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Small molecule antagonists of the CCR2b receptor. Part 2: Discovery process and initial structure-activity relationships of diamine derivatives |
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| Authors: | Moree Wilna J Kataoka Ken-ichiro Ramirez-Weinhouse Michele M Shiota Tatsuki Imai Minoru Sudo Masaki Tsutsumi Takaharu Endo Noriaki Muroga Yumiko Hada Takahiko Tanaka Hiroko Morita Takuya Greene Jonathan Barnum Doug Saunders John Kato Yoshinori Myers Peter L Tarby Christine M |
| Institution: | Deltagen Research Laboratories, 4570 Executive Drive, Suite 400, San Diego, CA 92121, USA. wmoree@neurocrine.com |
| Abstract: | 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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