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

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 bioch...

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Bibliographic Details
Published in:International journal of molecular sciences 2021-01, Vol.22 (2), p.566
Main Authors: Wells, Carrow I, Al-Ali, Hassan, Andrews, David M, Asquith, Christopher R M, Axtman, Alison D, Dikic, Ivan, Ebner, Daniel, Ettmayer, Peter, Fischer, Christian, Frederiksen, Mathias, Futrell, Robert E, Gray, Nathanael S, Hatch, Stephanie B, Knapp, Stefan, Lücking, Ulrich, Michaelides, Michael, Mills, Caitlin E, Müller, Susanne, Owen, Dafydd, Picado, Alfredo, Saikatendu, Kumar S, Schröder, Martin, Stolz, Alexandra, Tellechea, Mariana, Turunen, Brandon J, Vilar, Santiago, Wang, Jinhua, Zuercher, William J, Willson, Timothy M, Drewry, David H
Format: Article
Language:English
Subjects:
Annotations
Binding sites
Biology
Drug Discovery
Experiments
Humans
Initiatives
Kinases
Medical research
Pharmaceutical industry
Protein kinase inhibitors
Protein Kinase Inhibitors - chemistry
Protein Kinase Inhibitors - therapeutic use
Protein Serine-Threonine Kinases - antagonists & inhibitors
Protein Serine-Threonine Kinases - chemistry
Small Molecule Libraries - chemistry
Small Molecule Libraries - therapeutic use
Structure-Activity Relationship
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Description
Summary: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.
ISSN:1422-0067
1661-6596
1422-0067
DOI:10.3390/ijms22020566