Discovery of Therapeutic Phosphatase Activators and Inhibitors

Discovery of Therapeutic Phosphatase Activators and Inhibitors

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Discovery of Therapeutic Phosphatase Activators and Inhibitors


Creative BioMart provides our customers with integrated solutions for the discovery of therapeutic phosphatase activators and inhibitors to help them make the undruggable phosphatases druggable. Our team of scientists with diverse disciplinary backgrounds provides our customers with their extensive experience in developing phosphatase-directed therapeutics.


Phosphatases responsible for the removal of phosphate groups from a range of biomolecules are the important counter players of kinases. Together, these two enzyme families regulate the balance of phosphorylation and dephosphorylation. Imbalance in this physiological state may contribute to the development of diseases, making kinases and phosphatases important therapeutic targets. Phosphatases have both protective and promotive effects on the etiology of diseases and have long been implicated in cancer, neurodegenerative disorders, diabetes and more. Unlike kinases that have been successfully developed as targets for several approved drugs, phosphatases have long been considered “undruggable”. Their evolutionary diversity, conserved active sites within families, and the lack of distinguishing characteristics pose a great challenge for targeting phosphatases. Despite these difficulties, interest in phosphatases as targets for drug discovery has continued and efforts to drug phosphatases have persisted.

Small-molecule activators (left) and inhibitors (right) of protein phosphatases.

Figure 1. Small-molecule activators (left) and inhibitors (right) of protein phosphatases. (De Munter S, et al., 2013)

Overall Solutions

  • Discovery of Therapeutic Phosphatase Activators

    Activation of phosphatases by small molecules offers innovative ways to control signaling pathways and can be functionally complementary to strategies that inhibit kinases. As a solution provider with in-depth knowledge of phosphatases, Creative BioMart is committed to helping our customers tailor solutions for the discovery of small molecule activators of phosphatases and overcome the emerging challenges at every stage of the process.

  • Discovery of Therapeutic Phosphatase Inhibitors

    The ability to selectively inhibit phosphatases offers great therapeutic potential, yet the limited selectivity and adverse pharmacological properties of phosphatase inhibitors remain bottlenecks to their further development. Creative BioMart has developed and streamlined the discovery process for phosphatase inhibitors, particularly for orthosteric and oligomerization inhibitors. We offer end-to-end solution, from initial target identification and validation, through hit identification, to lead optimization.

  • Druggability Assessment

    Phosphatases have long been described as undruggable, making them a largely underexploited resource for therapeutic intervention. Creative BioMart provides both in silico and structure-based druggability assessment of phosphatases to unpack their undruggability and shed more light in the search for new small molecule activators and inhibitors. We help our customers identify druggable sites in phosphatases and drive a new paradigm in drug development.

  • Drugging the Undruggable with Allosteric Small Molecules

    The highly conserved active sites of phosphatases make it difficult to develop drugs that bind directly to orthosteric sites. Newly emerging allosteric small molecules that bind to secondary binding sites named allosteric sites make previously undruggable phosphatases now druggable. Creative BioMart offers advanced methods for the discovery of allosteric activators, inhibitors, and modulators to open new avenues for the development of therapeutics targeting phosphatases.

Related Services

Creative BioMart is a trusted solution provider with many years of experience in kinase/phosphatase biology research and drug development. We have always been committed to providing our customers with high-quality products and customized services to accelerate their cutting-edge research and drug development pipeline. We fully support your project every step of the way to success.

Contact Us

Contact us to find out how our scientists can help you with your drug development project.


  • De Munter S, et al. Challenges and opportunities in the development of protein phosphatase-directed therapeutics. ACS chemical biology, 2013, 8(1): 36-45.
  • Vintonyak V V & Waldmann H, Rauh D. Using small molecules to target protein phosphatases. Bioorganic & medicinal chemistry, 2011, 19(7): 2145-2155.
For research use only. Not intended for any clinical use.