3.4.22.27 (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 - 79815 3.4.22.27 (2R)-2-(2-cyclohexylethyl)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide - 63962 3.4.22.27 (2R)-2-(2-cyclopentylethyl)-4-morpholin-4-yl-4-oxo-N-[(1S)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide - 63963 3.4.22.27 (2R)-2-(2-cyclopentylethyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide - 63964 3.4.22.27 (2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)butanamide - 63965 3.4.22.27 (2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)butyl]butanamide - 63966 3.4.22.27 (2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide - 63967 3.4.22.27 (2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-phenyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]butanamide - 63968 3.4.22.27 (2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide - 63969 3.4.22.27 (2R)-2-(cyclohexylmethyl)-N-[(1R)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide - 63970 3.4.22.27 (2R)-2-(cyclohexylmethyl)-N-[(1R)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide - 63971 3.4.22.27 (2R)-2-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide - 63972 3.4.22.27 (2R)-2-(cyclopentylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1S)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)butyl]butanamide - 63973 3.4.22.27 (2R)-2-(cyclopentylmethyl)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide - 63974 3.4.22.27 (2R)-2-(cyclopentylmethyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide - 63975 3.4.22.27 (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 - 79822 3.4.22.27 (2R)-2-benzyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide - 63976 3.4.22.27 (2R)-2-[4'-(1-azabicyclo[2.2.2]oct-4-yl)-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide IC50: 1991 nM 52017 3.4.22.27 (2R)-2-[4'-(4-tert-butylpiperazin-1-yl)-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide IC50: 8340 nM 52018 3.4.22.27 (2R)-2-[4'-[1-(2-amino-2-methylpropyl)piperidin-4-yl]-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide IC50: 1427 nM 52019 3.4.22.27 (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-N-(1-cyanocyclopropyl)-3-(methylsulfanyl)propanamide - 63977 3.4.22.27 (2R)-4-dimethyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-2-(2-morpholin-4-yl-2-oxoethyl)pentanamide - 66550 3.4.22.27 (2R)-4-morpholin-4-yl-4-oxo-2-(2-phenylethyl)-N-[(1S)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide - 63984 3.4.22.27 (2R)-5-dimethyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-2-(2-morpholin-4-yl-2-oxoethyl)hexanamide - 66551 3.4.22.27 (2R)-N-(1-benzyl-4-cyanopiperidin-4-yl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide - 79792 3.4.22.27 (2R)-N-(1-cyanocyclopropyl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide - 79825 3.4.22.27 (2R)-N-(1-cyanocyclopropyl)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide - 64058 3.4.22.27 (2R)-N-(4-cyano-1-methylpiperidin-4-yl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide - 79826 3.4.22.27 (2R)-N-(cyanomethyl)-2-[4'-[4-(2-hydroxy-2-methylpropyl)-1-piperazinyl][1,1'-biphenyl]-3-yl]-4-methylpentanamide IC50 above 0.01 mM 52020 3.4.22.27 (2R)-N-(cyanomethyl)-2-[4'-[4-(2-hydroxyethyl)-1-piperazinyl][1,1'-biphenyl]-3-yl]-4-methylpentanamide IC50: 609 nM 52021 3.4.22.27 (2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)-[1,1'-biphenyl]-3-yl]pentanamide IC50: 2010 nM 16967 3.4.22.27 (2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1H-tetraazol-5-yl)-1,1'-biphenyl-3-yl]pentanamide IC50 above 0.01 mM 52022 3.4.22.27 (2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methyl-1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide IC50: 3931 nM 52023 3.4.22.27 (2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-pyrimidinyl)[1,1'-biphenyl]-3-yl]pentanamide IC50: 1365 nM 52024 3.4.22.27 (2R)-N-(cyanomethyl)-4-methyl-2-[4'-[4-(2-oxopropyl)-piperazin-1-yl]-1,1'-biphenyl-3-yl]pentanamide IC50: 2364 nM 52025 3.4.22.27 (2R)-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide - 79827 3.4.22.27 (2R)-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide - 64059 3.4.22.27 (2R)-N-[(1R)-2-[(4-chlorobenzyl)oxy]-1-cyanoethyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide - 64060 3.4.22.27 (2R)-N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-2-carboxamide IC50: 658 nM 59815 3.4.22.27 (2R)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide IC50: 18 nM 23879 3.4.22.27 (2R)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide - 23879 3.4.22.27 (2R)-N-[(1S)-1-cyano-3-phenylpropyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide - 64061 3.4.22.27 (2R)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-2-(2-morpholin-4-yl-2-oxoethyl)-5-phenylpentanamide - 64062 3.4.22.27 (2R)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-(2-phenylethyl)butanamide - 64063 3.4.22.27 (2R)-N-[(3R)-1-benzyl-3-cyanopiperidin-4-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide - 64064 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-(1-methylethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide - 64065 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-(2-methylpropyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide - 64066 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-(2-phenylethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide - 64067 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-(cyclopropylmethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide - 64068 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-(propan-2-yl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide - 79968 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-cycloheptylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide - 79791 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-cycloheptylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide - 64069 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(2,3-dihydro-1H-inden-2-ylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide - 79828 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(2,3-dihydro-1H-inden-2-ylmethyl)-4-morpholin-4-yl-4-oxobutanamide - 64070 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide - 79793 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide - 64071 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclopentylmethyl)-4-morpholin-4-yl-4-oxobutanamide - 64072 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(1-methylcyclohexyl)methyl]-4-(morpholin-4-yl)-4-oxobutanamide - 79768 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(1-methylcyclohexyl)methyl]-4-morpholin-4-yl-4-oxobutanamide - 64073 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(4-methylcyclohexyl)methyl]-4-(morpholin-4-yl)-4-oxobutanamide - 79789 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(4-methylcyclohexyl)methyl]-4-morpholin-4-yl-4-oxobutanamide - 64074 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-(morpholin-4-yl)-4-oxo-2-(1,2,3,4-tetrahydronaphthalen-2-ylmethyl)butanamide - 79790 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-(morpholin-4-yl)-4-oxo-2-[(4-phenylcyclohexyl)methyl]butanamide - 79795 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-morpholin-4-yl-4-oxo-2-(1,2,3,4-tetrahydronaphthalen-2-ylmethyl)butanamide - 64075 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-morpholin-4-yl-4-oxo-2-[(4-phenylcyclohexyl)methyl]butanamide - 64076 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-cyclopentylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide - 79389 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-cyclopentylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide - 64077 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-methylpiperidin-4-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide - 64078 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-methylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide - 79796 3.4.22.27 (2R)-N-[(3R)-3-cyano-1-methylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide - 64079 3.4.22.27 (2R)-N-[(3R)-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide - 79794 3.4.22.27 (2R)-N-[(3R)-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide - 64080 3.4.22.27 (2R)-N-[(3S)-1-benzyl-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide - 64081 3.4.22.27 (2R)-N-[(3S)-3-cyano-1-(cyclohexylmethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide - 64082 3.4.22.27 (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 - 79782 3.4.22.27 (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 - 79336 3.4.22.27 (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 - 79898 3.4.22.27 (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 - 79808 3.4.22.27 (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 - 79861 3.4.22.27 (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 - 79799 3.4.22.27 (2S)-2-(4-chlorophenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide - 64127 3.4.22.27 (2S)-2-(4-fluorophenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide - 64128 3.4.22.27 (2S)-2-(4-methoxyphenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide - 64129 3.4.22.27 (2S)-2-(4-methylphenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide - 64130 3.4.22.27 (2S)-2-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide - 64136 3.4.22.27 (2S)-2-amino-N-[(1S)-2-(biphenyl-4-yl)-1-cyanoethyl]butanamide - 7042 3.4.22.27 (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 - 79872 3.4.22.27 (2S)-4-morpholin-4-yl-4-oxo-2-phenyl-N-[(1S)-1-phenyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]butanamide - 64159 3.4.22.27 (2S)-4-morpholin-4-yl-4-oxo-2-phenyl-N-[(1S)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide - 64160 3.4.22.27 (2S)-4-morpholin-4-yl-4-oxo-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)-2-[4-(trifluoromethyl)phenyl]butanamide - 64161 3.4.22.27 (2S)-N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-2-carboxamide - 64163 3.4.22.27 (2S)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide IC50: 53 nM 23880 3.4.22.27 (2S)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide - 23880 3.4.22.27 (2S)-N-[(1S)-1-cyclopropyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide - 64164 3.4.22.27 (2S)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide - 64165 3.4.22.27 (2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-phenylbutanamide - 64166 3.4.22.27 (2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[2-(trifluoromethyl)phenyl]butanamide - 64167 3.4.22.27 (2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[3-(trifluoromethyl)phenyl]butanamide - 64168 3.4.22.27 (2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide - 64169 3.4.22.27 (2S)-N-[(2S)-3-methyl-1-[[4-(trifluoromethoxy)phenyl]amino]butan-2-yl]-4-(morpholin-4-yl)-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide - 79448 3.4.22.27 (2Z)-3-(4-[[5-(3,5-dimethylisoxazol-4-yl)-1,2,4-oxadiazol-3-yl]methoxy]phenyl)-2-(methylsulfonyl)prop-2-enenitrile - 72737 3.4.22.27 (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 - 79869 3.4.22.27 (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 - 79866 3.4.22.27 (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 - 79990 3.4.22.27 (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 75391 3.4.22.27 (3R)-3-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide - 64319 3.4.22.27 (3R)-tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate