Target Validation Information
TTD ID	T14834
Target Name	Cytosolic phospholipase A2 (GIVA cPLA2)
Type of Target	Clinical trial
Drug Potency against Target	1-Imidazol-1-yl-3-(4-octylphenoxy)propan-2-one	Drug Info	IC50 = 500 nM	[4]
	4-(2-oxohexadecanamido)butanoic acid	Drug Info	IC50 = 4400 nM	[1]
	AR-C70484XX	Drug Info	IC50 = 11 nM	[4]
	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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