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Assay Detail

CHEMBL1025549

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

Binding
Inhibition of PCAF HAT domain (493-658) expressed in Escherichia coli BL21 (DE3)
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Bisubstrate Inhibitors of the MYST HATs Esa1 and Tip60.
Wu J, Xie N, Wu Z, Zhang Y, Zheng YG.
Bioorg Med Chem (2009) 17 : 1381 -1386
PubMed 19114310 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.49 5.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL526343 1 5.64
CHEMBL1213327 COENZYME_A 3.0 1 4.38
CHEMBL500256 1 4.27
CHEMBL504265 1 4.23
CHEMBL509144 1 4.22
CHEMBL505605 1 4.18
CHEMBL448227 1 -
CHEMBL505121 1 -
CHEMBL455368 ANACARDIC ACID 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL526343 IC50 = 2270.0 nM 5.64
CHEMBL1213327 COENZYME_A IC50 = 41910.0 nM 4.38
CHEMBL500256 IC50 = 53570.0 nM 4.27
CHEMBL504265 IC50 = 58470.0 nM 4.23
CHEMBL509144 IC50 = 60540.0 nM 4.22
CHEMBL505605 IC50 = 65930.0 nM 4.18
CHEMBL448227 IC50 = 124300.0 nM -
CHEMBL505121 IC50 = 108300.0 nM -
CHEMBL455368 ANACARDIC ACID IC50 = 667050.0 nM -