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My name is Dr. Wayne Carter. Welcome to this lecture entitled drug refinement. Hit and lead.
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The detection of a molecule active against the target macromolecule in a screening assay is termed a hit. A hit compound will likely though require further modification and optimisation in order for it to be suitably efficacious. A lead compound is one that has undergone some level of optimisation, and therefore displays promise for further pre-clinical development as a possible drug candidate.
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High-throughput screening Part 1. A hit compound may be detected using high-throughput screening (HTS). This involves the assessment of libraries of chemicals, that is the ligands, to identify activity against a molecular target or targets. It can be undertaken without any prior knowledge of the drug binding site, and/or after prior in silico screening in an attempt to reduce the number of screened compounds.
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High throughput screening Part 2. The high throughput screening needs to be rapid, but also importantly cost-effective in order to be able to assess the large number of chemicals that may be present in a chemical library. This can be more than a million chemicals. It can utilise microtiter plates such as shown in the image here to perform individualised reactions. Subsequent tests, though, are needed to ensure that the hit is validated to counter the risk of false positives. Lead optimisation.

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