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Assay Detail

CHEMBL4331529

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

Binding
Inhibition of BRD4 in human MV4-11 cells using biotin labelled N-C:SGRG-K(Ac)-GG-K(Ac)-GLG-K(Ac)-GGA-K(Ac)-RHRKVGG-K as substrate preincubated for 15 mins followed by substrate addition measured after 5 mins by alpha screen assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MV4-11
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.
Xing J, Zhang R, Jiang X, Hu T, Wang X, Qiao G, Wang J, Yang F, Luo X, Chen K, Shen J, Luo C, Jiang H, Zheng M.
Eur J Med Chem (2019) 163 : 281 -294
PubMed 30529546 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.01 6.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1454910 NITROXOLINE 4.0 1 6.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1454910 NITROXOLINE IC50 = 980.0 nM 6.01