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

Kindon, Nicholas and Andrews, Glen and Baxter, Andrew and Cheshire, David and Hemsley, Paul and Johnson, Timothy and Liu, Yu-Zhen and McGinnity, Dermot and McHale, Mark and Mete, Antonio and Reuberson, James and Roberts, Bryan and Steele, John and Teobald, Barry and Unitt, John and Vaughan, Deborah and Walters, Iain and Stocks, Michael J. (2017) Discovery of AZD-2098 and AZD-1678, two potent and bioavailable CCR4 receptor antagonists. ACS Medicinal Chemistry Letters . ISSN 1948-5875

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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.

Item Type: Article
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
Keywords: Chemokine receptor 4; MDC; TARC; CCR4; Antagonist
Schools/Departments: University of Nottingham, UK > Faculty of Science > School of Pharmacy
Identification Number:
Depositing User: Eprints, Support
Date Deposited: 08 Sep 2017 11:45
Last Modified: 04 May 2020 19:03

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