Kv11.1 (hERG) Assay(s)

Background Information

Kv11.1, also known as hERG (human Ether-à-go-go Related Gene), is predominantly expressed in cardiac myocytes and the central nervous system, where it is essential for repolarizing the cardiac action potential and regulating neuronal excitability. Dysfunction or pharmacological inhibition of hERG channels leads to delayed cardiac repolarization, manifesting as drug-induced long QT syndrome—a potentially fatal arrhythmia of major concern in drug development. Because of this, regulatory agencies including the FDA mandate routine screening of new drug candidates for Kv11.1 inhibition.

Family: Ion Channel
Protein Name: Kv11.1 (hERG)
Gene Name: KCNH2

Organism : Human
Therapeutic Area: Cardiotoxicity

Assay Information

Validated Assay(s): Thallium-free GIRK Potassium Channel Assay, Brilliant Thallium Assay, Brilliant Thallium Snapshot Assay
Assay type: Cell-based
Method: Fluorescence

Instrumentation: FLIPR, Panoptic, Flexstation
Plate Format: 96- or 384-well
Expression: Stable
Cell type: CHO, HEK293T

Testing Information

Functional Mode(s): Inhibitor
Reference compound(s): Terfenadine

Dose response curve for a hERG channel inhibition assay using a thallium-free potassium channel assay and the inhibitor, terfenadine.

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