The AstraZeneca ATR serine/threonine kinase inhibitor, ceralasertib (AZD6738) , is a potent (1 nM biochemical IC50), orally bioavailable, ATP-competitive inhibitor, and is one of the most clinically advanced sulfoximines with ~32 registered clinical studies. An indole to azaindole change was key to mitigating CYP TDI during discovery, which [...]
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Dec. 16, 2021
Ceralasertib: a Serine/Threonine Kinase Inhibitor
ceralasertib (AZD6738)
ATR serine/threonine kinase inhibitor oral agent in Ph. II for cancer from mTOR-program derived hit + opt. Clinical Cancer Research AstraZeneca, Cambridge, UK
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