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Better ScienceFor Drug Discovery

Excellerate Bioscience is a UK-based contract research organisation (CRO) specialising in molecular and cellular pharmacology.

50+
Clients
150+
Completed Projects

Our Capabilities

& Drug Discovery Phases

Drug Discovery Phases

Excellerate specialize in developing validation packages across various target classes and therapeutic areas.


Services available within our target validation packages include:

  • Expression profiling performed at mRNA and protein level (qPCR, flow cytometry, Western analysis, immunofluorescence imaging)

  • Phenotypic assays in primary cells to assess target function

  • Libraries of known pathway modulators and approved drugs

  • Recombinant target tool generation

  • siRNA/nucleofection target validation in primary cells

  • Biomarker identification and validation

  • Binding assays (HTRF, TR-FRET, BRET)

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Excellerate provide the expertise and support required to perform efficient hit-to-lead projects in a timely manner for progression to lead series.

  • Comprehensive assay development spanning diverse targets and formats

  • MTS/HTS focused library screening

  • Orthogonal assays to eliminate false positives

  • Mechanism of action, SAR and target engagement studies


We are proficient at managing third-party and custom compound libraries and can profile in vitro HTS cascades (100k+ compound) down to single molecules for comprehensive mechanistic studies covering:

  • Phenotypic screening by single molecule & synergistic studies, cell and species selectivity panels, viability & cytotoxicity assays

  • Functional cellular, biochemical and high-definition kinetics (association/dissociation)

  • Biophysical quantification of target engagement 

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At Excellerate, we provide full support for lead optimization, to transform lead molecules into preclinical candidates.

Based on discussion cycles with clients led by our senior scientific team, Excellerate develop optimal screening strategies, selecting assays tailored to the drug class, target, and indication, advising on pharmacological design.

  • Compound profiling with robust assay validation
  • Assay automation to boost experimental throughput
  • Integration with client data management
  • Compound management with third parties

Our efficient screening, analysis, and reporting workflows minimize iteration times, whilst maintaining accuracy. We actively participate in project meetings, offering expert advice on in vitro pharmacology. Additionally, we provide ongoing support for client milestones, with flexible costing approaches.

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Excellerate provide in-depth mechanistic characterization of drug candidates, supporting clinical data interpretation and competitive profiling.


Our expertise extends to developing comprehensive preclinical publication strategies, integrating phenotypic screening, synergy matrix studies, and advanced cell-based assays.

  • Phenotypic screening

  • Mechanism of action studies

  • Toxicology/cytotoxicity assays

  • Competitor compound profiling

  • Publication strategies

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Capabilities

Excellerate has capabilities to deliver library screening for hit identification through to routine weekly support of lead optimisation projects.

  • Compound profiling with robust assay validation

  • Assay automation to boost throughput

  • Integration with client data management

  • Compound management with third parties


Our tailored approach to assay data handling, analysis and reporting ensures alignment with your specific assay requirements across all in vitro assay screening including:

  • Cellular, biochemical and kinetic assay screening

  • Iterative screening

  • Screening libraries (MTS/HTS; 100k+ compounds)

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Excellerate has capabilities across multiple disease areas, with successful track records in therapeutic drug discovery fields including, but not limited to;

  • Cardiovascular

  • Respiratory

  • Metabolic disease

  • Immunology

  • Oncology

  • CNS

  • Inflammation


Our precision-driven approach aims to address the unique challenges that each disease area poses. We closely align with your program requirements and tailor our scientific support to drive your research forward.

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Excellerate's expertise across diverse modalities can support you in unlocking the potential of your drug candidates.


