Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(2S)-4,4-dichloro-N-(1-cyanocyclopropyl)-2-([(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]amino)butanamide | - |
Oryctolagus cuniculus | |
(2S)-N-(1-cyanocyclopropyl)-4,4,4-trifluoro-2-([(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]amino)butanamide | - |
Oryctolagus cuniculus | |
(4R)-N-(1-cyanocyclopropyl)-5,5,5-trifluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide | - |
Oryctolagus cuniculus | |
(4S)-N-(1-cyanocyclopropyl)-5,5,5-trifluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide | - |
Oryctolagus cuniculus | |
balicatib | - |
Canis lupus familiaris | |
balicatib | shows no selectivity in cell-based assays over cathepsins B, L, and S | Homo sapiens | |
balicatib | - |
Macaca fascicularis | |
balicatib | - |
Macaca mulatta | |
balicatib | - |
Oryctolagus cuniculus | |
balicatib | - |
Rattus norvegicus | |
L-006235 | shows no selectivity in cell-based assays over cathepsins B, L, and S | Canis lupus familiaris | |
L-006235 | shows no selectivity in cell-based assays over cathepsins B, L, and S | Homo sapiens | |
L-006235 | shows no selectivity in cell-based assays over cathepsins B, L, and S | Macaca fascicularis | |
L-006235 | shows no selectivity in cell-based assays over cathepsins B, L, and S | Macaca mulatta | |
L-006235 | shows no selectivity in cell-based assays over cathepsins B, L, and S | Rattus norvegicus | |
L-13006235 | shows no selectivity in cell-based assays over cathepsins B, L, and S | Oryctolagus cuniculus | |
L-873724 | - |
Canis lupus familiaris | |
L-873724 | highly selective for cathespin K over other cathepsins, metabolization, overview | Homo sapiens | |
L-873724 | - |
Macaca fascicularis | |
L-873724 | the neutral Cat K inhibitor suppresses biochemical markers of bone resorption in vivo, highly selective for cathespin K over other cathepsins, metabolization, overview | Macaca mulatta | |
L-873724 | - |
Oryctolagus cuniculus | |
L-873724 | highly selective for cathespin K over other cathepsins, metabolization, overview | Rattus norvegicus | |
N-(1-cyano-1-methylethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide | - |
Oryctolagus cuniculus | |
N-(1-cyano-2-phenylethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide | - |
Oryctolagus cuniculus | |
N-(1-cyanocyclopropyl)-4,4-difluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-norvalinamide | - |
Oryctolagus cuniculus | |
N-[(1S)-1-cyanoethyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide | - |
Oryctolagus cuniculus | |
N-[cyano(dicyclobutyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide | - |
Oryctolagus cuniculus | |
N-[cyano(dicyclopropyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide | - |
Oryctolagus cuniculus | |
N-[cyano(phenyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide | - |
Oryctolagus cuniculus | |
odanacatib | i.e. MK-0822, a selective cathepsin K inhibitor, pharmacokinetics of odanacatib | Canis lupus familiaris | |
odanacatib | i.e. MK-0822, a selective cathepsin K inhibitor | Homo sapiens | |
odanacatib | i.e. MK-0822, a selective cathepsin K inhibitor | Macaca fascicularis | |
odanacatib | i.e. MK-0822, a selective cathepsin K inhibitor, pharmacokinetics of odanacatib | Macaca mulatta | |
odanacatib | i.e. MK-0822, a selective cathepsin K inhibitor | Oryctolagus cuniculus | |
odanacatib | i.e. MK-0822, a selective cathepsin K inhibitor, pharmacokinetics of odanacatib | Rattus norvegicus | |
relacatib | - |
Canis lupus familiaris | |
relacatib | a Cat K inhibitor in clinical development | Homo sapiens | |
relacatib | - |
Macaca fascicularis | |
relacatib | - |
Macaca mulatta | |
relacatib | - |
Oryctolagus cuniculus | |
relacatib | - |
Rattus norvegicus |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
lysosome | - |
Homo sapiens | 5764 | - |
lysosome | - |
Rattus norvegicus | 5764 | - |
lysosome | - |
Oryctolagus cuniculus | 5764 | - |
lysosome | - |
Canis lupus familiaris | 5764 | - |
lysosome | - |
Macaca mulatta | 5764 | - |
