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Assay Detail

CHEMBL4357124

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

Binding
Displacement of tetra-acetylated histone H4 peptide (1-21) from recombinant human N-terminal His-tagged BRD4 BD2 (349 to 460 residues) expressed in Escherichia coli incubated for 30 mins followed by further incubation with tetra-acetylated histone H4 peptide (1-21) for 30 mins by Alphascreen assay
ChEMBL ↗
62
Total Activities
62
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 Benzo[<i>cd</i>]indol-2(1<i>H</i>)-ones and Pyrrolo[4,3,2-<i>de</i>]quinolin-2(1<i>H</i>)-ones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the First Bromodomain with Potential High Efficiency against Acute Gouty Arthritis.
Jiang F, Hu Q, Zhang Z, Li H, Li H, Zhang D, Li H, Ma Y, Xu J, Chen H, Cui Y, Zhi Y, Zhang Y, Xu J, Zhu J, Lu T, Chen Y.
J Med Chem (2019) 62 : 11080 -11107
PubMed 31789032 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 62 5.73 7.61

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1957266 — — 1 7.61
CHEMBL4463970 — — 1 6.97
CHEMBL4577584 — — 1 6.62
CHEMBL4546955 — — 1 6.58
CHEMBL4456011 — — 1 6.58
CHEMBL4448388 — — 1 6.54
CHEMBL4540225 — — 1 6.50
CHEMBL4464353 — — 1 6.36
CHEMBL4446896 — — 1 6.36
CHEMBL4449151 — — 1 6.34
CHEMBL4552453 — — 1 6.18
CHEMBL4532972 — — 1 6.09
CHEMBL4562580 — — 1 6.01
CHEMBL4515594 — — 1 5.89
CHEMBL4436978 — — 1 5.82
CHEMBL4526843 — — 1 5.79
CHEMBL4554213 — — 1 5.68
CHEMBL4472607 — — 1 5.67
CHEMBL4583331 — — 1 5.66
CHEMBL4465670 — — 1 5.64
CHEMBL4579153 — — 1 5.61
CHEMBL4573342 — — 1 5.58
CHEMBL4584750 — — 1 5.57
CHEMBL4449002 — — 1 5.57
CHEMBL4463599 — — 1 5.46
CHEMBL4524199 — — 1 5.42
CHEMBL4574260 — — 1 5.39
CHEMBL4438552 — — 1 5.34
CHEMBL4436492 — — 1 5.22
CHEMBL4442989 — — 1 5.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1957266 — IC50 = 24.71 nM 7.61
CHEMBL4463970 — IC50 = 107.1 nM 6.97
CHEMBL4577584 — IC50 = 237.6 nM 6.62
CHEMBL4546955 — IC50 = 260.3 nM 6.58
CHEMBL4456011 — IC50 = 265.6 nM 6.58
CHEMBL4448388 — IC50 = 289.3 nM 6.54
CHEMBL4540225 — IC50 = 320.2 nM 6.50
CHEMBL4464353 — IC50 = 434.9 nM 6.36
CHEMBL4446896 — IC50 = 434.9 nM 6.36
CHEMBL4449151 — IC50 = 458.7 nM 6.34
CHEMBL4552453 — IC50 = 660.2 nM 6.18
CHEMBL4532972 — IC50 = 808.4 nM 6.09
CHEMBL4562580 — IC50 = 981.7 nM 6.01
CHEMBL4515594 — IC50 = 1284.0 nM 5.89
CHEMBL4436978 — IC50 = 1520.0 nM 5.82
CHEMBL4526843 — IC50 = 1640.0 nM 5.79
CHEMBL4554213 — IC50 = 2085.0 nM 5.68
CHEMBL4472607 — IC50 = 2117.0 nM 5.67
CHEMBL4583331 — IC50 = 2167.0 nM 5.66
CHEMBL4465670 — IC50 = 2283.0 nM 5.64
CHEMBL4579153 — IC50 = 2479.0 nM 5.61
CHEMBL4573342 — IC50 = 2621.0 nM 5.58
CHEMBL4584750 — IC50 = 2717.0 nM 5.57
CHEMBL4449002 — IC50 = 2717.0 nM 5.57
CHEMBL4463599 — IC50 = 3468.0 nM 5.46
CHEMBL4524199 — IC50 = 3828.0 nM 5.42
CHEMBL4574260 — IC50 = 4110.0 nM 5.39
CHEMBL4438552 — IC50 = 4599.0 nM 5.34
CHEMBL4436492 — IC50 = 6048.0 nM 5.22
CHEMBL4442989 — IC50 = 6623.0 nM 5.18
CHEMBL4461346 — IC50 = 7068.0 nM 5.15
CHEMBL4531683 — IC50 = 7068.0 nM 5.15
CHEMBL4446421 — IC50 = 12130.0 nM 4.92
CHEMBL4578457 — IC50 = 13675.0 nM 4.86
CHEMBL4457551 — IC50 = 15502.0 nM 4.81
CHEMBL4444741 — IC50 = 20540.0 nM 4.69
CHEMBL4435562 — IC50 = 29638.1 nM 4.53
CHEMBL4473458 — IC50 = 47000.0 nM 4.33
CHEMBL4474319 — IC50 - — -
CHEMBL4541250 — IC50 - — -
CHEMBL4538040 — IC50 - — -
CHEMBL4460838 — IC50 - — -
CHEMBL4444867 — IC50 - — -
CHEMBL4447507 — IC50 - — -
CHEMBL4583559 — IC50 - — -
CHEMBL4445306 — IC50 - — -
CHEMBL4452618 — IC50 - — -
CHEMBL4593926 — IC50 - — -
CHEMBL4476857 — IC50 - — -
CHEMBL4474370 — IC50 - — -