GPCR Product Solutions
Always find a GPCR Assay for Your Target of Interest
G protein-coupled receptors (GPCRs) are 7-transmembrane receptors representing the largest family of validated therapeutic targets with over 800 known human GPCRs. Therapeutics targeting GPCRs represent over 40% of all currently marketed drug therapeutics acting on GPCRs either directly or indirectly. GPCRs have a broad array of ligands, including growth factors, ions, lipids, nucleotides, hormones, and neurotransmitters.
Their physiological and pathological involvements are vast, ranging from regulation of hunger to the development of fetal structures, and from roles in cardiovascular disorders to rare diseases. To help researchers fully characterize their specific GPCR of interest, and the small molecules or biologics effecting their activity, Eurofins DiscoverX® encourages exploring all possible signaling scenarios with a variety of available biologically-relevant cell-based functional and binding assays, cell lines, detection kits, and membrane preparations.
The target-specific products in the Eurofins DiscoverX portfolio are sensitive, scalable, and robust for detecting receptor-mediated second messenger signals (cAMP and calcium), β-arrestin recruitment, receptor internalization, and ligand binding. These assays also support the characterization of orphan GPCRs without a known ligand or approved drug as part of the comprehensive GPCR solutions portfolio offered.
Product Highlights
- Broad Coverage – Over 90% targets covered across the human GPCRome to always find an assay for your target of interest
- Highly Applicable – Ideal for the development of small molecule and biologic therapeutics, from target ID through pre-clinical drug discovery programs
- Assay Options – Multiple mechanism of action (MOA) assay types are available (e.g., β-arrestin, cAMP, calcium, internalization, ligand binding, trafficking) offering a diverse array of GPCR assay solutions for maximum flexibility
- Largest Collection – Over 1,600 qualified functional and binding assays seen in >800 peer-reviewed publications, giving you the most comprehensive GPCR assay solutions available for the confidence you need
GPCR Cell Lines, Ready-to-Assay Cells and Kits, and Membrane Preps
- β-Arrestin Assays – Universal G-protein independent cell-based assays to quantify GPCR activation based on the recruitment of β-arrestin. Ideal for ligand bias analysis, antagonist mode screening, and studying virtually any GPCR including orphan receptors.
- cAMP Assays – Homogeneous cAMP detection cell-based assays to monitor the functional status of GPCRs upon small molecules or biologics binding. Characterize ligand pharmacology and obtain reproducible performance with large assay windows and broad sensitivity ranges.
- Calcium Assays – Fluorescent dye-based assays to measure calcium mobilization in cell lines as a direct indication of GPCR or ion channel activation or inhibition.
- GPCR Internalization Assays – Secondary, orthogonal screening cell-based assays for measuring GPCR desensitization and recycling as well as uncovering novel classes of compound pharmacologies and identifying safer drugs without imaging or antibodies.
- Pharmacotrafficking Assays – Quantitative cell-based assays to identify small molecule pharmacochaperones that act as therapeutic agents to stabilize and correct disease-relevant mutant GPCRs, ion channels, or transporters.
- Membrane Preparations – Purified membrane preps for obtaining GPCR and ion channel ligand binding affinities and evaluating GPCR activity through GTPγS functional studies in response to the addition of a ligand or therapeutic.
Whether you are developing small molecule or biologic therapeutic drugs, Eurofins DiscoverX provides you with a variety of drug discovery products with multiple assay types to meet your specific GPCR research needs.
Highlights of GPCR Product Solutions
Whether you are developing small molecule or biologic therapeutic drugs, Eurofins DiscoverX provides you with a variety of drug discovery and development products with multiple assay types and applications to meet your specific GPCR research needs.
