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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.

Featured Services:

Screening Platforms:

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

Ready GPCR Assays:

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.

Class
Ligand Type
GPCR Family
Receptor
Assay
A
 Non-peptide Acetylcholine (muscarinic) M1 / CHRM1
Ca2+, Radioligand
A
 Non-peptide Acetylcholine (muscarinic) M2 / CHRM2
Ca2+, Radioligand
A
 Non-peptide Acetylcholine (muscarinic) M3 / CHRM3
Ca2+, Radioligand
A
 Non-peptide Acetylcholine (muscarinic) M4 / CHRM4
Ca2+, Radioligand
A
 Non-peptide Acetylcholine (muscarinic) M5 / CHRM5
Ca2+, Radioligand
A
 Non-peptide Adenosine ADORA1
Ca2+
A
 Non-peptide Adenosine ADORA2A
Ca2+
A
 Non-peptide Adenosine ADORA2B
Ca2+
A
 Non-peptide Adenosine ADORA3
Ca2+
A
 Non-peptide Adrenoceptors ADRA1A
Ca2+, Radioligand
A
 Non-peptide Adrenoceptors ADRA1B
Ca2+, Radioligand
A
 Non-peptide Adrenoceptors ADRA1D
Ca2+, Radioligand
A
 Non-peptide Adrenoceptors ADRA2A
Ca2+
A
 Non-peptide Adrenoceptors ADRA2B
Ca2+
A
 Non-peptide Adrenoceptors ADRA2C
Ca2+
A
 Non-peptide Adrenoceptors ADRB1
Ca2+
A
 Non-peptide Adrenoceptors ADRB2
Ca2+, Radioligand
A
 Non-peptide Adrenoceptors ADRB3
Luciferase
A
 Peptide Anaphylotoxin C5a / C5AR1
Ca2+
A
 Peptide Angiotensin AT1
Ca2+
A
 Peptide Apelin AGTRL1
Ca2+
A
 Non-peptide Bile acid GPBAR1
Ca2+
A
 Peptide Bombesin BB1
Ca2+
A
 Peptide Bombesin BB2
Ca2+
A
 Peptide Bombesin BB3
Ca2+
A
 Peptide Bradykinin B1
Ca2+
A
 Peptide Bradykinin B2
Ca2+
A
 Non-peptide Cannabinoid CNR1 / CB1
Ca2+
A
 Non-peptide Cannabinoid CNR2 / CB2
Ca2+
A
 Peptide Chemoattractant ChemR23 / CMKLR1
Ca2+
A
 Peptide Cholecystokinin CCKA
Ca2+
A
 Peptide Cholecystokinin CCKB
Ca2+
A
 Non-peptide Dopamine D1 / DRD1
cAMP, Radioligand
A
 Non-peptide Dopamine D2 / DRD2
Ca2+
A
 Non-peptide Dopamine D2S / DRD2S
Ca2+, Radioligand
A
 Non-peptide Dopamine D4 / DRD4
cAMP
A
 Non-peptide Dopamine D5 / DRD5
Ca2+, Radioligand
A
 Peptide Endothelin EDNRA
Ca2+
A
 Peptide Endothelin EDNRB
Ca2+
A
 Non-peptide Free Fatty Acid FFA1 / GPR40
Ca2+
A
 Non-peptide Free Fatty Acid FFA2 / GPR43
Ca2+
A
 Peptide Galanin GAL1
Ca2+
A
 Peptide Galanin GAL2
Ca2+
A
 Peptide Ghrelin GHSR
Ca2+
A
 Peptide Gonadotropin-releasing Hormone GNRHR
Ca2+
A
 Non-peptide Histamine H1
Ca2+
A
 Non-peptide Histamine H2
Ca2+
A
