|
Synonyms: compound 3i [PMID: 28692295]
Compound class:
Synthetic organic
Comment: This compound (3i) is a TANK-binding kinase 1 (TBK1) PROTAC degrader [1]. The TBK1 inhibitor portion of the molecule binds the kinase and the Von Hippel-Lindau (VHL) binding portion of the molecule recruits an E3 ubiquitin ligase to the bound kinase and this leads to proteasomal degradation of the kinase protein. This PROTAC was used to evaluate TBK1 as a target in mutant KRAS cancer cells. 3i does not promote degradation of closely related IKKε which has 65% sequence homology with TBK1.
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. ✖ |
|
|||||||||||||||||||||||||||||||||||
For advanced searching click here to open chemical structure editor
