Table 3. EC50 Values Observed in the TR-FRET Coactivator Recruitment Assay, IC50 Values from the TR-FRET Competition Assay with PPARγ, and ΔTm Values (°C) from TSA Assaysa.
| fold-selective for
RORγt over PPARγ |
|||||
|---|---|---|---|---|---|
| compound | EC50 (μM) PPARγ | IC50 (μM) PPARγ (competition rosiglitazone) | ΔTm (°C) PPARγ | TR-FRET | TSA |
| 1 | 0.34 ± 0.02 | 6.3 ± 0.7 | 2.5 ± 0.2 | 26 | 3.1 |
| 2 | 8.2 ± 0.3 | 81 ± 7 | 0.3 ± 0.0 | 30 | 8.0 |
| 3 | 3.1 ± 0.1 | 63 ± 8 | 0.6 ± 0.0 | 100 | 8.1 |
| 4 | 18 ± 1 | >100 | 0.7 ± 0.0 | 2.7 | 0.5 |
| 5 | >100 | >100 | 0.0 ± 0.0 | ||
| 6 | 2.5 ± 0.1 | 64 ± 3 | 1.1 ± 0.2 | 125 | 5.8 |
| 7 | 7.5 ± 0.3 | >100 | 0.1 ± 0.0 | 15 | 7.0 |
| 8 | 15 ± 1 | >100 | 0.1 ± 0.0 | 1.6 | 7.0 |
| 9 | 5.8 ± 0.2 | 67 ± 6 | 0.4 ± 0.0 | 67 | 7.5 |
| 10 | 1.7 ± 0.1 | 29 ± 4 | 1.2 ± 0.0 | 7.1 | 2.3 |
| 11 | 3.6 ± 0.1 | 79 ± 11 | 0.7 ± 0.0 | 33 | 3.9 |
| 12 | 1.2 ± 0.1 | 20 ± 2 | 1.5 ± 0.0 | 0.36 | <0.1 |
| 13 | 0.79 ± 0.10 | 19 ± 3 | 1.5 ± 0.0 | 0.27 | <0.1 |
a
TR-FRET and TSA data are recorded in triplicate; values are representative of ≥3 repeated experiments.