Table 2. Inhibition of the RdRp activity by RK-0404678 for the full-length DENV1 and DENV2 NS5 mutant proteins.
| Activity compared to WT (%) | IC50 (μM) | |
|---|---|---|
| DENV1 NS5 | ||
| WT | 100 | 46.2 ± 2.7 |
| Site 1 | ||
| C779A | 82.2 | 65.5 ± 4.7 ** |
| C779Q | 94.9 | 137 ± 5.8 **** |
| Site 2 | ||
| C708A | 46.4 | 93.8 ± 7.0 **** |
| C708Q | 48.6 | 170 ± 8.3 **** |
| Site 1 & Site 2 | ||
| C779A/C708A | 24.8 | 163 ± 16 **** |
| C779Q/C708Q | 29.6 | 181 ± 13 **** |
| DENV2 NS5 | ||
| WT | 100 | 201 ± 4.9 |
| Site 1 | ||
| C780A | 31.8 | 206 ± 6.1 § |
| C780Q | 87.7 | 227 ± 6.9 **** |
| Site 2 | ||
| C709A | 54.7 | 427 ± 27 **** |
| C709Q | 53.7 | 368 ± 12 **** |
The results shown are the mean and standard deviation of quadruplicate measurements in a single experiment. The IC50 values were compared by Extra Sum-of-Squares F test in PRISM version 6 (GraphPad Software, Inc.).
**p < 0.01
***p < 0.001
****p < 0.0001, and
§p = 0.01, compared with WT.