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3.4.22.38: cathepsin K

This is an abbreviated version!
For detailed information about cathepsin K, go to the full flat file.

Word Map on EC 3.4.22.38

Reaction

Broad proteolytic activity. With small-molecule substrates and inhibitors, the major determinant of specificity is P2, which is preferably Leu, Met > Phe, and not Arg =

Synonyms

Cat K, Cat-K, cath K, cathepsin K, cathepsin O, Cathepsin O2, cathepsin-K, catK, Ctk, CTSK, Human osteoclast cathepsin K, More, OC-2 protein, rhCK

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.22 Cysteine endopeptidases
                3.4.22.38 cathepsin K

Inhibitors

Inhibitors on EC 3.4.22.38 - cathepsin K

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
((S)-1-[1-[4(R,S)-((S)-2-benzyloxycarbonylamino-4-methylpentanoylamino)-3-oxoazepan-1-yl]methanoyl]-3-methylbutl)carbamic acid benzyl ester
-
the faster eluting diastereomer C34H46N4O7*0.4H2O; the slower eluting diastereomer C34H46N4O7*0.3H2O
((S)-1-[[(3R,S)-((S)-2-benzyloxycarbonylamino-4-methylpentanoylamino)-3-oxopiperidin-1-yl]methanoyl]-3-methylbutyl)carbamic acid benzyl ester
-
-
((S)-1-[[(3R,S)-((S)-2-benzyloxycarbonylamino-4-methylpentanoylamino)-4-oxopyrrolidin-1-yl]methanoyl]-3-methylbutyl)carbamic acid benzyl ester
-
-
((S)-1-[[(3R,S)-((S)-2-benzyloxycarbonylmethylamino-4-methylpentanoylamino)-4-oxopyrrolidin-1-yl]methanoyl]-3-methylbutyl)carbamic acid benzyl ester
-
-
(1'S)-7-(1-aminoethyl)-2-(2-methoxyphenyl)pyrazolo[1,5-a] pyrimidine hydrochloride
-
(1'S)-7-(1-aminoethyl)-2-(3-trifluoromethylphenyl)pyrazolo-[1,5-a]pyrimidine hydrochloride
-
(1'S)-7-(1-aminoethyl)-2-benzyl-3-phenylpyrazolo[1,5-a]pyrimidine hydrochloride
-
(1'S)-7-(1-aminoethyl)-2-phenylpyrazolo[1,5-a]pyrimidine hydrochloride
-
(1'S)-7-(1-aminoethyl)pyrazolo[1,5-a]pyrimidine-3-(N-methylcarboxamide) hydrochloride
-
(1'S)-7-(1-aminoethyl)pyrazolo[1,5-a]pyrimidine-3-carboxylate hydrochloride
-
(11R,12R)-14,14-difluoro-34-(methylsulfanyl)-N-(prop-2-yn-1-yl)-11,12,13,14,15,16-hexahydro[11,21:22,31-terphenyl]-12-carboxamide
-
(1R)-1-benzyl-2-methylpropyl [(1S)-1-formylpentyl]carbamate
-
-
(1R)-1-benzyl-2-methylpropyl [(1S)-1-[(E)-[(morpholin-4-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
(1R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
(1R,2R)-2-[1-benzyl-5-[4-(methylsulfanyl)phenyl]-1H-1,2,3-triazol-4-yl]-N-(cyanomethyl)-5,5-difluorocyclohexanecarboxamide
(1R,2R)-5,5-dichloro-2-[4-[4-(methanesulfonyl)phenyl]-1-(2,2,2-trifluoroethyl)-1H-pyrrol-3-yl]-N-(prop-2-yn-1-yl)cyclohexane-1-carboxamide
-
(1R,2R)-5,5-dichloro-N-(1-cyanocyclopropyl)-2-[4-[4-(methylsulfonyl)phenyl]-1-(2,2,2-trifluoroethyl)-1H-pyrazol-3-yl]cyclohexanecarboxamide
-
i.e. MK-1256, a nonbasic, nitrile-containing cathepsin K inhibitor, that shows high selectivity for Cat K, 1100fold versus Cat B, L, S, C, H, Z, and V, 110fold versus Cat F
(1R,2R)-5,5-difluoro-2-[4-[4-(methanesulfonyl)phenyl]-1-(2,2,2-trifluoroethyl)-1H-pyrrol-3-yl]-N-(prop-2-yn-1-yl)cyclohexane-1-carboxamide
-
(1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carbonyl)cyclohexane-1-carboxamide
-
(1R,2R)-N-(1-cyanocyclopropyl)-5,5-difluoro-2-[4-[4-(methylsulfonyl)phenyl]-1-(2,2,2-trifluoroethyl)-1H-pyrazol-3-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-2-(4-[4-[(difluoromethyl)sulfanyl]phenyl]pyridin-3-yl)-5,5-difluorocyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[1-methyl-4-[4-(methylsulfanyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[1-methyl-4-[4-(methylsulfonyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-methyl-4-[4-(methylsulfanyl)phenyl]-1,3-thiazol-5-yl]cyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-[4-(methylsulfanyl)phenyl]pyridin-3-yl]cyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-1-oxidopyridin-4-yl]cyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]pyridin-4-yl]cyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[4-[4-(methylsulfonyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[5-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
(1R,2S)-N-(cyanomethyl)-2-[2-[4-(methylsulfanyl)phenyl]ethyl]cyclohexanecarboxamide
-
-
(1S)-1-methyl-2-phenylethyl [(1S)-1-formylpentyl]carbamate
-
-
(1S)-1-methyl-2-phenylethyl [(1S)-1-[(E)-[(morpholin-4-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
(1S)-1-[(5,6-dichloro-1H-benzimidazol-1-yl)methyl]-2,2-dimethylpropyl [(1S)-1-methyl-2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamate
-
-
(1S)-1-[(5,6-dichloro-1H-benzimidazol-1-yl)methyl]-2,2-dimethylpropyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-([[(6-fluoropyridin-2-yl)carbonyl]amino]acetyl)pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-methyl-2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-[oxo(1H-pyrazol-5-ylamino)acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-[[(morpholin-4-ylcarbonyl)amino]acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([4-[4-(trifluoromethyl)phenyl]-1H-imidazol-1-yl]methyl)propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([4-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-[(3-pyridin-3-yl-1H-pyrazol-1-yl)methyl]propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-[(3-pyridin-4-yl-1H-pyrazol-1-yl)methyl]propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-[[3-(trifluoromethyl)-1H-pyrazol-1-yl]methyl]propyl [(1S)-1-methyl-2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamate
-
-
(1S)-2,2-dimethyl-1-[[3-(trifluoromethyl)-1H-pyrazol-1-yl]methyl]propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
-
-
(2E,4E)-5-(1-hydroxy-2,6,6-trimethyl-4-oxocyclohex-2-en-1-yl)-3-methylpenta-2,4-dienoic acid
-
(2R)-2-[3'-[2-(4-tert-butylpiperazin-1-yl)-1,3-thiazol-4-yl]biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
-
-
(2R)-3,3-dimethyl-1-(5-phenyl-1,3,4-oxadiazol-2-yl)butan-2-yl [(3S)-1,2-dioxo-1-[[(1S)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(2R)-3,3-dimethyl-1-[2-oxo-3-[4-(trifluoromethyl)phenyl]imidazolidin-1-yl]butan-2-yl [(3S)-1,2-dioxo-1-(1H-pyrazol-5-ylamino)heptan-3-yl]carbamate
-
-
(2R)-3,3-dimethyl-1-[3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]butan-2-yl [(3S)-1,2-dioxo-1-(1H-pyrazol-5-ylamino)heptan-3-yl]carbamate
-
-
(2R)-3,3-dimethyl-1-[4-[4-(trifluoromethyl)phenyl]-1H-imidazol-1-yl]butan-2-yl [(3S)-1,2-dioxo-1-(1,3-thiazol-2-ylamino)heptan-3-yl]carbamate
-
-
(2R)-3,3-dimethyl-1-[4-[4-(trifluoromethyl)phenyl]-1H-imidazol-1-yl]butan-2-yl [(3S)-1,2-dioxo-1-(1H-pyrazol-5-ylamino)heptan-3-yl]carbamate
-
-
(2R)-3,3-dimethyl-1-[4-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]butan-2-yl [(3S)-1,2-dioxo-1-(1H-pyrazol-5-ylamino)heptan-3-yl]carbamate
-
-
(2R)-4-fluoro-4-methyl-N-(3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl)-2-((R)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2R)-N-(cyanomethyl)-2-[3'-(2-[[3-(dimethylamino)pyrrolidin-1-yl]methyl]-1,3-thiazol-4-yl)biphenyl-3-yl]-4-methylpentanamide
-
-
(2R)-N-(cyanomethyl)-4-methyl-2-[3'-[2-(piperazin-1-ylmethyl)-1,3-thiazol-4-yl]biphenyl-3-yl]pentanamide
-
-
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)-[1,1'-biphenyl]-3-yl]pentanamide
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methylpiperazin-1-yl)biphenyl-3-yl]pentanamide
-
-
(2R)-N-cyano-4-methyl-2-[4'-(piperazin-1-yl)[1,1'-biphenyl]-3-yl]pentanamide
-
(2S)-1-[5-(4-fluorophenyl)-1,3,4-oxadiazol-2-yl]-3,3-dimethylbutan-2-yl [(3S)-1,2-dioxo-1-[(pyridin-3-ylmethyl)amino]heptan-3-yl]carbamate
-
-
(2S)-1-[5-(4-fluorophenyl)-1,3,4-oxadiazol-2-yl]-3,3-dimethylbutan-2-yl [(3S)-1,2-dioxo-1-[[(1S)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(2S)-2-(biphenyl-2-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
-
-
(2S)-2-(biphenyl-3-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
-
-
(2S)-2-(biphenyl-4-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
-
-
(2S)-2-amino-N-[(1S)-2-(biphenyl-4-yl)-1-cyanoethyl]butanamide
-
-
(2S)-3,3-dimethyl-1-(5-phenyl-1,3,4-oxadiazol-2-yl)butan-2-yl [(3S)-1,2-dioxo-1-[[(1S)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(2S)-3,3-dimethyl-1-[5-[4-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]butan-2-yl [(3S)-1,2-dioxo-1-[(2-oxo-1,3-oxazolidin-3-yl)amino]heptan-3-yl]carbamate
-
-
(2S)-3-methyl-1-(5-phenyl-1,3,4-oxadiazol-2-yl)butan-2-yl [(3S)-1,2-dioxo-1-[[(1S)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(2S)-4,4-dichloro-N-(1-cyanocyclopropyl)-2-([(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]amino)butanamide
-
-
(2S)-4-fluoro-4-methyl-N-(1-(2-(methylsulfonyl)phenyl)-3-oxopiperidin-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-4-fluoro-4-methyl-N-(1-(methylsulfonyl)-3-oxoazepan-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-4-fluoro-4-methyl-N-(1-(methylsulfonyl)-4-oxopyrrolidin-3-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-4-fluoro-4-methyl-N-(3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
racemate
(2S)-4-fluoro-4-methyl-N-(3-oxo-1-(pyridin-2-ylsulfonyl)piperidin-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-4-fluoro-4-methyl-N-(3-oxo-1-phenylpiperidin-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-4-fluoro-4-methyl-N-(3-oxoazepan-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-4-fluoro-4-methyl-N-(4-oxo-1-(pyridin-2-ylsulfonyl)pyrrolidin-3-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-4-fluoro-4-methyl-N-(4-oxopyrrolidin-3-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-N-(1-(benzylsulfonyl)-3-oxoazepan-4-yl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-N-(1-acetyl-4-oxopyrrolidin-3-yl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-N-(1-benzoyl-4-oxopyrrolidin-3-yl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-N-(1-cyanocyclopropyl)-4,4,4-trifluoro-2-([(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]amino)butanamide
-
-
(2S)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-2-(3-phenoxyphenoxy)pentanamide
