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GPCR Reporter Cells
G protein-coupled receptors (GPCRs) regulate critical physiological processes and are key targets in drug discovery for conditions such as metabolic disorders, cardiovascular diseases, neurological disorders, and oncology. Through genetic engineering, we have developed over 100 off-the-shelf GPCR stable cell lines that express target receptors and downstream signaling components, enabling functional assays including calcium flux, cAMP accumulation, and β-arrestin recruitment. These validated cell models are ready for high-throughput screening and QC lot release to support GPCR drug development programs.
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Case Study
Figure 1. HTRF cAMP assay in ADORA2A Gα15 CHO-K1 (C1) cells
The left curve shows Imaradenant-mediated dose-dependent inhibition of NECA-induced cAMP response with IC50 = 37.4 nM. The right curve shows Ciforadenant-mediated dose-dependent inhibition with IC50 = 23.9 nM. The data demonstrate potent antagonist activity of both compounds at ADORA2A receptor, suitable for HTS and functional testing.
Figure 2. HTRF cAMP assay in ADORA2A Gα15 CHO-K1 (C1) cells
The left curve shows NECA induced a dose-dependent response with EC50 = 11 nM. The right curve shows Adenosine induced a dose-dependent response with EC50 = 250 nM. The data confirm functional ADORA2A receptor activity, supporting compound screening and receptor functional characterization.