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Assay Detail

CHEMBL2183649

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

Binding
Inhibition of VEGFR2
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel 3-Azaindolyl-4-arylmaleimides exhibiting potent antiangiogenic efficacy, protein kinase inhibition, and antiproliferative activity.
Ganser C, Lauermann E, Maderer A, Stauder T, Kramb JP, Plutizki S, Kindler T, Moehler M, Dannhardt G.
J Med Chem (2012) 55 : 9531 -9540
PubMed 23088521 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.91 7.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2180878 1 7.43
CHEMBL2180882 1 7.32
CHEMBL201511 MALEIMIDE 1 7.16
CHEMBL2180881 1 6.43
CHEMBL2177142 1 6.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2180878 IC50 = 37.0 nM 7.43
CHEMBL2180882 IC50 = 48.0 nM 7.32
CHEMBL201511 MALEIMIDE IC50 = 70.0 nM 7.16
CHEMBL2180881 IC50 = 373.0 nM 6.43
CHEMBL2177142 IC50 = 590.0 nM 6.23