P2Y2 Assay(s)

Background Information

Gq/G11-coupled purinergic receptor activated by extracellular ATP and UTP. Expressed on airway epithelium and immune cells; P2Y2 activation drives Cl⁻ secretion and mucociliary clearance. Diquafosol, a P2Y2/P2Y4 agonist, is approved in Japan for dry eye disease. Denufosol, a selective P2Y2 agonist developed for cystic fibrosis airway hydration, failed to meet its Phase 3 primary endpoint in 2011.

Family: GPCR
Protein Name: P2Y2 Receptor (Endogenous)
Gene Name: P2RY2

Organism: Human
Therapeutic Area: Respiratory, Immunology

Assay Information

Validated Assay(s): Calcium Assay
Assay type: Cell-based
Method: Fluorescence

Instrumentation: FLIPR
Plate Format: 384-well
Expression: Endogenous
Cell type: CHO-K1

Testing Information

Functional Mode(s): Agonist, Antagonist
Reference compound(s): ATP

ATP concentration-response curve for the human P2Y2 receptor in a Brilliant Calcium fluorescence assay using CHO-K1 cells.
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