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Compound class: Synthetic organic
Comment: BSJ-03-123 is a PROTAC (proteolysis targeting chimera) . It is a hybrid molecule that simultaneously inhibits CDK4/CDK6 kinase activity and recruits E3 ligase CRL4CRBN to target the kinases for destruction via E3 ligase-mediated ubiquitination and proteasomal degradation. BSJ-03-123 is a palbociclib-based selective CDK6 degrader.
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. Jiang B, Wang ES, Donovan KA, Liang Y, Fischer ES, Zhang T, Gray NS. (2019)
Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6.
Angew Chem Int Ed Engl, 58 (19): 6321-6326. [PMID:30802347]