GPCR Drug Discovery
Accelerate Your Research With Sygnature Discovery’s Custom Cell-Based Receptor Expertise
With expertise across 250+ GPCR targets, Sygnature Discovery delivers ready-to-go and custom end-to-end solutions for GPCR target validation, hit identification and lead optimization.
Broad GPCR Target Expertise
GPCRs are integral to many physiological processes, justifying them as key targets for drug discovery. At Sygnature Discovery, we support investigation of receptor signalling and discovery of novel GPCR modulators for a wide range of GPCR targets including:
Metabolic receptors
CNS receptors
Immune receptors
Orphan receptors
Comprehensive Assay Solutions for GPCR Drug Discovery
Our in-house expertise and proven success supports all aspects of GPCR drug discovery, from binding studies to development of complex cell-based solutions enabling investigation of signalling pathways, protein interations and receptor internalization.
Our comprehensive GPCR assay capabilities, including measurement of key secondary messengers and interrogation of bias signalling, offer innovative solutions to enable precise analysis of receptor signalling, protein interactions and receptor internalization, driving robust, data-driven discovery and development.
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Radioligand Binding
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Calcium Mobilization
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cAMP Measurements
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IP-1 Quantification
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ß-Arrestin Recruitment
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G Protein Dissociation
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Receptor Internalization
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Receptor Degradation
Custom GPCR Assay Development
At Sygnature Discovery, we know that each project presents unique challenges. Our dedicated scientists provide tailored assay development solutions, leveraging cell signalling know-how and customized tools to investigate signal transduction for challenging receptors. Whether you need enhanced signal amplificiation, deorphanization support or selective pathway bias profiling, our scientists deliver optimized solutions tailored to your receptor biology and discovery goals.
Assay development
Transient and stable cell-based systems
High-throughput screening
Cell-based signalling and functional assays
lead optimization
Supporting medicinal chemistry campaigns via robust assay cascades
Wider Expertise at Sygnature Discovery
STRUCTURAL BIOLOGY
In-depth structural insights to guide rational drug design
- X-Ray Crystallography
- Cryo-EM
- NMR
- Biophysical tools
IN VIVO PHARMACOLOGY
Translational models across major therapeutic areas including:
- Metabolic disease
- CNS disorders
- Oncology
- Inflammation & Immunology
Contact Syganture Discovery
To learn more about our services or to request a quote.
Customizable screening cascades to investigate 5HT receptor modulation
Serotonin (5-hydroxytryptamine [5HT]) receptors are a family of G-protein coupled receptors and one ligand-gated ion channel involved in signal transduction in response to the neurotransmitter 5HT. While 5HT and its receptors are thought to be involved in many physiological functions, dysfunction of 5HT receptors has also been implicated in numerous CNS disorders.
To aid the discovery of 5HT receptor targeted therapeutics, SB Drug Discovery provides access to a range of 5HT receptor tools, including a comprehensive portfolio of 5HT receptor-expressing cell lines, robust binding assays and downstream functional assays.
| 5HT Receptors and Related Targets | ||||
|---|---|---|---|---|
| 5HT1A | 5HT1B | 5HT2A | Mouse 5HT2A | Rat 5HT2A |
| 5HT2B | 5HT2C | 5HT3A | 5HT4 | 5HT5A |
| 5HT6 | 5HT7 | SERT | ||
With a broad selection of binding and cell-based assay technologies validated and ready to run in high-throughput screening or lead-optimization formats, our plug and play approach to 5HT receptor drug discovery enables custom designed screening cascades to suit your needs.
Customizable screening cascade to investigate adenosine receptor modulation.
Members of the G-protein coupled adenosine receptor family mediate the physiological actions of adenosine via a variety of signal transduction pathways. These receptors are implicated in many pathological functions relating to human disease and represent an important target for therapeutic intervention.
To facilitate adenosine receptor drug discovery research, SB Drug Discovery’s portfolio of adenosine receptor cell line has been used to validate robust off-the-shelf binding and cell-based assays to support your screening and lead optimization studies.
Figure 1: Reproducible dose response curve of NECA against Adenosine A2a in a radioligand binding assay.
Figure 2: Reproducible dose response curve for 8-(3-Chlorostyryl) caffeine against Adenosine A2a in a cell-based assay.
Figure 3: Validated reference inhibitors for Adenosine A2a when stimulated by NECA in a cell-based assay.
Figure 4: Validated reference inhibitors for Adenosine A2a when stimulated by Adenosine in a cell-based assay.
GPCR Case Studies
Here is a list of our GPCR Case Studies click on a title to view the full case study.
