GPCR Solutions

Comprehensive Solutions for the Entire GPCR Pathway

G-protein coupled receptors (GPCRs) represent a large class of important therapeutic targets. Screening and functional characterization of novel ligands 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 lines designed to detect GPCR signaling through second messenger activation, β-arrestin recruitment, receptor internalization, and pharmacotrafficking. These assays are offered in stable clonal cell lines and cryopreserved ready-to-use cells. 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.

 

Accelerate Novel Ligand Characterization with Multiple Functional Readouts Assay

With increasing awareness of the subtleties of GPCR signaling and potential for ligand bias, there is a greater need for monitoring multiple functional endpoints. Learn more about the duplexed assay developed to monitor calcium signaling with fluorescent dyes sensitive to intracellular Ca2+ ion flux in real time, followed by the recruitment of β-arrestin as an endpoint assay in the same assay plate, for characterization of H1 agonists and antagonist pharmacology.

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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 non-radioactive, chemiluminescent readout that can detect cAMP levels in cell lines, 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 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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Custom Assay Development Services

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

Webinars

β-Arrestin Signaling - The Pathway to Smarter, Safer, and More Effective Drugs Watch Webinar
Make Your Own Cell-Based Assays to Study β-Arrestin Recruitment Watch Webinar
Robust HitHunter® cAMP Assays for Biologics and Small Molecules Watch Webinar
Internalization & Receptor Recycling - Essential Tools for GPCR Biology Watch Webinar
 

Scientific Posters and Presentations

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
 

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