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

Consider Eurofins DiscoverX’s custom development capabilities for custom cell lines, assays, & enzyme development.

Product List

GPCR Product List

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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

Applications	Benefits	Product Portfolio	Credibility
Biologically relevant functional assays Broad coverage of human GPCRome, including both liganded and orphan GPCRs Ortholog receptor assays Multiple modalities (second messenger, β-arrestin, and internalization) for ligand bias studies Pharmacological profiling (e.g., agonist, antagonist, allosteric modulation) Ability to multiplex various readouts (in one cell line)	Homogeneous assays with easy-to follow, rapid, no-wash protocols Luminescent and fluorescent readouts Sensitive detection Robust dynamic range Low false positive rate Reproducible Suitable for miniaturization and high-throughput screening	Cell lines and ready-to-use assay kits Flexible toolbox (do-it-yourself) cell-based assay development products Membrane preps suitable for radio- and fluorescent ligand binding assays Qualified, optimized, and highly reproducible bioassays for development through QC lot-release applications Custom product development services	Accepted by industry and the scientific community with thousands of peer-reviewed publications & billions of data points screened Thorough technical documentation Helpful and experienced customer support

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

5-Hydroxytryptamine (Serotonin) to Chemokine

Gene ID (Common)	Gene ID (Common)	Gene ID (Common)	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

Chemokine to Melatonin

Gene ID (Common)	Gene ID (Common)	Gene ID (Common)	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)

Motilin to VIP & PACAP

Gene ID (Common)	Gene ID (Common)	Gene ID (Common)	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)

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

Application Notes Ligand Characterization of Mas-Related GPCR-X2 via Cell-Based Assays: Assessing the Regulation of Mast Cell Function and Implications in Safety Pharmacology

An Application Note Assessing the Regulation of Mast Cell Function and its Implications in Safety Pharmacology. MrgprX2 antagonism promotes fresh…

Application Notes Automating Cell-Based Bioassays on Tecan®’s Fluent Automation Workstation: Measuring β-Arrestin Recruitment of Cannabinoid Receptor 1

Through early discovery, screening, characterization, and particularly for market release and commercialization of biologics, drug candidates require physiologically relevant, functional…

Application Notes 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

As more is learned about the intricacies of GPCR signaling, the harder it becomes to accurately describe ligand activity using…

Application Notes Quantify GPCR Endocytosis and Recycling with PathHunter® GPCR Internalization Assays – Analyzing Therapeutics for Opioid and Cholecystokinin Receptors

Here we show how PathHunter GPCR Internalization assays can be used to differentiate between strongly internalizing and weakly internalizing agonist…

Application Notes Rapid Quantification of Bioactive Ligands in Serum and Human Plasma Using PathHunter® eXpress β-Arrestin GPCR Assays

Application Notes Chemiluminescent cAMP Detection Using DiscoverX HitHunter® Kits Compared With TR-FRET Assays

Application Notes Discovery of Novel G-Protein or Arrestin-Biased Ligands Using a Suite of GPCR Signaling Platforms

As more is learned about the intricacies of GPCR signaling, the harder it becomes to accurately describe ligand activity using…

Application Notes Enabling Functional Therapeutic Antibody Research Using PathHunter® β-Arrestin Technology

Application Notes Evaluation of a New Intracellular Calcium Fluorescent Reagent Using the FDSS6000

Application Notes Faster Chemiluminescent cAMP Detection by HitHunter® cAMP XS+ on the SpectraMax L Luminescence Microplate Reader

Brochures & Flyers GPCR PathHunter® Arrestin Publications

With a growing list of over 150 customer publications, PathHunter® Arrestin assays are among the most trusted functional GPCR assays…

Brochures & Flyers GPCR Reference Guide

As more is learned about the intricacies of GPCR signaling, the harder it becomes to accurately describe ligand activity using…

Brochures & Flyers Evaluate Glucose Metabolism Targeted Therapeutics

GLP Cell Lines & Ready-to-Use Assays from Characterization through QC Lot Release

Brochures & Flyers Expedite Cancer Drug Discovery & Development

Functional Cell-Based Assays, Cell Lines, & Proteins for Cancer Research Improved or novel small molecule or biologic therapeutics for cancer…

Brochures & Flyers Insights Into GPCR Drug Discovery & Development

Explore GPCR-Ligand Interactions & Signaling Pathways with Binding & Functional Assays

Brochures & Flyers Eurofins DiscoverX – Delivering Solutions from Discovery to Market

Products & Custom Development Capabilities.

