ArticleChemPlusChem2025
High-Throughput Drug Derivatization and Bioassay by Desorption Electrospray Ionization Mass Spectrometry.
Article in ChemPlusChem, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
5 citing papers in PubMed.
- Early-stage drug discovery in a new-generation ultrahigh-throughput mass spectrometry platform.Proceedings of the National Academy of Sciences of the United States of America · 2026Article
- Label-Free High-Throughput Screening of CYP3A4 Inhibitors Using Acoustic Ejection Mass Spectrometry.Analytical chemistry · 2026Article
- Accelerated and Green Synthesis ofJournal of the American Chemical Society · 2026Article
- High-Throughput Small-Scale Platform for Synthesis, Characterization, and Modeling of Per- and Polyfluoroalkyl Substances Analogs.Environmental science & technology letters · 2025Article
- Mechanisms of ionization and of chemical reactions in charged microdroplets.Chemical science · 2025Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors.
Funding
Abstract
Adapting high-throughput (HT) synthetic methods to the modification of drugs and to testing of their bioactivity should expedite drug discovery. Herein, the applicability of HT desorption electrospray ionization mass spectrometry (DESI MS) to achieve late-stage functionalization (LSF) and rapidly generate a modified opioid library is demonstrated. Specifically, aza-Michael addition and sulfur (VI) fluoride exchange reactions are used for functionalization. The modified drugs are both synthesized and characterized using an automated HT-DESI MS platform, with the reaction occurring during the droplet flight. Analysis by MS characterizes reaction products at a throughput of >1 reaction per second. With this platform, multiple nor-opioid scaffolds and functionalization reagents are screened and a selection of the hits obtained is subjected to HT label-free bioassays using the same DESI-MS platform. This combination of accelerated LSF reactions to rapidly create a diverse library of functionalized drugs with direct bioassays of the crude reaction mixtures for structure-activity relationship evaluation, both using the same platform, is anticipated to help expedite the early drug discovery process.
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What OpenQuestion holds
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.