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Journal of Biomolecular Screening
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Development and Evaluation of High Throughput Functional Assay Methods for hERG Potassium Channel

Weimin Tang

Department of Profiling and High Throughput Screening, Aventis Pharmaceuticals, Bridgewater, NJ

Jiesheng Kang

Department of Safety Pharmacology, Aventis Pharmaceuticals, Bridgewater, NJ

Xiaying Wu

Department of Profiling and High Throughput Screening, Aventis Pharmaceuticals, Bridgewater, NJ

David Rampe

Department of Safety Pharmacology, Aventis Pharmaceuticals, Bridgewater, NJ

Lin Wang

Department of Safety Pharmacology, Aventis Pharmaceuticals, Bridgewater, NJ

Hong Shen

Department of Analytical Chemistry, Aventis Pharmaceuticals, Bridgewater, NJ

Zhuyin Li

Department of Profiling and High Throughput Screening, Aventis Pharmaceuticals, Bridgewater, NJ

Damien Dunnington

Axiom Biotechnology, San Diego, CA

Tina Garyantes

Department of Profiling and High Throughput Screening, Aventis Pharmaceuticals, Bridgewater, NJ

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.

Journal of Biomolecular Screening, Vol. 6, No. 5, 325-331 (2001)
DOI: 10.1177/108705710100600506
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