ArticleACS combinatorial science2020
Off-DNA DNA-Encoded Library Affinity Screening.
Article in ACS combinatorial science, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
18 citing papers in PubMed, 37 citations in OpenAlex.
- Automated DNA-Encoded Library Synthesis and Activity-Based Screening at the Attomole Scale.Journal of medicinal chemistry · 2026Article
- Solid-phase DNA-encoded library synthesis: a master builder's instructions.Nature protocols · 2026Review
- Building Block-Centric Approach to DNA-Encoded Library Design.Journal of chemical information and modeling · 2024Article
- Evolution of chemistry and selection technology for DNA-encoded library.Acta pharmaceutica Sinica. B · 2024Review
- Dose-Response Activity-Based DNA-Encoded Library Screening.ACS medicinal chemistry letters · 2023Article
- Small-molecule discovery through DNA-encoded libraries.Nature reviews. Drug discovery · 2023Review
- Hydrogel-Encapsulated Beads Enable Proximity-Driven Encoded Library Synthesis and Screening.ACS central science · 2023Article
- Diversity-oriented synthesis encoded by deoxyoligonucleotides.Nature communications · 2023Article
- Target 2035 - an update on private sector contributions.RSC medicinal chemistry · 2023Article
- Liposomal Permeation Assay for Droplet-Scale Pharmacokinetic Screening.Journal of medicinal chemistry · 2023Article
- Translating the Genome into Drugs.Accounts of chemical research · 2023Article
- Recent advances in DNA-encoded dynamic libraries.RSC chemical biology · 2022Review
- DNA-encoded library versus RNA-encoded library selection enables design of an oncogenic noncoding RNA inhibitor.Proceedings of the National Academy of Sciences of the United States of America · 2022Article
- Strategies for developing DNA-encoded libraries beyond binding assays.Nature chemistry · 2022Review
- Macrocyclic DNA-encoded chemical libraries: a historical perspective.RSC chemical biology · 2022Review
- Antibacterial Discovery via Phenotypic DNA-Encoded Library Screening.ACS chemical biology · 2021Article
- DNA-Encoded Chemistry: Drug Discovery from a Few Good Reactions.Chemical reviews · 2021Review
- Considerations for Achieving Maximized DNA Recovery in Solid-Phase DNA-Encoded Library Synthesis.ACS combinatorial science · 2020Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 2 countries.
Funding
Abstract
DNA-encoded library (DEL) technology is emerging as a key element of the small molecule discovery toolbox. Conventional DEL screens (i.e., on-DNA screening) interrogate large combinatorial libraries via affinity selection of DNA-tagged library members that are ligands of a purified and immobilized protein target. In these selections, the DNA tags can materially and undesirably influence target binding and, therefore, the experiment outcome. Here, we use a solid-phase DEL and droplet-based microfluidic screening to separate the DEL member from its DNA tag (i.e., off-DNA screening), for subsequent in-droplet laser-induced fluorescence polarization (FP) detection of target binding, obviating DNA tag interference. Using the receptor tyrosine kinase (RTK) discoidin domain receptor 1 (DDR1) as a proof-of-concept target in a droplet-scale competition-binding assay, we screened a 67 100-member solid-phase DEL of drug-like small molecules for competitive ligands of DDR1 and identified several known RTK inhibitor pharmacophores, including azaindole- and quinazolinone-containing monomers. Off-DNA DEL affinity screening with FP detection is potentially amenable to a wide array of target classes, including nucleic acid binding proteins, proteins that are difficult to overexpress and purify, or targets with no known activity assay.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.