ArticleChemistry & biology2011
High-throughput kinase profiling: a more efficient approach toward the discovery of new kinase inhibitors.
Article in Chemistry & biology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 54 papers.
What it found
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Who cites it
54 citing papers in PubMed, 122 citations in OpenAlex.
- An AKR1C3-activated kinase inhibitor prodrug.RSC chemical biology · 2026Article
- XMD8-92 and JWG-045 exhibit anti-ferroptotic activities, independently of inhibiting ERK5.Scientific reports · 2026Article
- Discovery of SARS-CoV-2 PLpro inhibitors and RIPK1 inhibitors with synergistic antiviral efficacy in a mouse COVID-19 model.Acta pharmaceutica Sinica. B · 2026Article
- Inactivation of HIPK2 attenuates KRASJournal of experimental & clinical cancer research : CR · 2024Article
- Small Molecule Allosteric Inhibitor of HIPK2 as a Novel Therapy against Kidney Fibrosis.Journal of the American Society of Nephrology : JASN · 2024Article
- Structure-based development of potent and selective type-II kinase inhibitors of RIPK1.Acta pharmaceutica Sinica. B · 2024Article
- Article
- 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
- Human Polo-like Kinase Inhibitors as Antiplasmodials.ACS infectious diseases · 2023Article
- Artificial intelligence to guide precision anticancer therapy with multitargeted kinase inhibitors.BMC cancer · 2022Article
- KOPI: Kinase inhibitOr Proteome Impact analysis.Scientific reports · 2022Article
- 1,3-diarylpyrazolones as potential anticancer agents for non-small cell lung cancer: Synthesis and antiproliferative activity evaluation.Chemical biology & drug design · 2022Article
- Efficient Hit-to-Lead Searching of Kinase Inhibitor Chemical Space via Computational Fragment Merging.Journal of chemical information and modeling · 2021Article
- Abemaciclib is a potent inhibitor of DYRK1A and HIP kinases involved in transcriptional regulation.Nature communications · 2021Article
- Structural basis for small molecule targeting of Doublecortin Like Kinase 1 with DCLK1-IN-1.Communications biology · 2021Article
- A Chemical Probe for Dark Kinase STK17B Derives Its Potency and High Selectivity through a Unique P-Loop Conformation.Journal of medicinal chemistry · 2020Article
- Small molecule strategies to harness the unfolded protein response: where do we go from here?The Journal of biological chemistry · 2020Review
- Synthesis and Structure-Activity Relationships of DCLK1 Kinase Inhibitors Based on a 5,11-Dihydro-6Journal of medicinal chemistry · 2020Article
- Discovery of a selective inhibitor of doublecortin like kinase 1.Nature chemical biology · 2020Article
- Macrophage Syk-PI3Kγ Inhibits Antitumor Immunity: SRX3207, a Novel Dual Syk-PI3K Inhibitory Chemotype Relieves Tumor Immunosuppression.Molecular cancer therapeutics · 2020Article
Corrections and comments
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Authors and funding
15 authors at 5 institutions in 3 countries.
Funding
Abstract
Selective protein kinase inhibitors have only been developed against a small number of kinase targets. Here we demonstrate that "high-throughput kinase profiling" is an efficient method for the discovery of lead compounds for established as well as unexplored kinase targets. We screened a library of 118 compounds constituting two distinct scaffolds (furan-thiazolidinediones and pyrimido-diazepines) against a panel of 353 kinases. A distinct kinase selectivity profile was observed for each scaffold. Selective inhibitors were identified with submicromolar cellular activity against PIM1, ERK5, ACK1, MPS1, PLK1-3, and Aurora A,B kinases. In addition, we identified potent inhibitors for so far unexplored kinases such as DRAK1, HIPK2, and DCAMKL1 that await further evaluation. This inhibitor-centric approach permits comprehensive assessment of a scaffold of interest and represents an efficient and general strategy for identifying new selective kinase inhibitors.
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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.