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Assay Detail

CHEMBL4729575

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

Binding
Inhibition of human HDAC8 expressed in HEK293/T17 cells pre-incubated for 10 mins before Boc-Lys(TFA)-AM substrate addition and measured after 30 mins by fluorescence-based assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase 8 (CHEMBL3192)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Rational Design of Suprastat: A Novel Selective Histone Deacetylase 6 Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models.
Noonepalle S,Shen S,Ptáček J,Tavares MT,Zhang G,Stránský J,Pavlíček J,Ferreira GM,Hadley M,Pelaez G,Bařinka C,Kozikowski AP,Villagra A
J Med Chem (2020) 63 : 10246 -10262
PubMed 32815366 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.21 6.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4177129 1 6.32
CHEMBL4777296 1 6.30
CHEMBL4759584 1 6.21
CHEMBL2179618 NEXTURASTAT A 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4177129 IC50 = 478.0 nM 6.32
CHEMBL4777296 IC50 = 498.0 nM 6.30
CHEMBL4759584 IC50 = 614.0 nM 6.21
CHEMBL2179618 NEXTURASTAT A IC50 = 988.0 nM 6.00