The application of high-throughput screening to novel lead discovery

Part of the Progress in Drug Research book series (PDR, volume 51)


The ability to discover new lead compounds for novel therapeutic targets is a pivotal step in drug discovery programmes. High-throughput screening (HTS) utilises a number of platforms for the rapid screening of novel targets to accelerate this process. Key issues in HTS include assay configuration and the ability of a high-throughput screen to predict drug-target interactions accurately. This review highlights a number of issues in the HTS process and describes three key target areas that are likely to be sources of novel, therapeutically important drugs. Particular emphasis is placed on the mechanistic basis of drug-target interactions that are of prime importance in the design of HTS approaches. Critical aspects of information management related to HTS are summarised.


High-throughput screening automation informatics receptors G-proteins ion channels kinases drug discovery orphan receptors 

Glossary of abbreviations


high-throughput screening


scintillation proximity assay


homogeneous timeresolved fluorescence


enzyme-linked immunoabsorbtion assay


green fluorescent protein


receptor tyrosine kinases


G-protein-coupled receptor


epidermal growth factor receptor


fluorescence resonance energy transfer


cyclic-AMP response element


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Copyright information

© Springer Basel AG 1998

Authors and Affiliations

  1. 1.Cambridge Drug DiscoveryCambridgeUK

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