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Hit-to-lead
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Summary
Hit-to-lead (H2L) is a crucial phase in
Drug Discovery
where
Initial compounds
identified as 'hits' are optimized and refined to become 'lead' compounds with
Improved efficacy
, selectivity, and
Pharmacokinetic properties
. This process involves a series of
Chemical Modifications
and
Biological evaluations
to enhance the drug's potential for further development.
Concepts
Drug Discovery
Chemical Optimization
Pharmacokinetics
Structure-activity Relationship (SAR)
High-Throughput Screening (HTS)
Medicinal Chemistry
Biological Evaluation
Lead Optimization
Molecular Docking
ADME (Absorption, Distribution, Metabolism, And Excretion)
Phenotypic Screening
Lead Compound
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