(Q79399910)

English

Early evaluation of compound QT prolongation effects: a predictive 384-well fluorescence polarization binding assay for measuring hERG blockade

scientific article published on 18 October 2006

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scholarly article

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22 December 2019

Early evaluation of compound QT prolongation effects: a predictive 384-well fluorescence polarization binding assay for measuring hERG blockade (English)

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22 December 2019

author name string

Matt Deacon

1

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22 December 2019

David Singleton

2

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Nikki Szalkai

3

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Rodger Pasieczny

4

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Chris Peacock

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David Price

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James Boyd

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Helen Boyd

8

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22 December 2019

Jill V Steidl-Nichols

9

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Christine Williams

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publication date

18 October 2006

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22 December 2019

Journal of Pharmacological and Toxicological Methods

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3

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238-247

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22 December 2019

High throughput fluorescence polarization: a homogeneous alternative to radioligand binding for cell surface receptors

1 reference

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Predictive in silico modeling for hERG channel blockers

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Caco-2 monolayers in experimental and theoretical predictions of drug transport

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Considerations for using fluorescence polarization in the screening of G protein-coupled receptors

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Optimisation and validation of a medium-throughput electrophysiology-based hERG assay using IonWorks HT.

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Development and application of fluorescence polarization assays in drug discovery

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Drug-induced block of cardiac HERG potassium channels and development of torsade de pointes arrhythmias: the case of antipsychotics

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A high-throughput HERG potassium channel function assay: an old assay with a new look

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Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction

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7 January 2021

Validation of a [3H]astemizole binding assay in HEK293 cells expressing HERG K+ channels

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A molecular basis for cardiac arrhythmia: HERG mutations cause long QT syndrome

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7 January 2021

Safety of non-antiarrhythmic drugs that prolong the QT interval or induce torsade de pointes: an overview

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7 January 2021

The [3H]dofetilide binding assay is a predictive screening tool for hERG blockade and proarrhythmia: Comparison of intact cell and membrane preparations and effects of altering [K+]o

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Evaluation of a high-throughput fluorescence assay method for HERG potassium channel inhibition.

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Identifying modulators of hERG channel activity using the PatchXpress planar patch clamp

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The impact of drug-induced QT interval prolongation on drug discovery and development

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[3H]dofetilide binding to HERG transfected membranes: a potential high throughput preclinical screen.

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Fluorescence readouts in HTS: no gain without pain?

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Improved patch-clamp techniques for high-resolution current recording from cells and cell-free membrane patches

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Miniaturization of Fluorescence Polarization Receptor-Binding Assays Using CyDye-Labeled Ligands

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7 January 2021

The potential for QT prolongation and pro-arrhythmia by non-anti-arrhythmic drugs: clinical and regulatory implications. Report on a Policy Conference of the European Society of Cardiology.

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Can the pharmaceutical industry reduce attrition rates?

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Fluorescence polarization and anisotropy in high throughput screening: perspectives and primer

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Understanding the Structure−Activity Relationship of the Human Ether-a-go-go-Related Gene Cardiac K+ Channel. A Model for Bad Behavior

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Determination of equilibrium dissociation constants in fluorescence polarization

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Relationships between preclinical cardiac electrophysiology, clinical QT interval prolongation and torsade de pointes for a broad range of drugs: evidence for a provisional safety margin in drug development

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7 January 2021

A mechanistic link between an inherited and an acquired cardiac arrhythmia: HERG encodes the IKr potassium channel

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Role of Caco-2 cell monolayers in prediction of intestinal drug absorption.

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HERG K+ channels: friend and foe.

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Patch clamping by numbers

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Fluorescence assays for high-throughput screening of protein kinases

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A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays

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High throughput assay technologies for ion channel drug discovery.

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Properties of HERG channels stably expressed in HEK 293 cells studied at physiological temperature

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Identifiers

10.1016/J.VASCN.2006.09.003

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22 December 2019

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22 December 2019

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