[[[1-[(4-morpholinylcarbonyl)-amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
Homo sapiens
-
pH 6.5, 37°C
0.0000019
N-[(3S)-4-benzyloxy-3-[[[2-[(3-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
Homo sapiens
-
pH 6.5, 37°C
0.00013
N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]-2-phenylacetamide
Homo sapiens
-
-
0.00038
N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
Homo sapiens
-
-
0.00042
N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]piperidine-3-carboxamide
Homo sapiens
-
-
0.000046
N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-N2-[(3-methylphenyl)carbonyl]-L-leucinamide
Homo sapiens
-
IC50: 46 nM
0.000027
N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
Homo sapiens
-
IC50: 27 nM
0.000062
N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(3-methylphenyl)carbonyl]-L-leucinamide
Homo sapiens
-
IC50: 62 nM
0.000019
N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-4-(trifluoromethyl)-L-phenylalaninamide
Homo sapiens
-
IC50: 19 nM
0.000029
N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
Homo sapiens
-
IC50: 29 nM
0.000066
N-[2-[(4-methoxyphenyl)amino]ethyl]-O-methyl-Na-[(3-methylphenyl)carbonyl]-L-tyrosinamide
Homo sapiens
-
IC50: 66 nM
0.003236
N-[4-(4-cyano-1H-imidazo[4,5-c]pyridin-6-yl)-2-(trifluoromethyl)phenyl]formamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00019
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]-1-phenylethanamine
Homo sapiens
-
-
0.00058
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]-2-phenylethanamine
Homo sapiens
-
-
0.00035
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]benzamide
Homo sapiens
-
-
0.00016
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]benzenesulfonamide
Homo sapiens
-
-
0.000173
N2-(5-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 173 nM
0.000021
N2-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[(1S)-1-[(5-fluoro-2,3-dihydro-1H-indol-1-yl)methyl]-3-(methylsulfonyl)propyl]-L-alaninamide
Homo sapiens
-
IC50: 21 nM
0.000151
N2-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[(1S)-2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
Homo sapiens
-
IC50: 151 nM
0.000093
N2-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 93 nM
0.000026
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-(1-methyl-2-[[3-(methylsulfonyl)phenyl]amino]ethyl)-L-alaninamide
Homo sapiens
-
IC50: 26 nM
0.000011
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-(1-methyl-2-[[4-(methylsulfonyl)phenyl]amino]ethyl)-L-alaninamide
Homo sapiens
-
IC50: 11 nM
0.000015
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-2,2-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
Homo sapiens
-
IC50: 15 nM
0.000015
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
Homo sapiens
-
IC50: 15 nM
0.0000123
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-2-oxo-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
Homo sapiens
-
IC50: 12.3 nM
0.000003
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
Homo sapiens
-
IC50: 3 nM
0.000019
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 19 nM
0.000001
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]-1-methylethyl]-L-alaninamide
Homo sapiens
-
IC50: 1 nM
0.0000029
N2-(biphenyl-3-ylacetyl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 2.9 nM
0.0000091
N2-(biphenyl-4-ylacetyl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 9.1 nM
0.000026
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[(1S)-2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
Homo sapiens
-
IC50: 26 nM
0.000222
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)ethyl]-L-alaninamide
Homo sapiens
-
IC50: 222 nM
0.000094
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 94 nM
0.000029
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 29 nM
0.000005
N2-1,3-benzoxazol-2-yl-N-[(1R)-2-(benzyloxy)-1-[(5-fluoro-2,3-dihydro-1H-indol-1-yl)methyl]ethyl]-3-cyclohexyl-L-alaninamide
Homo sapiens
-
IC50: 5 nM
0.000041
N2-benzoyl-N1-(cyanomethyl)-L-leucinamide
Homo sapiens
-
IC50: 41 nM
0.0000074
N2-[(3'-chlorobiphenyl-4-yl)acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 7.4 nM
0.0000094
N2-[(5-chloro-1-benzofuran-2-yl)acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 9.4 nM
0.000049
N2-[[1-(5-bromopyrimidin-2-yl)piperidin-3-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 49 nM
0.000107
N2-[[1-(5-bromopyrimidin-2-yl)piperidin-4-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 107 nM
0.0000071
N2-[[5-(4-chlorophenyl)furan-2-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 7.1 nM
0.000021
paecilopeptin
Homo sapiens
-
i.e. acetyl-Leu-Val-CHO, IC50: 21 nM
0.00073
tert-butyl (3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoate
Homo sapiens
-
IC50: 730 nM
0.00001
tert-butyl 1'-[(2S)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]-4,4'-bipiperidine-1-carboxylate
Homo sapiens
-
-
0.001298
tert-butyl 4-[3'-[1-[[(cyanomethyl)amino]carbonyl]-3-methylbutyl]-1,1'-biphenyl-4-yl]piperazine-1-carboxylate
Homo sapiens
-
IC50: 1298 nM
0.00015
tert-butyl 4-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperazine-1-carboxylate
Homo sapiens
-
-
0.000004
tert-butyl [(2S)-1-(2-cyanopyrazolidin-1-yl)-1-oxo-3-phenylpropan-2-yl]carbamate
Homo sapiens
-
-
0.000023
tert-butyl [(2S)-1-(2-cyanopyrazolidin-1-yl)-3-methyl-1-oxobutan-2-yl]carbamate
Homo sapiens
-
-
0.000003
