ArticleSLAS discovery : advancing life sciences R & D2020
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
Article in SLAS discovery : advancing life sciences R & D, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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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.
- Unlabeled but Not Unseen: Cytotoxicity Classification of Re(I) Tricarbonyl Complexes via K‑Means Clustering.ACS omega · 2026Article
- Plant extracts and phytochemicals in canine and feline mammary cancer models: current evidence and comparative perspectives.Veterinary research communications · 2026Review
- Deep Learning-Guided Discovery of Dual Inhibitors of SARS-CoV-2 Entry and 3CL Protease.Molecules (Basel, Switzerland) · 2026Article
- Optogenetic Cancer Therapy Using the Light-Driven Outward Proton Pump Rhodopsin Archaerhodopsin-3 (AR3).Journal of the American Chemical Society · 2025Article
- Synthetic Linear Lipopeptides and Lipopeptoids Induce Apoptosis and Oxidative Stress: In Vitro Cytotoxicity and SAR Evaluation Against Cancer Cell Lines.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Advances in Cytotoxicity Testing: From In Vitro Assays to In Silico Models.International journal of molecular sciences · 2025Review
- Evaluation of the Anticancer Activity of Medicinal Plants Predominantly Accumulating Ellagic Acid Compounds.Antioxidants (Basel, Switzerland) · 2025Article
- Membrane Perturbations and Assay Interferences by Ivermectin Explain Its In Vitro SARS-CoV-2 Antiviral Activities and Lack of Translatability.Journal of medicinal chemistry · 2025Review
- Therapeutic Potential of Glucose Oxidase-Loaded Biogenic Mesoporous Silica Nanoparticles in Ovarian Cancer.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Cyto-Safe: A Machine Learning Tool for Early Identification of Cytotoxic Compounds in Drug Discovery.Journal of chemical information and modeling · 2024Article
- A Comprehensive Collection of Pain and Opioid Use Disorder Compounds for High-Throughput Screening and Artificial Intelligence-Driven Drug Discovery.ACS pharmacology & translational science · 2024Article
- Quantitative Bioactivity Signatures of Dietary Supplements and Natural Products.ACS pharmacology & translational science · 2023Article
- High-Throughput Screening of Natural Product and Synthetic Molecule Libraries for Antibacterial Drug Discovery.Metabolites · 2023Review
- Screening for bilayer-active and likely cytotoxic molecules reveals bilayer-mediated regulation of cell function.The Journal of general physiology · 2023Article
- SULT1A1-dependent sulfonation of alkylators is a lineage-dependent vulnerability of liver cancers.Nature cancer · 2023Article
- Nuisance compounds in cellular assays.Cell chemical biology · 2021Review
- Discovery of an Anion-Dependent Farnesyltransferase Inhibitor from a Phenotypic Screen.ACS medicinal chemistry letters · 2021Article
- Predictive models for estimating cytotoxicity on the basis of chemical structures.Bioorganic & medicinal chemistry · 2020Article
- Quantitative Chemotherapeutic Profiling of Gynecologic Cancer Cell Lines Using Approved Drugs and Bioactive Compounds.Translational oncology · 2019Article
Corrections and comments
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Authors and funding
13 authors.
Funding
Abstract
Cell-based phenotypic screening is a commonly used approach to discover biological pathways, novel drug targets, chemical probes, and high-quality hit-to-lead molecules. Many hits identified from high-throughput screening campaigns are ruled out through a series of follow-up potency, selectivity/specificity, and cytotoxicity assays. Prioritization of molecules with little or no cytotoxicity for downstream evaluation can influence the future direction of projects, so cytotoxicity profiling of screening libraries at an early stage is essential for increasing the likelihood of candidate success. In this study, we assessed the cell-based cytotoxicity of nearly 10,000 compounds in the National Institutes of Health, National Center for Advancing Translational Sciences annotated libraries and more than 100,000 compounds in a diversity library against four normal cell lines (HEK 293, NIH 3T3, CRL-7250, and HaCat) and one cancer cell line (KB 3-1, a HeLa subline). This large-scale library profiling was analyzed for overall screening outcomes, hit rates, pan-activity, and selectivity. For the annotated library, we also examined the primary targets and mechanistic pathways regularly associated with cell death. To our knowledge, this is the first study to use high-throughput screening to profile a large screening collection (>100,000 compounds) for cytotoxicity in both normal and cancer cell lines. The results generated here constitute a valuable resource for the scientific community and provide insight into the extent of cytotoxic compounds in screening libraries, allowing for the identification and avoidance of compounds with cytotoxicity during high-throughput screening campaigns.
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Registered trials
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