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Compound class: Synthetic organic
Comment: This compound is reported by Compain et al. (2018) as the protein kinase inhibitor component of a β-glucuronidase-responsive albumin-binding prodrug that was designed as a novel cancer therapeutic . The biological activity of inhibitor 2 is blocked when it is incoprorated in the enzyme-responsive prodrug. The active inhibitor is released only in the presence of β-glucuronidase (e.g. as exists in the tumour microenvironment), so should faciliate selective delivery of the drug to the tumour whilst minimising systemic off-target and adverse effects. Compound 2 is a multi-kinase inhibitor with a similar selectivity profile as seliciclib, but with additional potent inhibitory activity at DYRK3 and GSK3.
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. Compain G, Oumata N, Clarhaut J, Péraudeau E, Renoux B, Galons H, Papot S. (2018)
A β-glucuronidase-responsive albumin-binding prodrug for potential selective kinase inhibitor-based cancer chemotherapy.
Eur J Med Chem, 158: 1-6. [PMID:30199702]