Table 2.
Inhibitory potencies using an in vitro IN assay.a
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---|---|---|---|
No. | X | IC50 Values (μM)
|
|
3′-Processing | Strand transfer | ||
5a-1 | NHMe | 17.5 ± 3.0 | 0.12 ± 0.04 |
5a-2 | NEt2 | 9.5 ± 1.2 | 0.054 ± 0.009 |
5a-3 |
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14.7 ± 1.7 | 0.11 ± 0.01 |
5a-4 |
![]() |
15.9 ± 1.3 | 0.24 ± 0.02 |
5a-5 |
![]() |
30.2 ± 2.3 | 0.32 ± 0.05 |
5a-6 |
![]() |
19.3 ± 0.6 | 0.31 ± 0.03 |
5a-7 |
![]() |
23 ± 3 | 0.37 ± 0.04 |
5a-8 |
![]() |
23 ± 4 | 0.4 ± 0.08 |
5a-9 |
![]() |
21.2 ± 1.9 | 0.19 ± 0.08 |
5a-10 |
![]() |
6.8 ± 1.1 | 0.047 ± 0.007 |
5a-11 |
![]() |
11.7 ± 0.7 | 0.08 ± 0.01 |
5a-12 |
![]() |
6.9 ± 0.6 | 0.058 ± 0.01 |
Assays were performed using a gel-based protocol with Mg2+ cofactor as described in reference 12.