Table 1. Cofactor recruitment profile of F12016 bound to PPARγ.
| Cofactor | Rosiglitazone | F12016 | ||
|---|---|---|---|---|
| EC50/IC50 (nM) | Efficacy (%) | EC50/IC50 (nM) | Efficacy (%) | |
| TRAP220 | 24 | 100 | 5132 | 17 |
| RAP250 | 15 | 100 | 5765 | 25 |
| CBP | 52 | 100 | 349 | 10 |
| PGC-1α | 35 | 100 | 21810 | 57 |
| SRC1 | 102 | 100 | 17650 | 26 |
| TIF2 | 54 | 100 | 6437 | 17 |
| SRC3 | 122 | 100 | 15060 | 23 |
| NCoR | 7 | 100 | 4425 | 91 |
| SMRT | 50 | 100 | 2861 | 58 |
Effective (EC50) or inhibitory (IC50) concentrations and efficacy of F12016-induced recruitment of cofactor peptides to PPARγ were measured using a TR-FRET assay. Efficacy is the maximum recruitment relative to rosiglitazone-induced activation of PPAR.