TABLE 2.
EC50 values for compounds 1 and 3
| Compound | FXR EC50 a |
FXR EC50 b |
GPBAR1 EC50 b |
|---|---|---|---|
| BAR502 | 0.69 ± 0.15 | 2.0 ± 0.2 | 0.4 ± 0.1 |
| 1 | 3.4 ± 1.2 | 2.80 ± 0.01 | 0.37 ± 0.02 |
| 3 | 17.9 ± 2.6 | 25.0 ± 0.01 | 1.8 ± 0.35 |
a
EC50 measured by AlphaScreen coactivator recruitment assay measuring a direct interaction of FXR, with SRC-1; compounds were tested at 10 μM for FXR.
b
Transactivation assays on HepG2 cells or HEK-293T, cells. EC50 values (μM) were calculated from at least three experiments. Results are expressed as mean ± SD.