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Assay Detail

CHEMBL4836628

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

Binding
Inhibition of 6His-Thr-BRD2 (1 to 473 residues) BD2 domain Y386A or Y113A mutant (unknown origin) incubated for 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

Optimization of a Series of 2,3-Dihydrobenzofurans as Highly Potent, Second Bromodomain (BD2)-Selective, Bromo and Extra-Terminal Domain (BET) Inhibitors.
Lucas SCC, Atkinson SJ, Chung CW, Davis R, Gordon L, Grandi P, Gray JJR, Grimes T, Phillipou A, Preston AG, Prinjha RK, Rioja I, Taylor S, Tomkinson NCO, Wall I, Watson RJ, Woolven J, Demont EH.
J Med Chem (2021) 64 : 10711 -10741
PubMed 34260229 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.00 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4869149 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4869149 IC50 = 10.0 nM 8.00