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High-throughput screening and DNA-encoded libraries

Testing millions or billions of chemical compounds against a cancer target automatically to find starting points for new drugs.

Robotic HTS of 1-2 million compound libraries, fragment screening by NMR or crystallography, DNA-encoded libraries (X-Chem, HitGen, WuXi; billions of compounds per pool), affinity-selection mass spectrometry, and virtual screening of ultra-large make-on-demand spaces (Enamine REAL, tens of billions) supply hits; CRISPR pooled screens (Broad DepMap, Sanger) supply the targets. Automation vendors: Beckman, Hamilton, Tecan, Thermo Fisher; readouts increasingly imaging-based (cell painting).

Generic schematic · not to scale · placeholder for the drug discovery front
Guide RNA library · Knockout → dependency

How it works

Parallel assays in microtitre plates or barcoded pools identify binders or phenotypic modulators, followed by hit confirmation and medicinal chemistry.

Strengths
  • Unbiased hit discovery
  • DEL and virtual screening explore vast chemical space cheaply
Limitations
  • False positives and assay artefacts
  • Hits far from drugs
  • Undruggable targets still resist

Key papers

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Latest papers

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Latest papers · live from Europe PMC
Open in Europe PMC

Query for this technology: (TITLE:"High-throughput screening and DNA-encoded libraries" OR ABSTRACT:"High-throughput screening and DNA-encoded libraries") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about High-throughput screening and DNA-encoded libraries, not a curated reading list.

Connected

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