Compound name
Filgotinib
Protein family
Protein Kinase
Target name
JAK2@kinase 1
Affinity biochemical (nM)
28
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000626a
SMILES
C1CC1C(=O)NC2=NN3C(=N2)C=CC=C3C4=CC=C(C=C4)CN5CCS(=O)(=O)CC5
InChIKey
RIJLVEAXPNLDTC-UHFFFAOYSA-N
NCBI gene ID
3717
UniProt ID
O60674
Synonyms
JTK10
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Radiometric kinase assay (incorporation of phosphate into an ULight-JAK-1(Tyr1023) peptide using an europium-labeled anti-phosphotyrosine Ab)
Affinity Biochemical Source Knowledge
https://doi.org/10.4049/jimmunol.1201348
Affinity biochemical relation
=
Selectivity platform
Radioactive biochemical assays (Millipore and Galapagos N.V.)
Selectivity platform number of targets
175
Selectivity remarks
Screened at 1 µM, closest targets: IC50( FLT3) = 338 nM, IC50(FLT4) = 274 nM, IC50(CSF1R) = 488.9 nM, IC50(TYK2) = 116 nM
Selectivity Source Knowledge
https://doi.org/10.4049/jimmunol.1201348
Selectivity Number of Off-targets
4