Referenced in: none

Automatically associated channels: Kv11.1

Title: Overcoming HERG affinity in the discovery of the CCR5 antagonist maraviroc.

Authors: David A Price, Duncan Armour, Marcel de Groot, Derek Leishman, Carolyn Napier, Manos Perros, Blanda L Stammen, Anthony Wood

Journal, date & volume: Bioorg. Med. Chem. Lett., 2006 Sep 1 , 16, 4633-7

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/16782336

Abstract
The discovery of maraviroc 17 is described with particular reference to the generation of high selectivity over affinity for the HERG potassium channel. This was achieved through the use of a high throughput binding assay for the HERG channel that is known to show an excellent correlation with functional effects.