ArticleJournal of medicinal chemistry2024
Colloidal Aggregation Confounds Cell-Based Covid-19 Antiviral Screens.
Article in Journal of medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed.
- Library Docking for Cannabinoid-2 Receptor Ligands.Journal of medicinal chemistry · 2026Article
- Exploring Passive Permeability Profiles of Cyclic Heptapeptide Chemical Space Uncovers Bioactivity of Mortiamide Scaffold Driven by Colloidal Aggregation.Chembiochem : a European journal of chemical biology · 2026Article
- Experimental and machine learning-based exploration of repurposed drugs reveals chemical features underlying phospholipidosis.Patterns (New York, N.Y.) · 2026Article
- Article
- Library docking for Cannabinoid-2 Receptor ligands.bioRxiv : the preprint server for biology · 2026Article
- Idler Compounds: A Simple Protocol for Openly Sharing Fridge Contents for Cross-Screening.Journal of medicinal chemistry · 2026Article
- Drug-induced phospholipidosis as an artifact in antiviral drug repurposing.bioRxiv : the preprint server for biology · 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
- Mitigating Molecular Aggregation in Drug Discovery With Predictive Insights From Explainable AI.Angewandte Chemie (International ed. in English) · 2025Article
- Dual-Locking the SARS-CoV-2 Spike Trimer: An Amphipathic Molecular "Bolt" Stabilizes Conserved Druggable Interfaces for Coronavirus Inhibition.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Structure Activity of β-Amidomethyl Vinyl Sulfones as Covalent Inhibitors ofJournal of medicinal chemistry · 2024Article
- Structure Activity of β-Amidomethyl Vinyl Sulfones as Covalent Inhibitors ofbioRxiv : the preprint server for biology · 2024Article
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5 authors.
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Abstract
Colloidal aggregation is one of the largest contributors to false positives in early drug discovery. Here, we consider aggregation's role in cell-based infectivity assays in Covid-19 drug repurposing. We investigated the potential aggregation of 41 drug candidates reported as SARs-CoV-2 entry inhibitors. Of these, 17 formed colloidal particles by dynamic light scattering and exhibited detergent-dependent enzyme inhibition. To evaluate the impact of aggregation on antiviral efficacy in cells, we presaturated the colloidal drug suspensions with BSA or spun them down by centrifugation and measured the effects on spike pseudovirus infectivity. Antiviral potencies diminished by at least 10-fold following both BSA and centrifugation treatments, supporting a colloid-based mechanism. Aggregates induced puncta of the labeled spike protein in fluorescence microscopy, consistent with sequestration of the protein on the colloidal particles. These observations suggest that colloidal aggregation is common among cell-based antiviral drug repurposing and offers rapid counter-screens to detect and eliminate these artifacts.
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