Inactivation kinetic parameters for CYP3cide on CYP3A activities in HLM and rCYP3A enzymes
| Enzyme Source | Marker Substrate Activity | KI | kinact | kinact/KI |
|---|---|---|---|---|
| μM | min−1 | ml · min−1 · /μmol−1 | ||
| rCYP3A4 | Midazolam 1′-hydroxylase | 0.12 | 0.99 | 8250 |
| Testosterone 6β-hydroxylase | 0.17 | 1.2 | 7060 | |
| rCYP3A5 | Midazolam 1′-hydroxylase | 2.0 | 0.051 | 26 |
| Testosterone 6β-hydroxylase | 1.2 | 0.046 | 38 | |
| HLM CYP3A5 *3/*3 (HH189) | Midazolam 1′-hydroxylase | 0.42 | 1.6 | 3800 |
| Testosterone 6β-hydroxylase | 0.27 | 0.80 | 2960 | |
| HLM CYP3A5 *3/*3 (HH101) | Midazolam 1′-hydroxylase | 0.48 | 1.6 | 3300 |
| Testosterone 6β-hydroxylase | 0.26 | 0.80 | 3100 |