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ID: ALA3751831
Journal: Bioorg Med Chem Lett
Title: Discovery and synthesis of cyclohexenyl derivatives as modulators of CC chemokine receptor 2 activity.
Authors: Brown GD, Shi Q, Delucca GV, Batt DG, Galella MA, Cvijic ME, Liu RQ, Qiu F, Zhao Q, Barrish JC, Carter PH.
Abstract: A novel cyclohexenyl series of CCR2 antagonists has been discovered. This series of small, rigid compounds exhibits submicromolar binding affinity for CCR2. Modification of the substituents on the cyclohexene ring led to the identification of potent CCR2 antagonists. Progress from initial lead 5 (IC50=700nM) to (-)-38 (IC50=9.0nM) is discussed.
CiteXplore: 26631321