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Assay Detail

CHEMBL960944

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

Binding
Inhibition of TPR-fused Met phosphorylation expressed in human 293T cells by ELISA
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type 293T
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

N-(3-fluoro-4-(2-arylthieno[3,2-b]pyridin-7-yloxy)phenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors.
Raeppel S, Claridge S, Saavedra O, Gaudette F, Zhan L, Mannion M, Zhou N, Raeppel F, Granger MC, Isakovic L, Déziel R, Nguyen H, Beaulieu N, Beaulieu C, Dupont I, Robert MF, Lefebvre S, Dubay M, Rahil J, Wang J, Ste-Croix H, Robert Macleod A, Besterman J, Vaisburg A.
Bioorg Med Chem Lett (2009) 19 : 1323 -1328
PubMed 19211249 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.75 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL453613 1 7.40
CHEMBL254760 1 7.30
CHEMBL464211 1 7.30
CHEMBL445871 1 7.22
CHEMBL462835 1 7.22
CHEMBL465131 1 7.22
CHEMBL518676 1 7.10
CHEMBL503016 1 7.10
CHEMBL517469 1 7.00
CHEMBL462232 1 6.92
CHEMBL510676 1 6.92
CHEMBL455655 1 6.85
CHEMBL465130 1 6.80
CHEMBL459478 1 6.68
CHEMBL502621 1 6.64
CHEMBL447616 1 6.60
CHEMBL448993 1 6.57
CHEMBL449757 1 6.52
CHEMBL508776 1 6.52
CHEMBL464510 1 6.51
CHEMBL503524 1 6.50
CHEMBL518209 1 6.43
CHEMBL448276 1 6.38
CHEMBL508395 1 6.08
CHEMBL462231 1 6.00
CHEMBL462667 1 5.84
CHEMBL464409 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL453613 IC50 = 40.0 nM 7.40
CHEMBL254760 IC50 = 50.0 nM 7.30
CHEMBL464211 IC50 = 50.0 nM 7.30
CHEMBL445871 IC50 = 60.0 nM 7.22
CHEMBL462835 IC50 = 60.0 nM 7.22
CHEMBL465131 IC50 = 60.0 nM 7.22
CHEMBL518676 IC50 = 80.0 nM 7.10
CHEMBL503016 IC50 = 80.0 nM 7.10
CHEMBL517469 IC50 = 100.0 nM 7.00
CHEMBL462232 IC50 = 120.0 nM 6.92
CHEMBL510676 IC50 = 120.0 nM 6.92
CHEMBL455655 IC50 = 140.0 nM 6.85
CHEMBL465130 IC50 = 160.0 nM 6.80
CHEMBL459478 IC50 = 210.0 nM 6.68
CHEMBL502621 IC50 = 230.0 nM 6.64
CHEMBL447616 IC50 = 250.0 nM 6.60
CHEMBL448993 IC50 = 270.0 nM 6.57
CHEMBL449757 IC50 = 300.0 nM 6.52
CHEMBL508776 IC50 = 300.0 nM 6.52
CHEMBL464510 IC50 = 310.0 nM 6.51
CHEMBL503524 IC50 = 320.0 nM 6.50
CHEMBL518209 IC50 = 370.0 nM 6.43
CHEMBL448276 IC50 = 420.0 nM 6.38
CHEMBL508395 IC50 = 830.0 nM 6.08
CHEMBL462231 IC50 = 1000.0 nM 6.00
CHEMBL462667 IC50 = 1440.0 nM 5.84
CHEMBL464409 IC50 > 10000.0 nM -