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Assay Detail

CHEMBL3757071

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

Binding
Displacement of biotinylated H4(1 to 24 amino acid residues)-K5/8/12/16Ac from human N-terminal His6-tagged BRD4 bromodomain-1 expressed in Escherichia coli BL21(DE3) cells by alpha screen 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 4 (CHEMBL1163125)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Fragments in bromodomain drug discovery
Bamborough P, Chung C
Medchemcomm (2015) 6 : 1587 -1604
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.60 5.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL278041 SB-202190 1 5.60
CHEMBL14212 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL278041 SB-202190 IC50 = 2500.0 nM 5.60
CHEMBL14212 IC50 = 2500.0 nM 5.60