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Assay Detail

CHEMBL1119652

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

Binding
Inhibition of VEGFR1 at 3 uM
2
Total Activities
2
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 1 (CHEMBL1868)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

8-THP-DHI analogs as potent Type I dual TIE-2/VEGF-R2 receptor tyrosine kinase inhibitors.
Hudkins RL, Zulli AL, Underiner TL, Angeles TS, Aimone LD, Meyer SL, Pauletti D, Chang H, Fedorov EV, Almo SC, Fedorov AA, Ruggeri BA.
Bioorg Med Chem Lett (2010) 20 : 3356 -3360
PubMed 20430619 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.68 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1084337 1 7.80
CHEMBL1082829 1 7.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1084337 IC50 = 16.0 nM 7.80
CHEMBL1082829 IC50 = 28.0 nM 7.55