Table 2.
Effect of p-gp inhibitors on the potency of compounds against SARS-CoV-2 replicon
| EC50, nM | |||
| Compound | Vero | A549 | Calu-1 |
| GC373 | 309 ± 43 | 539 ± 69 | 30.1 ± 5.8 |
| GC373 + 0.5 µM CP-100356 | 99.2 ± 9.7 | 581 ± 16 | 29.4 ± 4.7 |
| GC373 + 2 µM CP-100356 | 64.2 ± 9.9 | 403 ± 30 | 20.9 ± 3.9 |
| GC373 + 0.5 µM Elacridar | 54.2 ± 0.4 | 656 ± 98 | 33.7 ± 8.4 |
| GC373 + 2 µM Elacridar | 35.8 ± 4.1 | 510 ± 147 | 27.0 ± 5.7 |
| GC376 | 237 ± 74 | 570 ± 182 | 19.8 ± 2.0 |
| GC376 + 0.5 µM CP-100356 | 63.8 ± 2.9 | 551 ± 3 | 9.16 ± 2.70 |
| GC376 + 2 µM CP-100356 | 44.0 ± 2.9 | 481 ± 83 | 9.42 ± 1.05 |
| GC376 + 0.5 µM Elacridar | 93.3 ± 15.7 | 631 ± 94 | 10.3 ± 2.04 |
| GC376 + 2 µM Elacridar | 46.4 ± 10.7 | 651 ± 124 | 9.40 ± 1.94 |
| PF-00835231 | 2,190 ± 221 | 76.3 ± 16.2 | 24.7 ± 3.8 |
| PF-00835231+ 0.5 µM CP-100356 | 68.4 ± 5.7 | 61.0 ± 4.0 | 9.67 ± 1.10 |
| PF-00835231+ 2 µM CP-100356 | 17.3 ± 0.6 | 33.6 ± 2.3 | 9.59 ± 1.73 |
| PF-00835231+ 0.5 µM Elacridar | 25.0 ± 6.1 | 61.5 ± 17.2 | 12.4 ± 1.4 |
| PF-00835231+ 2 µM Elacridar | 16.3 ± 2.0 | 50.3 ± 9.3 | 9.68 ± 2.0 |
| Boceprevir | 16,600 ± 4,480 | 19,900 ± 517 | 4,790 ± 405 |
| Boceprevir + 0.5 µM CP-100356 | 7,800 ± 1,930 | 19,800 ± 1480 | 4,340 ± 1,246 |
| Boceprevir + 2 µM CP-100356 | 4,300 ± 1,170 | 17,900 ± 892 | 4,050 ± 857 |
| Boceprevir + 0.5 µM Elacridar | 4,000 ± 1,290 | 16,500 ± 699 | 4,540 ± 570 |
| Boceprevir + 2 µM Elacridar | 4,290 ± 1,230 | 16,800 ± 261 | 4,080 ± 553 |
| CP-100356 | >4,670 | >4,670 | >5,000 |
| Elacridar | >4,670 | >4,670 | >8,400 |