Human P450 Isoform | Substrate | ||||||||
---|---|---|---|---|---|---|---|---|---|
AMMC | MeAMFC | CMC | CEC | MFC | BFC | DBF | BQ | BzRes | |
CYP1A1 | —3-b | 0.15 | 3.25 | 40.2 | 3.01 | 0.58 | 2.32 | 3.2 | 0.457 |
CYP1A2 | — | 0.17 | 6.43 | 8.60 | 1.58 | — | 0.08 | 2.6 | 0.009 |
CYP1B1 | — | 0.10 | 0.29 | 0.65 | 0.68 | 0.20 | 0.01 | — | 1.55 |
CYP2A6 | — | — | — | — | 0.49 | — | — | — | — |
CYP2B6 | — | — | 0.52 | 0.59 | 10.1 | — | — | — | 0.020 |
CYP2C8 | — | — | — | — | 0.09 | — | 0.26 | — | — |
CYP2C9 | — | — | 0.05 | — | 0.76 | — | 0.12 | — | — |
CYP2C18 | — | — | 0.11 | — | 1.13 | — | — | — | — |
CYP2C19 | — | — | 0.50 | 0.89 | 2.70 | 0.21 | 0.29 | — | — |
CYP2D6 | 1.2 | 0.61 | 0.10 | — | 1.49 | — | 0.02 | — | 0.009 |
CYP2E1 | — | — | 0.55 | 0.10 | 2.23 | — | — | — | — |
CYP3A4 | — | — | — | — | — | 1.54 | 1.28 | 22 | 0.079 |
CYP3A5 | — | — | — | — | — | — | 0.41 | 5.1 | 0.011 |
CYP3A7 | — | — | — | — | 0.19 | 0.08 | 0.16 | 1.5 | 0.046 |
CYP4A11 | — | — | — | — | — | — | — | — | — |
Substrate concentration (μM) | 1.5 | 25 | 25 | 25 | 50 | 50 | 1 | 40 | 50 |
Incubation time (min) | 30 | 45 | 20 | 20 | 30 | 20 | 30 | 30 | 30 |
Enzyme concentration (nM) | 503-c | 50 | 12.53-d | 12.53-e | 50 | 503-f | 10 | 50 | 503-g |
↵3-a Values, expressed as picomoles product per minute per picomoles enzyme, represent the mean of duplicate determinations. Bold values indicate the highest catalytic activity within the panel.
↵3-b Dashes indicate activity was below the limit of detection which was considered as that corresponding to a signal to background ratio of approximately 1.5. These values and their substrates were 0.03 min−1, AMMC; 0.07 min−1, BFC; 0.03 min−1, CMC; 0.07 min−1, CEC; 0.007 min−1, DBF; 0.08 min−1, MFC; 1.5 min−1, BQ; 0.09 min−1, MeAMFC; and 0.008 min−1, BzRes.
↵3-c Except for CYP2D6, which was 7.5 nM.
↵3-d Except for CYP1A1 which was 2.5 nM and CYP1A2 which was 0.5 nM.
↵3-e Except for CYP1A1 and CYP2C19 which were 2.5 nM and CYP1A2 which was 0.5 nM.
↵3-f Except for CYP3A4, CYP3A5, CYP3A7 which were 12.5 nM.
↵3-g Except for CYP1A1 and CYP1B1 which were 5 nM.