Literature summary for 3.4.22.38 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.

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Inhibitors

Inhibitors	Comment	Organism
(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

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

Organism	UniProt	Comment	Textmining
Canis lupus familiaris	-	-	-
Homo sapiens	-	-	-
Macaca fascicularis	-	-	-
Macaca mulatta	-	-	-
Oryctolagus cuniculus	-	-	-
Rattus norvegicus	-	-	-

Source Tissue

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

Synonyms	Comment	Organism
Cat K	-	Homo sapiens
Cat K	-	Rattus norvegicus
Cat K	-	Oryctolagus cuniculus
Cat K	-	Canis lupus familiaris

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor
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