Rapidly assess hERG channel block
The SelectScreen hERG Screening Service utilizes Thermo Fisher Scientific Predictor hERG Fluorescence Polarization Assay to quickly identify compounds that bind the hERG channel. This service will provide you with quick and reliable information regarding the potential liability of your compound to bind the hERG channel, giving you the confidence to move forward with your discovery research.
The SelectScreen hERG Screening Service offers:
- High quality data
- Guaranteed two-week turn around time
- 10-point dose response curves in duplicate
- Controls on every plate
- Open business model—no minimum commitment or licensing fees
Protocol and Assay Conditions
A stringent validation process ensures the highest quality data possible. Strict quality control protocols ensure that any assay results not meeting set specifications will automatically be repeated.
Technology behind the SelectScreen hERG Screening Service
The Predictor™ hERG Fluoresence Polarization assay uses a proprietary fluorescent tracer and membrane preparation to create a highly reproducible assay. Using the assay, IC50 values for over 10 known hERG channel blockers compared well to published patch clamp and radioligand binding data (Figure 1 and Table 1).
Figure 1. Predictor assay compared to patch-clamp analysis. Values obtained from the Predictor fluorescence polarization assay are compared to those obtained using patch-clamp techniques. Linear regression analysis indicates that the data are highly correlated with the slope near unity. Dotted lines represent the 95% confidence intervals of the fit.
Table 1. Comparison of IC50 data from Figure 1 to established patch-clamp and radioactive binding data for each compound.
| Compound | IC50 (nM) | Ki (nM) | |
|---|---|---|---|
| Predictorassay | Patch-clamp* | [3H] - dofetilide binding* | |
| Astemizole | 2.7 | 1.2 | 1 |
| Pimozide | 7.2 | 18 | 6 |
| Dofetilide | 11 | 12 | 40 |
| E-4031 | 17 | 48 | 20 |
| Terfenadine | 33 | 16 | 30 |
| Haloperidol | 187 | 174 | 90 |
| Bepridil | 279 | 550 | 170 |
| Thioridazine | 655 | 1250 | 510 |
| Fluoxetine | 2880 | 990 | 2230 |
| Amitryptiline | 8135 | 10000 | *2440 |
| *Patch-clamp values are derived from the following publications: Mol Pharmacol (1998) 54: 695; J Pharmacol Toxicol Methods (2004) 50: 187; Eur J Pharmacol (2002) 450: 37; Mol Pharmacol (1996) 49: 949; Lancet (2000) 355: 1825; Am J Physiol Heart Circ Physiol (2003) 284: H256. [3H]-dofetilide binding values are derived from J Pharmacol Toxicol Methods (2004) 50: 187 (with 60 mM K+, except amitryptiline with 5 mM K+). | |||
Personalized support
From project beginning to end, you can rely on our Drug Discovery Services project management team to provide frequent project communication via a single point of contact.
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