IC50: 42 nM 59817 3.4.22.27 (3S)-3-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide - 64428 3.4.22.27 (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 59812 3.4.22.27 (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 23872 3.4.22.27 (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 - 23872 3.4.22.27 (3S)-N-[2-(1H-indol-3-yl)ethyl]-3-[[(4-methylphenyl)sulfonyl]amino]-2-oxo-4-phenylbutanamide - 72771 3.4.22.27 (3S)-tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate IC50: 49 nM 59816 3.4.22.27 (4R)-1-acetyl-N-[(2R)-1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide - 204648 3.4.22.27 (4R)-1-acetyl-N-[(2S)-1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide - 204649 3.4.22.27 (4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxo-3-phenylpropan-2-yl]-4-(phenylsulfonyl)-L-prolinamide - 204650 3.4.22.27 (4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(ethylsulfonyl)-L-prolinamide - 204651 3.4.22.27 (4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfanyl)-L-prolinamide - 204652 3.4.22.27 (4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfinyl)-L-prolinamide - 204653 3.4.22.27 (4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide - 204654 3.4.22.27 (4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-phenoxy-L-prolinamide - 204655 3.4.22.27 (4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[(2-chlorophenyl)sulfonyl]-L-prolinamide - 204656 3.4.22.27 (4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[(4-fluorophenyl)sulfonyl]-L-prolinamide - 204657 3.4.22.27 (4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[[4-(1H-pyrazol-1-yl)phenyl]sulfonyl]-L-prolinamide - 204658 3.4.22.27 (4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxopropan-2-yl]-4-(phenylsulfonyl)-L-prolinamide - 204659 3.4.22.27 (4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-3-methyl-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide - 204660 3.4.22.27 (4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(2-methylpropanoyl)-4-(phenylsulfonyl)-L-prolinamide - 204661 3.4.22.27 (4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(2-oxopropyl)-4-(phenylsulfonyl)-L-prolinamide - 204662 3.4.22.27 (4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(3-chlorobenzoyl)-4-(phenylsulfonyl)-L-prolinamide - 204663 3.4.22.27 (4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(3-methoxypropanoyl)-4-(phenylsulfonyl)-L-prolinamide - 204664 3.4.22.27 (4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(4-chlorobenzoyl)-4-(phenylsulfonyl)-L-prolinamide - 204665 3.4.22.27 (4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(biphenyl-4-ylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide - 204666 3.4.22.27 (4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(cyclohexylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide - 204667 3.4.22.27 (4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(methylsulfinyl)-4-(phenylsulfonyl)-L-prolinamide - 204668 3.4.22.27 (4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-benzoyl-4-(phenylsulfonyl)-L-prolinamide - 204669 3.4.22.27 (4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-phenyl-4-(phenylsulfonyl)-L-prolinamide - 204670 3.4.22.27 (4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyridin-3-ylcarbonyl)-L-prolinamide - 204671 3.4.22.27 (4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyridin-4-ylcarbonyl)-L-prolinamide - 204672 3.4.22.27 (4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyrrolidin-1-ylcarbonyl)-L-prolinamide - 204673 3.4.22.27 (4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(trifluoroacetyl)-L-prolinamide - 204674 3.4.22.27 (4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-propanoyl-L-prolinamide - 204675 3.4.22.27 (4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide - 204676 3.4.22.27 (4R)-N-[2-(1,3-benzoxazol-2-yl)-2-oxoethyl]-1-(cyclohexylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide - 204677 3.4.22.27 (4S)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]hexanamide IC50 above 0.01 mM 52044 3.4.22.27 (S)-[1-[1-cyano-pyrrolidin-3(R)-ylcarbamoyl]-3-methyl-butyl]-carbamic acid benzyl ester - 52064 3.4.22.27 (S)-[1-[1-cyano-pyrrolidin-3(S)-ylcarbamoyl]-3-methyl-butyl]-carbamic acid benzyl ester - 52065 3.4.22.27 1,1-bis(cyanomethyl)-3-[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]urea - 72864 3.4.22.27 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 - 64513 3.4.22.27 1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene - 14140 3.4.22.27 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 - 79685 3.4.22.27 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 - 14495 3.4.22.27 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 - 14496 3.4.22.27 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 - 14497 3.4.22.27 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 - 14498 3.4.22.27 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 - 11954 3.4.22.27 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 - 11955 3.4.22.27 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 - 14499 3.4.22.27 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 - 14500 3.4.22.27 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 - 14501 3.4.22.27 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 - 14502 3.4.22.27 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 - 14503 3.4.22.27 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 - 14504 3.4.22.27 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 - 14505 3.4.22.27 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 - 79777 3.4.22.27 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 - 14506 3.4.22.27 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) - 79640 3.4.22.27 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 - 79767 3.4.22.27 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 - 79871 3.4.22.27 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 - 14507 3.4.22.27 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 - 14508 3.4.22.27 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 - 14509 3.4.22.27 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 - 14510 3.4.22.27 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 - 11956 3.4.22.27 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 - 14511 3.4.22.27 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 - 11957 3.4.22.27 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 - 11958 3.4.22.27 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 - 14512 3.4.22.27 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 - 14513 3.4.22.27 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 - 79764 3.4.22.27 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 - 79428 3.4.22.27 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 - 79769 3.4.22.27 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 - 79770 3.4.22.27 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 - 14514 3.4.22.27 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 - 14515 3.4.22.27 1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-sulfamoylphenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose - 14516 3.4.22.27 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 - 14517 3.4.22.27 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 - 14518 3.4.22.27 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 - 14519 3.4.22.27 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 - 14520 3.4.22.27 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 - 14521 3.4.22.27 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 - 11959 3.4.22.27 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 - 14522 3.4.22.27 1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[4-(methylsulfamoyl)benzoyl]amino]propanoyl]amino]-L-erythro-hex-2-ulose - 79500 3.4.22.27 1,4-anhydro-3,5,6-trideoxy-3-[[4-methyl-N-(thiophen-3-ylcarbonyl)-L-leucyl]amino]-L-erythro-hex-2-ulose - 159247 3.4.22.27 1,4-anhydro-3,5,6-trideoxy-3-[[4-methyl-N-(thiophen-3-ylcarbonyl)-L-leucyl]amino]-L-glycero-hex-2-ulose - 14523 3.4.22.27 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 - 79783 3.4.22.27 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 - 79727 3.4.22.27 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 - 14524 3.4.22.27 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 - 14525 3.4.22.27 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 - 14526 3.4.22.27 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 - 14527 3.4.22.27 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 - 14528 3.4.22.27 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 - 14529 3.4.22.27 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 - 14530 3.4.22.27 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 - 11960 3.4.22.27 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 - 14531 3.4.22.27 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 - 14532 3.4.22.27 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 - 79830 3.4.22.27 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 59745 3.4.22.27 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 59744 3.4.22.27 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 59748 3.4.22.27 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 35722 3.4.22.27 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 - 35722 3.4.22.27 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 59741 3.4.22.27 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 59751 3.4.22.27 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 59753 3.4.22.27 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 59737 3.4.22.27 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 - 80063 3.4.22.27 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 - 79714 3.4.22.27 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 59722 3.4.22.27 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 59733 3.4.22.27 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 59734 3.4.22.27 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 59736 3.4.22.27 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 59732 3.4.22.27 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 59735 3.4.22.27 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 59719 3.4.22.27 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 59728 3.4.22.27 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 59726 3.4.22.27 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 59725 3.4.22.27 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 59724 3.4.22.27 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 59727 3.4.22.27 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 59730 3.4.22.27 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 59718 3.4.22.27 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 59721 3.4.22.27 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 59731 3.4.22.27 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 - 79686 3.4.22.27 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 - 79779 3.4.22.27 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 - 79750 3.4.22.27 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 - 79420 3.4.22.27 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 59752 3.4.22.27 1-bromo-3-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene - 14141 3.4.22.27 1-bromo-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene - 