GPCR Targets By Therapeutic/Disease Area

DiscoveRx offers the the largest commercial portfolio of GPCR assay solutions for multiple therapeutic and disease areas.  Use the links below to browse our GPCR portfolio by therapeutic area.


ADORA1 ADORA2A ADORA2B ADORA3 ADRB1
ADRB2 ADRB3 BDKRB1 BDKRB2 BRS3
C5L2 CCKAR CCKBR CCR1 CCR10
CCR2 CCR3 CCR4 CCR5 CCR6
CCR7 CCR8 CCR9 CHRM1 CHRM2
CHRM3 CHRM4 CHRM5 CNR1 CNR2
CRHR1 CRHR2 CX3CR1 CXCR1 CYSLTR2
DRD1 DRD3 DRD4 DRD5 EDG2
EDG3 EDG4 EDG8 EDNRA EDNRB
FPR1 FPRL1 GPR119 GPR55 GRM2
GRM3 GRPR HCRTR2 HRH1 HRH2
HRH3 HTR1A HTR2A HTR2C HTR6
NMU1R NPBWR2 OPRD1 OPRK1 OPRL1
P2RY1 PRLHR PTGDR PTGER1 PTGER2
PTGER3 PTGER4 PTHR2 TACR2 TACR3
VIPR2 XCR1
Cancer Research

Cancer Research

Epigenetic, Kinase, Pathway, GPCR and NHR Functional Cellular Assays for Novel Therapeutic Discovery
Development of both small and large molecule inhibitors that target cellular signaling modalities involved in tumor growth, angiogenesis, cancer progression and metastasis are inherent in anticancer treatments, resulting in novel therapeutic approaches for cancer prevention and treatment.

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CNS Research

CNS Research

Epigenetic, Kinase, Pathway, GPCR and NHR Functional Cellular Assays for Novel Therapeutic Discovery
The rapid expansion of CNS drug discovery efforts is associated with an increase in neurological and psychiatric conditions in the growing geriatric population. While small molecules targeting extracellular receptors represent more than 80% of commercially available CNS-related drugs, considerable advancements have also been made in the development of antibodies, vaccines, aptamers, small interfering RNA, and other biologics for the treatment of Alzheimers, Parkinson’s, Multiple Sclerosis and other CNS disorders.

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Inflammation Research

Inflammation Research

Epigenetic, Kinase, Pathway, GPCR and NHR Functional Cellular Assays for Novel Therapeutic Discovery
Inflammatory diseases are slow to onset and chronic in nature and can lead to a host of debilitating diseases, such as rheumatoid arthritis, inflammatory bowel disease, Crohn’s disease, psoriasis, atherosclerosis and even cancer. As the molecular mechanisms that regulate functional inflammatory responses are now better understood, drug discovery programs are focused on developing highly efficacious anti-inflammatory therapeutics that show the least amount of side effects over prolonged treatment periods.

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Metabolic Research

Metabolic Research

GPCR, Kinase, Pathway, NHR and Protease Functional Cellular Assays for Novel Therapeutic Discovery
The increased prevalence of obesity, Type II diabetes and associated complications has become an alarming global health problem. G-Protein Coupled Receptors (GPCRs), Kinases, Nuclear Hormone Receptors (NHRs) and Proteases are important therapeutic drug targets for metabolic research as these receptors play a pivotal role in the regulation of insulin and glucagon secretion. Therefore, novel pharmacologic approaches are required to develop fast acting and efficacious compounds that can modulate the ways in which the body controls metabolism, weight gain and body composition.

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Cardiovascular Research

Cardiovascular Research

GPCR, Kinase, Pathway, NHR and Protease Functional Cellular Assays for Novel Therapeutic Discovery
Cardiovascular diseases (CVDs) are the number one cause of death worldwide, with more people dying each year from CVDs than from any other cause, including cancer. Because a wide variety of conditions can lead to heart disease including atherosclerosis, heart infections and structural or congenital defects, cardiovascular drug development programs are often quite complex and require multidisciplinary approaches. Now more than ever, novel pharmacological strategies that target specific receptors or proteins of interest involved in CVDs are required for the safe and effective treatment and prevention of cardiovascular disease.

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Respiratory Research

Respiratory Research

GPCR, Kinase, Pathway, NHR and Protease Functional Cellular Assays for Novel Therapeutic Discovery
Chronic respiratory diseases that arise from infectious agents, environmental pollutants, smoking or allergic reactions represent a major public health challenge in both industrialized and developing countries. Although several blockbuster drugs already exist that ease symptoms and improve the quality of life in patients suffering from these diseases, drug discovery programs continue to focus on the development of small molecules and other biologics against therapeutic targets for the treatment of asthma, chronic obstructive pulmonary disease (COPD) and lung cancer.

