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Assay Detail

CHEMBL5122320

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

Binding
Inhibition of human recombinant BRD4-BD2 expressed in Escherichia coli using C-Terminal-biotinylated histone H4 peptide as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by microplate reader method
1
Total Activities
1
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

Targeting Bromodomain-Selective Inhibitors of BET Proteins in Drug Discovery and Development.
Chen J, Tang P, Wang Y, Wang J, Yang C, Li Y, Yang G, Wu F, Zhang J, Ouyang L.
J Med Chem (2022) 65 : 5184 -5211
PubMed 35324195 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.69 6.69

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL222541 1 6.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL222541 IC50 = 204.0 nM 6.69