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Assay Detail

CHEMBL5235458

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

Binding
Inhibition of BRD4 (unknown origin)
6
Total Activities
6
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

Targeting MYC: From understanding its biology to drug discovery.
Ross J, Miron CE, Plescia J, Laplante P, McBride K, Moitessier N, Möröy T.
Eur J Med Chem (2021) 213 : 113137 -113137
PubMed 33460833 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.16 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3987016 MIVEBRESIB 2.0 1 8.52
CHEMBL4078100 AZD-5153 1.0 1 8.30
CHEMBL1232461 MOLIBRESIB 2.0 1 7.52
CHEMBL4303404 PELABRESIB 3.0 1 7.41
CHEMBL9 NORFLOXACIN 4.0 1 6.01
CHEMBL225164 CLOXYQUIN 2.0 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3987016 MIVEBRESIB IC50 = 3.0 nM 8.52
CHEMBL4078100 AZD-5153 IC50 = 5.0 nM 8.30
CHEMBL1232461 MOLIBRESIB IC50 = 30.0 nM 7.52
CHEMBL4303404 PELABRESIB IC50 = 39.0 nM 7.41
CHEMBL9 NORFLOXACIN IC50 = 980.0 nM 6.01
CHEMBL225164 CLOXYQUIN IC50 = 6470.0 nM 5.19