Table 4.
Sensitivity of mutated-pseudoviruses to the NBD compounds
| Substitutions | 48 IC50 (μM) |
39 IC50 (μM) |
55 IC50 (μM) |
BMS-626529 IC50 (nM) |
Location |
|---|---|---|---|---|---|
| HIV-1HXB2 WT | 0.36±0.01 | 0.15±0.01 | 0.13±0.003 | ~8 | - |
| L116P | 0.54±0.05 | 0.15±0.005 | 0.14±0.001 | >1000 | CD4 binding site |
| A204D | 0.52±0.05 | 0.87±0.2 | 0.65±0.05 | >1000 | V2 |
| S375H | 0.40±0.01 | 0.31±0.01 | 0.14±0.002 | >1000 | CD4 binding site |
| S375W | 0.63±0.03 | 0.17±0.03 | 0.13±0.001 | >1000 | CD4 binding site |
| S375Y | 0.44±0.01 | 0.3±0.01 | 0.19±0.02 | >1000 | CD4 binding site |
| I424F | 0.55±0.01 | 1.3±0.5 | 0.88±0.1 | >1000 | CD4 binding site |
| N425K | 1.5±0.1 | 0.37±0.03 | 0.18±0.03 | ~8 | CD4 binding site |
| M426L | 0.49±0.01 | 0.14±0.001 | 0.12±0.001 | 230±10 | CD4 binding site |
| M434I | 0.97±0.1 | 0.25±0.04 | 0.23±0.01 | ~8 | CD4 binding site |
| F468L | 0.24±0.05 | 0.14±0.01 | 0.12±0.006 | ~8 | V5 |
| M434I/I595F | 0.3±0.02 | 0.16±0.01 | 0.12±0.001 | ~8 | CD4 binding site/gp41 |
| M475I | 0.59±0.01 | 0.13±0.01 | 0.11±0.01 | ~50 | CD4 binding site |
The reported IC50 values represent the means ± standard deviation (n = 3).