GPCR Solutions - DiscoverX -

Applications & Products

GPCR Product Solutions

Always find a GPCR Assay for Your Target of Interest

G-protein coupled receptors (GPCRs) play a crucial role in many physiological functions and in the pathology of multiple diseases including cancer, neuro, endocrine, and metabolic disorders. GPCRs represent the largest class of therapeutic targets with approximately 30% of approved drugs targeting these receptors.

Choose the Solution That Best Meets Your GPCR Program Needs

Whether you are developing small molecule or biologic therapeutic drugs, Eurofins DiscoverX provides you with a variety of drug discovery products with multiple assay types to meet your specific GPCR research needs.

Broad Coverage – >90% targets covered across the human GPCRome to always find an assay for your target of interest
Highly Applicable – Ideal for the development of small molecule and biologic therapeutics, from target ID thru pre-clinical drug discovery programs, providing the most versatile and relevant assays for your specific use
Various Assay Options – 6 assay types (e.g. cAMP, calcium, GTPγS, β-arrestin, internalization, and trafficking) with luminescent or fluorescent read-outs – all offering an array of GPCR assay solutions for maximum flexibility
Largest Collection – >1600 qualified functional and binding assays seen in >800 peer-reviewed publications giving you the most GPCR assays available for the confidence you need

PathHunter® β-Arrestin Assays

Universal Assays for Ligand Bias, Receptor Deorphanization, and Antagonist Discovery

Universal G-protein independent assays to easily quantify GPCR activation based on the recruitment of β-arrestin. Ideal for antagonist mode screening and studying virtually any GPCR including orphan receptors. Multiplex with calcium or cAMP readouts for cost-effective screening and ligand bias analysis.

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ChemiSCREEN™ Membrane Preps

High Quality Membrane Preps for Radioligand Binding and Functional GTPγS Assays

Utilize high-quality membrane preparations to identify ligands that bind your GPCR. Membrane preps are available for saturation and competitive radioligand binding and GTPγS functional studies. Obtain consistent, reproducible results and high total binding values with large signal-to-background ratio.

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cAMP Cell Lines, Frozen Cells, and Kits

Complete assay solutions for monitoring cAMP

Monitor the functional status of GPCRs directly by quantifying cellular cAMP accumulation levels in a dose-dependent manner. Characterize ligand pharmacology with precision. Reproducible performance with large assay windows and broad sensitivity ranges. Simple assays with options for chemiluminescent or fluorescent readout.

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Calcium Cell Lines, Frozen Cells, and Kits

Directly measure calcium flux

Measure intracellular calcium mobilization in cells based on the activation status of GPCRs or ion channels. Cell lines and frozen cells qualified for use with FLIPR® or dye-based assays with fluorescent read-out. Robust and flexible assays with broad sensitivity ranges and large assay windows with protocols for adherent or suspension cells.

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PathHunter GPCR Internalization Assays

Quantitative secondary and orthogonal screening assays for identifying safer drugs

Measure GPCR internalization in live cells with chemiluminescent functional assays as a primary and orthogonal screening tool to help in identifying safer drugs. Quantify internalized GPCRs localized to intracellular endosomes. Monitor your activated GPCR in live cells without expensive microscopy, bulky labels, or antibodies.

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PathHunter Pharmacotrafficking Assays

Simple, Non-Imaging Assays to Identify and Optimize PHarmacochaperones

Identify and characterize small molecule compounds that enter the cell, function as pharmacological chaperones by promoting proper folding, and assist in trafficking to their intended location. Interrogate your compounds’ function in disease processes associated with protein trafficking and internalization due to protein misfolding. Quantitative chemiluminescent results without imaging.

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PathHunter β-Arrestin Parental Cell Lines, eXplorer Kit & Retroparticles

Create Your Own Target-Specific, Stable β-Arrestin Cell-Based Assays

Make your own stable β-arrestin cell lines and EFC cell-based assays for any target in any dividing cell type. Use the assays to analyze the activation and desensitization of GPCRs and regulation of other signaling molecules such as protein kinases that involve β-arrestin recruitment.

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Custom Assay Development Services

Custom Assays and Stable Cell Lines We Can Develop For You

When existing off-the-shelf solutions are not enough, trust Eurofins Discovery to develop a solution that will produce the quality results you expect. These services include custom assays with unique cell backgrounds, orthologs, and mutants as well as creation of custom cellular or biochemical assays for drug discovery, process development, and basic research.

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Knowledge-Based Videos

GPCR Assays: Which ones to use and why for your research and drug discovery and development programs. View Video
Internalization Assays: Identify safer therapeutics with simple, quantitative cell-based assays for measuring receptor internalization. View Video
Pharmacotrafficking Assays: Discover pharmacological chaperones that rescue disease relevant mutant membrane proteins like GPCRs, ion channels and transporters. View Video

Webinars

Archived GPCR Webinar Watch Webinar

Peer Reviewed Publications

GPCR Publications View List
β-Arrestin Publications Download Flyer

Scientific Posters and Presentations

Human GPCRome Poster Download Poster
View more GPCR Posters and Presentations

Blog Articles

Unlocking Orphan GPCRs with an Innovative Forward Trafficking Approach Read Article
Use of Automated Functional, Cell-Based Bioassays Read Article
Uses and Advantages of Membrane Preparations for GPCRs Read Article
Do-It-Yourself: Benefits and Challenges of Creating Your Own Cell-Based Assays Read Article
Why Study GPCR Arrestin Recruitment?  Read Article
Ideal Methods to Study Cellular Transport of Membrane Proteins  Read Article
Ligand Bias: Increasing specificity and Reducing Side Effects of Drug Compounds  Read Article
Four Reasons Why You Should Measure and Quantify Signaling bias in Your Molecules  Read Article

White Papers, Application Notes and Case Studies

Ligand Characterization of Mas-Related GPCR-X2 via Cell-Based Assays: Assessing the Regulation of Mast Cell Function and Implications in Safety Pharmacology Read Application Note
Automating Cell-Based Bioassays on Tecan’s Fluent® Automation Workstation (PathHunter CNR1 Bioassay focus) Read Application Note
Uncover Novel G-Protein or Arrestin-Biased Ligands using a Suite of GPCR Signaling Cell-Based Assays: A Study of Biased Agonism on Opioid Receptors Read Application Note
Quantify GPCR Endocytosis and Recycling with PathHunter GPCR Internalization Assays - Analyzing Therapeutics for Opioid and Cholecystokinin Receptors Read Application Note
White Paper: The New World of GPCR Allosteric Modulation Read Paper
Rapid Quantification of Bioactive Ligands in Serum and Human Plasma Using PathHunter eXpress β-Arrestin GPCR Assays Read Application Note

Brochures and Flyers

GPCR Products List PDF Download

GPCR Reference Guide  PDF Download
PathHunter Build Your Own β-Arrestin Assays  Download Flyer
HitHunter cAMP Assays  Download Flyer
PathHunter Protein Translocation Assays  Download Flyer
Human GPCRome Poster Request