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Assay Detail

CHEMBL3857917

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of NH2-terminal His-tagged MET kinase domain (1051 to 1348 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells preincubated for 60 mins followed by (poly(Glu, Tyr) 4:1) substrate addition for 2 to 4 hrs by luciferase-coupled chemiluminescence assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

The "Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.
Talele TT.
J Med Chem (2016) 59 : 8712 -8756
PubMed 27299736 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 9.40 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1230609 FORETINIB 2.0 1 9.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1230609 FORETINIB IC50 = 0.4 nM 9.40