Synonyms: compound 15 [PMID: 30335946]
Compound class:
Synthetic organic
Comment: This is a bivalent proteolysis-targeting chimera (PROTAC) molecule that promotes the degradation of the BCL6 transcription repressor protein [1]. It comprises a BCL6 binding domain linked to a thalidomide warhead that targets the bound BCL6 to the E3 ubiquitin ligase cereblon (CRBN), and on to ubiquitin-mediated proteosomal degradation. PROTAC 15 was developed by AstraZeneca for potential to treat lymphomas that are derived from germinal center B cells. Although PROTAC 15 leads to BCL6 degradation in vitro, the degradation is incomplete, and this produces only a weak antiproliferative effect on target diffuse large B-cell lymphoma (DLBCL) cells.
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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Classification | |
Compound class | Synthetic organic |
Ligand families/groups | PROTACs, molecular glues and other degraders |
Synonyms |
compound 15 [PMID: 30335946] |
Database Links | |
GtoPdb PubChem SID | 458923813 |
PubChem CID | 162366969 |
Search Google for chemical match using the InChIKey | YQWUMLVLLIWGQJ-UYEDPJPISA-N |
Search Google for chemicals with the same backbone | YQWUMLVLLIWGQJ |
UniChem Compound Search for chemical match using the InChIKey | YQWUMLVLLIWGQJ-UYEDPJPISA-N |
UniChem Connectivity Search for chemical match using the InChIKey | YQWUMLVLLIWGQJ-UYEDPJPISA-N |