tert-butyl [(2S)-1-(2-cyanopyrazolidin-1-yl)-4-methyl-1-oxopentan-2-yl]carbamate
Homo sapiens
-
-
0.000004
tert-butyl [(2S)-1-(2-cyanotetrahydropyridazin-1(2H)-yl)-3-methyl-1-oxobutan-2-yl]carbamate
Homo sapiens
-
-
0.000012
tetrahydro-2H-pyran-4-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
Homo sapiens
-
IC50: 12 nM
0.0000006
[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]benzene
Homo sapiens
-
-
0.00009
[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl](pyrrolidin-1-yl)methanone
Homo sapiens
-
-
0.000042
[1S-(1S-cyano-3-phenylpropylcarbamoyl)-3-methylbutyl]-amide
Homo sapiens
-
IC50: 42 nM
0.02
[1S-(2-cyano-1S-phenethyl-ethylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50 above 0.02 mM
0.000205
[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl](1H-1,2,4-triazol-3-yl)methanone
Homo sapiens
-
-
0.00119
[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl](pyrrolidin-1-yl)methanone
Homo sapiens
-
-
0.000355
[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl](thiophen-2-yl)methanone
Homo sapiens
-
-
additional information
2-cyano-4-[(6,8-dioxaspiro[3.5]non-7-ylmethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
0.000002
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000002
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000021
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000021
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000064
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000064
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00015
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00015
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00011
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00011
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00014
7-(2-cyclohexylethyl)-6-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00014
7-(2-cyclohexylethyl)-6-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00001
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00001
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000024
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000024
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
2-cyano-4-[(6,8-dioxaspiro[3.5]non-7-ylmethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
Homo sapiens
IC50 is above 0.001 mM, determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 is below 0.001 M, inhibition is determined by a fluorometric assay with recombinant Cat S
additional information
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 is below 0.001 M, inhibition is determined by a fluorometric assay with recombinant Cat S
additional information
N-benzyl-2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 is below 0.001 M, inhibition is determined by a fluorometric assay with recombinant Cat S
additional information
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 is below 0.001 M, inhibition is determined by a fluorometric assay with recombinant Cat S
additional information
(2R)-N-(1-benzyl-4-cyanopiperidin-4-yl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 207 - 347 nM
additional information
(2R)-N-(1-cyanocyclopropyl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 135 - 154 nM
additional information
(2R)-N-(4-cyano-1-methylpiperidin-4-yl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 251 - 641 nM
additional information
(2R)-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 37 - 63 nM
additional information
(2R)-N-[(3R)-3-cyano-1-(propan-2-yl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 66 - 82 nM
additional information
(2R)-N-[(3R)-3-cyano-1-cycloheptylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 23 - 35 nM
additional information
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 23 - 49 nM
additional information
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(1-methylcyclohexyl)methyl]-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 47 - 62 nM
additional information
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(4-methylcyclohexyl)methyl]-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 14 - 17 nM
additional information
(2R)-N-[(3R)-3-cyano-1-cyclopentylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 75 -78 nM
additional information
(2R)-N-[(3R)-3-cyano-1-methylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 155 - 172 nM
additional information
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methylpyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
Homo sapiens
-
IC50 above 20 microM, effect of R1 substituent on the Ii p10 cell assay at 37°C
additional information
2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
-
IC50: below 1 nM
additional information
6-(4-chlorobenzyl)-7-(2-piperidine-1-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
Chlorella powder
Homo sapiens
-
chlorella powder inhibits peptidase cathepsin S in a dose-concentration manner with 50% inhibitory concentration of 3.46 mg/l
-
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Schick, C.; Pemberton, P.A.; Shi, G.P.; Kamachi, Y.; Cataltepe, S.; Bartuski, A.J.; Gornstein, E.R.; Brmme, D.; Chapman, H.A.; Silverman, G.A.
Cross-class inhibition of the cysteine proteinases cathepsins K, L, and S by the serpin squamous cell carcinoma antigen I: a kinetic analysis
Biochemistry
37
5258-5266
1998
Homo sapiens
brenda
Baker, S.M.; Karlsson, L.; Thurmond, R.L.
