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Assay Detail

CHEMBL2020643

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

Binding
Inhibition of recombinant human VEGFR-2 using poly(Glu4/Tyr) and [gamma32P]ATP as substrate after 1 hr by scintillation counting
65
Total Activities
65
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Vascular endothelial growth factor receptor 2 (CHEMBL279)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of (aryloxy)quinazoline ureas as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors.
Garofalo A, Farce A, Ravez S, Lemoine A, Six P, Chavatte P, Goossens L, Depreux P.
J Med Chem (2012) 55 : 1189 -1204
PubMed 22229669 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 65 5.88 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2018886 1 8.70
CHEMBL2018884 1 8.40
CHEMBL2018885 1 8.22
CHEMBL2018882 1 8.22
CHEMBL1761942 1 7.52
CHEMBL2018883 1 7.40
CHEMBL2018881 1 7.40
CHEMBL1761939 1 7.40
CHEMBL1761937 1 7.30
CHEMBL1277162 1 7.22
CHEMBL179603 1 7.16
CHEMBL1761938 1 7.05
CHEMBL1761936 1 6.40
CHEMBL2018752 1 6.30
CHEMBL1277254 1 6.22
CHEMBL1278149 1 6.22
CHEMBL1761932 1 6.22
CHEMBL1277253 1 6.22
CHEMBL2018756 1 6.19
CHEMBL1761930 1 6.16
CHEMBL328106 1 6.10
CHEMBL2018757 1 6.07
CHEMBL2018755 1 6.07
CHEMBL2018766 1 6.00
CHEMBL205089 1 6.00
CHEMBL1277620 1 5.78
CHEMBL2018753 1 5.48
CHEMBL2018769 1 5.47
CHEMBL2018771 1 5.43
CHEMBL2018746 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2018886 IC50 = 2.0 nM 8.70
CHEMBL2018884 IC50 = 4.0 nM 8.40
CHEMBL2018882 IC50 = 6.0 nM 8.22
CHEMBL2018885 IC50 = 6.0 nM 8.22
CHEMBL1761942 IC50 = 30.0 nM 7.52
CHEMBL2018883 IC50 = 40.0 nM 7.40
CHEMBL2018881 IC50 = 40.0 nM 7.40
CHEMBL1761939 IC50 = 40.0 nM 7.40
CHEMBL1761937 IC50 = 50.0 nM 7.30
CHEMBL1277162 IC50 = 60.0 nM 7.22
CHEMBL179603 IC50 = 70.0 nM 7.16
CHEMBL1761938 IC50 = 90.0 nM 7.05
CHEMBL1761936 IC50 = 400.0 nM 6.40
CHEMBL2018752 IC50 = 500.0 nM 6.30
CHEMBL1277253 IC50 = 600.0 nM 6.22
CHEMBL1278149 IC50 = 600.0 nM 6.22
CHEMBL1761932 IC50 = 600.0 nM 6.22
CHEMBL1277254 IC50 = 600.0 nM 6.22
CHEMBL2018756 IC50 = 650.0 nM 6.19
CHEMBL1761930 IC50 = 700.0 nM 6.16
CHEMBL328106 IC50 = 800.0 nM 6.10
CHEMBL2018757 IC50 = 850.0 nM 6.07
CHEMBL2018755 IC50 = 850.0 nM 6.07
CHEMBL2018766 IC50 = 1000.0 nM 6.00
CHEMBL205089 IC50 = 1000.0 nM 6.00
CHEMBL1277620 IC50 = 1650.0 nM 5.78
CHEMBL2018753 IC50 = 3300.0 nM 5.48
CHEMBL2018769 IC50 = 3350.0 nM 5.47
CHEMBL2018771 IC50 = 3700.0 nM 5.43
CHEMBL2018746 IC50 = 4000.0 nM 5.40
CHEMBL1761944 IC50 = 4300.0 nM 5.37
CHEMBL2016600 IC50 = 4650.0 nM 5.33
CHEMBL2018777 IC50 = 4800.0 nM 5.32
CHEMBL2018754 IC50 = 4900.0 nM 5.31
CHEMBL2018750 IC50 = 5050.0 nM 5.30
CHEMBL2018748 IC50 = 5000.0 nM 5.30
CHEMBL2018751 IC50 = 5050.0 nM 5.30
CHEMBL1761933 IC50 = 5100.0 nM 5.29
CHEMBL2018768 IC50 = 5200.0 nM 5.28
CHEMBL2018759 IC50 = 5250.0 nM 5.28
CHEMBL2018758 IC50 = 5200.0 nM 5.28
CHEMBL2018775 IC50 = 5300.0 nM 5.28
CHEMBL301018 IC50 = 5300.0 nM 5.28
CHEMBL2018760 IC50 = 5550.0 nM 5.26
CHEMBL1761931 IC50 = 5600.0 nM 5.25
CHEMBL2018879 IC50 = 5700.0 nM 5.24
CHEMBL1761929 IC50 = 5800.0 nM 5.24
CHEMBL2018763 IC50 = 5800.0 nM 5.24
CHEMBL2018764 IC50 = 6200.0 nM 5.21
CHEMBL2018767 IC50 = 6450.0 nM 5.19