Compound name
PD173074
Protein family
Protein Kinase
Target name
FGFR1
Affinity biochemical (nM)
21.5
Affinity on-target cellular (nM)
15
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000699a
SMILES
O=C(NC(C)(C)C)NC2=NC1=NC(NCCCCN(CC)CC)=NC=C1C=C2C3=CC(OC)=CC(OC)=C3
InChIKey
DXCUKNQANPLTEJ-UHFFFAOYSA-N
NCBI gene ID
2260
UniProt ID
P11362
Synonyms
H2, H3, H4, H5, CEK, FLG, BFGFR, N-SAM, CD331
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzymatic inhibition assay (5 µM ATP)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/9774334/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Immunoblotting (inhibition of FGFR1 autophosphorylation in NIH 3T3 cells)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/9774334/
Affinity on-target cellular relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
317
Selectivity remarks
Screened at 10 μM, closest targets at % of contr.: DDR1 (1.1%), FLT4 (6.0%), CSF1R (6.6%), MST3 (7.0%), VEGFR1 (8.0%), YSK1 (9.4%);In-vitro potency of other targets: IC50(PDGFR, cytoplasmic domain) = 17.6 µM, IC50(c-Src) = 19.8 µM;
Selectivity Source Knowledge
https://lincs.hms.harvard.edu/db/datasets/20055/