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Related Concept Videos

Patch Clamp01:18

Patch Clamp

Many fundamental cell functions such as muscle contraction and nerve transmission rely on the electrical signals produced by the movement of positively and negatively charged ions across the cell membrane. One competent method to record current flowing across the whole cell or single ion channel is the patch-clamp technique.
In this method, a glass micropipette containing electrolyte solution is tightly sealed against a small portion of the cell membrane. As a result, a patch of the cell...
Ion Channels01:19

Ion Channels

The movement of ions like sodium, potassium, and calcium into and out of the cell is essential to maintain the electrochemical gradient in living cells. The ion channels—a class of membrane transport proteins—help maintain this ionic gradient for the smooth functioning of physiological activities such as maintaining cell size and volume, conducting nerve impulses, and gas and nutrient exchange.
Ion channels are specialized integral membrane proteins on the plasma membrane that allow specific...
Non-gated Ion Channels01:24

Non-gated Ion Channels

Ion channels are specialized proteins on the plasma membrane that allow charged ions to pass down their electrochemical gradient. Their main function is to maintain the membrane potential which is critical for cell viability. These channels are either gated or non-gated and can transport more than a thousand ions within milliseconds for the cellular event to occur.
Compared to the gated ion channels, the non-gated channels, also known as leakage or passive channels, have no gating mechanism.
Non-gated Ion Channels01:24

Non-gated Ion Channels

Ion channels are specialized proteins on the plasma membrane that allow charged ions to pass down their electrochemical gradient. Their main function is to maintain the membrane potential which is critical for cell viability. These channels are either gated or non-gated and can transport more than a thousand ions within milliseconds for the cellular event to occur.
Compared to the gated ion channels, the non-gated channels, also known as leakage or passive channels, have no gating mechanism.

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Related Experiment Video

Updated: Jul 2, 2026

Screening Ion Channels in Cancer Cells
06:19

Screening Ion Channels in Cancer Cells

Published on: June 16, 2023

Ion channel screening.

John Dunlop1, Mark Bowlby, Ravikumar Peri

  • 1Neuroscience Discovery Research and Chemical and Screening Sciences, Wyeth Research, CN-8000, Princeton, NJ 08543, USA. Dunlopj@wyeth.com.

Combinatorial Chemistry & High Throughput Screening
|August 13, 2008
PubMed
Summary
This summary is machine-generated.

High-throughput screening methods now enable efficient drug discovery for ion channels, overcoming limitations of traditional assays. Novel cell-based strategies and automated platforms accelerate the identification of potential therapeutics targeting these crucial drug targets.

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Area of Science:

  • Pharmacology and Drug Discovery
  • Molecular Biology
  • Biophysics

Background:

  • Ion channels represent significant targets in drug discovery, with voltage-gated and ligand-gated families being highly represented in pharmaceutical portfolios.
  • Traditional patch-clamp electrophysiology, while the gold standard, suffers from low throughput, limiting its application in large-scale screening.
  • The need for efficient screening methods is critical for advancing drug development for ion channel-related diseases.

Purpose of the Study:

  • To review and discuss available cell-based screening strategies for ion channels.
  • To highlight advancements in high-throughput screening (HTS) for ion channel drug discovery.
  • To present case studies demonstrating the successful implementation of HTS campaigns.

Main Methods:

  • Implementation of multi-well plate format cell-based screening strategies.
  • Utilization of various approaches to monitor ion flux or membrane potential, including radioactive, non-radioactive, spectroscopic, and fluorescence measurements.
  • Development and application of automated electrophysiological platforms.

Main Results:

  • Cell-based screening strategies have significantly improved throughput for ion channel drug discovery.
  • Fluorescent indicators for calcium and membrane potential have enabled successful HTS campaigns.
  • Automated electrophysiology platforms enhance screening capacity while maintaining assay quality.

Conclusions:

  • Modern cell-based screening techniques have overcome historical throughput limitations in ion channel drug discovery.
  • These advanced methods are crucial for both high-throughput screening and lead optimization efforts.
  • Successful HTS campaigns demonstrate the utility of these approaches for identifying novel ion channel modulators.