
G protein-coupled receptors (GPCRs) mediated signaling regulates key physiological processes, making them effective drug targets. Over 30% of all US FDA-approved drugs target GPCRs. Novel GPCR-based drugs discovery requires screening and characterization of potential drug candidates. GenScript provides a comprehensive portfolio of GPCR cell lines to evaluate GPCR signaling through second messenger assays.
Highlights
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Over 130 GRCP Cell Lines
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Single Clone
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Guaranteed Performance
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Stringent QC Standards
Applications
- Screening small molecules and biologics targeting GPCRs
- Characterizing MOA of small molecules and biologics binding with GPCRs in vitro
- Measuring binding affinity of small molecules and biologics binding with GPCRs
Receptor Family List
Note: Click on the G-protein coupled receptor family to find all related cell lines.
Ligand-bound and induced GPCR signaling can be studied by detecting second messenger molecules. GPCRs coupled to Gαs or Gαi activate the cAMP pathway, which stimulates or inhibits the accumulation of cellular cAMP. GPCR coupled to Gαq activates the PLC pathway, which induces the release of calcium. Second messenger assays enables measurement and characterization of both the agonist and the antagonist.
Calcium Assay
GPCRs can induce the PLC pathway releasing calcium as second messenger following ligand binding. A majority of GPCR cell lines from GenScript can utilize calcium assay for measurement and characterization. These include Gαq-coupled GPCR cell lines, and Gαs or Gαi-coupled GPCR cell lines with co-expression of Gα15.
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Figure 1: GLP-1 (7-37)-induced concentration-dependent stimulation of intracellular calcium mobilization in GLP-1R and Gα15 co-expression CHO-K1 cells (Cat. No. M00451 GenScript).
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Figure 2: Substance P-induced concentration-dependent stimulation of intracellular calcium mobilization in NK1 expression CHO-K1 cells (Cat. No. M00199, GenScript).
cAMP assay
Gαs or Gαi-coupled GPCR cell lines induce cAMP pathway using cAMP as second messenger following ligand binding. cAMP assay is a simple and straightforward method for measurement and characterization of binding between GPCR and its ligands.
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Figure 3: Dose dependent stimulation of intracellular cAMP mobilization upon treatment with dopamine in D1 expression CHO-K1 cells (Cat. No. M00247, GenScript).
Receptor Family | Receptor | Cell Line Name | Cat. No. |
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5-Hydroxytryptamine receptor | 5-HT1A/HTR1A | CHO-K1/5-HT1A/Gα15 | M00330 |
5-HT2A/HTR2A | CHO-K1/5-HT2A | M00251 | |
5-HT2B/HTR2B | CHO-K1/5-HT2B | M00249 | |
5-HT2C/HTR2C | CHO-K1/5-HT2C | M00253 | |
5-HT2C/HTR2C | HEK 293/5-HT2C | M00319 | |
5-HT4/HTR4 | CHO-K1/5-HT4/Gα15 | M00444 | |
Acetylcholine receptor (muscarinic) | M1/CHRM1 | CHO-K1/M1 | M00185 |
M2/CHRM2 | CHO-K1/M2/Gα15 | M00258 | |
M3/CHRM3 | CHO-K1/M3 | M00259 | |
M4/CHRM4 | CHO-K1/M4/Gα15 | M00238 | |
M5/CHRM5 | CHO-K1/M5 | M00186 | |
Adenosine receptor | ADORA1 | CHO-K1/ADORA1/Gα15 | M00324 |
ADORA1 | HEK293/ADORA1/Gα15 | M00255 | |
ADORA2A | CHO-K1/ADORA2A/Gα15 | M00246 | |
