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Assay Detail

CHEMBL5045654

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

Binding
Displacement of Alexafluor 647-JQ1 from GST-BRD4 BD1 BD2 (44 to 460 residues) (unknown origin) incubated for 60 mins by fluorescence polarization assay
20
Total Activities
20
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

Discovery of a Potent and Selective ATAD2 Bromodomain Inhibitor with Antiproliferative Activity in Breast Cancer Models.
Winter-Holt JJ, Bardelle C, Chiarparin E, Dale IL, Davey PRJ, Davies NL, Denz C, Fillery SM, Guérot CM, Han F, Hughes SJ, Kulkarni M, Liu Z, Milbradt A, Moss TA, Niu H, Patel J, Rabow AA, Schimpl M, Shi J, Sun D, Yang D, Guichard S.
J Med Chem (2022) 65 : 3306 -3331
PubMed 35133824 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 4.77 5.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5083025 1 5.10
CHEMBL5090538 1 5.10
CHEMBL5083653 1 4.80
CHEMBL5079885 1 4.70
CHEMBL5087319 1 4.60
CHEMBL5084768 1 4.60
CHEMBL5074983 1 4.50
CHEMBL5090410 1 -
CHEMBL5074753 1 -
CHEMBL5083337 1 -
CHEMBL5084439 1 -
CHEMBL5087156 1 -
CHEMBL5075463 1 -
CHEMBL5093167 1 -
CHEMBL5086260 1 -
CHEMBL5092181 1 -
CHEMBL5077167 1 -
CHEMBL5086059 1 -
CHEMBL5093862 1 -
CHEMBL5090369 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5083025 IC50 = 7943.28 nM 5.10
CHEMBL5090538 IC50 = 7943.28 nM 5.10
CHEMBL5083653 IC50 = 15848.93 nM 4.80
CHEMBL5079885 IC50 = 19952.62 nM 4.70
CHEMBL5087319 IC50 = 25118.86 nM 4.60
CHEMBL5084768 IC50 = 25118.86 nM 4.60
CHEMBL5074983 IC50 = 31622.78 nM 4.50
CHEMBL5090410 IC50 > 31622.78 nM -
CHEMBL5074753 IC50 > 31622.78 nM -
CHEMBL5083337 IC50 > 31622.78 nM -
CHEMBL5084439 IC50 > 31622.78 nM -
CHEMBL5087156 IC50 > 31622.78 nM -
CHEMBL5075463 IC50 > 31622.78 nM -
CHEMBL5093167 IC50 > 31622.78 nM -
CHEMBL5086260 IC50 > 31622.78 nM -
CHEMBL5092181 IC50 > 31622.78 nM -
CHEMBL5077167 IC50 > 31622.78 nM -
CHEMBL5086059 IC50 > 31622.78 nM -
CHEMBL5093862 IC50 > 31622.78 nM -
CHEMBL5090369 IC50 > 31622.78 nM -