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Assay Detail

CHEMBL830878

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Binding
Inhibitory concentration against Vascular endothelial growth factor receptor 2
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Vascular endothelial growth factor receptor 2 (CHEMBL279)
Type SINGLE PROTEIN
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 21 7.46 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL359652 1 8.52
CHEMBL369322 1 8.40
CHEMBL360118 1 8.30
CHEMBL178607 1 8.30
CHEMBL178174 1 8.15
CHEMBL178789 1 8.00
CHEMBL360769 1 7.85
CHEMBL179517 1 7.75
CHEMBL180603 1 7.52
CHEMBL360503 1 7.48
CHEMBL178583 1 7.40
CHEMBL180978 1 7.28
CHEMBL178248 1 7.26
CHEMBL181567 1 7.21
CHEMBL178596 1 7.19
CHEMBL360450 1 7.05
CHEMBL180807 1 6.82
CHEMBL181122 1 6.72
CHEMBL181636 1 6.51
CHEMBL178899 1 6.43
CHEMBL359507 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL359652 IC50 = 3.0 nM 8.52
CHEMBL369322 IC50 = 4.0 nM 8.40
CHEMBL360118 IC50 = 5.0 nM 8.30
CHEMBL178607 IC50 = 5.0 nM 8.30
CHEMBL178174 IC50 = 7.0 nM 8.15
CHEMBL178789 IC50 = 10.0 nM 8.00
CHEMBL360769 IC50 = 14.0 nM 7.85
CHEMBL179517 IC50 = 18.0 nM 7.75
CHEMBL180603 IC50 = 30.0 nM 7.52
CHEMBL360503 IC50 = 33.0 nM 7.48
CHEMBL178583 IC50 = 40.0 nM 7.40
CHEMBL180978 IC50 = 52.0 nM 7.28
CHEMBL178248 IC50 = 55.0 nM 7.26
CHEMBL181567 IC50 = 61.0 nM 7.21
CHEMBL178596 IC50 = 64.0 nM 7.19
CHEMBL360450 IC50 = 90.0 nM 7.05
CHEMBL180807 IC50 = 150.0 nM 6.82
CHEMBL181122 IC50 = 190.0 nM 6.72
CHEMBL181636 IC50 = 310.0 nM 6.51
CHEMBL178899 IC50 = 370.0 nM 6.43
CHEMBL359507 IC50 = 380.0 nM 6.42