| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1378487 | Bioorganic & Medicinal Chemistry Letters | 2007 | 4 Pages |
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 μM.
Graphical abstractA direct correlation between hERG binding and QTc prolongation was established for this series of aminomethyl tetrahydronaphthalene ketopiperazine MCH-R1 antagonists.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
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,