Background

G-Protein Coupled Receptors

At Sygnature Discovery, we provide end-to-end GPCR solutions grounded in more than 20 years of cell signalling expertise.

GPCRs play a vital role in numerous physiological processes, making them essential targets for drug discovery. Our integrated approach brings together advanced assay platforms and tailored strategies to support receptor research at every stage.

With experience investigating over 250 GPCR targets and developing more than 100 validated cell lines, we deliver robust, reproducible insights through tools such as ligand binding, G protein interaction studies, β-arrestin recruitment, and secondary messenger analysis. Our expertise, from deorphanization to bias signalling, ensures you have the solutions you need to address complex receptor challenges.

Automated laboratory equipment used for GPCR assays, supporting receptor activity analysis and pharmacological screening.

Comprehensive Assay Solutions for GPCR Drug Discovery

Our in-house capabilities enable precise analysis of receptor signalling, protein interactions, and receptor internalization. We combine innovative technologies with proven expertise to deliver data-driven discovery and development.

Our assay portfolio includes:

• Radioligand binding

• Calcium mobilization

• cAMP measurements

• IP-1 quantification

• β-arrestin recruitment

• G protein dissociation

• Receptor internalization

• Receptor degradation

These tools allow us to interrogate bias signaling and measure key secondary messengers, driving confident decision-making throughout your program.

Integrated Drug Discovery Support

Seamless GPCR expertise from target to candidate. Our integrated GPCR platform combines cell signalling know-how, structural biology, and medicinal chemistry to accelerate candidate selection. From high-throughput screening to in vivo pharmacology, we deliver seamless, data-driven support to advance your target with confidence.

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GPCR Assay Optimization with Chimeric G Proteins
GPCR Assay Optimization with Chimeric G Proteins
GPCR assay optimization using chimeric G proteins enables improved signalling control and enhanced assay performance.
Case Studies
5-HT2A Receptor Screening for Psychedelics
5-HT2A Receptor Screening for Psychedelics
5-HT2A receptor screening at Sygnature Discovery enables comparison of hallucinogenic and non-hallucinogeneic psychedelic compounds using…
Case Studies
GIP Receptor Screening & Custom Assays
GIP Receptor Screening & Custom Assays
GIP receptor screening tools developed at Sygnature Discovery enable tailored assay development and functional characterization…
Case Studies
Purifying 5-HT2AR GPCR for cryo-EM Structural Studies
Purifying 5-HT2AR GPCR for cryo-EM Structural Studies
Ben’s PIPs Placement Journey with Peak Proteins In this article PhD Student Ben Nash discusses…
Case Studies
Quantifying GPCR Activation with NanoBiT Assay for Ligand Screening
Quantifying GPCR Activation with NanoBiT Assay for Ligand Screening
A versatile NanoBiT assay for ligand screening GPCRs remain key therapeutic targets, yet many –…
Posters

Related Capabilities

We bring together a dynamic blend of new talent and experiences pharmaceutical industry experts from around the world, delivering excellence across each stage of discovery.

Cell line generation

Custom stable cell lines with robust expression and assay reproducibility, streamlined design and validation for confident drug discovery workflows.

High Throughput Screening

Integrated hit identification using HTS, fragment screening, and advanced automation delivering high-quality starting points for successful drug discovery.