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Assay Detail

CHEMBL4189289

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

Binding
Inhibition of human BRD2 BD2 after 30 mins by TR-FRET assay
2
Total Activities
2
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

Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.
Law RP, Atkinson SJ, Bamborough P, Chung CW, Demont EH, Gordon LJ, Lindon M, Prinjha RK, Watson AJB, Hirst DJ.
J Med Chem (2018) 61 : 4317 -4334
PubMed 29656650 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.75 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4213809 1 7.00
CHEMBL4218735 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4213809 IC50 = 100.0 nM 7.00
CHEMBL4218735 IC50 = 316.23 nM 6.50