TABLE 3
TDI of common CYP2B6 in HLM by PBD analogs
The concentrations of PBD and its analogs were 0, 0.032, 0.16, 0.8, 4, 20, and 100 µM in HLM mixtures preincubated w/wo NADPH for 30 min, and then dilution was performed before individual CYP-specific substrates were added to determine relative enzyme activity as previously described under Materials and Methods.
| Recombinant CYP2B6 | ||||
|---|---|---|---|---|
| Name | Structure | Direct Inhibition IC50 (µM) | - NADPH IC50 (µM) | + NADPH IC50 (µM) |
| PBD |  | >10 | 1.5 | 0.2 |
| PBD-1 |  | >10 | >10 | >10 |
| PBD-2 |  | >10 | >10 | >10 |
| PBD-3 |  | >10 | >10 | >10 |
| PBD-4 |  | >10 | >10 | >10 |