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Pain and Addiction Research

Pain and Addiction Research

GPCR, Kinase, Pathway and NHR Functional Cellular Assays for Novel Therapeutic Discovery
The combination of chronic pain and addiction is a complex, debilitating medical disorder that is extremely difficult to treat due to the high likelihood of opioid dependence. Recent advances in chronic pain research have uncovered the biological complexity of the disorder and led to the development of next generation non-steroidal anti-inflammatory drugs, antidepressants and anticonvulsant drugs to mitigate chronic pain. Researchers are now focused on developing small molecule and other biologics to target widely expressed pain receptors aimed at not only alleviating pain but also lessening abuse potential of opiod drugs.

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Digestive and Renal Research

Digestive and Renal Research

GPCR, Kinase, Pathway and NHR Functional Cellular Assays for Novel Therapeutic Discovery
Genetic and environmental factors that disrupt homeostatic digestive and renal processes can result in chronic kidney disease and/or kidney failure, glomerulonephritis, Celiac & Crohn’s diseases and more. G-Protein Coupled Receptors (GPCRs), Kinases and Nuclear Hormone Receptors (NHRs) expressed in renal and digestive tissues represent the most tractable targets for development of small and large molecule drugs that alleviate and prevent urological and metabolic abnormalities.

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Reproductive Research

Reproductive Research

GPCR, Kinase and NHR Functional Cellular Assays for Novel Therapeutic Discovery
The reproductive system coordinates signaling pathways in many different cell types which leads to oogenesis and spermatogenesis, ovulation, implantation, menstruation and ultimately childbirth. Precise control of this cellular communication and signaling is critical for normal development and fertility in humans. G-Protein Coupled Receptors (GPCRs), Kinases and Nuclear Hormone Receptors (NHRs) are important therapeutic targets for reproductive drug discovery as these receptors play key physiological roles and their dysfunction underlies many pathological conditions related to infertility and disease.

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Dermatology Research

Dermatology Research

GPCR, Kinase, Pathway and NHR Functional Cellular Assays for Novel Therapeutic Discovery
Skin is the largest organ in the body, susceptible to environmental stresses that can lead to early onset of aging and other conditions such as dermatitis, eczema, psoriasis, rosacea, alopecia, and even cancer. As the role of the skin (dermis) in whole body wellness becomes better defined, interest has grown in developing safe and efficacious therapeutics that combat disease processes and/or reverse age related ailments without the need for more invasive surgical treatment.

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Post-Traumatic Stress Disorder Research

Post-Traumatic Stress Disorder Research

GPCR, Kinase, Pathway and NHR Functional Cellular Assays for Novel Therapeutic Discovery
Post-Traumatic Stress Disorder Research (PTSD) is a severe anxiety disorder that develops following a psychologically traumatizing event. Largely ineffective antidepressants and anti-anxiety medications target glucocorticoid pathway, but do not treat the disorder. Researchers have studied genes encoding brain’s fear circuits, especially focusing on GPCRs, Kinases and NHRs as important therapeutic signaling modalities that regulate responses to fear and stress. For example, researchers have recently uncovered specific neurobiological differences including lower levels of Serotonin 1B in the brains of people who have PTSD and those who do not.

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Ocular Research

Ocular Research

GPCR, Kinase and Pathway Functional Cellular Assays for Novel Therapeutic Discovery
Eye-related pathologies such as inflammation, agerelated macular degeneration (AMD), diabetic retinopathy, cataracts or glaucoma affect millions of people worldwide and can result in long term vision loss. G-Protein Coupled Receptors (GPCRs), Kinases and Pathways have emerged as important therapeutic targets for ophthalmology drug discovery as these receptors are expressed in the eye and have a wide range of physiological functions.

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Auditory and Otology Research

Auditory and Otology Research

GPCR, Kinase, Pathway and NHR Functional Cellular Assays for Novel Therapeutic Discovery
Recent advances in auditory and otological research have led to a greater understanding of the molecular and physiologic basis for hearing loss. This has enabled novel discoveries in the area of ototoxicity as well as prospected the development of new and improved therapeutic options for patients in the treatment of ear disorders. G-protein Coupled Receptors (GPCRs), Kinases and Nuclear Hormone Receptors (NHRs) are widely expressed in the sensory system and targeted for development of safe and efficacious therapies to prevent degenerative hearing loss, inner ear disease, and long term damage from noise and our environment.

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