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Assay Detail

CHEMBL1040332

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

Binding
Inhibition of TPR-Met assessed as autophosphorylation
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

N-(4-(6,7-Disubstituted-quinolin-4-yloxy)-3-fluorophenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors.
Mannion M, Raeppel S, Claridge S, Zhou N, Saavedra O, Isakovic L, Zhan L, Gaudette F, Raeppel F, Déziel R, Beaulieu N, Nguyen H, Chute I, Beaulieu C, Dupont I, Robert MF, Lefebvre S, Dubay M, Rahil J, Wang J, Ste-Croix H, Robert Macleod A, Besterman JM, Vaisburg A.
Bioorg Med Chem Lett (2009) 19 : 6552 -6556
PubMed 19854051 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.69 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL574093 1 7.70
CHEMBL574050 1 7.52
CHEMBL574125 1 7.30
CHEMBL582927 1 7.10
CHEMBL575076 1 7.10
CHEMBL573761 1 7.05
CHEMBL574864 1 7.05
CHEMBL572389 1 6.89
CHEMBL575698 1 6.82
CHEMBL576752 1 6.82
CHEMBL574225 1 6.70
CHEMBL573974 1 6.62
CHEMBL577369 1 6.43
CHEMBL574406 1 6.20
CHEMBL575712 1 6.19
CHEMBL582925 1 6.07
CHEMBL573765 1 5.48
CHEMBL574230 1 5.30
CHEMBL574628 1 -
CHEMBL573768 1 -
CHEMBL575490 1 -
CHEMBL573762 1 -
CHEMBL574863 1 -
CHEMBL574870 1 -
CHEMBL576769 1 -
CHEMBL575713 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL574093 IC50 = 20.0 nM 7.70
CHEMBL574050 IC50 = 30.0 nM 7.52
CHEMBL574125 IC50 = 50.0 nM 7.30
CHEMBL582927 IC50 = 80.0 nM 7.10
CHEMBL575076 IC50 = 80.0 nM 7.10
CHEMBL573761 IC50 = 90.0 nM 7.05
CHEMBL574864 IC50 = 90.0 nM 7.05
CHEMBL572389 IC50 = 130.0 nM 6.89
CHEMBL575698 IC50 = 150.0 nM 6.82
CHEMBL576752 IC50 = 150.0 nM 6.82
CHEMBL574225 IC50 = 200.0 nM 6.70
CHEMBL573974 IC50 = 240.0 nM 6.62
CHEMBL577369 IC50 = 370.0 nM 6.43
CHEMBL574406 IC50 = 630.0 nM 6.20
CHEMBL575712 IC50 = 640.0 nM 6.19
CHEMBL582925 IC50 = 860.0 nM 6.07
CHEMBL573765 IC50 = 3300.0 nM 5.48
CHEMBL574230 IC50 = 5000.0 nM 5.30
CHEMBL574628 IC50 - -
CHEMBL573768 IC50 - -
CHEMBL575490 IC50 - -
CHEMBL573762 IC50 - -
CHEMBL574863 IC50 > 10000.0 nM -
CHEMBL574870 IC50 > 1000.0 nM -
CHEMBL576769 IC50 > 10000.0 nM -
CHEMBL575713 IC50 > 10000.0 nM -