Table 2.
Bioactivities (IC50 in µM; pIC50) measured in same assay type (‘Inibition of transepithelial transport’): different substrates, same cell line.
| Cell line=NIH-3T3-G185 | IC50 (µM), DNR | pIC50 | IC50 (µM), Rho | pIC50 | IC50 (µM), LDS | pIC50 |
|---|---|---|---|---|---|---|
| Carvedilol | 4.6 | 5.3 | 6.6 | 5.2 | 6 | 5.2 |
| Clarithromycin | 3.8 | 5.4 | 15.1 | 4.8 | 7.2 | 5.1 |
| Clofazimine | 0.6 | 6.2 | 1 | 6.0 | 1.1 | 6.0 |
| Cyclosporin A | 1.4 | 5.9 | 1.7 | 5.8 | 1.8 | 5.7 |
| Dipyridamole | 22.7 | 4.6 | 34.3 | 4.5 | 23.7 | 4.6 |
| Emetine | 9.2 | 5.0 | 9.6 | 5.0 | 2.4 | 5.6 |
| Felodipine | 26.3 | 4.6 | >60 | 4.2 | 32.3 | 4.5 |
| Fluphenazine | 6.5 | 5.2 | 10.4 | 5.0 | 5.7 | 5.2 |
| Ketoconazole | 5.6 | 5.3 | 53.4 | 4.3 | 23.4 | 4.6 |
| Lovastatin | 26.3 | 4.6 | 114.4 | 3.9 | 32.7 | 4.5 |
| Nicardipine | 3.2 | 5.5 | >25.8 | 4.6 | 5.6 | 5.3 |
| N-Norgallopamil | 3.6 | 5.4 | 8.6 | 5.1 | 4.9 | 5.3 |
| Progesterone | 96.2 | 4.0 | 192.2 | 3.7 | 88.1 | 4.1 |
| Quinidine | 18.8 | 4.7 | 33.9 | 4.5 | 1 | 6.0 |
| Quinine | 22.6 | 4.6 | 87.6 | 4.1 | 74.4 | 4.1 |
| Reserpine | 0.5 | 6.3 | 3.9 | 5.4 | 2.1 | 5.7 |
| Simvastatin | 8.9 | 5.1 | 56.8 | 4.2 | 26.1 | 4.6 |
| Tamoxifen | 6.4 | 5.2 | 31.4 | 4.5 | 12.1 | 4.9 |
| Taxol | 54 | 4.3 | 70.2 | 4.2 | 53.9 | 4.3 |
| Terfenadine | 1.8 | 5.7 | 2.7 | 5.6 | 2.5 | 5.6 |
| Trifluo-erazine | 7.2 | 5.1 | 10.9 | 5.0 | 6.3 | 5.2 |
| Troleando-mycin | 68.3 | 4.2 | 86.3 | 4.1 | 78.2 | 4.1 |
| Verapamil | 4.2 | 5.4 | 6.5 | 5.2 | 4.7 | 5.3 |
| Vinblastine | 17.7 | 4.8 | 29.5 | 4.5 | 19.9 | 4.7 |