Referenced in: none

Automatically associated channels: Kv11.1

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

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

Journal, date & volume: Bioorg. Med. Chem. Lett., 2006 Mar 15 , 16, 1692-5

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/16377185

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.