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Assay Detail

CHEMBL4809560

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

Binding
Inhibition of BRD4 (unknown origin)
10
Total Activities
10
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

Development of BET inhibitors as potential treatments for cancer: A search for structural diversity.
Hill MD, Fang H, Tokarski J, Fanslau C, Haarhoff Z, Huang C, Kramer M, Menard K, Monereau L, Morrison J, Ranasinghe A, Shields EE, Tye CK, Westhouse R, Everlof G, Sheriff S, Yan C, Marsilio F, Zhang L, Zvyaga T, Lee F, Gavai AV, Degnan AP.
Bioorg Med Chem Lett (2021) 44 : 128108 -128108
PubMed 33991625 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 8.78 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4846895 1 9.22
CHEMBL4859923 1 9.05
CHEMBL4848871 1 9.05
CHEMBL4864173 1 9.00
CHEMBL4863199 1 8.92
CHEMBL4869203 1 8.85
CHEMBL4857742 1 8.80
CHEMBL4875203 1 8.70
CHEMBL4871769 1 8.64
CHEMBL4850311 1 7.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4846895 IC50 = 0.6 nM 9.22
CHEMBL4859923 IC50 = 0.9 nM 9.05
CHEMBL4848871 IC50 = 0.9 nM 9.05
CHEMBL4864173 IC50 = 1.0 nM 9.00
CHEMBL4863199 IC50 = 1.2 nM 8.92
CHEMBL4869203 IC50 = 1.4 nM 8.85
CHEMBL4857742 IC50 = 1.6 nM 8.80
CHEMBL4875203 IC50 = 2.0 nM 8.70
CHEMBL4871769 IC50 = 2.3 nM 8.64
CHEMBL4850311 IC50 = 27.0 nM 7.57