EC Number | Inhibitors | Comment | Organism | Structure |
---|---|---|---|---|
3.4.22.38 | (2S)-4,4-dichloro-N-(1-cyanocyclopropyl)-2-([(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]amino)butanamide | - |
Oryctolagus cuniculus | |
3.4.22.38 | (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 | |
3.4.22.38 | (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 | |
3.4.22.38 | (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 | |
3.4.22.38 | balicatib | - |
Canis lupus familiaris | |
3.4.22.38 | balicatib | shows no selectivity in cell-based assays over cathepsins B, L, and S | Homo sapiens | |
3.4.22.38 | balicatib | - |
Macaca fascicularis | |
3.4.22.38 | balicatib | - |
Macaca mulatta | |
3.4.22.38 | balicatib | - |
Oryctolagus cuniculus | |
3.4.22.38 | balicatib | - |
Rattus norvegicus | |
3.4.22.38 | L-006235 | shows no selectivity in cell-based assays over cathepsins B, L, and S | Canis lupus familiaris | |
3.4.22.38 | L-006235 | shows no selectivity in cell-based assays over cathepsins B, L, and S | Homo sapiens | |
3.4.22.38 | L-006235 | shows no selectivity in cell-based assays over cathepsins B, L, and S | Macaca fascicularis | |
3.4.22.38 | L-006235 | shows no selectivity in cell-based assays over cathepsins B, L, and S | Macaca mulatta | |
3.4.22.38 | L-006235 | shows no selectivity in cell-based assays over cathepsins B, L, and S | Rattus norvegicus | |
3.4.22.38 | L-13006235 | shows no selectivity in cell-based assays over cathepsins B, L, and S | Oryctolagus cuniculus | |
3.4.22.38 | L-873724 | - |
Canis lupus familiaris | |
3.4.22.38 | L-873724 | highly selective for cathespin K over other cathepsins, metabolization, overview | Homo sapiens | |
3.4.22.38 | L-873724 | - |
Macaca fascicularis | |
3.4.22.38 | 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 | |
3.4.22.38 | L-873724 | - |
Oryctolagus cuniculus | |
3.4.22.38 | L-873724 | highly selective for cathespin K over other cathepsins, metabolization, overview | Rattus norvegicus | |
3.4.22.38 | N-(1-cyano-1-methylethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide | - |
Oryctolagus cuniculus | |
3.4.22.38 | N-(1-cyano-2-phenylethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide | - |
Oryctolagus cuniculus | |
3.4.22.38 | N-(1-cyanocyclopropyl)-4,4-difluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-norvalinamide | - |
Oryctolagus cuniculus | |
3.4.22.38 | N-[(1S)-1-cyanoethyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide | - |
Oryctolagus cuniculus | |
3.4.22.38 | N-[cyano(dicyclobutyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide | - |
Oryctolagus cuniculus | |
3.4.22.38 | N-[cyano(dicyclopropyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide | - |
Oryctolagus cuniculus | |
3.4.22.38 | N-[cyano(phenyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide | - |
Oryctolagus cuniculus | |
3.4.22.38 | odanacatib | i.e. MK-0822, a selective cathepsin K inhibitor, pharmacokinetics of odanacatib | Canis lupus familiaris | |
3.4.22.38 | odanacatib | i.e. MK-0822, a selective cathepsin K inhibitor | Homo sapiens | |
3.4.22.38 | odanacatib | i.e. MK-0822, a selective cathepsin K inhibitor | Macaca fascicularis | |
3.4.22.38 | odanacatib | i.e. MK-0822, a selective cathepsin K inhibitor, pharmacokinetics of odanacatib | Macaca mulatta | |
3.4.22.38 | odanacatib | i.e. MK-0822, a selective cathepsin K inhibitor | Oryctolagus cuniculus | |
3.4.22.38 | odanacatib | i.e. MK-0822, a selective cathepsin K inhibitor, pharmacokinetics of odanacatib | Rattus norvegicus | |
3.4.22.38 | relacatib | - |
Canis lupus familiaris | |
3.4.22.38 | relacatib | a Cat K inhibitor in clinical development | Homo sapiens | |
3.4.22.38 | relacatib | - |
Macaca fascicularis | |
3.4.22.38 | relacatib | - |
Macaca mulatta | |
3.4.22.38 | relacatib | - |
Oryctolagus cuniculus | |
3.4.22.38 | relacatib | - |
