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Assay Detail

CHEMBL5647702

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

Binding
Inhibition of VEGFR2 (unknown origin) using gastrin peptide as substrate and ATP concentration two-thirds of Km by HTRF assay
1
Total Activities
1
Compounds Tested
1
Activity Types
6
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

AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts.
Polverino A, Coxon A, Starnes C, Diaz Z, DeMelfi T, Wang L, Bready J, Estrada J, Cattley R, Kaufman S, Chen D, Gan Y, Kumar G, Meyer J, Neervannan S, Alva G, Talvenheimo J, Montestruque S, Tasker A, Patel V, Radinsky R, Kendall R.
Cancer Res (2006) 66 : 8715 -8721
PubMed 16951187 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.52 8.52

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - MONDO:0004992
EFO_ID EFO_ID - MONDO:0011719
EFO_ID EFO_ID - EFO:0000756
EFO_TERM EFO_TERM - cancer
EFO_TERM EFO_TERM - gastrointestinal stromal tumor
EFO_TERM EFO_TERM - melanoma

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL572881 MOTESANIB 3.0 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL572881 MOTESANIB IC50 = 3.0 nM 8.52