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Discovery of AZD-2098 and AZD-1678, Two Potent and Bioavailable CCR4 Receptor Antagonists

Nicholas Kindon, 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, etc.

ACS Med Chem Lett. 2017 Sep 1;8(9):981-986.

PMID: 28947948

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 subset 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.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP566203881 AZD-2098 AZD-2098 566203-88-1 Price
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