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Showing 1–2 of 2 results
Advanced filters: Author: Gergely Makara Clear advanced filters

  • By analysing the physicochemical properties of a database of hits and leads, Keserü and Makara conclude that high-throughput screening, as well as hit-to-lead optimization practices in general, are responsible for the unfavourable physicochemical profile of recent leads and clinical candidates. Major adjustments may be needed to enable a balanced lead-evolution process and reduce the likelihood of high compound-related attrition in clinical trials.

    • György M. Keserü
    • Gergely M. Makara
    Research
    Nature Reviews Drug Discovery
    Volume: 8, P: 203-212

  • Medicinal chemistry optimizations in the progression from hit to lead to drug candidate affect properties of small-molecule drugs such as their molecular weight and lipophilicity. This Perspective analyses the properties of orally administered small-molecule drug candidates reported in the period 2015–2022 and their corresponding hit and lead compounds, and compares them with the properties of drug candidates identified between 2000 and 2010 and their hits and leads, with the aim of improving understanding of the evolution of hit finding and optimization strategies.

    • Anita Rácz
    • Levente M. Mihalovits
    • György M. Keserű
    Reviews
    Nature Reviews Drug Discovery
    Volume: 24, P: 870-887