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Discovery of AZD-2098 and AZD-1678, two potent and bioavailable CCR4 receptor antagonists

Kindon, Nicholas; Andrews, Glen; Baxter, Andrew; Cheshire, David; Hemsley, Paul; Johnson, Timothy; Liu, Yu-Zhen; McGinnity, Dermot; McHale, Mark; Mete, Antonio; Reuberson, James; Roberts, Bryan; Steele, John; Teobald, Barry; Unitt, John; Vaughan, Deborah; Walters, Iain; Stocks, Michael J.

Authors

Glen Andrews

Andrew Baxter

David Cheshire

Paul Hemsley

Timothy Johnson

Yu-Zhen Liu

Dermot McGinnity

Mark McHale

Antonio Mete

James Reuberson

Bryan Roberts

John Steele

Barry Teobald

John Unitt

Deborah Vaughan

Iain Walters

MICHAEL STOCKS MICHAEL.STOCKS@NOTTINGHAM.AC.UK
Professor of Medicinal Chemistryand Drug Discovery



Abstract

N-(5-Bromo-3-methoxypyrazin-2-yl)-5-chlorothiophene-2-sulfonamide 1 was identified as a hit in a CCR4 receptor antagonist high throughput screen (HTS) of a sub-set of the AstraZeneca compound bank. As a hit with a lead-like profile, it was an excellent starting point for a CCR4 receptor antagonist program and enabled the rapid progression through the Lead Identification and Lead Optimization phases resulting in the discovery of two bioavailable CCR4 receptor antagonist candidate drugs.

Journal Article Type Article
Journal ACS Medicinal Chemistry Letters
Print ISSN 1948-5875
Electronic ISSN 1948-5875
Publisher American Chemical Society
Peer Reviewed Peer Reviewed
Volume 8
Issue 9
Pages 981–986
APA6 Citation Kindon, N., Andrews, G., Baxter, A., Cheshire, D., Hemsley, P., Johnson, T., …Stocks, M. J. (in press). Discovery of AZD-2098 and AZD-1678, two potent and bioavailable CCR4 receptor antagonists. ACS Medicinal Chemistry Letters, 8(9), 981–986. https://doi.org/10.1021/acsmedchemlett.7b00315
DOI https://doi.org/10.1021/acsmedchemlett.7b00315
Keywords Chemokine receptor 4; MDC; TARC; CCR4; Antagonist
Publisher URL https://doi.org/10.1021/acsmedchemlett.7b00315
Copyright Statement Copyright information regarding this work can be found at the following address: http://eprints.nottingh.../end_user_agreement.pdf
Additional Information This document is the Accepted Manuscript version of a Published Work that appeared in final form in ACS Medicinal Chemistry Letters, copyright © American Chemical Society after peer review and technical editing by the publisher.
To access the final edited and published work see https://doi.org/10.1021/acsmedchemlett.7b00315

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Copyright Statement
Copyright information regarding this work can be found at the following address: http://eprints.nottingham.ac.uk/end_user_agreement.pdf





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