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Assay Detail

CHEMBL5029809

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

Binding
Inhibition of BRD4 (unknown origin)
9
Total Activities
9
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 new carboline chemotype.
Hill MD, Quesnelle C, Tokarski J, Fang H, Fanslau C, Haarhoff Z, Kramer M, Madari S, Wiebesiek A, Morrison J, Simmermacher-Mayer J, Sinz M, Westhouse R, Xie C, Zhao J, Huang L, Sheriff S, Yan C, Marsilio F, Everlof G, Zvyaga T, Lee F, Gavai AV, Degnan AP.
Bioorg Med Chem Lett (2021) 51 : 128376 -128376
PubMed 34560263 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 9.10 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5091333 1 9.40
CHEMBL5075294 1 9.30
CHEMBL5089688 1 9.22
CHEMBL5084198 1 9.22
CHEMBL5090513 1 9.22
CHEMBL5090808 1 9.15
CHEMBL4297458 EZOBRESIB 2.0 1 9.10
CHEMBL5086429 1 8.89
CHEMBL5084636 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5091333 IC50 = 0.4 nM 9.40
CHEMBL5075294 IC50 = 0.5 nM 9.30
CHEMBL5089688 IC50 = 0.6 nM 9.22
CHEMBL5084198 IC50 = 0.6 nM 9.22
CHEMBL5090513 IC50 = 0.6 nM 9.22
CHEMBL5090808 IC50 = 0.7 nM 9.15
CHEMBL4297458 EZOBRESIB IC50 = 0.8 nM 9.10
CHEMBL5086429 IC50 = 1.3 nM 8.89
CHEMBL5084636 IC50 = 4.0 nM 8.40