ArticleACS medicinal chemistry letters2021
Rapid Evaluation of Small Molecule Cellular Target Engagement with a Luminescent Thermal Shift Assay.
Article in ACS medicinal chemistry letters, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
What it found
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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
16 citing papers in PubMed.
- Fragment-Based Discovery of Fenamic Acids as Pan-Species Inhibitors of the Soluble Epoxide Hydrolase Phosphatase Domain.ACS chemical biology · 2026Article
- Stability-Based Proteomic Methods Add Value to Activity-Based Protein Profiling Studies.ACS chemical biology · 2026Article
- CRISPR Gene Tagging for Illuminating Endogenous Protein Dynamics.International journal of molecular sciences · 2026Review
- Optimization and Characterization of SHIP1 Ligands for Cellular Target Engagement and Activity in Alzheimer's Disease Models.Journal of medicinal chemistry · 2026Article
- Optimization and Characterization of SHIP1 Ligands for Cellular Target Engagement and Activity in Alzheimer's Disease Models.bioRxiv : the preprint server for biology · 2026Article
- Development of Pyrimido Pyridazine Analogs through Increased Whole Cell Target Engagement of the Dihydropteroate Synthase Pterin Binding Site in Gram-Negative Bacteria.ACS infectious diseases · 2025Article
- Target Engagement Assays in Early Drug Discovery.Journal of medicinal chemistry · 2025Review
- A structural and mechanistic model for BSEP dysfunction in PFIC2 cholestatic disease.Communications biology · 2025Article
- Luciferase- and HaloTag-based reporter assays to measure small-molecule-induced degradation pathway in living cells.Nature protocols · 2024Review
- Insulin sensitization by small molecules enhancing GLUT4 translocation.Cell chemical biology · 2023Article
- Thermal unfolding methods in drug discovery.Biophysics reviews · 2023Review
- A Shift in Thinking: Cellular Thermal Shift Assay-Enabled Drug Discovery.ACS medicinal chemistry letters · 2023Review
- Discovery and Characterization of BAY-805, a Potent and Selective Inhibitor of Ubiquitin-Specific Protease USP21.Journal of medicinal chemistry · 2023Article
- Advances in luminescence-based technologies for drug discovery.Expert opinion on drug discovery · 2023Review
- HiBiT Cellular Thermal Shift Assay (HiBiT CETSA).Methods in molecular biology (Clifton, N.J.) · 2023Article
- Current Advances in CETSA.Frontiers in molecular biosciences · 2022Review
Corrections and comments
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Authors and funding
6 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Determination of target engagement for candidate drug molecules in the native cellular environment is a significant challenge for drug discovery programs. The cellular thermal shift assay (CETSA) has emerged as a powerful tool for determining compound target engagement through measurement of changes to a protein's thermal stability upon ligand binding. Here, we present a HiBiT thermal shift assay (BiTSA) that deploys a quantitative peptide tag for determination of compound target engagement in the native cellular environment using a high throughput, plate-based luminescence readout. We demonstrate that BiTSA can rapidly assess cellular target engagement of small molecule ligands against their cognate targets and highlight two applications of BiTSA for differentiating small molecules targeting mutant KRAS and TP53.
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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.