Compound name
BMS 777607
Protein family
Protein Kinase
Target name
MET
Affinity biochemical (nM)
3.9
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000624a
SMILES
CCOC1=C(C(=O)N(C=C1)C2=CC=C(C=C2)F)C(=O)NC3=CC(=C(C=C3)OC4=C(C(=NC=C4)N)Cl)F
InChIKey
VNBRGSXVFBYQNN-UHFFFAOYSA-N
NCBI gene ID
4233
UniProt ID
P08581
Synonyms
HGFR, RCCP2, DFNB97
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzyme activity assay
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/jm801586s
Affinity biochemical relation
=
Selectivity platform
Ambit kinome screening platform
Selectivity platform number of targets
200
Selectivity remarks
Screened at 10 µM (Ambit phage-based competition binding assay), closest targets as % of contr.: FRK (0.55%), FLT4 (0.85%), FLT3 (0.05%), EPHA3 (0.1%), CSF1R (0.8%), BLK (0.35%), STK10 (0%), AURKB (0%), KIT (0%), LCK (0.2%), MUSK (0%), PDGFRA/B (0.2/0.7%), TEK (0.15%), NTRK1/2/3 (0.55/ 0.1/ 0.1%), KDR (0.2%), MKNK2 (0.75%); In vitro follow up of closest targets: IC50(MERTK) = 14 nM, IC50(FLT3) = 16 nM, IC50(AURKB) = 78 nM, IC50(LCK) = 120 nM, IC50(KDR) = 180 nM, IC50(NTRK1/2) = 290/ 190 nM, IC50(PKA) = 550, IC50 >2 µM for: BTK, CDK2E, EGFR, GSK3B, IGFR1R, IKK1/2, INSR, JAK2, MAPKAPK2, MAPK14, PIM1, PLK1/3
Selectivity Source Knowledge
https://doi.org/10.1021/jm801586s
Selectivity Number of Off-targets
20