Consider Eurofins DiscoverX’s custom development capabilities for custom cell lines, assays, & enzyme development.
GPCR Product Solutions
Always find a GPCR Assay for Your Target of Interest
G protein-coupled receptors (GPCRs) are 7-transmembrane receptors representing the largest family of validated therapeutic targets with over 800 known human GPCRs. Therapeutics targeting GPCRs represent over 40% of all currently marketed drug therapeutics acting on GPCRs either directly or indirectly. GPCRs have a broad array of ligands, including growth factors, ions, lipids, nucleotides, hormones, and neurotransmitters.
Their physiological and pathological involvements are vast, ranging from regulation of hunger to the development of fetal structures, and from roles in cardiovascular disorders to rare diseases. To help researchers fully characterize their specific GPCR of interest, and the small molecules or biologics effecting their activity, Eurofins DiscoverX® encourages exploring all possible signaling scenarios with a variety of available biologically-relevant cell-based functional and binding assays, cell lines, detection kits, and membrane preparations.
The target-specific products in the Eurofins DiscoverX portfolio are sensitive, scalable, and robust for detecting receptor-mediated second messenger signals (cAMP and calcium), β-arrestin recruitment, receptor internalization, and ligand binding. These assays also support the characterization of orphan GPCRs without a known ligand or approved drug as part of the comprehensive GPCR solutions portfolio offered.
Product Highlights
- Broad Coverage – Over 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 through pre-clinical drug discovery programs
- Assay Options – Multiple mechanism of action (MOA) assay types are available (e.g., β-arrestin, cAMP, calcium, internalization, ligand binding, trafficking) offering a diverse array of GPCR assay solutions for maximum flexibility
- Largest Collection – Over 1,600 qualified functional and binding assays seen in >800 peer-reviewed publications, giving you the most comprehensive GPCR assay solutions available for the confidence you need
GPCR β-Arrestin Product Solutions
Universal G-protein independent cell-based assays to measure GPCR beta-arrestin recruitment and subsequent internalization upon ligand or therapeutic ...Show More
GPCR cAMP Product Solutions
Detect cellular cAMP levels via GPCR signaling by biologics or small molecule therapeutics using robust, simple, homogeneous & HTS assays.
GPCR Calcium Product Solutions
Measure intracellular calcium flux via GPCR signaling using stable cell lines, ready-to-assay kits, & HTS Calcium No WashPLUS detection kit.
Products
Targets
Highlights
Assay Principles
Resources
Related Pages
Products
Product Types
Eurofins DiscoverX GPCR products for specific known, orphan, or ortholog (multiple species) GPCRs.
- GPCR Bioassay Kits – Ready-to-use cell-based assay kits with a simple, homogenous protocol and are provided as qualified or target-based. These physiologically relevant, robust bioassays are fit-for-purpose for use in screening and characterization applications to potency testing in quality control lot-release programs. Learn more about Bioassay Kits.
- GPCR eXpress Assay Kits – Ready-to-use cell-based assay kits for quick analysis and implementation in early discovery phases for screening applications, proof-of-concept, mechanism of action confirmation, and rank-ordering studies. Learn more about eXpress Assay Kits.
- GPCR Cell Lines – Stable cell lines developed to reflect the target’s mechanism of action with a drug interaction in a standard cell line background. Learn more about Stable Cell Lines.
- GPCR Membrane Preparations – Purified membrane preps for obtaining GPCR and ion channel ligand binding affinities and evaluating GPCR activity through GTPγS functional studies in response to the addition of a ligand or therapeutic. Learn more about Membrane Preparations.
- GPCR Parental Cell Lines – Engineered cells to generate your own GPCR assays and investigate β-arrestin recruitment and GPCR desensitization and internalization of your GPCR target of interest.
- Retroviral Particles – Create target-specific, stable β-arrestin cell lines in any divided cell type. The product comes with a complete set of retroparticles and reagents combined with an easy-to-follow protocol to help you generate your own β-arrestin cell-based assays. Learn more about Toolbox Products.
Applications
- β-Arrestin Assays – Universal G-protein independent cell-based assays to quantify GPCR activation based on the recruitment of β-arrestin. Ideal for ligand bias analysis, antagonist mode screening, and studying virtually any GPCR including orphan receptors. Learn more about β-Arrestin Assays.
- cAMP Assays – Homogeneous cAMP detection cell-based assays to monitor the functional status of GPCRs upon small molecules or biologics binding. Characterize ligand pharmacology and obtain reproducible performance with large assay windows and broad sensitivity ranges. Learn more about cAMP Assays.
- Calcium Assays – Fluorescent dye-based assays to measure calcium mobilization in cell lines as a direct indication of GPCR or ion channel activation or inhibition. Learn more about Calcium Assays.
- GPCR Internalization Assays – Secondary, orthogonal screening cell-based assays for measuring GPCR desensitization and recycling as well as uncovering novel classes of compound pharmacologies and identifying safer drugs without imaging or antibodies. Learn more about GPCR Internalization Assays.
- GPCR Pharmacotrafficking Assays – Quantitative cell-based assays to identify small molecule pharmacochaperones that act as therapeutic agents to stabilize and correct disease-relevant mutant GPCRs, ion channels, or transporters. Learn more about GPCR Pharmacotrafficking Assays.