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

• Published in: International journal of molecular sciences Vol. 22; no. 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: Journal Article
• Language: English
• Published: Switzerland MDPI AG 08.01.2021; MDPI
• Subjects: Annotations; Binding sites; Biology; chemogenomic set; Drug Discovery; Experiments; Humans; Initiatives; KCGS; kinase inhibitor; Kinases; Medical research; Pharmaceutical industry; phenotypic screening; protein kinase; 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; small molecules; Structure-Activity Relationship; druggable genome; kinase inhibitor; chemogenomic set; drug discovery; KCGS; phenotypic screening; understudied kinase; protein kinase; small molecules
• ISSN: 1422-0067; 1661-6596; 1422-0067
• DOI: 10.3390/ijms22020566

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.