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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