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Title
Development of Safe Drugs: The hERG Challenge
Authors
Keywords
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Journal
MEDICINAL RESEARCH REVIEWS
Volume 38, Issue 2, Pages 525-555
Publisher
Wiley
Online
2017-05-04
DOI
10.1002/med.21445
References
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- (2016) Hai-bo Yu et al. ACTA PHARMACOLOGICA SINICA
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- (2016) Patric Schyman et al. Journal of Chemical Information and Modeling
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- (2016) Lin Tang et al. NATURE
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- (2016) Kelly Servick SCIENCE
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- (2016) J. R. Whicher et al. SCIENCE
- Individual Ion Binding Sites in the K + Channel Play Distinct Roles in C-type Inactivation and in Recovery from Inactivation
- (2016) Kimberly Matulef et al. STRUCTURE
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- (2016) P. Saxena et al. Scientific Reports
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- (2016) Yan Li et al. Scientific Reports
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- (2015) Hai-bo Yu et al. ACTA PHARMACOLOGICA SINICA
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- (2015) Bruno O. Villoutreix et al. ADVANCED DRUG DELIVERY REVIEWS
- Sequence of Gating Charge Movement and Pore Gating in hERG Activation and Deactivation Pathways
- (2015) Samuel J. Goodchild et al. BIOPHYSICAL JOURNAL
- In silico prediction of hERG inhibition
- (2015) Yankang Jing et al. Future Medicinal Chemistry
- An analysis of the attrition of drug candidates from four major pharmaceutical companies
- (2015) Michael J. Waring et al. NATURE REVIEWS DRUG DISCOVERY
- Tuning hERG Out: Antitarget QSAR Models for Drug Development
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- (2014) Anwar Anwar-Mohamed et al. TOXICOLOGY LETTERS
- An NMR investigation of the structure, function and role of the hERG channel selectivity filter in the long QT syndrome
- (2013) Andrée E. Gravel et al. BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES
- Role of the activation gate in determining the extracellular potassium dependency of block of HERG by trapped drugs
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- Gating charge movement precedes ionic current activation in hERG channels
- (2013) Samuel J Goodchild et al. Channels
- A fingerprint pair analysis of hERG inhibition data
- (2013) Clayton Springer et al. Chemistry Central Journal
- Recent Developments in Computational Prediction of hERG Blockage
- (2013) Sichao Wang et al. CURRENT TOPICS IN MEDICINAL CHEMISTRY
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- Strategies To Reduce hERG K+ Channel Blockade. Exploring Heteroaromaticity and Rigidity in Novel Pyridine Analogues of Dofetilide
- (2013) João F. S. Carvalho et al. JOURNAL OF MEDICINAL CHEMISTRY
- Structural Properties of PAS Domains from the KCNH Potassium Channels
- (2013) Ricardo Adaixo et al. PLoS One
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- (2010) Zeineb Es-Salah-Lamoureux et al. PLoS One
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- Side Chain Flexibilities in the Human Ether-a-go-go Related Gene Potassium Channel (hERG) Together with Matched-Pair Binding Studies Suggest a New Binding Mode for Channel Blockers
- (2009) Ulrich Zachariae et al. JOURNAL OF MEDICINAL CHEMISTRY
- Docking Model of Drug Binding to the Human Ether-à-go-go Potassium Channel Guided by Tandem Dimer Mutant Patch-Clamp Data: A Synergic Approach
- (2009) Yumi N. Imai et al. JOURNAL OF MEDICINAL CHEMISTRY
- Challenges Predicting Ligand-Receptor Interactions of Promiscuous Proteins: The Nuclear Receptor PXR
- (2009) Sean Ekins et al. PLoS Computational Biology
- Ligand Structural Aspects of hERG Channel Blockade
- (2008) Alex Aronov CURRENT TOPICS IN MEDICINAL CHEMISTRY
- The Impact of IKr Blockade on Medicinal Chemistry Programs
- (2008) Ian Bell et al. CURRENT TOPICS IN MEDICINAL CHEMISTRY
- Topological Mapping of the Asymmetric Drug Binding to the Human Ether-a-go-go-Related Gene Product (HERG) Potassium Channel by Use of Tandem Dimers
- (2008) T. Myokai et al. MOLECULAR PHARMACOLOGY
- 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
- A Composite Model for hERG Blockade
- (2007) Christian Kramer et al. ChemMedChem
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