Referenced in: none

Automatically associated channels: Kv11.1

Title: Bicyclo[3.1.0]hexyl urea melanin concentrating hormone (MCH) receptor-1 antagonists: impacting hERG liability via aryl modifications.

Authors: Mark D McBriar, Henry Guzik, Sherry Shapiro, Ruo Xu, Jaroslava Paruchova, John W Clader, Kim O'neill, Brian Hawes, Steve Sorota, Michael Margulis, Kristal Tucker, Daniel J Weston, Kathleen Cox

Journal, date & volume: Bioorg. Med. Chem. Lett., 2006 Aug 15 , 16, 4262-5

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/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.