期刊
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
卷 22, 期 2, 页码 -出版社
MDPI
DOI: 10.3390/ijms22020566
关键词
protein kinase; kinase inhibitor; chemogenomic set; phenotypic screening; small molecules; KCGS; drug discovery; druggable genome; understudied kinase
资金
- AbbVie
- Bayer Pharma AG
- Boehringer Ingelheim
- Canada Foundation for Innovation
- Eshelman Institute for Innovation
- Genentech
- Genome Canada through Ontario Genomics Institute [OGI-196]
- EU/EFPIA/OICR/McGill/KTH/Diamond Innovative Medicines Initiative 2 Joint Undertaking (EUbOPEN) [875510]
- Janssen
- Merck KGaA
- Merck Sharp and Dohme
- Novartis Pharma AG
- Pfizer
- Sao Paulo Research Foundation-FAPESP
- Takeda
- Wellcome Trust
- UNC Lineberger Comprehensive Cancer Center
- National Institutes of Health [1R44TR001916-02, 1R01CA218442-01, 1U24DK116204-01]
- Foundation for Food and Agriculture Research (FFAR) [A18-2129-S001]
- DFG, German Reaseach Foundation [2591307 SFB1177]
- PharmAlliance
The chemogenomic set of protein kinase inhibitors described in this study is a valuable open science resource for studying kinase biology, consisting of 187 inhibitors that target 215 human kinases. It is highly annotated and selective, making it a useful tool for researchers in cell-based screens.
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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