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GPCR Target Solutions

GPCR Target Solutions

G protein-coupled receptors (GPCRs), also known as seven-transmembrane domain receptors, comprise a superfamily of transmembrane receptors that sense extracelluar signal molecule and activate intracellular signaling pathway and, ultimately cellular response. GPCR is the largest known category of molecular targets with verified therapeutic value. Up to 40% of approved drugs are targeted to GPCRs. Among them, Clopidogrel and Olanzapine are two representative block-buster drugs. GPCRs still take up a significant share of drug development pipeline across the pharmaceutical industry.

In GPCR drug discovery, high throughput screening (HTS) is the essential tool to find drug candidates from the compound libraries. GenScript has developed fluorescence-based and radioisotope-based platforms to offer flexible solutions for your high throughput screening and profiling services.

Features:

Screening Platforms:

Platform
Instrument
Assay
Comment
FLIPRTetra®, FlexStation® 3, EnVison®, PHERAstar Plus
Calcium, cAMP, IP1, or reporter gene
Functional cell-based assay
TopCount®
Filtration or SPA
Binding assay

GPCR Assay Services and Products:

With the largest GPCR stable cell line collection, GenScript offers comprehensive GPCR assay services and products for your GPCR-based drug discovery and development.

Please feel free to contact us for more technical supports.

Class
Ligand Type
GPCR Family
Receptor
Cell Line
Membrane
A
Non-peptide Acetylcholine (muscarinic) M1 / CHRM1
A
Non-peptide Acetylcholine (muscarinic) M2 / CHRM2
A
Non-peptide Acetylcholine (muscarinic) M3 / CHRM3
A
Non-peptide Acetylcholine (muscarinic) M4 / CHRM4
A
Non-peptide Acetylcholine (muscarinic) M5 / CHRM5
A
Non-peptide Adenosine ADORA1  
A
Non-peptide Adenosine ADORA2A  
A
Non-peptide Adenosine ADORA2B  
A
Non-peptide Adenosine ADORA3
M00464
 
A
Non-peptide Adrenoceptors ADRA1A
A
Non-peptide Adrenoceptors ADRA1B
A
Non-peptide Adrenoceptors ADRA1D
A
Non-peptide Adrenoceptors ADRA2A  
A
Non-peptide Adrenoceptors ADRA2B
M00454
 
A
Non-peptide Adrenoceptors ADRA2C  
A
Non-peptide Adrenoceptors ADRB1  
A
Non-peptide Adrenoceptors ADRB2
A
Non-peptide Adrenoceptors ADRB3
A
Peptide Anaphylotoxin C5a / C5AR1  
A
Peptide Angiotensin AT1  
A
Peptide Apelin AGTRL1  
A
Non-peptide Bile acid GPBAR1  
A
Peptide Bombesin BB1 / NMBR  
A
Peptide Bombesin BB2 / GRPR  
A
Peptide Bombesin BB3 / BRS3  
A
Peptide Bradykinin B1 / BDKRB1  
A
Peptide Bradykinin B2 / BDKRB2  
A
Non-peptide Cannabinoid CNR1 / CB1  
A
Non-peptide Cannabinoid CNR2 / CB2  
A
Peptide Chemoattractant ChemR23 / CMKLR1  
A
Peptide Cholecystokinin CCKA  
A
Peptide Cholecystokinin CCKB  
A
Non-peptide Dopamine D1 / DRD1
M00408
A
Non-peptide Dopamine D2 / DRD2  
A
Non-peptide Dopamine D2S / DRD2S
A
Non-peptide Dopamine D5 / DRD5
A
Peptide Endothelin EDNRA  
A
Peptide Endothelin EDNRB  
A
Non-peptide Free Fatty Acid FFA1 / GPR40  
A
Non-peptide Free Fatty Acid FFA2 / GPR43  
A
Peptide Galanin GAL1  
A
Peptide Galanin GAL2  
A
Peptide Ghrelin GHSR  
A
Peptide Gonadotropin-releasing Hormone GNRHR  
A
Non-peptide Histamine H1  
A
Non-peptide Histamine H2  
A
Non-peptide Histamine H3  
A
Non-peptide Histamine H4  
A
Peptide KiSS1-derived Peptide KiSS1 / GPR54  
A
Non-peptide Leukotriene CysLT1
M00462
 
A
Non-peptide Leukotriene CysLT2  
A
Non-peptide Leukotriene LTB4  
A
Non-peptide Lysophospholipid EDG4 / LPA2
M00463
 
A
Peptide Melanin-concentrating Hormone MCH1  
A
Peptide Melanin-concentrating Hormone MCH2  
A
Peptide Melanocortin MC2  
A
Peptide Melanocortin MC3  
A
Peptide Melanocortin MC4  
A
Peptide Melanocortin MC5  
A
Peptide Melatonin MT1 / MTNR1A  
A
Peptide Melatonin MT2 / MTNR1B  
A
Peptide Motilin MTLR  
A
Peptide Neuromedin U NMU1  
A
Peptide Neuromedin U NMU2  
A
Peptide Neuropeptide B/W NPBW1 / GPR7
M00452
 
A
Peptide Neuropeptide FF NPFF1 / GPR147  
A
Peptide Neuropeptide S NPS1a  
A
Peptide Neuropeptide S NPS1b  
A
Peptide Neuropeptide Y NPY2  
A
Peptide Neuropeptide Y NPY4 / PPYR1  
A
Peptide Neurotensin NTS1  
A
Non-peptide Nicotinic Acid NIACR1 / GPR109A  
A
Peptide N-Formyl Peptide FPR1  
A
Peptide N-Formyl Peptide FPRL1  
A
Peptide Opioid OPRD1
A
Peptide Opioid OPRK1
A
Peptide Opioid OPRL1  
A
Peptide Opioid OPRM1  
A
Peptide Orexin OX1  
A
Peptide Orexin OX2  
A
Peptide Oxytocin OT / OXTR
M00468
A
Peptide Peptide P518 GPR103  
A
Non-peptide Platelet Activating Factor PAF / PTAFR  
A
Peptide Prolactin Releasing Peptide PRLHR  
A
Non-peptide Prostanoid DP1 / PTGDR
M00453
 
A
Non-peptide Prostanoid DP2 / GPR44  
A
Non-peptide Prostanoid FP / PTGFR  
A
Non-peptide Prostanoid EP1 / PTGER1  
A
Non-peptide Prostanoid EP2 / PTGER2  
A
Non-peptide Prostanoid IP1 / PTGIR