Table 4.
Comparison of biochemical inhibition against RT RNase H, RT pol and INST
| Compd | RT RNase H IC50a(µM) | RT Pol IC50 (µM) | IN IC50 (µM) |
|---|---|---|---|
| 10a | >25 | >25 | >100 |
| 10b | >25 | >25 | 37 |
| 10c | >25 | >25 | 35 |
| 10d | 17 | >25 | 35 |
| 10e | 16 ± 4.5 | >25 | 34 |
| 10f | 17 ± 5.2 | >25 | >100 |
| 10g | 13 ± 2.1 | >25 | >100 |
| 10h | 17 | >25 | 67 |
| 10i | 14 | >25 | 36 |
| 10j | 12 | >25 | 25 |
| 10k | 18 ± 2.8 | >25 | 44.5 ± 18.1 |
| 10l | >25 | >25 | >100 |
| 10m | 18 ± 4.5 | >25 | >100 |
| 10n | >25 | >25 | >100 |
| 10o | >25 | >25 | >100 |
| 10p | >25 | >25 | >100 |
| 10q | 2.5 ± 0.2 | >25 | >100 |
| 10r | 2.7 ± 0.6 | 8.5 ± 1.5 | 23 |
| 10s | 7.0 ± 0.7 | 19 ± 5.5 | 2.26 ± 0.87 |
| 10t | 1.5 ± 0.2 | 1.8 ± 0.1 | 14 |
| 10u | 7.7 ± 2.4 | >25 | 17 |
| 10v | 2.5 ± 0.4 | 2.2 ± 0.1 | 22 |
| 10w | 3.2 ± 0.3 | 3.2 ± 0.8 | 7.79 ± 1.93 |
| 10x | 0.90 ± 0.05 | 1.1 ± 0.1 | 16.0 ± 6.5 |
| 10y | 0.65 ± 0.05 | 1.2± 0.1 | >100 |
| 10z | 3.6 ± 0.2 | >25 | 35.0 ± 10.0 |
| 18 | >25 | >25 | >100 |
| 20 | 12 ± 1.8 | >25 | 32 |
| 22 | 7.5 ± 0.4 | 2.4 ± 0.1 | >100 |
a
Data with HTS-1 as substrate