Target Validation Information
Target ID T86591
Target Name Peroxisome proliferator activated receptor alpha
Target Type
Successful
Drug Potency against Target GW-501516 Drug Info IC50 = 463 nM [528850]
Fenofibrate Drug Info EC50 = 55000 nM [552515]
MURAGLITAZAR Drug Info IC50 = 190 nM [529499]
Ragaglitazar Drug Info Ki = 980 nM [527158]
BMS-687453 Drug Info IC50 = 260 nM [530777]
KRP-297 Drug Info Ki = 230 nM [527158]
GSK-9578 Drug Info IC50 = 120 nM [526879]
L-796449 Drug Info IC50 = 54 nM [526582]
L-165461 Drug Info IC50 = 570 nM [526582]
(9Z,12E)-12-nitrooctadeca-9,12-dienoic acid Drug Info IC50 = 9600 nM [530350]
(E)-13-Nitrooctadec-12-enoic Acid Drug Info IC50 = 1100 nM [530350]
FARGLITAZAR Drug Info IC50 = 2870 nM [528666]
(E)-12-Nitrooctadec-12-enoic Acid Drug Info IC50 = 1600 nM [530350]
PIRINIXIC ACID Drug Info Ki = 100 nM [526707]
TESAGLITAZAR Drug Info Ki = 1000 nM [527158]
Netoglitazone Drug Info EC50 = 3000 nM [552339]
References
Ref 528850Bioorg Med Chem Lett. 2007 Jul 1;17(13):3630-5. Epub 2007 Apr 24.Synthesis and SAR of selective benzothiophene, benzofuran, and indole-based peroxisome proliferator-activated receptor delta agonists.
Ref 552515Nuclear receptors as potential targets for modulating reverse cholesterol transport. Curr Top Med Chem. 2005;5(3):265-82.
Ref 529499Bioorg Med Chem Lett. 2008 Jun 15;18(12):3545-50. Epub 2008 May 6.Design, synthesis, and structure-activity relationships of piperidine and dehydropiperidine carboxylic acids as novel, potent dual PPARalpha/gamma agonists.
Ref 527158J Med Chem. 2004 Aug 12;47(17):4118-27.Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.
Ref 530777J Med Chem. 2010 Apr 8;53(7):2854-64.Discovery of an oxybenzylglycine based peroxisome proliferator activated receptor alpha selective agonist 2-((3-((2-(4-chlorophenyl)-5-methyloxazol-4-yl)methoxy)benzyl)(methoxycarbonyl)amino)acetic acid (BMS-687453).
Ref 527158J Med Chem. 2004 Aug 12;47(17):4118-27.Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.
Ref 526879J Med Chem. 2003 Nov 20;46(24):5121-4.Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist.
Ref 526582Bioorg Med Chem Lett. 2003 Apr 7;13(7):1277-80.Phenylacetic acid derivatives as hPPAR agonists.
Ref 526582Bioorg Med Chem Lett. 2003 Apr 7;13(7):1277-80.Phenylacetic acid derivatives as hPPAR agonists.
Ref 530350J Med Chem. 2009 Aug 13;52(15):4631-9.Activation of peroxisome proliferator-activated receptor gamma (PPARgamma) by nitroalkene fatty acids: importance of nitration position and degree of unsaturation.
Ref 530350J Med Chem. 2009 Aug 13;52(15):4631-9.Activation of peroxisome proliferator-activated receptor gamma (PPARgamma) by nitroalkene fatty acids: importance of nitration position and degree of unsaturation.
Ref 528666Bioorg Med Chem Lett. 2007 Apr 15;17(8):2312-6. Epub 2007 Jan 25.Discovery of tertiary aminoacids as dual PPARalpha/gamma agonists-I.
Ref 530350J Med Chem. 2009 Aug 13;52(15):4631-9.Activation of peroxisome proliferator-activated receptor gamma (PPARgamma) by nitroalkene fatty acids: importance of nitration position and degree of unsaturation.
Ref 526707Bioorg Med Chem Lett. 2003 Oct 6;13(19):3185-90.O-arylmandelic acids as highly selective human PPAR alpha/gamma agonists.
Ref 527158J Med Chem. 2004 Aug 12;47(17):4118-27.Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.
Ref 552339Treatment of non-insulin-dependent diabetes mellitus. Expert Opin Investig Drugs. 2003 Apr;12(4):623-33.

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