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Assay Detail

CHEMBL3111112

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

Binding
Displacement of biotinylated H3Kac14 peptide from His6-tagged human BAZ2B expressed in Escherichia coli BL21(DE3) after 30 mins by AlphaScreen assay
10
Total Activities
10
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

Publication

Targeting low-druggability bromodomains: fragment based screening and inhibitor design against the BAZ2B bromodomain.
Ferguson FM, Fedorov O, Chaikuad A, Philpott M, Muniz JR, Felletar I, von Delft F, Heightman T, Knapp S, Abell C, Ciulli A.
J Med Chem (2013) 56 : 10183 -10187
PubMed 24304323 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 3.64 4.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3110247 1 4.43
CHEMBL3110243 1 4.42
CHEMBL3110244 1 3.96
CHEMBL2441350 1 3.72
CHEMBL3110245 1 3.62
CHEMBL1650611 1 3.55
CHEMBL1568712 1 3.32
CHEMBL3110248 1 3.31
CHEMBL528463 1 3.08
CHEMBL3110246 1 2.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3110247 IC50 = 37000.0 nM 4.43
CHEMBL3110243 IC50 = 38000.0 nM 4.42
CHEMBL3110244 IC50 = 109000.0 nM 3.96
CHEMBL2441350 IC50 = 190000.0 nM 3.72
CHEMBL3110245 IC50 = 241000.0 nM 3.62
CHEMBL1650611 IC50 = 279000.0 nM 3.55
CHEMBL1568712 IC50 = 476000.0 nM 3.32
CHEMBL3110248 IC50 = 495000.0 nM 3.31
CHEMBL528463 IC50 = 826000.0 nM 3.08
CHEMBL3110246 IC50 = 1094000.0 nM 2.96