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Assay Detail

CHEMBL3136337

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

Binding
Inhibition of VEGFR2 (unknown origin) after 1 hr by Caliper mobility shift assay
9
Total Activities
9
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

Design and discovery of 4-anilinoquinazoline ureas as multikinase inhibitors targeting BRAF, VEGFR-2 and EGFR
Zhang Q, Diao Y, Wang F, Fu Y, Tang F, You Q, Zhou H
Medchemcomm (2013) 4 : 979 -986
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.71 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3133751 1 7.77
CHEMBL1336 SORAFENIB 4.0 1 7.28
CHEMBL3133756 1 7.12
CHEMBL3133757 1 7.04
CHEMBL3133758 1 7.02
CHEMBL3133752 1 6.67
CHEMBL3133755 1 5.67
CHEMBL3133754 1 5.07
CHEMBL3133753 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3133751 IC50 = 17.0 nM 7.77
CHEMBL1336 SORAFENIB IC50 = 52.0 nM 7.28
CHEMBL3133756 IC50 = 75.0 nM 7.12
CHEMBL3133757 IC50 = 91.0 nM 7.04
CHEMBL3133758 IC50 = 95.0 nM 7.02
CHEMBL3133752 IC50 = 213.0 nM 6.67
CHEMBL3133755 IC50 = 2165.0 nM 5.67
CHEMBL3133754 IC50 = 8568.0 nM 5.07
CHEMBL3133753 IC50 > 10000.0 nM -