ArticleInternational journal of molecular sciences2021
The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification.
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Article in International journal of molecular sciences, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 51 papers.
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51 citing papers in PubMed.
- 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
- Idler Compounds: A Simple Protocol for Openly Sharing Fridge Contents for Cross-Screening.Journal of medicinal chemistry · 2026Article
- Repositioning a Human Kinase Platelet-Derived Growth Factor Receptor Alpha Type II Inhibitor for Malaria and Inhibition of Hemozoin Formation.ACS medicinal chemistry letters · 2026Article
- Autophagy inhibitors block pathogenic NET release in immune-mediated inflammatory disease without impairing host defence.Rheumatology (Oxford, England) · 2025Article
- Enhancing accuracy of virtual kinase profiling via application of graph neural network to 3D pharmacophore ensembles.Journal of computer-aided molecular design · 2025Article
- Kinome analysis of Madurella mycetomatis identified kinases in the cell wall integrity pathway as novel potential therapeutic drug targets in eumycetoma caused by Madurella mycetomatis.PLoS neglected tropical diseases · 2025Article
- Drug Combinations Targeting FAK and MEK Overcomes Tumor Heterogeneity in Glioblastoma.Pharmaceutics · 2025Article
- Chemoproteomic Profiling ofJournal of medicinal chemistry · 2025Article
- Chemogenomics for steroid hormone receptors (NR3).Communications chemistry · 2025Article
- Chemoproteomic Profiling ofbioRxiv : the preprint server for biology · 2025Article
- Screening of a kinase inhibitor library identified novel targetable kinase pathways in triple-negative breast cancer.Anti-cancer drugs · 2025Article
- Probe my Pathway (PmP): a portal to explore the chemical coverage of the human Reactome.Database : the journal of biological databases and curation · 2024Article
- Milestones in chemoinformatics: global view of the field.Journal of cheminformatics · 2024Article
- Chemogenomics for NR1 nuclear hormone receptors.Nature communications · 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
- Illuminating function of the understudied druggable kinome.Drug discovery today · 2024Review
- 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
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Authors and funding
30 authors.
Carrow I WellsStructural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.ORCID 0000-0003-4799-6792
Hassan Al-AliThe Miami Project to Cure Paralysis, Peggy and Harold Katz Family Drug Discovery Center, Sylvester Comprehensive Cancer Center, and Departments of Neurological Surgery and Medicine, University of Miami Miller School of Medicine, Miami, FL 33136, USA.
David M AndrewsAstraZeneca, Darwin Building, Cambridge Science Park, Cambridge CB4 0WG, UK.ORCID 0000-0002-6716-6270
Christopher R M AsquithStructural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.ORCID 0000-0001-5871-3458
Alison D AxtmanStructural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.ORCID 0000-0003-4779-9932
Ivan DikicInstitute of Biochemistry 2, Faculty of Medicine, Goethe University Frankfurt, Theodor-Stern-Kai 7, 60438 Frankfurt am Main, Germany.
Daniel EbnerNuffield Department of Medicine, Target Discovery Institute, University of Oxford, Oxford OX3 7FZ, UK.ORCID 0000-0002-6495-7026
Peter EttmayerBoehringer Ingelheim RCV GmbH & Co KG, 1121 Vienna, Austria.
Christian FischerMSD, 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Mathias FrederiksenNovartis Institutes for BioMedical Research, Novartis Campus, 4056 Basel, Switzerland.
Robert E FutrellStructural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
Nathanael S GrayDepartment of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, USA.
Stephanie B HatchMRC Oxford Institute for Radiation Oncology, Department of Oncology, University of Oxford, Roosevelt Drive, Oxford OX3 7XB, UK.
Stefan KnappBuchmann Institute for Molecular Life Sciences, Goethe University Frankfurt, Max-von-Laue-Str. 15, 60438 Frankfurt am Main, Germany.ORCID 0000-0001-5995-6494
Ulrich LückingBayer Pharma AG, Drug Discovery, Müllerstrasse 178, 13353 Berlin, Germany.
Michael MichaelidesOncology Discovery, AbbVie, 1 North Waukegan Road, North Chicago, IL 60064, USA.
Caitlin E MillsLaboratory of Systems Pharmacology, Department of Systems Biology, Harvard Medical School, Boston, MA 02115, USA.
Susanne MüllerBuchmann Institute for Molecular Life Sciences, Goethe University Frankfurt, Max-von-Laue-Str. 15, 60438 Frankfurt am Main, Germany.ORCID 0000-0003-2402-4157
Dafydd OwenDiscovery Network Group, Pfizer Medicine Design, Cambridge, MA 02139, USA.
Alfredo PicadoStructural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
Kumar S SaikatenduGlobal Research Externalization, Takeda California, Inc., 9625 Towne Center Drive, San Diego, CA 92121, USA.
Martin SchröderBuchmann Institute for Molecular Life Sciences, Goethe University Frankfurt, Max-von-Laue-Str. 15, 60438 Frankfurt am Main, Germany.
Alexandra StolzInstitute of Biochemistry 2, Faculty of Medicine, Goethe University Frankfurt, Theodor-Stern-Kai 7, 60438 Frankfurt am Main, Germany.ORCID 0000-0002-3340-439X
Mariana TellecheaInstitute of Biochemistry 2, Faculty of Medicine, Goethe University Frankfurt, Theodor-Stern-Kai 7, 60438 Frankfurt am Main, Germany.
Brandon J TurunenGlaxoSmithKline, Chemical Biology, 1250 S Collegeville Rd, Collegeville, PA 19426, USA.
Santiago VilarTruvitech LLC, Miami, FL 33136, USA.
Jinhua WangDepartment of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, USA.
William J ZuercherStructural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.ORCID 0000-0002-9836-0068
Timothy M WillsonStructural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
David H DrewryStructural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.ORCID 0000-0001-5973-5798
Funding
Creation of in vivo active chemical probes for CAMKK2 to treat cancerR01CA218442 · NCI · UNIV OF NORTH CAROLINA CHAPEL HILL · PI DREWRY, DAVID HAROLD · 2017 to 2019
$2.0MCharacterization of an understudied kinase, NEK5, in acquisition of a mesenchymaland migratory cell phenotypeR03TR003386 · NCATS · TULANE UNIVERSITY OF LOUISIANA · PI BUROW, MATTHEW E., DREWRY, DAVID HAROLD · 2020 to 2020
$167kInnovative Medicines Initiative 875510NCATS NIH HHS R03 TR003386NCI NIH HHS R01 CA218442NIH HHS 1R01CA218442-01NIH HHS 1R44TR001916-02NIH HHS 1U24DK116204-01
Abstract
We describe the assembly and annotation of a chemogenomic set of protein kinase inhibitors as an open science resource for studying kinase biology. The set only includes inhibitors that show potent kinase inhibition and a narrow spectrum of activity when screened across a large panel of kinase biochemical assays. Currently, the set contains 187 inhibitors that cover 215 human kinases. The kinase chemogenomic set (KCGS), current Version 1.0, is the most highly annotated set of selective kinase inhibitors available to researchers for use in cell-based screens.
Indexed as
Drug DiscoveryHumansProtein Kinase InhibitorsProtein Serine-Threonine KinasesSmall Molecule LibrariesStructure-Activity RelationshipProtein Kinase InhibitorsProtein Serine-Threonine KinasesSmall Molecule Librarieschemogenomic setdrug discoverydruggable genomeKCGSkinase inhibitorphenotypic screeningprotein kinasesmall moleculesunderstudied kinase
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