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GNE-1858 is a novel, highly potent and ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor, with IC50s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA, respectively.
References: Hematopoietic Progenitor Kinase-1 Structure in a Domain-Swapped Dimer. Structure. 2019 Jan 2; 27(1):125-133.e4.
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