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hERG Electrophysiology Assay and Cell Lines
AVIVA's scientists have optimized the assay condition and performed extensive validation using as several hERG channel blockers with known cardiac liability.
The CHO-hERG cell line was generated at AVIVA biosciences. Using Sealchip-based high throughput electrophysiology this particular line was selected for
- Consistent hERG current expression
- Limited runup or rundown
- Robust pharmacology
The assay parameters for testing compounds' activity on the hERG channel have been optimized on the Sealchip-based high throughput electrophysiology to ensure
- Reliable IC50 even for more hydrophobic compounds by minimizing adsorption
- Detection of use-dependent blockers
- High reproducibility
- Data highly predictive of clinical cardiac liabilities
| Drug | cLogP | Literature (nM) | AVIVA (nM) | Structure |
|---|---|---|---|---|
| Astemizole | 5.65 | 1 - 26 | 6 ± 0.3 |
 |
| Cisapride | 2.97 | 2 - 45 | 8 ± 1 |  |
| Pimozide | 6.4 | 15 - 55 | 8 ± 0.7 |  |
| Terfenadine | 6.5 | 20 - 200 | 44 ± 3 |  |
| Haloperidol | 3.98 | 20 - 50 | 30 ± 2 |  |
| Thioridazine | 5.13 | 33 - 1250 | 246 ± 12 |  |
| Verapamil | 4.47 | 140 - 800 | 391 ± 20 |  |
| Quinidine | 2.79 | 300 - 1000 | 989 ± 72 |  |
| Amiodarone | 8.95 | 1000 - 9800 | 136 ± 10 |  |
| Diphenhydramine | 3.27 | 20000 - 50000 | 6800 ± 530 |  |
| Aspirin | 1.3 | 30000 - 100000 | 60000 |  |
For a complete report on the optimization and validation of the AVIVA assay,
please see
Tao et al. 2004.
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