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Assay Detail

CHEMBL5713045

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

Binding
Displacement of biotinylated peptide from BRD4 bromodomain 1 (unknown origin) incubated for 30 mins by AlphaScreen assay
6
Total Activities
6
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

Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.
Chen P, Chaikuad A, Bamborough P, Bantscheff M, Bountra C, Chung CW, Fedorov O, Grandi P, Jung D, Lesniak R, Lindon M, Müller S, Philpott M, Prinjha R, Rogers C, Selenski C, Tallant C, Werner T, Willson TM, Knapp S, Drewry DH.
J Med Chem (2016) 59 : 1410 -1424
PubMed 25799074 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 4.41 4.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3770112 1 4.41
CHEMBL3770847 1 -
CHEMBL3770199 1 -
CHEMBL3739699 1 -
CHEMBL3770277 1 -
CHEMBL3770214 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3770112 IC50 = 38900.0 nM 4.41
CHEMBL3770847 IC50 > 50000.0 nM -
CHEMBL3770199 IC50 > 50000.0 nM -
CHEMBL3739699 IC50 > 50000.0 nM -
CHEMBL3770277 IC50 > 50000.0 nM -
CHEMBL3770214 IC50 > 50000.0 nM -