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Assay Detail

CHEMBL1046768

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Binding
Inhibition of EphB4 by [gamma33-P]ATP based assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Ephrin type-B receptor 4 (CHEMBL5147)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4).
Lafleur K, Huang D, Zhou T, Caflisch A, Nevado C.
J Med Chem (2009) 52 : 6433 -6446
PubMed 19788238 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.68 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL566515 1 8.80
CHEMBL574236 1 7.33
CHEMBL575335 1 6.67
CHEMBL577156 1 5.36
CHEMBL271179 1 5.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL566515 IC50 = 1.6 nM 8.80
CHEMBL574236 IC50 = 47.0 nM 7.33
CHEMBL575335 IC50 = 213.0 nM 6.67
CHEMBL577156 IC50 = 4350.0 nM 5.36
CHEMBL271179 IC50 = 5680.0 nM 5.25