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Assay Detail

CHEMBL5378688

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

Binding
Inhibition of full length recombinant human HDAC3 expressed in Sf9 cells using 6-carboxyfluorescein peptide as substrate preincubated with compound for 6 hrs followed by substrate addition and measured after 3 hrs by electrophoretic mobility shift assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase 3 (CHEMBL1829)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of YSR734: A Covalent HDAC Inhibitor with Cellular Activity in Acute Myeloid Leukemia and Duchenne Muscular Dystrophy.
Raouf YS, Sedighi A, Geletu M, Frere GA, Allan RG, Nawar N, de Araujo ED, Gunning PT.
J Med Chem (2023) 66 : 16658 -16679
PubMed 38060537 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.25 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27759 ENTINOSTAT 3.0 1 7.46
CHEMBL5412725 1 7.44
CHEMBL5411315 1 6.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27759 ENTINOSTAT IC50 = 35.0 nM 7.46
CHEMBL5412725 IC50 = 36.0 nM 7.44
CHEMBL5411315 IC50 = 143.0 nM 6.84