14142 3.4.22.27 1-cyano-(3,4-didehydro)-Pro-Leu methyl ester - 52152 3.4.22.27 1-cyano-(D)-Pro-(D)-Leu methyl ester - 52153 3.4.22.27 1-cyano-(D)-Pro-Ala methyl ester - 52154 3.4.22.27 1-cyano-(D)-Pro-Leu benzyl ester - 52155 3.4.22.27 1-cyano-(D)-Pro-Leu benzylamide - 52156 3.4.22.27 1-cyano-(D)-Pro-Leu dimethylamide - 52157 3.4.22.27 1-cyano-(D)-Pro-Leu methyl ester - 52158 3.4.22.27 1-cyano-(trans-benzyloxy)prolylleucine methyl ester - 52159 3.4.22.27 1-cyano-(trans-hydroxy)-Pro-Leu methyl ester - 52160 3.4.22.27 1-cyano-Pro isoamylamide - 52161 3.4.22.27 1-cyano-Pro-(D)-Leu methyl ester - 52162 3.4.22.27 1-cyano-Pro-Ala methyl ester - 52163 3.4.22.27 1-cyano-Pro-Leu benzyl ester - 52164 3.4.22.27 1-cyano-Pro-Leu methyl ester - 52165 3.4.22.27 1-cyano-Pro-Leu-Gly ethyl ester - 52166 3.4.22.27 1-cyano-Pro-Leu-Leu-Leu methyl ester - 52167 3.4.22.27 1-cyano-Pro-Phe methyl ester - 52168 3.4.22.27 1-formyl-(D)-Pro-Leu benzyl ester - 114741 3.4.22.27 1-iminomethyl-(D)-Pro-Leu benzyl ester - 114746 3.4.22.27 1-methyl-6-[4-(piperidin-4-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86472 3.4.22.27 1-methyl-6-[4-(piperidin-4-yloxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86471 3.4.22.27 1-methyl-6-[4-(pyridin-2-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86466 3.4.22.27 1-methyl-6-[4-(pyridin-3-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86467 3.4.22.27 1-methyl-6-[4-(pyridin-4-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86468 3.4.22.27 1-methyl-6-[4-[(3-oxopiperazin-1-yl)oxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86475 3.4.22.27 1-methyl-6-[4-[2-(2-oxopyrrolidin-1-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86470 3.4.22.27 1-methyl-6-[4-[2-(6-methylpyridin-2-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86469 3.4.22.27 1-methyl-6-[4-[2-(piperidin-4-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86473 3.4.22.27 1-methyl-6-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86478 3.4.22.27 1-methyl-6-[4-[3-(pyrrolidin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86477 3.4.22.27 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 - 64549 3.4.22.27 1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(2-methylpropoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene - 64550 3.4.22.27 1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(4-fluorophenoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene - 64551 3.4.22.27 1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene - 14143 3.4.22.27 1-[(3R)-4-(methylsulfonyl)-2-oxo-3-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]butyl]cyclopropanecarbonitrile - 159111 3.4.22.27 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 - 14144 3.4.22.27 1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene - 64558 3.4.22.27 1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)methyl]-4-fluorobenzene - 64559 3.4.22.27 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 - 79740 3.4.22.27 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 59739 3.4.22.27 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 - 79908 3.4.22.27 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 - 79746 3.4.22.27 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 - 79747 3.4.22.27 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 - 79626 3.4.22.27 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 - 79397 3.4.22.27 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 - 79781 3.4.22.27 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 - 79732 3.4.22.27 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 - 79733 3.4.22.27 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 - 79547 3.4.22.27 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 - 79729 3.4.22.27 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 - 79493 3.4.22.27 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 - 79736 3.4.22.27 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 - 79907 3.4.22.27 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 - 79738 3.4.22.27 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 - 79734 3.4.22.27 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 - 79735 3.4.22.27 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 - 79991 3.4.22.27 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 - 27398 3.4.22.27 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 - 79349 3.4.22.27 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 - 79748 3.4.22.27 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 - 80014 3.4.22.27 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 59750 3.4.22.27 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 59720 3.4.22.27 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 59723 3.4.22.27 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 59729 3.4.22.27 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 59747 3.4.22.27 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 59746 3.4.22.27 1-[2-(dimethylamino)ethyl]-6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86460 3.4.22.27 1-[3-(dimethylamino)propyl]-6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86462 3.4.22.27 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 - 80009 3.4.22.27 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 - 79506 3.4.22.27 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 - 80010 3.4.22.27 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 - 80050 3.4.22.27 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 - 80025 3.4.22.27 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 - 80026 3.4.22.27 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 - 80020 3.4.22.27 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 - 79868 3.4.22.27 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 - 80024 3.4.22.27 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 - 79498 3.4.22.27 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 59717 3.4.22.27 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 - 79462 3.4.22.27 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 - 80027 3.4.22.27 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 - 80028 3.4.22.27 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 - 80029 3.4.22.27 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 - 80021 3.4.22.27 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 - 80018 3.4.22.27 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 - 79337 3.4.22.27 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 - 80022 3.4.22.27 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 - 80023 3.4.22.27 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 - 79350 3.4.22.27 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 - 79521 3.4.22.27 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 - 79890 3.4.22.27 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 - 80051 3.4.22.27 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 - 79983 3.4.22.27 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 - 79987 3.4.22.27 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 - 79904 3.4.22.27 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 - 79566 3.4.22.27 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 - 79811 3.4.22.27 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 - 79986 3.4.22.27 2,2'-[[3-(trifluoromethyl)phenyl]imino]bis[N-(4-methylphenyl)acetamide] - 72952 3.4.22.27 2,3,4,5,6-pentafluoro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide IC50: 0.020 mM 59776 3.4.22.27 2-(1,1'-biphenyl-3-yl)-N-(cyanomethyl)-4-methylpentanamide IC50: 1578 nM 52197 3.4.22.27 2-(1,1'-biphenyl-4-yl)-N-(cyanomethyl)-4-methylpentanamide IC50: 3343 nM 52198 3.4.22.27 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 - 80060 3.4.22.27 2-(4-tert-butylphenyl)-5-[[2-(3,4-dimethoxyphenyl)ethyl]amino]-1,3-oxazole-4-carbonitrile - 73009 3.4.22.27 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 59716 3.4.22.27 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 - 79544 3.4.22.27 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 - 79997 3.4.22.27 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 - 79998 3.4.22.27 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 - 79850 3.4.22.27 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 - 79741 3.4.22.27 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 - 79994 3.4.22.27 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 - 79995 3.4.22.27 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 - 79996 3.4.22.27 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 - 79884 3.4.22.27 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 - 80068 3.4.22.27 2-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)-1,3-thiazolidine - 64615 3.4.22.27 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 - 64616 3.4.22.27 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 - 79569 3.4.22.27 2-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide IC50: 35 nM 59764 3.4.22.27 2-cyano-4-(2-hydroxyethoxy)-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide brain-penetrating cathepsin S inhibitors 14534 3.4.22.27 2-cyano-4-(2-hydroxyethoxy)-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide - 14534 3.4.22.27 2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide - 7721 3.4.22.27 2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide - 10189 3.4.22.27 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 26125 3.4.22.27 2-cyano-4-[(2-cyclopentylethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide brain-penetrating cathepsin S inhibitors 26126 3.4.22.27 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 26127 3.4.22.27 2-cyano-4-[(cyclohexylmethyl)(methyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide - 14535 3.4.22.27 2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide - 10190 3.4.22.27 2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide - 10191 3.4.22.27 2-cyano-4-[[(4,4-difluorocyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide - 14675 3.4.22.27 2-cyano-4-[[(4,4-dimethylcyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide - 14676 3.4.22.27 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 26673 3.4.22.27 2-cyano-N-(1-methyl-4-phenylpiperidin-4-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide - 14536 3.4.22.27 2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide - 10192 3.4.22.27 2-cyano-N-(4,5-dimethoxybiphenyl-2-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide - 14537 3.4.22.27 2-cyano-N-methyl-4-(piperidin-4-ylmethoxy)-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide brain-penetrating cathepsin S inhibitors 25844 3.4.22.27 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 26054 3.4.22.27 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 26128 3.4.22.27 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 14538 3.4.22.27 2-cyano-N-methyl-4-[(spiro[3.5]non-7-ylmethyl)amino]-6-[(2,2,6,6-tetramethylpiperidin-4-yl)oxy]pyrimidine-5-carboxamide - 14538 3.4.22.27 2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide - 6328 3.4.22.27 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 6328 3.4.22.27 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 14539 3.4.22.27 2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide - 14539 3.4.22.27 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 26672 3.4.22.27 2-cyano-N-[(1-methyl-4-phenylpiperidin-4-yl)methyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide - 14491 3.4.22.27 2-cyano-N-[(1R)-2-pyridin-2-yl-1-(pyrrolidin-1-ylmethyl)ethyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide - 14540 3.4.22.27 2-cyano-N-[5-[(1-methylpiperidin-4-yl)oxy]biphenyl-2-yl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide - 14677 3.4.22.27 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 - 80059 3.4.22.27 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 - 79581 3.4.22.27 2-hydroxy-N'-[1H-indol-3-yl(oxo)acetyl]-2,2-diphenylacetohydrazide - 73051 3.4.22.27 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 - 79568 3.4.22.27 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 - 64624 3.4.22.27 2-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]biphenyl - 64625 3.4.22.27 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 - 80041 3.4.22.27 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 - 159349 3.4.22.27 2-[3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile - 86497 3.4.22.27 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 - 79416 3.4.22.27 2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9-(2-hydroxyethyl)-9H-purine-6-carbonitrile - 86501 3.4.22.27 2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9-ethyl-9H-purine-6-carbonitrile - 86500 3.4.22.27 2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile - 86499 3.4.22.27 2-[4-methoxy-3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile - 86498 3.4.22.27 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 59715 3.4.22.27 2-[N-(3-chlorophenyl)-L-leucyl]tetrahydropyridazine-1(2H)-carbonitrile - 80036 3.4.22.27 2-[N-(4-cyanophenyl)-L-leucyl]pyrazolidine-1-carbonitrile - 80037 3.4.22.27 2-[N-(4-cyanophenyl)-L-phenylalanyl]pyrazolidine-1-carbonitrile - 79960 3.4.22.27 2-[N-(4-fluorophenyl)-L-valyl]tetrahydropyridazine-1(2H)-carbonitrile - 80034 3.4.22.27 2-[N-[3-(trifluoromethyl)phenyl]-L-isoleucyl]tetrahydropyridazine-1(2H)-carbonitrile - 80055 3.4.22.27 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 - 80040 3.4.22.27 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 - 80031 3.4.22.27 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 - 80038 3.4.22.27 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 - 79618 3.4.22.27 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 - 80043 3.4.22.27 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 - 80044 3.4.22.27 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 - 80045 3.4.22.27 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 - 79505 3.4.22.27 2-{[3-(4-chloro-5-hydroxy-2-methoxyphenyl)-4-oxo-3,4-dihydroquinazolin-2-yl]sulfanyl}-N-[(1S)-1-cyano-1,2-dimethylpropyl]acetamide - 151611 3.4.22.27 3'-[1-[[(cyanomethy)amino]carbonyl]-3-methylbutyl]-1,1'biphenyl-4-carboxamide IC50: 1373 nM 52227 3.4.22.27 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 - 79982 3.4.22.27 3-(4-chloro-3-ethynylphenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine - 79916 3.4.22.27 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 - 79922 3.4.22.27 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 - 79365 3.4.22.27 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 - 79923 3.4.22.27 3-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide IC50: 33 nM 59763 3.4.22.27 3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-(naphthalen-2-ylacetyl)-L-alaninamide IC50: 5.0 nM 59777 3.4.22.27 3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-([5-[3-(trifluoromethyl)phenyl]furan-2-yl]acetyl)-L-alaninamide IC50: 3.3 nM 59791 3.4.22.27 3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(3-phenoxyphenyl)acetyl]-L-alaninamide IC50: 8.0 nM 59782 3.4.22.27 3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(4-morpholin-4-ylphenyl)acetyl]-L-alaninamide IC50: 4.0 nM 59784 3.4.22.27 3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(4-phenoxyphenyl)acetyl]-L-alaninamide IC50: 17 nM 59783 3.4.22.27 3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(5-methyl-1-phenyl-1H-pyrazol-4-yl)acetyl]-L-alaninamide IC50: 34 nM 59789 3.4.22.27 3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[[4-(1H-1,2,4-triazol-1-yl)phenyl]acetyl]-L-alaninamide IC50: 26 nM 59785 3.4.22.27 3-cyclohexyl-N2-(5-fluoro-1,3-benzoxazol-2-yl)-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide IC50: 197 nM 59794 3.4.22.27 3-cyclohexyl-N2-(6-fluoro-1,3-benzoxazol-2-yl)-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide IC50: 43 nM 59795 3.4.22.27 3-cyclohexyl-N2-([4-[(4,6-dimethylpyrimidin-2-yl)amino]phenyl]acetyl)-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide IC50: 2.0 nM 59786 3.4.22.27 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 59742 3.4.22.27 3-[3-(benzylsulfanyl)-4-chlorophenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine - 79419 3.4.22.27 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 - 79893 3.4.22.27 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 - 79891 3.4.22.27 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 - 79892 3.4.22.27 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 - 79895 3.4.22.27 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 - 79610 3.4.22.27 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 - 79897 3.4.22.27 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 - 79414 3.4.22.27 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 - 79925 3.4.22.27 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 - 79721 3.4.22.27 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 - 79906 3.4.22.27 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 - 79737 3.4.22.27 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 - 79901 3.4.22.27 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 - 79574 3.4.22.27 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 - 79905 3.4.22.27 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 - 79911 3.4.22.27 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 - 27390 3.4.22.27 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 - 79949 3.4.22.27 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 - 79745 3.4.22.27 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 - 14541 3.4.22.27 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 - 14542 3.4.22.27 3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]benzamide pyrrolopyrimidine inhibitor by modification of the P3 moieties 75392 3.4.22.27 4-(3-acetylphenyl)-6-propylpyrimidine-2-carbonitrile - 86482 3.4.22.27 4-(3-bromophenyl)-6-propylpyrimidine-2-carbonitrile - 86481 3.4.22.27 4-(3-chlorophenyl)-6-propylpyrimidine-2-carbonitrile - 86480 3.4.22.27 4-(3-cyclobutylphenyl)-6-propylpyrimidine-2-carbonitrile - 86489 3.4.22.27 4-(3-cyclopentylphenyl)-6-propylpyrimidine-2-carbonitrile - 27582 3.4.22.27 4-(3-cyclopropylphenyl)-6-propylpyrimidine-2-carbonitrile - 86488 3.4.22.27 4-(3-ethylphenyl)-6-propylpyrimidine-2-carbonitrile - 86483 3.4.22.27 4-(3-methylphenyl)-6-propylpyrimidine-2-carbonitrile - 27584 3.4.22.27 4-(3-tert-butylphenyl)-6-propylpyrimidine-2-carbonitrile - 27581 3.4.22.27 4-(acetylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide IC50: 123 nM 59768 3.4.22.27 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 - 79943 3.4.22.27 4-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide IC50: 16 nM 59762 3.4.22.27 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 - 79711 3.4.22.27 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 - 79454 3.4.22.27 4-methyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-N2-(morpholin-4-ylcarbonyl)-L-leucinamide - 64670 3.4.22.27 4-methyl-N2-(morpholin-4-ylcarbonyl)-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)-L-leucinamide - 64671 3.4.22.27 4-morpholinecarbonyl-Phe-(S-benzyl)Cys-PSI(CHO) - 114994 3.4.22.27 4-morpholinecarboxamide, N-[(1R)-2-[[(1S)-1-(2-benzoxazolylcarbonyl) propyl] amino]-1-[[(cyclopropylmethyl)-sulfonyl]methyl]-2-oxoethyl] previously reported as 05141, ihbitor-dosed mice are protected against ozone-induced airway hyperresponsiveness 75386 3.4.22.27 4-phenyl-6-propylpyrimidine-2-carbonitrile - 27577 3.4.22.27 4-propyl-6-(3-propylphenyl)pyrimidine-2-carbonitrile - 86484 3.4.22.27 4-propyl-6-[2-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile - 27578 3.4.22.27 4-propyl-6-[3-(trifluoromethoxy)phenyl]pyrimidine-2-carbonitrile - 86487 3.4.22.27 4-propyl-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile - 27576 3.4.22.27 4-propyl-6-[4-(trifluoromethoxy)-3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile - 86495 3.4.22.27 4-propyl-6-[4-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile - 27579 3.4.22.27 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 26135 3.4.22.27 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 - 79681 3.4.22.27 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 - 79533 3.4.22.27 4-[(4-[(E)-[(cyanoacetyl)hydrazono]methyl]phenoxy)methyl]benzoic acid - 71131 3.4.22.27 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 - 64708 3.4.22.27 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 - 79524 3.4.22.27 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 - 64709 3.4.22.27 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 - 79946 3.4.22.27 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 - 64710 3.4.22.27 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 - 64711 3.4.22.27 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 - 64712 3.4.22.27 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 - 64713 3.4.22.27 4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile - 14492 3.4.22.27 4-[2-chloro-5-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile - 86491 3.4.22.27 4-[3,5-bis(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile - 86490 3.4.22.27 4-[3-(2-methylpropyl)phenyl]-6-propylpyrimidine-2-carbonitrile - 86486 3.4.22.27 4-[3-(methylsulfonyl)phenyl]-6-propylpyrimidine-2-carbonitrile - 27583 3.4.22.27 4-[3-(propan-2-yl)phenyl]-6-propylpyrimidine-2-carbonitrile - 86485 3.4.22.27 4-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile - 86503 3.4.22.27 4-[4-(propan-2-yloxy)-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile - 86496 3.4.22.27 4-[4-chloro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile - 27580 3.4.22.27 4-[4-ethoxy-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile - 28578 3.4.22.27 4-[4-fluoro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile - 86492 3.4.22.27 4-[4-methoxy-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile - 86494 3.4.22.27 4-[4-methyl-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile - 86493 3.4.22.27 4-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile - 86504 3.4.22.27 4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]benzamide pyrrolopyrimidine inhibitor by modification of the P3 moieties 75393 3.4.22.27 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 151612 3.4.22.27 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 - 79429 3.4.22.27 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 - 79433 3.4.22.27 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 - 79434 3.4.22.27 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 - 79845 3.4.22.27 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 - 79430 3.4.22.27 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 - 79878 3.4.22.27 5-bromo-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile - 14543 3.4.22.27 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 59754 3.4.22.27 