List of Assays
|hERG||Potassium voltage-gated channel subfamily H member 2, Ether-a-go-go-related gene potassium channel 1, ERG, ERG1, HERG, KCNH2||Data sheet|
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.
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, % enzyme activity 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.