- Guide to PHARMACOLOGY
Synonyms: compound 2 [PMID: 24900658] | R-1530 | R1530 | RG1530
Compound class: Synthetic organic
Comment: RG-1530 is an orally active multikinase inhibitor, with a high affinity for polo like kinase 4 (PLK4). Its PLK4 inhibitory action was expoited for antiproliferative potential [1-4]. PLK4 is expressed at very low levels in normal cells, but its expression can be upregulated in cancer cells where it localises to the centriole and is essential for controlling centriole duplication and mitotic progression. This makes PLK4 an ideal target for disrupting mitosis in cancer cells.
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.✖