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

Structure of compound 23

“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…


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