Brochures & Flyers Obesity & Diabetes Product Solutions

Accelerate the Development of Peptide Therapeutics for Obesity & Diabetes With MOA-Reflective Assays — Assays for Screening, Profiling, Potency, &…

Target Lists GPCR Product Solutions

Your source for a complete offering of GPCR assays, cell lines, and membrane preps

Webinars Validated bioassays for metabolic & gastrointestinal diseases: Accelerating development of GLP-1 & -2 therapeutics

Therapeutics targeting glucagon-like peptide, GLP-1 and GLP-2, receptors are being developed to address globally prevalent medical disorders for managing diabetes,…

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Webinars Unlocking Orphan GPCRs with an Innovative Forward Trafficking Approach

The webinar addresses the challenge that much of the GPCR druggable space remains untapped for potential therapeutic targets. To address…

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Webinars Application of β Arrestin Assays to the Orphan GPCR World

GPCRs are privileged drug targets. Approximately 100 receptors still escape from the drug discovery process as they are orphans, without…

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Webinars Mu Opioid Receptor Splicing and Signaling: Another Dimension of GPCR Function

Opioid receptors are among the most well-known GPCRs that regulate the transmission and perception of pain. Clinical management of severe…

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Webinars How to Make Your Own Cell-Based Assays to Study β-Arrestin Recruitment

This 30-minute webinar shows you how to make your own cell-based assays to analyze β-arrestin recruitment in any cell type.…

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Webinars Duplexed Screening of GPCRs to Measure Calcium and β-Arrestin

The screening and functional characterization of novel ligands for G-Protein Coupled Receptors (GPCR) remains a key focus in drug discovery.…

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Videos GPCR Assays Overview

Short Overview of Eurofins DiscoverX GPCR assays. 5 min.

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Videos GPCR Assays: Which ones to use and why for your research and drug discovery and development programs

Learn about several GPCR assays and which ones to use and why for your research and drug discovery and development…

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Videos Receptor Internalization Assays

Learn about PathHunter Internalization assays developed to measure translocation of both single-pass and multi-pass receptors (like RTKs, checkpoint receptors and…

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Videos Pharmacotrafficking Assays

Learn about PathHunter pharmacotrafficking assays to identify small molecule compounds that rescue disease relevant mutant membrane proteins like GPCRs, ion…

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Videos Custom Development Capabilities

Learn about Eurofins DiscoverX cell line engineering, assay development, and recombinant enzyme production custom capabilities. Find out more about cell…

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Scientific Posters Qualified, Fit-for-Purpose Bioassays for Liraglutide and Exenatide as Frozen Ready-to-Use Cells

With more than 25% of the world’s population diagnosed with type II diabetes and/or metabolic syndrome, the requirement for cost…

Scientific Posters [Wall Poster] The Druggable GPCRome

DiscoveRx offers an industry-leading portfolio of over 600 naturally coupled human and ortholog G-protein coupled receptor (GPCR) cell lines designed…

Scientific Posters A Duplexed Calcium and β-Arrestin Assay Protocol for Human Histamine H1 Receptor PathHunter CHO-K1 HRH1 β-Arrestin Cell Line

The screening and functional characterization of novel ligands for G-protein-coupled receptors (GPCRs) remains a key activity in drug discovery process.…

Scientific Posters A Wide Range of Compound Efficacies Revealed Using PathHunter® Arrestin Assays

DiscoveRx has developed a novel application of our established Enzyme Fragment Complementation (EFC) technology that allows us to monitor protein-protein…

Scientific Posters Cell-Based Assays for G-Protein Independent Signaling Using Arrestin Binding and Endocytosis

GPCR activation results in G-protein dependent events such as second messenger signaling, as well as initiation of a host of…

Scientific Posters Detection of Endogenous Ligand Bias: A Case Study Using the Chemokine Receptor Family

The pattern of intracellular signaling downstream of GPCR activation is now known to be specific to the ligand-receptor pair as…

