| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1379093 | Bioorganic & Medicinal Chemistry Letters | 2006 | 4 Pages |
Abstract
The synthesis of the first high specific activity S-35-labeled hERG radioligand, [35S]MK-0499, for use in HTS assays of drug candidates for hERG interaction is described. The radioligand is prepared by [35S]sulfonylation of a high diastereomeric excess (de) aniline precursor prepared from unlabeled MK-0499.
Graphical abstractThe synthesis of hERG radioligand [35S]MK-0499 for use in an HTS assay for IKr activity is reportedFigure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Conrad E. Raab, John W. Butcher, Thomas M. Connolly, Jerzy Karczewski, Nathan X. Yu, Steven J. Staskiewicz, Nigel Liverton, Dennis C. Dean, David G. Melillo,