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The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification

Carrow I. Wells, Hassan Al‐Ali, David Andrews, Christopher R. M. Asquith, Alison D. Axtman, Ivan Đikić, Daniel Ebner, Peter Ettmayer, Christian Fischer, Mathias Frederiksen, Robert E. Futrell, Nathanael S. Gray, Stephanie B. Hatch, Stefan Knapp, Ulrich Lücking, Michel Michaelides, Caitlin E. Mills, Susanne Müller, Dafydd R. Owen, Alfredo Picado, Kumar Singh Saikatendu, Martin Schröder, Alexandra Stolz, Mariana Tellechea, Brandon J. Turunen, Santiago Vilar, Jinhua Wang, William J. Zuercher, Timothy M. Willson, David H. Drewry

2021International Journal of Molecular Sciences110 citationsDOIOpen Access PDF

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.

Topics & Concepts

KinaseComputational biologyIdentification (biology)Set (abstract data type)Cyclin-dependent kinase 4ASK1Computer scienceProtein kinase ACyclin-dependent kinase 2BiologyCell biologyBotanyProgramming languageComputational Drug Discovery MethodsMicrobial Natural Products and BiosynthesisBioinformatics and Genomic Networks
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