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TargetTyrosine Kinase c-Met Mutant (Y1230H)
LigandBDBM24466
Substrate/Competitorbiotinylated gastrin substrate
Meas. Tech.HTRF Kinase Inhibition Assay
pH7.4±n/a
Temperature295.15±n/a K
Ki 4.5±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 Chem 51:3688-91 (2008) [PubMed]  Article
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Tyrosine Kinase c-Met Mutant (Y1230H)
Name:Tyrosine Kinase c-Met Mutant (Y1230H)
Synonyms:HGF/SF receptor | Met proto-oncogene tyrosine kinase | SF receptor | Scatter factor receptor | c-Met
Type:Tyrosine-protein kinase
Mol. Mass.:30550.76
Organism:Homo sapiens (Human)
Description:n/a
Residue:268
Sequence:
VHFNEVIGRGHFGCVYHGTLLDNDGKKIHCAVKSLNRITDIGEVSQFLTEGIIMKDFSHP
NVLSLLGICLRSEGSPLVVLPYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKYLAS
KKFVHRDLAARNCMLDEKFTVKVADFGLARDMHDKEYYSVHNKTGAKLPVKWMALESLQT
QKFTTKSDVWSFGVVLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYCPDPLYEVML
KCWHPKAEMRPSFSELVSRISAIFSTFI
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  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