4.5 Article

Small molecule antagonists of the CCR2b receptor. Part 2: Discovery process and initial structure-activity relationships of diamine derivatives

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 14, Issue 21, Pages 5413-5416

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2004.08.009

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Structure-activity relationships (SAR) of a weakly active class of CCR2b inhibitors were utilized to initiate a ead evolution program employing the Drug Discovery Engine(TM). Several alternative structural series have been discovered that display nanomolar activity in the CCR2b binding and CCR2b-mediated chemotaxis assays. (C) 2004 Elsevier Ltd. All rights reserved.

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