High-throughput screening (HTS) is an experimental approach that rapidly tests very large numbers of chemical compounds, biological samples, or genetic perturbations against a defined biological target or assay to identify active candidates. Central to early drug discovery, it uses miniaturised assays in microplate …
High-throughput screening (HTS) is an experimental approach that rapidly tests very large numbers of chemical compounds, biological samples, or genetic perturbations against a defined biological target or assay to identify active candidates. Central to early drug discovery, it uses miniaturised assays in microplate formats, laboratory automation and robotics, sensitive detection systems, and data-analysis pipelines to evaluate thousands to millions of samples efficiently. Assays are designed as readouts of a biological response, such as enzyme activity, receptor binding, gene expression, or cellular signalling, and may be biochemical or cell-based; functional cellular assays, including calcium-transient and other phenotypic measurements in human induced pluripotent stem cell-derived cells, allow screening in physiologically relevant systems. Compounds that produce a desired effect are flagged as hits and progress through confirmation, dose-response characterisation, and counter-screening to remove artefacts and establish selectivity, yielding validated leads for medicinal-chemistry optimisation. HTS complements computational and structure-based methods, with in silico screening and rational design used to focus libraries and prioritise candidates for in vitro and in vivo testing. It is applied to small-molecule discovery, target validation, and the profiling of compound activity and toxicity. As a scalable engine for hit identification, high-throughput screening links library design, assay development, automation, and informatics within modern molecular biology and pharmaceutical research.
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