title: Overcoming HERG affinity in the discovery of the CCR5 antagonist maraviroc.
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.
authors.affiliation: Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, Kent, UK. david.a.price@pfizer.com
authors.forename: David A
authors.initials: DA
authors.lastname: Price
authors.forename: Duncan
authors.initials: D
authors.lastname: Armour
authors.forename: Marcel
authors.initials: M
authors.lastname: de Groot
authors.forename: Derek
authors.initials: D
authors.lastname: Leishman
authors.forename: Carolyn
authors.initials: C
authors.lastname: Napier
authors.forename: Manos
authors.initials: M
authors.lastname: Perros
authors.forename: Blanda L
authors.initials: BL
authors.lastname: Stammen
authors.forename: Anthony
authors.initials: A
authors.lastname: Wood
mesh_terms: D000998:Antiviral Agents / Q000737:chemistry / Q000494:pharmacology; D065100:CCR5 Receptor Antagonists; D002460:Cell Line; D054407:Chemokine CCL4; D051638:Ether-A-Go-Go Potassium Channels / Q000378:metabolism*; D006678:HIV / Q000187:drug effects; D006801:Humans; D019402:Macrophage Inflammatory Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D008958:Models, Molecular; D015394:Molecular Structure; D019713:Receptors, CCR5 / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000998:Antiviral Agents; D065100:CCR5 Receptor Antagonists; D054407:Chemokine CCL4; D051638:Ether-A-Go-Go Potassium Channels; D019402:Macrophage Inflammatory Proteins; D019713:Receptors, CCR5