-
-
(2S)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-2-(4-phenoxyphenoxy)pentanamide
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-
(2S)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-2-phenoxypentanamide
-
-
(2S,3S)-3-([(1S)-3-methyl-1-[(2-methylpropoxy)methyl]butyl]carbamoyl)oxirane-2-carboxylate
-
through screening, a potent orally active cathepsin K inhibitor named NC-2300 is obtained, which suppresses autoimmune inflammation of the joints as well as osteoclastic bone resorption in an adjuvant-induced arthritis animal model in rats. Computer-assisted simulation of the cathepsin K/NC-2300 complex indicates that NC-2300 blocks the active-site cleft where Cys25 and His162 of cathepsin K form the catalytic site. Pharmacological inhibition of cathepsin K results in defective Toll-like receptor 9 signaling in dendritic cells in response to unmethylated CpG DNA, which in turn leads to an attenuated induction of T helper 17 cells, without affecting the antigen-presenting ability of dendritic cells
(3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetic acid
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
(3S)-1-(1H-indol-6-ylcarbonyl)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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-
(3S)-1-(2,2-dimethylpropoxy)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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-
(3S)-1-(benzylcarbamoyl)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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-
(3S)-1-(benzylsulfonyl)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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-
(3S)-1-(biphenyl-4-ylcarbonyl)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-(dicyclopentylmethoxy)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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-
(3S)-1-(heptan-4-yloxy)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-([(2R)-1-[5-(4-fluorophenyl)-1,3,4-oxadiazol-2-yl]-3,3-dimethylbutan-2-yl]oxy)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(3S)-2-oxopiperidin-3-yl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-([(3S)-1-[(3,5-dimethyl-1,2-oxazol-4-yl)carbonyl]-4,4-dimethylpyrrolidin-3-yl]oxy)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-benzyl-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-tert-butoxy-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[(thiophen-2-ylmethyl)amino]heptan-3-yl]carbamate
-
-
(3S)-1-tert-butoxy-4,4-dimethylpyrrolidin-3-yl [(3S)-1-(ethylamino)-1,2-dioxoheptan-3-yl]carbamate
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-
(3S)-1-[(1-benzylcyclobutyl)methoxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[(2,4-dimethylpentan-3-yl)oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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-
(3S)-1-[(3,3-dimethylbutan-2-yl)oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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-
(3S)-1-[[(2R)-3,3-dimethyl-1-[5-[4-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]butan-2-yl]oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-(1H-pyrazol-5-ylamino)heptan-3-yl]carbamate
-
-
(3S)-1-[[(2R)-3,3-dimethyl-1-[5-[4-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]butan-2-yl]oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1S)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[[(3R)-2,2-dimethyl-6-phenylhexan-3-yl]oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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-
(3S)-1-[[(3R)-4,4-dimethyl-1-phenylpentan-3-yl]oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[[(3S)-1-(1-benzothiophen-2-ylcarbonyl)-4,4-dimethylpyrrolidin-3-yl]oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[[(3S)-1-benzoyl-4,4-dimethylpyrrolidin-3-yl]oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[[(3S)-4,4-dimethyl-1-phenylpentan-3-yl]oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[[1-(4-fluorobenzyl)cyclobutyl]methoxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-(1H-pyrazol-5-ylamino)heptan-3-yl]carbamate
-
-
(3S)-2-oxo-N-[(1R)-1-phenylethyl]-3-[([[1-(2-phenylethyl)cyclobutyl]oxy]acetyl)amino]heptanamide
-
-
(3S)-2-oxo-N-[(1R)-1-phenylethyl]-3-[([[1-(3-phenylpropyl)cyclobutyl]oxy]acetyl)amino]heptanamide
-
-
(3S)-3-([[(2-methyl-1-phenylpropan-2-yl)oxy]acetyl]amino)-2-oxo-N-[(1R)-1-phenylethyl]heptanamide
-
-
(3S)-4,4-dimethyl-1-(1,2-oxazol-5-ylcarbonyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-(4-phenylbutanoyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-(naphthalen-2-ylcarbonyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-(pentan-3-yloxy)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-(phenylacetyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-(phenylcarbamoyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-(phenylsulfonyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-(pyridin-3-ylcarbonyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-[(2,2,4,4-tetramethylpentan-3-yl)oxy]pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-[(2-phenylethyl)carbamoyl]pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-[4-(trifluoromethyl)benzoyl]pyrrolidin-3-yl [(3S)-1,2-dioxo-1-(1H-pyrazol-3-ylamino)heptan-3-yl]carbamate
-
-
(4-[[(2S)-2-([1-[([1,1'-biphenyl]-3-yl)amino]cyclohexane-1-carbonyl]amino)butyl]amino]phenoxy)acetic acid
-
(4R)-N-(1-cyanocyclopropyl)-5,5,5-trifluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
(4S)-N-(1-cyanocyclopropyl)-5,5,5-trifluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
(S)-N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(S,S)-piperidine-4-carboxylic acid [1-[1-(benzoxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
1,3-bis(CBZ-Leu-NH)-2-propanone
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([2-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-3-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-4-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(thiophen-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[methyl(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(methylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(phenylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[(1-[4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamido]cyclohexane-1-carbonyl)amino]-L-erythro-hex-2-ulose
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-([[4-([[(dimethylamino)methyl]sulfonyl]amino)phenyl]carbonyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([2-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-fluoro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([4-[(ethylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2,4-dimethyl-1,3-thiazol-5-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-(methylsulfamoyl)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-([[4-(1-methylethyl)-1,3-thiazol-2-yl]sulfonyl]amino)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-sulfamoylphenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methyl-1H-imidazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methylethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2,2,2-trifluoroethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2-methylphenyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methylpyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(5-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[4-methyl-N-(thiophen-3-ylcarbonyl)-L-leucyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([4-[(benzylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([4-[(butylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([4-[(cyclopropylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-chloropyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(3-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(4-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(cyclohexylmethyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,5-(N-benzyloxycarbonylleucyl)carbohydrazide
-
1,6-dimethyl-1,2-dihydrophenanthro[1,2-b]furan-10,11-dione
-
1-(3-chlorophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
-
-
1-(4-chlorophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
-
-
1-(4-cyanophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
-
-
1-(4-cyclohexylphenoxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
-
1-(4-ethylphenoxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
-
1-(biphenyl-2-ylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
-
1-(biphenyl-3-ylamino)-N-[(1R)-2-[(4-methoxyphenyl)amino]-1-methylethyl]cyclohexanecarboxamide
-
-
1-(biphenyl-3-ylamino)-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]butyl]cyclohexanecarboxamide
-
-
1-(biphenyl-3-ylamino)-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]pentyl]cyclohexanecarboxamide
-
-
1-(biphenyl-3-ylamino)-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]propyl]cyclohexanecarboxamide
-
-
1-(biphenyl-3-ylamino)-N-[(1S)-2-[(4-methoxyphenyl)amino]-1-methylethyl]cyclohexanecarboxamide
-
-
1-(biphenyl-3-ylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
-
1-(biphenyl-3-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
-
1-(biphenyl-4-ylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
-
1-(biphenyl-4-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
-
1-(N-benzyloxycarbonyl-leucyl)-5-(N-Boc-phenylalanylleucyl)carbohydrazide
-
cathepsin K inhibitor
1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
-
1-(phenoxymethyl)cyclobutyl (3aR,6aS)-6-oxohexahydro-1H-furo[3,2-c]pyrazole-1-carboxylate
-
1-(phenoxymethyl)cyclobutyl (3aS,6aR)-3-oxohexahydro-4H-furo[3,2-b]pyrrole-4-carboxylate
-
1-benzylcyclopentyl [(1S)-1-formylpentyl]carbamate
-
-
1-benzylcyclopentyl [(1S)-1-[(E)-[(2,3-dihydro-1H-indol-1-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
