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Potent antagonists of the CCR2b receptor. Part 3: SAR of the (R)-3-aminopyrrolidine series |
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| Authors: | Moree Wilna J Kataoka Ken-ichiro Ramirez-Weinhouse Michele M Shiota Tatsuki Imai Minoru Tsutsumi Takaharu Sudo Masaki Endo Noriaki Muroga Yumiko Hada Takahiko Fanning Dewey Saunders John Kato Yoshinori Myers Peter L Tarby Christine M |
| Institution: | Deltagen Research Laboratories (Former CombiChem, Inc.), 4570 Executive Drive, San Diego, CA 92121, USA. wmoree@neurocrine.com |
| Abstract: | SAR studies were conducted around lead compound 1 using high-throughput parallel solution and solid phase synthesis. Our lead optimization efforts led to the identification of several CCR2b antagonists with potent activity in both binding and functional assays Compound 71 CCR2b Binding IC(50) 3.2 nM; MCP-1-Induced Chemotaxis IC(50) 0.83 nM; Ca(2+) Flux IC(50) 7.5 nM]. |
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