ArticleChemistry (Weinheim an der Bergstrasse, Germany)2017
A Specific and Covalent JNK-1 Ligand Selected from an Encoded Self-Assembling Chemical Library.
Article in Chemistry (Weinheim an der Bergstrasse, Germany), 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
20 citing papers in PubMed, 76 citations in OpenAlex.
- On-resin Heck coupling enables small-molecule ligand discovery with covalent peptide-encoded libraries.Chemical science · 2026Article
- Fusion Strategy of DNA-Encoded Libraries Drives Discovery of Allosteric Inhibitors of SARS-CoV‑2 RdRp.JACS Au · 2026Article
- The Current Toolbox for Covalent Inhibitors: From Hit Identification to Drug Discovery.JACS Au · 2025Review
- RNA-Focused DNA-Encoded Library Construction, Screening, and Integration of Docking Identify Bioactive Ligands of Pathogenic r(GbioRxiv : the preprint server for biology · 2025Article
- Flexibility-tuning of dual-display DNA-encoded chemical libraries facilitates cyclic peptide ligand discovery.Nature communications · 2025Article
- Identification of Structurally Novel KRASJournal of medicinal chemistry · 2025Article
- Protein-templated ligand discovery via the selection of DNA-encoded dynamic libraries.Nature chemistry · 2024Article
- Evaluation of a Covalent Library of Diverse Warheads (CovLib) Binding to JNK3, USP7, or p53.Drug design, development and therapy · 2024Article
- Advances in covalent drug discovery.Nature reviews. Drug discovery · 2022Review
- Triazine-Based Covalent DNA-Encoded Libraries for Discovery of Covalent Inhibitors of Target Proteins.ACS medicinal chemistry letters · 2022Article
- Recent advances in DNA-encoded dynamic libraries.RSC chemical biology · 2022Review
- Strategies for developing DNA-encoded libraries beyond binding assays.Nature chemistry · 2022Review
- A mating mechanism to generate diversity for the Darwinian selection of DNA-encoded synthetic molecules.Nature chemistry · 2022Article
- Modular assembly and encoding strategies for dual-display DNA-encoded chemical libraries.Chemical communications (Cambridge, England) · 2021Article
- Recent Advances in Selective and Irreversible Covalent Ligand Development and Validation.Cell chemical biology · 2019Review
- DNA Barcoding a Complete Matrix of Stereoisomeric Small Molecules.Journal of the American Chemical Society · 2019Article
- Encoded Library Technologies as Integrated Lead Finding Platforms for Drug Discovery.Molecules (Basel, Switzerland) · 2019Review
- Development of a Selection Method for Discovering Irreversible (Covalent) Binders from a DNA-Encoded Library.SLAS discovery : advancing life sciences R & D · 2019Article
- DNA-Encoded Chemical Libraries: A Selection System Based on Endowing Organic Compounds with Amplifiable Information.Annual review of biochemistry · 2018Review
- DNA-Compatible Solid-Phase Combinatorial Synthesis of β-Cyanoacrylamides and Related Electrophiles.ACS combinatorial science · 2018Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
9 authors at 3 institutions in 3 countries.
Funding
Abstract
We describe the construction of a DNA-encoded chemical library comprising 148 135 members, generated through the self-assembly of two sub-libraries, containing 265 and 559 members, respectively. The library was designed to contain building blocks potentially capable of forming covalent interactions with target proteins. Selections performed with JNK1, a kinase containing a conserved cysteine residue close to the ATP binding site, revealed the preferential enrichment of a 2-phenoxynicotinic acid moiety (building block A82) and a 4-(3,4-difluorophenyl)-4-oxobut-2-enoic acid moiety (building block B272). When the two compounds were joined by a short PEG linker, the resulting bidentate binder (A82-L-B272) was able to covalently modify JNK1 in the presence of a large molar excess of glutathione (0.5 mm), used to simulate intracellular reducing conditions. By contrast, derivatives of the individual building blocks were not able to covalently modify JNK1 in the same experimental conditions. The A82-L-B272 ligand was selective over related kinases (BTK and GAK), which also contain targetable cysteine residues in the vicinity of the active site.
Indexed as
Identifiers
What OpenQuestion holds
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.