ArticleScience advances2021
Multicomponent reaction-derived covalent inhibitor space.
Article in Science advances, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 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
17 citing papers in PubMed.
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- The Evolution of Fluorescein into A Potential Theranostic Tool.Chemistry (Weinheim an der Bergstrasse, Germany) · 2025Article
- Predicting three-component reaction outcomes from ~40,000 miniaturized reactant combinations.Science advances · 2025Article
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- Covalent Proximity Inducers.Chemical reviews · 2025Review
- A new strategy for immobilization of copper on the FeHeliyon · 2024Article
- NiNanoscale advances · 2024Article
- Carbenoid-involved reactions integrated with scaffold-based screening generates a Nav1.7 inhibitor.Communications chemistry · 2024Article
- Direct-to-biology, automated, nano-scale synthesis, and phenotypic screening-enabled E3 ligase modulator discovery.Nature communications · 2023Article
- Multicomponent Reaction-Assisted Drug Discovery: A Time- and Cost-Effective Green Approach Speeding Up Identification and Optimization of Anticancer Drugs.International journal of molecular sciences · 2023Review
- Activation-Free Sulfonyl Fluoride Probes for Fragment Screening.Molecules (Basel, Switzerland) · 2023Article
- 'Chemistry at the speed of sound': automated 1536-well nanoscale synthesis of 16 scaffolds in parallel.Green chemistry : an international journal and green chemistry resource : GC · 2023Article
- Petasis Sequence Reactions for the Scaffold-Diverse Synthesis of Bioactive Polycyclic Small Molecules.ACS omega · 2023Article
- Design, synthesis and biological evaluation of 1,5-disubstituted α-amino tetrazole derivatives as non-covalent inflammasome-caspase-1 complex inhibitors with potential application against immune and inflammatory disorders.European journal of medicinal chemistry · 2022Article
- Pyromellitic diamide-diacid bridged mesoporous organosilica nanospheres with controllable morphologies: a novel PMO for the facile and expeditious synthesis of imidazole derivatives.Nanoscale advances · 2021Article
- Combining High-Throughput Synthesis and High-Throughput Protein Crystallography for Accelerated Hit Identification.Angewandte Chemie (International ed. in English) · 2021Article
Corrections and comments
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Authors and funding
7 authors.
Funding
Abstract
The area of covalent inhibitors is gaining momentum due to recently introduced clinical drugs, but libraries of these compounds are scarce. Multicomponent reaction (MCR) chemistry is well known for its easy access to a very large and diverse chemical space. Here, we show that MCRs are highly suitable to generate libraries of electrophiles based on different scaffolds and three-dimensional shapes and highly compatible with multiple functional groups. According to the building block principle of MCR, acrylamide, acrylic acid ester, sulfurylfluoride, chloroacetic acid amide, nitrile, and α,β-unsaturated sulfonamide warheads can be easily incorporated into many different scaffolds. We show examples of each electrophile on 10 different scaffolds on a preparative scale as well as in a high-throughput synthesis mode on a nanoscale to produce libraries of potential covalent binders in a resource- and time-saving manner. Our operational procedure is simple, mild, and step economical to facilitate future covalent library synthesis.
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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.