Cloning, expression, purification, and activity of dog (Canis familiaris) and monkey (Saimiri boliviensis) cathepsin S
Protein Expr. Purif.
28
93-101
2003
Bos taurus, Canis lupus familiaris, Homo sapiens, Mus musculus, Saimiri boliviensis
brenda
Bania, J.; Gatti, E.; Lelouard, H.; David, A.; Cappello, F.; Weber, E.; Camosseto, V.; Pierre, P.
Human cathepsin S, but not cathepsin L, degrades efficiently MHC class II-associated invariant chain in nonprofessional APCs
Proc. Natl. Acad. Sci. USA
100
6664-6669
2003
Homo sapiens
brenda
Cywin, C.L.; Firestone, R.A.; McNeil, D.W.; Grygon, C.A.; Crane, K.M.; White, D.M.; Kinkade, P.R.; Hopkins, J.L.; Davidson, W.; Labadia, M.E.; Wildeson, J.; Morelock, M.M.; Peterson, J.D.; Raymond, E.L.; Brown, M.L.; Spero, D.M.
The design of potent hydrazones and disulfides as cathepsin S inhibitors
Bioorg. Med. Chem.
11
733-740
2003
Homo sapiens
brenda
Dahl, S.W.; Halkier, T.; Lauritzen, C.; Dolenc, I.; Pedersen, J.; Turk, V.; Turk, B.
Human recombinant Pro-dipeptidyl peptidase I (cathepsin C) can be activated by cathepsins L and S but not by autocatalytic processing
Biochemistry
40
1671-1678
2001
Homo sapiens
brenda
Walker, B.; Lynas, J.F.; Meighan, M.A.; Bromme, D.
Evaluation of dipeptide alpha-keto-beta-aldehydes as new inhibitors of cathepsin S
Biochem. Biophys. Res. Commun.
275
401-405
2000
Homo sapiens
brenda
Katunuma, N.; Murata, E.; Kakegawa, H.; Matsui, A.; Tsuzuki, H.; Tsuge, H.; Turk, D.; Turk, V.; Fukushima, M.; Tada, Y.; Asao, T.
Structure based development of novel specific inhibitors for cathepsin L and cathepsin S in vitro and in vivo
FEBS Lett.
458
6-10
1999
Homo sapiens
brenda
Marquis, R.W.; Ru, Y.; LoCastro, S.M.; Zeng, J.; et al.
Azepanone-based Inhibitors of human and rat cathepsin K
J. Med. Chem.
44
1380-1395
2001
Homo sapiens
brenda
Guo, Y.L.; Kurz, U.; Schultz, J.E.; Lim, C.C.; Wiederanders, B.; Schilling, K.
The a 1/2 helical backbone of the prodomains defines the intrinsic inhibitory specificity in the cathepsin L-like cysteine protease subfamily
FEBS Lett.
469
203-207
2000
Homo sapiens
brenda
Katunuma, N.; Matsui, A.; Kakegawa, T.; Murata, E.; Asao, T.; Ohba, Y.
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Homo sapiens, Mus musculus, Rattus norvegicus
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Homo sapiens (P25774), Homo sapiens
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Identification of internal autoproteolytic cleavage sites within the prosegments of recombinant procathepsin B and procathepsin S. Contribution of a plausible unimolecular autoproteolytic event for the processing of zymogens belonging to the papain family
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Homo sapiens
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Homo sapiens
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Bos taurus, Canis lupus familiaris, Homo sapiens, Platyrrhini, Mus musculus
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Homo sapiens
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Homo sapiens
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Homo sapiens
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Homo sapiens
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Homo sapiens
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Potent inactivation of cathepsins S and L by peptidyl (acyloxy)methyl ketones
Biol. Chem. Hoppe-Seyler
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Homo sapiens
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Gour-Salin, B.J.; Lachance, P.; Bonneau, P.R.; Storer, A.C.; Kirschke, H.; Broemme, D.
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Homo sapiens
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Cheng, X.W.; Kuzuya, M.; Nakamura, K.; Di, Q.; Liu, Z.; Sasaki, T.; Kanda, S.; Jin, H.; Shi, G.P.; Murohara, T.; Yokota, M.; Iguchi, A.
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Homo sapiens
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Increased serum cathepsin S in patients with atherosclerosis and diabetes
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Homo sapiens
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Homo sapiens
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Liu, H.; Tully, D.C.; Epple, R.; Bursulaya, B.; Li, J.; Harris, J.L.; Williams, J.A.; Russo, R.; Tumanut, C.; Roberts, M.J.; Alper, P.B.; He, Y.; Karanewsky, D.S.