Access Products by Target Families
| Family | Gene ID (Common) | Family | Gene ID (Common) |
|---|---|---|---|
| 5-Hydroxytryptamine (Serotonin) | HTR1A (5HT1A) | Bombesin BRS3 | BRS3 (BB3) |
| HTR1B (5HT1B) | GRPR (BB2) | ||
| HTR1E (5HT1E) | NMBR (BB1) | ||
| HTR1F (5HT1F) | Bradykinin | BDKRB1 (B1) | |
| HTR2A (5HT2A) | BDKRB2 (B2) | ||
| HTR2B (5HT2B) | Calcitonin | CALCR (CT) | |
| HTR2C (5HT2C) | CALCR-RAMP1 (AMY1) | ||
| HTR5A (5HT5A) | CALCR-RAMP2 (AMY2) | ||
| HTR6 (5HT6) | CALCR-RAMP3 (AMY3) | ||
| HTR7A (5HT7A) | CALCRL-RAMP1 (CGRP1) | ||
| HTR7B (5HT7B) | CALCRL-RAMP2 (AM1) | ||
| HTR7D (5HT7D) | CALCRL-RAMP3 (AM2) | ||
| Acetylcholine (Muscarinic) | CHRM1 (M1) | Cannabinoid | CNR1 (CB1) |
| CHRM2 (M2) | CNR2 (CB2) | ||
| CHRM3 (M3) | Chemerin | CMKLR1 (ChemR23) | |
| CHRM4 (M4) | Chemokine | CCR1 | |
| CHRM5 (M5) | CCR2 | ||
| Adenosine | ADORA1 (A1) | CCR3 | |
| ADORA2A (A2A) | CCR4 | ||
| ADORA2B (A2B) | CCR5 | ||
| ADORA3 (A3) | CCR6 | ||
| Adrenoceptor | ADRA1A (a1A) | CCR7 | |
| ADRA1B (a1B) | CCR8 | ||
| ADRA1D (a1D) | CCR9 | ||
| ADRA2A (a2A) | CCR10 | ||
| ADRA2B (a2B) | CCRL1 | ||
| ADRA2C (a2C) | CX3CR1 | ||
| ADRB1 (b1AR) | CXCR1 (IL8RA) | ||
| ADRB2 (b2AR) | CXCR2 (IL8RB) | ||
| ADRB3 (b3AR) | CXCR3 | ||
| Angiotensin | AGTR1 (AT1) | CXCR4 | |
| Apelin | AGTRL1 (APJ) | CXCR5 | |
| Bile Acid (GPBA) | GPBAR1 (GPR131) | CXCR6 |
| Family | Gene ID (Common) | Family | Gene ID (Common) |
|---|---|---|---|
| Chemokine | CXCR7 (CMKOR1) | Glycoprotein Hormone | FSHR (FSH) |
| XCR1 (XC1) | LHCGR (LH) | ||
| Cholecystokinin | CCKAR (CCK1) | TSHR (TSH) | |
| CCKBR (CCK2) | Gonadotrophin-Releasing Hormone | GNRHR (GnRH) | |
| Complement Peptide (Anaphylatoxin) | C3AR1 (C3A) | Histamine | HRH1 (H1) |
| C5AR1 (C5A) | HRH2 (H2) | ||
| C5AR2 (C5L2/GPR77) | HRH3 (H3) | ||
| Corticotropin-Releasing Factor | CRHR1 (CRF1) | HRH4 (H4) | |
| CRHR2 (CRF2) | Hydroxycarboxylic Acid | HCAR1 (HCA1/GPR81) | |
| Dopamine | DRD1 (D1) | HCAR2 (HCA2/GPR109A/HM74A/NIC1) | |
| DRD2 (D2) | HCAR3 (HCA3/GPR109B/NIC2) | ||
| DRD3 (D3) | Kisspeptin | KISS1R (GPR54) | |
| DRD4 (D4) | Leukotriene | CYSLTR2 (LTC4) | |
| DRD5 (D5) | LTB4R (BLT1) | ||
| Endothelin | EDNRA (ETA) | OXER1 (GPR170) | |
| EDNRB (ETB) | Lysophospholipid (LPA & S1P) | LPAR1 (LPA1/EDG2) | |
| Formylpeptide | FPR1 (FPR) | LPAR2 (LPA2/EDG4) | |
| FPR2 (FPRL1/ALX) | LPAR3 (LPA3/EDG7) | ||
| FPR3 (FPRL2) | LPAR5 (LPA5/GPR92) | ||
| Free Fatty Acid | FFAR1 (FFA1/GPR40) | S1PR1 (S1P1/EDG1) | |
| FFAR2 (FFA2/GPR43) | S1PR2 (S1P2/EDG5) | ||
| FFAR3 (FFA3/GPR41) | S1PR3 (S1P3/EDG3) | ||
| FFAR4 (FFA4/GPR120) | S1PR4 (S1P4/EDG6) | ||
| Galanin | GALR1 (GAL1) | S1PR5 (S1P5/EDG8) | |
| GALR2 (GAL2) | Melanin-Concentrating Hormone | MCHR1 (MCH1) | |
| Ghrelin | GHSR (GRLN) | MCHR2 (MCH2) | |
| Glucagon | GCGR (Glucagon) | Melanocortin | MC1R (MC1) |
| GHRHR (GHRH) | MC3R (MC3) | ||
| GIPR (GIP) | MC4R (MC4) | ||
| GLP1R (GLP-1) | MC5R (MC5) | ||
| GLP2R (GLP-2) | Melatonin | MTNR1A (MT1) | |
| SCTR (Secretin) | MTNR1B (MT2) |
| Family | Gene ID (Common) | Family | Gene ID (Common) |
|---|---|---|---|
| Motilin | MLNR (Motilin) | Prostanoid | PTGER2 (EP2) |
| Neuromedin U | NMU1R (NMU1) | PTGER3 (EP3) | |
| Neuropeptide B & W | NPBWR1 (GPR7) | PTGER4 (EP4) | |
| NPBWR2 (GPR8) | PTGFR (FP) | ||
| Neuropeptide FF | NPFFR1 (GPR147) | PTGIR (IP) | |
| Neuropeptide S | NPSR1 (NPS) | TBXA2R (TP) | |
| Neuropeptide Y | NPY1R (Y1) | Proteinase-Activated | F2R (PAR1) |
| NPY2R (Y2) | F2RL1 (PAR2) | ||
| NPY4R (Y4/PPYR1) | F2RL3 (PAR4) | ||
| Neurotensin | Neurotensin | Relaxin Family Peptide | RXFP1 (LGR7) |
