Compound class:
Synthetic organic
Comment: M324 is the major metabolite of the PARP inhibitor rucaparib. The metabolite has a unique off-target kinase selectivity profile compared to the parent drug, with M324 potently inhibiting PLK2 and GSK3A [1]; neither of these kinases is so potently inhibited by rucaparib. It is suggested that the combined polypharmacology of the two chemical entities at PARP and kinase targets may offer potential clinically-relevant synergy for tumour therapy.
Ligand Activity Visualisation ChartsThese 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. ✖ |
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Selectivity at enzymes | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
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