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G-Protein Coupled Receptors (GPCRs) Market Report Scope & Overview:

The G-protein coupled receptors (GPCRs) market size was valued at USD 3.92 billion in 2024 and is expected to reach USD 6.04 billion by 2032, growing at a CAGR of 5.59% over the forecast period of 2025-2032.

The global G-protein coupled receptors (GPCRs) market is growing at a significant rate due to rising drug discovery efforts and the growing prevalence of chronic diseases, such as cancer. These receptors are key to targeting in therapeutic research for oncology, metabolism, and neurology. Rising admonitions between small biotech companies and big pharmaceutical companies, and increasing application of high-throughput screening and functional assay have also been powering the G-protein coupled receptors (GPCRs) market growth.

The U.S. G-protein coupled receptors (GPCRs) market size was valued at USD 1.11 billion in 2024 and is expected to reach USD 1.66 billion by 2032, growing at a CAGR of 5.21% over the forecast period of 2025-2032.

The U.S. leads the North American G-protein coupled receptors (GPCRs) market as it has better biotechnology and pharmaceutical infrastructure, and its established players in the industry, as compared to other countries. Country leadership in drug discovery and development, especially focused on GPCR, is reinforced by an excellent clinical trial infrastructure and approvals for innovative medicines. This has made the U.S. a major driver of growth in the regional GPCRs market.

Market Dynamics:

Drivers

  • Increasing Technological Advancements in GPCR Screening and Assay Technologies are Accelerating Market Growth

New advances in assay technology and screening strategies have greatly facilitated the investigation and understanding of GPCRs. Recent advances in technology, including high-throughput screening (HTS), label-free methods of detection (such as surface plasmon resonance, impedance-based systems), and biosensor assays, now allow for to measurement of receptor activity with increased speed, sensitivity, and precision. These advances facilitate the discovery of drug candidates and further clarify GPCR signaling pathways, which are imperative for the design of novel therapies. The market is growing due to the increasing adoption of these tools, especially by companies in the pharmaceutical and biotechnology sectors, which are further intensifying the market.

A recent survey indicates that more than 30% of FDA-approved medicines act upon GPCRs, highlighting the necessity for HTS in GPCR drug discovery.

Automated screening technologies, computational and experimental, for GPCRs will enable the paradigm shift from drug screening to personalized medicine applications. 

  • Rising R&D Expenditure by Pharmaceutical/Biotech Companies is One of the High-Impact Factors Contributing to The Market Growth

The pharmaceutical and biotech industries invest heavily in GPCR studies due to these receptors have been implicated in myriad diseases and have already been leveraged as drug targets. This further emphasizes that GPCRs are very interesting targets for further investigation, knowing that 30–40% of commercially available drugs exert their action at these receptors. Companies are also strengthening their GPCR portfolios via in-house R&D and licensing deals and collaborations with academic organisations and CROs. Other. This increased focus is complemented by venture capital financing and strategic mergers and acquisitions in the GPCR drug development space. This, in turn, also drives the GPCR market through growing R&D investments.

In May 2025, Novo Nordisk completed its historic USD 2.2billion transaction with Septerna to develop oral small-molecule GPCR drugs aimed at the GLP-1, GIP, and glucagon receptors. Septerna was paid over USD 200million in upfront funds.

Crinetics Pharmaceuticals and Radionetics Oncology completed a strategic collaboration with Eli Lilly, including USD 140M upfront to co-develop GPCR-targeted radiopharmaceuticals.

Restraint

  • High Time and Effort Investment in Development and Long Timelines are Restraining the Market from Growing

Ligand discovery for G-protein coupled receptors (GPCRs) is a considerable subtask due to the multifaceted nature of GPCR biology and the high investment of money and time needed to develop therapeutics that specifically target GPCRs. Due to  GPCRs are involved in countless physiological processes, which in many instances are controlled by multiple GPCR subtypes belonging to the same or different GPCR classes, rigorous preclinical studies are necessary to determine the specificity, efficacy, and safety of these agents. These assays need to be conducted using high-throughput technologies, functional screening, receptor binding analysis, and animal models, which pushes up the cost of these studies.

In addition, the period of clinical development is especially long for GPCR-targeted drugs, due to companies' need to perform various types of trials to investigate pharmacokinetics, pharmacodynamics, and adverse events. This entire journey — from the earliest research, through regulatory approval — can easily consume 10 to 15 years and hundreds of millions of dollars of investment. For smaller biotech companies and startups, these high hurdles could stifle innovation and postpone new product introductions.

Segmentation Analysis:

By Product

The cell lines segment dominated the G-protein coupled receptors (GPCRs) market share in 2024, with a 46.1% due to their extensive use in drug screening, receptor characterization, and functional assays. These cell lines are transfected with a construct to express certain GPCRs and provide the scientists with the ability to explore their activities in the controlled setting of a laboratory. This means that they are a key aspect in high-throughput screening platforms utilized by pharma and biotech companies due to their methods being easily reproducible, scalable, and compatible with a range of assay formats, which fuels their popularity.

