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 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.



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Choose the Solution That Best Meets Your GPCR Program Needs

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.

 

  • 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 thru pre-clinical drug discovery programs
  • Various 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
Humans | Orphans | Orthologs

Highlights of GPCR Product Solutions

Highlights of GPCR Product Solutions

eBooks

  • eBook: Insights into GPCR Drug Discovery & Development – Exploring GPCR-Ligand Interactions & Signaling Pathways with Binding & Functional Assays Access eBook

Application Notes, and White Paper

  • Ligand Characterization of Mas-Related GPCR-X2 via Cell-Based Assays: Assessing the Regulation of Mast Cell Function and Implications in Safety Pharmacology Read Application Note
  • Automating Cell-Based Bioassays on Tecan’s Fluent® Automation Workstation (PathHunter CNR1 Bioassay focus) Read Application Note
  • Uncover Novel G-Protein or Arrestin-Biased Ligands using a Suite of GPCR Signaling Cell-Based Assays: A Study of Biased Agonism on Opioid Receptors Read Application Note
  • Quantify GPCR Endocytosis and Recycling with PathHunter GPCR Internalization Assays - Analyzing Therapeutics for Opioid and Cholecystokinin Receptors Read Application Note
  • White Paper: The New World of GPCR Allosteric Modulation Read White Paper
  • Rapid Quantification of Bioactive Ligands in Serum and Human Plasma Using PathHunter eXpress β-Arrestin GPCR Assays Read Application Note

Videos

  • GPCR Assays: Which ones to use and why for your research and drug discovery and development programs. Short Overview Recording (5 min.) or Knowledge-Based Video (25 min.)
  • Internalization Assays: Identify safer therapeutics with simple, quantitative cell-based assays for measuring receptor internalization. View Video (13 min.)
  • Pharmacotrafficking Assays: Discover pharmacological chaperones that rescue disease relevant mutant membrane proteins like GPCRs, ion channels and transporters. View Video (30 min.)

Blog Articles

  • Unlocking Orphan GPCRs with an Innovative Forward Trafficking Approach Read Article
  • Use of Automated Functional, Cell-Based Bioassays Read Article
  • Uses and Advantages of Membrane Preparations for GPCRs Read Article
  • Do-It-Yourself: Benefits and Challenges of Creating Your Own Cell-Based Assays Read Article
  • Why Study GPCR Arrestin Recruitment? Read Article
  • Ideal Methods to Study Cellular Transport of Membrane Proteins Read Article
  • Ligand Bias: Increasing specificity and Reducing Side Effects of Drug Compounds Read Article
  • Four Reasons Why You Should Measure and Quantify Signaling bias in Your Molecules Read Article

Webinars

Peer Reviewed Publications

Scientific Posters and Presentations

Brochures and Flyers

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.

Custom and Toolbox Products

  • Custom Capabilities – Custom cell lines and assays capabilities optimized to fit your requirements
  • Toolbox Products – Complete set of parental cell lines, expression and cloning vectors, kits, and retroparticles to build your own stable cell lines and cell-based assays.

Access Products by Target Families

5-Hydroxytryptamine (Serotonin) to Chemokine

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

 

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Chemokine to Melatonin

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)

 

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Motilin to VIP & PACAP

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)    

 

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Orphan and Liganded Orphan Receptors

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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