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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
2-Mercaptoimidazoles, a new class of potent CCR2 antagonists
Guy Van Lomen1, Julien Doyon, Erwin Coesemans
1Inflammation Research, Johnson and Johnson Pharmaceutical Research and Development, Beerse, Belgium. gvlommen@prdbe.jnj.com
Abstract:
We describe the synthesis and SAR of a new class of CCR2 antagonists based on 2-mercaptoimidazole scaffold. The initial lead 1a was optimized to the 3,4-disubstituted analogues 1p-(S) and 1q-(S), which have IC(50) values in the MCP-1 induced Ca-flux below 0.01 microM.
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