4.5 Article

Overcoming HERG affinity in the discovery of the CCR5 antagonist maraviroc

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 16, Issue 17, Pages 4633-4637

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.06.012

Keywords

maraviroc; tropanes; triazoles; ion channel; HERG

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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. (c) 2006 Elsevier Ltd. All rights reserved.

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