| Literature DB >> 22683222 |
Daniel D Long1, Scott R Armstrong, David T Beattie, Seok-Ki Choi, Paul R Fatheree, Roland A L Gendron, Adam A Goldblum, Patrick P Humphrey, Daniel G Marquess, Jeng-Pyng Shaw, Jacqueline A M Smith, S Derek Turner, Ross G Vickery.
Abstract
Further application of our multivalent approach to drug discovery directed to 5-HT(4) receptor agonists is described. Optimization of the linker and secondary binding amine in the indazole-tropane primary binding group series, for binding affinity and functional potency at the 5-HT(4) receptor, selectivity over the 5-HT(3) receptor, oral pharmacokinetics, and in vivo efficacy in models of GI motility, resulted in the identification of clinical compound TD-2749.Entities:
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Year: 2012 PMID： 22683222 DOI： 10.1016/j.bmcl.2012.05.034
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823