GPCR Screening & Profiling Services
Background and Challenges in GPCR Drug Screening
GPCRs play a central role in regulating physiological processes by sensing extracellular signals, including hormones, neurotransmitters, photons, and odorant molecules, and transmitting them through intracellular signaling cascades. The complexity of GPCR signaling arises from multiple aspects: a single receptor can activate multiple downstream pathways (pleiotropy); different ligands can preferentially trigger specific signaling routes (biased signaling); and receptors can form homo- or heterodimers, further increasing signal diversity.
Figure 1. Status of GPCRs according to their most advanced compound. (Lorente JS, et al., 2025)
While these features enrich GPCR biology, they present unique challenges for drug screening: capturing activation of specific pathways, distinguishing ligand-specific signaling preferences, and maintaining data reliability during high-throughput screening.
GPCR Screening and Profiling Services
Leveraging years of expertise in membrane protein research and drug development, Creative Biogene has established a systematic GPCR screening and functional analysis platform. Our services support academic institutions, pharmaceutical companies, and biotechnology firms across the full spectrum of research—from fundamental studies to drug discovery.
Binding Assays
We offer multiple assays to assess direct interactions between compounds and GPCRs:
- Radioligand Binding Assays: A classical, highly sensitive method to quantify ligand affinity and competitive inhibition constants.
- Fluorescence Polarization Binding Assays: Non-radioactive alternatives suitable for medium-throughput screening.
- Surface Plasmon Resonance (SPR): Real-time monitoring of binding kinetics, providing association (kon) and dissociation (koff) rate constants.
These binding assays are ideal for preliminary screening, selectivity evaluation, and structure-activity relationship studies, laying the groundwork for subsequent functional analysis.
Functional Activity Analysis
Functional assays provide insight into the biological effects of compounds on GPCR signaling. We offer multi-pathway detection services, including:
- cAMP Assays: Applicable to Gαs- and Gαi-coupled receptors, using ELISA or reporter gene methods.
- Calcium Flux Assays: For Gαq-coupled receptors, using fluorescent dyes or genetically encoded calcium indicators.
- IP-1 Assays: Measures downstream metabolites of the Gαq pathway, suitable for models where calcium detection is challenging.
- Arrestin Recruitment Assays: Utilizing a luminescence- or fluorescence-based reporter system to monitor intracellular recruitment of arrestin proteins upon GPCR activation, supporting studies of ligand bias and receptor internalization.
- GTPγS Binding Assays: Directly measure G protein activation for diverse GPCR functional studies.
GPCR Target Landscape by Disease Area
Metabolic Diseases
Neuropsychiatric Disorders
Immunology & Inflammation
Oncology
Cardiovascular Diseases
Other Key Areas
| Gene Symbol | Common Name | Class |
| Metabolic Diseases | GLP1R | GLP-1 receptor | B1 |
| GIPR | GIP receptor | B1 |
| GCGR | Glucagon receptor | B1 |
| MC4R | Melanocortin 4 receptor | A |
| FFAR1 (GPR40) | Free fatty acid receptor 1 | A |
| GPR119 | GPR119 | A |
| Gene Symbol | Common Name | Class |
| Neuropsychiatric Disorders | HTR2A | 5-HT2A receptor | A |
| DRD2 | Dopamine D2 receptor | A |
| CHRM1/CHRM4 | Muscarinic M1/M4 receptors | A |
| GABABR1/R2 | GABA B receptor 1/2 | C |
| GRM2/GRM3 | Metabotropic glutamate receptor 2/3 | C |
| CNR1 | Cannabinoid CB1 receptor | A |
| OPRD/OPRK/OPRM1 | δ/κ/μ Opioid receptors | A |
| HRH3 | Histamine H3 receptor | A |
| Gene Symbol | Common Name | Class |
| Immunology & Inflammation | S1PR1 | Sphingosine-1-phosphate receptor 1 | A |
| CCR2/CCR5/CXCR4 | Chemokine receptors | A |
| C5AR1 (CD88) | Complement C5a receptor 1 | A |
| FPR2/ALX | Formyl peptide receptor 2 | A |
| LTB4R (BLT1) | Leukotriene B4 receptor | A |
| ADORA2A | Adenosine A2A receptor | A |
| Gene Symbol | Common Name | Class |
| Oncology | SMO | Smoothened receptor | F |
| CXCR4 | C-X-C chemokine receptor 4 | A |
| CCR4 | C-C chemokine receptor 4 | A |
| GPRC5D | GPRC5D | C |
| LPAR1 | Lysophosphatidic acid receptor 1 | A |
| F2RL1 (PAR2) | Protease-activated receptor 2 | A |
| Gene Symbol | Common Name | Class |
| Cardiovascular Diseases | ADRA1A/ADRB1 | α1/β1 Adrenoceptors | A |
| AGTR1 | Angiotensin II receptor type 1 | A |
| P2RY12 | P2Y12 receptor | A |
| EDNRA | Endothelin A receptor | A |
| Gene Symbol | Common Name | Class |
| Other Key Areas | MTNR1A/MTNR1B | Melatonin receptor 1A/1B | A |
| OXTR | Oxytocin receptor | A |
| AVPR2 | Arginine vasopressin V2 receptor | A |
| TSHR | Thyrotropin receptor | A |
Specialized Technical Platforms
Multiparametric Screening
Parallel monitoring of multiple signaling pathways enables comparison of compound effects across pathways under the same experimental conditions, facilitating the identification of biased ligands.
Non-Mammalian Expression Systems
Yeast-based GPCR screening platforms provide rapid growth, low background, and ease of operation, ideal for large-scale preliminary screening and initial functional characterization.
For specific research needs, we provide stable GPCR cell line development, custom reporter gene systems, tailored screening strategies, and professional support for data analysis and interpretation.
Quality Assurance and Data Reliability
We recognize the critical importance of high-quality data for research decision-making. All experiments adhere to stringent quality control standards, including:
- Inclusion of positive and negative controls
- Z'-factor assessment for screening quality
- Intra- and inter-experimental reproducibility verification
- Systematic dose-response analysis
Our experienced GPCR research team provides expert guidance in project design, experimental execution, and data interpretation to ensure reliable and reproducible outcomes.
Service Workflow
1Needs Assessment: Define research objectives and screening strategy
2Experimental Design: Develop customized protocols and quality control standards
3Execution: Conduct comprehensive screening and validation experiments
4Data Analysis: Professional processing and interpretation of results
5Reporting: Delivery of detailed experimental reports with recommendations
Contact Us
Creative Biogene is dedicated to delivering high-quality, reliable GPCR research services. We look forward to collaborating with you to advance the understanding of GPCR biology and accelerate drug discovery.
