Table 1.
Pgp IC50 values for test compounds determined by Fl-t-pgp and by LLC-MDR1 cell monolayers, and the Kd for binding of various test compounds (all in µM).
| Test compound | IC50 Fl-t-pgpa | Kdb | IC50 LLC-MDR1c |
|---|---|---|---|
| Tariquidar | 0.021 | ||
| Elacridar | 0.10 | 0.59 | |
| Telmisartan | 0.12 | 17 | |
| Ritonavir | 0.25 | 0.79 | 18 |
| Valspodar | 0.25 | 0.08 | |
| Reserpine | 0.31 | 0.73 | |
| Cyclosporin A | 0.58 | 0.3 | 1.4 |
| Nelfinavir | 0.59 | 0.98 | |
| Zosuquidar | 0.59 | 0.055 | |
| Indinavir | 0.93 | 0.94 | |
| Nicardipine | 0.93 | 6.5 | 11 |
| Paclitaxel | 1.2 | 0.038 | |
| Ketoconazole | 2.0 | 2.5 | 3.4 |
| Ivermectin | 2.5 | 2.5 | |
| Quinidine HCl | 2.5 | 7.8 | 56 |
| Nifedipine | 2.6 | 48 | |
| Amiodarone | 2.6 | 2 | 21 |
| Progesterone | 3.7 | 0.9 | |
| Carvedilol | 3.8 | 32 | |
| Troglitazone | 5.2 | 12 | |
| Nitrendipine | 5.8 | 7.1 | |
| Simvastatin lactone | 6.0 | ||
| Isradipine | 6.6 | 13 | 29 |
| Mibefradil | 7.1 | 11 | |
| Ko143 | 7.5 | ||
| Verapamil HCl | 9.1 | 2.4 | 57 |
| Vinblastine | 9.5 | 2.9 | |
| NAc-LLY-amide | 13 | 28 | |
| Tamoxifen | 14 | 4.1 | |
| Trifluoperazine | 15 | 7.7 | |
| Felopidine | 17 | 4.3 | 17 |
| Simvastatin acid | 20 | ||
| Sulfinpyrazone | 23 | 24 | |
| Diltiazem | 24 | 83 | |
| Pepstatin A | 29 | 36 | |
| Sertraline | 29 | 37 | |
| Benzbromarone | 44 | ||
| Indomethacin | 51 | 36 | |
| Ranolazine | 64 | 130 | |
| Digoxin | 80 | 53 | |
| ALLN | 140 | 83 | |
| Naloxone | 210 | 54 | |
| Colchicine | 230 | 160 | |
| Probenecid | 240 | ||
| Captopril | 430 | >1000 | |
| Digoxigenin | 520 | 260 |
a
Determined using the Fl-t-pgp inhibition assay
b
Determined using fluorescence quenching of purified Pgp
c
Determined using inhibition of net transport of [3H]digoxin in LLC-MDR1 cell monolayers