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Assay Detail

CHEMBL4727064

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

Binding
Binding affinity to full length BRD2 BD1 in human HuT78 cell lysates incubated for 45 mins by liquid chromatography-mass spectrometry based chemoproteomic binding assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HuT78
Subcellular Lysates
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bromodomain-containing protein 2 (CHEMBL1293289)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins.
Watson RJ,Bamborough P,Barnett H,Chung CW,Davis R,Gordon L,Grandi P,Petretich M,Phillipou A,Prinjha RK,Rioja I,Soden P,Werner T,Demont EH
J Med Chem (2020) 63 : 9045 -9069
PubMed 32691589 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 8.40 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4648362 GSK789 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4648362 GSK789 Kd = 3.981 nM 8.40