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Assay Detail

CHEMBL4433654

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

Binding
Inhibition of human recombinant his tagged HDAC1 expressed in baculovirus infected Sf6 insect cells using tertbutyloxycarbonyl (Boc)-(Ac)-Lys-7-amino-4-methylcoumarin as substrate incubated for 1 hr by fluorescence based assay
5
Total Activities
5
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 deacetylase 1 (CHEMBL325)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of the First-in-Class GSK-3β/HDAC Dual Inhibitor as Disease-Modifying Agent To Combat Alzheimer's Disease.
De Simone A, La Pietra V, Betari N, Petragnani N, Conte M, Daniele S, Pietrobono D, Martini C, Petralla S, Casadei R, Davani L, Frabetti F, Russomanno P, Novellino E, Montanari S, Tumiatti V, Ballerini P, Sarno F, Nebbioso A, Altucci L, Monti B, Andrisano V, Milelli A.
ACS Med Chem Lett (2019) 10 : 469 -474
PubMed 30996781 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.32 5.65

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4590543 1 5.65
CHEMBL4443876 1 5.43
CHEMBL4575045 1 5.30
CHEMBL4449010 1 4.89
CHEMBL322970 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4590543 IC50 = 2240.0 nM 5.65
CHEMBL4443876 IC50 = 3750.0 nM 5.43
CHEMBL4575045 IC50 = 5020.0 nM 5.30
CHEMBL4449010 IC50 = 12780.0 nM 4.89
CHEMBL322970 IC50 - -