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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Published in | International journal of molecular sciences Vol. 22; no. 2; p. 566 |
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Main Authors | , , , , , , , , , , , , , , , , , , , , , , , , , , , , , |
Format | Journal Article |
Language | English |
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08.01.2021
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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. |
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AbstractList | 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. |
Author | Al-Ali, Hassan Gray, Nathanael S Tellechea, Mariana Fischer, Christian Müller, Susanne Axtman, Alison D Owen, Dafydd Mills, Caitlin E Vilar, Santiago Saikatendu, Kumar S Futrell, Robert E Knapp, Stefan Frederiksen, Mathias Lücking, Ulrich Ettmayer, Peter Schröder, Martin Wang, Jinhua Drewry, David H Ebner, Daniel Wells, Carrow I Stolz, Alexandra Picado, Alfredo Asquith, Christopher R M Andrews, David M Michaelides, Michael Willson, Timothy M Dikic, Ivan Zuercher, William J Turunen, Brandon J Hatch, Stephanie B |
AuthorAffiliation | 3 Truvitech LLC, Miami, FL 33136, USA; santiago@truvitech.com 16 Institute for Pharmaceutical Chemistry, Johann Wolfgang Goethe-University, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany 9 Boehringer Ingelheim RCV GmbH & Co KG, 1121 Vienna, Austria; peter.ettmayer@boehringer-ingelheim.com 14 MRC Oxford Institute for Radiation Oncology, Department of Oncology, University of Oxford, Roosevelt Drive, Oxford OX3 7XB, UK; stephanie.hatch@ndm.ox.ac.uk 17 Bayer Pharma AG, Drug Discovery, Müllerstrasse 178, 13353 Berlin, Germany; ulrich.luecking@forxtherapeutics.com 22 GlaxoSmithKline, Chemical Biology, 1250 S Collegeville Rd, Collegeville, PA 19426, USA; brandon.j.turunen@gsk.com 15 Structural Genomics Consortium, Buchmann Institute for Molecular Life Sciences, Goethe University Frankfurt, Max-von-Laue-Straße 15, 60438 Frankfurt am Main, Germany 2 The Miami Project to Cure Paralysis, Peggy and Harold Katz Family Drug Discovery Center, Sylvester Comprehensive Cancer Center, Departments of Neur |
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Keywords | druggable genome kinase inhibitor chemogenomic set drug discovery KCGS phenotypic screening understudied kinase protein kinase small molecules |
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Title | The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification |
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