The detection kits segment is projected to be the fastest-growing segment during the forecast period. This increase is due to an increasing need for assays that are standardized, simple, and time-convenient in performing the GPCR function-related assays, ligand binding, and signal transduction. Detection kits simplify assay development, are compatible with many detection methods (FL, luminescence, etc.), and are gaining in use among academic institutions, CROs, and small biotech companies. Increasingly put to use in high-throughput screening and biomarker validation, they’re becoming more rapidly adopted in a wide array of research settings.

By Assay Type

The cAMP functional assays segment accounted for the largest share of the G protein-coupled receptor market in 2024, with around 28% market share, owing to its ability to measure intracellular cAMP, a major second messenger in GPCR-mediated signaling pathways. These assay systems are widely used for analyzing the activity of Gs- and Gi-coupled receptors and are thus essential for studying receptor pharmacology and for drug screening. Their high sensitivity and reproducibility, and compatibility with automation, have led to the gold standard in both academic and pharmaceutical research, resulting in their market leader position.

The calcium functional assays are anticipated to grow at a significant CAGR during the forecast period. This interest has increased due to a growing attention to the Gq-coupled GPCRs that mediate intracellular calcium signaling. These assays provide rapid, real-time measurements and are increasingly used in neuroscience, cardiovascular, and inflammation studies. Recent developments in calcium-sensitive dyes and high-throughput screening systems have made these assays reliable and easier to perform, leading to a maturing of the market across research labs and CROs, thereby providing a fillip to the growth of the market.

By Application

The cancer research segment led the G-protein coupled receptors (GPCRs) market in 2024 with a 31.2% market share, owing to the vital role of GPCRs in the progression, angiogenesis, and metastasis of the tumor. Given their frequently deregulated expression in various cancers, GPCRs have become the focus of clinical research in anticancer drug development. The rising focus that has been placed on oncology-based R&D and the growing number of clinical trials on GPCRs for different cancer types have greatly driven the demand for GPCR-associated assays, reagents, and screening platforms for cancer research.

The CNS research segment is projected to grow at the highest CAGR during the forecast period due to its key role of the GPCRs in regulating neurotransmission, neuroinflammation, and neurodegenerative processes. Alzheimer’s disease, Parkinson’s disease, schizophrenia, depression, and the diseases of the central nervous system are diseases with complicated GPCR signaling pathways. There is an increased focus on exploration of the GPCR targeted pharmacology for CNS disorders, with the burden of neurological diseases increasing across the globe, which is also driving the rapid expansion of this application area by research organizations and drug developers.

By End User

The pharmaceutical & biotechnology companies segment held a major share of the G-protein coupled receptors (GPCRs) market in 2024, with around 52.1% market share due to increasing demand for GPCR-focused drug discovery and development. These firms are frontrunners in conducting investment in research and in preclinical/clinical experiments, as almost one-third of all FDA-approved drugs result from action at GPCR targets. These companies boast strong innovation and possess cutting-edge GPCR screening technologies, cell lines, and assay platforms, and, in doing so, facilitate faster therapeutic pipeline development across cardiovascular diseases, metabolic diseases, CNS, and oncology to add impetus to GPCRs being perceived as the dominant targeting segment.

The contract research organizations (CROs) segment is expected to register the highest CAGR during the forecast period, owing to the rise in adoption of the outsourcing model for various complex drug discovery and development services. Pharmaceutical and biotech firms are using CROs for GPCR assay development, target validation, and HTS to reduce cost and time. An increase in dedicated CROs that are equipped with advanced GPCR technologies and growing global collaborations and clinical trial activity are supporting momentum in this space.

Regional Analysis:

North America dominated the G-protein coupled receptors (GPCRs) market analysis in 2024, with 37.10% primarily due to highly developed pharmaceutical and biotechnology industries, investment in R&D, high-tech advancement supporting artificial Intelligence, and the utilization of improved technology and presence of major market players in this region. The region is home to the most concentrated regions of academic and research institutions engaged in drug discovery, with a particular focus on GPCR-targeted therapies. Furthermore, robust government backing, positive regulatory environment, and high prevalence of chronic diseases such as cancer and cardiac ailments have contributed to demand for advanced therapies for GPCR pathways.

The Asia Pacific is experiencing the fastest growth in the G-protein coupled receptors (GPCRs) market with a 6.12% CAGR over the forecast period, due to growing life sciences investments, expanding biopharmaceutical industries, and awareness regarding precision medicine. Countries, including China, India, and South Korea, are building their capacity in drug discovery, helped by government programmes and working with international biotech companies. Furthermore, the rising number of patients, developing healthcare facilities, and rising clinical research activities are some of the factors fueling the growth of the regional market.

