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Assay Detail

CHEMBL4628105

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

Binding
Inhibition of human recombinant HDAC6 using fluorogenic HDAC substrate 3 preincubated for 30 mins followed by substrate addition and measured after 15 mins by fluorogenic assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histone deacetylase 6 (CHEMBL1865)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity.
Wu B, Fathi S, Mortley S, Mohiuddin M, Jang YC, Oyelere AK.
Bioorg Med Chem (2020) 28 : 115345 -115345
PubMed 32061484 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.30 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4635479 1 7.77
CHEMBL4636452 1 7.68
CHEMBL98 VORINOSTAT 4.0 1 7.47
CHEMBL4649487 1 7.34
CHEMBL4634096 1 7.14
CHEMBL4633409 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4635479 IC50 = 17.0 nM 7.77
CHEMBL4636452 IC50 = 21.0 nM 7.68
CHEMBL98 VORINOSTAT IC50 = 34.0 nM 7.47
CHEMBL4649487 IC50 = 46.0 nM 7.34
CHEMBL4634096 IC50 = 73.0 nM 7.14
CHEMBL4633409 IC50 = 400.0 nM 6.40