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Synthesis of the first sulfur-35-labeled hERG radioligand |
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| Authors: | Raab Conrad E Butcher John W Connolly Thomas M Karczewski Jerzy Yu Nathan X Staskiewicz Steven J Liverton Nigel Dean Dennis C Melillo David G |
| Affiliation: | Department of Drug Metabolism, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. conrad_raab@merck.com |
| 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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