Inhibition constants predicted from the best fit of models A to C
| Inhibitor | Predicted by Modela | Inhibition Constant | ||
|---|---|---|---|---|
| Ki | KI | kinact | ||
| μM | min−1 | |||
| Ketoconazole | C | 0.59 ± 0.09 | ||
| Fluconazole | C | 4.01 ± 0.62 | ||
| Aprepitant | C | 11.34 ± 0.72 | ||
| Voriconazole | C | 1.62 ± 0.13 | ||
| Nefazodone | B | 22.43 ± 7.37 | 0.05 ± 0.005 | |
| Troleandomycin | B | 5.93 ± 1.32 | 0.07 ± 0.003 | |
| Erythromycin | B | 25.15 ± 4.90 | 0.08 ± 0.005 | |
| Clarithromycin | B | 37.43 ± 9.24 | 0.09 ± 0.008 | |
| Diltiazem | B | 2.71 ± 0.73 | 0.04 ± 0.004 | |
| Saquinavir | B | 4.67 ± 2.35 | 0.03 ± 0.005 | |
| Itraconazole | B | 5.14 ± 1.37 | 0.05 ± 0.001 | |
| Conivaptan | B | 3.26 ± 1.10 | 0.03 ± 0.004 | |
| Ritonavir | A | 8.59 ± 3.75 | 0.82 ± 0.14 | 0.09 ± 0.01 |
| Ritonavir | C | 0.06 ± 0.01 | ||
↵ Three inhibition models incorporating irreversible inhibition (model B), reversible inhibition (model C), or both (model A) were used to estimate the inactivation parameters (KI and kinact) and/or reversible inhibition constant (Ki) for each inhibitor. Refer to Materials and Methods for details of the models.