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Synonyms: compound 23 [PMID: 30125504]
Compound class: Synthetic organic
Comment: This compound was designed as a dual inhibitor of the BET family protein BRD4 and polo like kinase 1 (PLK1) to investigate the potential of synergistic inhibition of these two proteins as an anti-cancer therapy . Compound 23 is an equipotent inhibitor of BRD4-BD1 and PLK1 that will facilitate exploration of this polypharmacological approach as a cancer treatment.
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. Liu S, Yosief HO, Dai L, Huang H, Dhawan G, Zhang X, Muthengi AM, Roberts J, Buckley DL, Perry JA et al.. (2018)
Structure-Guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitors.
J. Med. Chem., 61 (17): 7785-7795. [PMID:30125504]