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Assay Detail

CHEMBL4331295

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

Binding
Inhibition of human full-length recombinant HDAC6 expressed in baculovirus infected Sf9 insect cells using Boc-Lys (Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence assay
3
Total Activities
3
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 6 (CHEMBL1865)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Quinazolin-2,4-dione-Based Hydroxamic Acids as Selective Histone Deacetylase-6 Inhibitors for Treatment of Non-Small Cell Lung Cancer.
Yu CW, Hung PY, Yang HT, Ho YH, Lai HY, Cheng YS, Chern JW.
J Med Chem (2019) 62 : 857 -874
PubMed 30525585 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 8.52 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4554270 1 8.68
CHEMBL2018302 TUBASTATIN A 1 8.46
CHEMBL4438057 1 8.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4554270 Ki = 2.1 nM 8.68
CHEMBL2018302 TUBASTATIN A Ki = 3.43 nM 8.46
CHEMBL4438057 Ki = 3.89 nM 8.41