Synthesis of the first sulfur-35-labeled hERG radioligand

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.

The synthesis of hERG radioligand [35S]MK-0499 for use in an HTS assay for IKr activity is reportedFigure optionsDownload as PowerPoint slide