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

CHEMBL4809926

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

Binding
Displacement of Alexa Fluor 647 labelled ligand from 6His-Thr tagged BRD2 BD2/BD1 Y113A mutant (1 to 473 residues) (unknown origin) measured after 30 mins by TR-FRET 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 2 (CHEMBL1293289)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of a Series of <i>N</i>-Methylpyridine-2-carboxamides as Potent and Selective Inhibitors of the Second Bromodomain (BD2) of the Bromo and Extra Terminal Domain (BET) Proteins.
Harrison LA, Atkinson SJ, Bassil A, Chung CW, Grandi P, Gray JRJ, Levernier E, Lewis A, Lugo D, Messenger C, Michon AM, Mitchell DJ, Preston A, Prinjha RK, Rioja I, Seal JT, Taylor S, Wall ID, Watson RJ, Woolven JM, Demont EH.
J Med Chem (2021) 64 : 10742 -10771
PubMed 34232650 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.40 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4862372 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4862372 IC50 = 39.81 nM 7.40