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Assay Detail

CHEMBL2344644

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

Binding
Inhibition of EphB4 (unknown origin) transfected in CHO cells using [gamma-33P]ATP by radiometric assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Optimization of inhibitors of the tyrosine kinase EphB4. 2. Cellular potency improvement and binding mode validation by X-ray crystallography.
Lafleur K, Dong J, Huang D, Caflisch A, Nevado C.
J Med Chem (2013) 56 : 84 -96
PubMed 23253074 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.49 7.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2333603 1 7.09
CHEMBL2333602 1 6.88
CHEMBL2333595 1 6.86
CHEMBL271967 1 6.27
CHEMBL577156 1 5.36
CHEMBL2333593 1 -
CHEMBL2333594 1 -
CHEMBL2333596 1 -
CHEMBL2333597 1 -
CHEMBL2333598 1 -
CHEMBL2333599 1 -
CHEMBL2333600 1 -
CHEMBL2333601 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2333603 IC50 = 82.0 nM 7.09
CHEMBL2333602 IC50 = 133.0 nM 6.88
CHEMBL2333595 IC50 = 139.0 nM 6.86
CHEMBL271967 IC50 = 538.0 nM 6.27
CHEMBL577156 IC50 = 4350.0 nM 5.36
CHEMBL2333593 IC50 - -
CHEMBL2333594 IC50 - -
CHEMBL2333596 IC50 - -
CHEMBL2333597 IC50 - -
CHEMBL2333598 IC50 - -
CHEMBL2333599 IC50 - -
CHEMBL2333600 IC50 - -
CHEMBL2333601 IC50 - -