The G‑protein coupled receptors (GPCRs) market in the European region is increasing due to many initiatives implemented by the government and government-funded organisations to promote research and development in the region. This progress is driven by countries such as Germany, the U.K., and France, with deep roots in pharma and biotech. Concentration on precision medicine in the region, and recent progress on structural biology and AI application in drug discovery, all these have driven the continuous increase in GPCR-related research and clinical applications, and Europe has become an important market for the market.

The G-protein coupled receptors (GPCRs) market trends in Latin America and the Middle East & Africa (MEA) are anticipated to expand at a moderate pace of growth due to the rising investment in pharmaceutical and biotechnology research, especially in several countries in Latin America, and funding and establishment of GPCR-based drug discovery platforms that cater to the fields of oncology and metabolic diseases, is also aiding in this space.

G-protein coupled receptors (GPCRs) market growth in the MEA region is moderate due to the developing healthcare system and increasing research capabilities, especially in Gulf countries such as Saudi Arabia and the UAE. The increasing adoption of sophisticated therapies and diagnostic techniques, combined with remaining technical capacity shortfalls and a dependence on imported research tools, has driven consistent market growth.

Key Players:

The G-protein coupled receptors (GPCRs) market companies include Thermo Fisher Scientific, Merck KGaA, PerkinElmer, Abcam, Promega Corporation, BMG LABTECH, Eurofins Scientific, Isogenica, BD Biosciences, Qiagen, Enzo Life Sciences, Bio-Rad Laboratories, Tocris Bioscience, HD Biosciences Co., Ltd., Qiagen, Sienna Biopharmaceuticals, GenScript Biotech Corporation, Novo Nordisk, Takeda Pharmaceutical Company, AstraZeneca, and other players.

Recent Developments:

  • May 2025 – Novo Nordisk formed a strategic partnership worth USD 2.2 billion with Septerna to develop oral small-molecule medicines for obesity and associated cardiometabolic disorders. The alliance will initially be centered on four programs focused on G protein-coupled receptors (GPCRs), which include GLP-1, GIP, and glucagon receptors. Under the agreement, Septerna will collect more than USD 200 million in upfront and near-term payments, along with possible milestone-driven payments and royalties.

  • January 2025 – Isogenica, a global leader in the discovery of synthetic VHH antibodies, unveiled a strategic partnership with Cube Biotech, an expert in stabilized protein technologies. The partnership is to tackle one of drug discovery's most daunting fields—GPCR target engagement.

    G-Protein Coupled Receptors (GPCRs) Market Size, Share & Growth Report 2032

    Report Attributes

    Details

    Market Size in 2024

    USD 3.92 Billion 

    Market Size by 2032

    USD 6.04 Billion 

    CAGR

    CAGR of 5.59% From 2025 to 2032

    Base Year

    2024

    Forecast Period

    2025-2032

    Historical Data

    2021-2023

    Report Scope & Coverage

    Market Size, Segments Analysis, Competitive Landscape, Regional Analysis, DROC & SWOT Analysis, Forecast Outlook

    Key Segments

    • By Product (Cell Lines, Detection Kits, Cell Culture Reagents, Ligands)
    • By Assay Type (cAMP Functional Assays, Calcium Functional Assays, β-Arrestin Functional Assays, Radioligand Binding and GTPγS Functional Assays, Internalization Assays, Trafficking Assays)
    • By Application (Cancer Research, CNS Research, Metabolic Research, Cardiovascular Research, Inflammation Research, Respiratory Research, Other Applications [Ophthalmology, Immunology, Dermatology, etc.])
    • By End User (Pharmaceutical & Biotechnology Companies, Academic & Research Institutes, Contract Research Organizations [CROs])

    Regional Analysis/Coverage

    North America (US, Canada, Mexico), Europe (Germany, France, UK, Italy, Spain, Poland, Turkey, Rest of Europe), Asia Pacific (China, India, Japan, South Korea, Singapore, Australia, Rest of Asia Pacific), Middle East & Africa (UAE, Saudi Arabia, Qatar, South Africa, Rest of Middle East & Africa), Latin America (Brazil, Argentina, Rest of Latin America)

    Company Profiles

    The G-protein coupled receptors (GPCRs) market companies include Thermo Fisher Scientific, Merck KGaA, PerkinElmer, Abcam, Promega Corporation, BMG LABTECH, Eurofins Scientific, Isogenica, BD Biosciences, Qiagen, Enzo Life Sciences, Bio-Rad Laboratories, Tocris Bioscience, HD Biosciences Co., Ltd., Qiagen, Sienna Biopharmaceuticals, GenScript Biotech Corporation, Novo Nordisk, Takeda Pharmaceutical Company, AstraZeneca, and other players.