Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T05114 | ||||
Target Name | Chymase (CYM) | ||||
Type of Target |
Clinical trial |
||||
Drug Potency against Target | Drug Info | IC50 = 3530 nM | [3] | ||
Drug Info | IC50 = 32 nM | [4] | |||
CHYMOSTATIN | Drug Info | IC50 = 43 nM | [2] | ||
JNJ-10311795 | Drug Info | Ki = 2.3 nM | [1] | ||
Rac-2q | Drug Info | IC50 = 39 nM | [2] | ||
References | |||||
REF 1 | Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase. J Med Chem. 2007 Apr 19;50(8):1727-30. | ||||
REF 2 | Identification of 6-substituted 4-arylsulfonyl-1,4-diazepane-2,5-diones as a novel scaffold for human chymase inhibitors. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3431-4. | ||||
REF 3 | Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer. J Med Chem. 2008 Feb 28;51(4):1068-72. | ||||
REF 4 | MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease. Antimicrob Agents Chemother. 2010 Jan;54(1):305-11. | ||||
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