Table 4.
Activity profile of compounds 9 and clinical lead BMS-626529 against a panel of functional HIV-1 subtype B clinical envelope clones from 9 subjects in cell-cell (transfected HeLa cells) fusion susceptibility assays. Values provided as averages from three replicates.
| Clone ID | EC50 (nM) | Fold Change (vs LAI) | FC Ratio | ||
|---|---|---|---|---|---|
| 9 | 13 | 9 | 13 | 9/13 | |
| 27N4-20 | 7.4 | 0.2 | 0.22 | 0.20 | 1.1 |
| 36N3-5 | 5.5 | 0.4 | 0.16 | 0.40 | 0.40 |
| P15-2-18 | 62 | 1.2 | 1.8 | 1.2 | 1.5 |
| P23-1-13 | 110 | 2.4 | 3.2 | 2.4 | 1.3 |
| P22-2-45 | 73 | 2.5 | 2.1 | 2.5 | 0.84 |
| 66N2-8 | 160 | 8.6 | 4.7 | 8.6 | 0.55 |
| 66N2-16 | 350 | 22 | 10 | 22 | 0.45 |
| 12N1-13 | 550 | 56 | 16 | 56 | 0.29 |
| 21N4-169 | 4300 | 120 | 130 | 120 | 1.1 |
| 21N4-170 | 11000 | 860 | 320 | 860 | 0.38 |
| 16N4-17 | >40000 | 6200 | >1200 | 6200 | |
| 16N4-25 | >40000 | 6400 | >1200 | 6400 | |
| LAI | 34 | 1.0 | 1 | 1 | |