| Literature DB >> 20833036 |
Stefan Tasler1, Roland Baumgartner, Astrid Ammendola, Josef Schachtner, Tanja Wieber, Marcus Blisse, Sandra Rath, Mirko Zaja, Philipp Klahn, Udo Quotschalla, Peter Ney.
Abstract
Resulting from a vHTS based on a pharmacophore alignment on known β3-adrenoceptor ligands, an aryloxypropanolamine scaffold comprising a thienopyrimidine moiety was further optimized as a human β3-AR agonist, yielding a lead compound with an excellent cellular activity of EC(50)=20 pM, selectivity over hβ1- and hβ2-adrenoceptors and a promising safety profile.Entities:
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Year: 2010 PMID： 20833036 DOI： 10.1016/j.bmcl.2010.08.039
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823