The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist

Joseph Rimland, Angela Dunne, Suchete S Hunjan, Rosemary Sasse, Iain Uings, Dino Montanari, Matilde Caivano, Poonam Shah, David Standing, David Gray, David Brown, William Cairns, Ryan Trump, Paul W Smith, Nicolas Bertheleme, Pier D'Alessandro, Sheraz Gul, Mythily Vimal, David N Smith, Stephen P Watson

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    6 Citations (Scopus)

    Abstract

    The identification of novel, potent, non-steroidal/small molecule functional GR antagonist GSK1564023A selective over PR is described. Associated structure-activity relationships and the process of optimisation of an initial HTS hit are also described.
    Original languageEnglish
    Pages (from-to)2340-3
    Number of pages4
    JournalBioorganic & Medicinal Chemistry Letters
    Volume20
    Issue number7
    DOIs
    Publication statusPublished - Apr 2010

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    Rimland, J., Dunne, A., Hunjan, S. S., Sasse, R., Uings, I., Montanari, D., Caivano, M., Shah, P., Standing, D., Gray, D., Brown, D., Cairns, W., Trump, R., Smith, P. W., Bertheleme, N., D'Alessandro, P., Gul, S., Vimal, M., Smith, D. N., & Watson, S. P. (2010). The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist. Bioorganic & Medicinal Chemistry Letters, 20(7), 2340-3. https://doi.org/10.1016/j.bmcl.2010.01.133