ArticleACS omega2023
Diversity and Chemical Space Characterization of Inhibitors of the Epigenetic Target G9a: A Chemoinformatics Approach.
Article in ACS omega, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
What it found
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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
7 citing papers in PubMed.
- Article
- Computational Investigation of Phytochemicals Targeting Isocitrate Lyase to InhibitCurrent drug discovery technologies · 2026Article
- Targeting Histone H3K9 Methyltransferase G9a as a Potential Therapeutic Strategy for Neuropsychiatric Disorders.Medicinal research reviews · 2025Review
- G9a an Epigenetic Therapeutic Strategy for Neurodegenerative Conditions: From Target Discovery to Clinical Trials.Medicinal research reviews · 2025Review
- Chemoinformatic Characterization of NAPROC-13: A Database for Natural ProductJournal of natural products · 2024Article
- The Discovery of Selective Protein Arginine Methyltransferase 5 Inhibitors in the Management of β-Thalassemia through Computational Methods.Molecules (Basel, Switzerland) · 2024Article
- Lead-oriented synthesis of epigenetic relevant scaffolds.Chemical communications (Cambridge, England) · 2023Article
Corrections and comments
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Authors and funding
2 authors.
Funding
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Abstract
G9a is a histone-lysine methyltransferase that performs the mono- and dimethylation of lysine 9 at histone 3 of the nucleosome. It belongs to the SET PKMT family, and its methylations are related to promoter repression and activation. G9a is a promising epigenetic target. Despite the fact that there are several G9a inhibitors under development, there are no compounds in clinical use due to adverse in vivo ADMET (absorption, distribution, metabolism, excretion, and toxicity) issues. The goal of this study is to discuss the exploration, characterization, and analysis of the chemical space of 409 G9a inhibitors reported in a large public database. Exploring the chemical space of the inhibitors led to the quantification of their structural diversity based on molecular scaffolds and structural fingerprints of different designs. As part of the analysis, the G9a inhibitors were compared with commercial libraries focused on epigenetic targets. The findings of this work will help in the development of, in a follow-up study, predictive models to identify G9a inhibitors. This study also points out the relevance of screening commercial libraries to expand the epigenetic relevant chemical space, in particular, G9a inhibitors.
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Registered trials
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