GPCR Drug Discovery

Accelerate Your Research With SB Drug Discovery’s Custom Cell-Based Receptor Expertise

Accelerate your receptor drug discovery with SB Drug Discovery’s industry-leading expertise in membrane proteins and cell signalling. We offer a comprehensive suite of off-the-shelf and custom receptor assays designed to streamline and empower your GPCR research, from target development through to hit identification and lead optimization.

Broad GPCR Target Expertise

GPCRs are integral to many physiological processes, making them a key focus in drug discovery. At SB Drug Discovery, we support a wide range of GPCR targets, including:

Metabolic receptors

Metabolic receptors

CNS receptors

CNS receptors

Immune receptors

Immune receptors

Orphan receptors

Orphan receptors

Extensive GPCR Assay Capabilities

Our comprehensive portfolio of off-the-shelf and custom assays support every phase of GPCR research, from initial target validation to  hit identification and lead optimization.

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Assay development

Transient and stable cell-based systems

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High-throughput screening

Cell-based signalling and functional assays

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lead optimization

Supporting medicinal chemistry campaigns via robust assay cascades 

Custom GPCR Assay Development

At SB Drug Discovery, we know that each project presents unique challenges. Our dedicated scientists provide tailored assay development, leveraging cell signalling know-how and customized g-proteins to enhance signal transduction for challenging receptors. From custom assays to protocol modifications, we partner closely with you to optimize each GPCR assay, delivering robust data that enhances confidence in every stage of your drug discovery pipeline.

Comprehensive Assay Solutions for GPCR Drug Discovery

Our comprehensive GPCR drug discovery assay capabilities, featuring calcium mobilization, IP-1 measurement, cAMP accumulation, and more, offer innovative solutions to enable precise analysis of receptor signalling, protein interactions, and receptor internalization, driving robust, data-driven discovery and development.

  • Calcium Mobilization

  • IP-1 Measurement 

  • cAMP Accumulation

  • Reporter Assay

  • Biosensors

  • Biased Signalling

  • Protein Interaction

  • Receptor Internalization

Contact SB Drug 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.

Receptors- 5HT2A screening cascade options

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 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 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 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.

Figure 4: Validated reference inhibitors for Adenosine A2a when stimulated by Adenosine in a cell-based assay.

Case Study

Custom tools for GIP receptor drug discovery

Custom tools for GIP receptor drug discovery
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