Predictor™ hERG Fluorescence Polarization Assay Kit
The kit contains suitable volumes of reagents to generate 400 data points. The kit components are as follows:
•Validated hERG membranes
•hERG tracer red
•Known hERG channel blocker
The Predictor™ hERG kit is a homogeneous fluorescence assay that has a simple add-and-read format, supports high-throughput screening, and provides high accuracy, solvent tolerance, and stability over time.
Each kit contains enough reagents for 400 wells in a 384 well format.
The Predictor™ hERG Fluorescence Polarization Assay Kit provides a set of validated components to perform hERG channel biochemical binding studies in the absence of radioligands. The assay was designed to identify potential hERG channel blockers by producing data that accurately correlates with patch-clamp electrophysiology studies. The assay is based on the principle of fluorescence polarization, where a red-shifted fluorescent tracer displays a high polarization when bound to the hERG channel and a low polarization when displaced by compounds that bind to the channel. Assay performance was validated with a panel of established hERG channel blockers (Figure 1). Results from the Predictor™ assay demonstrate a high correlation with those obtained from patch-clamp techniques (Table 1 and Figure 2).
Read the frequently asked questions document and see the comparative data to patch clamp and radioligand binding using a 41 compound test set.
|Compound||IC50 (nM)||Ki (nM)|
|Predictor™ assay||Patch-clamp*||[3H] - dofetilide binding**|
|*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+).