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Assay Detail

CHEMBL4432495

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Binding
Inhibition of c-Met (unknown origin)
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Hepatocyte growth factor receptor (CHEMBL3717)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of c-Met kinase inhibitors bearing 2-oxo-1,2-dihydroquinoline scaffold.
Cui H, Peng X, Liu J, Ma C, Ji Y, Zhang W, Geng M, Li Y.
Bioorg Med Chem Lett (2016) 26 : 4483 -4486
PubMed 27524312 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.04 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1230609 FORETINIB 2.0 1 9.40
CHEMBL460702 BMS-777607 2.0 1 8.41
CHEMBL601719 CRIZOTINIB 4.0 1 7.96
CHEMBL4514997 1 7.85
CHEMBL3989914 GLESATINIB 2.0 1 7.54
CHEMBL404881 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1230609 FORETINIB IC50 = 0.4 nM 9.40
CHEMBL460702 BMS-777607 IC50 = 3.9 nM 8.41
CHEMBL601719 CRIZOTINIB IC50 = 11.0 nM 7.96
CHEMBL4514997 IC50 = 14.0 nM 7.85
CHEMBL3989914 GLESATINIB IC50 = 29.0 nM 7.54
CHEMBL404881 IC50 = 80.0 nM 7.10