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 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.

 

PathHunter GPCR Internalization Assays


 

Quantitative secondary and orthogonal screening assays for identifying safer drugs


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PathHunter Pharmacotrafficking Assays


 

Simple assays to identify and optimize pharmacochaperone and study GPCR trafficking to the membrane or endosome.

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PathHunter Parental Cell Lines & Vectors


 

Easily build your own GPCR assays

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Custom Assay Development Services


 

Assay development solutions tailored to your needs


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Webinars

Application of β-Arrestin Assays to the Orphan GPCR World  Watch Webinar
Discovery of Bacterial Effectors in the Human Microbiome and Isolation of a GPCR G2A/GPR132 Agonist  Watch Webinar
From Chemistry to Clinic: Discovery of Biased Apelin Receptor Agonists and Action in the Cardiovascular System  Watch Webinar
Mu Opioid Receptor Splicing and Signaling: Another Dimension of GPCR Function  Watch Webinar
Unlocking GPCRs for Oncology  Watch Webinar
Duplexed Screening of GPCRs to Measure Calcium and β-Arrestin  Watch Webinar
Understand Safety and Selectivity of Drug Candidates Before Expensive Animal Studies  Watch Webinar
Make Your Own Cell-Based Assays to Study β-Arrestin Recruitment Watch Webinar
More GPCR Webinars
 

Peer Reviewed Publications

GPCR Publications  View List
β-Arrestin Publications  Download Flyer
 

Scientific Posters and Presentations

Human GPCRome Poster Download Poster
Differentiated Receptor Pharmacology of Imipridone ONC201: The First DRD2 Antagonist in Clinical Development for Oncology  Download Poster
Interrogating Allosteric Interactions Using Multiple Readouts for GPCRs Download Poster
A Duplexed Calcium and β-Arrestin Assay Protocol for Human Histamine H1 Receptor PathHunter CHO-K1 HRH1 β-Arrestin Cell Line Download Poster
Novel Trafficking Assays for Pharmacochaperone Discovery Using Enzyme Fragment Complementation Applied to CFTR-ΔF508 Download Poster
 

Blog Articles

Do-It-Yourself: Benefits and Challenges of Creating Your Own Cell-Based Assays  Read Article
The Mast Cell Receptor Mrgx2 and Drug-Induced Anaphylaxis  Read Article
Unlocking GPCRs for Oncology  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
Accelerating GPCR Drug Discovery and Development  Download Brochure
PathHunter Build Your Own β-Arrestin Assays  Download Flyer
HitHunter cAMP Assays  Download Flyer
PathHunter Protein Translocation Assays  Download Flyer
Human GPCRome Poster Request
 

Custom Assay Development Services

Can't find your assay on the menu? We can develop it for you. Learn More
 

Technical Bulletins

Updated Cell Culture and Handling Procedure. Read Protocol