Compound name
PF-04217903
Protein family
Protein Kinase
Target name
MET
Affinity biochemical (nM)
4.8
Affinity on-target cellular (nM)
5
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000619a
SMILES
OCCN(N=C1)C=C1C2=CN=C3C(N(CC4=CC=C5C(C=CC=N5)=C4)N=N3)=N2
InChIKey
PDMUGYOXRHVNMO-UHFFFAOYSA-N
NCBI gene ID
4233
UniProt ID
P08581
Synonyms
HGFR, RCCP2, DFNB97
Mode of action
Inhibitor
Affinity biochemical definition
Ki
Affinity biochemical assay type
Continuous-coupled spectrophotometric assay (detecting ADP production)
Affinity Biochemical Source Knowledge
https://doi.org/10.1158/1535-7163.MCT-11-0839
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
ELISA (c-Met phosphorylation in HT29 cells)
Affinity on-target cellular relation
=
Selectivity platform
Kinase panel (Invitrogen)
Selectivity platform number of targets
125
Selectivity remarks
Screened at 1 µM and 10 µM, no target >50% inhibition; Screened in Dundee panel (51 kinases at 10 µM), no target >50% inhibition; Screened in Pfizer panel (48 kinases), no target >50% inhibition; Screened in Millipore panel (105 kinases at 1 µM an 10 µM), closest targets: ALK, EpHB2, INSR; IC50 follow-up showed all IC50 >10 µM; PF-04217903 is >1000-fold selective for c-Met;
Selectivity Source Knowledge
https://doi.org/10.1021/bi900438w
Selectivity Number of Off-targets
0