Table 1.
Biochemical and antiviral assay results of subtype 4
| Compd | Structure | RT IC50 a(μM) | INST IC50 a (μM) | MAGI Antiviral | ||
|---|---|---|---|---|---|---|
|
|
|
|||||
| RNase H | Pol | EC50b (μM) | CC50c (μM) | |||
| 4ad |
|
5.2 ± 0.8 | 0.45± 0.07 | >100 | 0.026 ± 0.002 | >100 |
| 4b |
|
2.7 ± 2 | 9.9 ± 0.04 | >100 | 2.4 ± 0.2 | >100 |
| 4c |
|
5.5 ± 0.2 | 2.3 ± 2 | >100 | 0.059 ± 0.004 | >100 |
| 4d |
|
5.8 ± 0.2 | 1.5 ± 0.5 | >100 | 0.039 ± 0.008 | >100 |
| 4e |
|
1.1 ± 0.3 | 6.5 ± 0.2 | >100 | 0.42 ± 0.1 | >100 |
| 4f |
|
1.7 ± 0.5 | >10 | >100 | 4.1 ± 0.5 | >100 |
| 4g |
|
10 | 7.0 ± 2 | >100 | 2.4 ± 0.3 | >100 |
| 4h |
|
2.1 ± 1 | 6.5 ± 1 | >100 | 0.43 ± 0.06 | >100 |
| 4i |
|
3.1 ± 1 | >10 | >100 | >15 | >100 |
| 4j |
|
2.2 ± 0.9 | >10 | >100 | >15 | >100 |
| 4k |
|
4.6 ± 0.4 | 10 | >100 | >15 | >100 |
| 4l |
|
7.6 ± 0.6 | 10 | >100 | >15 | >100 |
| 4m |
|
3.9 ± 0.2 | >10 | >100 | 10 ± 1.1 | >100 |
| 14 | -- | >10 | 0.42 ± 0.2 | -- | 0.011 ± 0.0001 | 58 ± 2 |
a
Concentration of compound inhibiting the target enzyme by 50%.
b
Concentration of compound inhibiting virus replication by 50%.
c
Concentration of compound resulting in 50% cell death. All assay results expressed as mean ± standard deviation from at least two independent experiments.
d
No pol inhibition was observed against RT mutants Y181C or K103N at concentrations up to 10 μM.