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Homo sapiens
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Bioorg. Med. Chem. Lett.
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Homo sapiens
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Cysteine protease cathepsin S as a key step in antigen presentation
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Bos taurus, Homo sapiens, Mus musculus, Rattus norvegicus
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Taleb, S.; Lacasa, D.; Bastard, J.P.; Poitou, C.; Cancello, R.; Pelloux, V.; Viguerie, N.; Benis, A.; Zucker, J.D.; Bouillot, J.L.; Coussieu, C.; Basdevant, A.; Langin, D.; Clement, K.
Cathepsin S, a novel biomarker of adiposity: relevance to atherogenesis
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2005
Homo sapiens
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Recombinant human procathepsin S is capable of autocatalytic processing at neutral pH in the presence of glycosaminoglycans
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2005
Homo sapiens
brenda
Wang, B.; Sun, J.; Kitamoto, S.; Yang, M.; Grubb, A.; Chapman, H.A.; Kalluri, R.; Shi, G.P.
Cathepsin S controls angiogenesis and tumor growth via matrix-derived angiogenic factors
J. Biol. Chem.
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Homo sapiens, Mus musculus, Mus musculus C57BL/6
brenda
Rodgers, K.J.; Watkins, D.J.; Miller, A.L.; Chan, P.Y.; Karanam, S.; Brissette, W.H.; Long, C.J.; Jackson, C.L.
Destabilizing role of cathepsin S in murine atherosclerotic plaques
Arterioscler. Thromb. Vasc. Biol.
26
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2006
Homo sapiens, Mus musculus
brenda
Rueckrich, T.; Brandenburg, J.; Cansier, A.; Mueller, M.; Stevanovic, S.; Schilling, K.; Wiederanders, B.; Beck, A.; Melms, A.; Reich, M.; Driessen, C.; Kalbacher, H.
Specificity of human cathepsin S determined by processing of peptide substrates and MHC class II-associated invariant chain
Biol. Chem.
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2006
Homo sapiens (P25774), Homo sapiens
brenda
Grice, C.A.; Tays, K.; Khatuya, H.; Gustin, D.J.; Butler, C.R.; Wei, J.; Sehon, C.A.; Sun, S.; Gu, Y.; Jiang, W.; Thurmond, R.L.; Karlsson, L.; Edwards, J.P.
The SAR of 4-substituted (6,6-bicyclic) piperidine cathepsin S inhibitors
Bioorg. Med. Chem. Lett.
16
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2006
Homo sapiens
brenda
Bekkali, Y.; Thomson, D.S.; Betageri, R.; Emmanuel, M.J.; Hao, M.H.; Hickey, E.; Liu, W.; Patel, U.; Ward, Y.D.; Young, E.R.; Nelson, R.; Kukulka, A.; Brown, M.L.; Crane, K.; White, D.; Freeman, D.M.; Labadia, M.E.; Wildeson, J.; Spero, D.M.
Identification of a novel class of succinyl-nitrile-based cathepsin S inhibitors
Bioorg. Med. Chem. Lett.
17
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2007
Homo sapiens
brenda
Chatterjee, A.K.; Liu, H.; Tully, D.C.; Guo, J.; Epple, R.; Russo, R.; Williams, J.; Roberts, M.; Tuntland, T.; Chang, J.; Gordon, P.; Hollenbeck, T.; Tumanut, C.; Li, J.; Harris, J.L.
Synthesis and SAR of succinamide peptidomimetic inhibitors of cathepsin S
Bioorg. Med. Chem. Lett.
17
2899-2903
2007
Homo sapiens
brenda
Gauthier, J.Y.; Black, W.C.; Courchesne, I.; Cromlish, W.; Desmarais, S.; Houle, R.; Lamontagne, S.; Li, C.S.; Masse, F.; McKay, D.J.; Ouellet, M.; Robichaud, J.; Truchon, J.F.; Truong, V.L.; Wang, Q.; Percival, M.D.
The identification of potent, selective, and bioavailable cathepsin S inhibitors
Bioorg. Med. Chem. Lett.
17
4929-4933
2007
Homo sapiens, Mus musculus, Rattus norvegicus
brenda
Gupta, S.; Singh, R.K.; Dastidar, S.; Ray, A.
Cysteine cathepsin S as an immunomodulatory target: present and future trends
Expert Opin. Ther. Targets
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2008
Homo sapiens
brenda
Flannery, T.; McQuaid, S.; McGoohan, C.; McConnell, R.S.; McGregor, G.; Mirakhur, M.; Hamilton, P.; Diamond, J.; Cran, G.; Walker, B.; Scott, C.; Martin, L.; Ellison, D.; Patel, C.; Nicholson, C.; Mendelow, D.; McCormick, D.; Johnston, P.G.
