High throughput screening technologies for ion channels

Development and Validation of a Thallium Flux-Based Functional Assay for the Sodium Channel NaV1.7 and Its Utility for Lead Discovery and Compound Profiling

(2015) Yu Du et al.   ACS Chemical Neuroscience

Alternative Paradigms for Ion Channelopathies: Disorders of Ion Channel Membrane Trafficking and Posttranslational Modification

(2015) Jerry Curran et al.   Annual Review of Physiology

Four basic residues critical for the ion selectivity and pore blocker sensitivity of TMEM16A calcium-activated chloride channels

(2015) Christian J. Peters et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Potent and selective inhibitors of the TASK-1 potassium channel through chemical optimization of a bis-amide scaffold

(2014) Daniel P. Flaherty et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of novel small molecule modulators of K2P18.1 two-pore potassium channel

(2014) J. Kyle Bruner et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

ANG-2 for quantitative Na+ determination in living cells by time-resolved fluorescence microscopy

(2014) Phillip Roder et al.   PHOTOCHEMICAL & PHOTOBIOLOGICAL SCIENCES

Development and Validation of Fluorescence-Based and Automated Patch Clamp–Based Functional Assays for the Inward Rectifier Potassium Channel Kir4.1

(2013) Rene Raphemot et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

Yellow Fluorescent Protein-Based Assay to Measure GABAA Channel Activation and Allosteric Modulation in CHO-K1 Cells

(2013) Teres Johansson et al.   PLoS One

A High-Throughput Screening Campaign for Detection of Ca2+–Activated K+ Channel Activators and Inhibitors Using a Fluorometric Imaging Plate Reader–Based Tl+-Influx Assay

(2012) Susanne Jørgensen et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

A novel series of benzimidazole NR2B-selective NMDA receptor antagonists

(2012) David J. Davies et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective Kv7.1 (KCNQ1) potassium channel activator

(2012) Margrith E. Mattmann et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of a Series of 2-Phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as Novel Molecular Switches that Modulate Modes of Kv7.2 (KCNQ2) Channel Pharmacology: Identification of (S)-2-Phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide (ML252) as a Potent, Brain Penetrant Kv7.2 Channel Inhibitor

(2012) Yiu-Yin Cheung et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

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

Modulation of hERG potassium channel gating normalizes action potential duration prolonged by dysfunctional KCNQ1 potassium channel

(2012) H. Zhang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Screening quality for Ca2+-activated potassium channel in IonWorks Quattro is greatly improved by using BAPTA-AM and ionomycin

(2012) Katsutoshi Ido et al.   JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS

Development of a high-throughput electrophysiological assay for the human ether-à-go-go related potassium channel hERG

(2012) Daniel J. Gillie et al.   JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS

Selective Inhibition of the Kir2 Family of Inward Rectifier Potassium Channels by a Small Molecule Probe: The Discovery, SAR, and Pharmacological Characterization of ML133

(2011) Hao-Ran Wang et al.   ACS Chemical Biology

Discovery, Synthesis, and Structure–Activity Relationship of a Series of N-Aryl-bicyclo[2.2.1]heptane-2-carboxamides: Characterization of ML213 as a Novel KCNQ2 and KCNQ4 Potassium Channel Opener

(2011) Haibo Yu et al.   ACS Chemical Neuroscience

hERGCentral: A Large Database to Store, Retrieve, and Analyze Compound-Human Ether-à-go-go Related Gene Channel Interactions to Facilitate Cardiotoxicity Assessment in Drug Development

(2011) Fang Du et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

Validation of a Patch Clamp Screening Protocol That Simultaneously Measures Compound Activity in Multiple States of the Voltage-Gated Sodium Channel Nav1.2

(2011) Yi Liu et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

Small-molecule activators of TMEM16A, a calcium-activated chloride channel, stimulate epithelial chloride secretion and intestinal contraction

(2011) Wan Namkung et al.   FASEB JOURNAL

Identification of ML204, a Novel Potent Antagonist That Selectively Modulates Native TRPC4/C5 Ion Channels

(2011) Melissa Miller et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Development and Validation of a Secondary Screening Assay for TRPM8 Antagonists Using QPatch HT

(2010) Edward J. Beck et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

Comparison of Human Ether-à-go-go Related Gene Screening Assays Based on IonWorks Quattro and Thallium Flux

(2010) Terry R. Bridal et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

Optimization of a Yellow Fluorescent Protein-Based Iodide Influx High-Throughput Screening Assay for Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Modulators

(2010) Jinliang Sui et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

Identification of Human Ether-à-go-go Related Gene Modulators by Three Screening Platforms in an Academic Drug-Discovery Setting

(2010) Xi-Ping Huang et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

Profiling Diverse Compounds by Flux- and Electrophysiology-Based Primary Screens for Inhibition of Human Ether-à-go-go Related Gene Potassium Channels

(2010) Beiyan Zou et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

Inhibition of Ca2+-activated Cl− channels by gallotannins as a possible molecular basis for health benefits of red wine and green tea

(2010) Wan Namkung et al.   FASEB JOURNAL

Screening technologies for ion channel drug discovery

(2010) Georg C Terstappen et al.   Future Medicinal Chemistry

TMEM16A Inhibitors Reveal TMEM16A as a Minor Component of Calcium-activated Chloride Channel Conductance in Airway and Intestinal Epithelial Cells

(2010) Wan Namkung et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Identification and Characterization of Novel NMDA Receptor Antagonists Selective for NR2A- over NR2B-Containing Receptors

(2010) E. Bettini et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Neurological channelopathies: new insights into disease mechanisms and ion channel function

(2010) Dimitri M. Kullmann et al.   JOURNAL OF PHYSIOLOGY-LONDON

A new homogeneous high-throughput screening assay for profiling compound activity on the human ether-a-go-go-related gene channel

(2009) Steven A. Titus et al.   ANALYTICAL BIOCHEMISTRY

An Ion Channel Library for Drug Discovery and Safety Screening on Automated Platforms

(2009) Barbara A. Wible et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

A Fluorescence-Based High-Throughput Screening Assay for the Identification of T-Type Calcium Channel Blockers

(2009) Francesco Belardetti et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

Sodium Channel Inhibitor Drug Discovery Using Automated High Throughput Electrophysiology Platforms

(2009) Neil Castle et al.   COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING

Robotic multiwell planar patch-clamp for native and primary mammalian cells

(2009) Carol J Milligan et al.   Nature Protocols

Antibacterial activity of six novel peptides from Tityus discrepans scorpion venom. A fluorescent probe study of microbial membrane Na+ permeability changes

(2009) Patricia Díaz et al.   TOXICON

A High-Throughput Assay for Evaluating State Dependence and Subtype Selectivity of Cav2 Calcium Channel Inhibitors

(2008) Ge Dai et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

Fluorescent Probes for Cellular Assays

(2008) George Hanson et al.   COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING

Chemical calcium indicators

(2008) R. Madelaine Paredes et al.   METHODS

Cellular HTS Assays for Pharmacological Characterization of NaV1.7 Modulators

(2007) Shephali Trivedi et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

Novel pharmacological activity of loperamide and CP-339,818 on human HCN channels characterized with an automated electrophysiology assay

(2007) Yan T. Lee et al.   EUROPEAN JOURNAL OF PHARMACOLOGY