Functional GPCR assays reveal more. GPCRProfiler services showed that Oxymetazoline, a nasal decongestant, exhibited full agonist, partial agonist, or antagonist activity depending on the specific GPCR receptor examined.
GPCRProfiler is the first complete cell-based functional platform that uses a common validated readout for over 155 GPCRs. The foundation of GPCRProfiler is our ChemiScreen GPCR stable cell lines that are used for real-time calcium flux assays to rapidly, reliably and reproducibly screen and profile compounds. Using one platform allows ligands to be screened with identical buffer conditions and incubation times for the entire spectrum of GPCRs for easy analysis and comparison.
Our unbiased profiling screens can determine if drugs are full or partial agonists or antagonists. We also perform dose-response assays to determine EC50 values for agonists and IC50 values for antagonists.
GPCRProfiler gives you the flexibility to choose from 1 to ≥155 different receptors to screen. Or, choose between 15 different service panels, including more than 60 distinct ligand families, 2 safety panels and 11 disease-focused panels.
GPCRProfiler Service Highlights:
- Cell-based functional assays for more than 155 GPCRs, covering more than 60 different ligand families, including chemokine, lysophospholipid and biogenic amines
- Dual-mode screening (agonist and antagonist) in a single well means you won’t miss the functionality of analogs at the directed target or off-target receptors
- 96- or 384-plate FLIPR™ assays with fully integrated and automated compound and plate handling
- GPCRProfiler disease and safety panels help direct your projects
- Quick turnaround times of 1-3 weeks depending on project types
- Visualization of both agonist and antagonist activity from a large profiling dataset with our web-based DART tool
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