Table 5. In Vitro CYP Inhibition with 36.
Enzyme | Substrate | Control Inhibitor (IC50 (μM)) | Cmpd 36 IC50 (μM) |
---|---|---|---|
CYP1A2 | Phenacetin | Furafylline (6.29) | 58.6 |
CYP2C8 | Paclitaxel | Quercetin (1.20) | 7.9 |
CYP2C9 | Tolbutamide | Sulfaphenazole (0.205) | 8.5 |
CYP2C19 | S-Mephentoin | Tranylcypromine (10.3) | 20.0 |
CYP2D6 | Bufuralol | Quinidine (0.035) | 148 |
CYP3A4 | Midazolam | Ketoconazole (0.018) | 81.9 |
CYP3A4 | Testosterone | Ketoconazole (0.015) | 12.5 |