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Assay Detail

CHEMBL3620703

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

Binding
Inhibition of HDAC8 (unknown origin) using RHK(Ac)K(Ac) fluorogenic acetylated peptide substrate by fluorometric 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 8 (CHEMBL3192)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
Muthyala R, Shin WS, Xie J, Sham YY.
Bioorg Med Chem Lett (2015) 25 : 4320 -4324
PubMed 26264503 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.14 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99 TRICHOSTATIN 1.0 1 6.77
CHEMBL98 VORINOSTAT 4.0 1 6.51
CHEMBL3260857 1 6.01
CHEMBL3260858 1 5.92
CHEMBL3617543 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99 TRICHOSTATIN IC50 = 170.0 nM 6.77
CHEMBL98 VORINOSTAT IC50 = 310.0 nM 6.51
CHEMBL3260857 IC50 = 980.0 nM 6.01
CHEMBL3260858 IC50 = 1200.0 nM 5.92
CHEMBL3617543 IC50 = 3300.0 nM 5.48