Abstract:Herein we report the discovery of a novel biaryl amide
series as
selective inhibitors of hematopoietic protein kinase 1 (HPK1). Structure–activity
relationship development, aided by molecular modeling, identified
indazole 5b as a core for further exploration because
of its outstanding enzymatic and cellular potency coupled with encouraging
kinome selectivity. Late-stage manipulation of the right-hand aryl
and amine moieties surmounted issues of selectivity over TRKA, MAP4K2,
and STK4 as well as generating comp… Show more
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