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Assay Detail

CHEMBL4839229

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Binding
Inhibition of VEGFR1 (unknown origin)
5
Total Activities
5
Compounds Tested
1
Activity Types
0
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 1 (CHEMBL1868)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery, Synthesis, and Evaluation of Highly Selective Vascular Endothelial Growth Factor Receptor 3 (VEGFR3) Inhibitor for the Potential Treatment of Metastatic Triple-Negative Breast Cancer.
Li Y, Yang G, Zhang J, Tang P, Yang C, Wang G, Chen J, Liu J, Zhang L, Ouyang L.
J Med Chem (2021) 64 : 12022 -12048
PubMed 34351741 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.16 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL572881 MOTESANIB 3.0 1 8.70
CHEMBL491473 CEDIRANIB 3.0 1 8.30
CHEMBL2220486 LUCITANIB 2.0 1 8.15
CHEMBL477772 PAZOPANIB 4.0 1 8.00
CHEMBL1289601 LENVATINIB 4.0 1 7.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL572881 MOTESANIB IC50 = 2.0 nM 8.70
CHEMBL491473 CEDIRANIB IC50 = 5.0 nM 8.30
CHEMBL2220486 LUCITANIB IC50 = 7.0 nM 8.15
CHEMBL477772 PAZOPANIB IC50 = 10.0 nM 8.00
CHEMBL1289601 LENVATINIB IC50 = 22.0 nM 7.66