Cathepsin S expression: An independent prognostic factor in glioblastoma tumours - A pilot study
Int. J. Cancer
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854-860
2006
Homo sapiens
brenda
Novinec, M.; Grass, R.N.; Stark, W.J.; Turk, V.; Baici, A.; Lenarcic, B.
Interaction between human cathepsins K, L, and S and elastins: mechanism of elastinolysis and inhibition by macromolecular inhibitors
J. Biol. Chem.
282
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2007
Homo sapiens
brenda
Chang, W.W.; Wu, H.; Yeh, C.; Wu, C.; Chang, J.
Lysosomal cysteine proteinase cathepsin S as a potential target for anti-cancer therapy
J. Cancer Mol.
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2007
Homo sapiens
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Patterson, A.W.; Wood, W.J.; Hornsby, M.; Lesley, S.; Spraggon, G.; Ellman, J.A.
Identification of selective, nonpeptidic nitrile inhibitors of cathepsin S using the substrate activity screening method
J. Med. Chem.
49
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2006
Homo sapiens
brenda
Burden, R.E.; Snoddy, P.; Buick, R.J.; Johnston, J.A.; Walker, B.; Scott, C.J.
Recombinant cathepsin S propeptide attenuates cell invasion by inhibition of cathepsin L-like proteases in tumor microenvironment
Mol. Cancer Ther.
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2008
Homo sapiens
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Kramer, G.; Paul, A.; Kreusch, A.; Schueler, S.; Wiederanders, B.; Schilling, K.
Optimized folding and activation of recombinant procathepsin L and S produced in Escherichia coli
Protein Expr. Purif.
54
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2007
Homo sapiens (P25774)
brenda
Cheng, F.C.; Feng, J.J.; Chen, K.H.; Imanishi, H.; Fujishima, M.; Takekoshi, H.; Naoki, Y.; Shimoda, M.
Chlorella powder inhibits the activities of peptidase cathepsin S, PLA2, cyclooxygenase-2, thromboxane synthase, tyrosine phosphatases, tumor necrosis factor-alpha converting enzyme, calpain and kinases
Int. J. Food Sci. Nutr.
60 Suppl 1
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2008
Homo sapiens
brenda
Irie, O.; Ehara, T.; Iwasaki, A.; Yokokawa, F.; Sakaki, J.; Hirao, H.; Kanazawa, T.; Teno, N.; Horiuchi, M.; Umemura, I.; Gunji, H.; Masuya, K.; Hitomi, Y.; Iwasaki, G.; Nonomura, K.; Tanabe, K.; Fukaya, H.; Kosaka, T.; Snell, C.R.; Hallett, A.
Discovery of selective and nonpeptidic cathepsin S inhibitors
Bioorg. Med. Chem. Lett.
18
3959-3962
2008
Homo sapiens
brenda
Irie, O.; Yokokawa, F.; Ehara, T.; Iwasaki, A.; Iwaki, Y.; Hitomi, Y.; Konishi, K.; Kishida, M.; Toyao, A.; Masuya, K.; Gunji, H.; Sakaki, J.; Iwasaki, G.; Hirao, H.; Kanazawa, T.; Tanabe, K.; Kosaka, T.; Hart, T.W.; Hallett, A.
4-Amino-2-cyanopyrimidines: novel scaffold for nonpeptidic cathepsin S inhibitors
Bioorg. Med. Chem. Lett.
18
4642-4646
2008
Homo sapiens (P25774)
brenda
Irie, O.; Kosaka, T.; Kishida, M.; Sakaki, J.; Masuya, K.; Konishi, K.; Yokokawa, F.; Ehara, T.; Iwasaki, A.; Iwaki, Y.; Hitomi, Y.; Toyao, A.; Gunji, H.; Teno, N.; Iwasaki, G.; Hirao, H.; Kanazawa, T.; Tanabe, K.; Hiestand, P.C.; Malcangio, M.; Fox, A.J.; Bevan, S.J.; Yaqoob, M.; Culshaw, A.J.; Hart, T.W.; Hallet, A.
Overcoming hERG issues for brain-penetrating cathepsin S inhibitors: 2-cyanopyrimidines. Part 2
Bioorg. Med. Chem. Lett.
18
5280-5284
2008
Homo sapiens (P25774)
brenda
Ayesa, S.; Lindquist, C.; Agback, T.; Benkestock, K.; Classon, B.; Henderson, I.; Hewitt, E.; Jansson, K.; Kallin, A.; Sheppard, D.; Samuelsson, B.
Solid-phase parallel synthesis and SAR of 4-amidofuran-3-one inhibitors of cathepsin S: effect of sulfonamides P3 substituents on potency and selectivity
Bioorg. Med. Chem.
