Balancing hERG affinity and absorption in the discovery of AZD5672, an orally active CCR5 antagonist for the treatment of rheumatoid arthritis
Modifications to a series of potent and selective substituted 1-(3,3-diphenylpropyl)-piperidine phenylacetamide CCR5 antagonists were explored with the aim of reducing affinity at the hERG cardiac ion channel. Replacement of one aromatic ring in the diphe
Cumming, John G.,Tucker, Howard,Oldfield, John,Fielding, Colin,Highton, Adrian,Faull, Alan,Wild, Martin,Brown, Dearg,Wells, Stuart,Shaw, John
p. 1655 - 1659
(2012/04/04)
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