{"entity":{"id":"high-throughput-screening-libraries","kind":"technology","name":"High-throughput screening and DNA-encoded libraries","aka":[],"tldr":"Testing millions or billions of chemical compounds against a cancer target automatically to find starting points for new drugs.","summary":"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).","status":"established","asOf":"2026-09-08","links":[{"label":"Goodnow et al., DNA-encoded chemistry: enabling the deeper sampling of chemical space (Nature Reviews Drug Discovery 2016)","url":"https://doi.org/10.1038/nrd.2016.213"}],"tags":["supporting"],"related":[],"cancers":[],"sections":["drug-discovery"],"technologies":["ai-drug-design","synthetic-lethality-approaches","protac-degrader"],"targets":[],"drugs":[],"companies":["thermo-fisher"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":["paper-depmap-tsherniak-cell-2017","paper-goodnow-nat-rev-drug-discov"],"journals":[],"dependsOn":[],"notes":[],"principle":"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"]},"route":"/technologies/high-throughput-screening-libraries/","neighbours":{"section":[{"id":"drug-discovery","kind":"section","name":"Drug Discovery Platforms","route":"/fronts/drug-discovery/"}],"technology":[{"id":"ai-drug-design","kind":"technology","name":"AI-driven drug & target discovery","route":"/technologies/ai-drug-design/"},{"id":"functional-precision-medicine-haematology","kind":"technology","name":"Ex vivo drug sensitivity screening in blood cancers (EXALT)","route":"/technologies/functional-precision-medicine-haematology/"},{"id":"protac-degrader","kind":"technology","name":"PROTACs & molecular glues (targeted protein degradation)","route":"/technologies/protac-degrader/"},{"id":"synthetic-lethality-approaches","kind":"technology","name":"Synthetic lethality approaches","route":"/technologies/synthetic-lethality-approaches/"}],"company":[{"id":"thermo-fisher","kind":"company","name":"Thermo Fisher Scientific","route":"/companies/thermo-fisher/"}],"paper":[{"id":"paper-depmap-tsherniak-cell-2017","kind":"paper","name":"Defining a Cancer Dependency Map: which genes each cancer cell line cannot live without","route":"/key-papers/paper-depmap-tsherniak-cell-2017/"},{"id":"paper-goodnow-nat-rev-drug-discov","kind":"paper","name":"DNA-encoded chemistry: enabling the deeper sampling of chemical space","route":"/key-papers/paper-goodnow-nat-rev-drug-discov/"}],"roadmap":[{"id":"drug-discovery-roadmap","kind":"roadmap","name":"Drug discovery roadmap: screening in mice → maps of dependency → designing in silico","route":"/roadmaps/drug-discovery-roadmap/"}]}}