GNE-9822

Inhibitor of ITK

Structure

Information

  • ITK
  • Inhibitor
  • up to 100 nM

In Vitro Validations

Uniprot ID: Q08881
Target Class: Kinase
Target SubClass: TK
Potency: Ki
Potency Value: 0.7 nM
Potency Assay: Biochemical Assay
PDB ID for probe-target interaction (3D structure): 4PQN
Structure-activity relationship: yes
Target aliases:
Tyrosine-protein kinase ITK/TSK, LYK, EMT, ITK, IT ...

DOI Reference: 10.1021/jm500550e

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency end-point : Ki Aurora A
Potency assay (off target): Aurora A Biochemical Assay
Probe Selectivity in Vitro:

Broad kinase selectivity of this molecule was observed: only six of 286 off-target kinases were inhibited >70% when tested at 0.1 μM (>100X ITK Ki).

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SERP ratings and comments


No SERP comments found for GNE-9822