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Assay Detail

CHEMBL3766680

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

Binding
Inhibition of recombinant human HDAC8 by fluorimetry
7
Total Activities
7
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

Design, Synthesis, and Pharmacological Evaluation of Novel N-Acylhydrazone Derivatives as Potent Histone Deacetylase 6/8 Dual Inhibitors.
Rodrigues DA, Ferreira-Silva GÀ, Ferreira AC, Fernandes RA, Kwee JK, Sant'Anna CM, Ionta M, Fraga CA.
J Med Chem (2016) 59 : 655 -670
PubMed 26705137 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.51 7.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3763386 1 7.27
CHEMBL3764728 1 6.96
CHEMBL3763388 1 6.89
CHEMBL3764525 1 6.64
CHEMBL99 TRICHOSTATIN 1.0 1 6.44
CHEMBL3764442 1 5.70
CHEMBL3765502 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3763386 IC50 = 54.0 nM 7.27
CHEMBL3764728 IC50 = 110.0 nM 6.96
CHEMBL3763388 IC50 = 130.0 nM 6.89
CHEMBL3764525 IC50 = 230.0 nM 6.64
CHEMBL99 TRICHOSTATIN IC50 = 360.0 nM 6.44
CHEMBL3764442 IC50 = 2000.0 nM 5.70
CHEMBL3765502 IC50 = 2200.0 nM 5.66