ADORA2A | CHO-K1/mouse ADORA2A | M00575 | |
ADORA2B | CHO-K1/ADORA2B/Gα15 | M00329 | |
ADORA3 | CHO-K1/ADORA3/Gα15 | M00464 |
Receptor Family | Receptor | Cell Line Name | Cat. No. |
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Adrenoceptors | ADRA1A | CHO-K1/ADRA1A | M00225 |
ADRA1B | CHO-K1/ADRA1B | M00260 | |
ADRA1D | CHO-K1/ADRA1D | M00340 | |
ADRA2A | CHO-K1/ADRA2A/Gα15 | M00281 | |
ADRA2B | CHO-K1/ADRA2B/Gqi5 | M00454 | |
ADRA2C | CHO-K1/ADRA2C/Gα15 | M00252 | |
ADRB1 | CHO-K1/ADRB1/Gα15 | M00269 | |
Angiotensin receptor | AT1 | HEK 293/AT1 | M00458 |
AT1 | HEK 293T/AT1 | M00448 | |
Apelin receptor | AGTRL1 | CHO-K1/AGTRL1/Gα15 | M00245 |
Bile acid receptor | GPBAR1 | CHO-K1/GPBAR1 | M00432 |
Bombesin receptor | BB1/NMBR | CHO-K1/BB1 | M00254 |
BB2/GRPR | CHO-K1/BB2 | M00182 | |
BB3/BRS3 | CHO-K1/BB3 | M00183 | |
Bradykinin receptor | B2 | CHO-K1/B2/Gα15 | M00184 |
Receptor Family | Receptor | Cell Line Name | Cat. No. |
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Calcitonin receptor | AMY1 | CHO-K1/Gα15/AMY1 | M00557 |
AMY2 | CHO-K1/Gα15/AMY2 | M00558 | |
AMY3 | CHO-K1/Gα15/AMY3 | M00559 | |
CALCR/CT | CHO-K1/CT/Gα15 | M00320 | |
Cannabinoid receptor | CNR1/CB1 | CHO-K1/CB1/Gα15 | M00299 |
CNR2/CB2 | CHO-K1/CB2 | M00433 | |
Chemerin receptor | CMKLR1 | CHO-K1/CMKLR1/Gα15 | M00301 |
Chemokine receptor | CCR1 | CHO-K1/CCR1/Gα15 | M00522 |
CCR5 | CHO-K1/CCR5/Gα15 | M00523 | |
CXCR1/IL8RA | CHO-K1/CXCR1/Gα15 | M00524 | |
CXCR3/CD183 | CHO-K1/CXCR3/Gα15 | M00525 | |
CXCR4/CD184 | CHO-K1/CXCR4/Gα15 | M00556 | |
CXCR5/CD185 | CHO-K1/CXCR5/Gα15 | M00526 | |
Cholecystokinin receptor | CCKA/CCKAR | CHO-K1/CCKA/Gα15 | M00271 |
CCKB/CCKBR | CHO-K1/CCKB | M00154 |
Receptor Family | Receptor | Cell Line Name | Cat. No. |
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Class A orphan | GPR68/OGR1 | CHO-K1/GPR68/Gα15 | M00439 |
MRGPRX2 | CHO-K1/MRGPRX2 | M00425 | |
Complement peptide receptor | C5a/C5AR1 | CHO-K1/C5a/Gα15 | M00327 |
Corticotropin releasing factor receptor | CRF1/CRHR1 | CHO-K1/CRF1/Gα15 | M00343 |
CRF2/CRHR2 | CHO-K1/CRF2/Gα15 | M00208 | |
Dopamine receptor | D1/DRD1 | CHO-K1/D1 | M00247 |
D2s/DRD2 | CHO-K1/D2s/Gα15 | M00274 | |
D2/DRD2 | CHO-K1/D2/Gα15 | M00152 | |
D5/DRD5 | CHO-K1/D5/Gα15 | M00322 | |
Endothelin receptor | ETA/EDNRA | CHO-K1/EDNRA | M00149 |
ETB/EDNRB | CHO-K1/EDNRB | M00150 | |
Formylpeptide receptor | FPR1 | CHO-K1/FPR1/Gα15 | M00429 |
Free fatty acid receptor | GPR40/FFA1 | CHO-K1/FFA1/Gα15 | M00273 |
GPR43/FFA2 | CHO-K1/FFA2/Gα15 | M00437 | |
Galanin receptor | GALR1 | CHO-K1/GALR1/Gα15 | M00277 |
GALR2 | CHO-K1/GALR2 | M00209 |
Receptor Family | Receptor | Cell Line Name | Cat. No. |
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Ghrelin receptor | GHSR | CHO-K1/GHSR | M00189 |
Glucagon receptor | GHRHR | HEK293/GHRH/Gα15 | M00314 |
GLP1R | CHO-K1/GLP1R/Gα15 | M00451 | |
GLP2R | CHO-K1/GLP2R/Gα15 | M00307 | |
GCGR | CHO-K1/GCGR/Gα15 | M00345 | |
GCGR | HEK 293/GCGR/Gα15 | M00422 | |
GIPR | CHO-K1/GIP/Gα15 | M00486 | |
Gonadotropin releasing hormone receptor | GNRHR | CHO-K1/GNRHR/Gα15 | M00426 |
Histamine receptor | H1/HRH1 | HEK293/H1 | M00131 |
H2/HRH2 | CHO-K1/H2/Gα15 | M00306 | |
H3/HRH3 | CHO-K1/H3/Gα15 | M00331 | |
H4/HRH4 | CHO-K1/H4/Gα15 | M00289 | |
Hydroxycarboxylic acid receptor | GPR109A/NIACR1 | CHO-K1/NIACR1/Gα15 | M00428 |
Kisspeptin receptor | KiSS1/GPR54 | CHO-K1/KiSS1 | M00190 |
