Table 4.
Biochemical inhibitory activity of selected compounds against HIV IN.
| Compd | RNase H IC50a (µM) |
INST IC50b (µM) |
SIc |
|---|---|---|---|
| 9b | 0.85 | 2.2 ± 0.66 | 2.6 |
| 9g | 0.75 | 4.4 ± 0.5 | 1.1 |
| 9k | 0.60 | 4.6 ± 2.1 | 7.7 |
| 9t | 1.2 | 30 ± 6.2 | 25 |
| 9v | 1.1 | 7.1 ± 2.6 | 6.5 |
| 9w | 1.6 | 25 ± 8.8 | 16 |
| 10g | 2.2 | 12 ± 3.2 | 5.5 |
| 10h | 0.90 | 7.1 ± 2.1 | 7.9 |
| 10p | 2.3 | 1.0 ± 0.28 | 0.43 |
| 11b | 0.40 | 93 ± 34 | 233 |
| 11c | 0.38 | 44 | 116 |
| 11i | 0.15 | >100 | >667 |
| 11j | 0.20 | >100 | >500 |
| 11k | 0.19 | 35 | 184 |
| 11l | 0.31 | 1.2 | 3.9 |
| 11m | 0.51 | 1.3 | 2.6 |
| 11o | 0.20 | >100 | >500 |
| L-731988d | -- | 0.40 ± 0.05 | -- |
a
Data with HTS-1 as substrate.
b
Expressed as mean ± standard deviation from at least three independent experiments.
c
Selectivity index defined as IC50 IN / IC50 RNase H.
d
Stereotypical DKA compound, reported as a selective INSTI.24