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Assay Detail

CHEMBL5345441

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Binding
Binding affinity to human BRD4 BD 1 assessed as dissociation constant by ITC analysis
3
Total Activities
3
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

Small Molecule Ligands of the BET-like Bromodomain, <i>Sm</i>BRD3, Affect <i>Schistosoma mansoni</i> Survival, Oviposition, and Development.
Schiedel M, McArdle DJB, Padalino G, Chan AKN, Forde-Thomas J, McDonough M, Whiteland H, Beckmann M, Cookson R, Hoffmann KF, Conway SJ.
J Med Chem (2023) 66 : 15801 -15822
PubMed 38048437 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 7.76 8.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2177300 1 8.21
CHEMBL5407959 1 7.87
CHEMBL5430618 1 7.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2177300 Kd = 6.23 nM 8.21
CHEMBL5407959 Kd = 13.5 nM 7.87
CHEMBL5430618 Kd = 64.4 nM 7.19