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Assay Detail

CHEMBL4033192

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

Binding
Inhibition of recombinant human N-terminal GST-tagged BRD3 bromodomain-2 (306 to 417 residues) expressed in Escherichia coli expression system after 120 mins by TR-FRET assay
2
Total Activities
2
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 3 (CHEMBL1795186)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer.
Ouyang L, Zhang L, Liu J, Fu L, Yao D, Zhao Y, Zhang S, Wang G, He G, Liu B.
J Med Chem (2017) 60 : 9990 -10012
PubMed 29172540 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.41 7.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2132936 1 7.41
CHEMBL4077274 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2132936 IC50 = 39.0 nM 7.41
CHEMBL4077274 IC50 > 100000.0 nM -