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Assay Detail

CHEMBL4190548

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

Binding
Displacement of Halo-tagged histone H3.3 from Nluc-BRD4 (unknown origin) expressed in HEK293 cells using furimazine as substrate pretreated for 18 hrs followed by substrate addition measured within 5 mins by NanoBRET assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bromodomain-containing protein 4 (CHEMBL1163125)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Chemical probes and inhibitors of bromodomains outside the BET family.
Moustakim M, Clark PGK, Hay DA, Dixon DJ, Brennan PE.
Medchemcomm (2016) 7 : 2246 -2264
PubMed 29170712 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.22 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3774655 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3774655 IC50 = 600.0 nM 6.22