HPK1-IN-3

HPK1-IN-3 : ATP-competitive of MAP4K1

Structure

Information

  • MAP4K1
  • ATP competitive
  • up to 1 uM

In Vitro Validations

Uniprot ID: Q92918
Target Class: Kinase
Target SubClass: STE
Potency: IC50
Potency Value: 0.25 nM
Potency Assay: HPK1 Biochemical Assay (TR-FRET)
PDB ID for probe-target interaction (3D structure): 7M0M
Target aliases:
Mitogen-activated protein kinase kinase kinase kin ...

DOI Reference: 10.1021/acsmedchemlett.1c00096

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity within target family: Improved kinome selectivity for HPK1-IN-3 (>100× selectivity in 252/265 kinases examined). MAP4K2/3/4 fold-selective 1150x/4x/3423x JAK1/2/3 fold-selective 1072x/262x/136x FTL3 fold-selective >10000x LCK fold-selective >10000x
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SERP ratings and comments


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