Development and evaluation of high throughput functional assay methods for HERG potassium channel.

Article Details

Citation

Tang W, Kang J, Wu X, Rampe D, Wang L, Shen H, Li Z, Dunnington D, Garyantes T

Development and evaluation of high throughput functional assay methods for HERG potassium channel.

J Biomol Screen. 2001 Oct;6(5):325-31.

PubMed ID
11689132 [ View in PubMed
]
Abstract

Three functional hERG channel assay methods have been developed and evaluated. The methods were tested against five known hERG channel inhibitors: dofetilide, terfenadine (Seldane), sertindole (Serdolect), astemizole (Hismanal), and cisapride (Propulsid). The DiBAC4(3)-based assays were found to be the most economical but had high false-hit rates as a result of the interaction of dye with the test compounds. The membrane potential dye assay had fewer color-quenching problems but was expensive and still gave false hits. The nonradioactive Rb+ efflux assay was the most sensitive of all the assays evaluated and had the lowest false-hit rate.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
SertindolePotassium voltage-gated channel subfamily H member 2ProteinHumans
Unknown
Inhibitor
Details