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Updated: Aug 21, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
Racemic and chiral lactams as potent, selective and functionally active CCR4 antagonists
Bradley Newhouse1, Shelley Allen, Benjamin Fauber
1Array BioPharma, 3200 Walnut Street, Boulder, CO 80301, USA.
Abstract:
A series of racemic and chiral, nonracemic lactams that display high binding affinities, functional chemotaxis antagonism, and selectivity toward CCR4 are described. Compound 41, which provides reasonably high blood levels in mice when dosed intraperitoneally, was identified as a useful pharmacological tool to explore the role of CCR4 antagonism in animal models of allergic disease.
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