ArticleJournal of biomolecular screening2013
High-throughput identification of promiscuous inhibitors from screening libraries with the use of a thiol-containing fluorescent probe.
Article in Journal of biomolecular screening, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
What it found
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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
12 citing papers in PubMed.
- Strategy for cysteine-targeting covalent inhibitors screening using in-house database based LC-MS/MS and drug repurposing.Journal of pharmaceutical analysis · 2025Article
- A Collection of Useful Nuisance Compounds (CONS) for Interrogation of Bioassay Integrity.JACS Au · 2024Article
- Lies and Liabilities: Computational Assessment of High-Throughput Screening Hits to Identify Artifact Compounds.Journal of medicinal chemistry · 2023Article
- Evaluating the utility of a high throughput thiol-containing fluorescent probe to screen for reactivity: A case study with the Tox21 library.Computational toxicology (Amsterdam, Netherlands) · 2023Article
- Mitogen-Activated Protein Kinase Phosphatases: No Longer Undruggable?Annual review of pharmacology and toxicology · 2023Review
- The Key Characteristics of Carcinogens: Relationship to the Hallmarks of Cancer, Relevant Biomarkers, and Assays to Measure Them.Cancer epidemiology, biomarkers & prevention : a publication of the American Association for Cancer Research, cosponsored by the American Society of Preventive Oncology · 2020Article
- DNA unchained: two assays to discover and study inhibitors of the DNA clustering function of barrier-to-autointegration factor.Scientific reports · 2020Article
- ALARM NMR for HTS triage and chemical probe validation.Current protocols in chemical biology · 2018Article
- Mimicking Intermolecular Interactions of Tight Protein-Protein Complexes for Small-Molecule Antagonists.ChemMedChem · 2017Article
- A Computational Investigation of Small-Molecule Engagement of Hot Spots at Protein-Protein Interaction Interfaces.Journal of chemical information and modeling · 2017Article
- PAINS in the assay: chemical mechanisms of assay interference and promiscuous enzymatic inhibition observed during a sulfhydryl-scavenging HTS.Journal of medicinal chemistry · 2015Article
- The essential roles of chemistry in high-throughput screening triage.Future medicinal chemistry · 2014Review
Corrections and comments
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Authors and funding
9 authors.
Funding
Abstract
Testing small molecules for their ability to modify cysteine residues of proteins in the early stages of drug discovery is expected to accelerate our ability to develop more selective drugs with lesser side effects. In addition, this approach also enables the rapid evaluation of the mode of binding of new drug candidates with respect to thiol reactivity and metabolism by glutathione. Herein, we describe the development of a fluorescence-based high-throughput assay that allows the identification of thiol-reactive compounds. A thiol-containing fluorescent probe, MSTI, was synthesized and used to evaluate small molecules from the Library of Pharmacologically Active Compounds (LOPAC) collection of bioactive molecules. LOPAC compounds that are known to react with sulfur nucleophiles were identified with this assay, for example, irreversible protease inhibitors, nitric oxide-releasing compounds, and proton-pump inhibitors. The results confirm that both electrophilic and redox reactive compounds can be quickly identified in a high-throughput manner, enabling the assessment of screening libraries with respect to thiol-reactive compounds.
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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.