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Assay Detail

CHEMBL3826482

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

Binding
Inhibition of human N-terminal GST-tagged BRD4-BD1 expressed in Escherichia coli using tetra-acetylated histone H4 measured after 60 mins by AlphaScreen assay
21
Total Activities
21
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

Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor.
Martin LJ, Koegl M, Bader G, Cockcroft XL, Fedorov O, Fiegen D, Gerstberger T, Hofmann MH, Hohmann AF, Kessler D, Knapp S, Knesl P, Kornigg S, Müller S, Nar H, Rogers C, Rumpel K, Schaaf O, Steurer S, Tallant C, Vakoc CR, Zeeb M, Zoephel A, Pearson M, Boehmelt G, McConnell D.
J Med Chem (2016) 59 : 4462 -4475
PubMed 26914985 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 4.80 5.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3823369 1 5.95
CHEMBL3823177 1 5.94
CHEMBL3822498 1 5.43
CHEMBL3823906 1 5.42
CHEMBL3822990 1 5.23
CHEMBL3824289 1 4.72
CHEMBL3823599 1 4.64
CHEMBL3824146 1 4.63
CHEMBL3823697 1 4.51
CHEMBL3822843 1 4.50
CHEMBL3822501 1 4.49
CHEMBL3823551 1 4.36
CHEMBL3822909 1 4.33
CHEMBL3824133 1 4.33
CHEMBL3824351 1 4.21
CHEMBL3822988 1 4.09
CHEMBL3822539 1 -
CHEMBL3823859 1 -
CHEMBL3823478 1 -
CHEMBL3824312 1 -
CHEMBL3823101 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3823369 IC50 = 1121.0 nM 5.95
CHEMBL3823177 IC50 = 1147.0 nM 5.94
CHEMBL3822498 IC50 = 3681.0 nM 5.43
CHEMBL3823906 IC50 = 3778.0 nM 5.42
CHEMBL3822990 IC50 = 5861.0 nM 5.23
CHEMBL3824289 IC50 = 19165.0 nM 4.72
CHEMBL3823599 IC50 = 23005.0 nM 4.64
CHEMBL3824146 IC50 = 23576.0 nM 4.63
CHEMBL3823697 IC50 = 30652.0 nM 4.51
CHEMBL3822843 IC50 = 31421.0 nM 4.50
CHEMBL3822501 IC50 = 32430.0 nM 4.49
CHEMBL3823551 IC50 = 43998.0 nM 4.36
CHEMBL3822909 IC50 = 47359.0 nM 4.33
CHEMBL3824133 IC50 = 47095.0 nM 4.33
CHEMBL3824351 IC50 = 61917.0 nM 4.21
CHEMBL3822988 IC50 = 81300.0 nM 4.09
CHEMBL3822539 IC50 > 100000.0 nM -
CHEMBL3823859 IC50 > 100000.0 nM -
CHEMBL3823478 IC50 > 100000.0 nM -
CHEMBL3824312 IC50 > 100000.0 nM -
CHEMBL3823101 IC50 > 100000.0 nM -