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  • Title: Reduction of hERG inhibitory activity in the 4-piperidinyl urea series of H3 antagonists.
    Author: Berlin M, Lee YJ, Boyce CW, Wang Y, Aslanian R, McCormick KD, Sorota S, Williams SM, West RE, Korfmacher W.
    Journal: Bioorg Med Chem Lett; 2010 Apr 01; 20(7):2359-64. PubMed ID: 20188550.
    Abstract:
    Structural features of the substituted 4-piperidinyl urea analogs 1, responsible for the H3 antagonist activity, have been identified. Structure-activity relationship of the H3 receptor affinity, hERG ion channel inhibitory activity and their separation is described. Preliminary pharmacokinetic evaluation of the compounds of the series is addressed.
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