GPCR Solutions

Comprehensive Solutions for the Entire GPCR Pathway

G-protein coupled receptors (GPCRs) represent one of the largest classes of important therapeutic targets. Screening and functional characterization of novel ligands, such as allosteric modulators, for GPCRs remains a key activity in drug discovery process. To simplify and speed exploration of GPCR biology and accelerate targeted drug discovery, choose from over 600 naturally-coupled GPCR cell-based assays designed to detect GPCR signaling through second messenger activation, β-arrestin recruitment, receptor internalization, and pharmacotrafficking. These assays are offered as stable clonal cell lines, cryopreserved cells in ready-to-use kits, and vector-based toolbox products. With the largest offering of human and ortholog GPCR assays in a wide variety of functional readouts, DiscoverX delivers complete flexibility to choose the ideal platform that meets your specific program needs.


Application of β-Arrestin Assays to the Orphan GPCR World

In this webinar, Dr.’s Ralf Jockers and Atsuro Oishi  highlight the application of several β-arrestin assays to analyze orphan GPCRs, discuss the advantages and characteristics of each assay, and describe allosteric modulation of β-arrestin pathway in GPCR heteromers.

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Highly Sensitive, Homogeneous, Biochemical cAMP Assays

HitHunter® cAMP Assays

Monitor functional status of GPCRs directly by quantifying cellular cAMP levels in a dose-dependent manner, with the robust, easy-to-use cell-based detection system. HitHunter kits are extremely versatile, providing a rapid and reliable chemiluminescent readout to obtain accurate ligand pharmacology, including allosteric modulation. Use these assays to detect cAMP levels in cell lines (cAMP Hunter™), primary cells, membrane preparations, and serum samples.

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Single Step Protocol for Direct Measurement of Intracellular Calcium

HitHunter Calcium No WashPLUS Assays

Measure intracellular calcium mobilization based on the activation status of GPCRs (from Gq-coupled cell lines) and ion channels. HTS-friendly HitHunter Calcium No WashPLUS kits use a homogeneous assay format with large assay windows, larger dynamic range and provide a fast, reliable, low cost approach compared to traditional wash and quench-based assays.

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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 tagsm, or radioactivity and offer the ability to multiplex with Ca2+ or cAMP readouts in the same cell line.

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A Simple Primary and Orthogonal Screening Tool 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 and Quantitative Tool 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. 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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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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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

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