Target Validation Information | |||||
---|---|---|---|---|---|
Target ID | T11388 | ||||
Target Name | Cathepsin K | ||||
Target Type | Clinical Trial |
||||
Drug Potency against Target | 2-cyclohexylamino-pyrimidine-4-carbonitrile | Drug Info | IC50 = 120 nM | [528643] | |
P2,P3 Ketoamide derivative | Drug Info | IC50 = 40 nM | [527197] | ||
4-cycloheptyl-6-propylpyrimidine-2-carbonitrile | Drug Info | IC50 = 84 nM | [530717] | ||
Z-Arg-Leu-Val-Agly-Val-Ala-NH2 | Drug Info | Ki = 2.13 nM | [526417] | ||
Z-Arg-Leu-Val-Agly-Ileu-Val-OMe | Drug Info | Ki = 21 nM | [526417] | ||
Boc-Agly-Val-Agly-OEt | Drug Info | Ki = 61 nM | [526417] | ||
Z-Ala-Leu-lle-Agly-Ile-Val-OMe | Drug Info | Ki = 2.12 nM | [526417] | ||
Z-Arg-Leu-Val-Agly-Ile-Val-Trp-NH2 | Drug Info | Ki = 72 nM | [526417] | ||
Z-Arg-Leu-Val-Agly-Trp-Val-Ala-NH2 | Drug Info | Ki = 100 nM | [526417] | ||
4-propyl-6-m-tolylpyrimidine-2-carbonitrile | Drug Info | IC50 = 182 nM | [531005] | ||
N-(4-phenylbenzoyl)-phenylalanyl-glycine-nitrile | Drug Info | Ki = 300 nM | [527885] | ||
N-(tert-butoxycarbonyl)-isoleucyl-glycine-nitrile | Drug Info | Ki = 5800 nM | [527885] | ||
4-cyclohexyl-6-propylpyrimidine-2-carbonitrile | Drug Info | IC50 = 680 nM | [530717] | ||
N-(tert-butoxycarbonyl)-norleucyl-glycine-nitrile | Drug Info | Ki = 1270 nM | [527885] | ||
(S)-tert-butyl 1-oxohexan-2-ylcarbamate | Drug Info | IC50 = 51 nM | [527872] | ||
N-(benzyloxycarbonyl)-leucyl-glycine-nitrile | Drug Info | Ki = 35 nM | [527885] | ||
GNF-PF-5434 | Drug Info | Ki = 1.2 nM | [529350] | ||
4-phenyl-6-propylpyrimidine-2-carbonitrile | Drug Info | IC50 = 1122 nM | [531005] | ||
L-873724 | Drug Info | IC50 = 6.1 nM | [529711] | ||
Odanacatib | Drug Info | IC50 = 0.2 nM | [536609] | ||
Z-leu-Val-Agly-Val-OBzl | Drug Info | Ki = 34 nM | [526417] | ||
Z-Ala-Leu-lle-Agly-Ile-Val-NHBzl | Drug Info | Ki = 2.45 nM | [526417] | ||
Z-Ala-Leu-His-Agly-Ile-Val-OMe | Drug Info | Ki = 0.86 nM | [526417] | ||
Z-Arg-Leu-Val-Agly-Ala-Gly-NH2 | Drug Info | Ki = 6.76 nM | [526417] | ||
Z-Ala-Leu-Nal-Agly-Ile-Val-OMe | Drug Info | Ki = 5.75 nM | [526417] | ||
Z-Ala-Leu-Phe-Agly-Ile-Val-OMe | Drug Info | Ki = 0.18 nM | [526417] | ||
L-006235-1 | Drug Info | IC50 = 0.5 nM | [527882] | ||
4-cyclooctyl-6-propylpyrimidine-2-carbonitrile | Drug Info | IC50 = 11 nM | [530717] | ||
Pyrrolidine-1-carbonitrile | Drug Info | Ki = 2100 nM | [527556] | ||
Tert-butyl (2S)-1-cyanopyrrolidine-2-carboxylate | Drug Info | Ki = 60 nM | [527556] | ||
Z-Ala-Leu-Tyr(Me)-Agly-Ile-Val-OMe | Drug Info | Ki = 8.42 nM | [526417] | ||
N-(tert-butoxycarbonyl)-methionyl-glycine-nitrile | Drug Info | Ki = 730 nM | [527885] | ||
N-(tert-butoxycarbonyl)-norvalyl-glycine-nitrile | Drug Info | Ki = 1100 nM | [527885] | ||
N-benzoyl-phenylalanyl-glycine-nitrile | Drug Info | Ki = 1500 nM | [527885] | ||
N-(tert-butoxycarbonyl)-leucyl-glycine-nitrile | Drug Info | Ki = 120 nM | [527885] | ||
(S)-1-benzylcyclopentyl 1-oxohexan-2-ylcarbamate | Drug Info | IC50 = 0.35 nM | [527872] | ||
N-acetyl-phenylalanyl-glycine-nitrile | Drug Info | Ki = 7500 nM | [527885] | ||
BOCEPREVIR | Drug Info | IC50 = 40 nM | [530459] | ||
Relacatib | Drug Info | Ki = 0.75 nM | |||
2-cyclohexylamino-pyridine-2-carbonitrile | Drug Info | IC50 = 1000 nM | [528643] | ||
4-cyclohexylamino-pyrimidine-2-carbonitrile | Drug Info | IC50 = 170 nM | [528643] | ||
