Gain comprehensive insight into on-target efficacy, off-target activity, and ligand-biased signaling with Eurofins Discovery’s GPCR functional assay solutions. Our scalable cellular assays support early discovery through lead optimization with rapid turnaround times and high-throughput screening capabilities.
gpcrMAX Target Distribution by GPCR Family
Why Choose Eurofins Discovery for Your Functional GPCR Research?
- Broad GPCR coverage across hundreds of validated targets
- Multiple functional readouts, including β-arrestin recruitment, cAMP, calcium mobilization, IP1 accumulation, internalization, and more
- Flexible assay formats for agonist, antagonist, PAM, and NAM evaluation
- Compatible with diverse modalities, including small molecules, biologics, peptides, conjugates, PROTAC®s, and controlled substances
- High-throughput screening and profiling capabilities for large compound libraries
- Custom assay development tailored to your program’s needs
- Expedited turnaround options available for select assays
| GPCR Functional Assay Panels | |||||
|---|---|---|---|---|---|
| Service | Panel Description | # Targets | # Assays | Assay Mode | Functional Readouts |
| gpcrMAX | Broad GPCR profiling | 168 | 336 | AG, AN | β-arrestin recruitment |
| orphanMAX | Orphan GPCR screening and deorphanization | 73 | 73 | AG | β-arrestin recruitment, deorphanization |
| Chemokine | Chemokine receptor profiling | 19 | 38 | AG, AN | β-arrestin recruitment, ligand bias characterization |
| obesityLITE | Obesity and metabolic receptor screening | 13 | 25 | AG, AN | β-arrestin recruitment, second messenger signaling, dimerization |
| Peptide Hormone Class B | Class B GPCR screening | 20 | 20 | AG | Second messenger signaling |
| gpcrBIAS | Ligand bias characterization | Choice of >150 | Choice of >150 | AG, AN | β-arrestin recruitment, second messenger signaling, internalization |
| GPCR Solutions “a la carte” Please inquire |
Tailored target and assay selection | Custom | Custom | AG, AN, PAM, NAM | β-arrestin recruitment and second messenger assays including cAMP modulation, calcium mobilization, IP1, internalization |
AG = Agonist, AN = Antagonist, PAM = Positive Allosteric Modulator, NAM = Negative Allosteric Modulator, SP = Single Point, DRC = Dose Response Curve
| GPCR Functional Assays | ||||
|---|---|---|---|---|
| Assay Type | Number of Assays | Assay Modes Available | Applications | |
| β-arrestin recruitment | > 336 | Agonist, Antagonist, PAM and NAM modes Some assays offered in Inverse Agonist mode |
Ligand bias analysis, antagonist screening, and profiling of GPCRs including orphan receptors. | |
| cAMP | > 390 | Agonist, Antagonist, PAM and NAM modes | Cell-based cAMP assays to monitor GPCR function following small molecule or biologic binding. | |
| Calcium Mobilization | >200 | Agonist, Antagonist and PAM modes | Fluorescent dye-based assays to measure calcium mobilization in cell lines as a direct indication of GPCR or ion channel activation or inhibition. | |
| Internalization | > 298 | Agonist, Antagonist and PAM modes Assays measure total internalization or activated internalization |
Measures GPCR internalization, desensitization, recycling, and novel compound pharmacology without imaging or antibodies. | |
| IP1 Accumulation | >200 | Agonist and Antagonist modes | Investigates IP-1 and Ca2+ GPCR-related pathways (Gq and Gα15). | |
| Pharmacotrafficking | 7 | Agonist mode | Identifies pharmacochaperones that stabilize and correct disease-relevant mutant GPCRs, ion channels, and transporters. | |
| GTPgammaS functional | 95 | Agonist, inverse agonist & antagonist modes | Evaluates early GPCR activation and distinguishes agonists, antagonists, inverse agonists, and allosteric modulators. | |
| Human β-Cell Glucose-Stimulated Insulin Secretion (GSIS) | 3 | Agonist and Antagonist modes | Evaluates glucose-stimulated insulin secretion, receptor activation, and cAMP signaling in human pancreatic β-cells. | |
| Custom Assays available: For EFC, please inquire. For TR-FRET/HTRF, please inquire. | ||||
