Lesson plan

Lead compound

A lead compound ( , i.e., a "leading" compound; not to be confused with various compounds of the element lead) in drug discovery is a chemical compound that has or biological activity likely to be therapeutically useful, but may have suboptimal structure that requires modification to fit better to the target; lead drugs offer the prospect of being followed by compounds. The chemical structure serves as a starting point for chemical modifications in order to improve potency, selectivity, or parameters. Furthermore, newly-invented active moieties may have poor druglikeness and may require chemical modification to become enough to be tested biologically or clinically. Lead compounds are sometimes called developmental candidates. This is because the discovery and selection of lead compounds occurs prior to preclinical and clinical development of the candidate.

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Article summary

A lead compound ( , i.e., a "leading" compound; not to be confused with various compounds of the element lead) in drug discovery is a chemical compound that has or biological activity likely to be therapeutically useful, but may have suboptimal structure that requires modification to fit better to the target; lead drugs offer the prospect of being followed by compounds. The chemical structure serves as a starting point for chemical modifications in order to improve potency, selectivity, or parameters. Furthermore, newly-invented active moieties may have poor druglikeness and may require chemical modification to become enough to be tested biologically or clinically. Lead compounds are sometimes called developmental candidates. This is because the discovery and selection of lead compounds occurs prior to preclinical and clinical development of the candidate.

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Discussion questions

  1. Summarise the article in your own words. Which single claim would you verify first, and why?
  2. Which claim in this article is most likely to be revised as the sources update? How would you check its current status?
  3. If two sources disagreed about one of these facts, what would you need in order to trust one over the other?

Bibliography

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Key claims and bibliography are generated from the same tracked claims and sources as the article page.