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Assay Detail

CHEMBL834791

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Functional
Inhibitory concentration against Human umbilical vein endothelial cells stimulated by VEGF was determined
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Cell line
Confidence 1 — Organism
Curated By Intermediate

Target

Cell line (CHEMBL614840)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors.
Borzilleri RM, Cai ZW, Ellis C, Fargnoli J, Fura A, Gerhardt T, Goyal B, Hunt JT, Mortillo S, Qian L, Tokarski J, Vyas V, Wautlet B, Zheng X, Bhide RS.
Bioorg Med Chem Lett (2005) 15 : 1429 -1433
PubMed 15713401 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.19 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL178607 1 9.00
CHEMBL369322 1 9.00
CHEMBL180978 1 8.52
CHEMBL360769 1 8.40
CHEMBL360118 1 8.30
CHEMBL359652 1 8.22
CHEMBL179517 1 8.10
CHEMBL178583 1 8.00
CHEMBL180603 1 7.70
CHEMBL360450 1 7.46
CHEMBL178596 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL178607 IC50 = 1.0 nM 9.00
CHEMBL369322 IC50 = 1.0 nM 9.00
CHEMBL180978 IC50 = 3.0 nM 8.52
CHEMBL360769 IC50 = 4.0 nM 8.40
CHEMBL360118 IC50 = 5.0 nM 8.30
CHEMBL359652 IC50 = 6.0 nM 8.22
CHEMBL179517 IC50 = 8.0 nM 8.10
CHEMBL178583 IC50 = 10.0 nM 8.00
CHEMBL180603 IC50 = 20.0 nM 7.70
CHEMBL360450 IC50 = 35.0 nM 7.46
CHEMBL178596 IC50 = 40.0 nM 7.40