Overcoming HERG affinity in the discovery of the CCR5 antagonist maraviroc |
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| Authors: | Price David A Armour Duncan de Groot Marcel Leishman Derek Napier Carolyn Perros Manos Stammen Blanda L Wood Anthony |
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| Affiliation: | Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, Kent, UK. david.a.price@pfizer.com |
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| 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. |
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