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HTRF Kinase Inhibition Assay from Article 10.1021/jm800401t: "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)."
Assay data:8 Active, 3 Activity ≤ 1 nM, 8 Activity ≤ 1 µM, 8 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB
Assay data:3598 Active, 421 Activity ≤ 1 nM, 2233 Activity ≤ 1 µM, 3598 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Inhibition of HGF-mediated c-Met autophosphorylation in human PC3 cells after 10 mins by quantitative electrochemiluminescent immunoassay
Assay data:45 Active, 45 Activity ≤ 1 µM, 45 Tested
Inhibition of IGF1R by HTRF assay
Assay data:48 Active, 40 Activity ≤ 1 µM, 49 Tested
Inhibition of VEGFR2 by HTRF assay
Assay data:46 Active, 34 Activity ≤ 1 µM, 48 Tested
Inhibition of c-Met by HTRF assay
Assay data:49 Active, 16 Activity ≤ 1 nM, 49 Activity ≤ 1 µM, 49 Tested
Inhibition of human c-MET
Assay data:448 Active, 13 Activity ≤ 1 nM, 373 Activity ≤ 1 µM, 448 Tested
Inhibition VEGFR2-mediated survival of HUVEC
Assay data:8 Active, 8 Activity ≤ 1 µM, 8 Tested
Assay data:8 Active, 6 Activity ≤ 1 µM, 8 Tested
Inhibition of HGF-mediated c-Met phosphorylation in human PC3 cells
Inhibition of c-Met phosphorylation by HTRF assay
Assay data:7 Active, 3 Activity ≤ 1 nM, 7 Activity ≤ 1 µM, 7 Tested
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