 Non-peptide Histamine H3
Ca2+
A
 Non-peptide Histamine H4
Ca2+
A
 Peptide KiSS1-derived Peptide KiSS1 / GPR54
Ca2+
A
 Non-peptide Leukotriene CysLT1
Ca2+
A
 Non-peptide Leukotriene CysLT2
Ca2+
A
 Non-peptide Leukotriene LTB4
Ca2+
A
 Non-peptide Lysophospholipid EDG3 / S1P3
Ca2+
A
 Non-peptide Lysophospholipid EDG4 / LPA2
Ca2+
A
 Non-peptide Lysophospholipid EDG6 / S1P4
Ca2+
A
 Peptide Melanin-concentrating Hormone MCH1
Ca2+
A
 Peptide Melanin-concentrating Hormone MCH2
Ca2+
A
 Peptide Melanocortin MC2
Ca2+
A
 Peptide Melanocortin MC3
Ca2+, Luciferase
A
 Peptide Melanocortin MC4
Ca2+
A
 Peptide Melanocortin MC5
Ca2+
A
 Peptide Melatonin MT1
Ca2+
A
 Peptide Melatonin MT2
Ca2+
A
 Peptide Motilin MTLR
Ca2+
A
 Peptide Neuromedin U NMU1
Ca2+
A
 Peptide Neuromedin U NMU2
Ca2+
A
 Peptide Neuropeptide B/W NPBW1 / GPR7
Ca2+
A
 Peptide Neuropeptide FF NPFF1 / GPR147
Ca2+
A
 Peptide Neuropeptide FF NPFF2 / GPR74
Ca2+
A
 Peptide Neuropeptide S NPS1a
Ca2+
A
 Peptide Neuropeptide S NPS1b
Ca2+
A
 Peptide Neuropeptide Y NPY1
Ca2+, cAMP
A
 Peptide Neuropeptide Y NPY2
Ca2+
A
 Peptide Neuropeptide Y NPY4 / PPYR1
Ca2+
A
 Peptide Neurotensin NTS1
Ca2+
A
 Non-peptide Nicotinic Acid NIACR1 / GPR109A
Ca2+
A
 Peptide N-Formyl Peptide FPR1
Ca2+
A
 Peptide N-Formyl Peptide FPRL1
Ca2+
A
 Peptide Opioid OPRD1
Ca2+, Radioligand
A
 Peptide Opioid OPRK1
Ca2+
A
 Peptide Opioid OPRL1
Ca2+
A
 Peptide Opioid OPRM1
Ca2+
A
 Peptide Orexin OX1
Ca2+
A
 Peptide Orexin OX2
Ca2+
A
 Peptide Oxytocin OT / OXTR
Ca2+
A
 Peptide Peptide P518 GPR103
Ca2+
A
 Non-peptide Platelet Activating Factor PAF / PTAFR
Ca2+
A
 Peptide Prolactin Releasing Peptide PRLHR
Ca2+
A
 Non-peptide Prostanoid DP1 / PTGDR
Ca2+
A
 Non-peptide Prostanoid DP2 / GPR44
Ca2+
A
 Non-peptide Prostanoid FP / PTGFR
Ca2+
A
 Non-peptide Prostanoid EP1 / PTGER1
Ca2+
A
 Non-peptide Prostanoid EP2 / PTGER2
Ca2+
A
 Non-peptide Prostanoid IP1 / PTGIR
Ca2+
A
 Non-peptide Prostanoid TP / TBXA2R
Ca2+
A
 Peptide Proteinase-activated Receptor PAR2 / F2RL1
Ca2+
A
 Peptide Proteinase-activated Receptor PAR4 / F2RL3
Ca2+
A
 Non-peptide Proton-sensor GPR68
Ca2+
A
 Non-peptide Purinergic P2Y1
Ca2+
A
 Non-peptide Purinergic P2Y2
Ca2+
A
 Non-peptide Purinergic P2Y4
Ca2+
A
 Non-peptide Purinergic P2Y6
Ca2+
A
 Non-peptide Purinergic P2Y11
Ca2+
A
 Non-peptide Purinergic P2Y12
Ca2+
A
 Non-peptide Serotonin 5-HT1A / HTR1A