N-(tert-butoxycarbonyl)-valyl-glycine-nitrile | Drug Info | Ki = 6500 nM | [527885] | ||
L-873724 | Drug Info | IC50 = 0.8 nM | [536609] | ||
(S)-tert-butyl 4-methyl-1-oxopentan-2-ylcarbamate | Drug Info | IC50 = 31 nM | [527872] | ||
N-(1-((cyanomethyl)carbamoyl)cyclohexyl)benzamide | Drug Info | IC50 = 78 nM | [528002] | ||
N-(cyanomethyl)cyclohex-1-ene-1-carboxamide | Drug Info | IC50 = 3400 nM | [528002] | ||
Action against Disease Model | Odanacatib | Odanacatib show greater than 100-fold h uMan Cat K enzyme (IC50= 0.2nM) selectivity and have similar IC(50) values against each cathepsin in cell-based and enzyme assays. | [537348] | Drug Info | |
The Effect of Target Knockout, Knockdown or Genetic Variations | Cathepsin K-deficient mice, generated by targeted disruption of the cathepsin K gene exhibit an osteopetrotic phenotype characterized by thick bone trabeculae. | [537348] | |||
References | |||||
Ref 537348 | Pharmacological inhibitors to identify roles of cathepsin K in cell-based studies: a comparison of available tools. Biol Chem. 2009 May 20. | ||||
Ref 528643 | J Med Chem. 2007 Feb 22;50(4):591-4. Epub 2007 Jan 27.2-Cyano-pyrimidines: a new chemotype for inhibitors of the cysteine protease cathepsin K. | ||||
Ref 527197 | Bioorg Med Chem Lett. 2004 Oct 4;14(19):4897-902.Potent and selective P2-P3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P1', P1, and/or P3 substitutions. | ||||
Ref 530717 | Bioorg Med Chem Lett. 2010 Mar 1;20(5):1524-7. Epub 2010 Jan 25.Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors. | ||||
Ref 526417 | J Med Chem. 2002 Sep 12;45(19):4202-11.Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases. | ||||
Ref 526417 | J Med Chem. 2002 Sep 12;45(19):4202-11.Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases. | ||||
Ref 526417 | J Med Chem. 2002 Sep 12;45(19):4202-11.Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases. | ||||
Ref 526417 | J Med Chem. 2002 Sep 12;45(19):4202-11.Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases. | ||||
Ref 526417 | J Med Chem. 2002 Sep 12;45(19):4202-11.Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases. | ||||
Ref 526417 | J Med Chem. 2002 Sep 12;45(19):4202-11.Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases. | ||||
Ref 531005 | Bioorg Med Chem Lett. 2010 Aug 1;20(15):4447-50. Epub 2010 Jun 15.2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors. | ||||
Ref 527885 | J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles. | ||||
Ref 527885 | J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles. | ||||
Ref 530717 | Bioorg Med Chem Lett. 2010 Mar 1;20(5):1524-7. Epub 2010 Jan 25.Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors. | ||||
Ref 527885 | J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles. | ||||
Ref 527872 | Bioorg Med Chem Lett. 2006 Feb 15;16(4):978-83. Epub 2005 Nov 15.Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?. | ||||
Ref 527885 | J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles. | ||||
Ref 529350 | Bioorg Med Chem. 2009 Feb 1;17(3):1064-70. Epub 2008 Feb 7.Substrate optimization for monitoring cathepsin C activity in live cells. | ||||
Ref 531005 | Bioorg Med Chem Lett. 2010 Aug 1;20(15):4447-50. Epub 2010 Jun 15.2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors. | ||||
