Target Validation Information
TTD ID T58921
Target Name Peroxisome proliferator-activated receptor gamma (PPAR-gamma)
Type of Target
Successful
Drug Potency against Target Pioglitazone Drug Info EC50 = 580 nM [3]
Rosiglitazone XR Drug Info EC50 = 40 nM [3]
Netoglitazone Drug Info EC50 = 100 nM [2]
Rosiglitazone + metformin Drug Info EC50 = 200 nM [5]
Rosiglitazone + simvastatin Drug Info IC50 = 23 nM [4]
TESAGLITAZAR Drug Info Ki = 200 nM [1]
References
REF 1 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 2 Treatment of non-insulin-dependent diabetes mellitus. Expert Opin Investig Drugs. 2003 Apr;12(4):623-33.
REF 3 Nuclear receptors as potential targets for modulating reverse cholesterol transport. Curr Top Med Chem. 2005;5(3):265-82.
REF 4 Targeting the cell division cycle in cancer: CDK and cell cycle checkpoint kinase inhibitors. Curr Opin Pharmacol. 2005 Aug;5(4):366-73.
REF 5 A potent antidiabetic thiazolidinedione with unique peroxisome proliferator-activated receptor gamma-activating properties. J Biol Chem. 1998 Dec 4;273(49):32679-84.

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