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Assay Detail

CHEMBL895789

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

Binding
Inhibition of HDAC in HeLa cells assessed as induction of human histone H3 hyperacetylation
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histone deacetylase (CHEMBL2093865)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
Mahboobi S, Sellmer A, Höcher H, Garhammer C, Pongratz H, Maier T, Ciossek T, Beckers T.
J Med Chem (2007) 50 : 4405 -4418
PubMed 17691763 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 5.57 6.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL390452 1 6.54
CHEMBL390907 1 6.00
CHEMBL243809 1 5.96
CHEMBL242533 1 5.89
CHEMBL244885 1 5.59
CHEMBL397904 1 5.58
CHEMBL388429 1 5.57
CHEMBL390910 1 5.56
CHEMBL390908 1 5.53
CHEMBL244670 1 5.42
CHEMBL244887 1 5.39
CHEMBL396559 1 5.37
CHEMBL243181 1 5.24
CHEMBL98 VORINOSTAT 4.0 1 5.18
CHEMBL244040 1 5.16
CHEMBL395976 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL390452 EC50 = 290.0 nM 6.54
CHEMBL390907 EC50 = 1000.0 nM 6.00
CHEMBL243809 EC50 = 1100.0 nM 5.96
CHEMBL242533 EC50 = 1300.0 nM 5.89
CHEMBL244885 EC50 = 2570.0 nM 5.59
CHEMBL397904 EC50 = 2650.0 nM 5.58
CHEMBL388429 EC50 = 2670.0 nM 5.57
CHEMBL390910 EC50 = 2780.0 nM 5.56
CHEMBL390908 EC50 = 2970.0 nM 5.53
CHEMBL244670 EC50 = 3770.0 nM 5.42
CHEMBL244887 EC50 = 4100.0 nM 5.39
CHEMBL396559 EC50 = 4270.0 nM 5.37
CHEMBL243181 EC50 = 5700.0 nM 5.24
CHEMBL98 VORINOSTAT EC50 = 6670.0 nM 5.18
CHEMBL244040 EC50 = 6900.0 nM 5.16
CHEMBL395976 EC50 = 7500.0 nM 5.12