Table 1.
Effect of pore helix, S5, and S6 mutations and mutations attenuating inactivation on IhERG inhibition by Cavalli-2
| Channel | Voltage step | K+ | IC50 (CI) | nH (CI) | Potency reduction compared with its WT-control (fold WT IC50) |
|---|---|---|---|---|---|
| mV | mm | nm | |||
| WT-1 | −40 | 4 | 35.6 (30.9–41.1) | 0.69 (0.62–0.77) | |
| WT-2 | −120 | 94 | 17.5 (13.8–22.1) | 0.99 (0.55–1.42) | |
| N588K | −40 | 4 | 544 (445–664) | 0.97 (0.76–1.17) | 15.3 |
| S620T | −40 | 4 | 1916 (1434–2561) | 0.63 (0.47–0.79) | 53.8 |
| T623A | −120 | 94 | 281 (196–403) | 0.54 (0.39–0.69) | 16.1 |
| S624A | −40 | 4 | 262 (209–328) | 0.72 (0.58–0.87) | 7.4 |
| Y652A | −40 | 4 | 594 (466–756) | 0.74 (0.58–0.90) | 16.7 |
| F656A | −120 | 94 | 1315 (1004–1725) | 0.93 (0.65–1.21) | 75.1 |
| F557L | −40 | 4 | 339 (293–392) | 1.20 (0.94–1.47) | 9.5 |