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 59743 3.4.22.27 6-(4-chlorobenzyl)-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile pyrrolopyrimidine inhibitor by modification of the P2 moieties 14545 3.4.22.27 6-(4-chlorobenzyl)-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile pyrrolopyrimidine inhibitor by modification of the P2 moieties 10193 3.4.22.27 6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile pyrrolopyrimidine inhibitor by modification of the P2 moieties 7789 3.4.22.27 6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile - 7789 3.4.22.27 6-(4-chlorobenzyl)-7-(2-cyclooctylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile pyrrolopyrimidine inhibitor by modification of the P2 moieties 10194 3.4.22.27 6-(4-chlorobenzyl)-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile pyrrolopyrimidine inhibitor by modification of the P2 moieties 10195 3.4.22.27 6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile pyrrolopyrimidine inhibitor by modification of the P2 moieties 7790 3.4.22.27 6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile - 7790 3.4.22.27 6-(4-chlorobenzyl)-7-(2-piperidine-1-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile pyrrolopyrimidine inhibitor by modification of the P2 moieties 75388 3.4.22.27 6-(4-chlorobenzyl)-7-(3,3-dimethylbutyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile pyrrolopyrimidine inhibitor by modification of the P2 moieties 14546 3.4.22.27 6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile pyrrolopyrimidine inhibitor by modification of the P2 moieties 7791 3.4.22.27 6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile - 7791 3.4.22.27 6-(4-chlorobenzyl)-7-(4,4-dimethylpentyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile pyrrolopyrimidine inhibitor by modification of the P2 moieties 14547 3.4.22.27 6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile pyrrolopyrimidine inhibitor by modification of the P2 moieties 7792 3.4.22.27 6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile - 7792 3.4.22.27 6-(4-chlorobenzyl)-7-[2-(3-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile pyrrolopyrimidine inhibitor by modification of the P2 moieties 10196 3.4.22.27 6-(4-chlorobenzyl)-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile pyrrolopyrimidine inhibitor by modification of the P2 moieties 10197 3.4.22.27 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 59738 3.4.22.27 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 59740 3.4.22.27 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 59749 3.4.22.27 6-[3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86450 3.4.22.27 6-[3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile - 86505 3.4.22.27 6-[4-(2-hydroxyethoxy)-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86464 3.4.22.27 6-[4-(2-hydroxyethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86453 3.4.22.27 6-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86465 3.4.22.27 6-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86455 3.4.22.27 6-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile - 86507 3.4.22.27 6-[4-(3-oxopropyl)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86454 3.4.22.27 6-[4-(ethylamino)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86457 3.4.22.27 6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86463 3.4.22.27 6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-[2-(morpholin-4-yl)ethyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86459 3.4.22.27 6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-[3-(morpholin-4-yl)propyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86461 3.4.22.27 6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86452 3.4.22.27 6-[4-ethoxy-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile - 86506 3.4.22.27 6-[4-methoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86451 3.4.22.27 6-[4-phenoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86456 3.4.22.27 6-[4-[2-(2-oxopyrrolidin-1-yl)ethoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile - 86510 3.4.22.27 6-[4-[2-(dimethylamino)ethoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86474 3.4.22.27 6-[4-[3-(2-ethyl-1H-imidazol-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile - 86509 3.4.22.27 6-[4-[3-(4-ethylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86479 3.4.22.27 6-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile - 86508 3.4.22.27 6-[4-[3-(dimethylamino)propoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile - 86476 3.4.22.27 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 75398 3.4.22.27 6-[[4-(1-acetylpiperidin-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile - 14548 3.4.22.27 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 75397 3.4.22.27 6-[[4-(4-acetyl-1,4-diazepan-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile - 18899 3.4.22.27 6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile - 5431 3.4.22.27 6-[[4-(4-acetylpiperazin-1-yl)-3-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile - 18898 3.4.22.27 6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile - 11965 3.4.22.27 6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile - 3763 3.4.22.27 6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile - 11963 3.4.22.27 6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile - 4433 3.4.22.27 6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile - 11964 3.4.22.27 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 75396 3.4.22.27 7-(2-cyclohexylethyl)-6-(4-methoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile pyrrolopyrimidine inhibitor by modification of the P3 moieties 14554 3.4.22.27 7-(2-cyclohexylethyl)-6-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile pyrrolopyrimidine inhibitor by modification of the P3 moieties 14555 3.4.22.27 7-(2-cyclohexylethyl)-6-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile - 14555 3.4.22.27 7-(2-cyclohexylethyl)-6-(naphthalen-1-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile pyrrolopyrimidine inhibitor by modification of the P3 moieties 73449 3.4.22.27 7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile pyrrolopyrimidine inhibitor by modification of the P3 moieties 10198 3.4.22.27 7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile - 10198 3.4.22.27 7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile pyrrolopyrimidine inhibitor by modification of the P3 moieties 10199 3.4.22.27 7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile - 10199 3.4.22.27 7-(2-cyclohexylethyl)-6-[(pyridine-2-yloxy)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile pyrrolopyrimidine inhibitor by modification of the P3 moieties 75389 3.4.22.27 7-(2-cyclohexylethyl)-6-[(pyridine-2-ylsulfanyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile pyrrolopyrimidine inhibitor by modification of the P3 moieties 75390 3.4.22.27 7-(2-cyclohexylethyl)-6-[[methyl(phenyl)amino]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile pyrrolopyrimidine inhibitor by modification of the P3 moieties 14556 3.4.22.27 7-tert-butyl-6-(4-chlorobenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile - 79371 3.4.22.27 9-[3-(dimethylamino)propyl]-2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile - 86502 3.4.22.27 APC-2848 irreversible vinyl-sulfone inhibitor 132508 3.4.22.27 benzoyl-Phe-Phe-CHN2 0.006 mM, 39% inhibition 115334 3.4.22.27 benzyl [(2S)-1-(2-cyanotetrahydropyridazin-1(2H)-yl)-3-methyl-1-oxopentan-2-yl]carbamate - 79474 3.4.22.27 benzyloxycarbonyl Phe-Ala-CH2F very potent time-dependent inhibitor, inhibits proteinase 30times more efficiently than it does cathepsin L and about 300times better than it does cathepsin B 115342 3.4.22.27 benzyloxycarbonyl-((CH3)3C-CH(NH2)-COOH)-Tyr-CHN2 t1/2 at 0.1 mM is 1.6 min 115343 3.4.22.27 benzyloxycarbonyl-((CH3)3C-CH2-CH(NH2)-COOH)-Leu-Tyr-CHN2 t1/2 at 0.0004 mM is 3.85 min 115344 3.4.22.27 benzyloxycarbonyl-Ala-Leu-COCHO - 52421 3.4.22.27 benzyloxycarbonyl-Ile-Met-CHN2 t1/2 at 0.001 mM is 5.4 min 115362 3.4.22.27 benzyloxycarbonyl-Ile-Trp-CHN2 t1/2 at 0.004 mM is 3.45 min 115363 3.4.22.27 benzyloxycarbonyl-Leu-Ala-CHN2 t1/2 at 0.0001 mM is 5.5 min 115365 3.4.22.27 benzyloxycarbonyl-Leu-Leu-CHN2 t1/2 at 0.00002 mM is 8.6 min 115366 3.4.22.27 benzyloxycarbonyl-Leu-Leu-Nle-CHN2 t1/2 at 0.000001 mM is 1.25 min 115367 3.4.22.27 benzyloxycarbonyl-Leu-Leu-Tyr-CHN2 t1/2 at 0.000001 mM is 5.5 min 31407 3.4.22.27 benzyloxycarbonyl-Leu-Nle-CHN2 t1/2 at 0.00001 mM is 3.4 min 115372 3.4.22.27 benzyloxycarbonyl-Leu-Nva-CHN2 t1/2 at 0.00001 mM is 4.5 min 115373 3.4.22.27 benzyloxycarbonyl-Leu-Thr(tert-butyl)-CHN2 t1/2 at 0.001 mM is 3.5 min 115374 3.4.22.27 benzyloxycarbonyl-Leu-Trp-CHN2 t1/2 at 0.0002 mM is 2.6 min 47122 3.4.22.27 benzyloxycarbonyl-Phe-Ala-CH2F - 52448 3.4.22.27 Benzyloxycarbonyl-Phe-Ala-CHN2 - 8055 3.4.22.27 benzyloxycarbonyl-Phe-Ala-COCHO - 52449 3.4.22.27 Benzyloxycarbonyl-Phe-Arg - 3801 3.4.22.27 benzyloxycarbonyl-Phe-Arg-COCHO - 115377 3.4.22.27 benzyloxycarbonyl-Phe-Leu-COCHO potent, reversible cathepsin S inhibitor, the inhibitor is 400fold more selective for cathepsin S than for cathepsin B 52451 3.4.22.27 benzyloxycarbonyl-Phe-Lys(benzyloxycarbonyl)-CH3 inhibition in the micromolar range, competitive 33394 3.4.22.27 Benzyloxycarbonyl-Phe-Phe-CHN2 - 3194 3.4.22.27 Benzyloxycarbonyl-Phe-Phe-CHN2 0.0005 mM: 51-58% inhibition after 10 min. 0.005 mM: 86-90% inhibition after 10 min 3194 3.4.22.27 Benzyloxycarbonyl-Phe-Phe-CHN2 0.001 mM, 98% inhibition 3194 3.4.22.27 Benzyloxycarbonyl-Phe-Phe-CHN2 t1/2 at 0.001 mM is 6.4 min 3194 3.4.22.27 benzyloxycarbonyl-Phe-Tyr(OBut)-COCHO - 52452 3.4.22.27 benzyloxycarbonyl-Phe-Tyr(tert-butyl)CHN2 t1/2 at 0.02 mM is 19.25 min, about 10000times more effective against cathepsin L than against cathepsin S 115379 3.4.22.27 benzyloxycarbonyl-Trp-Met-CHN2 t1/2 at 0.00001 mM is 3.0 min 47128 3.4.22.27 benzyloxycarbonyl-Tyr-Ala-CHN2 0.001 mM, 88% inhibition 47129 3.4.22.27 benzyloxycarbonyl-Tyr-Tyr(O-butyl)-CHN2 1 mM, 78% inhibition 115381 3.4.22.27 benzyloxycarbonyl-Val-Met-CHN2 t1/2 at 0.0001 mM is 3.5 min 115386 3.4.22.27 benzyloxycarbonyl-Val-Nle-CHN2 t1/2 at 0.00003 mM is 5.8 min 115387 3.4.22.27 benzyloxycarbonyl-Val-Trp-Nle-CHN2 t1/2 at 0.00001 mM is 5.7 min 115389 3.4.22.27 benzyloxycarbonyl-Val-Val-CHN2 t1/2 at 0.0001 mM is 47.0 min 115392 3.4.22.27 benzyloxycarbonyl-Val-Val-Lys-NHO-4-nitrobenzoyl - 52454 3.4.22.27 benzyloxycarbonyl-Val-Val-Nle-CHN2 t1/2 at 0.000001 is 2.5 min, 300times more effective in inactivating cathepsin S than cathepsin L 115393 3.4.22.27 benzyloxycarbonyl-Val-Val-Phe-CH3 inhibition in the micromolar range, competitive 52455 3.4.22.27 benzyloxycarbonyl-Val-Val-Tyr-CHN2 t1/2 at 0.000005 mM is 6.75 min 115394 3.4.22.27 BMV083 a near-infrared quenched activity-based probe (qABP) that selectively targets cathepsin S in immune cells 238658 3.4.22.27 BMV109 a pan-reactive cysteine cathepsin qABP 239853 3.4.22.27 BMV117 a near-infrared quenched activity-based probe (qABP) that selectively targets cathepsin S in immune cells 238659 3.4.22.27 BMV157 a near-infrared quenched activity-based probe (qABP) that targets cathepsin S in immune cells 238660 3.4.22.27 butyloxycarbonyl-Lys-Leu-Tyr-CHN2 t1/2 at 0.0001 mM is 2.9 min 115427 3.4.22.27 carbobishydrazide irreversible cathepsin S inhibitor 139082 3.4.22.27 cathepsin K propeptide - 11290 3.4.22.27 cathepsin L