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Assay Detail

CHEMBL4606193

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

Binding
Inhibition of HDAC1 in human MM96L cells assessed as activation of histone H4 acetylation at Lys5, Lys8, Lys12 and Lys16 residues by Western blot analysis
5
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MM96L
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Achiral Derivatives of Hydroxamate AR-42 Potently Inhibit Class I HDAC Enzymes and Cancer Cell Proliferation.
Tng J, Lim J, Wu KC, Lucke AJ, Xu W, Reid RC, Fairlie DP.
J Med Chem (2020) 63 : 5956 -5971
PubMed 32383881 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 6.22 6.70
Inhibition 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4642874 2 6.70
CHEMBL4634521 2 6.22
CHEMBL191091 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4642874 EC50 = 200.0 nM 6.70
CHEMBL4634521 EC50 = 600.0 nM 6.22
CHEMBL191091 EC50 = 1800.0 nM 5.75
CHEMBL4634521 Inhibition - % -
CHEMBL4642874 Inhibition - % -