Target Validation Information
Target ID T03818
Target Name mRNA of PPAR-gamma
Target Type
Research
Drug Potency against Target BRL-48482 Drug Info Ki = 22 nM
GNF-PF-3037 Drug Info IC50 = 10496 nM [531262]
GNF-PF-2893 Drug Info IC50 = 503.39 nM [531262]
PLOGLITAZONE Drug Info Ki = 1200 nM [527158]
MURAGLITAZAR Drug Info IC50 = 250 nM [529499]
FARGLITAZAR Drug Info IC50 = 217 nM [528666]
L-165461 Drug Info IC50 = 110 nM [526582]
L-796449 Drug Info IC50 = 94 nM [526582]
CHLOROCYCLINONE D Drug Info IC50 = 4400 nM [529182]
CHLOROCYCLINONE C Drug Info IC50 = 600 nM [529182]
CHLOROCYCLINONE B Drug Info IC50 = 1400 nM [529182]
L-Tryptophan-L-aspartic acid Drug Info IC50 = 5200 nM [529363]
Ragaglitazar Drug Info Ki = 90 nM [527158]
MBX-102 Drug Info IC50 = 220 nM [529363]
CHLOROCYCLINONE A Drug Info IC50 = 160 nM [529182]
L-Tryptophan-L-2-aminoadipic acid Drug Info IC50 = 15100 nM [529363]
GW-9662 Drug Info IC50 = 3300 nM [529363]
(E)-6-Nitrooctadec-5-enoic Acid Drug Info IC50 = 1720 nM [530350]
(E)-10-Nitrohexadec-9-enoic Acid Drug Info IC50 = 630 nM [530350]
(E)-9-nitrooctadec-9-enoic acid Drug Info IC50 = 980 nM [530350]
(E)-9-Nitrohexadec-9-enoicAcid Drug Info IC50 = 830 nM [530350]
L-Tryptophan-L-glutamine Drug Info IC50 = 18700 nM [529363]
L-Tryptophan-L-arginine Drug Info IC50 = 15400 nM [529363]
SB-213068 Drug Info Ki = 2.5 nM
(E)-5-Nitrooctadec-5-enoic Acid Drug Info IC50 = 1680 nM [530350]
(9Z,12E)-12-nitrooctadeca-9,12-dienoic acid Drug Info IC50 = 410 nM [530350]
2-chloro-5-nitro-N-(pyridin-4-yl)benzamide Drug Info IC50 = 1000 nM [529363]
L-Tryptophan-L-asparagine Drug Info IC50 = 18400 nM [529363]
PD-068235 Drug Info IC50 = 820 nM [529363]
KRP-297 Drug Info Ki = 330 nM [527158]
(E)-13-Nitrooctadec-12-enoic Acid Drug Info IC50 = 190 nM [530350]
(E)-10-nitrooctadec-9-enoic acid Drug Info IC50 = 1610 nM [530350]
(E)-12-Nitrooctadec-12-enoic Acid Drug Info IC50 = 39 nM [530350]
TESAGLITAZAR Drug Info Ki = 18 nM [529295]
References
Ref 531262Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2).
Ref 531262Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2).
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 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 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 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 529182J Nat Prod. 2007 Dec;70(12):1934-8. Epub 2007 Nov 29.Chlorocyclinones A-D, chlorinated angucyclinones from Streptomyces sp. strongly antagonizing rosiglitazone-induced PPAR-gamma activation.
Ref 529182J Nat Prod. 2007 Dec;70(12):1934-8. Epub 2007 Nov 29.Chlorocyclinones A-D, chlorinated angucyclinones from Streptomyces sp. strongly antagonizing rosiglitazone-induced PPAR-gamma activation.
Ref 529182J Nat Prod. 2007 Dec;70(12):1934-8. Epub 2007 Nov 29.Chlorocyclinones A-D, chlorinated angucyclinones from Streptomyces sp. strongly antagonizing rosiglitazone-induced PPAR-gamma activation.
Ref 529363Eur J Med Chem. 2008 Dec;43(12):2699-716. Epub 2008 Feb 3.Tryptophan-containing dipeptide derivatives as potent PPARgamma antagonists: design, synthesis, biological evaluation, and molecular modeling.
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 529363Eur J Med Chem. 2008 Dec;43(12):2699-716. Epub 2008 Feb 3.Tryptophan-containing dipeptide derivatives as potent PPARgamma antagonists: design, synthesis, biological evaluation, and molecular modeling.
Ref 529182J Nat Prod. 2007 Dec;70(12):1934-8. Epub 2007 Nov 29.Chlorocyclinones A-D, chlorinated angucyclinones from Streptomyces sp. strongly antagonizing rosiglitazone-induced PPAR-gamma activation.
Ref 529363Eur J Med Chem. 2008 Dec;43(12):2699-716. Epub 2008 Feb 3.Tryptophan-containing dipeptide derivatives as potent PPARgamma antagonists: design, synthesis, biological evaluation, and molecular modeling.
Ref 529363Eur J Med Chem. 2008 Dec;43(12):2699-716. Epub 2008 Feb 3.Tryptophan-containing dipeptide derivatives as potent PPARgamma antagonists: design, synthesis, biological evaluation, and molecular modeling.
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 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 529363Eur J Med Chem. 2008 Dec;43(12):2699-716. Epub 2008 Feb 3.Tryptophan-containing dipeptide derivatives as potent PPARgamma antagonists: design, synthesis, biological evaluation, and molecular modeling.
Ref 529363Eur J Med Chem. 2008 Dec;43(12):2699-716. Epub 2008 Feb 3.Tryptophan-containing dipeptide derivatives as potent PPARgamma antagonists: design, synthesis, biological evaluation, and molecular modeling.
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 529363Eur J Med Chem. 2008 Dec;43(12):2699-716. Epub 2008 Feb 3.Tryptophan-containing dipeptide derivatives as potent PPARgamma antagonists: design, synthesis, biological evaluation, and molecular modeling.
Ref 529363Eur J Med Chem. 2008 Dec;43(12):2699-716. Epub 2008 Feb 3.Tryptophan-containing dipeptide derivatives as potent PPARgamma antagonists: design, synthesis, biological evaluation, and molecular modeling.
Ref 529363Eur J Med Chem. 2008 Dec;43(12):2699-716. Epub 2008 Feb 3.Tryptophan-containing dipeptide derivatives as potent PPARgamma antagonists: design, synthesis, biological evaluation, and molecular modeling.
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 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 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 529295Bioorg Med Chem Lett. 2008 Mar 1;18(5):1617-22. Epub 2008 Jan 19.4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part I: synthesis and pharmacological evaluation.

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