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Assay Detail

CHEMBL4809931

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

ADMET
Displacement of Alexa Fluor 647 labelled ligand from 6His-FLAG-Tev-tagged BRDT BD1/BD2 Y309A (1 to 397 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 ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bromodomain testis-specific protein (CHEMBL1795185)
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 4.60 4.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4862372 1 4.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4862372 IC50 = 25118.86 nM 4.60