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Assay Detail

CHEMBL4733337

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Binding
Inhibition of N-terminal His-tagged human p300 HAT (1319 to 1710 residues) expressed in Escherichia coli using histone H3 (1 to 21 residues) as substrate
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 p300 (CHEMBL3784)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Current development of CBP/p300 inhibitors in the last decade.
He ZX,Wei BF,Zhang X,Gong YP,Ma LY,Zhao W
Eur J Med Chem (2021) 209 : 112861 -112861
PubMed 33045661 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.25 5.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL106011 1 5.27
CHEMBL1795624 1 5.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL106011 IC50 = 5350.0 nM 5.27
CHEMBL1795624 IC50 = 5920.0 nM 5.23