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GPCR Assay Services

GPCR, G protein-coupled receptor, is the largest known category of molecular targets with verified therapeutic value. It is comprised of approximately 600–1000 members. Currently, a great percentage of pharmaceutical drugs targets GPCRs for treatment of many diseases such as pain, asthma, hypertension, as well as immunological and neurological disorders.

To meet the demands of GPCR screening and profiling, GenScript not only provides a comprehensive collection of GPCR and parental cell lines, but also is able to construct any GPCR cell line through customization. Coupled with our advanced instrumentation and versatile assay platforms, GenScript brings a total solution for your biochemical and cell-based GPCR assays and speed up your drug discovery.

To expedite your drug discovery process, GenScript offers a variety of stable cell line products in our catalog, and a comprehensive collection of custom reagent services for gene, protein, peptide, and antibody.

Cat. No. Service
Price (USD)
Custom GPCR Assay Services

Assay Setup Showcases:

Fig1. Shown above are intracellular calcium responses from CHO-K1 cells stably expressing human NK3 Neurokinin receptors and from untransfected control cells. Cells were loaded with Calcium-4 and then stimulated with the indicated concentrations of Neurokinin B. Calcium responses were recorded on a FlexStation plate reader. Data represent the average +/- standard deviation of triplicate determinations.   Fig2. Shown above are the intracellular calcium responses of CHO-K1 cells stably expressing human arginine vasopressin receptor 1B and of untransfected control cells. Cells were loaded with Calcium-4 and then stimulated with the indicated concentrations of arginine vasopressin (AVP). Calcium responses were recorded on a FlexStation plate reader. Data represent the average +/- standard deviation of triplicate determinations.

Catalog GPCR Assay:

GenScript is continuously developing more GPCR catalog assays, utilizing various readouts such as Ca2+ flux, FRET, and luminescence, to cater the different needs of our customers. We constantly update our catalog assay list. However, for instances that your specific target(s) or readouts cannot be found within the list below, please feel free to contact our customer representatives and we'll provide a customized solution to your research.

All stable cell lines used in our GPCR screening/profiling services are available to purchase as catalog products. *Click here to know more*.

Assay Readout
Ligand Type
GPCR Family
Ca2+ flux
Non-peptide Acetylcholine (muscarinic) M1 Agonist    
Non-peptide Acetylcholine (muscarinic) M3 Agonist    
Non-peptide Acetylcholine (muscarinic) M5 Agonist    
Non-peptide Adenosine A1 Agonist    
Non-peptide Adrenoceptors ADRA1A Agonist    
Non-peptide Adrenoceptors ADRA1B Agonist    
Non-peptide Adrenoceptors ADRB1 Agonist    
Non-peptide Adrenoceptors ADRB2 Agonist    
Peptide Bombesin BB2 Agonist    
Peptide Bombesin BB3 Agonist    
Peptide Bradykinin B2 Agonist    
Peptide Calcitonin CALCR Agonist    
Peptide Chemoattractant CMKLR1 Agonist    
Peptide Cholecystokinin CCKA Agonist    
Peptide Cholecystokinin CCKB Agonist    
Peptide Corticotropin Releasing Factor CRF2 Agonist    
Non-peptide Dopamine D2 Agonist    
Non-peptide Dopamine D2S Agonist    
Peptide Endothelin EDNRA Agonist    
Peptide Endothelin EDNRB Agonist    
Non-peptide Free Fatty Acid FFA1/GPR40 Agonist Agonist  
Peptide Galanin GAL1 Agonist    
Peptide Galanin GAL2 Agonist    
Peptide Ghrelin GHSR Agonist    
Peptide Gonadotropin-Releasing Hormone GnRH   Agonist  
Non-peptide Histamine H1 Agonist    
Non-peptide Histamine H2 Agonist   Agonist
Non-peptide Histamine H3 Agonist    
Non-peptide Histamine H4 Agonist    
Peptide Melanin-concentrating Hormone MCH1 Agonist    
Peptide Melanin-concentrating Hormone MCH2 Agonist    
Peptide Melanocortin MC4 Agonist    
Peptide Neuromedin U NMU1 Agonist    
Peptide Neuropeptide GPR103 Agonist    
Peptide Neurotensin NTS1 Agonist    
Peptide N-Formyl Peptide FPRL1 Agonist    
Peptide Opioid OPRK1 Agonist    
Peptide Opioid OPRM1 Agonist    
Peptide Orexin OX1 Agonist    
Peptide Orexin OX2 Agonist    
Peptide Oxytocin OT/OXTR Agonist    
Peptide Parathyroid Hormone PTH1   Agonist  
Peptide Parathyroid Hormone PTH2   Agonist  
Non-peptide Platelet Activating Factor PAF/PTAFR Agonist    
Non-peptide Prostanoid FP Agonist    
Non-peptide Prostanoid IP1 Agonist    
Non-peptide Prostanoid PTGER1 Agonist    
Non-peptide Prostanoid PTGER2 Agonist    
Non-peptide Prostanoid TP Agonist    
Peptide Proteinase-activated Receptor PAR4 Agonist    
Non-peptide Serotonin 5-HT2A Agonist    
Non-peptide Serotonin 5-HT2B Agonist    
Non-peptide Serotonin 5-HT2C Agonist    
Peptide Somatostatin SST3 Agonist    
Peptide Somatostatin SST5 Agonist    
Non-peptide Purinergic P2Y2 Agonist    
Non-peptide Purinergic P2Y4 Agonist    
Non-peptide Purinergic P2Y11 Agonist    
Peptide Tachykinin NK1 Agonist    
Peptide Tachykinin NK2 Agonist    
Peptide Tachykinin NK3 Agonist    
Peptide Thyrtropin-releasing Hormone TRH1 Agonist    
Peptide Vasopressin V1A Agonist    
Peptide Vasopressin V1B Agonist    
Peptide Vasopressin V2 Agonist    

Quotations and Ordering:

To request a quotation, please download and complete the and send it back by email or fax.

To order, please send the completed Quotation Form to us by email or fax with a formal PO (Purchase Order) . You can also submit PO by phone or via our Secure Online Messaging System.

Our customer service representatives are available 24 hours a day, Monday through Friday to assist you.

Phone: 03-6803-0843
Fax:0303-3836-0371, 03-4496-5000(only for order)