Drug Discovery Services For GPCR Programs

Advance your GPCR discovery programs with Excellerate Bioscience, experts in in vitro GPCR pharmacology.

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Trusted by industry leaders:

50+

Drug Discovery Clients

150+

Drug Discovery Projects Completed

Expert GPCR Cell Signaling & GPCR Drug Discovery

Excellerate Bioscience are an established in vitro pharmacology contract research organisation (CRO) with specialist expertise in GPCR drug discovery.

Based in Nottingham, UK, we have extensive experience of applying our in-depth molecular and cellular pharmacology expertise to help pharmaceutical and biotechnology companies worldwide advance their GPCR drug discovery programs.

GPCRs are largest family of cell surface receptors and play key roles in all physiological processes. It’s no surprise therefore, that they continue to be key targets for drug discovery programs searching for effective new medicines, as well as the being the target for 35% of existing therapeutics.

Our team of scientists brings decades of experience in GPCR pharmacology to your projects, supporting confident decision-making throughout all phases of pre-clinical drug discovery. From target validation to lead optimisation, we work with you to provide both custom and standard assays in GPCR signaling, binding and phenotypic analysis, and support you with advanced pharmacological analysis. We have a track record of delivering programs of work that reduce risk and accelerate the path to the next discovery milestone.

GPCR Expertise You Can Trust

Choosing Excellerate Bioscience means working with scientists who bring deep drug discovery experience and a clear understanding of how data informs decisions. Our leadership team combines academic rigor with industry perspective, ensuring studies are designed to not just generate data but also to answer the right scientific questions.

As well as being internationally recognized expertise in GPCR biology, we have extensive capability in cell-based pharmacology and discovery screening. Our model is to work closely in collaboration with our partners as an extension of their research teams. This collaborative approach adds scientific insight, adding flexibility and helping programs progress efficiently while maintaining high standards of data quality, reproducibility, and interpretation.

Our focus is on delivering robust, decision-ready data that supports earlier and more confident go/no-go decisions, reducing risk and accelerating progression through the discovery pipeline.

Dr Nick Holliday

Nick Holliday

Chief Scientific Officer

Nick has over 25 years’ experience in the molecular pharmacology of GPCRs and other drug targets, and in leading development of biochemical and cellular assay systems for analytical pharmacology and compound profiling.

Dr Steve Briddon

Steve Briddon

Director of Pharmacology

Steve has 30 years’ of GPCR research experience with broad expertise in quantitative molecular pharmacology, biophysical techniques and advanced imaging.

Dr Steve Briddon

Leigh Stoddart

Principal Scientist

Leigh is a receptor pharmacologist with extensive experience of quantitative GCPR pharmacology and managing GPCR programs in a CRO environment.

150+

Studies Completed

50+

Client Programs Advanced

Trusted by Industry Leaders Worldwide

See how we've accelerated discovery programs across therapeutic areas.

"Excellerate is my first-choice recommendation for GPCR pharmacology assay services when advising pharma and life science organizations. The team consistently exceeds expectations in scientific expertise, attention to detail, communication, and project management.

Excellerate brings deep knowledge across GPCR pharmacology, spanning expression technologies and construct design, assay strategy and optimization, data analysis, and clear reporting. They are particularly strong in compound profiling and mechanism-of-action pharmacology, including binding and signaling kinetics.

Communication is a clear strength, with engaging project meetings and responsive turnaround that helps avoid roadblocks and keep programs moving. I strongly recommend Excellerate for GPCR and broader in vitro pharmacology services. "

Sam Hoare

Sam Hoare

Lead Consultant, US SME & Founder, Pharmechanics LLC

Explore Our Scientific Resources

The Excellerate team has made significant contributions to analytical pharmacology, particularly in the field of binding and signalling kinetics.

Here you can access useful resources from the team, as well as publications, presentations and technology spotlights.

Publications

22 April, 2026

Unravelling intrinsic efficacy and ligand bias at G protein coupled receptors: A practical guide to assessing functional data; 2016

Lisa A Stott, David A Hall, Nicholas D Holliday
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22 April, 2026

Discovery, Characterization, and Structure-Based Optimization of Small-Molecule in Vitro and in Vivo Probes for Human DNA Polymerase Theta; 2022

Martin L. Stockley et al. Excellerate contributing authors: Nicholas D. Holliday, Julija Sirina, Viral Patel
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22 April, 2026

High-throughput kinetics in drug discovery; 2024

Maria Filipa Pinto, Julija Sirina, Nicholas D Holliday, Claire L McWhirter
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22 April, 2026

Design, Synthesis, and Application of Fluorescent Ligands Targeting the Intracellular Allosteric Binding Site of the CXC Chemokine Receptor 2; 2023

Bianca Maria Casella, James P. Farmer, Desislava N. Nesheva, Huw E. L. Williams, Steven J. Charlton, Nicholas D. Holliday, Charles A. Laughton, Shailesh N. Mistry
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22 April, 2026

GRK-biased adrenergic agonists for the treatment of type 2 diabetes and obesity; 2025

Aikaterini Motso et al. Excellerate contributing authors: Leigh A. Stoddart, Nicholas D. Holliday
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22 April, 2026

Phenotypic pharmacology of novel Complex I inhibitors eliciting tissue repair concurrent to control of inflammation; 2025

Lisa Patel, Fatima Garcia-Raposo, Benjamin Moore, James Wood, Lily Morley, David Loczenski, Stephen A. Smith, Puneeta Nath, Nicholas Holliday, Sam Williams, Iain R. Greig, Paul Vink, Martyn L. Foster
Read Paper
22 April, 2026

An industrial perspective on ligand bias in GPCR drug discovery; 2025

James P. Farmer, James E. Mason, Nicholas D. Holliday, Stephen J. Briddon, Leigh A. Stoddart
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11 January, 2025

Micro-pharmacokinetics: Qualifying local drug concentration at live cell membranes; 2018

Karolina Gherbi, Stephen J Briddon, Steven J Charlton
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11 January, 2025

Airway remodeling disease: primary human structural cells and phenotypic and pathway assays to identify targets with potential to prevent or reverse remodeling; 2018

Elizabeth M Rosethorne, Steven J Charlton
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11 January, 2025

Extrapyramidal side effects of antipsychotics are linked to their association kinetics at dopamine D2 receptors; 2017

David A Sykes, Holly Moore, Lisa Stott, Nicholas Holliday, Jonathan A Javitch, J Robert Lane, Steven J Charton
Read Paper
11 January, 2025

GPCRs – Structure, Function and Drug Discovery; 2019

Chapter: “Kinetics of ligand binding and signalling”
Read Paper

Frequently Asked Questions

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Location
Excellerate Biosciences Ltd
21 The Triangle
NG2 Business Park
Nottingham
NG2 1AE

Company Number: 10228159

VAT Number: GB 248960957

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