Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetHepatocyte growth factor receptor [1078-1345,M1250T,L1272V]
LigandBDBM24466
Substrate/Competitorbiotinylated gastrin substrate
Meas. Tech.HTRF Kinase Inhibition Assay
pH7.4±n/a
Temperature295.15±n/a K
Ki 4.1±n/a nM
Citation Liu, LSiegmund, AXi, NKaplan-Lefko, PRex, KChen, ALin, JMoriguchi, JBerry, LHuang, LTeffera, YYang, YZhang, YBellon, SFLee, MShimanovich, RBak, ADominguez, CNorman, MHHarmange, JCDussault, IKim, TS Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458). J Med Chem51:3688-91 (2008) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Hepatocyte growth factor receptor [1078-1345,M1250T,L1272V]
Name:Hepatocyte growth factor receptor [1078-1345,M1250T,L1272V]
Synonyms:HGF/SF receptor | MET | MET_HUMAN | Met proto-oncogene tyrosine kinase | SF receptor | Scatter factor receptor | Tyrosine Kinase c-Met Mutant (M1250T) | c-Met
Type:Tyrosine-protein kinase
Mol. Mass.:30546.20
Organism:Homo sapiens (Human)
Description:P08581[1078-1345,M1250T,L1272V]
Residue:268
Sequence:
VHFNEVIGRGHFGCVYHGTLLDNDGKKIHCAVKSLNRITDIGEVSQFLTEGIIMKDFSHP
NVLSLLGICLRSEGSPLVVLPYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKYLAS
KKFVHRDLAARNCMLDEKFTVKVADFGLARDMYDKEYYSVHNKTGAKLPVKWTALESLQT
QKFTTKSDVWSFGVVLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYCPDPLYEVML
KCWHPKAEMRPSFSELVSRISAIFSTFI
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM24466
biotinylated gastrin substrate
Name:biotinylated gastrin substrate
Synonyms:n/a
Type:Peptide
Mol. Mass.:2100.22
Organism:n/a
Description:n/a
Residue:17
Sequence:
biotinyl-EEEEAYGWLDF