Compound class:
Synthetic organic
Comment: Compound 17 is an alectinib-based PROTAC degrader of anaplastic lymphoma kinase (ALK) [1]. The alectinib analogue is conjugated to pomalidomide through a linker, to deliver ALK protein for degradation via the ubiquitously expressed E3 ligase receptor cereblon. Compound 17 is one of the chemical structures claimed in ShanghaiTech University's patent WO2019114770A1 [2].
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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Bioactivity Comments |
ALK PROTAC 17 provides potent antiproliferative activity in ALK-dependent cancer cell lines and efficacy in a Karpas 299 xenograft mouse model [1]. Its DC50 value is 13.6 nM in Karpas 299 cells. |
Selectivity at catalytic receptors | ||||||||||||||||||||||||||||||||||
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