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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| 5-HT1A | APJ | CCR1 | D1 | GLP-1R | MT1 | DOR | P2Y1 |
| 5-HT1B | hCTR | CCR2 | D2L | Mouse GLP-1R | MT2 | KOR | P2Y2 |
| 5-HT1F | hAMY1 | CCR4 | D2S | Rat GLP-1R | M1 | MOR | P2Y6 |
| 5-HT2A | hAMY2 | CCR5 | D3 | Dog GLP1R | M2 | Rat MOR | P2Y12 |
| 5-HT2B | hAMY3 | CCR6 | D4 | Monkey GLP1R | M3 | Mouse MOR | SSTR1 |
| 5-HT2C | Rat CTR | CCR7 | D5 | Rabbit GLP1R | M4 | NOP | SSTR2 |
| 5-HT4A | Rat AMY1 | CCR8 | ETA | GLP-2R | Rat M4 | Rat NOP | SSTR3 |
| 5-HT4B | Rat AMY3 | CCR9A | ETB | GIPR | Mouse M4 | Mouse NOP | SSTR4 |
| 5-HT5A | Dog CTR | CCR9B | Rat ETB | Dog GIPR | Monkey M4 | DP1 | SSTR5 |
| 5-HT7A | Dog AMY3 | CXCR1 | Mouse ETB | Monkey GIPR | Dog M4 | EP1 | NK1 |
| 5-HT7B | Monkey CTR | CXCR2 | Dog ETB | Mouse GIPR | Rabbit M4 | EP2 | Rat NK1 |
| A1 | Monkey AMY3 | CXCR4 | FPR1 | Rat GIPR | M5 | Rat EP2 | Mouse NK1 |
| A2A | hCGRP1 | CCK1 | Mouse FPR1 | Rabbit GIPR | MC1 | Mouse EP2 | NK2 |
| A2B | hAM1 | CCK2 | Monkey FPR1 | GCGR | MC4 | EP3 | Mouse NK2 |
| Alpha 1A | hAM2 | MRGPRX1 | FPR2 | Mouse GCGR | MC5 | EP4 | Rat NK2 |
| Alpha 1B | Beta 1 | MRGPRX2 | FFAR3(GPR41) | Rat GCGR | mGlu2 | Rat EP4 | NK3 |
| Alpha 1D | Beta 2 | Dog MRGPRX2 | GPR3 | H1 | mGlu7 | Mouse EP4 | Rat NK3 |
| Alpha 2A | AT1 | Monkey MRGPRX2 | GPR6 | H2 | NPY2R | FP | Mouse NK3 |
| Alpha 2B | AT2 | MRGPRB2 | GPR12 | H3 | V1a | TP | Rabbit NK3 |
| Alpha 2C | TGR5 | hGPR52 | GPR65 | S1P1 | V1b | IP | GnRH |
| OXTR | BDKRB2 | mouse GPR52 | OX1 | S1P2 | V2 | PAR1 | Rat GnRH |
| Rat OXTR | BDKRB1 | rat GPR52 | OX2 | S1P3 | LPA1 | PAR4 | Mouse GnRH |
| BB1 | CB1 | Monkey GPR52 | GPR40 | C3aR1 | LPA3 | PAR2 | Rabbit GnRH |
| BB2 | CB2 | Dog GPR52 | TAAR1 | C5aR1 | PTH1R | GPR17-S | GPR17-L |
| BB3 | CASR | GPR35 | GPR84 | GPR75 |
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.
✅ 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
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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