Target Validation Information
TTD ID	T03818
Target Name	PPAR-gamma messenger RNA (PPARG mRNA)
Type of Target	Literature-reported
Drug Potency against Target	(9Z,12E)-12-nitrooctadeca-9,12-dienoic acid	Drug Info	IC50 = 410 nM	[8]
	(E)-10-Nitrohexadec-9-enoic Acid	Drug Info	IC50 = 630 nM	[8]
	(E)-10-nitrooctadec-9-enoic acid	Drug Info	IC50 = 1610 nM	[8]
	(E)-12-Nitrooctadec-12-enoic Acid	Drug Info	IC50 = 39 nM	[8]
	(E)-13-Nitrooctadec-12-enoic Acid	Drug Info	IC50 = 190 nM	[8]
	(E)-5-Nitrooctadec-5-enoic Acid	Drug Info	IC50 = 1680 nM	[8]
	(E)-6-Nitrooctadec-5-enoic Acid	Drug Info	IC50 = 1720 nM	[8]
	(E)-9-Nitrohexadec-9-enoicAcid	Drug Info	IC50 = 830 nM	[8]
	(E)-9-nitrooctadec-9-enoic acid	Drug Info	IC50 = 980 nM	[8]
	2-chloro-5-nitro-N-phenylbenzamide	Drug Info	IC50 = 3300 nM	[6]
	BRL-48482	Drug Info	Ki = 22 nM
	CHLOROCYCLINONE A	Drug Info	IC50 = 160 nM	[4]
	CHLOROCYCLINONE B	Drug Info	IC50 = 1400 nM	[4]
	CHLOROCYCLINONE C	Drug Info	IC50 = 600 nM	[4]
	CHLOROCYCLINONE D	Drug Info	IC50 = 4400 nM	[4]
	FARGLITAZAR	Drug Info	IC50 = 217 nM	[3]
	GNF-PF-2893	Drug Info	IC50 = 503.39 nM	[9]
	GNF-PF-3037	Drug Info	IC50 = 10496 nM	[9]
	KRP-297	Drug Info	Ki = 330 nM	[2]
	L-165461	Drug Info	IC50 = 110 nM	[1]
	L-796449	Drug Info	IC50 = 94 nM	[1]
	L-Tryptophan-L-2-aminoadipic acid	Drug Info	IC50 = 15100 nM	[6]
	L-Tryptophan-L-arginine	Drug Info	IC50 = 15400 nM	[6]
	L-Tryptophan-L-asparagine	Drug Info	IC50 = 18400 nM	[6]
	L-Tryptophan-L-aspartic acid	Drug Info	IC50 = 5200 nM	[6]
	L-Tryptophan-L-glutamine	Drug Info	IC50 = 18700 nM	[6]
	MBX-102	Drug Info	IC50 = 220 nM	[6]
	MURAGLITAZAR	Drug Info	IC50 = 250 nM	[7]
	PD-068235	Drug Info	IC50 = 820 nM	[6]
	Ploglitazone	Drug Info	Ki = 1200 nM	[2]
	Ragaglitazar	Drug Info	Ki = 90 nM	[2]
	SB-213068	Drug Info	Ki = 2.5 nM
	T0070907	Drug Info	IC50 = 1000 nM	[6]
	TESAGLITAZAR	Drug Info	Ki = 18 nM	[5]
References
REF 1	Phenylacetic acid derivatives as hPPAR agonists. Bioorg Med Chem Lett. 2003 Apr 7;13(7):1277-80.
REF 2	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 3	Discovery of tertiary aminoacids as dual PPARalpha/gamma agonists-I. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2312-6.
REF 4	Chlorocyclinones A-D, chlorinated angucyclinones from Streptomyces sp. strongly antagonizing rosiglitazone-induced PPAR-gamma activation. J Nat Prod. 2007 Dec;70(12):1934-8.
REF 5	4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part I: synthesis and pharmacological evaluation. Bioorg Med Chem Lett. 2008 Mar 1;18(5):1617-22.
REF 6	Tryptophan-containing dipeptide derivatives as potent PPARgamma antagonists: design, synthesis, biological evaluation, and molecular modeling. Eur J Med Chem. 2008 Dec;43(12):2699-716.
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	In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6.

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