Table 2.
Dofetilide and its derivatives: affinity for hERG potassium channels and concentration (D150) that prolongs the AP by 50%
| Compound | MW | hERG IC50 (nM) | D150 (nM) |
|---|---|---|---|
| Dofetilide | 441.567 | 3.1 ± 0.6 (n = 5) | 0.04 |
| Dofe54 | 395.84 | 2.6 ± 0.4 (n = 5) | 4.3 |
| Dofe81 | 409.87 | 10.7 ± 1.4 (n = 6) | 2.5 |
| Dofe60 | 413.83 | 15.3 ± 8.4 (n = 5) | 21.3 |
| Dofe78 | 345.35 | 28.2 ± 4.9 (n = 7) | 20 |
| Dofe35 | 381.82 | 22.1 ± 5.5 (n = 8) | 8.3 |
| Dofe45 | 336.82 | 38.6 ± 9.2 (n = 5) | 538 |
| Dofe33 | 319.88 | 221.6 ± 40.8 (n = 6) | 215 |
| Dofe31 | 360.71 | 125.2 ± 19.4 (n = 7) | 151 |
| Dofe30 | 291.82 | 296.9 ± 77.5 (n = 7) | 213 |
| Dofe41 | 326.26 | 164.6 ± 31.8 (n = 8) | 157.2 |
| Dofe42 | 321.84 | 213 ± 83.5 (n = 8) | 650 |
| Dofe43 | 305.84 | 184.3 ± 66.9 (n = 5) | 99.3 |
| Dofe44 | 360.71 | 38.1 ± 12.6(n = 6) | 650 |