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| |
CYP450
IC50 values (μM)a |
|||
|---|---|---|---|---|
| compound | X | R | CYP2D6 | CYP3A4 |
| 2a | H | OH | 18 ± 0.8 | 17 ± 3.4 |
| 2i, DQP-997-74 | F | OH | >20 | >20 |
| 2k | F | NH2 | >20b | 2.0 ± 0.4b |
| 2l | F | OEt | >20 | 7.8 ± 0.1 |
| 2m | F | Oi-Pr | >20 | 6.3 ± 1.1 |
| 2n | F | OCH2C3H5 | >20 | 6.7 ± 1.2 |
| 2o | F | ONp | >20 | 12 ± 0.04 |
| 2p | F | OBn | >20 | >20 |
| 2q | F | NHMe | >20 | 7.7 ± 1.7 |
| 2r | F | NMe2 | >20 | >20 |
n = 2.
n = 4/Compounds 2i (DQP-997-74), 2l, 2m, 2n, 2o, and 2p show some degree of autoactivation of CYP2D6.
