Baricitinib

Inhibitor of JAK1, JAK2

Structure

Information

  • JAK1
  • JAK2
  • Inhibitor
  • up to 100 nM

In Vitro Validations

Uniprot ID: P23458
Target Class: Kinase
Target SubClass: TK
Potency: IC 50
Potency Value: 5.9 nM
Potency Assay: Biochemical Assay (TR-FRET)
PDB ID for probe-target interaction (3D structure): --
Structure-activity relationship: yes
Target aliases:
Tyrosine-protein kinase JAK1, JAK1B, JAK1A, JAK1, ...

DOI Reference: 10.4049/jimmunol.0902819

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency end-point : IC50 Tyk2 53 nM, JAK3 560 nM, AAK1 17.2 nM, BIKE 39.8 nM, GAK134.4 nM, MPSK1 68.5 nM
Potency assay (off target): TR-FRET, ITC
Probe Selectivity in Vitro:

JAK3 IC50 ~ 560 nM, ~10-fold selectivity against Tyk2 (IC50 = 53 nM), c-Met (IC50 > 10,000 nM) and Chk2 (IC50 > 1,000 nM). Tested @ 500 nM against a diverse panel of 28 kinases with no significant inhibition observed. Additional Off Targets are (Kd): AAK1 17.2 nM, BIKE 39.8 nM, GAK134.4 nM , MPSK1 68.5 nM

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