Literature DB >> 23031591

The discovery of CCR3/H1 dual antagonists with reduced hERG risk.

Ash Bahl1, Patrick Barton, Keith Bowers, Steven Brough, Richard Evans, Christopher A Luckhurst, Tobias Mochel, Matthew W D Perry, Aaron Rigby, Robert J Riley, Hitesh Sanganee, Adam Sisson, Brian Springthorpe.   

Abstract

A series of dual CCR3/H(1) antagonists based on a bispiperidine scaffold were discovered. Introduction of an acidic group overcame hERG liability. Bioavailability was optimised by modulation of physico-chemical properties and physical form to deliver a compound suitable for clinical evaluation.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 23031591     DOI: 10.1016/j.bmcl.2012.08.124

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Early identification of hERG liability in drug discovery programs by automated patch clamp.

Authors:  Timm Danker; Clemens Möller
Journal:  Front Pharmacol       Date:  2014-09-02       Impact factor: 5.810

  1 in total

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