Table 3. CYP Inhibition of Compounds 18–21.
compound | 1A2 IC50 (uM)a | 2C9 IC50 (uM)a | 2C19 IC50 (uM)a | 2D6 IC50 (uM)a | 3A4 IC50 (uM)a m/tb |
---|---|---|---|---|---|
18 | >10 | >10 | >10 | >10 | 8.4/6.08 |
19 | 8.95 | 0.94 | 1.15 | 9.61 | 0.35/0.95 |
20 | >10 | 7.4 | 6.81 | >10 | 4.57/2.6 |
21 | >10 | 0.3 | 1.57 | 4.51 | 0.21/0.44 |
Values are expressed as the mean of three independent determinations.
Midazolam as substrate/testosterone as substrate.