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Compound class: Synthetic organic
Comment: The compound (from a pre-print) is selective KDM5 covalent inhibitor designed to target cysteine residues only present in the KDM5 sub-family . Target engagement and ChIP-seq analysis showed that compound 7 inhibited KDM5B in cells and induced a global increase of the H3K4me3 mark at transcriptional start sites. KDM5B is thus involved in the epigenetic regulatory pathway of immune response and potential targets for antipathogen and anticancer immunotherapy.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Vazquez-Rodriguez S, Wright M, Rogers CM, Cribbs AP, Velupillai S, Philpott M, Lee H, Dunford JE, Huber KVM, Robers MB et al.. (2019)
Design, Synthesis and Characterization of Covalent KDM5 Inhibitors.
Angew Chem Int Ed Engl, 58 (2): 515-519. DOI: 10.26434/chemrxiv.7072592.v1 [PMID:30431220]
2. Wu L, Cao J, Cai WL, Lang SM, Horton JR, Jansen DJ, Liu ZZ, Chen JF, Zhang M, Mott BT et al.. (2018)
KDM5 histone demethylases repress immune response via suppression of STING.
PLoS Biol, 16 (8): e2006134. [PMID:30080846]