Scientific Posters Dual Purpose Cell Lines for Analysis of GPCR/Arrestin Interaction using PathHunter® and Natural Gq-Coupling Using the Improved Calcium No-WashPLUS (CaNWPLUS) Kit

DiscoveRx has developed a panel of over 30 naturally Gq-coupled or dual coupled GPCR/Arrestin cell lines that can be used…

Scientific Posters GLP1 NAb Assay: A Case Study for Simple, Serum-tolerant Cell-based Assays to Detect Neutralizing Antibodies to Biosimilar and Bioinnovator drugs

Neutralizing antibodies (NAbs) to biological drugs may cause loss of therapeutic effi cacy and in some cases, loss of endogenous…

Scientific Posters HitHunter® cAMP and cAMP Hunter™ Cell Line: Your Solution for Use with High Serum Samples, Difficult Gi Targets and Identification of Allosteric Modulators

The cAMP detection technologies are widely used in high throughput screening (HTS) for measuring a functional response of a GPCR…

Scientific Posters Interrogating Allosteric Interactions Using Multiple Readouts for GPCRs

Compounds that bind to allosteric sites offer many benefits over those which interact orthosterically. These include enhanced specificity, ability to…

Scientific Posters Ligand Characterization of Mas-Related GPCR-X2 via Cell-Based Assays: Implications in Safety Liability Tests

Mast cells are principal players in IgE-, and more recently, non-IgE-mediated anaphylactoid reactions or pseudo-allergic Adverse Drug Reactions (ADR). A…

Scientific Posters Multi-Parameter GPCR Screening: An Essential Tool for Uncovering GPCR Mutant Phenotypes

The recent appreciation of functional selectivity/ligand bias in GPCR signaling has uncovered new opportunities for therapeutic discovery and continues to…

Scientific Posters Novel Trafficking Assays for Pharmacochaperone Discovery Using Enzyme Fragment Complementation

DiscoveRx® has pioneered a novel enzyme complementation system to monitor cellular events such as protein translocation, protein interactions, and degradation…

Scientific Posters Novel Trafficking Assays For Pharmacochaperone Discovery Using Enzyme Fragment Complementation Applied To CFTR-ΔF508

DiscoveRx® has pioneered a novel enzyme complementation system to monitor cellular events such as protein translocation, protein interactions, and degradation…

Scientific Posters The application of EFC technology to study forward trafficking of GPCRs

DiscoveRx has pioneered a novel enzyme complementation system to monitor cellular events such as protein translocation, protein interactions, and degradation…

Scientific Posters PathHunter® β-Arrestin Assays as a Universal Tool For Orphan GPCR Analysis

Orphan GPCRs continue to represent a target class with immense potential for the discovery of novel therapeutic compounds. In spite…

Scientific Posters PathHunter® β-Arrestin Assays: Determination of Pharmacology Differences Between Human and Ortholog GPCRs

DiscoveRx previously introduced a protein-protein interaction system using enzyme fragment complementation that provides a robust, HTS friendly format for monitoring…

Scientific Posters Quantifying GPCR Signaling Bias: A Simple Approach to Quantify Selectivity and Agonist Bias

Interest in GPCR ligand bias has increased in recent years due to evidence that positive and negative aspects of drug…

Scientific Posters Unique Properties of PathHunter® β-Arrestin Assays for GPCR Antagonist Discovery and Characterization

A common feature of 7TM receptors is that upon activation, the receptors are bound by cellular Arrestin proteins. DiscoveRx has…

Scientific Posters Utilization of PathHunter® Arrestin Cell Lines for Detection of Arrestin Biased Ligands and Compound Pharmacology Distinct from Second Messengers

DiscoveRx has developed a panel of over 120 characterized GPCR cell lines that monitor receptor activity using interaction with human…

Scientific Posters Accelerate Drug Development of GLP-1 & -2 Receptor Analogs with Ready-to-Use Cell-Based Assays

There is an increasing need to generate therapeutics targeting metabolic and gastrointestinal diseases to address the global burden of metabolic…

Scientific Posters Ultrasensitive, 3456 or 1536-Well Miniaturization-Friendly Chemiluminescent Detection of PathHunter® Cell-Based GPCR and Kinase Assays

DiscoveRx’s PathHunter® platform is a simple, cell-based, chemiluminescent assay format that allows for screening large numbers of small molecules or…

