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Developing a Kinase Chemogenomic Set: Facilitating Investigation into Kinase Biology by Linking Phenotypes to Targets

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Chemogenomics

Part of the book series: Methods in Molecular Biology ((MIMB,volume 2706))

Abstract

Advances in increasingly complex phenotypic screening with lower throughput have necessitated the screening of smaller more highly annotated sets. One such collection of compounds which has been recently assembled is the kinase chemogenomic set. This is a set of curated kinase inhibitors built upon previous iterations, PKIS and PKIS2, and donations from our partners. Each compound in the set has been carefully selected based on selectivity, potency, and kinome coverage. These compounds as a set have been made available to the scientific community, enabling phenotypic screens to identify kinases that drive novel biology. Additionally, the associated data deposited in the public domain have also been used to inform new inhibitor design. Further expansion of this set to complete kinome coverage will allow for a greater understanding of kinase biology and its role in disease.

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Acknowledgement

This work was supported by the Eshelman Institute for Innovation (http://unceii.org/). The SGC is a registered charity (number 1097737) that receives funds from AbbVie, Bayer Pharma AG, Boehringer Ingelheim, Canada Foundation for Innovation, Eshelman Institute for Innovation, Genome Canada, Innovative Medicines Initiative (EU/EFPIA) [ULTRA-DD grant no. 115766], Janssen, Merck & Co., Novartis Pharma AG, Ontario Ministry of Economic Development and Innovation, Pfizer, São Paulo Research Foundation-FAPESP, Takeda, and Wellcome Trust [092809/Z/10/Z]. GlaxoSmithKline, Pfizer, Takeda, AstraZeneca, Boehringer Ingelheim, Bayer, Abbvie, Merck, and Nathanael Gray are gratefully acknowledged for donation of KCGS compounds.

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Authors and Affiliations

  1. Structural Genomics Consortium (SGC), UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill (UNC-CH), Chapel Hill, NC, USA

    Carrow I. Wells & David H. Drewry

  2. Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, UNC-CH, Chapel Hill, NC, USA

    Carrow I. Wells & David H. Drewry

Authors
  1. Carrow I. Wells
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  2. David H. Drewry
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Correspondence to Carrow I. Wells .

Editor information

Editors and Affiliations

  1. Department of Pharmacy, Ludwig-Maximilians-Universität München, Munich, Germany

    Daniel Merk

  2. Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Frankfurt am Main, Germany

    Apirat Chaikuad

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© 2023 The Author(s), under exclusive license to Springer Science+Business Media, LLC, part of Springer Nature

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Wells, C.I., Drewry, D.H. (2023). Developing a Kinase Chemogenomic Set: Facilitating Investigation into Kinase Biology by Linking Phenotypes to Targets. In: Merk, D., Chaikuad, A. (eds) Chemogenomics. Methods in Molecular Biology, vol 2706. Humana, New York, NY. https://doi.org/10.1007/978-1-0716-3397-7_2

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  • DOI: https://doi.org/10.1007/978-1-0716-3397-7_2

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  • Publisher Name: Humana, New York, NY

  • Print ISBN: 978-1-0716-3396-0

  • Online ISBN: 978-1-0716-3397-7

  • eBook Packages: Springer Protocols

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