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Assay Detail

CHEMBL4812299

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

Binding
Inhibition of N-terminal GST-tagged full-length human HDAC6 expressed in Sf9 infected baculovirus system using FTS as substrate preincubated for 10 mins followed by substrate addition and measured for 30 mins
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

Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction.
Guo Z, Zhang Z, Zhang Y, Wang G, Huang Z, Zhang Q, Li J.
Eur J Med Chem (2021) 218 : 113383 -113383
PubMed 33799069 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.20 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3655950 1 8.77
CHEMBL3655978 1 8.12
CHEMBL2018302 TUBASTATIN A 1 7.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3655950 IC50 = 1.7 nM 8.77
CHEMBL3655978 IC50 = 7.5 nM 8.12
CHEMBL2018302 TUBASTATIN A IC50 = 18.9 nM 7.72