“Compound 25,” inhibits HPK1 via a rare “P-loop folded” active site conformation. The molecule was nominated by reviewer Julien Lefranc , and structural biologist Yoana Dimitrova shares some insight here: “The ‘folded P-loop’ conformation is considered “extremely unusual” – authors of a 2011 paper looked into this and found it in only 62 out [...]
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Jan. 17, 2022
Inhibition of HPK1 via Rare “P-Loop Folded” Active Site Conformation
“compound 25”
HPK1 kinase inhibitor unusual P-loop-folded conformation inhibitor from HTS + SBDD ACS Medicinal Chemistry Letters Genentech, South San Francisco, CA
Reviewer:
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