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Synthesis of the first sulfur-35-labeled hERG radioligand. | LitMetric

Synthesis of the first sulfur-35-labeled hERG radioligand.

Bioorg Med Chem Lett

Department of Drug Metabolism, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA.

Published: March 2006

AI Article Synopsis

Article Abstract

The synthesis of the first high specific activity S-35-labeled hERG radioligand, [(35)S]MK-0499, for use in HTS assays of drug candidates for hERG interaction is described. The radioligand is prepared by [(35)S]sulfonylation of a high diastereomeric excess (de) aniline precursor prepared from unlabeled MK-0499.

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Source
http://dx.doi.org/10.1016/j.bmcl.2005.12.021DOI Listing

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