  • LMw and Biologics: Tailored strategies to optimize efficacy and safety

  • Orthosteric/Allosteric Interactions: Comprehensive analyses of drug-target interactions and mode of action

  • Kinetics and Covalent Inhibitors: Expertise in kinetics for targeted intervention and duration

  • Innovative Biologics: Bispecific antibodies, BiTEs, and ligand-directed therapies

  • Next-Generation Therapies: PROTACs, molecular glues, and novel drug delivery systems

  • Advanced Therapeutic Approaches: Prodrugs, immunomodulators, and synergistic combinations

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Excellerate is internationally recognized for its proficiency in designing and executing in vitro pharmacological assays and utilizing complex theoretical models for data analysis.

Binding & Signaling Kinetics:

  • Binding rate constants (kon/koff)
  • Covalent mechanism analyses, including two-step model and kinact/Ki derived kinetic analyses
  • Real-time quantification of second messenger signaling
  • Integrate kinetics data to comprehend drug action over time

Mode of Action:

  • Competitive and allosteric modulation of drug-target interactions
  • Enzyme mechanisms and inhibition profiles
  • Signaling pathway and ligand bias analysis
  • These descriptors of drug action can be used to better predict clinical efficacy.

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Excellerate has extensive experience working with a wide range of drug target families, including G protein-coupled receptors (GPCRs), kinases, nuclear receptors, enzymes and E3 ligases (targeted protein degradation).


  • GPCRs: Signaling cascades (e.g. cAMP, β-arrestin, calcium)

  • Kinases: Phosphorylation assays, allosteric & orthosteric binding

  • Enzymes: Activity kinetics and substrate profiling

  • Nuclear receptors: Hormone response pathways (e.g. nuclear translocation, transcriptional activity)

  • Cytokines/growth factors: Immune modulation assessment, cytokine release assays, ELISAs

  • E3 ligases/targeted degradation: Targeted protein degradation through ubiquitination assays, PROTAC profiling

  • Subcellular organelle proteins: Subcellular localization (e.g. mitochondrial, lysosomal assays, organelle isolation)

  • Protein-protein interactions

  • Cell cycle/apoptosis/autophagy regulators

  • Non-standard targets

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Excellerate’s team of scientists are highly experienced in the development of in vitro assays report functional outcomes in relevant human cells.

Our reputation extends beyond target-directed pharmacology to dedicated expertise in human primary cell biology, and its application to target validation, screening and mechanism of action.


Phenotypic assays include, but are not limited to: proliferation, differentiation, apoptosis, viability, adhesion, migration, chemoattraction, phagocytosis, live imaging, cytokine release, knockout studies, flow cytometry analysis and cellular metabolism.

Broad panel phenotypic assays/systems covering:

  • Cell health and metabolism

  • Immunophenotyping

  • Multiplex cytokine disease panels

  • Complex models – 3D/spheroid, co-culture

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    As Enterprise Therapeutics, we have worked with Excellerate Bioscience since 2016. The team have enormous experience and have supported two of our drug discovery programs using a range of in vitro assays.

    Most recently Excellerate scientists have become integral members of the wider project team, developing and running primary assays to an exceptionally high quality and providing their broader input across the project. The team are a pleasure to work with, communicating openly and showing great flexibility and proactivity to meet the needs of the project.

    Henry Danahay
    Henry Danahay Head of Biology, Enterprise Therapeutics

    I've been working with Excellerate for over three years now and they certainly exceeded all my expectations. They truly distinguish themselves by taking initiative: they are regularly coming up with new ideas and technologies that have been essential for gaining new insights into the underlying biology of the molecule. Besides, what impresses me is their flexibility and their never lacking engagement, and they're reachable at all times. For more specialized expertise such as electron microscopy (EM), Excellerate ensures collaborations are established to still conduct experiments. Their proactive approach to problem-solving has earned my trust and unwavering recommendation.

    Paul Vink
    Paul Vink Senior Consultant, Biology Lead for UK SME

    Get in touch with the Excellerate team today to speak to one of our of expert scientists

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

    Company Number: 10228159

    VAT Number: GB 248960957

    UK BioIndustry Association
    UK BioIndustry Association
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