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  • Title: Bicyclo[3.1.0]hexyl urea melanin concentrating hormone (MCH) receptor-1 antagonists: impacting hERG liability via aryl modifications.
    Author: McBriar MD, Guzik H, Shapiro S, Xu R, Paruchova J, Clader JW, O'neill K, Hawes B, Sorota S, Margulis M, Tucker K, Weston DJ, Cox K.
    Journal: Bioorg Med Chem Lett; 2006 Aug 15; 16(16):4262-5. PubMed ID: 16753297.
    Abstract:
    Herein, we report the discovery of an effective strategy to modulate liabilities related to affinity of previously disclosed bicyclohexane MCHR-1 antagonists for the hERG channel. This paper describes one of several strategies incorporated to limit hERG binding via modifications of a terminal aryl group in an otherwise promising bicyclohexyl urea series.
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