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Assay Detail

CHEMBL950347

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Binding
Inhibition of VEGFR2
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

TIE-2/VEGF-R2 SAR and in vitro activity of C3-acyl dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole analogs.
Underiner TL, Ruggeri B, Aimone L, Albom M, Angeles T, Chang H, Hudkins RL, Hunter K, Josef K, Robinson C, Weinberg L, Yang S, Zulli A.
Bioorg Med Chem Lett (2008) 18 : 2368 -2372
PubMed 18343109 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.97 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL402531 1 9.00
CHEMBL428876 1 8.70
CHEMBL255405 1 8.52
CHEMBL410100 1 8.40
CHEMBL255959 1 8.30
CHEMBL444105 1 8.22
CHEMBL269924 1 8.15
CHEMBL411520 1 8.10
CHEMBL401881 1 8.00
CHEMBL271301 1 8.00
CHEMBL271861 1 7.96
CHEMBL406909 1 7.89
CHEMBL271849 1 7.89
CHEMBL402182 1 7.82
CHEMBL270828 1 7.82
CHEMBL258437 1 7.80
CHEMBL271042 1 7.80
CHEMBL346631 CEP-7055 1.0 1 7.80
CHEMBL270827 1 7.77
CHEMBL401900 1 7.68
CHEMBL403158 1 7.60
CHEMBL255406 1 7.58
CHEMBL404497 1 7.46
CHEMBL255404 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL402531 IC50 = 1.0 nM 9.00
CHEMBL428876 IC50 = 2.0 nM 8.70
CHEMBL255405 IC50 = 3.0 nM 8.52
CHEMBL410100 IC50 = 4.0 nM 8.40
CHEMBL255959 IC50 = 5.0 nM 8.30
CHEMBL444105 IC50 = 6.0 nM 8.22
CHEMBL269924 IC50 = 7.0 nM 8.15
CHEMBL411520 IC50 = 8.0 nM 8.10
CHEMBL401881 IC50 = 10.0 nM 8.00
CHEMBL271301 IC50 = 10.0 nM 8.00
CHEMBL271861 IC50 = 11.0 nM 7.96
CHEMBL406909 IC50 = 13.0 nM 7.89
CHEMBL271849 IC50 = 13.0 nM 7.89
CHEMBL402182 IC50 = 15.0 nM 7.82
CHEMBL270828 IC50 = 15.0 nM 7.82
CHEMBL258437 IC50 = 16.0 nM 7.80
CHEMBL271042 IC50 = 16.0 nM 7.80
CHEMBL346631 CEP-7055 IC50 = 16.0 nM 7.80
CHEMBL270827 IC50 = 17.0 nM 7.77
CHEMBL401900 IC50 = 21.0 nM 7.68
CHEMBL403158 IC50 = 25.0 nM 7.60
CHEMBL255406 IC50 = 26.0 nM 7.58
CHEMBL404497 IC50 = 35.0 nM 7.46
CHEMBL255404 IC50 = 75.0 nM 7.12