1-benzylcyclopentyl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
1-cyano-3-azetidinyl cyclohexylmethyl ether
-
IC 50: 20 nM
1-ethyl-2-[(4-methylpiperazin-1-yl)methyl]-6-[3-(trifluoromethyl)phenyl]-2,3-dihydro-1H-indole-4-carbonitrile
-
1-Isopropyl-2-methylpropyl (1S)-1-cyclohexylmethyl-2,3-dioxo-3-[(thien-2-ylmethyl)-amino]propylcarbamate
-
IC50: 14 nM
1-Isopropyl-2-methylpropyl (1S)-1-isoprpyl-2,3-dioxo-3-[(thien-2-ylmethyl)-amino]propylcarbamate
-
IC50: 47 nM
1-Isopropyl-2-methylpropyl (1S)-1-methyl-2,3-dioxo-3-[(thien-2-ylmethyl)-amino]propylcarbamate
-
IC50: 360 nM
1-Isopropyl-2-methylpropyl (1S)-1-[(isoxazol-3-ylamino)(oxo)acetyl]pentylcarbamate
-
IC50: 5.1 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(1,3,4-thiadiazol-2-ylamino)acetyl]pentylcarbamate
-
IC50: 83 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(1,3-thiazol-2-ylamino)acetyl]pentylcarbamate
-
IC50: 40 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(1H-pyrazol-5-ylamino)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(isoquinolin-2-ylamino)acetyl]pentylcarbamate
-
IC50: 4.8 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(pyrazin-2-ylamino)acetyl]pentylcarbamate
-
IC50: 52 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(pyridin-2-ylamino)acetyl]pentylcarbamate
-
IC50: 32 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(pyridin-3-ylamino)acetyl]pentylcarbamate
-
IC50: 95 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(quinolin-2-ylamino)acetyl]pentylcarbamate
-
IC50: 250 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-2-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-4-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(3-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(4-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(thien-2-ylmethyl)-amino]acetyl]pentylcarbamate
-
IC50: 9.2 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclohexyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclopentyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-ethyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isopropyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-3-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(3-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.71 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-bromo-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.24 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-cyano-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.91 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-fluoro-1H-indazol-3-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.26 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(3,3-dimethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(cyclopropylmethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-2,3-dioxo--1-phenyl-3-[(thien-2-ylmethyl)-amino]propylcarbamate
-
IC50: 27 nM
1-Isopropyl-2-methylpropyl (1S)-3-methyl-1-[oxo[(thien-2-ylmethyl)-amino]acetyl]butylcarbamate
-
IC50: 24 nM
1-Isopropyl-2-methylpropyl (1S,2S)-2-methyl-1-[oxo[(thien-2-ylmethyl)-amino]acetyl]butylcarbamate
-
IC50: 87 nM
1-Isopropyl-2-methylpropyl 2,3-dioxo-3-[(thien-2-ylmethyl)-amino]propylcarbamate
-
IC50: 0.012 mM
1-methylethyl (2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazinecarboxylate
-
-
1-[(1H-imidazol-4-yl)methyl]-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole
-
1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-(3-methylphenyl)urea
-
-
1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-phenylurea
-
-
1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-[3-(trifluoromethyl)phenyl]urea
-
-
13-methyl-2H,10H-[1,3]benzodioxolo[5,6-c][1,3]dioxolo[4,5-i]phenanthridin-13-ium
-
2,2'-N,N'-bis(benzyloxycarbonyl)-L-leucinylcarbohydrazide
-
-
2-(2,4-dihydroxyphenyl)-5,7-dihydroxy-6-[5-methyl-2-(prop-1-en-2-yl)hex-4-en-1-yl]-2,3-dihydro-4H-1-benzopyran-4-one
-
2-(3-methoxyphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-(3-methylphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-(3-tert-butylphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-(4-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-3-oxoazepan-1-ylsulfonyl)pyridine 1-oxide
-
-
2-(biphenyl-3-yl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-(cyclohexylamino)pyrimidine-4-carbonitrile
-
-
2-(cyclohexylmethyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-amino-4-bromo-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
-
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
2-cyano-4-(cyclohexylamino)-N-(4-methoxyphenethyl)-pyrimidine-5-carboxamide
-
-
2-cyano-4-(cyclohexylamino)-N-[2-(3-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-(cyclohexylamino)-N-[2-(4-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-(cyclohexylamino)-N-[2-(4-pyrrolidin-1-ylphenyl)ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-(cyclohexylamino)-N-[2-[4-(4-methylpiperazin-1-yl)phenyl]ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[3-[2-(1H-imidazol-1-yl)ethoxy]-4-methoxyphenyl]ethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[3-[2-(1H-imidazol-1-yl)ethoxy]phenyl]ethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[4-[(1-methylpiperidin-4-yl)oxy]phenyl]ethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]ethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[4-[2-(1H-imidazol-1-yl)ethoxy]phenyl]ethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-(3-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-(4-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-(4-pyrrolidin-1-ylphenyl)ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-[3-(4-methylpiperazin-1-yl)phenyl]ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-[4-(4-methylpiperazin-1-yl)phenyl]ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-[(cyclohexylmethyl)(methyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-4-[[(4,4-difluorocyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[[(4,4-dimethylcyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-N-(1-methyl-4-phenylpiperidin-4-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-(4,5-dimethoxybiphenyl-2-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-(4-methoxyphenethyl)-4-(neopentylamino)pyrimidine-5-carboxamide
-
-
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-[(1-methyl-4-phenylpiperidin-4-yl)methyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-[(1R)-2-pyridin-2-yl-1-(pyrrolidin-1-ylmethyl)ethyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-[5-[(1-methylpiperidin-4-yl)oxy]biphenyl-2-yl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cycloheptyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-cycloheptyl-3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-cycloheptyl-4-[2-(dimethylamino)ethyl]-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-cycloheptyl-4-[3-(morpholin-4-yl)propyl]-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-cyclohexyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-cyclopentyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-methyl-1-phenylpropan-2-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
2-methylpropyl [(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamate
-
-
2-phenylethyl (4S)-4-[[(4S)-4-([[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamoyl]oxy)-3,3-dimethylpyrrolidin-1-yl]oxy]-3,3-dimethylpyrrolidine-1-carboxylate
-
-
2-phenylpropan-2-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
2-[3-(hydroxymethyl)phenyl]-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-[[2-cyano-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methyl]-N-cyclohexyl-1,3-dioxo-2,8-diazaspiro[4.5]decane-8-carboxamide
-
-
2-[[2-cyano-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methyl]-N-methyl-1,3-dioxo-2,8-diazaspiro[4.5]decane-8-carboxamide
-
-
3,3'-[(3-carboxy-4-oxocyclohexa-2,5-dien-1-ylidene)methylene]bis(6-hydroxybenzoic acid)
-
3,5-dioxo-2-phenyl-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3,5-dioxo-2-[3-(propan-2-yl)phenyl]-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3,5-dioxo-4-(2-phenylethyl)-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3,5-dioxo-4-phenyl-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3,5-dioxo-4-propyl-2-[4-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3,5-dioxo-4-[2-(piperidin-1-yl)ethyl]-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2-[3-(propan-2-yl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-2-oxopropylcarbamate
-
-
3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxo-N-(phenylsulfonyl)pyrrolidine-1-carboxamide
-
-
3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxo-N-phenylpyrrolidine-1-carboxamide
-
-
3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxamide
-
-
3-(4-([4'-((1-[(cyanomethyl)carbamoyl]cyclohexyl)carbamoyl)biphenyl-4-yl]oxy)piperidin-1-yl)propanoic acid
-
-
3-(4-[[(2S)-2-([[1-(biphenyl-3-ylamino)cyclohexyl]carbonyl]amino)butyl]amino]phenoxy)propanoic acid
-
-
3-(benzyloxy)-1-cyanoazetidine
-
IC 50: 40 nM
3-(cyclohexylamino)benzonitrile
-
-
3-amino-4-[(tetrahydro-2-furanylmethyl)amino] benzoic acid
-
-
3-benzylpentan-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
3-bromo-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
3-bromo-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
-
moderate inhibition
3-[(6-deoxy-L-mannopyranosyl)oxy]-5-hydroxy-2-(4-methoxyphenyl)-8-(3-methylbut-2-en-1-yl)-4-oxo-4H-1-benzopyran-7-yl D-glucopyranoside
-
3-[(benzyloxy)methyl]-1-cyanopyrrolidine
-
IC 50: 100 nM
3-[4-([(2S)-2-[(N-biphenyl-3-yl-L-leucyl)amino]butyl]amino)phenoxy]propanoic acid
-
-
3-[[(2S)-2-[([3-acetyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
3-[[(2S)-2-[[(4-[[(4-aminophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
4'-(4-tert-butylpiperazin-1-yl)-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-4-carboxamide
-
-