Scientific Posters Identify Effective Therapeutics with Simple, Quantitative Cell-Based Assays That Measure Receptor Internalization

Both multi- and single-pass membrane receptors constitutively exhibit complicated and dynamic membrane receptor trafficking as well as internalization induced by…

Blogs & Articles Accelerating Development of GLP-1 & GLP-2 Therapeutics with Validated Bioassays

Glucagon-like peptides, GLP-1 & GLP-2, are well-researched, metabolically significant peptide hormones secreted from the L-cells of the small intestine in…

Blogs & Articles GPCR Drug Discovery & Development Insights with Dr. Terry Kenakin

GPCRs have long been regarded as a low-hanging fruit drug target as they are conveniently located on the cell surface…

Blogs & Articles Employing Assay “Volume Control” to Unveil Efficacies in Allosteric Lead Molecules for GPCRs

Drugs interact with living physiology; an in vitro assay of drug activity can be considered a snapshot of the full…

Blogs & Articles Evaluate GLP-1R Targeted Therapeutics using First-to-Market Semaglutide Qualified GLP-1R Bioassay

Glucagon-Like Peptide-1 (GLP-1), a member of the glucagon-secretin peptide family, is secreted from L-cells of the small intestine and binds…

Blogs & Articles Insights Into GPCR Drug Discovery & Development

Explore GPCR-Ligand Interactions & Signaling Pathways with Binding & Functional Assays

Blogs & Articles Use of Automated Functional, Cell-Based Bioassays

Importance in Drug Discovery & Development for Quality Testing Programs. GPCR CNR1 Bioassay example.

Blogs & Articles Uses and Advantages of Membrane Preparations for GPCRs

Cellular membrane proteins play important functions in many biological processes. Understanding their roles often requires that these proteins be isolated…

Blogs & Articles Do-It-Yourself: Benefits and Challenges of Creating Your Own Cell-Based Assays

Cell-based assays are useful for understanding cellular pathways; characterizing targets and their function; identifying, screening, and optimizing ligands or drugs…

Blogs & Articles The Mast Cell Receptor Mrgx2 and Drug-induced Anaphylaxis

Presenting a compelling narrative on the pharmacological characterization of the MRGX2 gene. Dr. Brown emphasized the receptor’s importance as a…

Blogs & Articles Four Reasons Why You Should Measure and Quantify Signaling bias in Your Molecules

Most GPCRs are pleiotropically coupled to multiple signaling pathways in cells and the availability of functional assays to separately measure…

Blogs & Articles Ideal Methods to Study Cellular Transport Of Membrane Proteins

Translocation and Trafficking of Membrane Proteins

Blogs & Articles Why Study GPCR Arrestin Recruitment?

Arrestins are ubiquitously expressed and function in the activation of GPCRs, desensitization of most 7-transmembrane receptors (7-TMs), and regulation of…

Blogs & Articles Ligand Bias: Increasing specificity and Reducing Side Effects of Drug Compounds

Ligand bias is the ability of compounds to exert differential signal transduction responses on activation of a GPCR. This is…

Blogs & Articles Unlocking Orphan GPCRs with an innovative forward trafficking approach

Application of GPCR Pharmacotrafficking & Cell-Based Assays

Publications Allosteric “beta-blocker” isolated from a DNA-encoded small molecule library.

The β2-adrenergic receptor (β2AR) has been a model system for understanding regulatory mechanisms of G-protein-coupled receptor (GPCR) actions and plays…

Publications Alternatively spliced mu opioid receptor C termini impact the diverse actions of morphine.

Extensive 3′ alternative splicing of the mu opioid receptor gene OPRM1 creates multiple C-terminal splice variants. However, their behavioral relevance…

Publications Distinct conformations of GPCR-β-arrestin complexes mediate desensitization, signaling, and endocytosis.

β-Arrestins (βarrs) interact with G protein-coupled receptors (GPCRs) to desensitize G protein signaling, to initiate signaling on their own, and…

Publications Identification of resolvin D2 receptor mediating resolution of infections and organ protection.

Endogenous mechanisms that orchestrate resolution of acute inflammation are essential in host defense and the return to homeostasis. Resolvin (Rv)D2…

Publications Ligand-Based Discovery of a New Scaffold for Allosteric Modulation of the mu-Opioid Receptor.

