Reaction Details |
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Target | Hepatocyte growth factor receptor [1078-1345,M1250T,L1272V] |
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Ligand | BDBM24466 |
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Substrate/Competitor | biotinylated gastrin substrate |
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Meas. Tech. | HTRF Kinase Inhibition Assay |
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pH | 7.4±n/a |
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Temperature | 295.15±n/a K |
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Ki | 4.1±n/a nM |
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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 Chem51:3688-91 (2008) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Hepatocyte growth factor receptor [1078-1345,M1250T,L1272V] |
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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
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BDBM24466 |
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biotinylated gastrin substrate |
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Name: | biotinylated gastrin substrate |
Synonyms: | n/a |
Type: | Peptide |
Mol. Mass.: | 2100.22 |
Organism: | n/a |
Description: | n/a |
Residue: | 17 |
Sequence: | |