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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. Select targets shown - view more GPCR targets.

ADCYAP1R1 ADORA1 ADORA2A ADORA2B ADORA3
ADRA1A ADRA1B ADRA1D(82-572) ADRA2A ADRA2B
ADRA2C ADRB1 ADRB2 ADRB2(W158A) ADRB3
AGTR1 AGTRL1 AVPR1A AVPR1B AVPR2
AVPR2(S167T) BAI1 BAI2 BAI3 BDKRB1
BDKRB2 BRS3 C3AR1 C5AR1 C5L2
CALCR CALCRL-RAMP1 CALCRL-RAMP2 CALCRL-RAMP3 CALCR-RAMP2
CALCR-RAMP3 CASR CCKAR CCKBR CCR1
CCR10 CCR2 CCR3 CCR4 CCR5
CCR6 CCR7 CCR8 CCR9 CCRL1
CCRL2 cEDG5 cGPR91 CHRM1 CHRM2
CHRM3 CHRM4 CHRM5 CMKLR1 CNR1
CNR2 CRHR1 CRHR2 CRTH2 CX3CR1
CXCR1 CXCR2 CXCR3 CXCR4 CXCR5
CXCR6 CXCR7 cyno CXCR1 cyno CXCR2 cyno GPR120
cyno MRGPRX2 CYSLTR2 DARC DRD1 DRD2L
DRD2S DRD3 DRD4 DRD5 EBI2
EDG1 EDG2 EDG3 EDG4 EDG5
EDG6 EDG7 EDNRA EDNRB F2R
F2RL1 F2RL3 FFAR1 FFAR2 FFAR3
FPR1 FPR3 FPRL1 FSHR GABBR1-GABBR2
GALR1 GALR2 GCGR GHRHR GHSR
GHSR1b GIPR GLP1R GLP2R GNRHR
GPBAR1 GPR1 GPR101 GPR103 GPR107
GPR109A GPR109B GPR119 GPR12 GPR120
GPR120S GPR123 GPR132 GPR135 GPR137
GPR139 GPR141 GPR142 GPR143 GPR146
GPR148 GPR149 GPR15 GPR150 GPR151
GPR152 GPR157 GPR161 GPR162 GPR17
GPR171 GPR173 GPR176 GPR18 GPR182
GPR20 GPR22 GPR23 GPR25 GPR26
GPR27 GPR3 GPR30 GPR31 GPR32
GPR35 GPR37 GPR37L1 GPR39 GPR4
GPR45 GPR50 GPR52 GPR55 GPR6
GPR61 GPR65 GPR75 GPR78 GPR79
GPR81 GPR83 GPR84 GPR85 GPR88
GPR92 GPR97 GRM1 GRM2 GRM3
GRM4 GRM5 GRM6 GRPR HCRTR1
HCRTR2 HRH1 HRH2 HRH3 HRH4
HTR1A HTR1B HTR1E HTR1F HTR2A
HTR2B HTR2C HTR2C(VGV) HTR2C(VNV) HTR2C(VSV)
HTR5A HTR6 HTR7A HTR7B HTR7D
KISS1R LGR4 LGR5 LGR6 LHCGR
LTB4R mADCYAP1R1 mADORA2B mADORA3 mADRA1B
mAGTRL1 mAVPR2 mBRS3 MC1R MC3R
MC4R MC4R(T162I) mC5AR1 MC5R mCCKAR
mCCR1 mCCR2 mCCR3 mCCR4 mCCR5
mCCR6 mCCR7 mCCR8 mCCR9 MCHR1
MCHR2 mCMKLR1 mCNR1 mCNR2 mCRHR1
mCRTH2 mCX3CR1 mCXCR2 mCXCR3 mCXCR4
mCXCR5 mCXCR6 mCXCR7 mDRD5 mEBI2
mEDG1 mEDG3 mEDG5 mEDNRA mEDNRB
mF2RL1 mFFAR1 mFPR1 mFPR2 mGALR1
mGALR2 mGCGR mGHSR mGIPR mGLP1R
mGLP1R-ADCY2 mGPR1 mGPR120 mGPR84 mHCRTR1
mHTR2A mHTR2C MLNR mLTB4R mMC3R
mMC4R mMC5R mMCHR1 mNPY1R mNPY2R
mOPRD1 mOPRK1 mOPRM1 mOXTR mP2RY12
mP2RY6 mPPYR1 mPTAFR mPTGER4 mPTGIR
MRGPRD MRGPRE MRGPRF MRGPRX1 MRGPRX2
MRGPRX4 mRHO(P23H) mRXFP1 mRXFP3 mRXFP4
mSSTR2 mSSTR5 mTAAR1 mTACR1 MTNR1A
MTNR1B mUTR2 mVIPR1 NMBR NMU1R
NPBWR1 NPBWR2 NPFFR1 NPSR1b NPY1R
NPY2R NTSR1 OPN5 OPRD1 OPRK1
OPRL1 OPRM1 OXER1 OXGR1 OXTR
P2RY1 P2RY11 P2RY12 P2RY2 P2RY4
P2RY6 P2RY8 PPYR1 PRLHR PROKR1
PROKR2 PTAFR PTGDR PTGER1 PTGER2
PTGER3 PTGER4 PTGFR PTGIR PTHR1
PTHR2 rCHRM4 rCNR2 rCRTH2 rDRD1
rDRD2L rDRD2S rEDG5 rFFAR1 rGPR120
rGPR35 rHTR2C rOPRM1 rPROKR1 rPROKR2
rPTGER4 rTAAR1 rVIPR1 RXFP1 RXFP2
RXFP3 RXFP4 SCTR sEDG5 SMO(W535L)
SSTR1 SSTR2 SSTR3 SSTR4 SSTR5
TAAR1 TAAR5 TACR1 TACR2 TACR3
TBXA2R TRHR TSHR(L) UTR2 VIPR1
VIPR2 XCR1

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

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

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

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

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

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

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

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

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

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

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

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

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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