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Assay Detail

CHEMBL932336

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Binding
Inhibition of EphB4
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Inhibitors of the tyrosine kinase EphB4. Part 1: Structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines.
Bardelle C, 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 : 2776 -2780
PubMed 18434142 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 5.74 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL257553 1 7.40
CHEMBL445162 1 7.05
CHEMBL256725 1 6.62
CHEMBL256348 1 6.52
CHEMBL169186 1 6.46
CHEMBL404444 1 6.34
CHEMBL254588 1 6.26
CHEMBL255874 1 6.24
CHEMBL258016 1 6.20
CHEMBL402903 1 6.19
CHEMBL255875 1 6.00
CHEMBL256724 1 5.94
CHEMBL258435 1 5.90
CHEMBL401907 1 5.88
CHEMBL402934 1 5.81
CHEMBL404445 1 5.80
CHEMBL257576 1 5.71
CHEMBL402584 1 5.64
CHEMBL253741 1 5.59
CHEMBL403672 1 5.53
CHEMBL253957 1 5.41
CHEMBL402933 1 5.30
CHEMBL255947 1 5.22
CHEMBL257771 1 5.11
CHEMBL255949 1 4.95
CHEMBL254157 1 4.86
CHEMBL403673 1 4.80
CHEMBL428067 1 4.69
CHEMBL403614 1 4.45
CHEMBL404178 1 4.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL257553 IC50 = 40.0 nM 7.40
CHEMBL445162 IC50 = 90.0 nM 7.05
CHEMBL256725 IC50 = 240.0 nM 6.62
CHEMBL256348 IC50 = 300.0 nM 6.52
CHEMBL169186 IC50 = 350.0 nM 6.46
CHEMBL404444 IC50 = 460.0 nM 6.34
CHEMBL254588 IC50 = 550.0 nM 6.26
CHEMBL255874 IC50 = 580.0 nM 6.24
CHEMBL258016 IC50 = 630.0 nM 6.20
CHEMBL402903 IC50 = 640.0 nM 6.19
CHEMBL255875 IC50 = 1000.0 nM 6.00
CHEMBL256724 IC50 = 1150.0 nM 5.94
CHEMBL258435 IC50 = 1250.0 nM 5.90
CHEMBL401907 IC50 = 1330.0 nM 5.88
CHEMBL402934 IC50 = 1550.0 nM 5.81
CHEMBL404445 IC50 = 1600.0 nM 5.80
CHEMBL257576 IC50 = 1940.0 nM 5.71
CHEMBL402584 IC50 = 2300.0 nM 5.64
CHEMBL253741 IC50 = 2540.0 nM 5.59
CHEMBL403672 IC50 = 2960.0 nM 5.53
CHEMBL253957 IC50 = 3880.0 nM 5.41
CHEMBL402933 IC50 = 5000.0 nM 5.30
CHEMBL255947 IC50 = 6000.0 nM 5.22
CHEMBL257771 IC50 = 7850.0 nM 5.11
CHEMBL255949 IC50 = 11320.0 nM 4.95
CHEMBL254157 IC50 = 13960.0 nM 4.86
CHEMBL403673 IC50 = 16000.0 nM 4.80
CHEMBL428067 IC50 = 20490.0 nM 4.69
CHEMBL403614 IC50 = 35500.0 nM 4.45
CHEMBL404178 IC50 = 41000.0 nM 4.39