Discovery of a potent protein kinase D inhibitor: insights in the binding mode of pyrazolo[3,4-d]pyrimidine analogues.

Abstract

In this study, we set out to rationally optimize PKD inhibitors based on the pyrazolo[3,4-d]pyrimidine scaffold. The lead compound for this study was 1-NM-PP1, which was previously found by us and others to inhibit PKD. In our screening we identified one compound (3-IN-PP1) displaying a 10-fold increase in potency over 1-NM-PP1, opening new possibilities… (More)
DOI: 10.1039/c6md00675b

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Cite this paper

@article{Verschueren2017DiscoveryOA, title={Discovery of a potent protein kinase D inhibitor: insights in the binding mode of pyrazolo[3,4-d]pyrimidine analogues.}, author={Klaas Verschueren and Mathias Cobbaut and Joachim Demaerel and Lina Saadah and Arnout R. D. Voet and Johan van Lint and Wim M De Borggraeve}, journal={MedChemComm}, year={2017}, volume={8 3}, pages={640-646} }