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

Wilna J Moree Ken-ichiro Kataoka Michele M Ramirez-Weinhouse Tatsuki Shiota Minoru Imai Masaki Sudo Takaharu Tsutsumi Noriaki Endo Yumiko Muroga Takahiko Hada Hiroko Tanaka Takuya Morita Jonathan Greene Doug Barnum John Saunders Yoshinori Kato Peter L Myers Christine M Tarby

Bioorg Med Chem Lett

Deltagen Research Laboratories, 4570 Executive Drive, Suite 400, San Diego, CA 92121, USA.

Published: November 2004

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

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http://dx.doi.org/10.1016/j.bmcl.2004.08.009DOI Listing

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