Biomedical Basics

Hit-to-lead process

  • Created by Henry Stewart Talks
Published on September 30, 2026   4 min

A selection of talks on Pharmaceutical Sciences

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The following session will cover hit to lead process, focusing on the main stages of the hit to lead process in drug discovery, focusing on the transition from initial hit identification to the selection and optimization of promising lead compounds. We will discuss key screening techniques, hit triage, and criteria for advancing compounds, including drug likeness and developability. Lecture will highlight the iterative process of structure activity relationship studies, early Ad MET assessments, and the technologies that enhance efficiency. By the end, you will understand how the integration of various scientific disciplines and risk management strategies drive successful lead compound identification for further drug development. The journey from initial hit identification to the establishment of robust lead compounds is central to early drug discovery. This phase is the critical bridge between biological screening and medicinal chemistry optimization. The main goal is to refine and prioritize promising hits into advanced leads suitable for further drug development, integrating chemistry, biology, and computational tools to maximize success and minimize costly failures. Our journey begins with hit identification, high throughput, fragment based, and in silico screening help locate molecules capable of interacting with the therapeutic target. In high throughput screening, millions of compounds are tested, but less than one tenth of 1% become hits. These undergo rigorous filtering through computational and experimental triage,

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