Table 1. In Vitro PPARγ Profile of Compounds 1, 7, and 10.
| compound | 1 | 7 | 10 |
|---|---|---|---|
| PPARγ binding IC50 (nM)a | 90 ± 27 | 154 ± 12 | 24 ± 14 |
| PPARγ GAL4 reporter gene EC50 (nM)/max agonist effectb (%)a | 27 ± 16/86 ± 17 | 726c/28 ± 7 | >50 000/27 ± 7 |
| PPARγ pS273 IC50 (nM)a | 4,400 ± 820 | 580 ± 44 | 160 ± 6 |
Values presented as the mean ± standard deviation (n ≥ 3).
Agonist effect at the highest assay concentration (50 μM).
Estimated EC50. (See the Supporting Information.)