Compound name
Filgotinib
Protein family
Protein Kinase
Target name
JAK1@kinase 1
Affinity biochemical (nM)
10
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
3716
UniProt ID
P23458
Synonyms
JAK1A, JTK3
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