17
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2009
Homo sapiens
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Spielmann, N.; Mutch, D.M.; Rousseau, F.; Tores, F.; Hager, J.; Bertrais, S.; Basdevant, A.; Tounian, P.; Dubern, B.; Galan, P.; Clement, K.
Cathepsin S genotypes are associated with Apo-A1 and HDL-cholesterol in lean and obese French populations
Clin. Genet.
74
155-163
2008
Homo sapiens (P25774), Homo sapiens
brenda
Seo, H.R.; Bae, S.; Lee, Y.S.
Radiation-induced cathepsin S is involved in radioresistance
Int. J. Cancer
124
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2009
Homo sapiens
brenda
Luetzner, N.; Kalbacher, H.
Quantifying cathepsin S activity in antigen presenting cells using a novel specific substrate
J. Biol. Chem.
283
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2008
Homo sapiens
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Markt, P.; McGoohan, C.; Walker, B.; Kirchmair, J.; Feldmann, C.; De Martino, G.; Spitzer, G.; Distinto, S.; Schuster, D.; Wolber, G.; Laggner, C.; Langer, T.
Discovery of novel cathepsin S inhibitors by pharmacophore-based virtual high-throughput screening
J. Chem. Inf. Model.
48
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2008
Homo sapiens
brenda
Irie, O.; Kosaka, T.; Ehara, T.; Yokokawa, F.; Kanazawa, T.; Hirao, H.; Iwasaki, A.; Sakaki, J.; Teno, N.; Hitomi, Y.; Iwasaki, G.; Fukaya, H.; Nonomura, K.; Tanabe, K.; Koizumi, S.; Uchiyama, N.; Bevan, S.J.; Malcangio, M.; Gentry, C.; Fox, A.J.; Yaqoob, M.; Culshaw, A.J.; Allan Hallett, A.J.
Discovery of orally bioavailable cathepsin S inhibitors for the reversal of neuropathic pain
J. Med. Chem.
51
5502-5505
2008
Homo sapiens, Mus musculus, Rattus norvegicus (Q02765)
brenda
Minematsu, N.; Nakamura, H.; Furuuchi, M.; Nakajima, T.; Takahashi, S.; Tsujimura, S.; Tateno, H.; Ishizaka, A.
Common functional polymorphisms in the cathepsin S promoter in Japanese subjects: possible contribution to pulmonary emphysema
Respirology
13
498-504
2008
Homo sapiens (P25774), Homo sapiens
brenda
Coppini, L.P.; Barros, N.M.; Oliveira, M.; Hirata, I.Y.; Alves, M.F.; Paschoalin, T.; Assis, D.M.; Juliano, M.A.; Puzer, L.; Broemme, D.; Carmona, A.K.
Plasminogen hydrolysis by cathepsin S and identification of derived peptides as selective substrate for cathepsin V and cathepsin L inhibitor
Biol. Chem.
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2010
Homo sapiens
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Ameriks, M.K.; Axe, F.U.; Bembenek, S.D.; Edwards, J.P.; Gu, Y.; Karlsson, L.; Randal, M.; Sun, S.; Thurmond, R.L.; Zhu, J.
Pyrazole-based cathepsin S inhibitors with arylalkynes as P1 binding elements
Bioorg. Med. Chem. Lett.
19
6131-6134
2009
Homo sapiens, Mus musculus
brenda
Ameriks, M.K.; Cai, H.; Edwards, J.P.; Gebauer, D.; Gleason, E.; Gu, Y.; Karlsson, L.; Nguyen, S.; Sun, S.; Thurmond, R.L.; Zhu, J.
Pyrazole-based arylalkyne cathepsin S inhibitors. Part II: optimization of cellular potency
Bioorg. Med. Chem. Lett.
19
6135-6139
2009
Homo sapiens
brenda
Lee-Dutra, A.; Wiener, D.K.; Arienti, K.L.; Liu, J.; Mani, N.; Ameriks, M.K.; Axe, F.U.; Gebauer, D.; Desai, P.J.; Nguyen, S.; Randal, M.; Thurmond, R.L.; Sun, S.; Karlsson, L.; Edwards, J.P.; Jones, T.K.; Grice, C.A.
Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors: part 1
Bioorg. Med. Chem. Lett.
20
2370-2374
2010
Homo sapiens
brenda
Wiener, J.J.; Wickboldt, A.T.; Wiener, D.K.; Lee-Dutra, A.; Edwards, J.P.; Karlsson, L.; Nguyen, S.; Sun, S.; Jones, T.K.; Grice, C.A.
Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors. Part 2: Modification of P3, P4, and P5 regions
Bioorg. Med. Chem. Lett.
