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Inhibition of P-gp-mediated efflux in 12D7 T-cells and P-gp substrate binding competition in vitro
| Compound | IC50 (µM) 12D7-MDR (Calcein-AM) |
IC50 (µM) 12D7-MDR (NBD-Aba) |
IC50 [125I]IAAP competition |
|---|---|---|---|
| abacavir | > 500 | > 500 | >100 µM |
| AbaS2 | 4.8 ± 0.1 | 4.9 ± 0.4 | 170 ± 42 nM |
| AbaS2Me2 | 2.4 ± 0.1 | 2.1 ± 0.2 | 62 ± 24 nM |
| AbaS2Me4 | 0.6 ± 0.1 | 0.7 ± 0.1 | 65 ± 28 nM |