Ca2+, Radioligand
A
 Non-peptide Serotonin 5-HT2A / HTR2A
Ca2+
A
 Non-peptide Serotonin 5-HT2B / HTR2B
Ca2+
A
 Non-peptide Serotonin 5-HT2C / HTR2C
Ca2+, Radioligand
A
 Non-peptide Serotonin 5-HT4 / HTR4
Ca2+
A
 Non-peptide Serotonin 5-HT7 / HTR7
cAMP, Radioligand
A
 Peptide Somatostatin SST1
Ca2+
A
 Peptide Somatostatin SST2
Ca2+
A
 Peptide Somatostatin SST3
Ca2+
A
 Peptide Somatostatin SST4
Ca2+
A
 Peptide Somatostatin SST5
Ca2+
A
 Peptide Tachykinin NK1 / TACR1
Ca2+
A
 Peptide Tachykinin NK2 / TACR2
Ca2+
A
 Peptide Tachykinin NK3 / TACR3
Ca2+
A
 Peptide Thyrtropin-releasing Hormone TRH1
Ca2+
A
 Peptide Urotensin UT2
Ca2+
A
 Peptide Vasopressin V1A / AVPR1A
Ca2+
A
 Peptide Vasopressin V1B / AVPR1B
Ca2+, Radioligand
A
 Peptide Vasopressin V2 / AVPR2
Ca2+, Radioligand
A
   Orphan GPR120
Ca2+
A
   Orphan MRGD / MRGPRD
Ca2+
A
   Orphan MRGX2 / MRGPRX2
Ca2+
A
   Orphan P2Y5
Ca2+
A
   Orphan SUCNR1 / GPR91
Ca2+
B
 Peptide Calcitonin CALCR / CT
Ca2+
B
 Peptide Calcitonin AMY1 (RAMP1 + CALCR)
Ca2+
B
 Peptide Calcitonin AMY2 (RAMP2 + CALCR)
Ca2+
B
 Peptide Calcitonin AMY3 (RAMP3 + CALCR)
Ca2+
B
 Peptide Calcitonin AM1 (RAMP2 + CALCRL)
Ca2+
B
 Peptide Calcitonin AM2 (RAMP3 + CALCRL)
Ca2+
B
 Peptide Corticotropin Releasing Factor CRF1
Ca2+
B
 Peptide Corticotropin Releasing Factor CRF2
Ca2+
B
 Peptide Glucagon GCGR
Ca2+
B
 Peptide Glucagon GHRH
Ca2+
B
 Peptide Glucagon GLP1
Ca2+
B
 Peptide Glucagon GLP2
Ca2+
B
 Peptide Glucagon SCTR
Ca2+
B
 Peptide Parathyroid Hormone PTH1
Ca2+
B
 Peptide Parathyroid Hormone PTH2
Ca2+
B
 Peptide VIP / PACAP PAC1
Ca2+
B
 Peptide VIP / PACAP VPAC1
Ca2+
B
 Peptide VIP / PACAP VPAC2
Ca2+
C
 Non-peptide Calcium-sensor CASR
Ca2+
C
 Non-peptide Glutamate mGlu2 / GRM2
Ca2+
C
 Non-peptide Glutamate mGlu3 / GRM3
Ca2+
Non-peptide Sigma Sigma-2
Radioligand

Quotations and Ordering:

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

  • For fluorescence-based platform, please download the Quotation;

  • For radioisotope-based platform, please download the Quotation;

To order, please send the completed Quotation Form to us by email or fax with a formal PO (Purchase Order) or credit card information. You can also submit PO/credit card information 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.

Email: bioassay@genscript.com
Phone: 1-877-436-7274 (Toll-Free), 1-732-885-9188
Fax: 1-732-210-0262, 1-732-885-5878