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Assay Detail

CHEMBL981082

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

Binding
Inhibition of VEGF-induced VEGFR2 phosphorylation in HUVEC
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor.
Harris PA, Boloor A, Cheung M, Kumar R, Crosby RM, Davis-Ward RG, Epperly AH, Hinkle KW, Hunter RN, Johnson JH, Knick VB, Laudeman CP, Luttrell DK, Mook RA, Nolte RT, Rudolph SK, Szewczyk JR, Truesdale AT, Veal JM, Wang L, Stafford JA.
J Med Chem (2008) 51 : 4632 -4640
PubMed 18620382 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.10 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL477772 PAZOPANIB 4.0 1 8.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL477772 PAZOPANIB IC50 = 8.0 nM 8.10