Compound name
PD-166866
Protein family
Protein Kinase
Target name
FGFR1
Affinity biochemical (nM)
52.4
Affinity on-target cellular (nM)
10.8
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0001087a
SMILES
COc1cc(OC)cc(-c2cc3cnc(N)nc3nc2NC(=O)NC(C)(C)C)c1
InChIKey
NHJSWORVNIOXIT-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
Radiometric kinase assay (full-length FGFR1)
Affinity Biochemical Source Knowledge
https://jpet.aspetjournals.org/content/286/1/569.long
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Immunoblot (inhibition of FGFR1 autophosphorylation in NIH3T3 cells)
Affinity on-target cellular source knowledge
https://jpet.aspetjournals.org/content/286/1/569.long
Affinity on-target cellular relation
=
Selectivity platform
Kinase panel (DSF assay)
Selectivity platform number of targets
100
Selectivity remarks
Screened at 20 µM, closest targets in the screen: dTm FLT1 = 7.6 K, STK10 = 4.8K, clean profile;
Screened in enzymatic assays: IC50(PDGFR) >50 µM, IC50(EGFR) >50 µM, IC50(SRC) >50 µM, IC50(MAPK1) >50 µM, IC50(PRKCA) >50 µM, IC50(INSR) >50 µM, IC50(CDK4) >50 µM; In-cellulo follow-up of closest targets (autophosphorylation of PDGFR in rat aortic smooth muscle cells, EGF receptors in A431 cells, and INSR in NIHIR cells): IC50(EGFR) >1 µM, IC50(INSR) >1 µM, IC50(PDGF) >30 µM (https://jpet.aspetjournals.org/content/286/1/569.long);
Screened in enzymatic assays: IC50(PDGFR) >50 µM, IC50(EGFR) >50 µM, IC50(SRC) >50 µM, IC50(MAPK1) >50 µM, IC50(PRKCA) >50 µM, IC50(INSR) >50 µM, IC50(CDK4) >50 µM; In-cellulo follow-up of closest targets (autophosphorylation of PDGFR in rat aortic smooth muscle cells, EGF receptors in A431 cells, and INSR in NIHIR cells): IC50(EGFR) >1 µM, IC50(INSR) >1 µM, IC50(PDGF) >30 µM (https://jpet.aspetjournals.org/content/286/1/569.long);
Selectivity Source Knowledge
https://jpet.aspetjournals.org/content/286/1/569.long
Selectivity Number of Off-targets
2