The global G-protein coupled receptors market size was estimated at USD 3.92 billion in 2024 and is projected to grow at a CAGR of 6.10% from 2025 to 2030. G-Protein Coupled Receptors (GPCRs), known as seven transmembrane receptors, bind the chemicals and transmit signals. These GPCRs have effectively identified pharmaceutically relevant drug candidates, which drives the adoption of these receptors in the drug discovery processes. The presence of many approved drugs and drugs under clinical and preclinical studies that target these receptors boost the demand for GPCR screening assays in drug development. Moreover, increasing allosteric modulators, biological drugs, and biased agonists targeting these receptors are accelerating the demand for associated assays.
Due to the rise in lifestyle-related diseases such as cancer, cardiovascular and respiratory diseases, the G-protein coupled receptors industry is expected to grow significantly. Increasing governmental expenditures for research & development purposes for new drugs and therapies is also one of the key drivers of this market. The development of many drugs that require and target these receptors is also the reason for the boost of this market. Although the high costs associated with these cell lines pose a challenge to this market and are also one of the restraints in the growth, the need for more skilled medical professionals and trained experts is also a reason that limits growth to a certain extent.
Structure-based drug Design (SBDD) leverages high-resolution structural data of GPCRs to design and optimize ligands with improved selectivity, efficacy, and safety. Recent advances in structural biology, particularly cryo-electron microscopy (cryo-EM) and X-ray crystallography, have revolutionized GPCR-targeted drug discovery.
For instance, in February 2024, Nature Reviews Endocrinology published a comprehensive review titled "Cryo-electron Microscopy for GPCR Research and Drug Discovery in Endocrinology and Metabolism." This article delves into the transformative role of cryo-electron microscopy (cryo-EM) in advancing the understanding of GPCRs, particularly within endocrinology and metabolic diseases. The review emphasizes the potential of integrating cryo-EM with other biophysical and computational techniques to elucidate GPCR functions further. Such multidisciplinary approaches are anticipated to accelerate the discovery of innovative treatments for endocrine and metabolic diseases.
AI has been utilized across various aspects of GPCR research, including machine learning (ML) for GPCR classification, forecasting activation levels, modeling 3D structures and molecular interactions, deciphering G-protein selectivity, facilitating structural elucidation, and enhancing drug discovery efforts. For instance, a 2024 review published in PubMed highlighted AI's expanding role in GPCR drug discovery, emphasizing its utility in understanding receptor functions, identifying new ligand-GPCR interactions, and predicting clinical responses.
Moreover, scientists in the market focus more on research to explore the novel biological functions of drug candidates. For instance, in January 2024, St. Jude Children's Research Hospital announced a nearly USD 13 million investment in a collaborative research initiative with scientists from Columbia University, Duke University, and Stanford University. This partnership aims to deepen the understanding of G protein-coupled receptors, vital proteins implicated in over 100 human diseases and disorders. Such investments underscore the importance of collaborative efforts in advancing our understanding of GPCRs and developing innovative treatments for diseases affecting children worldwide.
Furthermore, drugs that target the GPCRs have shown the potential to alleviate COVID-19 symptoms. They tend to reduce the pathogenic symptoms associated with this disease. Since these receptors were significant in drug discovery in the initial phase of COVID-19, this market showed significant growth in the initial phase. However, when the pandemic subsided and the R&D activities slowed, the market also witnessed a downfall, although it is expected to maintain stable growth in the forecast period.
The degree of innovation in the G protein-coupled receptors industry is high, driven by advances in structural biology, computational methods, and drug design strategies. For instance, GPCR-Targeting Antibodies & Nanobodies such as engineered antibodies and nanobodies offer high specificity for modulating GPCR activity. Moreover, targeted GPCR Degradation, including PROTACs (proteolysis-targeting chimeras) and molecular glues, selectively degrade disease-causing GPCRs.