4'-(4-tert-butylpiperazin-1-yl)-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]biphenyl-4-carboxamide
-
strong inhibition
4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-fluoro-4-methyl-1-oxopentan-2-yl]amino)-2,2,2-trifluoroethyl][1,1'-biphenyl]-4-sulfonic acid
-
4'-[(1S)-1-([(2S)-1-[(cyanomethyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2,2-trifluoroethyl][1,1'-biphenyl]-4-sulfonic acid
-
4'-[4-(tert-butylamino)piperidin-1-yl]-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-4-carboxamide
-
-
4'-[4-(tert-butylamino)piperidin-1-yl]-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]biphenyl-4-carboxamide
-
strong inhibition
4-(2-[(3R)-3-aminopyrrolidin-1-yl]-1,3-thiazol-4-yl)-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
4-(3,4-dimethylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-cyanophenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-cyclopentylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-methylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-tert-butylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(4-acetylpiperazin-1-yl)-5-amino-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
-
-
4-(cyclohexylamino)-6-(piperazin-1-yl)-1,3,5-triazine-2-carbonitrile
-
4-(cyclohexylamino)pyrimidine-2-carbonitrile
-
-
4-(dimethylamino)-N-[1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]benzamide
-
-
4-(trifluoromethoxy)-N-(1-[[(1S)-1-([5-[3-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]carbonyl)butyl]carbamoyl]cyclohexyl)benzamide
-
-
4-(trifluoromethoxy)-N-(1-[[(1S)-1-([5-[4-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]carbonyl)butyl]carbamoyl]cyclohexyl)benzamide
-
-
4-amino-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
4-amino-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
-
moderate inhibition
4-benzyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-bromo-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
4-bromo-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
-
moderate inhibition
4-butyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-cyano-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
-
moderate inhibition
4-cycloheptyl-6-propylpyrimidine-2-carbonitrile
-
-
4-cycloheptyl-6-[3-(piperidin-1-yl)propyl]pyrimidine-2-carbonitrile
4-cyclohexyl-6-propylpyrimidine-2-carbonitrile
-
-
4-cyclooctyl-6-propylpyrimidine-2-carbonitrile
-
-
4-cyclopentyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-dihydrotanshinone
potent exosite inhibitor of cathepsin K
4-ethyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-fluoro-N-(3-oxoazepan-4-yl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-(4-oxopyrrolidin-3-yl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-(5-oxo-2-phenylpiperidin-4-yl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-prop-2-yn-1-yl-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
4-fluoro-N-[1-(methylsulfonyl)-3-oxoazepan-4-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[1-(methylsulfonyl)-4-oxopyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]benzamide
-
-
4-fluoro-N-[2-[2-(methylsulfonyl)phenyl]-5-oxopiperidin-4-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[3-oxo-1-(pyridin-2-ylsulfonyl)piperidin-4-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[4-oxo-1-(phenylcarbamoyl)pyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[4-oxo-1-(phenylcarbonyl)pyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[4-oxo-1-(pyridin-2-ylsulfonyl)pyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[4-oxo-1-[(phenylsulfonyl)carbamoyl]pyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-methyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-Morpholinecarbonyl-Ala-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-aminohexanoic acid-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-Gly-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-Ile-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-Leu-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-Met-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-methionine dioxide-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-Phe-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-Val-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-phenyl-6-propylpyrimidine-2-carbonitrile
-
-
4-propyl-6-[2-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-propyl-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
moderate cathepsin K potency
4-propyl-6-[4-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-[(2,2-dimethylpropyl)(4-iodobenzyl)amino]pyrimidine-2-carbonitrile
-
-
4-[(2,2-dimethylpropyl)amino]-5-(3-[4-[(4-methoxyphenyl)sulfonyl]piperazin-1-yl]prop-1-yn-1-yl)pyrimidine-2-carbonitrile
-
-
4-[(2,2-dimethylpropyl)amino]-5-[3-(pyridin-3-yloxy)prop-1-yn-1-yl]pyrimidine-2-carbonitrile
-
-
4-[(2,2-dimethylpropyl)amino]-5-[3-[4-(4-methylpiperazin-1-yl)phenyl]prop-1-yn-1-yl]pyrimidine-2-carbonitrile
-
-
4-[(2,2-dimethylpropyl)[4-(1H-1,2,4-triazol-1-ylmethyl)benzyl]amino]pyrimidine-2-carbonitrile
-
-
4-[(2,2-dimethylpropyl)[4-(3-piperidin-1-ylprop-1-yn-1-yl)benzyl]amino]pyrimidine-2-carbonitrile
-
-
4-[(2,2-dimethylpropyl)[4-[3-(1H-1,2,4-triazol-1-yl)prop-1-yn-1-yl]benzyl]amino]pyrimidine-2-carbonitrile
-
-
4-[(2,2-dimethylpropyl)[4-[3-(4-methylpiperazin-1-yl)prop-1-yn-1-yl]benzyl]amino]pyrimidine-2-carbonitrile
-
-
4-[2-(1,4'-bipiperidin-1'-yl)-1,3-thiazol-4-yl]-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
4-[2-(1,4'-bipiperidin-1'-yl)-1,3-thiazol-4-yl]-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
-
strong inhibition
4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
-
4-[2-(4-methylpiperazin-1-yl)-4,5-dihydro-1,3-thiazol-4-yl]-N-(1-[[(3S,4R)-2-oxo-4-phenoxyazetidin-3-yl]carbamoyl]cyclohexyl)benzamide
-
4-[2-(4-tert-butylpiperazin-1-yl)-1,3-thiazol-4-yl]-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
4-[2-(4-tert-butylpiperazin-1-yl)-1,3-thiazol-4-yl]-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
-
strong inhibition
4-[2-(dimethylamino)ethyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-[2-chloro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[2-[(3R)-3-aminopyrrolidin-1-yl]-1,3-thiazol-4-yl]-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
-
strong inhibition
4-[3-(dimethylamino)propyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-[3-(methylsulfonyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[3-(morpholin-4-yl)propyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-[3-(pentan-3-ylamino)propyl]-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-[3-(piperidin-1-yl)propyl]-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-[3-(tert-butylamino)propyl]-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-[4-chloro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[benzyl(2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
-
-
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzoic acid
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
4-[[4-[3-(1,4'-bipiperidin-1'-yl)prop-1-yn-1-yl]benzyl](2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
-
-
4-[[4-[3-(4-acetylpiperazin-1-yl)prop-1-yn-1-yl]benzyl](2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
-
-
5-(3-[4-[(3-chloropropyl)sulfonyl]piperazin-1-yl]prop-1-yn-1-yl)-4-[(2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
-
-
5-amino-4-(3-hydroxyazetidin-1-yl)-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
-
-
5-amino-4-(bicyclo[2.2.1]hept-2-ylamino)-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-(cyclohexylamino)-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-(cyclopentylamino)-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-morpholin-4-yl-6-(phenylamino)pyrimidine-2-carbonitrile
-
-
5-amino-4-morpholin-4-yl-6-(tetrahydrofuran-3-ylamino)pyrimidine-2-carbonitrile
-
-
5-amino-4-morpholin-4-yl-6-piperidin-1-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-morpholin-4-yl-6-pyrrolidin-1-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-[(1,1-dioxidotetrahydrothiophen-3-yl)amino]-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
-
-
5-amino-4-[(1-methylethyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-[(1-methylpropyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-[(2,2-dimethylpropyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-[(2-methoxyethyl)amino]-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
-
-
5-amino-4-[(2-methylpropyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-[(2-methylpropyl)amino]-6-piperazin-1-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-[(2-methylpropyl)amino]-6-[(tetrazolidin-5-ylmethyl)amino]pyrimidine-2-carbonitrile
-
-
5-bromo-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
-
5-bromo-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)thiophene-2-carboxamide
-
-
5-bromo-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]thiophene-2-carboxamide
-
moderate inhibition
5-[3-(1,3-dihydro-2H-isoindol-2-yl)prop-1-yn-1-yl]-4-[(2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
-
-
5-[3-(3,4-dihydroisoquinolin-2(1H)-yl)prop-1-yn-1-yl]-4-[(2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
-
-
5-[3-(4,5-dichloro-1H-imidazol-1-yl)prop-1-yn-1-yl]-4-[(2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
-
-
6,8-dihydroxy-3-(3,4,5-trihydroxyphenyl)-2,3-dihydro-1,4-benzodioxin-2-yl 3,4,5-trihydroxybenzoate
-
6-(4-chlorobenzyl)-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-(2-cyclooctylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-(2-piperidin-1-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(3,3,3-trifluoropropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(3,3-dimethylbutyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-(4,4,4-trifluorobutyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(4,4-dimethylpentyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-cyclohexyl-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-[2-(3-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-[2-(piperidin-1-yl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(bromomethyl)-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(cyclohexylamino)-9-[(2S,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-9H-purine-2-carbonitrile
