molecules of the month

“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

Structure of compound 23
1 min read

“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 existing kinase inhibitors in their compound collection, showing how rapidly useful tools to assess structural roles of kinases can be generated through the degradation platform.

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