The G protein-coupled receptors industry has witnessed a significant increase in collaboration and partnership activities, reflecting a collective effort to advance GPCR-targeted therapeutics. These strategic alliances combine various organizations' expertise to overcome drug discovery and development challenges. For instance, in December 2022, Sosei Group Corporation announced its partnership with Eli Lilly and Company, a global biopharmaceutical firm. The collaboration aims to facilitate drug discovery for novel G protein-coupled receptor targets linked to diabetes and metabolic diseases, including developing and commercializing small molecules with therapeutic potential.
The G protein-coupled receptors industry is experiencing significant product expansion, driven by advancements in drug discovery, AI integration, allosteric modulators, biologics, and multi-target approaches. As companies diversify pipelines and enter new therapeutic areas, the market is seeing a surge in first-in-class and best-in-class GPCR-targeted therapies. The market is also witnessing expansion into new therapeutic areas such as CNS disorders, metabolic disorders, and autoimmune diseases, among others.
The G protein-coupled receptors industry is experiencing notable regional expansion, driven by advancements in drug discovery, increased healthcare investments, and a rising prevalence of chronic diseases. North America holds the largest share of the GPCR market. The Asia-Pacific region is experiencing the fastest growth in the GPCR market over the forecast period.
Based on products, the G-protein coupled receptors industry is segmented into cell lines and detection kits. The cell lines segment dominated the market with the largest revenue share in 2022, owing to the availability of an extensive range of cell lines for the assays. Cell lines play a major role in the cellular impedance assays for detecting GPCR targets, thus attributing to the estimated revenue share. Detection kits have gained popularity in recent years, as they are easy-to-use, robust, and highly sensitive products to evaluate activity through different pathways. Moreover, new detection strategies based on nonlabelled systems, such as resonance wave-guide grating or impedance-based sensors, are anticipated to support the segment's growth.
Based on assay, the G protein-coupled receptors industry is segmented into cAMP functional assays, calcium functional assays, β-arrestin functional assays, radioligand binding and GTPγS functional assays, internalization assays, trafficking assays, and other assays. The cAMP functional assays segment dominated the market with the largest revenue share of 32.5% in 2024 because cyclic Adenosine Monophosphate is an important intracellular second messenger in GPCR signal transduction. The extensive range of reagent kits for measuring cAMP messenger levels significantly boosts the segment's growth.
The calcium functional assays segment is expected to grow at a significant CAGR from 2025 to 2030 because of the advantages of using calcium flux assays, such as high sensitivity, ease in estimating calcium flux, and user configurability.
The market is segmented by application into cancer research, CNS research, metabolic research, cardiovascular research, respiratory research, and inflammation research. The cancer research segment dominated the market, with the largest revenue share of 31.5% in 2024. Many applications are associated with G-protein-coupled receptor activity for treating several disorders. The majority of tumor angiogenesis and immunotherapy-related detections are associated with GPCR activity. The ubiquitously expressed protein is involved in intercellular communication, paving the path for developing potential therapeutics.
Implementation of GPCR assays in cancer research generates substantial revenue. Several studies have proved that GPCR activity reveals tumor proliferation, invasiveness, angiogenesis, metastasis, and drug resistance in cancer patients. As per the research, each cancer cell/tumor product expresses a common set of GPCR. It has also been observed that >150 different GPCRs are expressed by some products of cells, out of which one is expressed at a comparatively high level.
The CNS research application segment is expected to witness a significant CAGR during the forecast period. G protein-coupled receptors play a crucial role in central nervous system function and are key targets for neurological and psychiatric drug development. Their involvement in neurotransmission, neuroprotection, and neuroinflammation makes them essential for understanding and treating CNS disorders.
North America G-protein coupled receptors industry dominated globally with the largest revenue share of 36.9% in 2024 due to strategic investments in cancer research, approval of GPCR-targeted drugs, and increased focus on drug discovery & development activities. Increasing healthcare-related awareness is another factor contributing to GPCR market growth High throughput screening (HTS) techniques assist researchers to identify the biomarkers for therapeutics drugs. An increasing number of diagnostics labs and biomarker-specific detection kits used for the detection of GPCR targets is driving the market growth.