| Opioid | OPRD1 (δ) | RXFP2 (LGR8) | |
| OPRK1 (κ) | OPRK1 (κ) | RXFP3 (SALPR) | |
| OPRL1 (NOP) | RXFP4 | ||
| OPRM1 (μ) | Somatostatin | SSTR1 (SST1) | |
| Orexin | HCRTR1 (OX1) | SSTR2 (SST2) | |
| HCRTR2 (OX2) | SSTR3 (SST3) | ||
| Oxoglutarate | OXGR1 (GPR99/GPR80) | SSTR4 (SST4) | |
| P2Y P2RY1 (P2Y1) | SSTR5 (SST5) | ||
| P2RY2 (P2Y2) | Succinate | SUCNR1 (GPR91) | |
| P2RY4 (P2Y4) | Tachykinin | TACR1 (NK1) | |
| P2RY6 (P2Y6) | TACR2 (NK2) | ||
| P2RY11 (P2Y11) | TACR3 (NK3) | ||
| P2RY12 (P2Y12) | Thyrotropin-Releasing Hormone | TRHR (TRH1) | |
| Parathyroid Hormone | PTH1R (PTH1) | Trace Amine | TAAR1 (TA1) |
| PTH2R (PTH2) | Urotensin | UTS2R (UTR2) | |
| Peptide P518 | QRFPR (QRFP/GPR103) | Vasopressin & Oxytocin | AVPR1A (V1A) |
| Platelet-Activating Factor | PTAFR (PAF) | AVPR1B (V1B) | |
| Prokineticin | PROKR1 (PKR1/GPR73) | AVPR2 (V2) | |
| PROKR2 (PKR2) | OXTR (OT) | ||
| Prolactin-Releasing Peptide | PRLHR (PRRP) | VIP & PACAP | ADCYAP1R1 (PAC1) |
| Prostanoid | PTGDR (DP1) | VIPR1 (VPAC1) | |
| PTGDR2 (DP2/CRTH2) | VIPR2 (VPAC2) | ||
| PTGER1 (EP1) |
| Gene ID (Common) | Gene ID (Common) | Gene ID (Common) | Gene ID (Common) |
|---|---|---|---|
| BAI1 | GPR32 | GPR101 | GPR161 |
| BAI2 | GPR35 | GPR107 | GPR162 |
| BAI3 | GPR37 (Pael Receptor, EDNRBL) | GPR119 | GPR171 |
| CCRL2 | GPR37L1 | GPR123 | GPR173 (SREB3) |
| GHSR1b | GPR39 | GPR132 | GPR176 (HB954) |
| GPER (GPR30) | GPR45 (PSP24) | GPR135 (HUMNPIIY20) | GPR182 |
| GPR1 | GPR50 | GPR137 (TM7SF1) | GPR183 (EBI2) |
| GPR3 | GPR52 | GPR139 (PGR3) | LGR4 (GPR48) |
| GPR4 | GPR55 | GPR141 (AXOR115) | LGR5 (GPR49) |
| GPR6 | GPR61 | GPR142 (AXOR103) | LGR6 |
| GPR12 | GPR65 | GPR143 | MRGPRD |
| GPR17 | GPR68 | GPR146 (AXOR120) | MRGPRE |
| GPR18 | GPR75 | GPR148 | MRGPRF |
| GPR20 | GPR78 | GPR149 (R35, PGR10) | MRGPRX1 (MRGX1) |
| GPR22 | GPR79 | GPR15 (Bob) | MRGPRX2 (MRGX2) |
| GPR23 (LPA4, P2Y9) | GPR83 | GPR150 (AXOR70) | MRGPRX4 |
| GPR25 | GPR84 | GPR151 (AXOR40) | OPN5 |
| GPR26 | GPR85 (SREB2) | GPR152 | P2RY8 |
| GPR27 (SREB1) | GPR88 | GPR157 | TAAR5 |
| GPR31 | GPR97 |
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Universal G-protein independent cell-based assays to quantify GPCR activation based on the recruitment of β-arrestin
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Accurately monitor GPCR activation by biologics or small molecules & detect cellular cAMP production levels for a variety of applications
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Fluorescent assays to measure calcium mobilization in cell lines as a direct indication of GPCR or ion channel activation or…
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Screening cell-based assays for analyzing the movement of proteins to multiple membrane compartments within the cell
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Quantitative cell-based assays to identify pharmacochaperones that stabilize & correct disease-relevant mutant GPCRs, ion channels, or transporters
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Complete set of parental cell lines, vectors, kits, & retroparticles to build your own stable cell lines & cell-based assays
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Custom cell lines, kits, assays, & protein development capabilities optimized to fit your requirements
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Non-imaging, cell-based internalization assays for screening & identifying safer drugs for GPCRs
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