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Assay Detail

CHEMBL3379494

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

Binding
Inhibition of HDAC-mediated histone H4 deacetylation in human NCI-H460 cells after 3 hrs by Western blot analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type NCI-H460
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Histone deacetylase (CHEMBL2093865)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

ST7612AA1, a thioacetate-ω(γ-lactam carboxamide) derivative selected from a novel generation of oral HDAC inhibitors.
Giannini G, Vesci L, Battistuzzi G, Vignola D, Milazzo FM, Guglielmi MB, Barbarino M, Santaniello M, Fantò N, Mor M, Rivara S, Pala D, Taddei M, Pisano C, Cabri W.
J Med Chem (2014) 57 : 8358 -8377
PubMed 25233084 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.60 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3353926 1 8.30
CHEMBL3356948 1 7.51
CHEMBL3356940 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3353926 IC50 = 5.0 nM 8.30
CHEMBL3356948 IC50 = 31.0 nM 7.51
CHEMBL3356940 IC50 = 100.0 nM 7.00