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- W2921000810 abstract "Robotic high-throughput compound screening (HTS) and, increasingly, DNA-encoded library (DEL) screening are driving bioactive chemical matter discovery in the postgenomic era. HTS enables activity-based investigation of highly complex targets using static compound libraries. Conversely, DEL grants efficient access to novel chemical diversity, although screening is limited to affinity-based selections. Here, we describe an integrated droplet-based microfluidic circuit that directly screens solid-phase DELs for activity. An example screen of a 67 100-member library for inhibitors of the phosphodiesterase autotaxin yielded 35 high-priority structures for nanomole-scale synthesis and validation (20 active), guiding candidate selection for synthesis at scale (5/5 compounds with IC50 values of 4–10 μM). We further compared activity-based hits with those of an analogous affinity-based DEL selection. This miniaturized screening platform paves the way toward applying DELs to more complex targets (signaling pathways, cellular response) and represents a distributable approach to small molecule discovery." @default.
- W2921000810 created "2019-03-22" @default.
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- W2921000810 creator A5081641289 @default.
- W2921000810 date "2019-03-18" @default.
- W2921000810 modified "2023-10-16" @default.
- W2921000810 title "Activity-Based DNA-Encoded Library Screening" @default.
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- W2921000810 doi "https://doi.org/10.1021/acscombsci.9b00037" @default.
- W2921000810 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/6786493" @default.
- W2921000810 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30884226" @default.
- W2921000810 hasPublicationYear "2019" @default.
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