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To complement our functional assays for hERG safety assessment, Eurofins provides membrane preps for hERG radioligand binding assays. These have been tested to work with commonly used radioligands, [3H]- astemizole, [125I]-BeKm and [3H]-dofetilide, to provide comparable data to that found in the literature. While not providing a functional measure of hERG activity, the high throughput nature of radioligand binding assays has made this a useful approach for monitoring potential hERG liability at the earliest phase of drug discovery. Here, the primary aims are to raise flags which could trigger follow-up studies, such as electrophysiological screening.
Advantages of PrecisION™ Membrane Preps:
Figure 1. Radioligand binding assays for hERG screening
A) Competition binding data for hERG ligands using Eurofins membrane preparations from hERG expressing HEK293 cells (Cat. No. CYL4039) were incubated with 3.0 nM [3H]-Astemizole and increasing concentrations of different compounds. B) Ki values obtained compared to published data.