Table 2.
Inhibitory effect on polykaryon formation induced by WT or mutant forms of H3 HA a .
| Compound | EC50 b (µM) | ||
|---|---|---|---|
| HA‐WT | HA‐E572K | HA‐D1122N | |
| pH: 5.2c | pH: 5.2c | pH: 5.6c | |
| 2c | 7.6 | ≥ 28 | > 50 |
| 4c | 1.4 | 12 | > 50 |
The two mutations in the HA2 subunit (E572K and D1122N) were previously identified in influenza A/H3N2 viruses selected for resistance to imidazo[2,1‐b]thiazole analogue 4c (Vanderlinden et al. 2010). The mutations were introduced in an expression plasmid encoding the X‐31 H3 HA, to perform the polykaryon assay.
EC50: compound concentration at which the number of polykaryons was 50% relative to the number observed in the no compound control. The EC50 values for compound 4c were reported earlier (Vanderlinden et al. 2010),
Fusion pH: pH at which the number of polykaryons was 50% relative to the number seen at pH 4.9. Values reported in (Vanderlinden et al. 2010).