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Synonyms: compound 7 [PMID: 34110416] | SJ-988497
Compound class:
Synthetic organic
Comment: SJ988497 is a PROTAC class degrader that targets Janus kinase 2 (JAK2) protein for proteosomal degradation [1]. It was designed for potential to treat cytokine receptor-like factor 2 (CRLF2)-rearranged acute lymphoblastic leukemia (ALL), based on evidence that overexpression of CRLF2 promotes activation of the JAK-STAT pathway in this form of ALL. The JAK2 binding moiety of SJ988497 is based on the portion of the JAK inhibitor baricitinib that interacts with the JAK2 tyrosine kinase domain. It ligates the target protein with the cereblon (CRBN) E3 ubiquitin ligase to induce ubiquitin-mediated proteosomal degradation.
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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