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 170 GPCR targets, continually expanding to align with emerging research needs.
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1. A comprehensive collection of ready-to-use GPCR assays featuring over 170 targets across seven species.
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.
✅ 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.
✅ 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
Additional Resources
APPLICATION NOTE:
1. Unlocking New Potential in Drug Discovery with APJ Targeting
2. Screening GPR75 Modulators Using Medium-Throughput Reporter Gene Assay
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.
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