ArticleACS medicinal chemistry letters2019
Evaluating the Advantages of Using 3D-Enriched Fragments for Targeting BET Bromodomains.
Article in ACS medicinal chemistry letters, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
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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.
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Who cites it
19 citing papers in PubMed, 34 citations in OpenAlex.
- Natural Product-like Fragments Unlock Novel Chemotypes for a Kinase Target─Exploring Options beyond the Flatland.Journal of chemical information and modeling · 2026Article
- Developments and challenges in hit progression within fragment-based drug discovery.Nature communications · 2026Review
- Return to Flatland.Nature reviews. Chemistry · 2025Article
- Stereocontrolled and time-honored access to piperidine- and pyrrolidine-fused 3-methylenetetrahydropyrans using lactam-tethered alkenols.RSC advances · 2024Article
- Photogeneration of α-Bimetalloid Radicals via Selective Activation of Multifunctional C1 Units.Journal of the American Chemical Society · 2024Article
- Implementation of an AI-assisted fragment-generator in an open-source platform.RSC medicinal chemistry · 2022Article
- Kinetic Resolution of 2-Aryl-4-methylenepiperidines toward Enantioenriched Functionalizable Piperidine Fragments.The Journal of organic chemistry · 2022Article
- Puckering the Planar Landscape of Fragments: Design and Synthesis of a 3D Cyclobutane Fragment Library.ChemMedChem · 2022Article
- Review
- The Growing Importance of Chirality in 3D Chemical Space Exploration and Modern Drug Discovery Approaches for Hit-ID: Topical Innovations.ACS medicinal chemistry letters · 2021Article
- Opportunity knocks for uncovering the new function of an understudied nucleosome remodeling complex member, the bromodomain PHD finger transcription factor, BPTF.Current opinion in chemical biology · 2021Review
- Fragment-based drug discovery: opportunities for organic synthesis.RSC medicinal chemistry · 2020Review
- Quantifying the Selectivity of Protein-Protein and Small Molecule Interactions with Fluorinated Tandem Bromodomain Reader Proteins.ACS chemical biology · 2020Article
- The precious fluorine on the ring: fluorine NMR for biological systems.Journal of biomolecular NMR · 2020Article
- Combined Protein- and Ligand-Observed NMR Workflow to Screen Fragment Cocktails against Multiple Proteins: A Case Study Using Bromodomains.Molecules (Basel, Switzerland) · 2020Article
- New inhibitors for the BPTF bromodomain enabled by structural biology and biophysical assay development.Organic & biomolecular chemistry · 2020Article
- Efficient Synthesis of 1,4-Thiazepanones and 1,4-Thiazepanes as 3D Fragments for Screening Libraries.Organic letters · 2020Article
- Demonstration of the utility of DOS-derived fragment libraries for rapid hit derivatisation in a multidirectional fashion.Chemical science · 2020Article
- SAR by (Protein-Observed)Accounts of chemical research · 2019Review
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
Fragment-based ligand discovery has been successful in targeting diverse proteins. Despite drug-like molecules having more 3D character, traditional fragment libraries are largely composed of flat, aromatic fragments. The use of 3D-enriched fragments for enhancing library diversity is underexplored especially against protein-protein interactions. Here, we evaluate using 3D-enriched fragments against bromodomains. Bromodomains are highly ligandable, but selectivity remains challenging, particularly for bromodomain and extraterminal (BET) family bromodomains. We screened a 3D-enriched fragment library against BRD4(D1) via
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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.