With the hope of discovering effective analgesics with fewer side effects, attention has recently shifted to allosteric modulators of the…

Publications Measurement of β-Arrestin Recruitment for GPCR Targets.

β-Arrestins are ubiquitously expressed in all cell types, and function in the desensitization of G- protein coupled receptors (GPCRs), the…

Publications Navigating CYP1A induction and arylhydrocarbon receptor agonism in drug discovery. A case history with S1P1 agonists.

This article describes the finding of substantial upregulation of mRNA and enzymes of the cytochrome P450 1A family during a…

Publications New Screening Strategy and Analysis for Identification of Allosteric Modulators for GLP-1 Receptor Using GLP-1(9-36)amide.

The glucagon-like peptide-1 receptor (GLP-1R) is an important physiologic regulator of insulin secretion and a major therapeutic target for diabetes…

Publications Orphan GPR61, GPR62 and GPR135 receptors and the melatonin MT2 receptor reciprocally modulate their signaling functions

Understanding the function of orphan G protein-coupled receptors (GPCRs), whose cognate ligand is unknown, is of major importance as GPCRs…

Publications MRGPRX2 activation as a rapid, high-throughput mechanistic-based approach for detecting peptide-mediated human mast cell degranulation liabilities

Mast cells play key roles in allergy, anaphylaxis/anaphylactoid reactions, and defense against pathogens/toxins. These cells contain cytoplasmic granules with a…

Publications A Pharmacochaperone-Based High-Throughput Screening Assay for the Discovery of Chemical Probes of Orphan Receptors.

G-protein-coupled receptors (GPCRs) have varying and diverse physiological roles, transmitting signals from a range of stimuli, including light, chemicals, peptides,…

Publications PathHunter Pharmacotrafficking: Review how customers used a pharmacochaperone-based high-throughput screening assay approach to discover chemical probes of orphan GPCRs

G-protein-coupled receptors (GPCRs) have varying and diverse physiological roles, transmitting signals from a range of stimuli, including light, chemicals, peptides,…

Publications Use of pharmacotrafficking assays therapeutically beneficial for Type 2 Diabetes

Type 2 diabetes (T2D) affects Latinos at twice the rate seen in populations of European descent. We recently identified a…

Publications Discovery of Potent Agonists for the Predominant Variant of the Orphan MAS-Related GPCR X4 (MRGPRX4)

The MAS-related Gq protein-coupled receptor X4 (MRGPRX4) is poorly investigated. MRGPRX4 has been proposed to be involved in pain transmission,…

White Papers The New World of GPCR Allosteric Modulation

There are at least three unique features of allosteric ligand-receptor interactions that lead to potentially valuable therapeutic behaviors…

eBooks Insights into GPCR Drug Discovery & Development – Exploring GPCR-Ligand Interactions & Signaling Pathways with Binding & Functional Assays

Explore Functional Systems Driving GPCRs to the Forefront of Focused & Safe Therapeutics. Gain insights from industry experts on GPCR…

GPCR β-Arrestin Product Solutions

Universal G-protein independent cell-based assays to quantify GPCR activation based on the recruitment of β-arrestin

GPCR cAMP Product Solutions

Accurately monitor GPCR activation by biologics or small molecules & detect cellular cAMP production levels for a variety of applications

GPCR Calcium Product Solutions

Fluorescent assays to measure calcium mobilization in cell lines as a direct indication of GPCR or ion channel activation or…

Protein Translocation Assays

Screening cell-based assays for analyzing the movement of proteins to multiple membrane compartments within the cell

Pharmacotrafficking Assays

Quantitative cell-based assays to identify pharmacochaperones that stabilize & correct disease-relevant mutant GPCRs, ion channels, or transporters

Build Your Own Assay Tools

Complete set of parental cell lines, vectors, kits, & retroparticles to build your own stable cell lines & cell-based assays

Custom Capabilities

Custom cell lines, kits, assays, & protein development capabilities optimized to fit your requirements

GPCR Internalization Assays

Non-imaging, cell-based internalization assays for screening & identifying safer drugs for GPCRs

Membrane Preparations

Purified GPCR & ion channel membrane preps for binding & functional analysis

GPCR PRODUCT SOLUTIONS