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Therapeutic GPCR Panels

Functional GPCR assays grouped by therapeutic area

DiscoveRx offers a number of focused therapeutic area assay panels that may be used to broadly screen for new leads or profile compounds of interest.  These panels are organized based on current scientific understanding and are updated regularly.  Listed below are the GPCR therapeutic panels available for screening and profiling.

Available Therapeutic Panels

Cancer Panel
Cardiovascular Panel
Chemokine Panel
Digestive & Renal Panel
Inflammation Panel
Metabolic Panel
Neurological Panel
Psychiatric Disorders Panel
Reproduction Panel
Respiratory Panel
Sensory Panel

Cancer Panel

G-protein coupled receptors (GPCRs), Kinases and Nuclear Hormone Receptors (NHRs) are the largest and most diverse classes of receptors that are involved in tumor growth, angiogenesis, cancer progression and metastasis. Development of both small and large molecule inhibitors (e.g. monoclonal antibodies) that target these extracellular receptors and interfere with normal receptor signaling and cell function can result in novel therapeutic approaches for cancer prevention and treatment.

Cardiovascular Panel

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.

Chemokine Panel

Chemokine receptors and their associated ligands play a key role in both normal and pathological conditions. Understanding their regulatory roles in various disease states such as allergic reactions, cardiovascular disease, metabolic syndromes, sepsis and cancer is critical to the development of safe and efficacious therapeutics. Our complete panel of chemokine receptors utilizes a single common assay readout to rapidly, reliably and reproducibly screen and profile compounds

Digestive & Renal Panel

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) 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.

Inflammation Panel

Inflammatory diseases are often characterized by slow onset, are typically chronic in nature and often 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.

Metabolic Panel

The increased prevalence of obesity, Type II diabetes and associated complications has become an alarming global health problem. G-Protein Coupled Receptors (GPCRs) 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.

Neurological Panel

The rapid expansion of CNS drug discovery efforts are 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, siRNA, and other biologics for the treatment of Alzheimers, Parkinson's, Multiple Sclerosis and other CNS disorders.

Psychiatric Disorders Panel

Psychiatric disorders can have a profound effect on one's ability to function and interact in society and has received increasing attention as a focus for therapeutic intervention. Successful approaches targeting dopamine and serotonin receptors have led to the development of antidepressant medications that treat mood disorders, major depression anxiety and obsessive compulsive disorders. Although widely prescribed, current therapeutics address a narrow range of disorders, vary in efficacy and are often associated have adverse effects. DiscoveRx offers a growing panel of GPCR targets important for discovery of novel psychiatric therapeutics.

Reproduction Panel

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) 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.

Respiratory Panel

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 respiratory targets for the treatment of asthma, chronic obstructive pulmonary disease (COPD) and lung cancer.

Sensory Panel

Basic research into the etiology and dysregulation of molecular pathways associated with sensory disorders, such as those of ocular, dermatologic and olfactory, receptors is growing rapidly as recognition of their impact beyond 'quality of life' issues is elucidated and implication in other disease processes is recognized.