Receptor Family | Receptor | Cell Line Name | Cat. No. |
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Leukotriene receptor | FPRL1 | CHO-K1/FPRL1/Gα15 | M00305 |
CysLT1 | CHO-K1/CysLT1/Gα15 | M00462 | |
LTB4R | CHO-K1/LTB4/Gα15 | M00435 | |
Lysophospholipid receptor | EDG4/LAP2 | RH7777/EDG4 | M00463 |
Melanin concentrating hormone receptor | MCH1/GPR24 | HEK293/MCH1 | M00211 |
MCH2/GPR145 | CHO-K1/MCH2 | M00280 | |
Melanocortin receptor | MC2 | CHO-K1/MC2/Gα15 | M00336 |
MC3 | CHO-K1/MC3/Gα15 | M00242 | |
MC4 | CHO-K1/MC4/Gα15 | M00272 | |
MC5 | CHO-K1/MC5/Gα15 | M00243 | |
Melatonin receptor | MT1/MTNR1A | CHO-K1/MT1/Gα15 | M00424 |
MT2/MTNR1B | CHO-K1/MT2/Gα15 | M00312 | |
Metabrotropic glutamate receptor | mGlu2/GRM2 | CHO-K1/GRM2/Gα15 | M00427 |
Motilin receptor | MTLR/MLNR | CHO-K1/MTLR/Gα15 | M00347 |
Neuromedin U receptor | NMUR1/GPR66 | CHO-K1/NMU1 | M00191 |
NMUR2 | HEK293T/NMU2 | M00244 |
Receptor Family | Receptor | Cell Line Name | Cat. No. |
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Neuropeptide S receptor | NPSR1/NPS1b | CHO-K1/NPS1b/Gα15 | M00344 |
NPSR1/NPS1a | CHO-K1/NPS1a/Gα15 | M00338 | |
Neuropeptide Y receptor | NPY2R | CHO-K1/NPY2/Gqi5 | M00460 |
NPY4R | CHO-K1/NPY4/Gα15 | M00237 | |
Neurotensin receptor | NTS1/NT1 | CHO-K1/NTS1 | M00194 |
Opioid & opioid-like receptor | OPRD1 | CHO-K1/OPRD1/Gα15 | M00323 |
OPRK1 | CHO-K1/OPRK1/Gα15 | M00290 | |
OPRL1 | CHO-K1/OPRL1/Gα15 | M00447 | |
OPRM1 | CHO-K1/OPRM1/Gα15 | M00304 | |
Orexin receptor | OX1 | CHO-K1/OX1 | M00224 |
OX2 | CHO-K1/OX2 | M00316 | |
P2Y receptor | P2Y1 | 1321N1/P2Y1 | M00250 |
P2Y2 | 1321N1/P2Y2 | M00318 | |
P2Y4 | 1321N1/P2Y4 | M00297 | |
P2Y6 | 1321N1/P2Y6 | M00346 | |
P2Y11 | 1321N1/P2Y11 | M00298 | |
P2Y12 | 1321N1/P2Y12/Gα15 | M00261 |
Receptor Family | Receptor | Cell Line Name | Cat. No. |
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Parathyroid hormone receptor | PTH1/PTHR1 | CHO-K1/PTH1/Gα15 | M00315 |
Peptide P518 receptor | QRFP/GPR103 | CHO-K1/GPR103/Gα15 | M00321 |
Platelet-activating factor receptor | PAFR/PTAFR | CHO-K1/PTAFR | M00262 |
Prolactin releasing peptide receptor | PRLHR | CHO-K1/PRLHR | M00341 |
Prostanoid receptor | EP1/PTGER1 | HEK293/EP1 | M00228 |
EP2/PTGER2 | CHO-K1/EP2/Gα15 | M00311 | |
FP/PTGFR | HEK293/FP/Gα15 | M00155 | |
IP1/PTGIR | CHO-K1/IP1/Gα15 | M00310 | |
TP/TBXA2R | HEK293/TP | M00309 | |
PTGDR/DP1 | CHO-K1/DP1/Gα15 | M00453 | |
PTGDR2/DP2 | CHO-K1/DP2/Gα15 | M00436 | |
Protease-activated receptor | PAR2/GPR11 | CHO-K1/PAR2/Gα15 | M00446 |
PAR4/F2RL3 | CHO-K1/PAR4 | M00206 |
Receptor Family | Receptor | Cell Line Name | Cat. No. |
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Somatostatin receptor | SST1/SSTR1 | CHO-K1/SST1/Gqi5 | M00473 |
SST2/SSTR2 | CHO-K1/SST2/Gα15 | M00325 | |
SST3/SSTR3 | CHO-K1/SST3/Gα15 | M00285 | |
SST4/SSTR4 | CHO-K1/SST4/Gα15 | M00334 | |
SST5/SSTR5 | CHO-K1/SST5/Gα15 | M00286 | |
Tachykinin receptor | NK1/TACR1 | CHO-K1/NK1 | M00199 |
NK2/TACR2 | CHO-K1/NK2 | M00200 | |
NK3/TACR3 | CHO-K1/NK3 | M00201 | |
Thyrotropin releasing hormone receptor | TRH1/TRHR | CHO-K1/TRH1 | M00202 |
Urotensin receptor | UTR2 | CHO-K1/UT2/Gα15 | M00339 |
Vasopressin and oxytocin receptor | OT/OXTR | CHO-K1/OXTR | M00195 |
V1B | CHO-K1/V1B | M00205 | |
V2 | CHO-K1/V2/Gα15 | M00170 | |
VIP and PACAP receptor | PAC1R | CHO-K1/PAC1/Gα15 | M00203 |
VPAC1/VIPR1 | CHO-K1/VPAC1/Gα15 | M00342 | |
VPAC2/VIPR2 | CHO-K1/VPAC2/Gα15 | M00226 |