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  3. Ion Channel Screening

Ion Channel Screening

Ion channels are integral membrane proteins that catalyze the flux of ions across cell membranes, and play fundamental roles in a wide variety of functions include maintaining a resting membrane potential, conducting action potentials and other electrical signals. The malfunction of ion channels causes a variety of human diseases.

Therefore, ion channels represent a class of attractive drug targets and a class of important off-targets for in vitro pharmacological profiling. In addition, ion channels are also critically important in evaluating drug safety. Many drugs withdrawn from the market due to cardiac-related adverse effects have been shown to block the human ether-a-go-go (hERG) ion channel, which delays repolarization of the cardiac action potential.

hERG Channel Block Action Potential Prolonged QT Interval Torsades de Pointes

Screening Process

Patch clamp electrophysiology is the gold standard for ion channel studies. High-throughput identification of compound ion channel efficacy, potency, specificity, or potential for off-target effects is a critical step in early drug discovery. MedChemExpress offers high-throughput fluorescence-based assays, automated patch clamp electrophysiology assays as well as manual patch assays to identify the most promising candidates.

Advantages

The broad range of platforms for different throughputs: including Qpatch 16X, Qpatch HTX, IonWorks Barracuda, FDSS/μCell, and conventional manual patch clamp electrophysiology

A long list of ion channel assay models: chloride channel, potassium channel, sodium channel, calcium channel models with efficient signal read-out and good stability

Manual patch clamp: Gold standard for detailed characterization

One-stop shopping: 6,000,000+ available, lead-like compounds

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