ReviewNature chemical biology2026
Advances in BRET probes for intracellular target engagement studies.
Review in Nature chemical biology, 2026. 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
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
- Virtual screening and experimental validation of a METTL3-targeting peptide withJournal of enzyme inhibition and medicinal chemistry · 2026Article
- How to Perform a Tracer Displacement BRET Assay for the TRPML1 Ion Channel.Bio-protocol · 2026Article
- BRET-Based Approaches for Ion Channels: Emerging Applications and Future Directions.Archiv der Pharmazie · 2026Review
- Quantification of Binding of Small Molecules to Native Kinases by Flow Cytometry Reveals Divergence from Biochemical Affinities.Journal of the American Chemical Society · 2026Article
- Development of NanoBRET cellular target engagement assays in primary neurons for activating mutants of p21-activated kinase 1.bioRxiv : the preprint server for biology · 2026Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
11 authors.
Funding
Abstract
Assessing drug-target engagement in living cells is essential for verifying the activity of pharmacological agents. Traditional binding assays often overlook key factors such as permeability, intracellular distribution and complex formation that influence target occupancy in cells. Bioluminescence resonance energy transfer (BRET)-based probes enable direct, quantitative assessment of small-molecule binding to proteins in live, intact cells. BRET provides sensitive detection of target engagement across a wide range of target classes, including less-tractable proteins in membrane compartments. Compared to other existing methods, BRET offers quantification of drug occupancy at steady state and open system regimens. Recent innovations in this platform have expanded its utility beyond occupancy confirmation to include applications in polypharmacology and mechanism-of-action studies. Here, we provide an updated perspective on BRET target engagement assays as versatile tools for chemical biology and early-stage drug discovery.
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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.