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Bioorg Med Chem Lett. 2006 Sep 1;16(17):4633-7. Epub 2006 Jun 16.

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

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1
Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, Kent, UK. david.a.price@pfizer.com

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.

PMID:
16782336
DOI:
10.1016/j.bmcl.2006.06.012
[Indexed for MEDLINE]
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