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Pubmed for Handhelds

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  • Title: From astemizole to a novel hit series of small-molecule somatostatin 5 receptor antagonists via GPCR affinity profiling.
    Author: Guba W, Green LG, Martin RE, Roche O, Kratochwil N, Mauser H, Bissantz C, Christ A, Stahl M.
    Journal: J Med Chem; 2007 Dec 13; 50(25):6295-8. PubMed ID: 18020391.
    Abstract:
    The H1R antagonist astemizole was identified as a somatostatin 5 (SST5) receptor antagonist by a comparative sequence analysis of the consensus drug binding pocket of GPCRs. Subsequently, a similarity analysis of GPCR affinity profiles of astemizole versus a set of in-house GPCR-biased combinatorial libraries revealed new chemical entry points that led to a second lead series with nanomolar binding affinity.
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