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Assay Detail

CHEMBL5662442

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

Binding
Inhibition of VEGFR-2 phosphorylation in serum starved human HUVEC cells incubated for 1 hr by immunoblotting analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
2
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

KRN951, a highly potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, has antitumor activities and affects functional vascular properties.
Nakamura K, Taguchi E, Miura T, Yamamoto A, Takahashi K, Bichat F, Guilbaud N, Hasegawa K, Kubo K, Fujiwara Y, Suzuki R, Kubo K, Shibuya M, Isae T.
Cancer Res (2006) 66 : 9134 -9142
PubMed 16982756 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 9.80 9.80

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - MONDO:0004992
EFO_TERM EFO_TERM - cancer

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1289494 TIVOZANIB 4.0 1 9.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1289494 TIVOZANIB IC50 = 0.16 nM 9.80