Balancing hERG affinity and absorption in the discovery of AZD5672, an orally active CCR5 antagonist for the treatment of rheumatoid arthritis.

Cumming, John G; Tucker, Howard; Oldfield, John; Fielding, Colin; Highton, Adrian; Faull, Alan; Wild, Martin; Brown, Dearg; Wells, Stuart; Shaw, John

Cumming, John G; Tucker, Howard; Oldfield, John; Fielding, Colin; Highton, Adrian; Faull, Alan; Wild, Martin; Brown, Dearg; Wells, Stuart; Shaw, John.

Affiliation

Cumming JG; Respiratory and Inflammation Research Area, AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire, UK. john.cumming@astrazeneca.com

Bioorg Med Chem Lett ; 22(4): 1655-9, 2012 Feb 15.

Article in En | MEDLINE | ID: mdl-22266038

Subject(s)

Arthritis, Rheumatoid; Benzeneacetamides/chemical synthesis; CCR5 Receptor Antagonists; Drug Discovery; Ether-A-Go-Go Potassium Channels/metabolism; Sulfonamides/chemical synthesis; Absorption; Administration, Oral; Arthritis, Rheumatoid/drug therapy; Benzeneacetamides/administration & dosage; Benzeneacetamides/pharmacology; ERG1 Potassium Channel; Ether-A-Go-Go Potassium Channels/chemistry; Humans; Inhibitory Concentration 50; Molecular Structure; Protein Binding/drug effects; Receptors, CCR5/metabolism; Sulfonamides/administration & dosage; Sulfonamides/pharmacology

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Full text: 1 Database: MEDLINE Main subject: Arthritis, Rheumatoid / Sulfonamides / Benzeneacetamides / Ether-A-Go-Go Potassium Channels / Drug Discovery / CCR5 Receptor Antagonists Limits: Humans Language: En Year: 2012 Type: Article

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