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Assay Detail

CHEMBL1250684

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

Binding
Inhibition of His-tagged human VEGFR2 expressed in Sf9 cells
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

N-phenyl-N'-[4-(5H-pyrrolo[3,2-d]pyrimidin-4-yloxy)phenyl]ureas as novel inhibitors of VEGFR and FGFR kinases.
Oguro Y, Miyamoto N, Takagi T, Okada K, Awazu Y, Miki H, Hori A, Kamiyama K, Imamura S.
Bioorg Med Chem (2010) 18 : 7150 -7163
PubMed 20833551 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 7.84 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1254193 1 8.57
CHEMBL1253837 1 8.57
CHEMBL1254277 1 8.54
CHEMBL1254190 1 8.43
CHEMBL1254278 1 8.42
CHEMBL1253916 1 8.40
CHEMBL1254355 1 8.40
CHEMBL1254356 1 8.12
CHEMBL1253194 1 8.05
CHEMBL1253838 1 8.05
CHEMBL1254515 1 8.03
CHEMBL1254755 1 8.03
CHEMBL1255098 1 8.01
CHEMBL1255097 1 7.96
CHEMBL1254839 1 7.92
CHEMBL1253917 1 7.85
CHEMBL1254006 1 7.75
CHEMBL1254671 1 7.72
CHEMBL1254437 1 7.72
CHEMBL1254840 1 7.70
CHEMBL1255013 1 7.64
CHEMBL1254927 1 7.22
CHEMBL1254595 1 7.21
CHEMBL1254097 1 6.68
CHEMBL1254098 1 6.64
CHEMBL1254192 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1254193 IC50 = 2.7 nM 8.57
CHEMBL1253837 IC50 = 2.7 nM 8.57
CHEMBL1254277 IC50 = 2.9 nM 8.54
CHEMBL1254190 IC50 = 3.7 nM 8.43
CHEMBL1254278 IC50 = 3.8 nM 8.42
CHEMBL1253916 IC50 = 4.0 nM 8.40
CHEMBL1254355 IC50 = 4.0 nM 8.40
CHEMBL1254356 IC50 = 7.6 nM 8.12
CHEMBL1253194 IC50 = 8.9 nM 8.05
CHEMBL1253838 IC50 = 9.0 nM 8.05
CHEMBL1254515 IC50 = 9.4 nM 8.03
CHEMBL1254755 IC50 = 9.3 nM 8.03
CHEMBL1255098 IC50 = 9.7 nM 8.01
CHEMBL1255097 IC50 = 11.0 nM 7.96
CHEMBL1254839 IC50 = 12.0 nM 7.92
CHEMBL1253917 IC50 = 14.0 nM 7.85
CHEMBL1254006 IC50 = 18.0 nM 7.75
CHEMBL1254671 IC50 = 19.0 nM 7.72
CHEMBL1254437 IC50 = 19.0 nM 7.72
CHEMBL1254840 IC50 = 20.0 nM 7.70
CHEMBL1255013 IC50 = 23.0 nM 7.64
CHEMBL1254927 IC50 = 60.0 nM 7.22
CHEMBL1254595 IC50 = 61.0 nM 7.21
CHEMBL1254097 IC50 = 210.0 nM 6.68
CHEMBL1254098 IC50 = 230.0 nM 6.64
CHEMBL1254192 IC50 = 650.0 nM 6.19