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Assay Detail

CHEMBL3883090

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

Binding
Inhibition of active N-terminal His6-tagged human recombinant EphB4 (amino acids 561 to end) using poly(glu4tyr) substrate incubated for 60 mins by luciferase-based assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Benzotriazine inhibitors of kinases
(2008)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.14 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL400402 1 7.80
CHEMBL249821 1 7.51
CHEMBL230686 1 7.40
CHEMBL436137 1 7.31
CHEMBL268825 1 7.24
CHEMBL3648039 1 7.18
CHEMBL3648061 1 7.18
CHEMBL3648058 1 7.16
CHEMBL231218 1 7.13
CHEMBL230685 1 6.41
CHEMBL3651269 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL400402 IC50 = 15.9 nM 7.80
CHEMBL249821 IC50 = 30.8 nM 7.51
CHEMBL230686 IC50 = 40.0 nM 7.40
CHEMBL436137 IC50 = 49.0 nM 7.31
CHEMBL268825 IC50 = 58.0 nM 7.24
CHEMBL3648039 IC50 = 66.0 nM 7.18
CHEMBL3648061 IC50 = 66.1 nM 7.18
CHEMBL3648058 IC50 = 68.7 nM 7.16
CHEMBL231218 IC50 = 73.7 nM 7.13
CHEMBL230685 IC50 = 391.0 nM 6.41
CHEMBL3651269 IC50 = 596.0 nM 6.22