IC50 values of CCR5 antagonists in inhibiting ligand binding and HIV-cell fusion
Data are presented as mean ± S.E.; data were derived from three independent experiments. Kd values are for various ligands binding to the WT CCR5.
Ligand Binding Assay | CCF Assay | Antiviral Assay | |||||
|---|---|---|---|---|---|---|---|
| 125I-RANTES | 125I-MIP-1α | 125I-MIP-1β | |||||
| nM | |||||||
| Ligand Kd (nM) | 0.59 ± 0.1 | 1.4 ± 0.5 | 0.4 ± 0.5 | ||||
| Vicriviroc | 14 ± 1 | 11 ± 8 | 12 ± 3 | 1.2 ± 0.4 | 7.2 ± 2 | ||
| Maraviroc | 9 ± 9 | 4 ± 1 | 3 ± 1 | 1.2 ± 0.5 | 1.4 ± 1 | ||
| TAK779 | 4 ± 5 | 7.5 ± 5 | 4.5 ± 1 | 18 ± 2 | 13 ± 6 | ||
| TAK 220 | 17 ± 5 | 7 ± 1 | 4,100 ± 320 | 6.1 ± 4 | 3 ± 4 | ||
| Aplaviroc | 12 ± 2 | 8.5 ± 3 | 7.3 ± 0.2 | 1 ± 0.6 | 1 ± 1 | ||
CCF, cell-cell fusion.