Table 2.
Calculated Ki-values of the bile acid analogues for NTCP, OATP1B1, and BSEP. Data are mean ± SD (n = 3). ∗3βFCA IC50-values were extracted from literature [13] and used to calculate the Ki-values.
| Ki for NTCP (µM) | Ki for OATP1B1 (µM) | Ki for BSEP (µM) | |
|---|---|---|---|
| CA | 12.96 ± 4.26 | 42.70 ± 0.16 | 95.46 ± 33.97 |
| 3αFCA | 2.53 ± 0.76 | 5.22 ± 0.56 | 198.93 ± 39.47 |
| 3βFCA∗ | 6.18 ± 0.59 | 9.67 ± 0.83 | 216.30 ± 52.99 |
| 3βFGCA | 1.09 ± 0.34 | 4.24 ± 0.16 | 87.38 ± 14.61 |
| 3βFCDCA | 0.91 ± 0.02 | 0.64 ± 0.07 | 48.24 ± 3.94 |
| 12βFCA | 30.08 ± 9.40 | 4.56 ± 0.25 | 367.02 ± 38.11 |