lysosome | - |
Macaca fascicularis | 5764 | - |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Canis lupus familiaris | - |
- |
- |
Homo sapiens | - |
- |
- |
Macaca fascicularis | - |
- |
- |
Macaca mulatta | - |
- |
- |
Oryctolagus cuniculus | - |
- |
- |
Rattus norvegicus | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
Hep-G2 cell | - |
Homo sapiens | - |
hepatocyte | - |
Homo sapiens | - |
hepatocyte | - |
Rattus norvegicus | - |
hepatocyte | - |
Oryctolagus cuniculus | - |
hepatocyte | - |
Canis lupus familiaris | - |
hepatocyte | - |
Macaca mulatta | - |
hepatocyte | - |
Macaca fascicularis | - |
liver | - |
Homo sapiens | - |
liver | - |
Rattus norvegicus | - |
liver | - |
Oryctolagus cuniculus | - |
liver | - |
Canis lupus familiaris | - |
liver | - |
Macaca mulatta | - |
liver | - |
Macaca fascicularis | - |
osteoclast | - |
Homo sapiens | - |
osteoclast | - |
Rattus norvegicus | - |
osteoclast | - |
Oryctolagus cuniculus | - |
osteoclast | - |
Canis lupus familiaris | - |
osteoclast | - |
Macaca mulatta | - |
osteoclast | - |
Macaca fascicularis | - |
Synonyms | Comment | Organism |
---|---|---|
Cat K | - |
Homo sapiens |
Cat K | - |
Rattus norvegicus |
Cat K | - |
Oryctolagus cuniculus |
Cat K | - |
Canis lupus familiaris |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000002 | - |
- |
Oryctolagus cuniculus | odanacatib | |
0.0000002 | - |
- |
Oryctolagus cuniculus | L-873724 | |
0.0000002 | - |
- |
Oryctolagus cuniculus | L-13006235 | |
0.0000002 | - |
above, humanized rabbit cathepsin K | Oryctolagus cuniculus | (2S)-4,4-dichloro-N-(1-cyanocyclopropyl)-2-([(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]amino)butanamide | |
0.0000002 | - |
humanized rabbit cathepsin K | Oryctolagus cuniculus | N-(1-cyanocyclopropyl)-4,4-difluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-norvalinamide | |
0.0000002 | - |
isolated Cat K | Homo sapiens | odanacatib | |
0.0000002 | - |
isolated Cat K | Homo sapiens | L-873724 | |
0.0000003 | - |
humanized rabbit cathepsin K | Oryctolagus cuniculus | (4S)-N-(1-cyanocyclopropyl)-5,5,5-trifluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide | |
0.0000003 | - |
humanized rabbit cathepsin K | Oryctolagus cuniculus | N-[cyano(dicyclopropyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide | |
0.0000004 | - |
humanized rabbit cathepsin K | Oryctolagus cuniculus | (4R)-N-(1-cyanocyclopropyl)-5,5,5-trifluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide | |
0.0000006 | - |
humanized rabbit cathepsin K | Oryctolagus cuniculus | N-(1-cyano-2-phenylethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide | |
0.0000006 | - |
humanized rabbit cathepsin K | Oryctolagus cuniculus | N-[cyano(phenyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide | |
0.0000006 | - |
isolated Cat K | Homo sapiens | balicatib | |
0.000001 | - |
- |
Oryctolagus cuniculus | balicatib | |
0.0000012 | - |
humanized rabbit cathepsin K | Oryctolagus cuniculus | N-[(1S)-1-cyanoethyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide | |
0.0000015 | - |
humanized rabbit cathepsin K | Oryctolagus cuniculus | (2S)-N-(1-cyanocyclopropyl)-4,4,4-trifluoro-2-([(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]amino)butanamide | |
0.0000027 | - |
- |
Oryctolagus cuniculus | relacatib | |
0.000004 | - |
humanized rabbit cathepsin K | Oryctolagus cuniculus | N-(1-cyano-1-methylethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide | |
0.0000051 | - |
humanized rabbit cathepsin K | Oryctolagus cuniculus | N-(1-cyano-2-phenylethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide | |
0.000014 | - |
Hep-G2 cell based assay | Homo sapiens | relacatib | |
0.000016 | - |
humanized rabbit cathepsin K | Oryctolagus cuniculus | N-[cyano(dicyclobutyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide | |
0.000061 | - |
Hep-G2 cell based assay | Homo sapiens | balicatib | |
0.00105 | - |
Hep-G2 cell based assay | Homo sapiens | odanacatib | |
0.004807 | - |
Hep-G2 cell based assay | Homo sapiens | L-873724 |