Table 1.
IC50 and Hill coefficient values of the hERG channel retrieved from the literature to calculate Bnet5×Cma x for the 16 validation drugs.
| Compound | IC50 (µM) | Hill coefficient | Model | Literature | Temperature (°C) | Technique |
|---|---|---|---|---|---|---|
| Ibutilide | 2 | ≒1 | XO | (Lin et al., 2008) | 21.5 | Voltage-clamp 2-electrode |
| Azimilide | 0.61 | 1 | CHO | (Walker et al., 2000) | 22 | Whole-cell PC |
| Disopyramide | 7.23 | 0.89 | CHO | (Paul et al., 2001) | 36 | Whole-cell PC |
| Domperidone | 0.057 | 0.99 | HEK | (Claassen and Zünkler, 2005) | 21 | Whole-cell PC |
| Droperidol | 0.0322 | 1.39 | HEK | (Drolet et al., 1999) | 22.5 | Whole-cell PC |
| Pimozide | 0.001 | 1.1 | HEK | (Kirsch et al., 2004) | 35 | Whole-cell PC |
| Astemizole | 0.0013 | 0.95 | HEK | (Tarantino et al., 2005) | 35 | Whole-cell PC |
| Clozapine | 2.5 | 0.82 | HEK | (Lee et al., 2006) | 35 | Whole-cell PC |
| Clarithromycin | 750 | 1.7 | CHO | (Abbott et al., 1999) | Whole-cell PC | |
| Risperidone | 0.167 | 1 | CHO | (Kongsamut et al., 2002) | 23 | Whole-cell PC |
| Metoprolol | 145 | 1.1 | HEK | (Kawakami et al., 2006) | 23 | Whole-cell PC |
| Tamoxifen | 1.2 | 1.4 | HEK | (Chae et al., 2015) | 23 | Whole-cell PC |
| Nifedipine | >50 | HEK | (Zhang et al., 1999) | 23 | Whole-cell PC | |
| Nitrendipine | 10 | (Redfern et al., 2003) | ||||
| Loratadine | 173 | HEK | (Crumb, 2000) | 36 ± 1 | Whole-cell PC | |
| Vandetanib | 1.15 | 0.76 | HEK | (Lee et al., 2018) | 37 ± 0.5 | Whole-cell PC |
CHO, Chinese hamster ovary cells; HEK, human embryonic kidney (HEK293) cells; Whole-cell PC, Whole-cell voltage-clamp recordings.