Compound name
PF-04554878
Protein family
Protein Kinase
Target name
PTK2
Affinity biochemical (nM)
0.2
Affinity on-target cellular (nM)
3
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000138c
SMILES
CNC(C1=CC=C(NC2=NC=C(C(F)(F)F)C(NCC3=C(N(S(C)(=O)=O)C)N=CC=N3)=N2)C=C1)=O
InChIKey
FWLMVFUGMHIOAA-UHFFFAOYSA-N
NCBI gene ID
5747
UniProt ID
Q05397
Synonyms
FAK, FADK, FAK1, PPP1R71
Mode of action
Inhibitor
Negative control
PF-00911705
Affinity biochemical definition
IC50
Affinity biochemical assay type
Binding assay
Affinity Biochemical Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04554878
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Inhibition of human PTK2 phosphorylation in A431 cells
Affinity on-target cellular relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
448
Selectivity remarks
Screened at 0.1 µM, closest targets as % of contr.: CLK2 (0%), FLT3(N841I) (0%), FLT3(D835V) (0.2%), YSK4 (1.7%), JAK2 (4.8%), FLT3(D835Y) (5.9%), STK16 (7.7%), JAK3 (8.2), TTK (8.3%), FLT3(ITD,F691L) (9%), FLT3(D835H) (9.8%); Screened in Invitrogen panel at 10 µM, closest targets: IC50(NTRK1) = 56 nM, IC50(MAP3K9) = 75.3 nM; Screened in CEREP panel against 122 human receptors, ion channels, enzymes, closest target: Ki(ADORA3) = 27 nM; Screened in GPCR screen against 45 targets at 10 µM, clean profile;
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04554878
Selectivity Number of Off-targets
11