The lead compound may be a screening compound or a series of homologs, or a compound derived from literature. However, for high-throughput screening, discrete, multiple series of emerging compounds may be generated, which requires selecting one of the series to continue research. This process is called "Hit to Lead". After obtaining the seed compound (Hit) through early virtual screening, high-throughput screening, new drug design and other methods, finding the lead compound (Lead) is a key step (Hit-to-Lead) in the development of new drugs.
The discovery of lead compounds is the process of turning the "hits" found in screening into "lead compounds" that can be further optimized. This process uses methods such as skeleton transition, group replacement, structure simplification, and molecular hybridization to modify the chemical structure of the seed compound. The biological activity and selectivity of the seed compound are improved, and the physical and chemical properties, pharmacokinetics, and toxicological properties are also improved. Finally, one or more lead compounds with developmental value are produced, which lays the foundation for the later optimization of lead compounds.
Hit-to-Lead, which explores the chemistry and biology of hits to eliminate dead-end structures and provides improvements to the remaining hit series so that development time and costs are saved, is now a key process in drug discovery organisations. This process explores the chemical space around each hit-series of compounds and narrows it down to more clinic-ready lead structures.
Creative Bioarray has a professional research team and a rich database. We can provide Hit-to-Lead service and solutions according to your research purpose, and we can develop a comprehensive research plan for you.
Creative Bioarray provides you with high-quality data and highly efficient experimental cycles to meet the needs of customers from early drug discovery to new drug application, and is well received by many customers at home and abroad. Hit-to-Lead, which explores the chemistry and biology of hits to eliminate dead-end structures and provides improvements to the remaining hit series so that development time and costs are saved, is now a key process in drug discovery organizations. This process explores the chemical space around each hit-series of compounds and narrows it down to more ‘clinic-ready’ lead structures.
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