Table 3. Cytochrome P450 inhibition data for compounds 5b, 5d and BMS-790052a.
| CYP1A2 (μM) | CYP3A4 (μM) | CYP2D6 (μM) | CYP2C9 (μM) | |||||
|---|---|---|---|---|---|---|---|---|
|
| ||||||||
| Cmpd | IC50 | IC90 | IC50 | IC90 | IC50 | IC90 | IC50 | IC90 |
| 5b | > 100 | > 100 | 13.8 ± 11.2 | > 100 | > 100 | > 100 | 81.6 ± 26.1 | > 100 |
| 5d | > 100 | > 100 | 3.1 ± 2.3 | > 100 | > 100 | > 100 | > 100 | > 100 |
| BMS-790052 | > 100 | > 100 | 7.2 ± 1.7 | > 100 | > 100 | > 100 | 59.5 ± 13.6 | > 100 |
a
Mean ± SD of at least two independent assays; IC50 = 50% inhibitory concentration. The following positive controls were used (IC50, μM): α -naphthoflavone for 1A2 (> 93% at 3 μM); ketoconazole for 3A4 (> 93% at 10 μM); PH-053 (proprietary) for 2D6 (> 70% at 100 μM); sulfaphenazole for 2C9 (> 90% at 10 μM).