Synonyms: compound 23 [PMID: 32803978]
Compound class:
Synthetic organic
Comment: This molecule is aproteolysis-targeting chimera (PROTAC) degrader of interleukin 1 receptor associated kinase 3 (IRAK3) [1]. It promotes ternary complex formation between IRAK3 and the cereblon (CRBN) E3 ubiquitin ligase. IRAK3 is a regulatory protein that suppresses proinflammatory signalling in monocytes, macrophages, and neutrophils. Blocking IRAK3's immunosuppressive function is being investigated as an anti-tumour mechanism [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. ✖ |
References |
1. Degorce SL, Tavana O, Banks E, Crafter C, Gingipalli L, Kouvchinov D, Mao Y, Pachl F, Solanki A, Valge-Archer V et al.. (2020)
Discovery of Proteolysis-Targeting Chimera Molecules that Selectively Degrade the IRAK3 Pseudokinase. J Med Chem, 63 (18): 10460-10473. [PMID:32803978] |
2. Rhyasen GW, Starczynowski DT. (2015)
IRAK signalling in cancer. Br J Cancer, 112 (2): 232-7. [PMID:25290089] |