TABLE 6.
hERG channel inhibition of ELP‐004 [0.5–100 μM].
| hERG channel inhibition | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| % Mean inhibition | IC50 determination | |||||||||
| Test compound: ELP‐004 | ||||||||||
| Compound | 0.5 μM | 1 μM | 5 μM | 10 μM | 50 μM | 100 μM | IC50 (μM) | pIC50 | pIC50 SE | N |
| 2.11 | 1.44 | 2.03 | 3 | 13.96 | 27.87 | >100 | <4 | ‐ | 4 | |
| Negative control: Vehicle (0.5% DMSO) | ||||||||||
| Compound | 1st addition | 2nd addition | 3rd addition | 4th addition | 5th addition | 6th addition | IC50 (μM) | pIC50 | pIC50 SE | N |
| 3.8 | 4.97 | 5.39 | 3.95 | 3.37 | 4.03 | ‐ | ‐ | ‐ | 3 | |
| Positive control: E‐4031 | ||||||||||
| Compound | 0.001 μM | 0.003 μM | 0.011 μM | 0.033 μM | 0.1 μM | 0.3 μM | IC50 (μM) | pIC50 | pIC50 SE | N |
| 0.79 | 5.36 | 26.5 | 52.71 | 80.06 | 91.55 | 0.03 | 7.53 | 0.03 | 5 | |