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Assay Detail

CHEMBL1040331

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

Binding
Inhibition of GST-tagged VEGFR expressed in Sf9 cells
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Sf9
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 32 7.13 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL489326 EXELIXIS 1 8.15
CHEMBL462232 1 8.10
CHEMBL573761 1 8.00
CHEMBL574225 1 7.82
CHEMBL577369 1 7.70
CHEMBL574864 1 7.70
CHEMBL575713 1 7.70
CHEMBL582927 1 7.70
CHEMBL572389 1 7.70
CHEMBL254760 1 7.58
CHEMBL574870 1 7.52
CHEMBL574125 1 7.52
CHEMBL576752 1 7.52
CHEMBL573974 1 7.52
CHEMBL575698 1 7.52
CHEMBL404881 1 7.50
CHEMBL574093 1 7.40
CHEMBL576769 1 7.30
CHEMBL575076 1 7.00
CHEMBL574050 1 6.92
CHEMBL535 SUNITINIB 4.0 1 6.73
CHEMBL582925 1 6.68
CHEMBL573768 1 6.64
CHEMBL575712 1 6.43
CHEMBL574406 1 6.22
CHEMBL574628 1 6.20
CHEMBL450786 PHA-665752 1 6.06
CHEMBL574230 1 5.89
CHEMBL573762 1 5.85
CHEMBL575490 1 5.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL489326 EXELIXIS IC50 = 7.0 nM 8.15
CHEMBL462232 IC50 = 8.0 nM 8.10
CHEMBL573761 IC50 = 10.0 nM 8.00
CHEMBL574225 IC50 = 15.0 nM 7.82
CHEMBL577369 IC50 = 20.0 nM 7.70
CHEMBL574864 IC50 = 20.0 nM 7.70
CHEMBL575713 IC50 = 20.0 nM 7.70
CHEMBL582927 IC50 = 20.0 nM 7.70
CHEMBL572389 IC50 = 20.0 nM 7.70
CHEMBL254760 IC50 = 26.0 nM 7.58
CHEMBL574870 IC50 = 30.0 nM 7.52
CHEMBL574125 IC50 = 30.0 nM 7.52
CHEMBL576752 IC50 = 30.0 nM 7.52
CHEMBL573974 IC50 = 30.0 nM 7.52
CHEMBL575698 IC50 = 30.0 nM 7.52
CHEMBL404881 IC50 = 32.0 nM 7.50
CHEMBL574093 IC50 = 40.0 nM 7.40
CHEMBL576769 IC50 = 50.0 nM 7.30
CHEMBL575076 IC50 = 100.0 nM 7.00
CHEMBL574050 IC50 = 120.0 nM 6.92
CHEMBL535 SUNITINIB IC50 = 185.0 nM 6.73
CHEMBL582925 IC50 = 210.0 nM 6.68
CHEMBL573768 IC50 = 230.0 nM 6.64
CHEMBL575712 IC50 = 370.0 nM 6.43
CHEMBL574406 IC50 = 600.0 nM 6.22
CHEMBL574628 IC50 = 630.0 nM 6.20
CHEMBL450786 PHA-665752 IC50 = 863.0 nM 6.06
CHEMBL574230 IC50 = 1300.0 nM 5.89
CHEMBL573762 IC50 = 1400.0 nM 5.85
CHEMBL575490 IC50 = 5900.0 nM 5.23
CHEMBL573765 IC50 > 2000.0 nM -
CHEMBL574863 IC50 > 2000.0 nM -