TABLE 4.
Antiretroviral activities of the BDM-2 series in single-round compared to multiple-round infectivity assays with NL4-3 HIV-1 isolate in MT4 cellsa
| Compound | EC50 in single-round infection (μM) | EC50 ratio (single/multiple-round infection)b |
|---|---|---|
| RAL | 0.0035 ± 0.0010 | 0.25 |
| DTG | 0.00044 ± 0.00013 | 0.16 |
| BI-224436 | 1.4 ± 0.3 | 27 |
| S-I-82 | 9.2 ± 1.1 | 767 |
| BDM-2 | 1.4 ± 0.3 | 161 |
| MUT871 | 0.63 ± 0.01 | 203 |
| MUT872 | 8.8 ± 0.3 | 196 |
| MUT884 | 3.9 ± 0.8 | 260 |
| MUT916 | 2.1 ± 0.2 | 105 |
a
EC50 values were determined in the single-round infectivity assay using a single-cycle NL4-3 HIV-1 clone. Two INSTIs (RAL, DTG) and two INLAIs (BI-224436, S-I-82) were used as references. Data are mean ± SD of n > 5 independent experiments.
b
Ratios of EC50 obtained in the single- and multiple-round infection assays. The corresponding EC50 from multiple-round infection assays are given in Table 2.