propeptide - 22297 3.4.22.27 cathepsin S propeptide 0.0002 mM, blocks gelatinase, collagenase and elastinase activities of mature cathepsin S 8495 3.4.22.27 cathespin S propeptide - 33402 3.4.22.27 cathespin S propeptide tight binding/slow reacting inhibition 33402 3.4.22.27 cathespin S propeptide more selective for inhibition of cathepsin L than cathepsin S 33402 3.4.22.27 chimeric propeptide of cathepsin S and cathepsin L S1-54/L44-86 - 115471 3.4.22.27 Chlorella powder - 25960 3.4.22.27 CLIK-060 0.001 mM, complete inhibition 52486 3.4.22.27 CLIK-060 strong 52486 3.4.22.27 CLIK-066 0.01 mM, 28% inhibition 115482 3.4.22.27 CLIK-088 0.01 mM, 64% inhibition 115483 3.4.22.27 CLIK-112 0.01 mM, 77% inhibition 115484 3.4.22.27 CLIK-121 0.01 mM, complete inhibition 115485 3.4.22.27 CLIK-148 0.01 mM, complete inhibition 11292 3.4.22.27 CLIK-164 - 115486 3.4.22.27 CLIK-181 0.01 mM, 80% inhibition 115487 3.4.22.27 CLIK-195 0.01 mM, complete inhibition 115488 3.4.22.27 CLIK60 selective CatS inhibitor, CatS inhibition increases macrophage cholesterol accumulation and efflux 75387 3.4.22.27 cystatin - 1600 3.4.22.27 cystatin 0.001 mM, complete inhibition 1600 3.4.22.27 cystatin 0.5 mg/ml, 82% inhibition 1600 3.4.22.27 cystatin A inhibition in the subnanomolar range 7539 3.4.22.27 cystatin B inhibition in the subnanomolar range 9663 3.4.22.27 cystatin C - 1994 3.4.22.27 cystatin C wild-type and mutant forms 1994 3.4.22.27 cystatin C inhibition in the picomolar range 1994 3.4.22.27 cystatin C specific endogenous inhibitor, potency against smooth muscle cell invasion, overview 1994 3.4.22.27 cystatin C endogenous specific inhibitor 1994 3.4.22.27 cystatin C endogenous specific enzyme inhibitor, absence of cystatin C results in increased angiogene sis and tumor cell proliferation 1994 3.4.22.27 cystatin C endogenous specific enzyme inhibitor, absence of cystatin C results in increased angiogenesis and tumor cell proliferation 1994 3.4.22.27 cystatin F - 18063 3.4.22.27 dipeptide-vinyl sulfone LHVS irreversible cathepsin S inhibitor 139083 3.4.22.27 E-64 0.001 mM, 96% inhibition 559 3.4.22.27 E-64 0.005 mM, 96% inhibition 559 3.4.22.27 E-64 - 559 3.4.22.27 E-64 irreversible inhibitor 559 3.4.22.27 E-64 strong inhibition 559 3.4.22.27 E64 - 1457 3.4.22.27 E64 64 nM 1457 3.4.22.27 E64 potency against smooth muscle cell invasion, overview 1457 3.4.22.27 E64 general cathepsin inhibitor 1457 3.4.22.27 E64 cysteine protease inhibitor 1457 3.4.22.27 egg white cystatin - 37027 3.4.22.27 EM053 a pan-reactive cysteine cathepsin qABP 239854 3.4.22.27 Ep-475 0.01 mM, complete inhibition 8103 3.4.22.27 epoxysuccinyl-Ala benzyl ester - 115626 3.4.22.27 epoxysuccinyl-Arg benzyl ester - 115627 3.4.22.27 epoxysuccinyl-D-Phe benzyl amide - 115628 3.4.22.27 epoxysuccinyl-D-Phe benzyl ester - 115629 3.4.22.27 epoxysuccinyl-Ile benzyl ester - 115630 3.4.22.27 epoxysuccinyl-Leu benzyl amide - 115631 3.4.22.27 epoxysuccinyl-Leu benzyl ester - 115632 3.4.22.27 epoxysuccinyl-Phe benzyl amide - 115633 3.4.22.27 epoxysuccinyl-Phe benzyl ester - 115634 3.4.22.27 epoxysuccinyl-Val benzyl ester - 115635 3.4.22.27 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 59813 3.4.22.27 GM6001 - 1952 3.4.22.27 iodoacetic acid 1 mM, 92% inhibition 213 3.4.22.27 JNJ 10329670 - 6185 3.4.22.27 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 6185 3.4.22.27 JNJ 10329670 competitive, reversible inhibition, 4-(2-keto-1-benzimidazolinyl)-piperidin-1-yl derivative, IC50: 100 nM 6185 3.4.22.27 kininogen domain 3 - 66496 3.4.22.27 L-873724 - 2797 3.4.22.27 leupeptin 5.2 nM 217 3.4.22.27 leupeptin 1 mM, complete inhibition 217 3.4.22.27 leupeptin - 217 3.4.22.27 LHVS - 10061 3.4.22.27 LO143 a near-infrared quenched activity-based probe (qABP) that targets cathepsin S in immune cells 238685 3.4.22.27 LO219 a near-infrared quenched activity-based probe (qABP) that targets cathepsin S in immune cells 238686 3.4.22.27 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 - 79798 3.4.22.27 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 - 66552 3.4.22.27 methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfenate - 64799 3.4.22.27 methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfinate - 14149 3.4.22.27 methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(3-fluorophenyl)ethyl]amino]propane-1-sulfinate - 64800 3.4.22.27 methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfenate - 14150 3.4.22.27 methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfinate - 14151 3.4.22.27 methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propane-1-sulfinate - 64801 3.4.22.27 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 - 79343 3.4.22.27 methyl (2Z)-4-[4-(dimethylamino)phenyl]-4-oxo-2-[(phenylcarbonyl)hydrazono]butanoate - 73549 3.4.22.27 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 - 79832 3.4.22.27 methyl (3R)-3-[[(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanoyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate - 64803 3.4.22.27 methyl (3S)-3-[[(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanoyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate - 64804 3.4.22.27 methyl (3S)-3-[[3-cyclohexyl-N-(morpholin-4-ylcarbonyl)-L-alanyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate - 64805 3.4.22.27 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 - 64807 3.4.22.27 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 - 64808 3.4.22.27 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 - 64809 3.4.22.27 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 - 64810 3.4.22.27 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 - 64811 3.4.22.27 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 - 64812 3.4.22.27 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 - 64813 3.4.22.27 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 - 79496 3.4.22.27 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 - 64814 3.4.22.27 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 - 64815 3.4.22.27 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 - 64816 3.4.22.27 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 - 64817 3.4.22.27 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 - 64818 3.4.22.27 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 - 64819 3.4.22.27 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 - 64820 3.4.22.27 methyl 2-amino-4-([(1S)-2-(1-[(benzyloxy)methyl]-3-[(2-ethoxy-2-oxoethyl)amino]-2,3-dioxopropylamino)-1-(cyclohexylmethyl)-2-oxoethyl]aminocarbonyl)benzoate - 159186 3.4.22.27 methyl 2-[[(1S)-1-(cyclohexylmethyl)-2-([2-[(4-fluorophenyl)amino]ethyl]amino)-2-oxoethyl]amino]-1,3-benzoxazole-6-carboxylate IC50: 43 nM 59799 3.4.22.27 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 - 64825 3.4.22.27 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 - 64826 3.4.22.27 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 - 64827 3.4.22.27 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 - 64828 3.4.22.27 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 - 64829 3.4.22.27 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 - 64830 3.4.22.27 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 - 64831 3.4.22.27 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 - 64832 3.4.22.27 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 - 64833 3.4.22.27 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 - 64834 3.4.22.27 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 - 64835 3.4.22.27 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 - 64836 3.4.22.27 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 - 64837 3.4.22.27 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 - 64838 3.4.22.27 methyl 4'-[(1S)-1-([(1S)-1-[(1-cyanocyclopropyl)carbamoyl]pentyl]amino)-2,2,2-trifluoroethyl]biphenyl-4-sulfinate - 64841 3.4.22.27 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 - 159189 3.4.22.27 methyl 4-[(E)-[[(3-[2-[(2-chlorobenzyl)oxy]phenyl]-1H-pyrazol-5-yl)carbonyl]hydrazono]methyl]benzoate - 73569 3.4.22.27 additional information inhibitory potential in vivo on Ii degradation in JY cells 2 3.4.22.27 additional information analysis of inhibition mechanisms and binding to the active site; design and synthesis of arylaminoethyl amides as noncovalent inhibitors of cathepsin S, overview 2 3.4.22.27 additional information diverse arylaminoethyl amides as noncovalent inhibitors of cathepsin S with IC50 in the nanomolar range, optimization of P1 and N-aryl, binding specificities of positions P1 and P2, and of subsite S1, overview 2 3.4.22.27 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 2 3.4.22.27 additional information synthesis and inhibitory effects of diverse arylaminoethyl carbamate inhibitors possessing a substrate peptidomimetic scaffold, structue-activity relationship, pharmacokinetics, overview 2 3.4.22.27 additional information reversible inhibition by a dipeptide-nitrile inhibitor 2 3.4.22.27 additional information no inhibition by proteasome inhibitors 2 3.4.22.27 additional information effect of cathepsin S inhibition on bronchoalveolar lavage fluid cytokines: inhibition reduces ozone-induced interleukin-6 levels at 3 h and 20-24 h and TNF-alpha levels are inhibited at 20-24 h 2 3.4.22.27 additional information design and synthesis of a near-infrared quenched activity-based probes (qABP) that selectively target cathepsin S which is highly expressed in immune cells, green-fluorescent pan-reactive cysteine cathepsin qABP in dual color labeling studies in bone marrow-derived immune cells, and identification of vesicles containing exclusively cathepsin S activity, method optimization and evaluation, overview. The high degree of selectivity is retained both in vitro and in vivo 2 3.4.22.27 morpholine-4-carboxylic acid [1-[1S-(N-benzoyl-hydrazinomethyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide IC50: 565 mM 52670 3.4.22.27 morpholine-4-carboxylic acid [1R-(1S-cyano-3-phenyl-propylcarbamoyl)-1,3-dimethyl-butyl]-amide - 116086 3.4.22.27 morpholine-4-carboxylic acid [1R-(1S-cyano-3-phenyl-propylcarbamoyl)-3-methylbutyl]amide IC50: 0.011 mM 52671 3.4.22.27 morpholine-4-carboxylic acid [1S-(1R-cyano-3-phenylpropylcarbamoyl)-3-methylbutyl]amide IC50: 387 nM 52672 3.4.22.27 morpholine-4-carboxylic acid [1S-(1S-cyano-2,2-dimethylpropylcarbamoyl)-3-methylbutyl]amide IC50: 0.107 mM 52673 3.4.22.27 morpholine-4-carboxylic acid [1S-(1S-cyano-2-methyl-propylcarbamoyl)-3-methylbutyl]amide IC50: 1400 nM 52674 3.4.22.27 morpholine-4-carboxylic acid [1S-(1S-cyano-2-phenylethylcarbamoyl)-3-methylbutyl]amide IC50: 130 nM 52675 3.4.22.27 morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenyl-propylcarbamoyl)-1,3-dimethyl-butyl]-amide IC50: 0.076 mM 52676 3.4.22.27 morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-cyclohexyl-ethyl]-amide IC50: 5 mM 52677 3.4.22.27 morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-methyl-propyl]-amide IC50: 0.006 mM 52678 3.4.22.27 morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-phenyl-ethyl]-amide IC50: 173 mM 52679 3.4.22.27 morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-3,3-dimethyl-butyl]-amide IC50: 23 nM 52680 3.4.22.27 morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-cyclohexyl-R-methyl]-amide IC50: 84 nM 52681 3.4.22.27 morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-ethyl]-amide IC50: 0.134 mM 52682 3.4.22.27 morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-pentyl]-amide