The U.S. G-Protein coupled receptors industry dominated the global market in 2024. The presence of large global players as well as small to mid-sized players in this region generates a huge percentage of revenue for the GPCR market. Large companies are involved in growth strategies to strengthen their GPCR offerings. For instance, in December 2024, Exicure entered into a Memorandum of Understanding (MOU) with GPCR Therapeutics to acquire its U.S. subsidiary, GPCR USA. This partnership aims to advance GPCR Therapeutics' drug development pipelines, including a CXCR4 inhibitor currently in Phase 2 clinical trials targeting multiple myeloma and acute myeloid leukemia.
The Asia-Pacific G-Protein coupled receptors industry is expected to witness a CAGR of 8.24% over the forecast period due to the increasing cases of lifestyle disorders in the growing population of India, China, and other regions of Asia Pacific and the need to cure these diseases with the receptors. Moreover, the presence of several emerging companies, such as Sosei Heptares, HD Biosciences Co., Ltd., and NB Health Laboratory, and the growth initiatives the companies undertake to improve their market presence drive regional growth. For instance, in November 2024, Nxera Pharma and Antiverse entered a multi-target partnership to design novel GPCR-targeted antibody therapeutics using generative AI. This collaboration leverages Antiverse's AI-driven antibody design platform and Nxera's GPCR target selection expertise to develop transformative therapies for diseases with high unmet needs.
China G-protein coupled receptors industry is rapidly expanding, driven by the ongoing research projects related to GPCR by Chinese researchers and scientists, which are expected to drive the China market. Moreover, China dominates the region with growing pharmaceutical R&D activities and government support for drug discovery targeting GPCRs.
Japan G-protein coupled receptors industry is marked by numerous initiatives adopted by the Japan GPCR key players to reinforce their global market presence and strengthen their GPCR offerings. Few players are involved in expanding their drug discovery capabilities, which in turn increases the demand for GPCR assays in drug discovery and development procedures.
Europe G-protein coupled receptors industry registered significant growth in 2024. The growth is supported by strong pharmaceutical and biotechnology industries and government funding for healthcare innovations. Countries like Germany, the UK, and France are key contributors to the region.
The UK G-protein coupled receptors industry holds several potential opportunities favoring the growing usage of GPCR assays. Numerous efforts undertaken by the UK-based GPCR companies and funding initiatives supported by private and public entities drive the UK market growth.
The G-protein coupled receptors industry in Germany is growing due to a combination of factors such as the presence of developed global companies such as Merck KGaA and QIAGEN that are involved in offering GPCR assays and related products such as antibodies, reagents, and ligands.
Latin AmericaG-protein coupled receptors industry is set to grow at a steady pace over the years. This is attributed to increasing awareness regarding novel drug discovery and manufacturing technologies among the companies operating in this region. In addition, the expansion by market players of developed economies across Latin American countries is set to intensify the market competition in the near future.
Brazil G-protein coupled receptors industry is expected to grow in the near future. Brazil’s expanding pharmaceutical and biotechnology sectors drive market trends for targeted drug development in oncology and metabolic disorders.
These companies' key strategies for maintaining their market presence include mergers, acquisitions, and licensing deals for R&D activities. Moreover, they are integrating automation and innovative technologies with drug development screening procedures to improve their capabilities in therapeutic production.
The following are the leading companies in the G-protein coupled receptors market. These companies collectively hold the largest market share and dictate industry trends.
View a comprehensive list of companies in the G-protein Coupled Receptors Market
In January 2025, Isogenica and Cube Biotech announced a strategic collaboration to accelerate GPCR-targeted therapeutics. The partnership combines Cube Biotech's advanced GPCR stabilization technology with Isogenica's proprietary synthetic VHH libraries, aiming to streamline the discovery of antibodies against challenging GPCR targets.
In September 2024, Superluminal Medicines, Inc., a Boston-based biotechnology company, announced the successful closure of a USD 120 million Series A funding round. The round was led by RA Capital Management and participated in by Insight Partners, NVentures (NVIDIA's venture capital arm), Catalio Capital Management, Eli Lilly and Company, Gaingels, and Cooley LLP.
