CID/MLTargetEC50 [SID, AID]Anti-TargetEC50 [SID, AID]Fold SelectiveSecondary Assays:
EC50 (nM) [SID, AID]
NEW Probe: CID 53239856/ML244PPARγ Lantha Binding Assay80 nM [SID 124349301, AID 504943] ActivePPARα>10 μM [SID 124349301] Inactive>125PPRE::Luc Transactivation Reporter Assay: Inactive [SID 124349301, AID 504939] Probe is a ligand, non agonist.
Inhibition of Cdk5-Mediated PPARγ Phosphorylation: Active [SID 124349301, AID 504938]
Efficacy Studies: Reductions in Ob/Ob Mouse Glucose and Insulin Levels: Active [SID 124349301, AID 540293].
Modulation of Adipocyte Differentiation Genes: Inactive [SID 124349301, AID 540286 (Ap2); 540289 (PPARγ); 540290 (CD36); 540291 (LPL); 540292 (FASN); 540294 (Glut4)]
Modulation of Osteoblast Differentiation Genes: Inactive [SID 124349301, 540282 (PPARγ); AID 540283 (RANKL); 540284 (COLI); 540285 (Alp)]
Old Probe: CID 1328217/ML215194 nM [SID 91762765, (AID 504446] ActivePPARα>3 μM [SID 91762765, AID 504735] Inactive>10.6PPRE::Luc Transactivation Assay (2X%INH): 48% of Rosi and 98% of MRL-24 activity; [SID 91762765, AID 504452] Active. Old probe is a partial agonist.
PPRE::Luc Dose Response Assay: 0.283 μM [SID 91762765, AID 504447] Active
PPARγ PolarScreen Binding Assay: 152 nM [SID 91762765, AID 504453] Active.

From: Potent Anti-Diabetic Actions of a Novel Non-Agonist PPARγ Ligand that Blocks Cdk5-Mediated Phosphorylation

Cover of Probe Reports from the NIH Molecular Libraries Program
Probe Reports from the NIH Molecular Libraries Program [Internet].

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