ArticleChemistry (Weinheim an der Bergstrasse, Germany)2020
Activity-Directed Synthesis of Inhibitors of the p53/hDM2 Protein-Protein Interaction.
Article in Chemistry (Weinheim an der Bergstrasse, Germany), 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 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
10 citing papers in PubMed.
- A Direct-to-Biology Amine-Acid Amination for Rapid Phenotypic Profiling of Lysosomotropic Natural Products.Journal of the American Chemical Society · 2026Article
- Covalent Peptide-Based N-Myc/Aurora-A Inhibitors Bearing Sulfonyl Fluoride Warheads.Journal of peptide science : an official publication of the European Peptide Society · 2026Article
- Direct-to-Biology: Streamlining the Path From Chemistry to Biology in Drug Discovery.ChemMedChem · 2026Review
- Toward target 2035: EUbOPEN - a public-private partnership to enable & unlock biology in the open.RSC medicinal chemistry · 2025Article
- Modular synthesis of functional libraries by accelerated SuFEx click chemistry.Chemical science · 2024Article
- Efficient Ligand Discovery Using Sulfur(VI) Fluoride Reactive Fragments.ACS chemical biology · 2023Article
- Natural product-informed exploration of chemical space to enable bioactive molecular discovery.RSC medicinal chemistry · 2021Review
- Computational Mapping of Dirhodium(II) Catalysts.Chemistry (Weinheim an der Bergstrasse, Germany) · 2021Article
- Activity-Directed Synthesis: A Flexible Approach for Lead Generation.ChemMedChem · 2020Article
- Activity-Directed Synthesis of Inhibitors of the p53/hDM2 Protein-Protein Interaction.Chemistry (Weinheim an der Bergstrasse, Germany) · 2020Article
Corrections and comments
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Authors and funding
6 authors.
Funding
Abstract
Protein-protein interactions (PPIs) provide a rich source of potential targets for drug discovery and biomedical science research. However, the identification of structural-diverse starting points for discovery of PPI inhibitors remains a significant challenge. Activity-directed synthesis (ADS), a function-driven discovery approach, was harnessed in the discovery of the p53/hDM2 PPI. Over two rounds of ADS, 346 microscale reactions were performed, with prioritisation on the basis of the activity of the resulting product mixtures. Four distinct and novel series of PPI inhibitors were discovered that, through biophysical characterisation, were shown to have promising ligand efficiencies. It was thus shown that ADS can facilitate ligand discovery for a target that does not have a defined small-molecule binding site, and can provide distinctive starting points for the discovery of PPI inhibitors.
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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.