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Assay Detail

CHEMBL3860985

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

ADMET
Inhibition of full length recombinant human HDAC2 expressed in baculovirus infected Sf9 cells using RHKK-Ac as substrate by fluorescence analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histone deacetylase 2 (CHEMBL1937)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
Rabal O, Sánchez-Arias JA, Cuadrado-Tejedor M, de Miguel I, Pérez-González M, García-Barroso C, Ugarte A, Estella-Hermoso de Mendoza A, Sáez E, Espelosin M, Ursua S, Haizhong T, Wei W, Musheng X, Garcia-Osta A, Oyarzabal J.
J Med Chem (2016) 59 : 8967 -9004
PubMed 27606546 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 9.48 9.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2105763 QUISINOSTAT 2.0 1 9.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2105763 QUISINOSTAT IC50 = 0.33 nM 9.48