4.5 Article

Identification of novel series of human CCR1 antagonists

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 6, Pages 2215-2221

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.09.068

Keywords

chemokine receptor 1; CCR1 antagonist

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A hit-to-lead optimization process was carried out on the high throughput screening hit compound 1 resulting in the identification of several potent and selective CCR1 receptor antagonists. Compound 37 shows the best overall profile with IC50 values of < 100 nM in binding and functional assays. (C) 2008 Published by Elsevier Ltd.

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