TABLE 1
Channel blockage and antiviral activity of M2-S31N inhibitors
| Structure | ||
|---|---|---|
 |  | |
| M2-S31N channel inhibitiona | 85%/65%b | 76%/N.T.c |
| Plaque assay EC50 (µM)d | 0.49 | 2.2 |
| CPE EC50 (µM)e | 0.36 | 6.20 |
| Cellular toxicity CC50 (µM)f | 125 | 123c |
| SIg | 255 | 56c |
N.T., not tested; SI, selectivity index.
↵a M2-S31N channel inhibition was measured using two-electrode voltage clamp assay as described (Wang et al., 2013b; Wu et al., 2014). The data are expressed as percentage inhibition at 100/30 µM compound concentration.
↵b Reported in Wang et al. (2013b).
↵c Reported in Wu et al. (2014).
↵d EC50 in plaque assays was determined with the A/WSN/33 (H1N1) virus.
↵e EC50 in CPE assay was determined with the A/WSN/33 (H1N1) virus using MTT.
↵f CC50 was assayed using MTT after incubating MDCK cells with increasing concentrations of compounds for 72 hours.
↵g SI was calculated by dividing CC50 values over plaque assay EC50 values.