Table 1. Inhibition of the RdRp activity by RK-0404678 for the full-length DENV1-4 NS5 proteins (determined as IC50) and inhibition of the viral replication of DENV1-4 by RK-0404678 (determined as EC50).
DENV1 | DENV2 | DENV3 | DENV4 | |
---|---|---|---|---|
IC50 (μM) Polymerase assay |
46.2 ± 2.8 | 201 ± 4.9 | 287 ± 11 | 445 ± 23 |
EC50 (μM) Cell-based assay |
29.5 ± 4.2 | 6.0 ± 0.30 | 29.4 ± 1.8 | 31.9 ± 2.8 |
The results shown are the mean and standard deviation of quadruplicate measurements for IC50 values in a single experiment and triplicate measurements for EC50 values. For EC50 values, one representative result of three independent experiments is shown. The IC50 and EC50 values were compared by Extra Sum-of-Squares F test in PRISM version 6 (GraphPad Software, Inc.). The p-values for differences in IC50 values were p < 0.0001 for all combinations of the four serotypes. The p-values for differences in EC50 values are as follows: p < 0.0001 for DENV1–DENV2, DENV2–DENV3, and DENV2–DENV4; p = 0.135 for DENV1–DENV3; p = 0.131 for DENV1–DENV4; p = 0.294 for DENV3–DENV4.