selective inhibitor of unphosphorylated HPK1

non-ATP competitive, IC50 = 1.2 µM

from 700k cmpd HTS for non-ATP comp. inh.

Biochemistry

Janssen R&D, Spring House, PA

Chemical structure of compound 1 Janssen non-ATP competitive HPK1 inhibitor

The Janssen non-ATP competitive HPK1 inhibitor, “compound 1,” was identified from a screening cascade specifically looking for allosteric inhibitors, which may provide a selectivity advantage over ATP-competitive starting points.…


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