Table 3.
Bioactivities (IC50 in µM; pIC50) measured in same assay type (‘Increase in X intracellular accumulation’): same substrate, different cell lines.
| Calcein accumulation/cell line: | IC50 (µM), L-MDR1 | pIC50 | IC50 (µM), PBCEC | pIC50 |
|---|---|---|---|---|
| Astemizole | 1.30 | 5.9 | 0.30 | 6.5 |
| Cimetidine | >50 | 4.3 | >50 | 4.3 |
| Clotrimazole | 6.70 | 5.2 | 1.30 | 5.9 |
| Colchicine | >50 | 4.3 | >50 | 4.3 |
| Cyclosporin A | 0.80 | 6.1 | 0.50 | 6.3 |
| Dexamethasone | >50 | 4.3 | >50 | 4.3 |
| Digoxin | >50 | 4.3 | >50 | 4.3 |
| Enkephalin (dpdpe) | >50 | 4.3 | >50 | 4.3 |
| Erythromycin | >50 | 4.3 | 43.00 | 4.4 |
| Etoposide | >50 | 4.3 | >50 | 4.3 |
| Hydrocortisone | >50 | 4.3 | >50 | 4.3 |
| Ivermectin | 0.10 | 7.0 | 0.20 | 6.7 |
| Ketoconazole | 4.8 | 5.3 | 1.00 | 6.0 |
| Mibefradil | 1.80 | 5.7 | 1.50 | 5.8 |
| Miconazole | 3.50 | 5.5 | 2.00 | 5.7 |
| Midazolam | >50 | 4.3 | >50 | 4.3 |
| Morphin | >50 | 4.3 | >50 | 4.3 |
| Nelfinavir | 3.40 | 5.5 | 0.35 | 6.5 |
| Nicardipine | 2.3 | 5.6 | 0.95 | 6.0 |
| Pimozide | 2.90 | 5.5 | 0.80 | 6.1 |
| Quinidine | 5.6 | 5.3 | 2.20 | 5.7 |
| Ranitidine | >50 | 4.3 | >50 | 4.3 |
| Ritonavir | 12.00 | 4.9 | 1.50 | 5.8 |
| Saquinavir | 12.00 | 4.9 | 1.60 | 5.8 |
| Terfenadine | 1.4 | 5.9 | 1.10 | 6.0 |
| Verapamil | 6.3 | 5.2 | 0.40 | 6.4 |
| Vinblastine | >50 | 4.3 | 2.00 | 5.7 |