Compound name
FGF401
Protein family
Protein Kinase
Target name
FGFR4
Affinity biochemical (nM)
0.9
Affinity on-target cellular (nM)
4.3
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0002059a
SMILES
CN1CC(N(CC2=CC(CCCN3C(NC4=NC=C(C#N)C(NCCOC)=C4)=O)=C3N=C2C=O)CC1)=O
InChIKey
BHKDKKZMPODMIQ-UHFFFAOYSA-N
NCBI gene ID
2264
UniProt ID
P22455
Synonyms
JTK2, CD334
Mode of action
Reversible covalent inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Caliper microfluidic mobility shift assay (conc. ATP = Km)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/32930584/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Cellular assay (FGFR4 autophosphorylation in BaF3 cells)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/32930584/
Affinity on-target cellular relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
456
Selectivity remarks
Screened at 3 µM, S-Score =0.003, in-vitro potency of closest targets: IC50(FGFR1) >10 µM, IC50(FGFR2) >10 µM, IC50(FGFR3) >10 µM, IC50(FGFR4) = 1.9 nM, IC50(FGFR4, C552A) >10 µM, IC50(FGFR4, rat) >10 µM, IC50(FGFR4, N535K) = 0.9 nM, IC50(FGFR4, V550E) = 110 nM, IC50(AURKA) = 5.6 µM, IC50(MAPKAPK2) = 9.4 µM;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/32930584/
Selectivity Number of Off-targets
0