-
-
6-(cyclohexylamino)-9-[2-(4-methylpiperazin-1-yl)ethyl]-9H-purine-2-carbonitrile
-
-
6-(cyclohexylamino)pyrazine-2-carbonitrile
-
-
6-(cyclohexylamino)pyridine-2-carbonitrile
-
-
6-benzyl-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-benzyl-7-cyclohexyl-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-cyano-2-(3-trifluoromethyl-phenyl)-3,5-dioxo-1,2,4-triazine
-
poor catK potency
6-[(1'-acetyl-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[(4,5-dichloro-1H-imidazol-1-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[(5,5-dimethyl-2,4-dioxo-1,3-oxazolidin-3-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[(8-acetyl-1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[(8-benzyl-1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[4-[(diethylamino)methyl]benzyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[4-[3-(diethylamino)propoxy]-3-(trifluoromethyl)phenyl]-1-ethyl-2,3-dihydro-1H-indole-4-carbonitrile
-
6-[[4-(1-acetyl-1,2,3,6-tetrahydropyridin-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
6-[[4-(1-acetylpiperidin-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
6-[[4-(4-acetyl-1,4-diazepan-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-[[4-(4-acetylpiperazin-1-yl)-3-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[8-(2,4-dimethoxyphenyl)-1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl]methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethyl-propyl)-6-(1,3-dioxo-2,8-diaza-spiro[4.5]dec-2-ylmethyl)-7H-pyrrolo[2,3-d] pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-(1H-1,2,3-triazol-1-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-(1H-imidazol-1-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(1'-methyl-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(1,3-dioxo-2,8-diazaspiro[4.5]decan-2-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-3-propyl-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-8-propyl-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-[(2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(3-methyl-2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-[(5-fluoro-1'-methyl-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(5-fluoro-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-[(5-methoxy-1'-methyl-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(5-methoxy-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-[(pyridin-4-yloxy)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[4-(4-methylpiperazin-1-yl)benzyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[4-(morpholin-4-yl)benzyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[[2-oxo-1'-(propan-2-yl)spiro[indole-3,4'-piperidin]-1(2H)-yl]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[[4-(4-fluorophenyl)piperazin-1-yl]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[[8-(morpholin-4-ylacetyl)-1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2-cyclohexylethyl)-6-(4-methoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[(pyridin-2-yloxy)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[(pyridin-2-ylsulfanyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[[methyl(phenyl)amino]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
AAE581
-
-
acetyl-strophanthidin
-
AFG-495
-
-
-
antipain
98.91% inhibition at 0.1 mM
Aprotinin
25.08% inhibition at 0.1 mM
balicatib
benzofuran-2-carboxylic acid [(S)-3-methyl-1-[2-oxo-3-(pyridin-2-ylsulfonylamino)propylcarbamoyl]butyl]amide
-
-
benzyl (1-[(cyanomethyl)carbamoyl]-2-hydroxypropyl)carbamate
-
-
benzyl (2S)-2-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)-4-methylpentanoate
-
-
benzyl (2S,3R)-1-(cyanomethylamino)-3-hydroxy-1-oxobutan-2-ylcarbamate
-
weak inhibition
benzyl (2S,3S)-1-(cyanomethylamino)-3-methyl-1-oxopentan-2-ylcarbamate
-
weak inhibition
benzyl 1-cyano-3-pyrrolidinylcarbamate
-
IC 50: 40 nM
benzyl [(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamate
-
-
benzyl [(1S)-1-[(cyanomethyl)carbamoyl]-2,2-dimethylpropyl]carbamate
-
weak inhibition
benzyl [(1S)-2-[(cyanomethyl)amino]-1-(naphthalen-2-ylmethyl)-2-oxoethyl]carbamate
benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate
benzyl [(5S,13S)-11,15-dimethyl-5-(2-methylpropyl)-3,6,9,12-tetraoxo-1-phenyl-2-oxa-4,7,11-triazahexadecan-13-yl]carbamate
-
benzyl [1-[(cyanomethyl)carbamoyl]cyclohexyl]carbamate
benzyl [1-[(cyanomethyl)carbamoyl]cyclopentyl]carbamate
-
weak inhibition
Benzyloxycarbonyl-Phe-Ala-CHN2
-
-
Benzyloxycarbonyl-Phe-Phe-CHN2
-
-
biphenyl-4-yl (4S)-4-([[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamoyl]oxy)-3,3-dimethylpyrrolidine-1-carboxylate
-
-
biphenyl-4-ylmethyl (4S)-4-([[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamoyl]oxy)-3,3-dimethylpyrrolidine-1-carboxylate
-
-
BML-244
Boc-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
-
Boc-I
-
lysosomotropic, water-soluble polymer selective catK inhibitor. Inhibition of catK greatly reduces melanoma cell invasion through Matrigel basement membrane matrix and increases detection of internalized collagen
Boc-Phe-Leu-NHNH-CO-NHNH-Leu-Z
calpeptin
-
-
carbobenzyloxy-Phe-Phe-CH2F
-
-
carboxybenzoyl-Phe-Phe-CHN2
-
-
cathepsin K inhibitor II
-
-
cathepsin K propeptide
-
-
-
CatK-II
-
specific inhibitor
-
CatK-selective inhibitor II
chicken cystatin
-
-
-
chymostatin
CID444556
-
-
Co2+
5.09% residual activity at 5 mM
CRA-013783
-
-
Cu2+
24.86% residual activity at 5 mM
cystatin
-
different types, expression analysis in various cell types isolated from normal and neoplastic breast tissue, overview
-
cystatin C
-
dibenzyl [(2-oxopropane-1,3-diyl)bis[azanediyl[(2S)-4-methyl-1-oxopentane-1,2-diyl]]]biscarbamate
-
dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate
E-64d
-
-
E64d
-
-
EDTA
3.72% inhibition at 0.1 mM
ellipticine
-
ethyl (4S)-4-[(4-fluoro-N-[2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucyl)amino]-3-oxopiperidine-1-carboxylate
-
ethyl 3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxylate
-
-
ethyl 3-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-4-oxopyrrolidine-1-carboxylate
-
-
ethyl 4-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-3-oxoazepane-1-carboxylate
-
-
ethyl 4-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-3-oxopiperidine-1-carboxylate
-
-
ethyl 4-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-3-oxoazepane-1-carboxylate
-
-
ethyl 4-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-5-oxopiperidine-2-carboxylate
-
-
Ethyl 5-[((3S)-3[[(isopropyl-2-methylpropoxy)carbonyl]amide]-2-oxoheptanoyl)amino]-1H-pyrazole-4-carboxylate
-
IC50: 1.7 nM
ethyl N-[[(2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazino]carbonyl]-b-alaninate
-
-
ethyl N-[[(2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazino]carbonyl]glycinate
-
-
H-kininogen
-
natural inhibitor of cathepsin K, reversible, tight-binding competitive inhibitor
-
Hg2+
25.27% residual activity at 5 mM
Human squamous cell carcinoma antigen 1
-
i.e. SCCA1
-
iodoacetate
-
-
kushennol F
shows inhibitory effects on the bone resorption process related to cathepsin K
L-006235
L-13006235
-
shows no selectivity in cell-based assays over cathepsins B, L, and S
L-873724
L-kininogen
-
natural inhibitor of cathepsin K, reversible, tight-binding competitive inhibitor
-
leupeptazin
-
isolated from a liquid culture of soil Streptomyces sp. IS2-4
leupeptin
methyl (3S)-3-[(4-fluoro-N-[2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucyl)amino]-4-oxopyrrolidine-1-carboxylate
-
methyl 3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxylate
-
-
methyl 3-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-4-oxopyrrolidine-1-carboxylate
-
-
methyl 4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-fluoro-4-methyl-1-oxopentan-2-yl]amino)-2,2-difluoroethyl]biphenyl-4-sulfinate
-
-
methyl 4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2,2-trifluoroethyl]biphenyl-4-sulfinate
-
-
methyl 4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2-difluoroethyl]biphenyl-4-sulfinate
-
-
methyl 4'-[(1S)-1-([(2S)-1-[(cyanomethyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2-difluoroethyl]biphenyl-4-sulfinate
-
-
methyl 5-acetoxy-dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
-
-
methyl 5-hydroxy-7,12-dioxo-7,12-dihydrodinaphtho[1,2-b:2',3'-d]furan-6-carboxylate
-
methyl 5-hydroxy-dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
-
furanquinone from Paulownia tomentosa stem
methyl 5-methoxy dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
-
-
methyl 5-propoxy-dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
-
-
methyl methanethiolsulfonate
-
methyl N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-methioninate
-
-
methyl [[(2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazino]carbonyl]carbamate
-
-
MIV-701
-
-
MIV-701/710
-
-
-
MK-0674
MK-0822
-
-
MK-1256
-
-
mPEG-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
conjugate
MSX-081
-
-
-
Mu-Leu-Hph-fluoromethylketone
MV061194
-
selective, potent reversible cathepsin K inhibitor
MV061606
-
-
-
MV061645
-
-
-
MV061748
-
-
-
MV061940
-
-
-
MV076159
-
-
-
N'-cyano-N,N',4-trimethyl-2-(4'-(methylsulfonyl)-[1,1'-biphenyl]-3-yl)pentanehydrazide
N'-cyano-N,N',4-trimethyl-2-(4'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)pentanehydrazide
N'-cyano-N,N',4-trimethyl-2-([11,21:24,31-terphenyl]-14-yl)pentanehydrazide
-
N-((S)-4-methyl-1-oxo-1-((S)-3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-ylamino)pentan-2-yl)benzofuran-2-carboxamide
-
-
N-(1-([(cyanomethyl)amino]carbonyl)cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
