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Assay Detail

CHEMBL673896

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Functional
Inhibition of VEGF-stimulated mitogenesis in human umbilical vein endothelial cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Endothelial cell
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Vascular endothelial growth factor receptor (CHEMBL2095227)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Synthesis and initial SAR studies of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines: a new class of KDR kinase inhibitors.
Fraley ME, Hoffman WF, Rubino RS, Hungate RW, Tebben AJ, Rutledge RZ, McFall RC, Huckle WR, Kendall RL, Coll KE, Thomas KA.
Bioorg Med Chem Lett (2002) 12 : 2767 -2770
PubMed 12217372 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.59 6.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL92516 1 6.90
CHEMBL329350 1 6.82
CHEMBL92461 1 6.41
CHEMBL92279 1 6.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL92516 IC50 = 127.0 nM 6.90
CHEMBL329350 IC50 = 150.0 nM 6.82
CHEMBL92461 IC50 = 387.0 nM 6.41
CHEMBL92279 IC50 = 622.0 nM 6.21