Rattus norvegicus |
EC Number | Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|---|
3.4.22.38 | lysosome | - |
Homo sapiens | 5764 | - |
3.4.22.38 | lysosome | - |
Rattus norvegicus | 5764 | - |
3.4.22.38 | lysosome | - |
Oryctolagus cuniculus | 5764 | - |
3.4.22.38 | lysosome | - |
Canis lupus familiaris | 5764 | - |
3.4.22.38 | lysosome | - |
Macaca mulatta | 5764 | - |
3.4.22.38 | lysosome | - |
Macaca fascicularis | 5764 | - |
EC Number | Organism | UniProt | Comment | Textmining |
---|---|---|---|---|
3.4.22.38 | Canis lupus familiaris | - |
- |
- |
3.4.22.38 | Homo sapiens | - |
- |
- |
3.4.22.38 | Macaca fascicularis | - |
- |
- |
3.4.22.38 | Macaca mulatta | - |
- |
- |
3.4.22.38 | Oryctolagus cuniculus | - |
- |
- |
3.4.22.38 | Rattus norvegicus | - |
- |
- |
EC Number | Source Tissue | Comment | Organism | Textmining |
---|---|---|---|---|
3.4.22.38 | Hep-G2 cell | - |
Homo sapiens | - |
3.4.22.38 | hepatocyte | - |
Homo sapiens | - |
3.4.22.38 | hepatocyte | - |
Rattus norvegicus | - |
3.4.22.38 | hepatocyte | - |
Oryctolagus cuniculus | - |
3.4.22.38 | hepatocyte | - |
Canis lupus familiaris | - |
3.4.22.38 | hepatocyte | - |
Macaca mulatta | - |
3.4.22.38 | hepatocyte | - |
Macaca fascicularis | - |
3.4.22.38 | liver | - |
Homo sapiens | - |
3.4.22.38 | liver | - |
Rattus norvegicus | - |
3.4.22.38 | liver | - |
Oryctolagus cuniculus | - |
3.4.22.38 | liver | - |
Canis lupus familiaris | - |
3.4.22.38 | liver | - |
Macaca mulatta | - |
3.4.22.38 | liver | - |
Macaca fascicularis | - |
3.4.22.38 | osteoclast | - |
Homo sapiens | - |
3.4.22.38 | osteoclast | - |
Rattus norvegicus | - |
3.4.22.38 | osteoclast | - |
Oryctolagus cuniculus | - |
3.4.22.38 | osteoclast | - |
Canis lupus familiaris | - |
3.4.22.38 | osteoclast | - |
Macaca mulatta | - |
3.4.22.38 | osteoclast | - |
Macaca fascicularis | - |
EC Number | Synonyms | Comment | Organism |
---|---|---|---|
3.4.22.38 | Cat K | - |
Homo sapiens |
3.4.22.38 | Cat K | - |
Rattus norvegicus |
3.4.22.38 | Cat K | - |
Oryctolagus cuniculus |
3.4.22.38 | Cat K | - |
Canis lupus familiaris |
EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|---|
3.4.22.38 | 0.0000002 | - |
- |
Oryctolagus cuniculus | odanacatib | |
3.4.22.38 | 0.0000002 | - |
- |
Oryctolagus cuniculus | L-873724 | |
3.4.22.38 | 0.0000002 | - |
- |
Oryctolagus cuniculus | L-13006235 | |
3.4.22.38 | 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 | |
3.4.22.38 | 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 | |
3.4.22.38 | 0.0000002 | - |
isolated Cat K | Homo sapiens | odanacatib | |
3.4.22.38 | 0.0000002 | - |
isolated Cat K | Homo sapiens | L-873724 | |
3.4.22.38 | 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 | |
3.4.22.38 | 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 | |
3.4.22.38 | 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 | |
3.4.22.38 | 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 | |
3.4.22.38 | 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 | |
3.4.22.38 | 0.0000006 | - |
isolated Cat K | Homo sapiens | balicatib | |
3.4.22.38 | 0.000001 | - |
- |
Oryctolagus cuniculus | balicatib | |
3.4.22.38 | 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 | |
3.4.22.38 | 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 | |
3.4.22.38 | 0.0000027 | - |
- |
Oryctolagus cuniculus | relacatib | |
3.4.22.38 | 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 | |
3.4.22.38 | 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 | |
3.4.22.38 | 0.000014 | - |
Hep-G2 cell based assay | Homo sapiens | relacatib | |
3.4.22.38 | 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 | |
3.4.22.38 | 0.000061 | - |
Hep-G2 cell based assay | Homo sapiens | balicatib | |
3.4.22.38 | 0.00105 | - |
Hep-G2 cell based assay | Homo sapiens | odanacatib | |
3.4.22.38 | 0.004807 | - |
Hep-G2 cell based assay | Homo sapiens | L-873724 |