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Assay Detail

CHEMBL5713112

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

Binding
Displacement of biotinylated tetra-acetylated histone H4 (1 to 21) peptide from His6-tagged BRD2 (1 to 473 residues) (unknown origin) expressed in Escherichia coli measured after 1 hr by TR-FRET assay
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 2 (CHEMBL1293289)
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 1 5.70 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1950956 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1950956 IC50 = 2000.0 nM 5.70