IC50 values obtained for a series of compounds in different CYP3A4 assays
Compound | Fluorescent Probe in Intact Cells | Conventional Probe in Liver Microsomes | ||||
|---|---|---|---|---|---|---|
| IC50a | Type of Inhibitorb | IC50 | Type of Inhibitor | |||
| Ketoconazole | <0.3 | potent | <0.3 | potent | ||
| Cyclosporine | 1.5 | potent | 20.0 | moderate | ||
| Nifedipine | 6.7 | moderate | 2.8 | potent | ||
| Quercetin | 34.2 | poor | 20.1 | moderate | ||
| Verapamil | 42.3 | poor | 35.6 | poor | ||
| Omeprazole | 83.5 | poor | 104 | poor | ||
| Amiodarone | 136 | poor | 237 | poor | ||
| Sulfaphenazole | 152 | poor | 238 | poor | ||
| Ticlopidine | 162 | poor | 148 | poor | ||
| Erythromycin | 170 | poor | 196 | poor | ||
| Tranylcypromine | 235 | poor | 208 | poor | ||
| Quinine | 254 | poor | 172 | poor | ||
| Cimetidine | 274 | poor | 300 | poor | ||
| Lovastatin | >300 | noninhibitor | 88.0 | poor | ||
| Quinidine | >300 | noninhibitor | 283 | poor | ||
| Diethyldithiocarbamate | >300 | noninhibitor | >300 | noninhibitor | ||
| Furafylline | >300 | noninhibitor | >300 | noninhibitor | ||