ArticleSLAS discovery : advancing life sciences R & D2018
Using Microscale Thermophoresis to Characterize Hits from High-Throughput Screening: A European Lead Factory Perspective.
Article in SLAS discovery : advancing life sciences R & D, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 37 papers.
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Who cites it
37 citing papers in PubMed.
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- Monoclonal antibody neutralizesInfection and immunity · 2025Article
- Fortilin binds CTNNA3 and protects it against phosphorylation, ubiquitination, and proteasomal degradation to guard cells against apoptosis.Communications biology · 2025Article
- Advancing Target Validation and Ligandability Assessment: Fragment Screening viaMethods in molecular biology (Clifton, N.J.) · 2025Article
- Discovery of new Hsp90-Cdc37 protein-protein interaction inhibitors:RSC advances · 2024Article
- Small-Molecule Disruptors of the Interaction between Calcium- and Integrin-Binding Protein 1 and Integrin αACS pharmacology & translational science · 2024Article
- Article
- Discovery and Synthesis of a Naturally Derived Protein Kinase Inhibitor that Selectively Inhibits Distinct Classes of Serine/Threonine Kinases.Journal of natural products · 2023Article
- Targeting RNA Structure to Inhibit Editing in Trypanosomes.International journal of molecular sciences · 2023Article
- Biochemical Discovery, Intracellular Evaluation, and Crystallographic Characterization of Synthetic and Natural Product Adenosine 3',5'-Cyclic Monophosphate-Dependent Protein Kinase A (PKA) Inhibitors.ACS pharmacology & translational science · 2023Article
- Computational Design, Synthesis, and Biophysical Evaluation of β-Amido Boronic Acids as SARS-CoV-2 MMolecules (Basel, Switzerland) · 2023Article
- Targeted systematic evolution of an RNA platform neutralizing DNMT1 function and controlling DNA methylation.Nature communications · 2023Article
- The Inhibitory Properties of a Novel, Selective LMTK3 Kinase Inhibitor.International journal of molecular sciences · 2023Article
- Fluorescence Anisotropy and Polarization in the Characterization of Biomolecular Association Processes and Their Application to Study SH2 Domain Binding Affinity.Methods in molecular biology (Clifton, N.J.) · 2023Article
- An Optimized Microscale Thermophoresis Method for High-Throughput Screening of DNA Methyltransferase 2 Ligands.ACS pharmacology & translational science · 2022Article
- Ebola Entry Inhibitors Discovered fromInternational journal of molecular sciences · 2022Article
- Peptide Linked Diacetylene Amphiphiles for Detection of Epitope Specific Antibodies.Chemosensors (Basel, Switzerland) · 2022Article
- Molecular interaction between small nuclear ribonucleoprotein polypeptide G and heat shock protein 70.14: a microscale thermophoresis exposition towards developing anti-cancer drugs.American journal of translational research · 2022Article
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Authors and funding
3 authors.
Funding
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Abstract
High-throughput screening (HTS) is a proven method for discovering new lead matter for drug discovery and chemical biology. To maximize the likelihood of identifying genuine binders to a molecular target, and avoid wasting resources following up compounds with unproductive/nonspecific mechanisms of action, it is important to employ a range of assays during an HTS campaign that build confidence of target engagement for hit compounds. Biophysical methods that measure direct target/compound engagement have established themselves as key techniques in generating this confidence, and they are now integral to the latter stages of HTS triage at the European Lead Factory (ELF). One relatively new technique that the ELF is using is microscale thermophoresis (MST), which measures the differences in rate of movement through a temperature gradient that are caused when single molecular species form complexes. Here we provide an overview of the MST assay development workflow that the ELF employs and a perspective of our experience to date of using MST to triage the output of HTS campaigns and how it compares and contrasts with the use of other biophysical techniques.
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