20
2375-2378
2010
Homo sapiens
brenda
Wiener, D.K.; Lee-Dutra, A.; Bembenek, S.; Nguyen, S.; Thurmond, R.L.; Sun, S.; Karlsson, L.; Grice, C.A.; Jones, T.K.; Edwards, J.P.
Thioether acetamides as P3 binding elements for tetrahydropyrido-pyrazole cathepsin S inhibitors
Bioorg. Med. Chem. Lett.
20
2379-2382
2010
Homo sapiens
brenda
Li, J.; Petrassi, H.; Tumanut, C.; Masick, B.; Trussell, C.; Harris, J.
Substrate optimization for monitoring cathepsin C activity in live cells
Bioorg. Med. Chem.
17
1064-1070
2009
Homo sapiens
brenda
Gu, F.F.; Lue, S.Z.; Chen, Y.D.; Zhou, Y.J.; Song, X.T.; Jin, Z.N.; Liu, H.
Relationship between plasma cathepsin S and cystatin C levels and coronary plaque morphology of mild to moderate lesions: an in vivo study using intravascular ultrasound
Chin. Med. Sci.
122
2820-2826
2009
Homo sapiens
brenda
Burden, R.E.; Gormley, J.A.; Jaquin, T.J.; Small, D.M.; Quinn, D.J.; Hegarty, S.M.; Ward, C.; Walker, B.; Johnston, J.A.; Olwill, S.A.; Scott, C.J.
Antibody-mediated inhibition of cathepsin S blocks colorectal tumor invasion and angiogenesis
Clin. Cancer Res.
15
6042-6051
2009
Homo sapiens
brenda
Wiener, J.J.; Sun, S.; Thurmond, R.L.
Recent advances in the design of cathepsin S inhibitors
Curr. Top. Med. Chem.
10
717-732
2010
Homo sapiens
brenda
Schoenefuss, A.; Wendt, W.; Schattling, B.; Schulten, R.; Hoffmann, K.; Stuecker, M.; Tigges, C.; Luebbert, H.; Stichel, C.
Upregulation of cathepsin S in psoriatic keratinocytes
Exp. Dermatol.
19
e80-e88
2009
Homo sapiens
brenda
Paraoan, L.; Gray, D.; Hiscott, P.; Garcia-Finana, M.; Lane, B.; Damato, B.; Grierson, I.
Cathepsin S and its inhibitor cystatin C: imbalance in uveal melanoma
Front. Biosci.
14
2504-2513
2009
Homo sapiens
brenda
Costantino, C.M.; Ploegh, H.L.; Hafler, D.A.
Cathepsin S regulates class II MHC processing in human CD4+ HLA-DR+ T cells
J. Immunol.
183
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2009
Homo sapiens
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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
J. Med. Chem.
53
4545-4549
2010
Homo sapiens
brenda
Lorenz, J.C.; Busacca, C.A.; Feng, X.; Grinberg, N.; Haddad, N.; Johnson, J.; Kapadia, S.; Lee, H.; Saha, A.; Sarvestani, M.; Spinelli, E.M.; Varsolona, R.; Wei, X.; Zeng, X.; Senanayake, C.H.
Large-scale asymmetric synthesis of a cathepsin S inhibitor
J. Org. Chem.
75
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2010
Homo sapiens
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Deng, X.; Liang, J.T.; Peterson, M.; Rynberg, R.; Cheung, E.; Mani, N.S.
Practical synthesis of a Cathepsin S inhibitor: route identification, purification strategies, and serendipitous discovery of a crystalline salt form
J. Org. Chem.
75
1940-1947
2010
Homo sapiens
brenda
Oliveira, M.; Torquato, R.J.; Alves, M.F.; Juliano, M.A.; Broemme, D.; Barros, N.M.; Carmona, A.K.
Improvement of cathepsin S detection using a designed FRET peptide based on putative natural substrates
Peptides
31
562-567
2010
Homo sapiens
brenda
Wilder, C.L.; Park, K.Y.; Keegan, P.M.; Platt, M.O.
Manipulating substrate and pH in zymography protocols selectively distinguishes cathepsins K, L, S, and V activity in cells and tissues
Arch. Biochem. Biophys.
516
52-57
2011
Homo sapiens
brenda
Cai, J.; Baugh, M.; Black, D.; Long, C.; Jonathan Bennett, D.; Dempster, M.; Fradera, X.; Gillespie, J.; Andrews, F.; Boucharens, S.; Bruin, J.; Cameron, K.S.; Cumming, I.; Hamilton, W.; Jones, P.S.; Kaptein, A.; Kinghorn, E.; Maidment, M.; Martin, I.; Mitchell, A.; Rankovic, Z.; Robinson, J.; Scullion, P.; Uitdehaag, J.C.; Vink, P.; Westwood, P.; van Zeeland, M.; van Berkom, L.; Bastiani, M.; Meulemans, T.
