Referenced in: none

Automatically associated channels: Kv11.1

Title: Aminomethyl tetrahydronaphthalene ketopiperazine MCH-R1 antagonists--Increasing selectivity over hERG.

Authors: Kenneth M Meyers, José L Méndez-Andino, Anny-Odile Colson, Namal C Warshakoon, John A Wos, Maria C Mitchell, Karen M Hodge, Jeremy M Howard, David C Ackley, Jerry K Holbert, Scott W Mittelstadt, Martin E Dowty, Cindy M Obringer, Ofer Reizes, X Eric Hu

Journal, date & volume: Bioorg. Med. Chem. Lett., 2007 Feb 1 , 17, 819-22

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/17107796

Abstract
A direct correlation between hERG binding and QTc prolongation was established for a series of aminomethyl tetrahydronaphthalene ketopiperazine MCH-R1 antagonists. Compounds within this class with greater selectivity over hERG were developed. Compound 4h proved to have the best profile, with MCH-R1 Ki = 16 nm and hERG IC50 = 25 microM.