Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5044553

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

Binding
Inhibition of BRD4 D1 (unknown origin) by competitive fluorescence anisotropy assay
33
Total Activities
33
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

A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes.
Cui H, Divakaran A, Hoell ZJ, Ellingson MO, Scholtz CR, Zahid H, Johnson JA, Griffith EC, Gee CT, Lee AL, Khanal S, Shi K, Aihara H, Shah VH, Lee RE, Harki DA, Pomerantz WCK.
J Med Chem (2022) 65 : 2342 -2360
PubMed 35007061 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 6.17 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5086716 1 7.00
CHEMBL5089270 1 6.96
CHEMBL5090760 1 6.96
CHEMBL5088918 1 6.72
CHEMBL5079869 1 6.70
CHEMBL5081513 1 6.70
CHEMBL5082969 1 6.58
CHEMBL5087306 1 6.57
CHEMBL5084290 1 6.52
CHEMBL5085763 1 6.51
CHEMBL5084552 1 6.44
CHEMBL5091410 1 6.37
CHEMBL5079566 1 6.36
CHEMBL5080722 1 6.30
CHEMBL5085543 1 6.21
CHEMBL5092030 1 6.06
CHEMBL5075239 1 5.96
CHEMBL5092296 1 5.96
CHEMBL5088397 1 5.72
CHEMBL5085815 1 5.62
CHEMBL5088844 1 5.62
CHEMBL5079170 1 5.57
CHEMBL5078369 1 5.52
CHEMBL5089289 1 5.42
CHEMBL5085512 1 5.03
CHEMBL4521096 1 4.96
CHEMBL5085224 1 -
CHEMBL5078890 1 -
CHEMBL5087797 1 -
CHEMBL5075050 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5086716 IC50 = 100.0 nM 7.00
CHEMBL5089270 IC50 = 110.0 nM 6.96
CHEMBL5090760 IC50 = 110.0 nM 6.96
CHEMBL5088918 IC50 = 190.0 nM 6.72
CHEMBL5079869 IC50 = 200.0 nM 6.70
CHEMBL5081513 IC50 = 200.0 nM 6.70
CHEMBL5082969 IC50 = 260.0 nM 6.58
CHEMBL5087306 IC50 = 270.0 nM 6.57
CHEMBL5084290 IC50 = 300.0 nM 6.52
CHEMBL5085763 IC50 = 310.0 nM 6.51
CHEMBL5084552 IC50 = 360.0 nM 6.44
CHEMBL5091410 IC50 = 430.0 nM 6.37
CHEMBL5079566 IC50 = 440.0 nM 6.36
CHEMBL5080722 IC50 = 500.0 nM 6.30
CHEMBL5085543 IC50 = 610.0 nM 6.21
CHEMBL5092030 IC50 = 880.0 nM 6.06
CHEMBL5075239 IC50 = 1100.0 nM 5.96
CHEMBL5092296 IC50 = 1100.0 nM 5.96
CHEMBL5088397 IC50 = 1900.0 nM 5.72
CHEMBL5085815 IC50 = 2400.0 nM 5.62
CHEMBL5088844 IC50 = 2400.0 nM 5.62
CHEMBL5079170 IC50 = 2700.0 nM 5.57
CHEMBL5078369 IC50 = 3000.0 nM 5.52
CHEMBL5089289 IC50 = 3800.0 nM 5.42
CHEMBL5085512 IC50 = 9400.0 nM 5.03
CHEMBL4521096 IC50 = 11000.0 nM 4.96
CHEMBL5085224 IC50 < 92.0 nM -
CHEMBL5078890 IC50 < 92.0 nM -
CHEMBL5087797 IC50 < 92.0 nM -
CHEMBL5075050 IC50 < 92.0 nM -
CHEMBL5085236 IC50 < 92.0 nM -
CHEMBL5082732 IC50 < 92.0 nM -
CHEMBL1957266 IC50 < 92.0 nM -