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

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

  • Bioorg Med Chem Lett. 2004 Nov 1;14(21):5413-6. doi: 10.1016/j.bmcl.2004.08.009.
Wilna J Moree 1,  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
Affiliations

Affiliation

  • 1 Deltagen Research Laboratories, 4570 Executive Drive, Suite 400, San Diego, CA 92121, USA. wmoree@neurocrine.com
PMID: 15454236 DOI: 10.1016/j.bmcl.2004.08.009
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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