ArticleJournal of the American Chemical Society2016
Real-Time Biological Annotation of Synthetic Compounds.
Article in Journal of the American Chemical Society, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 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
21 citing papers in PubMed.
- Structure revision of scytonemin imine and its relationship to scytonemin chromism and cyanobacterial adaptability.Scientific reports · 2025Article
- Chemical Variation of Leaves and Pseudobulbs inPlants (Basel, Switzerland) · 2025Article
- Cell Painting: a decade of discovery and innovation in cellular imaging.Nature methods · 2025Review
- Molecular complexity as a driving force for the advancement of organic synthesis.Nature reviews. Chemistry · 2024Review
- Natural Product Synthesis in the 21st Century: Beyond the Mountain Top.ACS central science · 2024Review
- Predicting compound activity from phenotypic profiles and chemical structures.Nature communications · 2023Article
- Reference compounds for characterizing cellular injury in high-content cellular morphology assays.Nature communications · 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
- The Use of Informer Sets in Screening: Perspectives on an Efficient Strategy to Identify New Probes.SLAS discovery : advancing life sciences R & D · 2021Article
- Pd-Catalyzed Cascade Reactions of Aziridines: One-Step Access to Complex Tetracyclic Amines.Organic letters · 2021Article
- Image-based profiling for drug discovery: due for a machine-learning upgrade?Nature reviews. Drug discovery · 2021Review
- Comparison of Approaches for Determining Bioactivity Hits from High-Dimensional Profiling Data.SLAS discovery : advancing life sciences R & D · 2021Article
- Rapid Access to Azabicyclo[3.3.1]nonanes by a Tandem Diverted Tsuji-Trost Process.Chemistry (Weinheim an der Bergstrasse, Germany) · 2020Article
- Synthetic, Mechanistic, and Biological Interrogation ofJournal of the American Chemical Society · 2020Article
- Multimodal small-molecule screening for human prion protein binders.The Journal of biological chemistry · 2020Article
- Harnessing the power of microscopy images to accelerate drug discovery: what are the possibilities?Expert opinion on drug discovery · 2020Article
- Synergistic Effects of Stereochemistry and Appendages on the Performance Diversity of a Collection of Synthetic Compounds.Journal of the American Chemical Society · 2018Article
- Mechanism of Action of the Cytotoxic Asmarine Alkaloids.ACS chemical biology · 2018Article
- Chemical probes and drug leads from advances in synthetic planning and methodology.Nature reviews. Drug discovery · 2018Review
- High-resolution phenotypic profiling of natural products-induced effects on the single-cell level.Scientific reports · 2017Article
Corrections and comments
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Authors and funding
12 authors.
Funding
Abstract
Organic chemists are able to synthesize molecules in greater number and chemical complexity than ever before. Yet, a majority of these compounds go untested in biological systems, and those that do are often tested long after the chemist can incorporate the results into synthetic planning. We propose the use of high-dimensional "multiplex" assays, which are capable of measuring thousands of cellular features in one experiment, to annotate rapidly and inexpensively the biological activities of newly synthesized compounds. This readily accessible and inexpensive "real-time" profiling method can be used in a prospective manner to facilitate, for example, the efficient construction of performance-diverse small-molecule libraries that are enriched in bioactives. Here, we demonstrate this concept by synthesizing ten triads of constitutionally isomeric compounds via complexity-generating photochemical and thermal rearrangements and measuring compound-induced changes in cellular morphology via an imaging-based "cell painting" assay. Our results indicate that real-time biological annotation can inform optimization efforts and library syntheses by illuminating trends relating to biological activity that would be difficult to predict if only chemical structure were considered. We anticipate that probe and drug discovery will benefit from the use of optimization efforts and libraries that implement this approach.
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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.