Target Validation Information
TTD ID	T86591
Target Name	Peroxisome proliferator-activated receptor alpha (PPARA)
Type of Target	Successful
Drug Potency against Target	Fenofibrate	Drug Info	EC50 = 55000 nM	[11]
	Netoglitazone	Drug Info	EC50 = 3000 nM	[10]
	(9Z,12E)-12-nitrooctadeca-9,12-dienoic acid	Drug Info	IC50 = 9600 nM	[8]
	(E)-12-Nitrooctadec-12-enoic Acid	Drug Info	IC50 = 1600 nM	[8]
	(E)-13-Nitrooctadec-12-enoic Acid	Drug Info	IC50 = 1100 nM	[8]
	BMS-687453	Drug Info	IC50 = 260 nM	[9]
	FARGLITAZAR	Drug Info	IC50 = 2870 nM	[5]
	GSK-9578	Drug Info	IC50 = 120 nM	[3]
	GW-501516	Drug Info	IC50 = 463 nM	[6]
	KRP-297	Drug Info	Ki = 230 nM	[4]
	L-165461	Drug Info	IC50 = 570 nM	[1]
	L-796449	Drug Info	IC50 = 54 nM	[1]
	MURAGLITAZAR	Drug Info	IC50 = 190 nM	[7]
	PIRINIXIC ACID	Drug Info	Ki = 100 nM	[2]
	Ragaglitazar	Drug Info	Ki = 980 nM	[4]
	TESAGLITAZAR	Drug Info	Ki = 1000 nM	[4]
References
REF 1	Phenylacetic acid derivatives as hPPAR agonists. Bioorg Med Chem Lett. 2003 Apr 7;13(7):1277-80.
REF 2	O-arylmandelic acids as highly selective human PPAR alpha/gamma agonists. Bioorg Med Chem Lett. 2003 Oct 6;13(19):3185-90.
REF 3	Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist. J Med Chem. 2003 Nov 20;46(24):5121-4.
REF 4	Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes. J Med Chem. 2004 Aug 12;47(17):4118-27.
REF 5	Discovery of tertiary aminoacids as dual PPARalpha/gamma agonists-I. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2312-6.
REF 6	Synthesis and SAR of selective benzothiophene, benzofuran, and indole-based peroxisome proliferator-activated receptor delta agonists. Bioorg Med Chem Lett. 2007 Jul 1;17(13):3630-5.
REF 7	Design, synthesis, and structure-activity relationships of piperidine and dehydropiperidine carboxylic acids as novel, potent dual PPARalpha/gamma ... Bioorg Med Chem Lett. 2008 Jun 15;18(12):3545-50.
REF 8	Activation of peroxisome proliferator-activated receptor gamma (PPARgamma) by nitroalkene fatty acids: importance of nitration position and degree ... J Med Chem. 2009 Aug 13;52(15):4631-9.
REF 9	Discovery of an oxybenzylglycine based peroxisome proliferator activated receptor alpha selective agonist 2-((3-((2-(4-chlorophenyl)-5-methyloxazol... J Med Chem. 2010 Apr 8;53(7):2854-64.
REF 10	Treatment of non-insulin-dependent diabetes mellitus. Expert Opin Investig Drugs. 2003 Apr;12(4):623-33.
REF 11	Nuclear receptors as potential targets for modulating reverse cholesterol transport. Curr Top Med Chem. 2005;5(3):265-82.

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