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

CHEMBL4612966

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

Binding
Inhibition of BRD4 bromodomain 1 (unknown origin) by AlphaScreen displacement assay
13
Total Activities
13
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

Synthesis and Structure-Activity Relationships of DCLK1 Kinase Inhibitors Based on a 5,11-Dihydro-6<i>H</i>-benzo[<i>e</i>]pyrimido[5,4-<i>b</i>][1,4]diazepin-6-one Scaffold.
Ferguson FM, Liu Y, Harshbarger W, Huang L, Wang J, Deng X, Capuzzi SJ, Muratov EN, Tropsha A, Muthuswamy S, Westover KD, Gray NS.
J Med Chem (2020) 63 : 7817 -7826
PubMed 32530623 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.85 6.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4636475 1 6.90
CHEMBL4643632 1 6.28
CHEMBL4634326 1 6.08
CHEMBL1673039 1 6.05
CHEMBL4649318 1 5.92
CHEMBL4640016 1 5.80
CHEMBL4646882 1 5.62
CHEMBL1673048 1 5.38
CHEMBL4644273 1 5.34
CHEMBL4635720 1 5.13
CHEMBL1672987 1 -
CHEMBL4639395 1 -
CHEMBL4641263 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4636475 IC50 = 125.0 nM 6.90
CHEMBL4643632 IC50 = 520.0 nM 6.28
CHEMBL4634326 IC50 = 830.0 nM 6.08
CHEMBL1673039 IC50 = 888.0 nM 6.05
CHEMBL4649318 IC50 = 1200.0 nM 5.92
CHEMBL4640016 IC50 = 1570.0 nM 5.80
CHEMBL4646882 IC50 = 2380.0 nM 5.62
CHEMBL1673048 IC50 = 4170.0 nM 5.38
CHEMBL4644273 IC50 = 4600.0 nM 5.34
CHEMBL4635720 IC50 = 7490.0 nM 5.13
CHEMBL1672987 IC50 > 10000.0 nM -
CHEMBL4639395 IC50 > 10000.0 nM -
CHEMBL4641263 IC50 > 10000.0 nM -