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The Kinase Chemogenomic Set (KCGS) is a collection of narrow spectrum small molecule kinase inhibitors that has been assembled by the SGC-UNC to study the biology of dark kinases. KCGS is the most diverse and highly annotated publicly available collection of kinase inhibitors. We have recently updated to version 2.0 of the set. KCGSv2.0 is distributed by CancerTools.org, a non-profit community of cancer researchers, working together to accelerate cancer research. This is a link to the KCGSv2.0 product page.

 KCGSv2.0 contains 295 kinase inhibitors sourced from eight pharma companies and academic laboratories with potent activity on 262 human kinases. Each inhibitor has been cross screened across hundreds of kinases and only those meeting strict selectivity criteria are included in the set. An open access scientific paper and supporting information describing KCGSv1.0 with details of the kinases covered and its use in cell-based assays has been published in the International Journal of Molecular Sciences. More on details of KCGSv2.0 will follow, but to get started you can look at this blog post. You can find more details using the spreadsheet deposited in zenodo. This spreadsheet provides the KCGSv2.0 plate map, and details about the compounds in KCGSv2.0 and the kinases these compounds cover.

For additional information see the KCGS FAQ

KCGSv2.0 Availability
The current set is available to any investigator at a non-for-profit organization for an access fee of $3100 that off-sets the resynthesis cost of the small molecule inhibitors. Requestors receive:

  •       A copy of KCGS in 384-well plates as 1 µL of 10 mM DMSO solution

  •       A spreadsheet that lists chemical structure, target kinase, and literature references for each inhibitor

  •       5 x 1 µL of 10 mM DMSO cherry picks upon request

  •       Access to the full kinase selectivity data for each inhibitor

For UNC Investigators KCGSv2.0 is available through Infoporte CORES. For all other investigators, KCGSv2.0 is available from our distribution partner CancerTools/org.

KCGS Resynthesis
To ensure the continued availability of KCGSv2.0, we have completed a project to resupply all of the inhibitors in the set.

Acknowledgment
Funding to support the assembly and annotation of KCGS was provided by the UNC Eshelman Institute for Innovation, the NIH Illuminating the Druggable Genome (1U24DK116204-01), and the SGC. Kinase inhibitors were made available by AbbVie, Bayer, Boehringer Ingelheim, GlaxoSmithKline, Merck Sharp & Dohme, Pfizer, Takeda, AstraZeneca, and Vertex. Additional kinase inhibitors were provided by Nathanael Gray (Dana Farber Cancer Institute) and Julian Blagg (Cancer Research UK). Screening assays were supported by Promega and Eurofins-DiscoverX. Funding to support resynthesis of KCGS was provided by the University Cancer Research Fund, UNC Eshelman Institute for Innovation, the Office of the UNC Vice Chancellor for Research, the UNC School of Medicine, and the SGC.