Applications & Products / GPCR Solutions

GPCR Solutions

Your Source for a Complete Offering of GPCR Products and Services

G-protein coupled receptors (GPCRs) play a crucial role in many physiological functions and in the pathology of multiple diseases including cancer, endocrine, and metabolic disorders. These receptors represent the largest class of therapeutic targets. Over 30% of currently marketed drugs target these receptors, while GPCRs continue to be the focus of many active drug discovery programs.

Always find an assay for your target of interest - Take advantage of multiple assay types covering >90% human GPCRome.
GPCR Solutions

Choose the Solution That Best Meets Your GPCR Program Needs

Whether you are developing small molecule or biologic therapeutic drugs, Eurofins Pharma Discovery Services provides you with a variety of drug discovery products and services to meet your specific GPCR research needs.


 

Evaluate Compound Mechanism of Action or Binding Mode

GPCR Screening and Profiling Services

Reduce your time and cost of GPCR discovery, whether your focus is hit identification, selectivity profiling, or SAR optimization. GPCR profiling services offer a collection of over 600 naturally coupled stable GPCR cell lines that enable multiple downstream signaling events to be studied in response to compound activation. Determine compound mechanism of action or choose a compound that shows ligand bias for developing better and safer drugs.

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Universal Platform for Ligand Bias and Receptor Deorphanization

PathHunter® β-Arrestin Assays

Monitor activation or desensitization of GPCRs, and regulation of other signaling molecules such as protein kinases by measuring β-arrestin recruitment and binding to the activated receptor. PathHunter β-Arrestin assays offer a powerful and universal functional screening platform that can be applied to virtually any GPCR without imaging, fluorescent protein tags, or radioactivity and offer the ability to multiplex with Ca2+ or cAMP readouts in the same cell line.

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Quantitative Primary and Orthogonal Screening Assays for Identifying Safer Drugs

PathHunter GPCR Internalization Assays

Measure GPCR trafficking in live cells with the non-imaging, non-antibody-based chemiluminescent functional assays. PathHunter GPCR Internalization assays are whole cell functional assays that provide a direct and quantitative measurement of internalized GPCRs localized to intracellular endosomes and allow the fate of activated GPCRs to be monitored in live cells without the requirement of antibodies, bulky labels or expensive microscopy equipment.

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Simple Assays to Identify and Optimize Pharmacochaperones

PathHunter Pharmacochaperone Trafficking Assays

Identify and characterize compounds which function as pharmacochaperones by promoting proper folding of misfolded protein and assist in trafficking to their intended location. Eurofins DiscoverX’s PathHunter cell-based pharmacotrafficking assays offer a validated, cell-based platform for broad pharmacological characterization and interrogation of compound function in disease processes associated with protein trafficking and internalization due to protein misfolding.

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Complete Assay Solutions for Monitoring cAMP

Cell Lines, Frozen Cells, and Kits

Monitor functional status of GPCRs directly by quantifying cellular cAMP levels in a dose-dependent manner. Detect cAMP levels in cell lines, primary cells, membrane preparations, and serum samples with robust, easy-to-use HitHunter® assays. Cell-based assays available in multiple formats for chemiluminescent or fluorescent read-outs.


 

  

Directly Measure IP1 and IP3/Calcium Flux

Cell Lines, Frozen Cells, and Kits

Measure intracellular calcium mobilization in cells based on the activation status of GPCRs and ion channels. Detect calcium flux rapidly with HTS-friendly HitHunter Calcium No WashPLUS kits that are homogeneous assays that provide a fast, reliable, and low cost approach compared to traditional wash and quench-based assays.

High Quality Membrane Preps for Radioligand Binding and Functional GTPγS Assays

ChemiScreen Membrane Preps

Receptor and G-protein binding assays are long-established and successful approaches to identify ligands for GPCRs. Yet, often the most challenging aspect of a radioligand binding or functional GTPγS assay is the generation of reliable, high quality membrane preps. That's why we developed one of the largest collections of commercially available GPCR membrane preps, so you can focus on reviewing results instead of troubleshooting your assays.
  • ChemiScreen membrane preps on Eurofins Pharma Discovery Services website
  

Easily Build Your Own GPCR Assays

PathHunter Parental Cell Lines and Vectors

Take advantage of Eurofins DiscoverX’s robust proprietary Enzyme Fragment Complementation technology to develop your own stable GPCR cell lines and cell-based assays to study cAMP or calcium accumulation, β-arrestin recruitment, internalization, or trafficking. Design your own workflows and utilize engineered parental cell lines, retroparticles, and plasmid vectors to introduce your own target of interest and create cell-based assays for multiple applications.


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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

The Druggable GPCRome  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 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
 

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