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Assay Detail

CHEMBL5261609

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

Binding
Displacement of biotinylated small-molecule ligand from recombinant His-tagged BRD4 bromodomain 2 (unknown origin) measured after 10 mins by TR-FRET assay
11
Total Activities
11
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

Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance.
Crawford TD, Vartanian S, Côté A, Bellon S, Duplessis M, Flynn EM, Hewitt M, Huang HR, Kiefer JR, Murray J, Nasveschuk CG, Pardo E, Romero FA, Sandy P, Tang Y, Taylor AM, Tsui V, Wang J, Wang S, Zawadzke L, Albrecht BK, Magnuson SR, Cochran AG, Stokoe D.
Bioorg Med Chem Lett (2017) 27 : 3534 -3541
PubMed 28606761 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.09 5.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4519632 1 5.85
CHEMBL5286608 1 5.21
CHEMBL5284261 1 5.17
CHEMBL5270178 1 5.08
CHEMBL5285110 1 4.91
CHEMBL5268936 1 4.87
CHEMBL5280605 1 4.84
CHEMBL5279182 1 4.76
CHEMBL5282240 1 -
CHEMBL5289762 1 -
CHEMBL5268484 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4519632 IC50 = 1400.0 nM 5.85
CHEMBL5286608 IC50 = 6100.0 nM 5.21
CHEMBL5284261 IC50 = 6700.0 nM 5.17
CHEMBL5270178 IC50 = 8300.0 nM 5.08
CHEMBL5285110 IC50 = 12300.0 nM 4.91
CHEMBL5268936 IC50 = 13500.0 nM 4.87
CHEMBL5280605 IC50 = 14400.0 nM 4.84
CHEMBL5279182 IC50 = 17400.0 nM 4.76
CHEMBL5282240 IC50 > 20000.0 nM -
CHEMBL5289762 IC50 > 20000.0 nM -
CHEMBL5268484 IC50 > 20000.0 nM -