ArticlePloS one2017
Progress towards a public chemogenomic set for protein kinases and a call for contributions.
Article in PloS one, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 84 papers.
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Who cites it
84 citing papers in PubMed.
- Paradoxical non-catalytic kinase functions are driven by inhibitor-induced displacement of autoinhibitory domains.Molecular systems biology · 2026Article
- Polypharmacology is an enduring and nearly universal property of kinase inhibitors.bioRxiv : the preprint server for biology · 2026Article
- Pharmacophore-driven kinase profiling applied to the PKIS2 chemogenomic dataset.Scientific reports · 2026Article
- Cellular Context Influences Kinase Inhibitor Selectivity.Journal of medicinal chemistry · 2026Article
- Cellular Selectivity Analyses Reveal Distinguishing Profiles for Type II Kinase Inhibitors.bioRxiv : the preprint server for biology · 2025Article
- Enhancing accuracy of virtual kinase profiling via application of graph neural network to 3D pharmacophore ensembles.Journal of computer-aided molecular design · 2025Article
- The fast-evolving FIKK kinase family of Plasmodium falciparum can be inhibited by a single compound.Nature microbiology · 2025Article
- Chemoproteomic Profiling ofJournal of medicinal chemistry · 2025Article
- Chemoproteomic Profiling ofbioRxiv : the preprint server for biology · 2025Article
- Benchmarking Cross-Docking Strategies in Kinase Drug Discovery.Journal of chemical information and modeling · 2024Article
- Milestones in chemoinformatics: global view of the field.Journal of cheminformatics · 2024Article
- Lessons learned during the journey of data: from experiment to model for predicting kinase affinity, selectivity, polypharmacology, and resistance.bioRxiv : the preprint server for biology · 2024Article
- Identification of kinase inhibitors as potential host-directed therapies for intracellular bacteria.Scientific reports · 2024Article
- Discovery and optimization of narrow spectrum inhibitors of Tousled like kinase 2 (TLK2) using quantitative structure activity relationships.European journal of medicinal chemistry · 2024Article
- Chemical proteomics reveals the target landscape of 1,000 kinase inhibitors.Nature chemical biology · 2024Article
- Catalysts of Healing: A Symphony of Synthesis and Clinical Artistry in Small-Molecule Agents for Breast Cancer Alleviation.Molecules (Basel, Switzerland) · 2024Review
- Identification of kinase modulators as host-directed therapeutics against intracellular methicillin-resistantFrontiers in cellular and infection microbiology · 2024Article
- Discovery and Optimization of Narrow Spectrum Inhibitors of Tousled Like Kinase 2 (TLK2) Using Quantitative Structure Activity Relationships.bioRxiv : the preprint server for biology · 2023Article
- Article
- Benchmarking Cross-Docking Strategies for Structure-Informed Machine Learning in Kinase Drug Discovery.bioRxiv : the preprint server for biology · 2023Article
24 more citing papers are in PubMed but not listed here.
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24 authors.
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Abstract
Protein kinases are highly tractable targets for drug discovery. However, the biological function and therapeutic potential of the majority of the 500+ human protein kinases remains unknown. We have developed physical and virtual collections of small molecule inhibitors, which we call chemogenomic sets, that are designed to inhibit the catalytic function of almost half the human protein kinases. In this manuscript we share our progress towards generation of a comprehensive kinase chemogenomic set (KCGS), release kinome profiling data of a large inhibitor set (Published Kinase Inhibitor Set 2 (PKIS2)), and outline a process through which the community can openly collaborate to create a KCGS that probes the full complement of human protein kinases.
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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 Socratic graph.