hERG Assay Services

Human ether-a-go-go-related gene potassium channel 1 (hERG) is an ion channel important for cardiac function. In addition to our suite of cell-based assays for cardiac safety assessment, we offer a biochemical binding assay for hERG screening.

Low scale, large scale screening, and high-throughput options for hERG assays screening are available
The fluorescent polarization assay allows rapid screening of early drug candidates for inexpensive assessment of hERG interaction
hERG safety assays are usually the beginning of a series of cardiac safety screening measures

Contact an expert

Meet us at your next conference

Name	Synonyms	Data
hERG	Potassium voltage-gated channel subfamily H member 2, Ether-a-go-go-related gene potassium channel 1, ERG, ERG1, HERG, KCNH2	Data sheet

hERG Binding Assay Information

Assay Format

To identify potential hERG channel blockers we employ the Predictor hERG Fluorescence Polarization Assay Kit (ThermoFisher) which provides a set of validated components to perform hERG channel biochemical binding studies in the absence of radioligand. The assay was designed by producing data that accurately correlates with patch clamp electrophysiology studies.

The assay principle is based on fluorescence polarization where a red-shifted fluorescent tracer is displaced from the hERG channel by compounds that bind to the channel.

Please see our FAQ page to access our assay condition form (US facility).

Assay Setup

Setups: Single-dose screening in duplicates or IC50 value determination with 5 or 10 concentrations. Other screening formats are available upon request.

Controls: No inhibitor (DMSO vehicle) control and for every assay, one target-specific control compound is tested in 10-dose IC50 format.

Turnaround time: 10 business days for standard projects. Expedited scheduling and data delivery can be arranged prior to the commencement of the studies.

Report: The raw data, % tracer binding and control compound IC50 values will be reported in Excel format for single-dose assays. For IC50 orders, raw data, IC50 values, and curve fitting will be delivered in Excel format. Assay conditions, target, and substrate information are available upon request. Requirements for this information should be noted prior to the commencement of the study.

Screening facility: This assay is performed at our screening facility in Malvern, PA, US.

Compound requirements: In brief, for a standard project, 20ul of a 10mM DMSO stock or solid material is needed. Less material is needed for large scale screening. Please refer to our FAQs for information regarding compound preparation and shipping.

FAQs:

What is a hERG binding assay?

A hERG binding assay is a biochemical test used to assess the potential of compounds to bind to the hERG potassium channel, which is critical for cardiac repolarization. Identifying such interactions is essential, as hERG channel inhibition can lead to cardiac arrhythmias.

Why is hERG binding assessment important in drug development?

Assessing hERG binding is crucial in drug development to predict and mitigate potential cardiotoxic effects. Compounds that inhibit the hERG channel can prolong the QT interval, leading to serious arrhythmias. Early detection helps in modifying or eliminating such compounds from the development pipeline.

What are the advantages of using a fluorescence polarization assay for hERG screening?

Fluorescence polarization assays offer a homogeneous, non-radioactive method for assessing hERG binding. They are suitable for high-throughput screening, provide rapid results, and reduce safety concerns associated with radioactive materials.

Does Reaction Biology offer both hERG binding and patch-clamp assays for assessing hERG channel inhibition?

Reaction Biology offers both hERG binding assays and patch-clamp electrophysiology assays for cardiac safety assessment. The hERG binding assay provides a reliable, high-throughput method that correlates strongly with patch-clamp studies, making it valuable for early detection of potential hERG channel blockers. For more detailed characterization of compound effects on ion channel activity, patch-clamp electrophysiology provides direct, functional measurements. Together, these assays offer complementary insights into hERG inhibition and potential cardiotoxicity risks.

What types of compounds can be assessed using Reaction Biology's hERG binding assay?

Reaction Biology’s hERG binding assay can evaluate a wide range of compounds, including small molecules and biologics, for their potential to interact with the hERG channel, aiding in comprehensive cardiac safety profiling.