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Assay Detail

CHEMBL4135538

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

Binding
Inhibition of recombinant human full length HDAC1 expressed in baculovirus infected Sf9 insect cells using p53 (379 to 382 residues) derived RHKKAc as substrate preincubated for 5 to 10 mins followed by substrate addition measured after 2 hrs by fluorescence assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase 1 (CHEMBL325)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and Pharmacological Evaluation of Selective Histone Deacetylase 6 Inhibitors in Melanoma Models.
Tavares MT, Shen S, Knox T, Hadley M, Kutil Z, Bařinka C, Villagra A, Kozikowski AP.
ACS Med Chem Lett (2017) 8 : 1031 -1036
PubMed 29057046 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.71 7.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL98 VORINOSTAT 4.0 1 7.51
CHEMBL4166281 1 6.22
CHEMBL4170768 1 6.14
CHEMBL4162826 1 5.56
CHEMBL4177129 1 5.54
CHEMBL4166504 1 5.24
CHEMBL4174193 1 5.21
CHEMBL4167374 1 5.12
CHEMBL4159465 1 4.84
CHEMBL4162010 1 -
CHEMBL4169931 1 -
CHEMBL4165452 1 -
CHEMBL4173367 1 -
CHEMBL4168877 1 -
CHEMBL4176731 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL98 VORINOSTAT IC50 = 31.0 nM 7.51
CHEMBL4166281 IC50 = 604.0 nM 6.22
CHEMBL4170768 IC50 = 721.0 nM 6.14
CHEMBL4162826 IC50 = 2740.0 nM 5.56
CHEMBL4177129 IC50 = 2913.0 nM 5.54
CHEMBL4166504 IC50 = 5740.0 nM 5.24
CHEMBL4174193 IC50 = 6130.0 nM 5.21
CHEMBL4167374 IC50 = 7540.0 nM 5.12
CHEMBL4159465 IC50 = 14400.0 nM 4.84
CHEMBL4162010 IC50 > 30000.0 nM -
CHEMBL4169931 IC50 - -
CHEMBL4165452 IC50 > 30000.0 nM -
CHEMBL4173367 IC50 - -
CHEMBL4168877 IC50 - -
CHEMBL4176731 IC50 - -