Table 3:
Expanded activity profile of selected RNaseH inhibitors
| Compound | EC50 | CC50 | q-PCR TI HepDES19 | q-PCR TI HepDE19 | bDNA TI HepDE19 | |||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| q-PCR HepDES19 (μM) | q-PCR HepDE19 (μM) | bDNA_rcDNA HepDE19 (μM) | MTS HepDES19 (μM) | MTS HepDE19 (μM) | CTG HepDE19 (μM) | |||||||
| (+) strand | (−) strand | (+) strand | (−) strand | (+) strand | (−) strand | |||||||
| HID | ||||||||||||
| A19 | 3.8 ± 1.7 | ND (a) | ND | 7.6 ± 4.7 | >25 | 100 ± 0.2 | ND | >25 | 26 | NA | >3.2 | |
| HPD | ||||||||||||
| A13 | 0.54 ± 0.3 | 56 ± 8 | ND | ND | 10.7 ± 2.2 | >25 | 85 ± 15 | ND | >25 | 157 | NA | >2.3 |
| A15 | 0.46 ± 0.1 | 9.8 ± 3 | ND | ND | 4.4 ± 2.7 | ~25 | 71 ± 17 | ND | ~25 | 154 | NA | ~5.7 |
| A22 | 0.32 ± 0.2 | 32 ± 17 | 0.33 ± 0.2 | 11± 7 | 3.4 ± 2.5 | >25 | 90 ± 6 | 71 ± 17 | >25 | 281 | 215 | >7.3 |
| A23 | 0.11 ± 0.01 | 10 ± 2 | 0.1 ± 0.03 | 6.7 ± 4 | 5.2 ± 1.6 | >25 | 33 ± 8 | 48 ± 20 | ~25 | 300 | 480 | ~4.8 |
| A24 | 0.29 ± 0.1 | 31 ± 16 | 0.4 ± 0.01 | 32 ± 10 | 7.1 | >25 | 102 ± 3 | 97 ± 3 | >25 | 352 | 243 | >3.5 |
| A25 | 0.5 ± 0.1 | 30 ± 12 | ND | ND | 3.7 ± 2.3 | >25 | 91 ± 16 | ND | ~25 | 182 | NA | ~6.7 |
(a)
Not determined (ND)