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| CYP450
inhibition (μM) |
|||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| compd | human whole plasma (DXS activation 6.25 μg/mL) PKa IC50 (nM) | potency ratio isolated IC50:plasma IC50 | hERGa (μM) | 1A2 | 2B6 | 2C8 | 2C9 | 2C19 | 2D6 | 3A4(M) | 3A4(T) |
| 13b | 500 | 1:84 | >33 | >25 | >25 | 14 | 13 | >25 | >25 | 19 | 11 |
| 14w | 54 | 1:9 | >33 | >25 | >25 | >25 | >25 | >25 | >25 | >25 | >25 |
| 16 | 76 | 1:24 | >33 | >25 | n.d. | n.d. | >25 | >25 | >25 | >25 | >25 |
hERG measured using a whole cell (Chinese hamster ovary) patch clamp technique.
