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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