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A Thallium-Sensitive, Fluorescence-Based Assay for Detecting and Characterizing Potassium Channel Modulators in Mammalian Cells

Vanderbilt Institute of Chemical Biology and Department of Pharmacology 812 Robinson Research Building Nashville, TN 37232-6600david.weaver{at}vanderbilt.edu

David Harden

Lead Discovery, Bristol-Myers Squibb Pharmaceuticals Research Institute, Wallingford, CT.

Steven I. Dworetzky

Neuroscience Drug Discovery, Bristol-Myers Squibb Pharmaceuticals Research Institute, Wallingford, CT.

Barbara Robertson

Ronald J. Knox

Lead Discovery, Bristol-Myers Squibb Pharmaceuticals Research Institute, Wallingford, CT.

Potassium channels have been identified as targets for a large number of therapeutic indications. The ability to use a high-throughput functional assay for the detection and characterization of small-molecule modulators of potassium channels is very desirable. However, present techniques capable of screening very large chemical libraries are limited in terms of data quality, temporal resolution, ease of use, and requirements for specialized instrumentation. To address these issues, the authors have developed a fluorescence-based thalliumflux assay. This assay is capable of detectingmodulators of both voltageand ligand-gated potassium channels expressed inmammalian cells. The thalliumflux assay can use instruments standard to most high-throughput screening laboratories, and using such equipment has been successfully employed to screen large chemical libraries consisting of hundreds of thousands of compounds.

Key Words: fluorescent • thallium • potassium • channel

Journal of Biomolecular Screening, Vol. 9, No. 8, 671-677 (2004)
DOI: 10.1177/1087057104268749


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