ArticleMolecules (Basel, Switzerland)2022
Image-Based Annotation of Chemogenomic Libraries for Phenotypic Screening.
Article in Molecules (Basel, Switzerland), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- Deep Learning for Anticancer Drug Discovery Targeting Non-Apoptotic Regulated Cell Death Mechanisms.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Covalent Targeting Leads to the Development of a LIMK1 Isoform-Selective Inhibitor.Journal of medicinal chemistry · 2025Article
- Functional Characterization of Pathway Inhibitors for the Ubiquitin-Proteasome System (UPS) as Tool Compounds for CRBN and VHL-Mediated Targeted Protein Degradation.ACS chemical biology · 2025Article
- Unlocking the potential: unveiling tyrphostins with Michael-reactive cyanoacrylate motif as promising inhibitors of human 5-lipoxygenase.Pflugers Archiv : European journal of physiology · 2024Article
- Chemogenomics for NR1 nuclear hormone receptors.Nature communications · 2024Article
- Discovery of a Small Molecule Activator of Slack (Kcnt1) Potassium Channels That Significantly Reduces Scratching in Mouse Models of Histamine-Independent and Chronic Itch.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Article
- Deep Annotation of Donated Chemical Probes (DCP) in Organotypic Human Liver Cultures and Patient-Derived Organoids from Tumor and Normal Colorectum.ACS chemical biology · 2023Article
- Characterization of Cellular Viability Using Label-Free Brightfield Live-Cell Imaging.Methods in molecular biology (Clifton, N.J.) · 2023Article
- Annotation of the Effect of Chemogenomic Compounds on Cell Health Using High-Content Microscopy in Live-Cell Mode.Methods in molecular biology (Clifton, N.J.) · 2023Article
- An Introduction to Chemogenomics.Methods in molecular biology (Clifton, N.J.) · 2023Article
- High-content live-cell multiplex screen for chemogenomic compound annotation based on nuclear morphology.STAR protocols · 2022Article
- Discovery of 3-Amino-1International journal of molecular sciences · 2022Article
- Structural basis for specific inhibition of the deubiquitinase UCHL1.Nature communications · 2022Article
Corrections and comments
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Authors and funding
7 authors.
Funding
Abstract
Phenotypical screening is a widely used approach in drug discovery for the identification of small molecules with cellular activities. However, functional annotation of identified hits often poses a challenge. The development of small molecules with narrow or exclusive target selectivity such as chemical probes and chemogenomic (CG) libraries, greatly diminishes this challenge, but non-specific effects caused by compound toxicity or interference with basic cellular functions still pose a problem to associate phenotypic readouts with molecular targets. Hence, each compound should ideally be comprehensively characterized regarding its effects on general cell functions. Here, we report an optimized live-cell multiplexed assay that classifies cells based on nuclear morphology, presenting an excellent indicator for cellular responses such as early apoptosis and necrosis. This basic readout in combination with the detection of other general cell damaging activities of small molecules such as changes in cytoskeletal morphology, cell cycle and mitochondrial health provides a comprehensive time-dependent characterization of the effect of small molecules on cellular health in a single experiment. The developed high-content assay offers multi-dimensional comprehensive characterization that can be used to delineate generic effects regarding cell functions and cell viability, allowing an assessment of compound suitability for subsequent detailed phenotypic and mechanistic studies.
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