Our promise to you:
Guaranteed product quality, expert customer support.
24x7 CUSTOMER SERVICE
CONTACT US TO ORDER
G protein-coupled receptors (GPCRs) are ubiquitous cell-surface receptors that play central roles in signal transduction across neurobiology, immunology, metabolism, and endocrinology. As drug development targets, GPCRs remain among the most studied and clinically exploited—around 30% to 50% of approved drugs act on GPCRs. Yet the majority of the GPCR family remains underexploited—especially orphan GPCRs—offering rich opportunities for novel therapeutic development.
GPCR binding assays occupy a strategic position in drug discovery. Compared with functional assays, binding experiments directly and sensitively reveal ligand-receptor interactions, assess affinity, competition, and structure-activity relationships. These assays are particularly crucial during the lead identification, mechanism validation, and pharmacological profiling stages.
Figure 1. G-protein-coupled receptor signal transduction. (Hilger D, et al., 2018)
Creative Biogene's GPCR binding analysis service is supported by a diverse suite of assay technologies, including Radioligand Binding, TR-FRET, SPA, and traditional filtration-based approaches. Radioligand binding remains the gold standard for sensitive and quantitative affinity determination, suitable for saturation binding, competitive displacement, and specificity assessment, yielding key pharmacological parameters. For clients who prefer non-radioactive methods or require high throughput, TR-FRET and SPA platforms offer "mix-and-read" formats ideal for automation and parallel processing with excellent data consistency.
We maintain an in-house membrane preparation resource spanning 100+ human GPCR targets, including dopamine, serotonin, adenosine, adrenergic, chemokine, and peptide receptors. We also accept client-provided receptor constructs or engineered cell lines to build bespoke assay systems, ensuring specificity and reproducibility tailored to your project.
Clients may choose between single-point binding assays, full dose–response curve analyses (IC₅₀/Ki), or high-throughput library screening. Whether you require an affinity ranking of candidate ligands or screening of thousands of compounds for hit discovery, our assay design adapts to your needs.
In addition to binding strength measurements, we offer advanced characterization options: kinetic rate analysis (kon/koff), saturation curve modeling, and receptor density quantification (Bmax). For enhanced insight, binding assays can be seamlessly paired with functional GPCR readouts—such as cAMP, IP1, or β-arrestin recruitment—to establish comprehensive pharmacological profiles.
Your final deliverables include clean, well-structured data reports containing raw readings, standard curves, binding plots, non-linear regression fits, and summary parameters, along with detailed method descriptions—ready for research, regulatory, or patent preparation.
We recognize that speed and flexibility are essential in academic and industrial drug discovery. Creative Biogene consistently delivers routine binding assay projects within 3–4 weeks, while medium-scale screens are generally completed within 4–6 weeks, thanks to our automation-enabled workflows. For clients with specific requirements such as bespoke ligand labels, optimized incubation conditions, custom buffer systems, or multi-point concentration designs, our experienced scientists offer one-on-one guidance to optimize assay setup, execution, and analysis. We also offer flexible pricing and engagement models tailored to sponsor type, enabling cost-effective yet scientifically rigorous outcomes.
Compared to larger service providers who rely on broader assay panels and standardized delivery formats, Creative Biogene emphasizes individualized experimental solutions, rapid turnaround, and affordable pricing. We prioritize close technical collaboration and co-design of assays rather than purely transactional outsourcing, strengthening strategic support across drug discovery stages.
We don't just perform binding assays—we deliver integrated pharmacology profiling, linking ligand binding to receptor activation and downstream signaling. Whether you are repositioning known GPCR targets or exploring orphan receptors, Creative Biogene can serve as your trusted discovery partner, offering flexible assay design, technical expertise, and execution reliability.
If you're seeking expert GPCR binding analysis solutions, designed to be fast, accurate, and budget-conscious, please reach out to our team to discuss your project, receive customized proposals, and arrange pilot studies. A single binding assay may be the key to unlocking your next breakthrough. Get in touch through our website or contact email to begin collaboration today!
GPCR Stable Cell Line Development
Epigenetic Screening & Profiling Services
Ion Channel Screening & Profiling Services
Nuclear Receptor Screening & Profiling Services
Transporter Screening & Profiling Services
Q: What type of input material do I need to provide to initiate a custom GPCR binding assay?
A: We typically require either the recombinant GPCR-expressing cells or membrane preparations. If you are unable to provide these, Creative Biogene can generate the membranes in-house from a wide range of expression systems, including HEK293, CHO, and Sf9 cells. For radioligand-based assays, the corresponding labeled ligand is preferred if it is not commercially available. All reagents provided by clients must be accompanied by relevant COAs or specification sheets.
Q: Can you accommodate binding assays for orphan GPCRs or non-commercially validated targets?
A: Yes. We offer custom assay development for orphan or low-characterized GPCRs, including de novo membrane expression, assay condition optimization, and ligand sourcing. For orphan GPCRs, we can conduct ligand fishing and use surrogate ligands to initiate preliminary screening if no known ligand is available.
Q: How do you validate the specificity of ligand-receptor interactions in the absence of known reference compounds?
A: For poorly characterized or novel GPCRs, we apply orthogonal validation strategies, such as non-specific binding controls, competition with structurally related analogs, and testing across a panel of non-target GPCRs to evaluate cross-reactivity. If needed, functional assays can be introduced to support binding results.
Copyright © Creative Biogene. All rights reserved.