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Literature summary extracted from

  • Gauthier, J.Y.; Chauret, N.; Cromlish, W.; Desmarais, S.; Duong, l.e..T.; Falgueyret, J.P.; Kimmel, D.B.; Lamontagne, S.; Leger, S.; LeRiche, T.; Li, C.S.; Masse, F.; McKay, D.J.; Nicoll-Griffith, D.A.; Oballa, R.M.; Palmer, J.T.; Percival, M.D.; Riendeau, D.; Robichaud, J.; Rodan, G.A.; Rodan, S.B.; Seto, C.
    The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K (2008), Bioorg. Med. Chem. Lett., 18, 923-928.
    View publication on PubMed

Inhibitors

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

Localization

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
-

Organism

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
-
-
-

Source Tissue

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
-

Synonyms

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

IC50 Value

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