TABLE 2.
Inhibition by quinine, quinidine, and derivatives of hERG channels expressed in CHO cells using the Ionworks patch clamp assaya
| Compound | IC50 (μM) |
Hill coefficient (SD) | % at max concn | hERG inhibitor | |
|---|---|---|---|---|---|
| Reportedb | Experimental (SD) | ||||
| Dofetilide | 0.1 | 0.05 (0.01) | 2.27 (0.79) | −100 | Yes |
| Quinine | 57 | 42.2 (7.41) | 1.3 (0.3) | −83.4 | Yes |
| HEQ | >100 | −35.2 | No | ||
| HEAQ | 109 (20.9) | 1.8 (0.83) | −49.4 | Yes | |
| Quinidine | 4.6 | 3.95 (0.75) | 0.96 (0.18) | −95.8 | Yes |
| HEQD | 94.3 (8.12) | 4 (0) | −70.1 | Yes | |
| HEAQD | 27.3 (7.57) | 3 (0) | −87.0 | Yes | |
a
Compounds were tested in quadruplicate. SD, standard deviation.
b
Reported values of hERG inhibition from reference 11.