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Assay Detail

CHEMBL1007023

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

Binding
Inhibition of Myc-His-tagged EphB4 expressed in CHOK1 cells assessed as phosphorylation by ELISA
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-K1
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Inhibitors of the tyrosine kinase EphB4. Part 2: structure-based discovery and optimisation of 3,5-bis substituted anilinopyrimidines.
Bardelle C, Coleman T, Cross D, Davenport S, Kettle JG, Ko EJ, Leach AG, Mortlock A, Read J, Roberts NJ, Robins P, Williams EJ.
Bioorg Med Chem Lett (2008) 18 : 5717 -5717
PubMed 18851911 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.21 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL468970 1 7.77
CHEMBL497198 1 7.50
CHEMBL523744 1 6.77
CHEMBL257553 1 6.76
CHEMBL445162 1 6.72
CHEMBL497194 1 6.68
CHEMBL496574 1 6.13
CHEMBL500724 1 6.05
CHEMBL517720 1 6.05
CHEMBL523088 1 5.69
CHEMBL496968 1 5.14
CHEMBL496760 1 4.85
CHEMBL497195 1 4.65
CHEMBL255874 1 -
CHEMBL498404 1 -
CHEMBL460600 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL468970 IC50 = 17.0 nM 7.77
CHEMBL497198 IC50 = 32.0 nM 7.50
CHEMBL523744 IC50 = 170.0 nM 6.77
CHEMBL257553 IC50 = 172.0 nM 6.76
CHEMBL445162 IC50 = 190.0 nM 6.72
CHEMBL497194 IC50 = 209.0 nM 6.68
CHEMBL496574 IC50 = 741.0 nM 6.13
CHEMBL500724 IC50 = 900.0 nM 6.05
CHEMBL517720 IC50 = 887.0 nM 6.05
CHEMBL523088 IC50 = 2054.0 nM 5.69
CHEMBL496968 IC50 = 7175.0 nM 5.14
CHEMBL496760 IC50 = 14117.0 nM 4.85
CHEMBL497195 IC50 = 22200.0 nM 4.65
CHEMBL255874 IC50 - -
CHEMBL498404 IC50 > 30000.0 nM -
CHEMBL460600 IC50 > 30000.0 nM -