“compound 23” is a selective CRBN-based degrader of the pseudokinase, IRAK3, with in vitro activity in primary human cells. A volcano plot shows remarkable separation between IRAK3 degradation vs. most other proteins, with very little activity against family members IRAK1 and IRAK4. The authors were able to quickly generate this degrader from [...]
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Sep. 18, 2021
Compound 23: A Selective Degrader of IRAK3 Pseudokinase
"compound 23"
selective degrader of IRAK3 pseudokinase in vitro degradation in primary macrophages from mining of internal kinase inh. and linking J. Med. Chem., Sep. 24, 2020 AstraZeneca, Waltham, MA / Cambridge, UK
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