N-(1-acetyl-4-oxopyrrolidin-3-yl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-carbamoyl-4-oxopyrrolidin-3-yl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-cyano-1-methylethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-cyano-2-phenylethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-cyano-3-pyrrolidinyl)benzamide
-
IC 50: 370 nM
N-(1-cyano-3-pyrrolidinyl)[1,1'-biphenyl]-4-carboxamide
-
IC 50: 290 nM
N-(1-cyano-3pyrrolidinyl)benzenesulfonamide
-
IC 50: 50 nM
N-(1-cyanocyclopropyl)-4,4-difluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-norvalinamide
-
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(1-hydroxycyclopropyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(1-hydroxycyclopropyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(2-hydroxypropan-2-yl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(2-hydroxypropan-2-yl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4-(4-methyl-4,5-dihydro-1,3-thiazol-2-yl)phenyl]ethyl]-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4-(quinolin-6-yl)phenyl]ethyl]-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4-[5-(1-hydroxycyclopropyl)pyridin-2-yl]phenyl]ethyl]-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4-[6-(methylsulfonyl)pyridin-3-yl]phenyl]ethyl]-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1R)-2,2-difluoro-1-hydroxyethyl]biphenyl-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1R)-2,2-difluoro-1-hydroxyethyl][1,1'-biphenyl]-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
-
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1S)-2,2-difluoro-1-hydroxyethyl]biphenyl-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1S)-2,2-difluoro-1-hydroxyethyl][1,1'-biphenyl]-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
-
N-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(2,2,2-trifluoro-1-hydroxyethyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-N2-[(1S)-2,2-difluoro-1-[4'-(2,2,2-trifluoro-1-hydroxyethyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-ethynylcyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-2-pyridin-4-yl-1,3-thiazole-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-(4-fluoropiperidin-4-yl)biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-(dimethylamino)biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-(piperazin-1-ylsulfonyl)biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-([(2S)-1-methylpyrrolidin-2-yl]methoxy)biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-([1-(2-hydroxyethyl)piperidin-4-yl]oxy)biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-([4-(2,2,2-trifluoroethyl)piperazin-1-yl]sulfonyl)biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-isoxazol-5-ylbiphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-piperazin-1-ylbiphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-[(1-methylpiperidin-3-yl)oxy]biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-[(1-methylpiperidin-4-yl)oxy]biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-[methyl(1-methylpyrrolidin-3-yl)amino]biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-(4-[(1-methylethyl)amino]piperidin-1-yl)-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-(4-[methyl(1-methylethyl)amino]piperidin-1-yl)-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-morpholin-4-yl-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[(4-methylpiperazin-1-yl)amino]-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[(4-methylpiperazin-1-yl)methyl]-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[3-(dimethylamino)pyrrolidin-1-yl]-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[4-(2-methoxyethyl)piperazin-1-yl]-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[4-(tetrahydro-2H-pyran-4-yl)piperazin-1-yl]-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(4-methylpiperazin-1-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(4-propylpiperazin-1-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(dimethylamino)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-ethynylbenzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-morpholin-4-ylbenzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[(4-methylpiperazin-1-yl)carbonyl]benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[(4-methylpiperazin-1-yl)sulfonyl]benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(1,4-dimethylpiperidin-4-yl)-1,3-thiazol-4-yl]benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(1-methylpiperidin-4-yl)-1,3-thiazol-4-yl]benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(4-morpholin-4-ylpiperidin-1-yl)-1,3-thiazol-4-yl]benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(morpholin-4-ylmethyl)-1,3-thiazol-4-yl]benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(piperidin-4-yloxy)-1,3-thiazol-4-yl]benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-3-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-4-carboxamide
-
-
N-(1-[[(1S)-1-[[5-(1-methylethyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamoyl]cyclohexyl)-4-(trifluoromethoxy)benzamide
-
-
N-(1-[[(1S)-1-[[5-(3-methoxyphenyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamoyl]cyclohexyl)-4-(trifluoromethoxy)benzamide
-
-
N-(1-[[(1S)-1-[[5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamoyl]cyclohexyl)-4-(trifluoromethoxy)benzamide
-
-
N-(2,3-dichlorophenyl)triazolyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
IC50: 9 nM
N-(2-chlorophenyl)triazolyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
IC50: 6 nM
N-(3-bromoprop-2-yn-1-yl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-(3-[[(3R)-3-([1,1'-biphenyl]-3-yl)-5-methylhex-1-en-2-yl]amino]-2-oxopropyl)-4-phenoxybenzene-1-sulfonamide
-
N-(4-benzyl-1-methylpiperidin-4-yl)-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-(4-chlorophenyl)-2-methylalanyl-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-L-leucinamide
-
IC50 is below 1 nM
N-(4-methyl-1-oxo-1-[[3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]amino]pentan-2-yl)-1-benzofuran-2-carboxamide
-
-
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)propanamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
N-(5-isopropyl)pyridine-2-carboxyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
IC50: less than 3 nM
N-(cyanomethyl)-1-[(3-phenylpropanoyl)amino]cyclohexanecarboxamide
-
-
N-(cyanomethyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-(cyanomethyl)-4-methyl-2-[3'-(2-piperazin-1-yl-1,3-thiazol-4-yl)biphenyl-3-yl]pentanamide
-
-
N-(cyanomethyl)-4-methyl-2-[3'-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]biphenyl-3-yl]pentanamide
-
-
N-(cyanomethyl)-4-methyl-2-[4'-(2-piperazin-1-yl-1,3-thiazol-4-yl)biphenyl-3-yl]pentanamide
-
-
N-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(piperazin-1-yl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-4-benzyloxybenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
IC50: 6 nM
N-4-isopropylbenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
IC50: less than 3 nM
N-4-methoxybenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
-
N-4-propylbenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
IC50: less than 3 nM
N-Acetyl-Leu-Leu-methional
-
-
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)oxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-benzyl-2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-benzyl-3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxamide
-
-
N-but-3-yn-2-yl-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-cyano-N2-[4-[4-(piperazin-1-yl)phenyl]thiophen-3-yl]-L-leucinamide
-
N-cyano-tetrahydro-pyridazine compounds
-
-
-
N-[(1-cyano-2-pyrrolidinyl)methyl]benzamide
-
IC 50: 0.013 mM
N-[(1-cyano-2-pyrrolidinyl)methyl]benzenesulfonamide
-
IC 50: 0.012 mM
N-[(1-cyano-3-azetidinyl)methyl]benzamide
-
IC 50: 70 nM
N-[(1-cyano-3-azetidinyl)methyl]benzenesulfonamide
-
IC 50: 20 nM
N-[(1-cyano-3-azetidinyl)methyl]cyclohexanecarboxamide
-
IC 50: 5 nM
N-[(1-cyano-3pyrrolidinyl)methyl]benzenesulfonamide
-
IC 50: 200 nM
N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-norvalinamide
-
-
N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-N2-(piperazin-1-ylcarbonyl)-D-leucinamide
-
i.e. APC3328
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylpropyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[(2-methyl-1H-imidazol-1-yl)acetyl]-L-leucinamide
-
IC50: 190 nM
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[(4-phenylpiperidin-1-yl)acetyl]-L-leucinamide
-
IC50: 84 nM
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[(4-pyridin-4-ylpiperazin-1-yl)acetyl]-L-leucinamide
-
IC50: 9 nM
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[(5-methyl-1H-imidazol-4-yl)acetyl]-L-leucinamide
-
IC50: 24 nM
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[2-(4-chlorophenoxy)-2-methylpropanoyl]-L-leucinamide
-
IC50 is below 1 nM
N-[(1S)-1-((3-hydroxy-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl)carbamoyl)-3-methylbutyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
-
-
N-[(1S)-1-([(1R)-2-(benzyloxy)-1-cyanoethyl]carbamoyl)-3-methylbutyl]-1-methyl-1H-indole-2-carboxamide
-
IC50 is below 1 nM
N-[(1S)-1-([(1R)-2-(benzyloxy)-1-cyanoethyl]carbamoyl)-3-methylbutyl]-1H-indole-2-carboxamide
-
IC50: 430 nM
N-[(1S)-1-([1-(2-hydroxy-2,3-dihydro-1,4-benzodioxin-2-yl)ethenyl]carbamoyl)-3-methylbutyl]-1-benzofuran-2-carboxamide
-
-
N-[(1S)-1-([3-(2-hydroxyphenoxy)-1-methylidene-2-oxopropyl]carbamoyl)-3-methylbutyl]-1-benzofuran-2-carboxamide
-
-
N-[(1S)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-[(1S)-1-carbamoyl-3-(methylsulfonyl)propyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[(1S)-1-carbamoyl-3-phenylpropyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[(1S)-1-cyano-2-phenylethyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[(1S)-1-cyano-3-(methylsulfanyl)propyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[(1S)-1-cyanoethyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
