Development and evaluation of high throughput functional assay methods for HERG potassium channel.
Article Details
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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
Drug Target Kind Organism Pharmacological Action Actions Sertindole Potassium voltage-gated channel subfamily H member 2 Protein Humans UnknownInhibitorDetails