- Guide to PHARMACOLOGY
Synonyms: compound 12c [PMID: 22070629]
Compound class: Synthetic organic
Comment: MLN0905 is an orally bioavailable inhibitor of Polo-like kinase 1 (PLK1) with in vivo antitumour activity . Despite apparent off-target binding in a kinase profile screen, none of these targets would be expected to produce the cellular and pharmacodynamic effects associated with MLN0905, and in fact the phenotype observed with MLN0905 inhibition is consistent with that observed with PLK1 knockdown by RNAi and other PLK1 inhibitors.
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. Duffey MO, Vos TJ, Adams R, Alley J, Anthony J, Barrett C, Bharathan I, Bowman D, Bump NJ, Chau R et al.. (2012)
Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of Polo-like kinase 1 (MLN0905).
J Med Chem, 55 (1): 197-208. [PMID:22070629]