Imidazoles with PXR transactivation agonist and antagonist data from HepG2 cells
The luciferase based reporter assay was performed using HepG2 cells as described previously (Zhu et al., 2004) using an 11-point dose-response curve from 2.5 to 50 μM. Maximum activation observed is percentage of rifampicin response at 10 μM. For further experimental details, see Materials and Methods.
Compound | Luciferase-DMSO (Agonist Mode) | Luciferase-Rifampicin (Antagonist Mode) | ||||
|---|---|---|---|---|---|---|
| EC50 | Maximum Activation Observed | EC50 | Maximum Activation Observed | |||
| μM | % | μM | % | |||
| CDD3508 | 4.4 | 73 | 23.9 | 108 | ||
| CDD3530 | 1.5 | 70 | 14.3 | 110 | ||
| CDD3532 | 1.3 | 81 | 14.4 | 110 | ||
| CDD3538 | 1.4 | 92 | 18.4 | 108 | ||
| CDD3540 | 1.9 | 56 | 15.8 | 110 | ||
| Clotrimazole | 1.1 | 96 | 16.7 | 107 | ||