N-[(1S)-1-cyclohexyl-3-[(2Z)-2-[(4R)-3,4-dimethyl-1,3-thiazolidin-2-ylidene]hydrazinyl]-2,3-dioxopropyl]cycloheptanecarboxamide
-
N-[(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]-2-phenylacetamide
-
-
N-[(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]-3-phenylpropanamide
-
-
N-[(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]-N2-(2,2,2-trifluoroethyl)-L-leucinamide
-
-
N-[(1S)-1-[2-(methylsulfanyl)ethyl]-2-oxopropyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-3-(methylsulfonyl)-L-alaninamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-alaninamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-methioninamide
-
excellent selectivity against the cathepsins B, L and S
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-methionine
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-phenylalaninamide
-
excellent selectivity against the cathepsins B, L and S
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N,N-dimethyl-L-methioninamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N-(2,2,2-trifluoroethyl)-L-methioninamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N-(methylsulfonyl)-L-methioninamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N-benzyl-L-methioninamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N-methyl-L-methioninamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-S-methyl-L-cysteinamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucylglycinamide
-
-
N-[(1S)-3-methyl-1-(((4R)-3-oxo-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl)carbamoyl)butyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
-
-
N-[(1S)-3-methyl-1-([(1S)-1-methyl-2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamoyl)butyl]-1-benzofuran-2-carboxamide
-
-
N-[(1S)-3-methyl-1-([(4S)-3-oxo-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl]carbamoyl)butyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
N-[(1S)-3-methyl-1-[[3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]carbamoyl]butyl]-1-benzofuran-2-carboxamide
-
-
N-[(2S)-1-[4-(benzyloxy)anilino]butan-2-yl]-N2-(morpholine-4-carbonyl)-L-leucinamide
-
N-[(2S)-1-[4-(morpholin-4-yl)anilino]butan-2-yl]-N2-[(1S)-2,2,2-trifluoro-1-(4-hydroxyphenyl)ethyl]-L-leucinamide
-
N-[(2S)-1-[[(2R,4S)-2,4-dimethyl-3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]amino]-4-methyl-1-oxopentan-2-yl]-1-benzofuran-2-carboxamide
-
-
N-[(2S)-1-[[(4S,5S)-4,5-dimethyl-3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]amino]-4-methyl-1-oxopentan-2-yl]-1-benzofuran-2-carboxamide
-
-
N-[(2S)-4-methyl-1-([2-[4-(2-methylpropoxy)anilino]ethyl]amino)-1-oxopentan-2-yl]-2,3-dihydro-1-benzofuran-2-carboxamide
-
N-[(2S)-4-methyl-1-oxo-1-[(3aS,6aR)-3-oxohexahydro-4H-furo[3,2-b]pyrrol-4-yl]pentan-2-yl]-4-(4-methylpiperazin-1-yl)benzamide
-
N-[(2S)-4-methyl-1-oxo-1-[(3aS,7aR)-3-oxohexahydrofuro[3,2-b]pyridin-4(2H)-yl]pentan-2-yl]-4-(4-methylpiperazin-1-yl)benzamide
-
N-[(2S)-4-methyl-1-oxo-1-[[(4R)-3-oxo-1-(pyridine-2-sulfonyl)azepan-4-yl]amino]pentan-2-yl]-2,3-dihydro-1-benzofuran-2-carboxamide
-
N-[(2S)-4-methyl-1-[(3aS,6S,6aR)-6-methyl-3-oxohexahydro-4H-furo[3,2-b]pyrrol-4-yl]-1-oxopentan-2-yl]-4-[2-(1-methylpiperidin-4-yl)-1,3-thiazol-4-yl]benzamide
-
N-[(2S)-4-methyl-1-[[(4S,7R)-7-methyl-3-oxo-1-(pyridine-2-sulfonyl)azepan-4-yl]amino]-1-oxopentan-2-yl]-2,3-dihydro-1-benzofuran-2-carboxamide
-
N-[(4S)-3-oxo-1-(pyridine-2-sulfonyl)azepan-4-yl]-N2-[2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-[1-(benzylcarbamoyl)-4-oxopyrrolidin-3-yl]-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[1-(benzylsulfonyl)-3-oxoazepan-4-yl]-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[1-([(1S)-1-[(5-ethyl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
N-[1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
N-[1-([(1S)-1-[(5-methoxy-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
N-[1-([(1S)-1-[(5-phenyl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
N-[1-([(1S)-1-[(5-tert-butyl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
N-[1-([(1S)-1-[(5-thiophen-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-2-pyridin-4-yl-1,3-thiazole-4-carboxamide
-
moderate inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-(4-fluoropiperidin-4-yl)biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-(dimethylamino)biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-(piperazin-1-ylsulfonyl)biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-isoxazol-5-ylbiphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-piperazin-1-ylbiphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[(1-methylpiperidin-3-yl)oxy]biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[(1-methylpiperidin-4-yl)oxy]biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[methyl(1-methylpyrrolidin-3-yl)amino]biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[[(2S)-1-methylpyrrolidin-2-yl]methoxy]biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[[1-(2-hydroxyethyl)piperidin-4-yl]oxy]biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[[1-(2-methoxyethyl)piperidin-4-yl]oxy]biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[[4-(2,2,2-trifluoroethyl)piperazin-1-yl]sulfonyl]biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(2-morpholin-4-yl-1,3-thiazol-4-yl)benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(2-[4-[(1-methylethyl)amino]piperidin-1-yl]-1,3-thiazol-4-yl)benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(2-[4-[methyl(1-methylethyl)amino]piperidin-1-yl]-1,3-thiazol-4-yl)benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(4-methylpiperazin-1-yl)benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(4-propylpiperazin-1-yl)benzamide
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-morpholin-4-ylbenzamide
-
moderate inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[(4-methylpiperazin-1-yl)carbonyl]benzamide
-
moderate inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[(4-methylpiperazin-1-yl)sulfonyl]benzamide
-
moderate inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(1-methylpiperidin-4-yl)-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(4-morpholin-4-ylpiperidin-1-yl)-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(morpholin-4-ylmethyl)-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(piperidin-4-yloxy)-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-[(4-methylpiperazin-1-yl)methyl]-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-[3-(dimethylamino)pyrrolidin-1-yl]-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-[4-(tetrahydro-2H-pyran-4-yl)piperazin-1-yl]-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-[methyl(4-methylpiperazin-1-yl)amino]-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]biphenyl-3-carboxamide
-
moderate inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]biphenyl-4-carboxamide
-
moderate inhibition
N-[2-[(4-methoxyphenyl)amino]ethyl]-1-(phenylamino)cyclohexanecarboxamide
-
-
N-[2-[(4-methoxyphenyl)amino]ethyl]-1-phenoxycyclohexanecarboxamide
-
-
N-[2-[(4-methoxyphenyl)amino]ethyl]-1-[4-(1-methylethyl)phenoxy]cyclohexanecarboxamide
-
-
N-[4-methyl-1-oxo-1-([2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]amino)pentan-2-yl]-1-benzofuran-2-carboxamide
-
-
N-[cyano(dicyclobutyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[cyano(dicyclopropyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[cyano(phenyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N2-(3-cyclohexylphenyl)-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-leucinamide
-
-
N2-(morpholin-4-ylcarbonyl)-N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-leucinamide
-
-
N2-biphenyl-3-yl-N-[(1S)-1-[([4-[2-(1H-tetrazol-5-yl)ethoxy]phenyl]amino)methyl]propyl]-L-leucinamide
-
-
N2-biphenyl-3-yl-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]propyl]-L-leucinamide
-
-
N2-biphenyl-3-yl-N-[(1S)-2-[(4-methoxyphenyl)amino]-1-methylethyl]-L-leucinamide
-
-
N2-biphenyl-3-yl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-leucinamide
-
-
N2-[(1S)-1-[4'-(1-carbamoylcyclopropyl)-2'-fluorobiphenyl-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
-
-
N2-[(1S)-1-[4'-(1-carbamoylcyclopropyl)-2'-fluorobiphenyl-4-yl]-2,2-difluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
-
-
N2-[(1S)-1-[4'-(1-carbamoylcyclopropyl)biphenyl-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
-
-
N2-[(1S)-1-[4'-(1-carbamoylcyclopropyl)[1,1'-biphenyl]-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
-
N2-[(1S)-1-[4'-(2-amino-2-oxoethyl)[1,1'-biphenyl]-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
-
N2-[(1S)-1-[4'-[(2S)-1-amino-1-oxopropan-2-yl]biphenyl-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
-
-
N2-[(1S)-1-[4-[5-(1-carbamoylcyclopropyl)pyridin-2-yl]phenyl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
-
-
N2-[(benzyloxy)carbonyl]-N-((1S)-1-cyano-2-[4-(trifluoromethyl)phenyl]ethyl)-L-leucinamide
-
IC50: 43 nM
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-2-methylleucinamide
-
weak inhibition
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-4-methyl-L-leucinamide
-
moderate inhibition
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-5,5,5-trifluoro-D-leucinamide
-
-
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-5,5,5-trifluoroleucinamide
-
moderate inhibition
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-D-leucinamide
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-L-isoleucinamide
-
-
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-L-leucinamide
-
-
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-L-norleucinamide
N2-[(benzyloxy)carbonyl]-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-L-leucinamide
-
IC50: 9 nM
N2-[(benzyloxy)carbonyl]-N-[(1R)-2-tert-butoxy-1-cyanoethyl]-L-leucinamide
