Binding modes of hERG blockers: an unsolved mystery in the drug design arena

Development of Safe Drugs: The hERG Challenge

(2017) Subha Kalyaanamoorthy et al.   MEDICINAL RESEARCH REVIEWS

Towards a Structural View of Drug Binding to hERG K + Channels

(2017) Jamie I. Vandenberg et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Evolution of strategies to improve preclinical cardiac safety testing

(2016) Gary Gintant et al.   NATURE REVIEWS DRUG DISCOVERY

Structure of the voltage-gated K+ channel Eag1 reveals an alternative voltage sensing mechanism

(2016) J. R. Whicher et al.   SCIENCE

New potential binding determinant for hERG channel inhibitors

(2016) P. Saxena et al.   Scientific Reports

The Comprehensive in Vitro Proarrhythmia Assay (CiPA) initiative — Update on progress

(2016) Thomas Colatsky et al.   JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS

Computational investigations of hERG channel blockers: New insights and current predictive models

(2015) Bruno O. Villoutreix et al.   ADVANCED DRUG DELIVERY REVIEWS

A human ether-á-go-go-related (hERG) ion channel atomistic model generated by long supercomputer molecular dynamics simulations and its use in predicting drug cardiotoxicity

(2014) Anwar Anwar-Mohamed et al.   TOXICOLOGY LETTERS

Reducing safety-related drug attrition: the use of in vitro pharmacological profiling

(2012) Joanne Bowes et al.   NATURE REVIEWS DRUG DISCOVERY

hERG K+ Channels: Structure, Function, and Clinical Significance

(2012) Jamie I. Vandenberg et al.   PHYSIOLOGICAL REVIEWS

How can we improve our understanding of cardiovascular safety liabilities to develop safer medicines?

(2011) HG Laverty et al.   BRITISH JOURNAL OF PHARMACOLOGY

Insights into the Molecular Mechanism of hERG1 Channel Activation and Blockade by Drugs

(2010) S. Durdagi et al.   CURRENT MEDICINAL CHEMISTRY

Drug Binding to the Inactivated State Is Necessary but Not Sufficient for High-Affinity Binding to Human Ether-a-go-go-Related Gene Channels

(2008) M. J. Perrin et al.   MOLECULAR PHARMACOLOGY