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) |
SC1402 |
Custom GPCR Assay Services |
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Assay Setup Showcases:
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| 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. |
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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. |
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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.
|
Class |
Ligand Type |
GPCR Family |
Receptor |
Functional Assay |
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 |
Adrenoceptors |
ADRA1A |
|
A |
Non-peptide |
Adrenoceptors |
ADRA1B |
|
A |
Non-peptide |
Adrenoceptors |
ADRA1D |
|
A |
Non-peptide |
Adrenoceptors |
ADRA2A |
|
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 |
AT2 |
Ca2+ |
A |
Peptide |
Apelin |
AGTRL1 |
|
A |
Non-peptide |
Bile acid |
GPBAR1 |
|
A |
Peptide |
Bombesin |
BB1 |
|
A |
Peptide |
Bombesin |
BB2 |
|
A |
Peptide |
Bombesin |
BB3 |
|
A |
Peptide |
Bradykinin |
B2 |
|
B |
Peptide |
Calcitonin |
CALCR |
|
A |
Non-peptide |
Cannabinoid |
CNR1 / CB1 |
|
A |
Peptide |
Chemoattractant |
CMKLR1 |
|
A |
Peptide |
Cholecystokinin |
CCKA |
|
A |
Peptide |
Cholecystokinin |
CCKB |
|
B |
Peptide |
Corticotropin Releasing Factor |
CRF1 |
|
B |
Peptide |
Corticotropin Releasing Factor |
CRF2 |
|
A |
Non-peptide |
Dopamine |
D1 / DRD1 |
|
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 |
GPR120 |
Ca2+ |
A |
Non-peptide |
Free Fatty Acid |
FFA1 / GPR40 |
|
A |
Non-peptide |
Free Fatty Acid |
FFA2 / GPR43 |
Ca2+ |
A |
Peptide |
Galanin |
GAL1 |
|
A |
Peptide |
Galanin |
GAL2 |
|
A |
Peptide |
Ghrelin |
GHSR |
|
B |
Peptide |
Glucagon |
GCGR |
Ca2+ |
B |
Peptide |
Glucagon |
GHRH |
|
B |
Peptide |
Glucagon |
GLP2 |
|
B |
Peptide |
Glucagon |
SCTR |
|
C |
Non-peptide |
Glutamate |
mGlu2 / GRM2 |
Ca2+ |
A |
Peptide |
Gonadotropin-releasing Hormone |
GNRHR |
Ca2+ |
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 |
LTB4 |
Ca2+ |
A |
Non-peptide |
Mas-related gene |
MRGX2 / MRGPRX2 |
Ca2+ |
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 |
Ca2+ |
A |
Peptide |
Melatonin |
MT2 |
|
A |
Peptide |
Motilin |
MTLR |
Ca2+ |
A |
Peptide |
Neuromedin U |
NMU1 |
|
A |
Peptide |
Neuropeptide FF |
NPFF1 / GPR147 |
Ca2+ |
A |
Peptide |
Neuropeptide S |
NPS1a |
|
A |
Peptide |
Neuropeptide S |
NPS1b |
Ca2+ |
A |
Peptide |
Neuropeptide Y |
NPY1 |
Ca2+ |
A |
Peptide |
Neuropeptide Y |
NPY4 / PPYR1 |
Ca2+ |
A |
Peptide |
Neurotensin |
NTS1 |
|
A |
Non-peptide |
Nicotinic Acid |
GPR109A |
Ca2+ |
A |
Peptide |
N-Formyl Peptide |
FPR1 |
Ca2+ |
A |
Peptide |
N-Formyl Peptide |
FPRL1 |
|
A |
Peptide |
Opioid |
OPRD1 |
|
A |
Peptide |
Opioid |
OPRK1 |
|
A |
Peptide |
Opioid |
OPRM1 |
|
A |
Peptide |
Orexin |
OX1 |
Ca2+ |
A |
Peptide |
Orexin |
OX2 |
|
A |
Peptide |
Oxytocin |
OT / OXTR |
|
B |
Peptide |
Parathyroid Hormone |
PTH1 |
Ca2+ |
B |
Peptide |
Parathyroid Hormone |
PTH2 |
|
A |
Peptide |
Peptide P518 |
GPR103 |
|
A |
Non-peptide |
Platelet Activating Factor |
PAF / PTAFR |
|
A |
Peptide |
Prolactin Releasing Peptide |
PRLHR |
|
A |
Non-peptide |
Prostanoid |
DP2 / GPR44 |
Ca2+ |
A |
Non-peptide |
Prostanoid |
FP / PTGFR |
|
A |
Non-peptide |
Prostanoid |
EP1 / PTGER1 |
|
A |
Non-peptide |
Prostanoid |
EP2 / PTGER2 |
|
A |
Non-peptide |
Prostanoid |
IP1 / PTGIR |
|
A |
Non-peptide |
Prostanoid |
TP / TBXA2R |
|
A |
Peptide |
Proteinase-activated Receptor |
PAR2 / F2RL1 |
Ca2+ |
A |
Peptide |
Proteinase-activated Receptor |
PAR4 / F2RL3 |
|
A |
Non-peptide |
Proton-sensor |
GPR68 |
Ca2+ |
A |
Non-peptide |
Purinergic |
P2Y1 |
Ca2+ |
A |
Non-peptide |
Purinergic |
P2Y2 |
|
A |
Non-peptide |
Purinergic |
P2Y4 |
|
A |
Non-peptide |
Purinergic |
P2Y6 |
|
A |
Non-peptide |
Purinergic |
P2Y9 |
Ca2+ |
A |
Non-peptide |
Purinergic |
P2Y11 |
|
A |
Non-peptide |
Purinergic |
P2Y12 |
|
A |
Non-peptide |
Serotonin |
5-HT1A / HTR1A |
|
A |
Non-peptide |
Serotonin |
5-HT2A / HTR2A |
|
A |
Non-peptide |
Serotonin |
5-HT2B / HTR2B |
|
A |
Non-peptide |
Serotonin |
5-HT2C / HTR2C |
|
A |
Non-peptide |
Serotonin |
5-HT4 / HTR4 |
Ca2+ |
A |
Non-peptide |
Serotonin |
5-HT7 / HTR7 |
Luciferase |
A |
Peptide |
Somatostatin |
SST2 |
|
A |
Peptide |
Somatostatin |
SST3 |
|
A |
Peptide |
Somatostatin |
SST4 |
|
A |
Peptide |
Somatostatin |
SST5 |
|
A |
Peptide |
Tachykinin |
NK1 / TACR1 |
|
A |
Peptide |
Tachykinin |
NK2 / TACR2 |
|
A |
Peptide |
Tachykinin |
NK3 / TACR3 |
|
A |
Peptide |
Thyrtropin-releasing Hormone |
TRH1 |
|
A |
Peptide |
Urotensin |
UT2 |
|
A |
Peptide |
Vasopressin |
V1A / AVPR1A |
|
A |
Peptide |
Vasopressin |
V1B / AVPR1B |
|
A |
Peptide |
Vasopressin |
V2 / AVPR2 |
|
B |
Peptide |
VIP / PACAP |
PAC1 |
|
B |
Peptide |
VIP / PACAP |
VPAC1 |
|
B |
Peptide |
VIP / PACAP |
VPAC2 |
|
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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) 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.
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Email: bioassay@genscript.com |
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Phone: 1-877-436-7274 (Toll-Free), 1-732-885-9188 |
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Fax: 1-732-210-0262, 1-732-885-5878 |
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