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Assay Detail

CHEMBL818398

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Concentration required to achieve 50% inhibition of tyrosine phosphorylation on murine VEGF receptor (FLK-1 RTK).
54
Total Activities
54
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 1 (CHEMBL3516)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases.
Sun L, Tran N, Tang F, App H, Hirth P, McMahon G, Tang C.
J Med Chem (1998) 41 : 2588 -2603
PubMed 9651163 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 54 5.50 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL86943 1 7.16
CHEMBL313433 1 6.85
CHEMBL316008 1 6.75
CHEMBL89483 1 6.52
CHEMBL86755 1 6.41
CHEMBL89363 1 6.40
CHEMBL328710 1 6.10
CHEMBL330321 1 6.00
CHEMBL276711 SEMAXANIB 3.0 1 5.98
CHEMBL315546 1 5.80
CHEMBL90277 1 5.68
CHEMBL89721 1 5.63
CHEMBL89040 1 5.60
CHEMBL86480 1 5.60
CHEMBL313578 1 5.57
CHEMBL316020 1 5.57
CHEMBL314217 1 5.52
CHEMBL89809 1 5.52
CHEMBL431025 1 5.52
CHEMBL314146 1 5.47
CHEMBL421548 1 5.39
CHEMBL89723 1 5.37
CHEMBL315701 1 5.35
CHEMBL329367 1 5.34
CHEMBL48760 1 5.28
CHEMBL316009 1 5.20
CHEMBL87402 1 5.13
CHEMBL87810 1 5.12
CHEMBL89505 1 5.08
CHEMBL85021 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL86943 IC50 = 70.0 nM 7.16
CHEMBL313433 IC50 = 140.0 nM 6.85
CHEMBL316008 IC50 = 180.0 nM 6.75
CHEMBL89483 IC50 = 300.0 nM 6.52
CHEMBL86755 IC50 = 390.0 nM 6.41
CHEMBL89363 IC50 = 400.0 nM 6.40
CHEMBL328710 IC50 = 800.0 nM 6.10
CHEMBL330321 IC50 = 1000.0 nM 6.00
CHEMBL276711 SEMAXANIB IC50 = 1040.0 nM 5.98
CHEMBL315546 IC50 = 1600.0 nM 5.80
CHEMBL90277 IC50 = 2100.0 nM 5.68
CHEMBL89721 IC50 = 2340.0 nM 5.63
CHEMBL89040 IC50 = 2500.0 nM 5.60
CHEMBL86480 IC50 = 2500.0 nM 5.60
CHEMBL316020 IC50 = 2700.0 nM 5.57
CHEMBL313578 IC50 = 2700.0 nM 5.57
CHEMBL314217 IC50 = 3000.0 nM 5.52
CHEMBL89809 IC50 = 3000.0 nM 5.52
CHEMBL431025 IC50 = 3000.0 nM 5.52
CHEMBL314146 IC50 = 3400.0 nM 5.47
CHEMBL421548 IC50 = 4100.0 nM 5.39
CHEMBL89723 IC50 = 4300.0 nM 5.37
CHEMBL315701 IC50 = 4500.0 nM 5.35
CHEMBL329367 IC50 = 4600.0 nM 5.34
CHEMBL48760 IC50 = 5200.0 nM 5.28
CHEMBL316009 IC50 = 6300.0 nM 5.20
CHEMBL87402 IC50 = 7410.0 nM 5.13
CHEMBL87810 IC50 = 7600.0 nM 5.12
CHEMBL89505 IC50 = 8400.0 nM 5.08
CHEMBL85021 IC50 = 8500.0 nM 5.07
CHEMBL87783 IC50 = 15400.0 nM 4.81
CHEMBL86631 IC50 = 20400.0 nM 4.69
CHEMBL86921 IC50 = 22600.0 nM 4.65
CHEMBL85403 IC50 = 31000.0 nM 4.51
CHEMBL328452 IC50 = 41200.0 nM 4.38
CHEMBL87746 IC50 = 46600.0 nM 4.33
CHEMBL89697 IC50 = 73600.0 nM 4.13
CHEMBL86432 IC50 > 100000.0 nM -
CHEMBL87325 IC50 > 100000.0 nM -
CHEMBL89646 IC50 > 100000.0 nM -
CHEMBL312826 IC50 > 100000.0 nM -
CHEMBL420411 IC50 > 100000.0 nM -
CHEMBL86837 IC50 > 100000.0 nM -
CHEMBL87208 IC50 < 780.0 nM -
CHEMBL313259 IC50 > 100000.0 nM -
CHEMBL86945 IC50 > 100000.0 nM -
CHEMBL87080 IC50 > 10000.0 nM -
CHEMBL87324 IC50 < 780.0 nM -
CHEMBL86944 IC50 > 100000.0 nM -
CHEMBL314021 IC50 > 100000.0 nM -