G protein-coupled receptors (GPCRs), a diverse superfamily of transmembrane receptors, are key targets for a significant fraction of clinically approved therapeutics. Eurofins Discovery offers over 2,750 automation-compatible, customizable, high quality and robust assays – enabling comprehensive GPCR profiling at scale. Our validated solutions streamline the characterization of ligand binding, signal transduction, and mechanism of action – helping you move faster from discovery to drug candidate. Additionally, Eurofins DiscoverX GPCR products provides 1500+ qualified cell-based assays for detecting ligand binding, second messengers, beta-arrestin recruitment, and many more.
Comprehensive Solutions for GPCR Pathway Investigation
| GPCR SOLUTIONS | |||
|---|---|---|---|
| GOAL | SOLUTION | ASSAY FORMAT | |
| BINDING ASSAYS |
|
Ligand Binding | Radioligand Binding ([3H], [125I], filtration & SPA) |
| Label-free Mass-Spectrometry / Biophysics with Purified & Refolded GPCRs | |||
| FUNCTIONAL ASSAYS |
|
G protein Recruitment | [35S]-GTPγS Binding |
| cAMP Accumulation | Enzyme Fragment Complementation (EFC) by Chemiluminescence | ||
| Time-Resolved Fluorescence (TR-FRET) | |||
| Calcium Mobilization | Calcium Flux (Gq and Gα15 Coupling) by Fluorescence | ||
| IP-1 Accumulation | Time-Resolved Fluorescence (TR-FRET) | ||
| β-arrestin Recruitment | Enzyme Fragment Complementation (EFC) by Chemiluminescence | ||
| Receptor Internalization | Enzyme Fragment Complementation (EFC) by Chemiluminescence | ||
| CUSTOM SOLUTIONS |
|
Custom; Please Inquire | Customized to Meet Program Needs |
| HUMAN PRIMARY-LIKE PANCREATIC BETA CELL-BASED ASSAYS |
|
GSIS: Insulin-release | Agonist |
| cAMP Accumulation | Time-Resolved Fluorescence (TR-FRET) | ||
GPCR Functional and Binding Assays
Design Your Screening Cascade
End-to-End GPCR Solutions
Eurofins Discovery provides the industry’s most extensive collection of validated GPCR assays. Our solutions help you:
- Measure response along every step of the GPCR signaling cascade.
- Understand binding and mechanistic regulation of G proteins in response to active compounds and allosteric modulators.
- Deorphanize receptors, evaluate ligand bias, identify multi-targeted therapeutics.
- Validate AI-predicted hits with data-rich outputs compatible with machine learning pipelines.
- Rapidly screen 500K+ compound libraries with high-throughput screening platforms.
- Profile using our readily available GPCR-focused, diversity-focused and virtual small molecule libraries.
- Utilize integrated drug discovery workflow from compound management to data analysis.
- Partner in every research phase from early discovery to hit finding to lead optimization to candidate selection.
Eurofins Discovery offers a comprehensive suite of GPCR solutions designed to meet your project’s unique need. Whether you are focused on hit identification, selectivity profiling, lead optimization, or mechanism of action (MoA), our flexible platforms help reduce time and cost across the GPCR drug discovery pipeline. Partner with us to move from insight to impact – faster!
