Table 3. In Vitro Profile of Compound 18.
| RORγt GAL4 EC50 (nM) | 16 ± 9 |
|---|---|
| RORα GAL4 EC50 (nM) | >10 000 |
| RORβ GAL4 EC50 (nM) | 8400 ± 2100 |
| IL-17 hWB EC50 (nM) | 43 ± 24 |
| mouse Th17 EC50 (nM) | 25 ± 20 |
| PXR EC50 (nM) | >50 000 |
| LXRα EC50 (nM) | >7500 |
| LXRβ EC50 (nM) | >7500 |
| rCYP IC50 (nM) | |
| 1A2 | >20 000 |
| 2C8 | >20 000 |
| 2C9 | 4900 |
| 2C19 | >20 000 |
| 2D6 | >20 000 |
| 3A4 | >20 000 |
| HepG2 EC50 (nM) | >100 000 |
| LM t1/2 (min) h, m, r | >120, >120, >120 |
| protein binding, % free (h, m) | 2.5, 1.3 |
| CACO-2 A-B, B-A (nm/s) | 93, 190 |
| CACO-2 efflux ratio | 2.0 |
| solubility (mg/mL): | |
| @pH 1 (0.1 N HCl solvent) | <0.001 |
| @pH 4 (50 nM acetate buffer) | <0.001 |
| @pH 6.5 (50 nM acetate buffer) | <0.001 |