TABLE 1.
Activities of the identified inhibitors using the NoV RdRp and cell culture models
| Compound | CLogPa | GII.4 RdRp IC50 (μM)b | GI.1 replicon EC50 (μM)c | GV.1 MNV EC50 (μM)c |
|---|---|---|---|---|
| NIC02 | 3.6 | 5.0 (3.6–6.9) | 30.1 (19.6–45.9) | 4.8 (1.7–13.3) |
| NIC04 | 3.5 | 5.5 (4.5–6.7) | 71.1 (56.7–89.1) | 32.8 (22.0–48.9) |
| NIC10 | 0.8 | 9.2 (7.4–11.3) | >100 | 34.5 (22.6–52.5) |
| NIC12 | 0.4 | 9.8 (7.4–13.0) | >100 | 38.1 (17.7–82.4) |
a
CLogP, calculated partition coefficient.
b
IC50s were determined by in vitro radioactive-GTP incorporation RdRp assays (95% CI in parentheses).
c
EC50s were determined using cell-based replicon and infectious-NoV model systems (95% CI in parentheses).