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Assay Detail

CHEMBL4310084

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

Binding
Inhibition of human BRDT bromodomain 1 (unknown origin) expressed in Escherichia coli Bl21(DE3) by fluorescence anisotropy
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 testis-specific protein (CHEMBL1795185)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.
Divakaran A, Talluri SK, Ayoub AM, Mishra NK, Cui H, Widen JC, Berndt N, Zhu JY, Carlson AS, Topczewski JJ, Schonbrunn EK, Harki DA, Pomerantz WCK.
J Med Chem (2018) 61 : 9316 -9334
PubMed 30253095 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 4.90 5.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4521096 1 5.46
CHEMBL4452281 1 5.33
CHEMBL13880 1 4.89
CHEMBL417255 1 4.75
CHEMBL14682 1 4.06
CHEMBL14339 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4521096 IC50 = 3500.0 nM 5.46
CHEMBL4452281 IC50 = 4700.0 nM 5.33
CHEMBL13880 IC50 = 13000.0 nM 4.89
CHEMBL417255 IC50 = 18000.0 nM 4.75
CHEMBL14682 IC50 = 88000.0 nM 4.06
CHEMBL14339 IC50 > 250000.0 nM -