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TargetTyrosine Kinase c-Met Mutant (H1094R)
LigandBDBM24466
Substrate/Competitorbiotinylated gastrin substrate
Meas. Tech.HTRF Kinase Inhibition Assay
pH7.4±n/a
Temperature295.15±n/a K
Ki 0.5±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
 
Tyrosine Kinase c-Met Mutant (H1094R)
Name:Tyrosine Kinase c-Met Mutant (H1094R)
Synonyms:HGF/SF receptor | Met proto-oncogene tyrosine kinase | SF receptor | Scatter factor receptor | c-Met
Type:Tyrosine-protein kinase
Mol. Mass.:30595.85
Organism:Homo sapiens (Human)
Description:n/a
Residue:268
Sequence:
VHFNEVIGRGHFGCVYRGTLLDNDGKKIHCAVKSLNRITDIGEVSQFLTEGIIMKDFSHP
NVLSLLGICLRSEGSPLVVLPYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKYLAS
KKFVHRDLAARNCMLDEKFTVKVADFGLARDMYDKEYYSVHNKTGAKLPVKWMALESLQT
QKFTTKSDVWSFGVVLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYCPDPLYEVML
KCWHPKAEMRPSFSELVSRISAIFSTFI
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM24466
NameBDBM24466
Synonyms:1-(2-hydroxy-2-methylpropyl)-N-{5-[(7-methoxyquinolin-4-yl)oxy]pyridin-2-yl}-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide | Substituted Pyrazolone, 17
TypeSmall organic molecule
Emp. Form.C30H29N5O5
Mol. Mass.539.5818
SMILESCOc1ccc2c(Oc3ccc(NC(=O)c4c(C)n(CC(C)(C)O)n(-c5ccccc5)c4=O)nc3)ccnc2c1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
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