GPCR Assay Services

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GPCR-targeted Assay Service

GPCRs (G protein-coupled receptors) constitute a crucial class of membrane receptors, surpassing 800 members. These receptors, characterized by seven transmembrane domains, orchestrate various physiological processes through intricate signaling pathways. Their pivotal role has positioned GPCRs as attractive therapeutic targets for a multitude of diseases.

ICE Bioscience has diligently developed a comprehensive range of solutions for efficient GPCR-based drug discovery and development. Presently, we provide ready-to-use assays covering more than 190 GPCR targets, continually expanding to align with emerging research needs.

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190+ GPCR Targets Covered Across Human and Preclinical Species (Including Species Variants)
5-HT1AAPJCCR1D1GLP-1RMT1DORP2Y1
5-HT1BhCTRCCR2D2LMouse GLP-1RMT2KORP2Y2
5-HT1FhAMY1CCR4D2SRat GLP-1RM1MORP2Y6
5-HT2AhAMY2CCR5D3Dog GLP1RM2Rat MORP2Y12
5-HT2BhAMY3CCR6D4Monkey GLP1RM3Mouse MORSSTR1
5-HT2CRat CTRCCR7D5Rabbit GLP1RM4NOPSSTR2
5-HT4ARat AMY1CCR8ETAGLP-2RRat M4Rat NOPSSTR3
5-HT4BRat AMY3CCR9AETBGIPRMouse M4Mouse NOPSSTR4
5-HT5ADog CTRCCR9BRat ETBDog GIPRMonkey M4DP1SSTR5
5-HT7ADog AMY3CXCR1Mouse ETBMonkey GIPRDog M4EP1NK1
5-HT7BMonkey CTRCXCR2Dog ETBMouse GIPRRabbit M4EP2Rat NK1
A1Monkey AMY3CXCR4FPR1Rat GIPRM5Rat EP2Mouse NK1
A2AhCGRP1CCK1Mouse FPR1Rabbit GIPRMC1Mouse EP2NK2
A2BhAM1CCK2Monkey FPR1GCGRMC4EP3Mouse NK2
Alpha 1AhAM2MRGPRX1FPR2Mouse GCGRMC5EP4Rat NK2
Alpha 1BBeta 1MRGPRX2FFAR3(GPR41)Rat GCGRmGlu2Rat EP4NK3
Alpha 1DBeta 2Dog MRGPRX2GPR3H1mGlu7Mouse EP4Rat NK3
Alpha 2AAT1Monkey MRGPRX2GPR6H2NPY2RFPMouse NK3
Alpha 2BAT2MRGPRB2GPR12H3V1aTPRabbit NK3
Alpha 2CTGR5hGPR52GPR65S1P1V1bIPGnRH
OXTRBDKRB2mouse GPR52OX1S1P2V2PAR1Rat GnRH
Rat OXTRBDKRB1rat GPR52OX2S1P3LPA1PAR4Mouse GnRH
BB1CB1Monkey GPR52GPR40C3aR1LPA3PAR2Rabbit GnRH
BB2CB2Dog GPR52TAAR1C5aR1PTH1RGPR17-SGPR17-L
BB3CASRGPR35GPR84GPR75


Key Features

1. 190+ GPCR targets covered across human and preclinical species (including species variants).

2. Various binding and functional assays available.

3. Assessment of agonist, antagonist, and PAM functional modes.

4. Custom cell line develpment services, providing flexibility in cell line choices.

5. Options for single-dose screening or dose-response for EC50 and IC50 determination.

6. Rapid screening with turnaround time of 1-2 weeks.

ICE Bioscience can provide a rapid assessment of drug efficacy, potency, selectivity, and safety, reducing downstream attrition rates in drug development. Benefiting from a comprehensive GPCR target platform, ICE Bioscience offers a versatile spectrum of panel screening solutions for the GPCR family. This includes specialized GPCR panels, safety panels, along with customizable panel testing services. These panels are comprehensively supported by high-throughput instruments, enabling fast and efficient screening and analysis.

GPCR Binding Assays

Biophysical Binding Assay: Our assay combines Biacore 8K's real-time SPR for detailed GPCR-ligand kinetics with Dianthus's Spectral Shift and TRIC technologies for rapid, high-throughput binding assays, providing comprehensive, high-sensitivity binding data.

Radioligand Binding Assay: This assay provides highly sensitive and precise measurements of ligand-receptor interactions.

Flow Cytometry-Based Binding Assay: This assay is valuable for studying cell surface GPCRs, where fluorescently labeled ligands or antibodies can detect and quantify receptor binding in real time.

✅ Tag-Lite Binding Assay: This system operates via a competitive binding format, and the resulting signal change enables quantification of binding affinity.

GPCR Functional Assays Featuring Multiple Readouts

cAMP Assay: Our GPCR Cell-Based cAMP Assay is specifically designed to measure cAMP levels, providing a key readout for G protein-dependent signaling through Gs or Gi-coupled GPCRs.

IP1 Assay: This assay is designed to measure the buildup of inositol monophosphate (IP1), it's especially valuable for studying GPCRs that activate through the Gq pathway.

Calcium Flux Assay by FLIPR: Our Calcium Flux Assay utilizes the FLIPR (Fluorescence Imaging Plate Reader) system to measure changes in intracellular calcium levels, a key indicator of Gq protein-dependent signaling.

Reporter Gene Assay: The assay measures GPCR activation by utilizing reporter genes like luciferase that are linked to specific signaling pathways.

β-Arrestin Recruitment Assay: Unlike traditional functional assays that measure second messengers (e.g., cAMP or calcium flux), this assay provides insights into β-arrestin-dependent signaling.

GTPγS Binding Assay: GTPγS, a non-hydrolyzable analog of GTP, binds to the G-protein, allowing for the direct assessment of GPCR-mediated G-protein activation without further signaling turnover.

Internalization Assay: High-content imaging allows for real-time, quantitative measurement of receptor internalization following ligand binding.

✅ pERK/pAKT In-Cell Western Assay 

✅ Chemotaxis Assay



Contact Us

We value your inquiries and are here to provide you with tailored solutions for your drug discovery and development needs. Whether you have questions, require more information, or are interested in discussing potential collaborations, our team of experts is just a message away.
Feel free to reach out to us.

We are a CRO service organization, not a hospital




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