-
IC50: 240 nM
N2-[(benzyloxy)carbonyl]-N-[(1S)-1-cyano-2-(3-methylphenyl)ethyl]-L-leucinamide
-
IC50: 120 nM
N2-[(benzyloxy)carbonyl]-N-[(1S)-1-cyano-2-(4-methoxyphenyl)ethyl]-L-leucinamide
-
IC50: 63 nM
N2-[(benzyloxy)carbonyl]-N-[(1S)-1-cyano-2-(4-methylphenyl)ethyl]-L-leucinamide
-
IC50: 48 nM
N2-[(benzyloxy)carbonyl]-N-[(1S)-2-(4-tert-butoxyphenyl)-1-cyanoethyl]-L-leucinamide
-
IC50: 398 nM
N2-[(benzyloxy)carbonyl]-N-[2-oxo-3-[(4-phenoxybenzene-1-sulfonyl)amino]propyl]-L-leucinamide
-
N2-[(benzyloxy)carbonyl]-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-leucinamide
-
-
N2TY
-
slow-binding inhibitor of cathepsin K
-
Nalpha-3-chlorobenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
less efficient than Nalpha-benzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
Nalpha-3-methoxybenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
less efficient than Nalpha-benzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
Nalpha-3-methylbenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
-
Nalpha-4-chlorobenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
-
Nalpha-4-methoxybenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
IC50: 64 nM
Nalpha-4-methylbenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
-
Nalpha-benzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
IC50: 470 nM
naphthalen-2-yl (4S)-4-([[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamoyl]oxy)-3,3-dimethylpyrrolidine-1-carboxylate
-
-
NC-2300
NSC13345
NSC1335
-
-
odabnacatib
-
MK-0822
odanacatib
odanacatib 1
-
i.e. MK-0822, a reversible, non-basic, potent and selective Cat K inhibitor. The nitrile forms a hydrogen bond-stabilized thioimidate intermediate with Cys25. The leucine moiety interacts with the hydrophobic S2 subsite and the biphenyl moiety with the S3 subsite, and the hydrogen bond of the trifluroethylamine amide isostere interact with Gly66. Furthermore, odanacatib does not interact with the prime side of Cat K, binding structure, overview
ONO-5334
-
-
pepstatin A
17.29% inhibition at 0.1 mM
Phe-Phe-fluoromethylketone
-
phenyl (4S)-4-([[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamoyl]oxy)-3,3-dimethylpyrrolidine-1-carboxylate
-
-
phenylmethylsulfonyl fluoride
53.68% inhibition at 0.1 mM
PHPMA-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
conjugate
PHPMA-GG-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
conjugate
piperidin-2-yl-[2-(trifluoromethyl)-6-[4-(trifluoromethyl)phenyl]pyridin-4-yl] methanol
-
-
piperidine-4-carboxylic acid [3-methyl-1[1-(1-oxa-3-aza-cyclopenta[a]naphthalene-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
piperidine-4-carboxylic acid [3-methyl-1[1-(naphtho[1,2-d]oxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
procathepsin K
-
-
-
procathepsin L
-
-
-
procathepsin S
-
-
-
pyridoxal phosphate
-
at 1 mM 85% inhibition
quinoline-2-carboxylic acid [(S)-1-((3R,S)-4-oxotetrahydrofuran-3ylcarbamoyl)-3-methylbutyl]amide
-
-
relacatib
relicatib
-
also known as SB-462795, highly potent human cathepsin K inhibitor
RH00369
-
-
S-(1-methylethyl) (2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazinecarbothioate
-
-
S-[2-[2-(dihydroxymethyl)anilino]-2-oxoethyl] carbamothioate
-
SB-357114
-
specific inhibitor
SB-553484
-
inhibits bone and cartilage degradation in vivo
SB462595
-
-
-
SDS
77.28% residual activity at 0.05% (w/v)
SM934-testosterone
inhibits proliferation and metastasis ability of breast cancer cells via inhibiting the expression of cathepsin K followed by the inhibition of Bcl-xL
sodium (2S,3S)-3-[[(2S)-4-methyl-1-(2-methylpropoxy)pentan-2-yl]amino]oxirane-2-carboxylate
-
sophoraflavanone G
shows inhibitory effects on the bone resorption process related to cathepsin K
Stefin A
-
slow-binding inhibitor of cathepsin K
-
Stefin B
-
natural inhibitor of cathepsin K, reversible, tight-binding competitive inhibitor
-
STPHPMA-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
conjugate
Synthetic inhibitors
-
-
-
tert-butyl ([1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]carbamoyl)carbamate
-
-
tert-butyl 3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxylate
-
-
tert-butyl 3-(4-[[(2S)-2-([[1-(biphenyl-3-ylamino)cyclohexyl]carbonyl]amino)butyl]amino]phenoxy)propanoate
-
-
tert-butyl 3-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-4-oxopyrrolidine-1-carboxylate
-
-
tert-butyl 3-[4-([(2S)-2-[(N-biphenyl-3-yl-L-leucyl)amino]butyl]amino)phenoxy]propanoate
-
-
tert-butyl [(1S)-1-([5-[4-(dimethylamino)phenyl]-1,3,4-oxadiazol-2-yl]carbonyl)butyl]carbamate
-
-
tert-butyl [(1S)-1-formylpentyl]carbamate
-
-
tert-butyl [(1S)-1-[(5-thiophen-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-(4,5-dihydro-1,3-thiazol-2-ylhydrazono)methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-(carbamimidoylhydrazono)methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-(carbamoylhydrazono)methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(2,3-dihydro-1H-indol-1-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(3,4-dihydroisoquinolin-2(1H)-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(3,4-dihydroquinolin-1(2H)-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(3-methylbutanoyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(benzylcarbamoyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(diethylcarbamoyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(dimethylcarbamoyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(dimethylsulfamoyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(ethylcarbamoyl)hydrazono]methyl]pentyl]carbamate
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tert-butyl [(1S)-1-[(E)-[(methylcarbamoyl)hydrazono]methyl]pentyl]carbamate
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tert-butyl [(1S)-1-[(E)-[(morpholin-4-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
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tert-butyl [(1S)-1-[(E)-[(phenylcarbamoyl)hydrazono]methyl]pentyl]carbamate
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tert-butyl [(1S)-1-[(E)-[(phenylcarbonyl)hydrazono]methyl]pentyl]carbamate
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tert-butyl [(1S)-1-[(E)-[(piperidin-1-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
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tert-butyl [(1S)-1-[(E)-[(pyrrolidin-1-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
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tert-butyl [(1S)-1-[(E)-[(tert-butylcarbamoyl)hydrazono]methyl]pentyl]carbamate
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tert-butyl [(1S)-1-[(E)-[(trifluoroacetyl)hydrazono]methyl]pentyl]carbamate
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tert-butyl [(1S)-1-[(E)-[methyl[(2-phenylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
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tert-butyl [(1S)-1-[(E)-[methyl[methyl(2-phenylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
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tert-butyl [(1S)-1-[(E)-[[(1-methylethyl)carbamothioyl]hydrazono]methyl]pentyl]carbamate
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tert-butyl [(1S)-1-[(E)-[[(1-methylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
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tert-butyl [(1S)-1-[(E)-[[(2-phenylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
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tert-butyl [(1S)-1-[(E)-[[(morpholin-4-ylcarbonyl)oxy]imino]methyl]pentyl]carbamate
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tert-butyl [(1S)-1-[(E)-[[methyl(2-phenylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
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tert-butyl [(1S)-1-[[5-(1-methylethyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamate
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tert-butyl [(1S)-1-[[5-(2-methoxyphenyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamate
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tert-butyl [(3S)-1,2-dioxo-1-(phenylamino)heptan-3-yl]carbamate
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tert-butyl [(3S)-1,2-dioxo-1-(propan-2-ylamino)heptan-3-yl]carbamate
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tert-butyl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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tert-butyl [(3S)-1,2-dioxo-1-[[(1S)-1-phenylethyl]amino]heptan-3-yl]carbamate
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tert-butyl [(3S)-1-(benzylamino)-1,2-dioxoheptan-3-yl]carbamate
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tert-butyl [(3S)-1-amino-1,2-dioxoheptan-3-yl]carbamate
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tert-butyl [1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]carbamate
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trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
VEL-0230
highly selective inhibitor of CatK that significantly decreases bone resorption and increases bone formation biomarkers
Zn2+
47.5% residual activity at 5 mM
[(S)-1-((3R,S)-1-acetyl-4-oxopyrrolidin-3-ylcarbamoyl)-3-methylbutyl]carbamic acid benzyl ester
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[(S)-1-((3R,S)-4-oxotetrahydrofuran-3-ylcarbamoyl)-3-methylbutyl]carbamic acid benzyl ester
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[(S)-1-((4R,S)-3-oxotetrahydropyran-4-ylcarbamoyl)-3-methylbutyl]carbamic acid benzyl ester
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[1-(2-cyano-tetrahydro-pyridazine-1-carbonyl)-2-methyl-propyl]-carbamic acid benzyl ester
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inhibits the bone resorptive activity of mature osteoclasts, structure and interaction pattern with cathepsin K, overview
additional information
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