Discovery of disubstituted cyclohexanes as a new class of CC chemokine receptor 2 antagonists

…, YC Lo, G Yang, PA Scherle, S Mandlekar…

Index: Wacker, Dean A; Santella 3rd., Joseph B; Gardner, Daniel S; Varnes, Jeffrey G; Estrella, Melissa; DeLucca, George V; Ko, Soo S; Tanabe, Keiichi; Watson, Paul S; Welch, Patricia K; Covington, Maryanne; Stowell, Nicole C; Wadman, Eric A; Davies, Paul; Solomon, Kimberly A; Newton, Robert C; Trainor, George L; Friedman, Steven M; Decicco, Carl P; Duncia, John V Bioorganic and medicinal chemistry letters, 2002 , vol. 12, # 13 p. 1785 - 1789

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Citation Number: 40

Abstract

... by binding to its receptor, CC chemokine receptor 2 (CCR2), which is a member of the G-protein coupled ... 2,4-dimethyl substitution pattern was met with some difficulty, as the addition of a third methyl to ... cmpd, R, X, R 1, CCR2 binding IC 50 a (μM), CCR3 binding % inh at 10 μM b. ...