In August 2022, Sosei Group Corporation and AbbVie Inc., a research-based global biopharmaceutical company, announced a new drug discovery partnership and option-to-license agreement. The primary objective of this collaboration is to identify, develop, and bring to market small molecules that effectively modulate novel G protein-coupled receptor (GPCR) targets associated with neurological diseases.
In April 2021, Tectonic Therapeutics announced its launch with a successful Series A financing of USD 80 million. The company aims to revolutionize the discovery of novel therapies targeting G-Protein Coupled Receptors (GPCRs).
Report Attribute |
Details |
Market size in 2025 |
USD 4.13 billion |
Revenue Forecast in 2030 |
USD 5.55 billion |
Growth rate |
CAGR of 6.10% from 2025 to 2030 |
Actual Data |
2018 - 2024 |
Forecast period |
2025 - 2030 |
Quantitative units |
Revenue in USD million/billion and CAGR from 2025 to 2030 |
Report Coverage |
Revenue forecast, company ranking, competitive landscape, growth factors, and trends |
Segments Covered |
Product, assay, application, region |
Regional scope |
North America, Europe, Asia Pacific, Latin America, MEA |
Country scope |
U.S., Canada, Mexico, UK, Germany, France, Italy, Spain, Denmark, Sweden, Norway, China, Japan, India, Australia, South Korea, Thailand, Brazil, Argentina, Saudi Arabia, South Africa, UAE, Kuwait |
Key companies profiled |
Thermo Fisher Scientific Inc.; Eurofins Scientific; QIAGEN; WuXi AppTec; Promega Corporation; Abcam plc; Merck KGaA; PerkinElmer Inc.; Enzo Biochem Inc.; BD |
Customization scope |
Free report customization (equivalent up to 8 analyst’s working days) with purchase. Addition or alteration to country, regional & segment scope |
Pricing and purchase options |
Avail customized purchase options to meet your exact research needs. Explore purchase options |
This report forecasts global, regional, and country revenue growth and analyzes the latest industry trends in each sub-segment from 2018 to 2030. For this study, Grand View Research has segmented the global G-protein coupled receptors market report based on product, assay, application, and region:
Product Outlook (Revenue, USD Million, 2018 - 2030)
Cell Lines
Detection Kits
Cell Culture Reagents
Ligands
Assay Type Outlook (Revenue, USD Million, 2018 - 2030)
cAMP Functional Assays
Calcium Functional Assays
β-Arrestin Functional Assays
Radioligand Binding & GTPγS Functional Assays
Internalization Assays
Trafficking Assays
Other Assays
Application Outlook (Revenue, USD Million, 2018 - 2030)
Cancer Research
CNS Research
Metabolic Research
Cardiovascular Research
Respiratory Research
Inflammation Research
Other Applications
Regional Outlook (Revenue, USD Million, 2018 - 2030)
North America
U.S.
Canada
Mexico
Europe
UK
Germany
France
Italy
Spain
Denmark
Sweden
Norway
Asia Pacific
Japan
China
India
Australia
Thailand
South Korea
Latin America
Brazil
Argentina
Middle East & Africa
South Africa
Saudi Arabia
UAE
Kuwait
b. The global G-protein coupled receptors market size was estimated at USD 3.92 billion in 2024 and is expected to reach USD 4.13 billion in 2025.
b. The global G-protein coupled receptors market is expected to grow at a compound annual growth rate of 6.10% from 2025 to 2030 to reach USD 5.55 billion by 2030.
b. Some of the market opportunities for market growth include the advancements in the understanding of GPCR biology in oncology for the development of combined therapies and technological advancements in the market.
b. Key factors that are driving the market growth include growing demand for GPCR assays in drug discovery studies; wide application of GPCRs in the treatment for various medical conditions; the rising number of initiatives by government and key players.
b. Some key players operating in the G-protein coupled receptors market include Thermo Fisher Scientific, Inc.; Eurofins Scientific; QIAGEN; WuXi AppTec(HD Biosciences Co. Ltd); Promega Corporation; Abcam plc; Perkin Elmer Inc.(Cisbio Bioassays); Enzo Biochem Inc.; Merck KGaA; and Becton-Dickinson and Company.
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