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Assay Detail

CHEMBL5114964

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

Binding
Inhibition of BRD4 BD1 (unknown origin) TR-FRET analysis
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 4 (CHEMBL1163125)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 2-((2-methylbenzyl)thio)-6-oxo-4-(3,4,5-trimethoxyphenyl)-1,6-dihydropyrimidine-5-carbonitrile as a novel and effective bromodomain and extra-terminal (BET) inhibitor for the treatment of sepsis.
Chen X, Meng F, Zhang J, Zhang Z, Ye X, Zhang W, Tong Y, Ji X, Xu R, Xu XL, You QD, Jiang ZY.
Eur J Med Chem (2022) 238 : 114423 -114423
PubMed 35544982 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.96 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4303404 PELABRESIB 3.0 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4303404 PELABRESIB IC50 = 11.0 nM 7.96