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Assay Detail

CHEMBL904249

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Binding
Inhibition of GST-p300 HAT assessed as histone acetylation
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Histone acetyltransferase p300 (CHEMBL3784)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Cinnamoyl compounds as simple molecules that inhibit p300 histone acetyltransferase.
Costi R, Di Santo R, Artico M, Miele G, Valentini P, Novellino E, Cereseto A.
J Med Chem (2007) 50 : 1973 -1977
PubMed 17348637 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 4.70 5.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL222328 1 5.30
CHEMBL222573 1 4.68
CHEMBL221782 1 4.48
CHEMBL129964 1 4.34
CHEMBL222543 1 -
CHEMBL129148 1 -
CHEMBL17205 CYCLOVALONE 2.0 1 -
CHEMBL140 CURCUMIN 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL222328 IC50 = 5000.0 nM 5.30
CHEMBL222573 IC50 = 21000.0 nM 4.68
CHEMBL221782 IC50 = 33000.0 nM 4.48
CHEMBL129964 IC50 = 46000.0 nM 4.34
CHEMBL222543 IC50 = 168000.0 nM -
CHEMBL129148 IC50 = 233000.0 nM -
CHEMBL17205 CYCLOVALONE IC50 = 111000.0 nM -
CHEMBL140 CURCUMIN IC50 > 400000.0 nM -