Building chemogenomic sets that enable target discovery.
The SGC offers a variety of chemogenomic sets to support research in target discovery and biological mechanisms. The first was the kinase chemogenomic set (KCGS), comprising well-annotated kinase inhibitors, which allows screening in disease-relevant assays, pointing toward significant kinases for in-depth study. The KCGS includes inhibitors with narrow profiles, targeting specific kinase subsets, and exploring inhibition across the kinome.
The KCGS is extended by the EUbOPEN chemogenomics library. The targets include a variety of proteins families, including kinases, GPCRs, SLCs, E3 ligases, epigenetic targets and others.
The Kinase Chemogenomic Set by SGC at UNC
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. 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.
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 their use in cell-based assays has been published in International Journal of Molecular Sciences.
EUbOPEN Chemogenomic Sets
The chemogenomic sets, generated by the EUbOPEN project, is organized into subsets covering major target families, including protein kinases, membrane proteins and epigenetic modulators. The set is steadily growing and will cover 1000 targets by the end of the project in 2025.
In this dataset, you will find the actual chemogenomics sets and the data will also be available on the EUbOPEN Gateway. The chemogenomic compounds shall be used as a set to be able to link a phenotype to a specific target at the recommended concentration provided for each compound.