Effect of nonspecific binding on the determination of in vitro Ki values of fluvoxamine toward CYP2C19
| System | Protein Conc. | Ki,total | Free Fraction2-a | Ki,ub |
|---|---|---|---|---|
| mg/ml | nM | f u,mic | nM | |
| HLM | 1 | 400 ± 37 | 0.20 ± 0.05 | 80 |
| HLM | 0.5 | 226 ± 19 | 0.31 ± 0.03 | 70 |
| Supersomes | 0.15 | 96 ± 14 | 0.81 ± 0.03 | 78 |
Supersomes, cDNA-expressed CYP2C19.
↵2-a Fluvoxamine spiked concentration was 0.3 μM.