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Advanced filters: Author: "Anne Hersey" Clear advanced filters

  • The success of mechanism-based drug discovery depends on the definition of the drug target, but targets are often poorly defined in the literature. Here, Overington and colleagues present a comprehensive map of the molecular targets of approved drugs, and explore aspects including the footprint of target classes across disease areas, the success of privileged target families and drug target orthologues across standard model organisms.

    • Rita Santos
    • Oleg Ursu
    • John P. Overington
    Research
    Nature Reviews Drug Discovery
    Volume: 16, P: 19-34

  • A common assumption in current drug discovery strategies is that compounds with highin vitro potency at their target(s) have a greater potential to translate into successful, low-dose therapeutics, which is reflected in screening cascades with in vitro potency embedded as an early filter. This analysis of the publicly available ChEMBL database, which includes more than 500,000 drug discovery and marketed oral drug compounds, suggests that the perceived benefit of high in vitropotency may be negated by poorer absorption, distribution, metabolism, elimination and toxicity (ADMET) properties.

    • M. Paul Gleeson
    • Anne Hersey
    • John Overington
    Research
    Nature Reviews Drug Discovery
    Volume: 10, P: 197-208