Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T14834 | ||||
Target Name | Cytosolic phospholipase A2 (GIVA cPLA2) | ||||
Type of Target |
Clinical trial |
||||
Drug Potency against Target | Drug Info | IC50 = 500 nM | [4] | ||
Drug Info | IC50 = 11 nM | [4] | |||
4-(2-oxohexadecanamido)butanoic acid | Drug Info | IC50 = 4400 nM | [1] | ||
ARACHIDONYL TRIFLUOROMETHYLKETONE | Drug Info | IC50 = 2300 nM | [4] | ||
ECOPLADIB | Drug Info | IC50 = 150 nM | [3] | ||
EFIPLADIB | Drug Info | IC50 = 40 nM | [3] | ||
WAY-196025 | Drug Info | IC50 = 10 nM | [3] | ||
[3,4''']biflavone | Drug Info | IC50 = 8420 nM | [2] | ||
[4',4''']-biflavone | Drug Info | IC50 = 6000 nM | [2] | ||
[6,3''']biflavone | Drug Info | IC50 = 16800 nM | [2] | ||
[6,4''']biflavone | Drug Info | IC50 = 11900 nM | [2] | ||
References | |||||
REF 1 | Discovery of Ecopladib, an indole inhibitor of cytosolic phospholipase A2alpha. J Med Chem. 2007 Mar 22;50(6):1380-400. | ||||
REF 2 | Inhibitory effect of synthetic C-C biflavones on various phospholipase A(2)s activity. Bioorg Med Chem. 2007 Nov 15;15(22):7138-43. | ||||
REF 3 | Reactions of functionalized sulfonamides: application to lowering the lipophilicity of cytosolic phospholipase A2alpha inhibitors. J Med Chem. 2009 Feb 26;52(4):1156-71. | ||||
REF 4 | 1-Indol-1-yl-propan-2-ones and related heterocyclic compounds as dual inhibitors of cytosolic phospholipase A(2)alpha and fatty acid amide hydrolase. Bioorg Med Chem. 2010 Jan 15;18(2):945-52. | ||||
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