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. These receptors represent the largest class of therapeutic targets representing over 30% of the currently marketed drugs target.


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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, b-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 Deophanization, 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 &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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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
GPCR Allosteric Modulation: Another Shot on Goal Download Poster
More GPCR Posters and presentations View List

 


Blog Articles

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

 


 

Application Notes and Case Studies

PathHunter GPCR Internalization Assays for Monitoring Receptor Endocytosis and Recycling Read Case Study
Discovery of Novel G-Protein or Arrestin-Biased Ligands Using a Suite of GPCR Signaling Platforms Read Application Note
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 Flip Book or 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