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Assay Detail

CHEMBL4154431

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

Binding
Inhibition of BRD4 (unknown origin) by Alphascreen assay
3
Total Activities
3
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

Bromodomain-containing protein 4 (CHEMBL1163125)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of benzo[cd]indol-2(1H)-ones derivatives as BRD4 inhibitors.
Feng Y, Xiao S, Chen Y, Jiang H, Liu N, Luo C, Chen S, Chen H.
Eur J Med Chem (2018) 152 : 264 -273
PubMed 29730189 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.87 7.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4177351 1 7.11
CHEMBL3410002 1 6.85
CHEMBL2179387 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4177351 IC50 = 77.0 nM 7.11
CHEMBL3410002 IC50 = 140.0 nM 6.85
CHEMBL2179387 IC50 = 220.0 nM 6.66