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

CHEMBL4668934

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

Binding
Binding affinity to N-terminal His-tagged BRD4 BD2 (unknown origin) by isothermal calorimetric titration assay
1
Total Activities
1
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

Design and Synthesis of a Highly Selective and In Vivo-Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of Proteins.
Preston A,Atkinson S,Bamborough P,Chung CW,Craggs PD,Gordon L,Grandi P,Gray JRJ,Jones EJ,Lindon M,Michon AM,Mitchell DJ,Prinjha RK,Rianjongdee F,Rioja I,Seal J,Taylor S,Wall I,Watson RJ,Woolven J,Demont EH
J Med Chem (2020) 63 : 9070 -9092
PubMed 32691591 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 6.87 6.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2393130 APABETALONE 3.0 1 6.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2393130 APABETALONE Kd = 135.0 nM 6.87