molecules of the month


JAK1-selective kinase inhibitor

in clinical development for cancer

from HTS and SBDD of promiscuous hit

J. Med. Chem., Apr. 28, 2020

AstraZeneca, Waltham, MA

1 min read

AZD4205 is a JAK1-selective kinase inhibitor which is in clinical development for oncology rather than the inflammatory diseases most JAK1 inhibitors have aimed for. The compound has excellent PK in dog, and the authors demonstrate that JAK1 inhibition doesn’t have strong single-agent activity in a xenograft model but can synergize significantly with an EGFR-kinase inhibitor. The azaindole amide makes an uncommon bidentate interaction with the DFG-loop aspartate residue.

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