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Assay Detail

CHEMBL3757063

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Binding
Inhibition of PCAF bromodomain (719 to 832 amino acid residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells by NMR analysis
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

Histone acetyltransferase KAT2B (CHEMBL5500)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Fragments in bromodomain drug discovery
Bamborough P, Chung C
Medchemcomm (2015) 6 : 1587 -1604
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.55 5.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL609728 1 5.80
CHEMBL1234797 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL609728 IC50 = 1600.0 nM 5.80
CHEMBL1234797 IC50 = 5000.0 nM 5.30