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Assay Detail

CHEMBL816967

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Binding
Inhibitory activity against Vascular endothelial growth factor receptor 2
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Vascular endothelial growth factor receptor 2 (CHEMBL279)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases.
Sun L, Tran N, Liang C, Tang F, Rice A, Schreck R, Waltz K, Shawver LK, McMahon G, Tang C.
J Med Chem (1999) 42 : 5120 -5130
PubMed 10602697 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.18 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL89363 1 7.70
CHEMBL149073 1 7.16
CHEMBL148514 1 7.05
CHEMBL149201 1 6.85
CHEMBL147761 1 6.70
CHEMBL435227 1 6.62
CHEMBL347074 1 6.52
CHEMBL358728 1 6.52
CHEMBL148744 1 6.46
CHEMBL148984 1 6.35
CHEMBL150151 1 6.28
CHEMBL276711 SEMAXANIB 3.0 1 6.16
CHEMBL146697 1 6.04
CHEMBL443296 1 6.00
CHEMBL150177 1 5.90
CHEMBL149243 1 5.87
CHEMBL147112 1 5.83
CHEMBL357803 1 5.76
CHEMBL344319 1 5.67
CHEMBL274654 ORANTINIB 3.0 1 5.61
CHEMBL146694 1 5.36
CHEMBL356245 1 5.08
CHEMBL450622 1 4.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL89363 IC50 = 20.0 nM 7.70
CHEMBL149073 IC50 = 70.0 nM 7.16
CHEMBL148514 IC50 = 90.0 nM 7.05
CHEMBL149201 IC50 = 140.0 nM 6.85
CHEMBL147761 IC50 = 200.0 nM 6.70
CHEMBL435227 IC50 = 240.0 nM 6.62
CHEMBL347074 IC50 = 300.0 nM 6.52
CHEMBL358728 IC50 = 300.0 nM 6.52
CHEMBL148744 IC50 = 350.0 nM 6.46
CHEMBL148984 IC50 = 450.0 nM 6.35
CHEMBL150151 IC50 = 520.0 nM 6.28
CHEMBL276711 SEMAXANIB IC50 = 700.0 nM 6.16
CHEMBL146697 IC50 = 920.0 nM 6.04
CHEMBL443296 IC50 = 1000.0 nM 6.00
CHEMBL150177 IC50 = 1260.0 nM 5.90
CHEMBL149243 IC50 = 1350.0 nM 5.87
CHEMBL147112 IC50 = 1470.0 nM 5.83
CHEMBL357803 IC50 = 1730.0 nM 5.76
CHEMBL344319 IC50 = 2140.0 nM 5.67
CHEMBL274654 ORANTINIB IC50 = 2430.0 nM 5.61
CHEMBL146694 IC50 = 4370.0 nM 5.36
CHEMBL356245 IC50 = 8290.0 nM 5.08
CHEMBL450622 IC50 = 28300.0 nM 4.55