High-throughput screening (HTS) is a drug discovery technique that uses automated equipment to test millions of samples for biological activity. HTS is a standard method in the pharmaceutical industry.
Regulatory Toxicology: the role, content and evolution of toxicology and pathology in non-clinical studies
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High-throughput
screening
, Commonly used terms in drug discovery
• High throughput screen: an optimized, miniaturized assay format that enables the testing of >
100,000 chemically diverse compounds per day.
• Assay: a test system in which biological activity can be detected
• Hit: a molecule with confirmed concentration-dependent activity in a screen, and known chemical
structure. The output of most screens
• Progressible hit: a representative of a compound series with activity via acceptable mechanism of
action and some limited structure-activity relationship information
• Lead: a compound with potential (as measured by potency, selectivity, physico-chemical properties,
absence of toxicity or novelty) to progress to a full drug development programme
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