Ref 529711 | J Med Chem. 2008 Oct 23;51(20):6410-20. Epub 2008 Sep 24.Identification of a nonbasic, nitrile-containing cathepsin K inhibitor (MK-1256) that is efficacious in a monkey model of osteoporosis. | ||||
Ref 536609 | The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8. Epub 2008 Jan 15. | ||||
Ref 526417 | J Med Chem. 2002 Sep 12;45(19):4202-11.Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases. | ||||
Ref 526417 | J Med Chem. 2002 Sep 12;45(19):4202-11.Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases. | ||||
Ref 526417 | J Med Chem. 2002 Sep 12;45(19):4202-11.Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases. | ||||
Ref 526417 | J Med Chem. 2002 Sep 12;45(19):4202-11.Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases. | ||||
Ref 526417 | J Med Chem. 2002 Sep 12;45(19):4202-11.Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases. | ||||
Ref 526417 | J Med Chem. 2002 Sep 12;45(19):4202-11.Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases. | ||||
Ref 527882 | J Med Chem. 2005 Dec 1;48(24):7535-43.Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. | ||||
Ref 530717 | Bioorg Med Chem Lett. 2010 Mar 1;20(5):1524-7. Epub 2010 Jan 25.Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors. | ||||
Ref 527556 | Bioorg Med Chem Lett. 2005 Jun 15;15(12):3039-43.Acyclic cyanamide-based inhibitors of cathepsin K. | ||||
Ref 527556 | Bioorg Med Chem Lett. 2005 Jun 15;15(12):3039-43.Acyclic cyanamide-based inhibitors of cathepsin K. | ||||
Ref 526417 | J Med Chem. 2002 Sep 12;45(19):4202-11.Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases. | ||||
Ref 527885 | J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles. | ||||
Ref 527885 | J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles. | ||||
Ref 527885 | J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles. | ||||
Ref 527885 | J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles. | ||||
Ref 527872 | Bioorg Med Chem Lett. 2006 Feb 15;16(4):978-83. Epub 2005 Nov 15.Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?. | ||||
Ref 527885 | J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles. | ||||
Ref 530459 | Antimicrob Agents Chemother. 2010 Jan;54(1):305-11. Epub 2009 Oct 19.MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease. | ||||
Ref 528643 | J Med Chem. 2007 Feb 22;50(4):591-4. Epub 2007 Jan 27.2-Cyano-pyrimidines: a new chemotype for inhibitors of the cysteine protease cathepsin K. | ||||
Ref 528643 | J Med Chem. 2007 Feb 22;50(4):591-4. Epub 2007 Jan 27.2-Cyano-pyrimidines: a new chemotype for inhibitors of the cysteine protease cathepsin K. | ||||
Ref 527885 | J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles. | ||||
Ref 536609 | The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8. Epub 2008 Jan 15. | ||||
Ref 527872 | Bioorg Med Chem Lett. 2006 Feb 15;16(4):978-83. Epub 2005 Nov 15.Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?. | ||||
Ref 528002 | J Med Chem. 2006 Feb 9;49(3):1066-79.Beta-substituted cyclohexanecarboxamide: a nonpeptidic framework for the design of potent inhibitors of cathepsin K. | ||||
Ref 528002 | J Med Chem. 2006 Feb 9;49(3):1066-79.Beta-substituted cyclohexanecarboxamide: a nonpeptidic framework for the design of potent inhibitors of cathepsin K. |
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