Table I.
K m Values of Probe Substrates and Inhibition IC50 Values of Positive Inhibitors to CYP Isoforms
| CYP | Substrate/metabolite/inhibitor | K m tested (μM) | K m reported (μM) (24) | IC50 tested (μM) | IC50 reported (μM) |
|---|---|---|---|---|---|
| 1A2 | PHE/dEtPHE/NAP | 13.6 (1.7) | 1.7–152 | 0.054 (0.009) | 0.041 (25), 0.07 (26) |
| 2C19 | OME/OHOME/TIC | 11.4 (0.5) | 17–26 | 2.80 (0.49) | 1.2–10 (24,25) |
| 2C9 | TOL/OHTOL/FLU | 80.0 (11.3) | 67–838 | 6.85 (1.42) | 7–8 (27) |
| 2D6 | DEX/dMeDEX/QUI | 8.0 (3.3) | 0.44–8.5 | 0.16 (0.02) | 0.05 (25), 0.0579 (21), 0.06 (26), 0.12 (28) |
| 3A4 | MID/OHMID/KET | 1.2 (0.3) | 1–14 | 0.075 (0.018) | 0.0187 (22), 0.045 (28), 0.10 (26), 0.0037–0.18 (24) |
| 3A4 | TES/OHTES/KET | 55.1 (2.6) | 52–94 | 0.024 (0.004) | 0.0261 (21), 0.04 (25), 0.05 (28), 0.0037–0.18 (24) |
Data in the brackets suggested standard error of the results (n = 4). For abbreviations of substrates, metabolites, and inhibitors please refer to the “Chemicals and reagents” section