6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors
Bioorg. Med. Chem. Lett.
20
4350-4354
2010
Homo sapiens
brenda
Cai, J.; Bennett, D.J.; Rankovic, Z.; Dempster, M.; Fradera, X.; Gillespie, J.; Cumming, I.; Finlay, W.; Baugh, M.; Boucharens, S.; Bruin, J.; Cameron, K.S.; Hamilton, W.; Kerr, J.; Kinghorn, E.; McGarry, G.; Robinson, J.; Scullion, P.; Uitdehaag, J.C.; van Zeeland, M.; Potin, D.; Saniere, L.; Fouquet, A.; Chevallier, F.; Deronzier, H.; Dorleans, C.; Nicolai, E.
2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors
Bioorg. Med. Chem. Lett.
20
4447-4450
2010
Homo sapiens
brenda
Cai, J.; Fradera, X.; van Zeeland, M.; Dempster, M.; Cameron, K.S.; Bennett, D.J.; Robinson, J.; Popplestone, L.; Baugh, M.; Westwood, P.; Bruin, J.; Hamilton, W.; Kinghorn, E.; Long, C.; Uitdehaag, J.C.
4-(3-Trifluoromethylphenyl)-pyrimidine-2-carbonitrile as cathepsin S inhibitors: N3, not N1 is critically important
Bioorg. Med. Chem. Lett.
20
4507-4510
2010
Homo sapiens
brenda
Hamm-Alvarez, S.; Janga, S.; Edman, M.; Madrigal, S.; Shah, M.; Frousiakis, S.; Renduchintala, K.; Zhu, J.; Bricel, S.; Silka, K.; Bach, D.; Heur, M.; Christianakis, S.; Arkfeld, D.; Irvine, J.; Mack, W.; Stohl, W.
Tear cathepsin s as a candidate biomarker for sjgrens syndrome
Arthritis Rheumatol.
66
1872-1881
2014
Homo sapiens (P25774), Homo sapiens
brenda
Fonovic, U.P.; Jevnikar, Z.; Kos, J.
Cathepsin S generates soluble CX3CL1 (fractalkine) in vascular smooth muscle cells
Biol. Chem.
394
1349-1352
2013
Homo sapiens (P25774)
brenda
Kim. M.; Jeon. J.; Song. J.; Suh. K.H.; Kim. Y.H.; Min. K.H.; Lee. K.O.
Synthesis of proline analogues as potent and selective cathepsin S inhibitors
Bioorg. Med. Chem. Lett.
23
3140-3144
2013
Homo sapiens (P25774)
brenda
Li, X.; Cheng, X.W.; Hu, L.; Wu, H.; Guo-Ping, H.; Hao, C.N.; Jiang, H.; Zhu, E.; Huang, Z.; Inoue, A.; Sasaki, T.; Du, Q.; Takeshita, K.; Okumura, K.; Murohara, T.; Kuzuya, M.
Cathepsin S activity controls ischemia-induced neovascularization in mice
Int. J. Cardiol.
183
198-208
2015
Mus musculus (O70370), Homo sapiens (P25774), Homo sapiens
brenda
Barry, Z.T.; Platt, M.O.
Cathepsin S cannibalism of cathepsin K as a mechanism to reduce type I collagen degradation
J. Biol. Chem.
287
27723-27730
2012
Homo sapiens (P25774)
brenda
Klinngam, W.; Fu, R.; Janga, S.R.; Edman, M.C.; Hamm-Alvarez, S.F.
Cathepsin S alters the expression of pro-inflammatory cytokines and MMP-9, partially through protease-activated receptor-2, in human corneal epithelial cells
Int. J. Mol. Sci.
19
E3530
2018
Homo sapiens (P25774), Homo sapiens
brenda
Kumar Vr, S.; Darisipudi, M.N.; Steiger, S.; Devarapu, S.K.; Tato, M.; Kukarni, O.P.; Mulay, S.R.; Thomasova, D.; Popper, B.; Demleitner, J.; Zuchtriegel, G.; Reichel, C.; Cohen, C.D.; Lindenmeyer, M.T.; Liapis, H.; Moll, S.; Reid, E.; Stitt, A.W.; Schott, B.; Gruner, S.; Haap, W.; Ebeling, M.; Hartmann, G.
Cathepsin S cleavage of protease-activated receptor-2 on endothelial cells promotes microvascular diabetes complications
J. Am. Soc. Nephrol.
27
1635-1649
2016
Mus musculus (O70370), Mus musculus, Homo sapiens (P25774), Homo sapiens
brenda