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Related Experiment Video

Updated: Jul 1, 2026

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
13:22

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays

Published on: October 23, 2019

Kinase array design, back to front: biaryl amides.

Ian Baldwin1, Paul Bamborough, Claudine G Haslam

  • 1GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK.

Bioorganic & Medicinal Chemistry Letters
|September 16, 2008
PubMed
Summary
This summary is machine-generated.

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Researchers discovered novel kinase inhibitors using a unique pharmacophore-guided array approach. This method identified potent compounds targeting p38alpha and cFMS kinases, showing promise in cell-based assays and good pharmacokinetic profiles.

Area of Science:

  • Medicinal Chemistry
  • Drug Discovery
  • Biochemistry

Background:

  • Identifying novel kinase inhibitors is crucial for developing targeted therapies.
  • Current array strategies often focus on modifying fragments within the ATP-binding site's purine subpocket.
  • An alternative approach is needed to discover diverse binding groups for kinase inhibition.

Purpose of the Study:

  • To describe a novel pharmacophore-guided array approach for discovering kinase inhibitors.
  • To identify new binding groups targeting the purine subpocket of kinases.
  • To evaluate the potency and pharmacokinetic properties of newly discovered inhibitors.

Main Methods:

  • Design and synthesis of targeted compound arrays using a pharmacophore-guided strategy.

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Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
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Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

A Guided Materials Screening Approach for Developing Quantitative Sol-gel Derived Protein Microarrays
10:44

A Guided Materials Screening Approach for Developing Quantitative Sol-gel Derived Protein Microarrays

Published on: August 26, 2013

Related Experiment Videos

Last Updated: Jul 1, 2026

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
13:22

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays

Published on: October 23, 2019

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
10:33

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

A Guided Materials Screening Approach for Developing Quantitative Sol-gel Derived Protein Microarrays
10:44

A Guided Materials Screening Approach for Developing Quantitative Sol-gel Derived Protein Microarrays

Published on: August 26, 2013

  • Screening of compound arrays against p38alpha and cFMS kinases.
  • Evaluation of compound potency in biochemical and cell-based assays.
  • Assessment of pharmacokinetic properties of promising inhibitor candidates.

    • Main Results:

    • Multiple distinct series of novel purine subpocket-binding groups were discovered.
    • Compounds demonstrated nanomolar potency against p38alpha and cFMS kinases.
    • Several identified compounds exhibited cell-based assay potency and favorable pharmacokinetic properties.

    Conclusions:

    • The pharmacophore-guided array approach is effective for discovering novel kinase inhibitors.
    • This strategy enables the identification of diverse chemical series targeting specific kinase subpockets.
    • The discovered compounds represent promising leads for further drug development.