ArticlePloS one2014
A comparison of protein kinases inhibitor screening methods using both enzymatic activity and binding affinity determination.
Article in PloS one, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers.
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Who cites it
35 citing papers in PubMed.
- 3H-pyrazolo[4,3-f]quinoline hinge binder, a tunable scaffold for development of novel kinase inhibitors against FLT3-driven leukemia.European journal of medicinal chemistry · 2026Article
- Functional proteoform group deconvolution reveals a broader spectrum of ibrutinib off-targets.Nature communications · 2025Article
- DeepKinome: quantitative prediction of kinase binding affinity by a compound using deep learning based regression model.Frontiers in molecular biosciences · 2025Article
- JAK inhibitor selectivity: new opportunities, better drugs?Nature reviews. Rheumatology · 2024Review
- HTRF-based assay for detection of mono-ADP-ribosyl hydrolyzing macrodomains and inhibitor screening.iScience · 2024Article
- Chemical proteomics reveals the target landscape of 1,000 kinase inhibitors.Nature chemical biology · 2024Article
- Selective ROCK Inhibitor Enhances Blood Flow Recovery after Hindlimb Ischemia.International journal of molecular sciences · 2023Article
- How many kinases are druggable? A review of our current understanding.The Biochemical journal · 2023Article
- Article
- Structure-based design of selective, orally available salt-inducible kinase inhibitors that stimulate bone formation in mice.Proceedings of the National Academy of Sciences of the United States of America · 2022Article
- Predictive validity in drug discovery: what it is, why it matters and how to improve it.Nature reviews. Drug discovery · 2022Review
- KUALA: a machine learning-driven framework for kinase inhibitors repositioning.Scientific reports · 2022Article
- Identification of 4-Anilinoquin(az)oline as a Cell-Active Protein Kinase Novel 3 (PKN3) Inhibitor Chemotype.ChemMedChem · 2022Article
- Assisting Multitargeted Ligand Affinity Prediction of Receptor Tyrosine Kinases Associated Nonsmall Cell Lung Cancer Treatment with Multitasking Principal Neighborhood Aggregation.Molecules (Basel, Switzerland) · 2022Article
- Chemoproteomic-enabled characterization of small GTPase Rab1a as a target of anRSC chemical biology · 2022Article
- An overview of kinase downregulators and recent advances in discovery approaches.Signal transduction and targeted therapy · 2021Review
- Trends in kinase drug discovery: targets, indications and inhibitor design.Nature reviews. Drug discovery · 2021Review
- Synthesis and Evaluation of Novel 1,2,6-Thiadiazinone Kinase Inhibitors as Potent Inhibitors of Solid Tumors.Molecules (Basel, Switzerland) · 2021Article
- Mobility shift-based electrophoresis coupled with fluorescent detection enables real-time enzyme analysis of carbohydrate sulfatase activity.The Biochemical journal · 2021Article
- An immunochemistry-based screen for chemical inhibitors of DNA-protein interactions and its application to human CGGBP1.BMC cancer · 2020Article
Corrections and comments
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Authors and funding
5 authors.
Funding
Abstract
Binding assays are increasingly used as a screening method for protein kinase inhibitors; however, as yet only a weak correlation with enzymatic activity-based assays has been demonstrated. We show that the correlation between the two types of assays can be improved using more precise screening conditions. Furthermore a marked improvement in the correlation was found by using kinase constructs containing the catalytic domain in presence of additional domains or subunits.
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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.