Search
Streamline early cardiac safety assessment with comprehensive hERG Screening Services that identify potential hERG channel liabilities early in drug discovery. Using the validated Predictor hERG Fluorescence Polarization Assay, we deliver reliable, high-quality binding data that correlates closely with patch-clamp electrophysiology, enabling informed lead optimization and candidate selection.
- High-quality data
- Guaranteed two-week turnaround 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 helps ensure the high-quality data. Strict quality control protocols help ensure that any assay results not meeting set specifications will automatically be repeated.
Technology overview
The Predictor hERG Fluorescence 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) |
|
|---|---|---|---|
Predictor assay |
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
Personalized support is at the core of every SelectScreen project. From project initiation through data delivery, you'll work with a dedicated project manager who serves as your single point of contact, providing proactive communication, coordinating timelines and milestones, and ensuring proficient project execution.
Backed by experienced scientists and technical specialists, our team works as an extension of yours to deliver a responsive, collaborative experience and high-quality results tailored to your research goals.
For Research Use Only. Not for use in diagnostic procedures.