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Assay Detail

CHEMBL4038394

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

Binding
Inhibition of BRD4 (unknown origin) expressed in human H1299 cells co-expressing HPV16-LCR/E2 after 24 hrs by Bright Glo-luciferase reporter gene assay
ChEMBL ↗
36
Total Activities
36
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

Methylpyrrole inhibitors of BET bromodomains.
Hasvold LA, Sheppard GS, Wang L, Fidanze SD, Liu D, Pratt JK, Mantei RA, Wada CK, Hubbard R, Shen Y, Lin X, Huang X, Warder SE, Wilcox D, Li L, Buchanan FG, Smithee L, Albert DH, Magoc TJ, Park CH, Petros AM, Panchal SC, Sun C, Kovar P, Soni NB, Elmore SW, Kati WM, McDaniel KF.
Bioorg Med Chem Lett (2017) 27 : 2225 -2233
PubMed 28268136 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 36 6.40 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4097720 — — 1 7.40
CHEMBL4079684 — — 1 7.34
CHEMBL4064089 — — 1 7.33
CHEMBL4063051 — — 1 7.29
CHEMBL4096183 — — 1 7.25
CHEMBL4064625 — — 1 7.12
CHEMBL4097227 — — 1 7.12
CHEMBL4068902 — — 1 7.04
CHEMBL4087079 — — 1 6.92
CHEMBL4088466 — — 1 6.82
CHEMBL4086135 — — 1 6.75
CHEMBL4102516 — — 1 6.66
CHEMBL4104934 — — 1 6.55
CHEMBL4098863 — — 1 6.55
CHEMBL4074813 — — 1 6.55
CHEMBL4068988 — — 1 6.55
CHEMBL3786012 — — 1 6.54
CHEMBL4069994 — — 1 6.52
CHEMBL4080682 — — 1 6.39
CHEMBL4067320 — — 1 6.38
CHEMBL4065327 — — 1 6.35
CHEMBL4078245 — — 1 6.16
CHEMBL4095264 — — 1 6.12
CHEMBL4088536 — — 1 6.06
CHEMBL4103937 — — 1 5.96
CHEMBL4098709 — — 1 5.85
CHEMBL4060309 — — 1 5.85
CHEMBL4079208 — — 1 5.85
CHEMBL4076251 — — 1 5.80
CHEMBL4080666 — — 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4097720 — EC50 = 40.0 nM 7.40
CHEMBL4079684 — EC50 = 46.0 nM 7.34
CHEMBL4064089 — EC50 = 47.0 nM 7.33
CHEMBL4063051 — EC50 = 51.0 nM 7.29
CHEMBL4096183 — EC50 = 56.0 nM 7.25
CHEMBL4064625 — EC50 = 75.0 nM 7.12
CHEMBL4097227 — EC50 = 75.0 nM 7.12
CHEMBL4068902 — EC50 = 91.0 nM 7.04
CHEMBL4087079 — EC50 = 120.0 nM 6.92
CHEMBL4088466 — EC50 = 150.0 nM 6.82
CHEMBL4086135 — EC50 = 180.0 nM 6.75
CHEMBL4102516 — EC50 = 220.0 nM 6.66
CHEMBL4068988 — EC50 = 280.0 nM 6.55
CHEMBL4074813 — EC50 = 280.0 nM 6.55
CHEMBL4098863 — EC50 = 280.0 nM 6.55
CHEMBL4104934 — EC50 = 280.0 nM 6.55
CHEMBL3786012 — EC50 = 290.0 nM 6.54
CHEMBL4069994 — EC50 = 300.0 nM 6.52
CHEMBL4080682 — EC50 = 410.0 nM 6.39
CHEMBL4067320 — EC50 = 420.0 nM 6.38
CHEMBL4065327 — EC50 = 450.0 nM 6.35
CHEMBL4078245 — EC50 = 700.0 nM 6.16
CHEMBL4095264 — EC50 = 750.0 nM 6.12
CHEMBL4088536 — EC50 = 880.0 nM 6.06
CHEMBL4103937 — EC50 = 1100.0 nM 5.96
CHEMBL4079208 — EC50 = 1400.0 nM 5.85
CHEMBL4060309 — EC50 = 1400.0 nM 5.85
CHEMBL4098709 — EC50 = 1400.0 nM 5.85
CHEMBL4076251 — EC50 = 1600.0 nM 5.80
CHEMBL4080666 — EC50 = 2000.0 nM 5.70
CHEMBL4080820 — EC50 = 2100.0 nM 5.68
CHEMBL4074891 — EC50 = 2300.0 nM 5.64
CHEMBL4086753 — EC50 = 2800.0 nM 5.55
CHEMBL4095330 — EC50 = 4500.0 nM 5.35
CHEMBL4096256 — EC50 = 7100.0 nM 5.15
CHEMBL4073935 — EC50 > 10000.0 nM -