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Assay Detail

CHEMBL3404456

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Binding
Inhibition of c-Met kinase in human A549 cells assessed as inhibition of phosphorylation after 45 mins by electrochemiluminescence assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A549
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors.
Dorsch D, Schadt O, Stieber F, Meyring M, Grädler U, Bladt F, Friese-Hamim M, Knühl C, Pehl U, Blaukat A.
Bioorg Med Chem Lett (2015) 25 : 1597 -1602
PubMed 25736998 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.20 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3402762 TEPOTINIB 4.0 1 7.92
CHEMBL3402760 1 7.82
CHEMBL3402756 1 7.82
CHEMBL3402758 1 7.55
CHEMBL3402761 1 7.47
CHEMBL3402742 1 7.11
CHEMBL3402757 1 6.85
CHEMBL3402743 1 6.82
CHEMBL3402759 1 6.70
CHEMBL3402741 1 5.96
CHEMBL3402754 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3402762 TEPOTINIB IC50 = 12.0 nM 7.92
CHEMBL3402760 IC50 = 15.0 nM 7.82
CHEMBL3402756 IC50 = 15.0 nM 7.82
CHEMBL3402758 IC50 = 28.0 nM 7.55
CHEMBL3402761 IC50 = 34.0 nM 7.47
CHEMBL3402742 IC50 = 78.0 nM 7.11
CHEMBL3402757 IC50 = 140.0 nM 6.85
CHEMBL3402743 IC50 = 150.0 nM 6.82
CHEMBL3402759 IC50 = 200.0 nM 6.70
CHEMBL3402741 IC50 = 1100.0 nM 5.96
CHEMBL3402754 IC50 > 1.0 nM -