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Assay Detail

CHEMBL1764819

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

Binding
Inhibition of human EphB4 autophosphorylation expressed in CHOK1 cells
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct 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 4: Discovery and optimization of a benzylic alcohol series.
Barlaam B, Ducray R, Lambert-van der Brempt C, Plé P, Bardelle C, Brooks N, Coleman T, Cross D, Kettle JG, Read J.
Bioorg Med Chem Lett (2011) 21 : 2207 -2211
PubMed 21441027 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 7.58 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1762529 1 8.15
CHEMBL1738764 1 8.15
CHEMBL1762550 1 8.10
CHEMBL1762525 1 8.00
CHEMBL1762546 1 7.96
CHEMBL1762537 1 7.96
CHEMBL1762549 1 7.92
CHEMBL1762524 1 7.92
CHEMBL1762530 1 7.92
CHEMBL1762548 1 7.89
CHEMBL1762531 1 7.89
CHEMBL1762547 1 7.85
CHEMBL1762527 1 7.68
CHEMBL1762543 1 7.64
CHEMBL1762541 1 7.60
CHEMBL1762536 1 7.57
CHEMBL1762534 1 7.55
CHEMBL1762538 1 7.55
CHEMBL1762523 1 7.55
CHEMBL1762522 1 7.55
CHEMBL1762535 1 7.52
CHEMBL1762539 1 7.50
CHEMBL1762545 1 7.50
CHEMBL1762544 1 7.46
CHEMBL1762526 1 7.42
CHEMBL1762533 1 7.39
CHEMBL1762540 1 7.35
CHEMBL1762521 1 7.08
CHEMBL1762551 1 6.97
CHEMBL1762528 1 6.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1762529 IC50 = 7.0 nM 8.15
CHEMBL1738764 IC50 = 7.0 nM 8.15
CHEMBL1762550 IC50 = 8.0 nM 8.10
CHEMBL1762525 IC50 = 10.0 nM 8.00
CHEMBL1762546 IC50 = 11.0 nM 7.96
CHEMBL1762537 IC50 = 11.0 nM 7.96
CHEMBL1762549 IC50 = 12.0 nM 7.92
CHEMBL1762524 IC50 = 12.0 nM 7.92
CHEMBL1762530 IC50 = 12.0 nM 7.92
CHEMBL1762548 IC50 = 13.0 nM 7.89
CHEMBL1762531 IC50 = 13.0 nM 7.89
CHEMBL1762547 IC50 = 14.0 nM 7.85
CHEMBL1762527 IC50 = 21.0 nM 7.68
CHEMBL1762543 IC50 = 23.0 nM 7.64
CHEMBL1762541 IC50 = 25.0 nM 7.60
CHEMBL1762536 IC50 = 27.0 nM 7.57
CHEMBL1762534 IC50 = 28.0 nM 7.55
CHEMBL1762522 IC50 = 28.0 nM 7.55
CHEMBL1762523 IC50 = 28.0 nM 7.55
CHEMBL1762538 IC50 = 28.0 nM 7.55
CHEMBL1762535 IC50 = 30.0 nM 7.52
CHEMBL1762539 IC50 = 32.0 nM 7.50
CHEMBL1762545 IC50 = 32.0 nM 7.50
CHEMBL1762544 IC50 = 35.0 nM 7.46
CHEMBL1762526 IC50 = 38.0 nM 7.42
CHEMBL1762533 IC50 = 41.0 nM 7.39
CHEMBL1762540 IC50 = 45.0 nM 7.35
CHEMBL1762521 IC50 = 84.0 nM 7.08
CHEMBL1762551 IC50 = 106.0 nM 6.97
CHEMBL1762528 IC50 = 114.0 nM 6.94
CHEMBL1762532 IC50 = 180.0 nM 6.75
CHEMBL1762542 IC50 = 459.0 nM 6.34