Application | Comment | Organism |
---|---|---|
drug development | the enzyme is a drug target in the treatment of osteoporosis | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
3-bromo-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide | moderate inhibition | Homo sapiens | |
4'-(4-tert-butylpiperazin-1-yl)-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]biphenyl-4-carboxamide | strong inhibition | Homo sapiens | |
4'-[4-(tert-butylamino)piperidin-1-yl]-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]biphenyl-4-carboxamide | strong inhibition | Homo sapiens | |
4-amino-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide | moderate inhibition | Homo sapiens | |
4-bromo-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide | moderate inhibition | Homo sapiens | |
4-cyano-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide | moderate inhibition | Homo sapiens | |
4-[2-(1,4'-bipiperidin-1'-yl)-1,3-thiazol-4-yl]-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide | strong inhibition | Homo sapiens | |
4-[2-(4-tert-butylpiperazin-1-yl)-1,3-thiazol-4-yl]-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide | strong inhibition | Homo sapiens | |
4-[2-[(3R)-3-aminopyrrolidin-1-yl]-1,3-thiazol-4-yl]-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide | strong inhibition | Homo sapiens | |
5-bromo-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]thiophene-2-carboxamide | moderate inhibition | Homo sapiens | |
benzyl (2S,3R)-1-(cyanomethylamino)-3-hydroxy-1-oxobutan-2-ylcarbamate | weak inhibition | Homo sapiens | |
benzyl (2S,3S)-1-(cyanomethylamino)-3-methyl-1-oxopentan-2-ylcarbamate | weak inhibition | Homo sapiens | |
benzyl [(1S)-1-[(cyanomethyl)carbamoyl]-2,2-dimethylpropyl]carbamate | weak inhibition | Homo sapiens | |
benzyl [(1S)-2-[(cyanomethyl)amino]-1-(naphthalen-2-ylmethyl)-2-oxoethyl]carbamate | weak inhibition | Homo sapiens | |
benzyl [1-[(cyanomethyl)carbamoyl]cyclohexyl]carbamate | moderate inhibition | Homo sapiens | |
benzyl [1-[(cyanomethyl)carbamoyl]cyclopentyl]carbamate | weak inhibition | Homo sapiens | |
additional information | construction of a three-dimensional pharmacophore model for cathepsin K inhibitor screening and development using the enzyme crystal structure complexed with a ketoamide inhibitor, docking and inhibitor binding structure, validation of pharmacophore hypothesis, overview | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-2-pyridin-4-yl-1,3-thiazole-4-carboxamide | moderate inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-(4-fluoropiperidin-4-yl)biphenyl-4-carboxamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-(dimethylamino)biphenyl-4-carboxamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-(piperazin-1-ylsulfonyl)biphenyl-4-carboxamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-isoxazol-5-ylbiphenyl-4-carboxamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-piperazin-1-ylbiphenyl-4-carboxamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[(1-methylpiperidin-3-yl)oxy]biphenyl-4-carboxamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[(1-methylpiperidin-4-yl)oxy]biphenyl-4-carboxamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[methyl(1-methylpyrrolidin-3-yl)amino]biphenyl-4-carboxamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[[(2S)-1-methylpyrrolidin-2-yl]methoxy]biphenyl-4-carboxamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[[1-(2-hydroxyethyl)piperidin-4-yl]oxy]biphenyl-4-carboxamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[[1-(2-methoxyethyl)piperidin-4-yl]oxy]biphenyl-4-carboxamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[[4-(2,2,2-trifluoroethyl)piperazin-1-yl]sulfonyl]biphenyl-4-carboxamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(2-morpholin-4-yl-1,3-thiazol-4-yl)benzamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(2-[4-[(1-methylethyl)amino]piperidin-1-yl]-1,3-thiazol-4-yl)benzamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(2-[4-[methyl(1-methylethyl)amino]piperidin-1-yl]-1,3-thiazol-4-yl)benzamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(4-methylpiperazin-1-yl)benzamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(4-propylpiperazin-1-yl)benzamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-morpholin-4-ylbenzamide | moderate inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[(4-methylpiperazin-1-yl)carbonyl]benzamide | moderate inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[(4-methylpiperazin-1-yl)sulfonyl]benzamide | moderate inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(1-methylpiperidin-4-yl)-1,3-thiazol-4-yl]benzamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(4-morpholin-4-ylpiperidin-1-yl)-1,3-thiazol-4-yl]benzamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(morpholin-4-ylmethyl)-1,3-thiazol-4-yl]benzamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(piperidin-4-yloxy)-1,3-thiazol-4-yl]benzamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-[(4-methylpiperazin-1-yl)methyl]-1,3-thiazol-4-yl]benzamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-[3-(dimethylamino)pyrrolidin-1-yl]-1,3-thiazol-4-yl]benzamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-[4-(tetrahydro-2H-pyran-4-yl)piperazin-1-yl]-1,3-thiazol-4-yl]benzamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-[methyl(4-methylpiperazin-1-yl)amino]-1,3-thiazol-4-yl]benzamide | strong inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]biphenyl-3-carboxamide | moderate inhibition | Homo sapiens | |
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]biphenyl-4-carboxamide | moderate inhibition | Homo sapiens | |
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-2-methylleucinamide | weak inhibition | Homo sapiens | |
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-4-methyl-L-leucinamide | moderate inhibition | Homo sapiens | |
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-5,5,5-trifluoroleucinamide | moderate inhibition | Homo sapiens | |
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-D-leucinamide | weak inhibition | Homo sapiens | |
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-L-norleucinamide | moderate inhibition | Homo sapiens | |
RH00369 | - |
Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
lysosome | - |
Homo sapiens | 5764 | - |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | Homo sapiens | cathepsin K is a lysosomal cysteine protease that is highly and selectively expressed in osteoclasts, the cells which degrade bone during the continuous cycle of bone degradation and formation | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
bone | - |
Homo sapiens | - |
osteoclast | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | cathepsin K is a lysosomal cysteine protease that is highly and selectively expressed in osteoclasts, the cells which degrade bone during the continuous cycle of bone degradation and formation | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
Cat K | - |
Homo sapiens |