TABLE 3.
In vitro enzyme inhibition and nucleic acid binding by BMS-791325
| Enzyme or assay typea | BMS-791325 IC50 (μM)b |
|---|---|
| HCV NS5B 1b (Con1) | 0.003 |
| Bovine polymerase α | >25 |
| Human polymerase β | >25 |
| Human polymerase γ | >25 |
| BVDV polymerase | >25 |
| HIV reverse transcriptase | >25 |
| Klenow polymerase | >25 |
| HIV integrase | >40 |
| DNA binding | >25 |
| RNA binding | >20 |
a
Positive controls were run in each experiment: mammalian DNA polymerases (IC50 of ddTTP, 5 to 20 mM), BVDV polymerase (IC50 of BMS-514, 6.3 ± 2.6 mM), HIV RT (IC50 of Sustiva, 0.017 ± 0.017 mM), Klenow polymerase and nucleoside triphosphate binding (IC50 of actinomycin D, 1.9 ± 0.4 mM), and HIV integrase (IC50 of BMS-035, 0.004 ± 0.001 mM). Compounds BMS-514 and BMS-035 are Bristol-Myers Squibb proprietary compounds that inhibit BVDV polymerase and HIV integrase, respectively.
b
From two or more independent experiments.