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Bioorg Med Chem Lett. 2010 Oct 15;20(20):6108-15. doi: 10.1016/j.bmcl.2010.08.039. Epub 2010 Aug 12.

Thienopyrimidines as β3-adrenoceptor agonists: hit-to-lead optimization.

Author information

1
4SC AG, Am Klopferspitz 19a, 82152 Planegg-Martinsried, Germany. stefan.tasler@4sc.com

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.

PMID:
20833036
DOI:
10.1016/j.bmcl.2010.08.039
[Indexed for MEDLINE]

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