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Assay Detail

CHEMBL686829

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

Functional
Concentration required to inhibit the partially purified HDAC enzyme by 50% obtained from H1299 cell lysate
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type H1299
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Histone deacetylase (CHEMBL2093865)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates.
Remiszewski SW, Sambucetti LC, Atadja P, Bair KW, Cornell WD, Green MA, Howell KL, Jung M, Kwon P, Trogani N, Walker H.
J Med Chem (2002) 45 : 753 -757
PubMed 11831887 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.40 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2000089 TRAPOXIN B 1 8.40
CHEMBL99 TRICHOSTATIN 1.0 1 7.00
CHEMBL140000 1 5.79
CHEMBL143047 1 5.66
CHEMBL98 VORINOSTAT 4.0 1 5.14
CHEMBL162423 1 -
CHEMBL165162 1 -
CHEMBL353581 PYROXAMIDE 1.0 1 -
CHEMBL164872 1 -
CHEMBL349015 1 -
CHEMBL57107 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2000089 TRAPOXIN B IC50 = 4.0 nM 8.40
CHEMBL99 TRICHOSTATIN IC50 = 100.0 nM 7.00
CHEMBL140000 IC50 = 1620.0 nM 5.79
CHEMBL143047 IC50 = 2180.0 nM 5.66
CHEMBL98 VORINOSTAT IC50 = 7200.0 nM 5.14
CHEMBL162423 IC50 > 10000.0 nM -
CHEMBL165162 IC50 > 10000.0 nM -
CHEMBL353581 PYROXAMIDE IC50 > 10000.0 nM -
CHEMBL164872 IC50 > 10000.0 nM -
CHEMBL349015 IC50 > 10000.0 nM -
CHEMBL57107 IC50 > 10000.0 nM -