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Fragment-based drug discovery services have emerged as a revolutionary approach to identifying novel chemical starting points for a wide range of biological targets, including those once considered undruggable. By utilising smaller, basic building blocks known as fragments, this cutting-edge method offers unique advantages in the search for potent drug candidates.

Why Fragments?

Fragment-based drug discovery (FBDD) is an established complementary approach to high-throughput screening (HTS). Contrary to HTS, where large libraries of drug-like molecules are screened, FBDD screens involve smaller and less complex molecules which, despite a low affinity to protein targets, display more ‘atom-efficient’ binding interactions than larger molecules. Fragment hits can, therefore, serve as a more efficient start point for subsequent optimisation, particularly for hard-to-drug targets. Since the number of possible molecules increases exponentially with molecular size, small fragment libraries allow for a proportionately greater coverage of their respective ‘chemical space’ compared with larger HTS libraries comprising larger molecules.

o2h discovery's fragment based drug discovery services

Our Approach

o2h Med Chemists in conjunction with academic computational chemists have designed the library to ensure pharmacophore diversity, molecular complexity, and with the necessary physicochemical characteristics. We continue to expand our library and fill in gaps. We utilise Biacore T200 Surface Plasmon Resonance (SPR) as a primary screening modality to efficiently evaluate fragments for direct binding at high micromolar concentration and subsequently, fragments with confirmed activity are validated in orthogonal experiments such as thermal stability (TS).  If required, we can also plugin support for your X-ray Crystallography and NMR. o2h discovery’s chemists holds expertise in Fragment-Based drug discovery services.

Our Development Strategy

Our SPR assay development team follows a meticulous experimental design strategy:

  • Target immobilisation based on literature precedence
  • Buffer scouting and direct binding with preferred natural peptides or control compounds
  • Competitive displacement or allosteric interaction studies
  • Detailed sensorgrams with graphical illustrations of Kd, Kon, and Koff
  • Optimization of injection time window for maximum signal response
  • Evaluation of immobilised protein stability and target responsiveness

Ascertaining the Future Scaffolds Quality

Initial fragment screening identifies hits with activities >50% of theoretical Rmax, followed by full kinetic characterization. Our approach includes:

  • Discrimination between specific and non-specific interactions using suitable controls
  • Counter screens against unrelated controls or mutant proteins
  • Identity and purity confirmation via LC-MS

Empowering Your Discovery Journey

We can support orthogonal assay validation experiments for better confidence in hit identification such as fluorescence based thermal stability experiments.

Shortlisted fragments can be evolved through:

  • “SAR by catalogue” approach for related molecules
  • Design and synthesis of analogues for improved potency
  • Integrated drug discovery services for multi-platform profiling
  • Leverage structural and computational insights to understand lead molecule binding modes. 
  • Possibility to use site-directed mutagenesis studies to aid SAR elucidation and lead optimization.

Join us on an exciting journey of Fragment-based drug discovery services with o2h discovery. We’re your one-stop solution, offering strategic planning and flawless execution to transform innovative pharmaceutical ideas into reality. Reach out to us at discovery@o2h.com to get a quote.

our team

prashant shah

Prashant Shah

CEO - o2h discovery and Co-Founder - o2h group

Prashant's Biography

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Prashant Shah

CEO - o2h discovery and Co-Founder - o2h group

Prashant is a serial entrepreneur in life sciences and tech in which one of those companies was acquired by a public company. He is currently active in seed investing (a portfolio of ~50 companies), product/IP development, services, and building lab/office infrastructure. The early career was with the Strategy group at Accenture. He has a BEng, an MSc, in which he worked on the Human Genome Program at the Sanger Centre, and an MPhil in Management from the Judge Institute. Prashant is also a General Partner in the o2h SEIS/EIS Human Health Funds.


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Sunil

Sunil Shah

CEO - o2h Ventures and Co-Founder - o2h discovery

Sunil's Biography

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Sunil Shah

CEO - o2h Ventures and Co-Founder - o2h discovery

A serial entrepreneur having begun a career in the Life Sciences team at PA Consulting group followed by co-founding two companies in the information technology and life sciences sector. The second of these companies, Oxygen Healthcare Ltd was acquired by Piramal Enterprises Ltd (BSE: PEL). Sunil co-founded o2h ventures which involves discovery services / collaborations, seeding drug discovery, academic in-licensing and biotechnology incubation. Sunil has a degree in Biochemistry and an MBA from Cambridge University


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Andy Morley

Andy Morley

Chief Scientific Officer

Andy's Biography

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Andy Morley

Chief Scientific Officer

Andy is a highly experienced and accomplished Medicinal Chemist with over 25 years of experience in major pharmaceutical companies such as Sanofi-Aventis and AstraZeneca. He has extensive experience across all phases of drug discovery and has played a key role in the development of five candidates that have reached clinical trials. Andy is a prolific author and inventor, with over 55 publications and patents to his name. Since 2013, he has been working full-time with o2h Limited, where he leads the scientific evaluation of investment opportunities and provides scientific support. He has also served as CSO for two early-stage collaborations within the o2h Ventures portfolio, demonstrating his ability to successfully guide drug discovery projects from concept to clinical development.


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David Davies - o2h

David Davies

Head of Medicinal Chemistry

David's Biography

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David Davies

Head of Medicinal Chemistry

David Davies has 25 years of experience in medicinal chemistry within the pharmaceutical industry with a focus on the antibacterial area (clavulanates, penicillinates, pseudomonates and bacterial topoisomerase inhibitors). He previously worked at GSK and currently holds a part-time academic position at University College London (UCL). He served as the Head of Medicinal Chemistry at Antabio for nearly a decade, specialising in antibacterial research, and has extensive experience managing chemistry projects in multiple countries including France, UK, India and China. He is the inventor of 40 patents and has authored 37 publications.


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o2h group launched revolutionary project management app for drug discovery

o2h group launched revolutionary project management app for drug discovery. The app’s full suite of project management tools is available exclusively to live project collaborators and a lighter version is open for researchers looking for a quote for the synthesis of small molecules.

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