Compound | P450 Isoform | Enzyme Source | KI | kinact | Reference |
---|---|---|---|---|---|
μM | min-1 | ||||
Tienilic acid | CYP2C9 | rCYP2C9 | 2 | 0.19 | This laboratory |
rCYP2C9 (2C10) | 4 | 0.20 | Lopez-Garcia et al., 1994 | ||
Human hepatocytes | 2 | 0.05 | This laboratory | ||
Erythromycin | CYP3A4 | rCYP3A4 | 9 | 0.12 | This laboratory Atkinson et al., 2005 |
rCYP3A4 | 5 | 0.12 | Chan and Delucchi, 2000 | ||
HLMs | 16a | 0.07 | Kanamitsu et al., 2000 | ||
HLMs | 82a | 0.07 | Yamano et al., 2001 | ||
HLMs | 13a | 0.02 | Ito et al., 2003 | ||
HLMs | 10a | 0.08 | Dai et al., 2003 | ||
HLMs | 11a | 0.05 | McConn et al., 2004 | ||
HLMs | 15a | 0.07 | Zhao et al., 2005 | ||
Human hepatocytes | 11 | 0.07 | This laboratory | ||
Troleandomycin | CYP3A4 | rCYP3A4 | 0.3 | 0.12 | This laboratory Atkinson et al., 2005 |
rCYP3A4 | 0.2 | 0.15 | Chan and Delucchi, 2000 | ||
HLMs | 2a | 0.03 | Zhao et al., 2005 | ||
Human hepatocytes | 0.4 | 0.05 | This laboratory | ||
Fluoxetine | CYP3A4 | rCYP3A4 | 2 | 0.03 | This laboratory |
HLMs | 5a (0.5) | 0.01 | This laboratory | ||
HLMs | 5a | 0.02 | Mayhew et al., 2000 | ||
Human hepatocytes | 1 | 0.01 | This laboratory | ||
CYP2C19 | rCYP2C19 | 0.4 | 0.5 | This laboratory | |
HLMs | 8a (0.8) | 0.03 | This laboratory | ||
Human hepatocytes | 0.2 | 0.04 | This laboratory | ||
AZ1 | CYP2C9 | rCYP2C9 | 30 | 0.02 | This laboratory |
|
| Human hepatocytes | 19 | 0.02 | This laboratory |
↵ a Apparent KI values. All other values including those in parentheses are unbound KI estimates.