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  • Title: Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity.
    Author: Judd AS, Souers AJ, Wodka D, Zhao G, Mulhern MM, Iyengar RR, Gao J, Lynch JK, Freeman JC, Falls HD, Brodjian S, Dayton BD, Reilly RM, Gintant G, Limberis JT, Mikhail A, Leitza ST, Houseman KA, Diaz G, Bush EN, Shapiro R, Knourek-Segel V, Hernandez LE, Marsh KC, Sham HL, Collins CA, Kym PR.
    Journal: Bioorg Med Chem Lett; 2007 Apr 15; 17(8):2365-71. PubMed ID: 17350253.
    Abstract:
    A series of potent 2-carboxychromone-based melanin-concentrating hormone receptor 1 (MCHr1) antagonists were synthesized and evaluated for hERG (human Ether-a-go-go Related Gene) channel affinity and functional blockade. Basic dialkylamine-terminated analogs were found to weakly bind the hERG channel and provided marked improvement in a functional patch-clamp assay versus previously reported antagonists of the series.
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