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Target
Hepatocyte growth factor receptor [1078-1345,Y1230H,L1272V]
Ligand
BDBM24466
Substrate
biotinylated gastrin substrate
Meas. Tech.
HTRF Kinase Inhibition Assay
pH
7.4±n/a
Temperature
295.15±n/a K
Ki
4.5±n/a nM
Citation
 Liu, L; Siegmund, A; Xi, N; Kaplan-Lefko, P; Rex, K; Chen, A; Lin, J; Moriguchi, J; Berry, L; Huang, L; Teffera, Y; Yang, Y; Zhang, Y; Bellon, SF; Lee, M; Shimanovich, R; Bak, A; Dominguez, C; Norman, MH; Harmange, JC; Dussault, I; Kim, 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 
Target
Name:
Hepatocyte growth factor receptor [1078-1345,Y1230H,L1272V]
Synonyms:
HGF/SF receptor | MET | MET_HUMAN | Met proto-oncogene tyrosine kinase | SF receptor | Scatter factor receptor | Tyrosine Kinase c-Met Mutant (Y1230H) | c-Met
Type:
Tyrosine-protein kinase
Mol. Mass.:
30550.76
Organism:
Homo sapiens (Human)
Description:
P08581[1078-1345,Y1230H,L1272V]
Residue:
268
Sequence:
VHFNEVIGRGHFGCVYHGTLLDNDGKKIHCAVKSLNRITDIGEVSQFLTEGIIMKDFSHPNVLSLLGICLRSEGSPLVVLPYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKYLASKKFVHRDLAARNCMLDEKFTVKVADFGLARDMHDKEYYSVHNKTGAKLPVKWMALESLQTQKFTTKSDVWSFGVVLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYCPDPLYEVMLKCWHPKAEMRPSFSELVSRISAIFSTFI
  
Inhibitor
Name:
BDBM24466
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
Type:
Small organic molecule
Emp. Form.:
C30H29N5O5
Mol. Mass.:
539.5818
SMILES:
COc1ccc2c(Oc3ccc(NC(=O)c4c(C)n(CC(C)(C)O)n(-c5ccccc5)c4=O)nc3)ccnc2c1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
biotinylated gastrin substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2100.22
Organism:
n/a
Description:
n/a
Residue:
17
Sequence:
ITINYLEEEEAYGWLDF