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Assay Detail

CHEMBL1067993

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

Binding
Inhibition of recombinant GST-fused c-Met expressed in baculovirus infected high five cells by DELFIA
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Identification of potent and selective VEGFR receptor tyrosine kinase inhibitors having new amide isostere headgroups.
Gaudette F, Raeppel S, Nguyen H, Beaulieu N, Beaulieu C, Dupont I, Macleod AR, Besterman JM, Vaisburg A.
Bioorg Med Chem Lett (2010) 20 : 848 -852
PubMed 20071170 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.68 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL464510 1 7.52
CHEMBL465130 1 7.40
CHEMBL602704 1 7.05
CHEMBL602703 1 6.92
CHEMBL602905 1 6.75
CHEMBL600603 1 6.17
CHEMBL600632 1 6.16
CHEMBL591924 1 6.08
CHEMBL600604 1 6.04
CHEMBL600398 1 -
CHEMBL603082 1 -
CHEMBL612137 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL464510 IC50 = 30.0 nM 7.52
CHEMBL465130 IC50 = 40.0 nM 7.40
CHEMBL602704 IC50 = 90.0 nM 7.05
CHEMBL602703 IC50 = 120.0 nM 6.92
CHEMBL602905 IC50 = 180.0 nM 6.75
CHEMBL600603 IC50 = 680.0 nM 6.17
CHEMBL600632 IC50 = 700.0 nM 6.16
CHEMBL591924 IC50 = 840.0 nM 6.08
CHEMBL600604 IC50 = 910.0 nM 6.04
CHEMBL600398 IC50 > 5000.0 nM -
CHEMBL603082 IC50 > 5000.0 nM -
CHEMBL612137 IC50 > 5000.0 nM -