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Assay Detail

CHEMBL4729574

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

Binding
Inhibition of human HDAC7 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 7 (CHEMBL2716)
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 5.55 5.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4777296 1 5.83
CHEMBL4177129 1 5.71
CHEMBL2179618 NEXTURASTAT A 1 5.61
CHEMBL4759584 1 5.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4777296 IC50 = 1470.0 nM 5.83
CHEMBL4177129 IC50 = 1930.0 nM 5.71
CHEMBL2179618 NEXTURASTAT A IC50 = 2430.0 nM 5.61
CHEMBL4759584 IC50 = 9000.0 nM 5.05