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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