Reported Km and Vmax values for various human P450 substrates
Enzyme | Substrate | Product | Km | Vmax |
|---|---|---|---|---|
| 1A1 | 7-Ethoxyresorufin | Resorufin | 1.4 (0.6)a,b | 2.4 (0.4) |
| 1A2 | Bufuralol | 1′-OH-Bufuralol | 176 | 4.56 |
| 2B6 | DZ | NDZ | 181 | 8.5 |
| Testosterone | 6β-OH-Testosterone | 50.5 | 87 | |
| 2C9 | Diclofenac | 4′-OH-Diclofenac | 15.5 | 1.3 |
| 2C19 | (S)-Mephenytoin | 4′-OH-Mephenytoin | 31-339 | 87-536 |
| Bufuralol | 1′-OH-Bufuralol | 36 | 36.9 | |
| 2D6 | Bufuralol | 1′-OH-Bufuralol | 10 | 2.5 |
| Metoprolol | α-OH-Metaprolol | 21.4 | 2.17 | |
| Dextromethorphan | Dextrorphan | 5.4, 6.5, 0.5, 1.6 | 0.47, 1.3, 0.5, 0.03 | |
| 3A4 | DZ | TMZ | 140 | 30 |
| Testosterone | 6β-OH-Testosterone | 56, 93 | 3.5, 16.5 | |
| Dextromethorphan | 3-Methoxymorphinan | 660, 1155 | 6.7, 11.9 | |
| 3A5 | Testosterone | 6β-OH-Testosterone | 243 | 21 |
| HLMs | DZ | NDZ | 184 | 1.4 |
| TMZ | 188, 230 | 6.8, 16.2 | ||
| Testosterone | 6β-OH-Testosterone | 67 | 5.3 | |
| (S)-Mephenytoin | 4′-OH-Mephenytoin | 11 | 0.07 | |
| Diclofenac | 4′-OH-Diclofenac | 3.7, 5.4 | 1.8, 1.2 | |
| Dextromethorphan | Dextrorphan | 11, 4.4 | 0.25, 5.2 | |
| 3-Methoxymorphinan | 850, 188-335 | 1.8, 1.7-2 | ||
| 7-Ethoxyresorufin | Resorufin (low Km) | 1.4 (0.2)b | 1.3 (0.2) | |
| Resorufin (high Km) | 97.9 (23.8)b | 10.3 (1.3) | ||
|
|
Bufuralol
|
1′-OH-Bufuralol
|
2.8, 36, 9.4
|
0.1, 0.2, 0.2
|
↵ a Km (μM) and Vmax (nmol/min/nmol) were obtained from the Metabolism and Transport Drug Interaction Database (www.druginteractioninfo.org) established by Dr. René Levy, University of Washington, Seattle, WA
↵ b Data were obtained from our laboratory, and the values in parentheses are the standard deviation