Table 2.
Summary of the transporter inhibition properties of the drugs examined. Approximate IC50 (μM) values were determined by nonlinear regression analysis of the data shown in the results section, using GraphPad prism software (version 5.01, GraphPad, La Jolla, CA, USA).
| Estimated Transporter Inhibition—IC50 (µM) | ||||||||
|---|---|---|---|---|---|---|---|---|
| ABCB1 | ABCC1 | ABCG2 | OATP Cellular Assays |
|||||
| Potential anti-COVID-19 compounds | cellular assay | vesicular assay | cellular assay | vesicular assay | cellular assay | vesicular assay | OATP1A2 | OATP2B1 |
| chloroquine | - | - | - | - | - | - | 17.0 | 119 |
| hydroxychloroquine | - | - | - | - | - | - | 18.9 | 84 |
| ivermectin | 0.6 | 0.3 | 3.3 | 13.3 | 3.1 | 1.1 | 5.2 | 8.6 |
| lopinavir | 6.3 | 0.6 | 10.7 | 10 | 13.1 | 4.2 | 1.5 | 1.0 |
| ritonavir | 8.4 | 0.3 | 7.7 | - | 8.3 | 7.5 | 2.3 | 1.4 |
| remdesivir | - | >20 | - | -* | >50 | >50 | 3.8 | 3.8 |
| remdesivir-SBECD | - | >20 | - | NA | >50 | >50 | 6.1 | 5.6 |
| favipiravir | - | - | - | - | - | - | - | - |
* Stimulation of substrate transport.