IC50: 41 nM 52683 3.4.22.27 morpholine-4-carboxylic acid [1S-(1S-cyanobutylcarbamoyl)-3-methylbutyl]amide IC50: 82 nM 52684 3.4.22.27 morpholine-4-carboxylic acid [1S-(1S-cyanobutylcarbamoyl)-3-methylpentyl]amide IC50: 56 nM 52685 3.4.22.27 morpholine-4-carboxylic acid [1S-(1S-cyanomethylcarbamoyl)-3-methylbutyl]amide IC50: 142 nM 52686 3.4.22.27 morpholine-4-carboxylic acid [1S-(2-benzyloxy-1R-cyano-ethylcarbamoyl)-3-methylbutyl]amide IC50: 19 nM 52687 3.4.22.27 morpholine-4-carboxylic acid [1S-(cyanomethylcarbamoyl)-3-methylbutyl]amide IC50: 124 nM 52688 3.4.22.27 morpholine-4-carboxylic acid [1S-[(1-cyano-1-methyl)ethylcarbamoyl]-3-methylbutyl]amide IC50: 114 nM 52689 3.4.22.27 morpholine-4-carboxylic acid [1S-[(cyano-phenyl-S-methyl)carbamoyl]-3-methylbutyl]amide IC50: 51 nM 52690 3.4.22.27 morpholine-4-carboxylic acid [1S-[1S-(benzoyl-hydrazonomethyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide IC50: 11 nM 33504 3.4.22.27 morpholine-4-carboxylic acid [1S-[1S-cyano-2-(3,4-dichlorophenyl)ethylcarbamoyl]-3-methylbutyl]amide IC50: 56 nM 52691 3.4.22.27 morpholine-4-carboxylic acid [1S-[1S-[(2-hydroxy-benzoyl)-hydrazonomethyl]-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide IC50: 7 nM 33505 3.4.22.27 morpholine-4-carboxylic acid [1S-[1S-[(4-hydroxybenzoyl)-hydrazonomethyl]-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide IC50: 35 nM 33506 3.4.22.27 morpholine-4-carboxylic acid [1S-[2-(2-chlorobenzyloxy)-1R-cyanoethylcarbamoyl]-3-methylbutyl]amide 9 nM 116087 3.4.22.27 morpholine-4-carboxylic acid [1S-[2-(3-chlorobenzyloxy)-1R-cyanoethylcarbamoyl]-3-methylbutyl]amide 9 nM 116088 3.4.22.27 morpholine-4-carboxylic acid [1S-[2-(4-chlorobenzyloxy)-1R-cyanoethylcarbamoyl]-3-methylbutyl]amide 27 nM 116089 3.4.22.27 morpholine-4-carboxylic acid [3-methyl-1S-(1-prop-2-ynylcarbamoyl)butyl]amide IC50: 0.097 m 52692 3.4.22.27 morpholine-4-carboxylic acid [3-methyl-1S-(1R-methyl-3-phenylpropylcarbamoyl)butyl]amide IC50 above 0.339 mM 52693 3.4.22.27 morpholine-4-carboxylic acid [3-methyl-1S-(3-phenyl-propylcarbamoyl)butyl]amide IC50 above 0.028 mM 52694 3.4.22.27 morpholineurea-leucyl-homophenylalanine-vinylsulfone phenyl LHVS, CatS-specific inhibitor at a concentration of 10 nM, other cathepsins are not inhibited 60881 3.4.22.27 morpholinurea-leucine-homophenylalanine-vinyl sulfone-phenyl irreversible inhibitor 160032 3.4.22.27 morpholinurea-leucinehomophenylalanine-vinyl phenyl sulfone irreversible CatS inhibitor 139084 3.4.22.27 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 - 79643 3.4.22.27 N-(1-cyanocyclopropyl)-3-(methylsulfinyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide - 79599 3.4.22.27 N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-(4'-fluorobiphenyl-4-yl)ethyl]-L-alaninamide - 79600 3.4.22.27 N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide - 79667 3.4.22.27 N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-phenylethyl]-L-alaninamide - 79551 3.4.22.27 N-(1-cyanocyclopropyl)-3-[(3,4-dichlorophenyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide - 79604 3.4.22.27 N-(1-cyanocyclopropyl)-3-[(4-fluorobenzyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-phenylethyl]-L-alaninamide - 79588 3.4.22.27 N-(1-cyanocyclopropyl)-3-[(4-fluorophenyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide - 79902 3.4.22.27 N-(1-cyanocyclopropyl)-3-[[2-(4-fluorophenyl)propan-2-yl]sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide - 79487 3.4.22.27 N-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide - 79421 3.4.22.27 N-(4-benzyl-1-methylpiperidin-4-yl)-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide - 14558 3.4.22.27 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 - 79571 3.4.22.27 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 - 73642 3.4.22.27 N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetamide - 14559 3.4.22.27 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 75394 3.4.22.27 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 75395 3.4.22.27 N-(cyanomethyl)-2-[3-(1H-indol-5-yl)phenyl]-4-methylpentanamide IC50: 922 nM 52709 3.4.22.27 N-(cyanomethyl)-2-[3-(1H-indol-6-yl)phenyl]-4-methylpentanamide IC50: 1257 nM 52710 3.4.22.27 N-(cyanomethyl)-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]-3-phenylpropanamide IC50 above 0.01 mM 52712 3.4.22.27 N-(cyanomethyl)-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]acetamide IC50 above 0.01 mM 52711 3.4.22.27 N-(cyanomethyl)-3-cyclobutyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]propanamide IC50: 2310 nM 52713 3.4.22.27 N-(cyanomethyl)-3-cyclopropyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]propanamide IC50: 6597 nM 52714 3.4.22.27 N-(cyanomethyl)-4-methyl-2-(2-phenyl-1,3-thiazol-4-yl)pentanamide IC50 above 0.01 mM 52715 3.4.22.27 N-(cyanomethyl)-4-methyl-2-(3'-piperazin-1-yl-1,1'-biphenyl-3-yl)pentanamide methanesulfonate IC50 above 0.01 mM 52716 3.4.22.27 N-(cyanomethyl)-4-methyl-2-(3-pyridin-3-ylphenyl)-pentanamide IC50 above 0.01 nM 52717 3.4.22.27 N-(cyanomethyl)-4-methyl-2-(3-pyridin-4-ylphenyl)-pentanamide trifluoroacetate IC50: 1748 nM 52718 3.4.22.27 N-(cyanomethyl)-4-methyl-2-(3-pyrimidin-5-ylphenyl)pentanamide IC50 above 0.01 mM 52719 3.4.22.27 N-(cyanomethyl)-4-methyl-2-(5-phenylpyridin-3-yl)-pentanamide trifluoroacetate IC50 above 0.01 mM 52720 3.4.22.27 N-(cyanomethyl)-4-methyl-2-[2'-(1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide IC50: 521 nM 52721 3.4.22.27 N-(cyanomethyl)-4-methyl-2-[2'-(4-morpholinyl)[1,1'-biphenyl]-3-yl]pentanamide IC50: 3368 nM 52722 3.4.22.27 N-(cyanomethyl)-4-methyl-2-[3'-(4-morpholinyl)[1,1'-biphenyl]-3-yl]pentanamide IC50 above 0.01 mM 52723 3.4.22.27 N-(cyanomethyl)-4-methyl-2-[4'-(1,2,3,6-tetrahydro-4-pyridinyl)[1,1'-biphenyl]-3-yl]pentanamide IC50: 652 nM 52724 3.4.22.27 N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide IC50: 1245 nM 52725 3.4.22.27 N-(cyanomethyl)-4-methyl-2-[4'-(4-methyl-1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide IC50: 1695 nM 52726 3.4.22.27 N-(cyanomethyl)-4-methyl-2-[4'-(4-morpholinyl)[1,1'-biphenyl]-3-yl]pentanamide IC50: 9422 nM 52727 3.4.22.27 N-(cyanomethyl)-4-methyl-2-[4'-(4-piperidinyl)[1,1'-biphenyl]-3-yl]pentanamide IC50: 1421 nM 52728 3.4.22.27 N-(cyanomethyl)-4-methyl-2-[4'-(methylsulfonyl)-1,1'-biphenyl-3-yl]pentanamide IC50: 6623 nM 52708 3.4.22.27 N-(trans-epoxysuccinyl)-L-leucine 4-guanidinobutylamide - 206268 3.4.22.27 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 - 79602 3.4.22.27 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 - 79596 3.4.22.27 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 - 79854 3.4.22.27 N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide - 14560 3.4.22.27 N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)oxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide - 14561 3.4.22.27 N-benzyl-2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide - 14562 3.4.22.27 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 - 79427 3.4.22.27 N-morpholinurea-leucine-homophenylalanine-vinylsulfone-phenyl i.e. LHVS, specific inhibitor, potency against smooth muscle cell invasion, overview 35834 3.4.22.27 N-morpholinurea-leucine-homophenylalanine-vinylsulfone-phenyl specific inhibitor 35834 3.4.22.27 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 60872 3.4.22.27 N-morpholinurea-leucyl-homophenylalanyl-vinylsulfone-phenyl i.e. LHVS, irreversible inhibition, the inhibitor binds covalently to the active site 60872 3.4.22.27 N-morpholinurealeucine-homophenylalanine-vinylsulfone-phenyl - 160031 3.4.22.27 N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-norvalinamide - 7040 3.4.22.27 N-[(1R)-1-([2-[(1,3-benzoxazol-2-ylsulfanyl)acetyl]hydrazino]carbonyl)propyl]-2-[(phenylcarbonyl)amino]benzamide - 73687 3.4.22.27 N-[(1R)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide - 14563 3.4.22.27 N-[(1R)-1-benzyl-2-pyrrolidin-1-ylpropyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide - 14564 3.4.22.27 N-[(1S)-1-(1H-indol-2-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide IC50: 29 nM 59774 3.4.22.27 N-[(1S)-1-(biphenyl-4-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide IC50: 34 nM 59775 3.4.22.27 N-[(1S)-1-(cyclohexylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide IC50: 62 nM 59758 3.4.22.27 N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-1-benzofuran-2-carboxamide IC50: 17 nM 23875 3.4.22.27 N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-1-benzofuran-2-carboxamide - 23875 3.4.22.27 N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-(3-fluorophenyl)furan-2-carboxamide IC50: 34 nM 23874 3.4.22.27 N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-(3-fluorophenyl)furan-2-carboxamide - 23874 3.4.22.27 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 23873 3.4.22.27 N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-[3-(trifluoromethyl)phenyl]furan-2-carboxamide - 23873 3.4.22.27 N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-2-carboxamide IC50: 47 nM 23876 3.4.22.27 N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-2-carboxamide - 23876 3.4.22.27 N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-3-carboxamide IC50: 6 nM 23877 3.4.22.27 N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-3-carboxamide - 23877 3.4.22.27 N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]morpholine-4-carboxamide - 64872 3.4.22.27 N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-3-carboxamide IC50: 213 nM 23878 3.4.22.27 N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-3-carboxamide - 23878 3.4.22.27 N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[[(1S)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]amino]ethyl]morpholine-4-carboxamide - 64873 3.4.22.27 N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide IC50: 11 nM 23884 3.4.22.27 N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide - 23884 3.4.22.27 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 23882 3.4.22.27 N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydro-2H-pyran-4-carboxamide - 23882 3.4.22.27 N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-3-carboxamide IC50: 21 nM 23881 3.4.22.27 N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-3-carboxamide - 23881 3.4.22.27 N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-2-(5-fluoro-2,2-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]amino]-2-oxoethyl]morpholine-4-carboxamide - 64874 3.4.22.27 N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]amino]-2-oxoethyl]morpholine-4-carboxamide - 64875 3.4.22.27 N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-2-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]amino]-2-oxoethyl]morpholine-4-carboxamide - 64876 3.4.22.27 N-[(1S)-1-(cyclopentylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide - 64877 3.4.22.27 N-[(1S)-1-(furan-2-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide IC50: 0.020 mM 59771 3.4.22.27 N-[(1S)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide - 14565 3.4.22.27 N-[(1S)-1-cyclohexyl-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide IC50: 23 nM 59757 3.4.22.27 N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1,2-dimethylpropyl]benzamide - 36831 3.4.22.27 N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1,2-dimethylpropyl]thiophene-3-carboxamide - 64878 3.4.22.27 N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-(4-methylcyclohexyl)ethyl]thiophene-3-carboxamide - 64879 3.4.22.27 N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-(trans-4-methylcyclohexyl)ethyl]thiophene-3-carboxamide - 79653 3.4.22.27 N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-cyclohexylethyl]benzamide - 64880 3.4.22.27 N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-cyclohexylethyl]thiophene-3-carboxamide - 24763 3.4.22.27 N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-1-(naphthalen-2-ylmethyl)-2-oxoethyl]-3-methylbenzamide IC50: 16 nM 59773 3.4.22.27 N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(1,3-thiazol-5-ylmethyl)ethyl]-3-methylbenzamide IC50: 0.065 mM 59772 3.4.22.27 N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(pyridin-3-ylmethyl)ethyl]-3-methylbenzamide IC50: 3707 nM 59769 3.4.22.27 N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(pyridin-4-ylmethyl)ethyl]-3-methylbenzamide IC50: 6769 nM 59770 3.4.22.27 N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-phenylethyl]-3-methylbenzamide IC50: 285 nM 59760 3.4.22.27 N-[(1S)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxo-1-[(2-phenylethyl)sulfanyl]ethyl]morpholine-4-carboxamide - 64881 3.4.22.27 N-[(1S)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxo-1-[(2-phenylethyl)sulfonyl]ethyl]morpholine-4-carboxamide - 64882 3.4.22.27 N-[(1S)-3-cyclohexyl-1-([2-[(4-methoxyphenyl)amino]ethyl]carbamoyl)propyl]-3-methylbenzamide IC50: 38 nM 59759 3.4.22.27 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 - 115031 3.4.22.27 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 - 159206 3.4.22.27 N-[(2S)-1-[[(1R)-2-(benzyloxy)-1-cyanoethyl]amino]-3-cyclohexyl-1-oxopropan-2-yl]morpholine-4-carboxamide - 79651 3.4.22.27 N-[(2S)-2-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-3-methylbutan-2-yl]thiophene-3-carboxamide - 79652 3.4.22.27 N-[(2S)-3-cyclohexyl-1-([2-[(4-methoxyphenyl)amino]ethyl]amino)-1-oxopropan-2-yl]-5-[3-(trifluoromethyl)phenyl]furan-2-carboxamide - 159239 3.4.22.27 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 - 159321 3.4.22.27 N-[(2S)-3-methyl-2-[1-[(2S)-1-oxohexan-2-yl]-1H-1,2,3-triazol-4-yl]butan-2-yl]thiophene-3-carboxamide - 80019 3.4.22.27 N-[(3S)-4-benzyloxy-(2S)-4-methyl-[[[2-[(9-oxo-9H-1-fluorenyl)carbonyl]amino]propaneyl]amino]-1,2-dioxobutyl]glycine ethyl ester - 159273 3.4.22.27 N-[(3S)-4-benzyloxy-3-[[[(2S)-2-[(3-amino-4-chlorobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester - 159121 3.4.22.27 N-[(3S)-4-benzyloxy-3-[[[(2S)-2-[(3-[(tert-butoxycarbonyl)amino]-4-chlorobenzoyl amino)]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ester - 159198 3.4.22.27 N-[(3S)-4-benzyloxy-3-[[[1-[(4-morpholinylcarbonyl)-amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester - 79649 3.4.22.27 N-[(3S)-4-benzyloxy-3-[[[2-[((1-methylcyclopropyl)carbonyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester - 159241 3.4.22.27 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 - 159204 3.4.22.27 N-[(3S)-4-benzyloxy-3-[[[2-[((5-nitro-2-thienyl)carbonyl)amino]cyclo-hexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester - 159205 3.4.22.27 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 - 160033 3.4.22.27 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 - 159203 3.4.22.27 N-[(3S)-4-benzyloxy-3-[[[2-[(2-(2-thienyl)acetyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester - 159257 3.4.22.27 N-[(3S)-4-benzyloxy-3-[[[2-[(2-chloro-5-(methylsulfanyl)benzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester - 159110 3.4.22.27 N-[(3S)-4-benzyloxy-3-[[[2-[(3-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester - 79538 3.4.22.27 N-[(3S)-4-benzyloxy-3-[[[2-[(4-chloro-3-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester - 159066 3.4.22.27 N-[(3S)-4-benzyloxy-3-[[[2-[(4-methoxybenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester - 159141 3.4.22.27 N-[(3S)-4-benzyloxy-3-[[[2-[(5-chloro-2-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester - 159142 3.4.22.27 N-[(3S)-4-benzyloxy-3-[[[2-[(5-methoxy-2-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester - 159115 3.4.22.27 N-[2-(1-methylethyl)phenyl]-Na-(phenoxycarbonyl)-L-tryptophanamide - 73728 3.4.22.27 N-[2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)ethyl]-N2-(3-methylbenzoyl)-L-leucinamide - 159212 3.4.22.27 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 - 27322 3.4.22.27 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 - 79537 3.4.22.27 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 - 79366 3.4.22.27 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 - 75385 3.4.22.27 N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-N2-[(3-methylphenyl)carbonyl]-L-leucinamide IC50: 46 nM 59756 3.4.22.27 N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide IC50: 27 nM 59765 3.4.22.27 N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-(3-methylbenzoyl)-L-leucinamide - 79842 3.4.22.27 N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(3-methylphenyl)carbonyl]-L-leucinamide IC50: 62 nM 59755 3.4.22.27 N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-4-(trifluoromethyl)-L-phenylalaninamide IC50: 19 nM 59766 3.4.22.27 N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide IC50: 29 nM 59761 3.4.22.27 N-[2-[(4-methoxyphenyl)amino]ethyl]-O-methyl-Na-[(3-methylphenyl)carbonyl]-L-tyrosinamide IC50: 66 nM 59767 3.4.22.27 N-[4-(4-cyano-1H-imidazo[4,5-c]pyridin-6-yl)-2-(trifluoromethyl)phenyl]formamide - 86458 3.4.22.27 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 - 79523 3.4.22.27 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 - 79819 3.4.22.27 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 - 79519 3.4.22.27 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 - 79520 3.4.22.27 N-[[(2S)-1-[[(1S)-1-cyano-3-phenylpropyl]amino]-3-cyclohexyl-1-oxopropan-2-yl]carbamoyl]morpholine-4-carboxamide - 159053 3.4.22.27 N2-(5-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide IC50: 173 nM 59797 3.4.22.27 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 59811 3.4.22.27 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 59810 3.4.22.27 N2-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide IC50: 93 nM 59796 3.4.22.27 N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-(1-methyl-2-[[3-(methylsulfonyl)phenyl]amino]ethyl)-L-alaninamide IC50: 26 nM 59802 3.4.22.27 N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-(1-methyl-2-[[4-(methylsulfonyl)phenyl]amino]ethyl)-L-alaninamide IC50: 11 nM 59801 3.4.22.27 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 - 79576 3.4.22.27 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 59804 3.4.22.27 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 59803 3.4.22.27 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 59806 3.4.22.27 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 59805 3.4.22.27 N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide IC50: 19 nM 59798 3.4.22.27 N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]-1-methylethyl]-L-alaninamide IC50: 1 nM 59800 3.4.22.27 N2-(biphenyl-3-ylacetyl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide IC50: 2.9 nM 59779 3.4.22.27 N2-(biphenyl-4-ylacetyl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide IC50: 9.1 nM 59780 3.4.22.27 N2-(morpholin-4-ylcarbonyl)-N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-leucinamide - 7041 3.4.22.27 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 59808 3.4.22.27 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 59807 3.4.22.27 N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide IC50: 94 nM 59793 3.4.22.27 N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide IC50: 29 nM 59792 3.4.22.27 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 59809 3.4.22.27 N2-benzoyl-N1-(cyanomethyl)-L-leucinamide IC50: 41 nM 52744 3.4.22.27 N2-[(3'-chlorobiphenyl-4-yl)acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide IC50: 7.4 nM 59781 3.4.22.27 N2-[(5-chloro-1-benzofuran-2-yl)acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide IC50: 9.4 nM 59778 3.4.22.27 N2-[[1-(5-bromopyrimidin-2-yl)piperidin-3-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide IC50: 49 nM 59788 3.4.22.27 N2-[[1-(5-bromopyrimidin-2-yl)piperidin-4-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide IC50: 107 nM 59787 3.4.22.27 N2-[[5-(4-chlorophenyl)furan-2-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide IC50: 7.1 nM 59790 3.4.22.27 Na-(morpholin-4-ylcarbonyl)-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)-L-phenylalaninamide - 64901 3.4.22.27 NEM 1 mM, complete inhibition 89 3.4.22.27 o-aminobenzoic acid-Leu-Phe-Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine - 40415 3.4.22.27 o-aminobenzoic acid-Val-Leu-Phe-Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine - 40414 3.4.22.27 p-chloromercuriphenylsulfonic acid 1 mM, 96% inhibition 1416 3.4.22.27 p41 fragment - 66494 3.4.22.27 paecilopeptin i.e. acetyl-Leu-Val-CHO, IC50: 21 nM 52808 3.4.22.27 Peptidyl(acyloxy)methyl ketones extremely potent inactivator 99577 3.4.22.27 propeptide1-98 of chimeric cathepsin S - 116584 3.4.22.27 RO5461111 - 239855 3.4.22.27 RO5461111 inhibits Cat-S activity and reduces podocyte loss, proteinuria, glomerulosclerosis, and renal inflammation in T2D db/db mice 239855 3.4.22.27 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 33595 3.4.22.27 Stefin A human stefin A 10951 3.4.22.27 Stefin A - 10951 3.4.22.27 Stefin B bovine stefin B, competitive 12910 3.4.22.27 Stefin B human and bovine stefin B 12910 3.4.22.27 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 59814 3.4.22.27 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 - 79565 3.4.22.27 tert-butyl 4-[3'-[1-[[(cyanomethyl)amino]carbonyl]-3-methylbutyl]-1,1'-biphenyl-4-yl]piperazine-1-carboxylate IC50: 1298 nM 52927 3.4.22.27 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 - 79460 3.4.22.27 tert-butyl [(2S)-1-(2-cyanopyrazolidin-1-yl)-1-oxo-3-phenylpropan-2-yl]carbamate - 79694 3.4.22.27 tert-butyl [(2S)-1-(2-cyanopyrazolidin-1-yl)-3-methyl-1-oxobutan-2-yl]carbamate - 79558 3.4.22.27 tert-butyl [(2S)-1-(2-cyanopyrazolidin-1-yl)-4-methyl-1-oxopentan-2-yl]carbamate - 79559 3.4.22.27 tert-butyl [(2S)-1-(2-cyanotetrahydropyridazin-1(2H)-yl)-3-methyl-1-oxobutan-2-yl]carbamate - 79560 3.4.22.27 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 23883 3.4.22.27 tetrahydro-2H-pyran-4-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate - 23883 3.4.22.27 tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate - 36838 3.4.22.27 Tg1 domain of testican-1 - 66495 3.4.22.27 Triton X-100 - 61 3.4.22.27 Tween 20 - 555 3.4.22.27 [(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]benzene - 64913 3.4.22.27 [(2',3',4'-trifluorobiphenyl-2-yl)oxy]acetaldehyde - 79697 3.4.22.27 [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 - 79562 3.4.22.27 [1S-(1S-cyano-3-phenylpropylcarbamoyl)-3-methylbutyl]-amide IC50: 42 nM 52128 3.4.22.27 [1S-(2-cyano-1S-phenethyl-ethylcarbamoyl)-3-methylbutyl]amide IC50 above 0.02 mM 52129 3.4.22.27 [2-[[(4-chlorophenyl)sulfanyl]methyl]-4-hydroxy-6,7-dimethoxyquinazolin-3(4H)-yl]acetonitrile - 73844 3.4.22.27 [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 - 79700 3.4.22.27 [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 - 79356 3.4.22.27 [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 - 79921 3.4.22.27 [[2',3'-difluoro-4'-(2-methylpropyl)biphenyl-2-yl]oxy]acetaldehyde - 79698