Table 1. LXRα and LXRβ modulatory potency of compounds selected for phase 2.
Potency was determined in cellular Gal4-based hybrid reporter gene assays. EC50 values and fold activation are reported as mean ± SE (n = 3). n.d., not determined.
| ID | LXRα | LXRβ | Selectivity for LXRα | ||
| EC50 (μM) | Fold activation | EC50 (μM) | Fold activation | (LXRβ/LXRα) | |
| 1 | 4.5 ± 0.1 | 20.5 ± 0.2 | >10 | n.d. | >2.2 |
| 2 | >10 | n.d. | >10 | n.d. | n.d. |
| 3 | >10 | n.d. | >10 | n.d. | n.d. |
| 5 | 0.26 ± 0.01 | 18.1 ± 0.1 | 1.30 ± 0.03 | 25.3 ± 0.3 | 5.0 ± 0.2 |
| 6 | 0.183 ± 0.006 | 32.4 ± 0.2 | 0.40 ± 0.01 | 23.3 ± 0.1 | 2.19 ± 0.09 |
| 8 | 1.05 ± 0.01 | 15.2 ± 0.1 | 1.72 ± 0.04 | 24.7 ± 0.3 | 1.64 ± 0.04 |
| 9 | 1.68 ± 0.03 | 20.3 ± 0.1 | 4.0 ± 0.1 | 22.2 ± 0.1 | 2.38 ± 0.07 |
| 10 | 1.19 ± 0.01 | 11.2 ± 0.1 | 3.1 ± 0.1 | 20.0 ± 0.4 | 2.61 ± 0.09 |
| 11 | 1.31 ± 0.03 | 23.0 ± 0.2 | 2.37 ± 0.02 | 19.2 ± 0.1 | 1.81 ± 0.04 |
| 12 | 0.8 ± 0.3 | 24.7 ± 0.7 | 1.08 ± 0.02 | 27.9 ± 0.3 | 1.4 ± 0.5 |
| 13 | 1.1 ± 0.1 | 13.5 ± 0.2 | 2.23 ± 0.02 | 19.0 ± 0.1 | 2.0 ± 0.2 |
| 14 | 0.30 ± 0.01 | 26.6 ± 0.1 | 1.41 ± 0.02 | 30.1 ± 0.2 | 4.7 ± 0.2 |
| 15 | 0.24 ± 0.04 | 22 ± 2 | 0.34 ± 0.02 | 38.3 ± 0.3 | 1.4 ± 0.3 |
| 17 | 0.21 ± 0.02 | 18.5 ± 0.1 | 1.25 ± 0.01 | 22.9 ± 0.1 | 6.0 ± 0.6 |