Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 6, Pages 1869-1873Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.02.015
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SAR studies were conducted around lead compound 1 using high-throughput parallel solution and solid phase synthesis. Our lead optimization efforts led to the identification of several CCR2b antagonists with potent activity in both binding and functional assays [Compound 71 CCR2b Binding IC50 3.2 nM; MCP-1-Induced Chemotaxis IC50 0.83 nM; Ca2+ Flux IC50 7.5 nM]. (C) 2008 Elsevier Ltd. All rights reserved.
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