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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.

Original publication

DOI

10.3390/ijms22020566

Type

Journal article

Journal

Int J Mol Sci

Publication Date

08/01/2021

Volume

22

Keywords

KCGS, chemogenomic set, drug discovery, druggable genome, kinase inhibitor, phenotypic screening, protein kinase, small molecules, understudied kinase, Drug Discovery, Humans, Protein Kinase Inhibitors, Protein Serine-Threonine Kinases, Small Molecule Libraries, Structure-Activity Relationship