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Assay Detail

CHEMBL5036493

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

Binding
Inhibition of recombinant HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based assay
23
Total Activities
12
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

Melatonin- and Ferulic Acid-Based HDAC6 Selective Inhibitors Exhibit Pronounced Immunomodulatory Effects <i>In Vitro</i> and Neuroprotective Effects in a Pharmacological Alzheimer's Disease Mouse Model.
He F, Chou CJ, Scheiner M, Poeta E, Yuan Chen N, Gunesch S, Hoffmann M, Sotriffer C, Monti B, Maurice T, Decker M.
J Med Chem (2021) 64 : 3794 -3812
PubMed 33769811 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.43 8.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2364628 RICOLINOSTAT 2.0 1 8.33
CHEMBL5076794 2 7.95
CHEMBL5090786 2 7.72
CHEMBL141502 2 7.67
CHEMBL5080111 2 7.59
CHEMBL5072502 2 7.51
CHEMBL5070312 2 7.47
CHEMBL5081920 2 7.28
CHEMBL5092272 2 7.27
CHEMBL5092694 2 7.24
CHEMBL5078976 2 7.16
CHEMBL5087002 2 6.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2364628 RICOLINOSTAT IC50 = 4.7 nM 8.33
CHEMBL5076794 IC50 = 11.2 nM 7.95
CHEMBL5076794 IC50 = 11.22 nM 7.95
CHEMBL5090786 IC50 = 19.1 nM 7.72
CHEMBL5090786 IC50 = 19.05 nM 7.72
CHEMBL141502 IC50 = 21.4 nM 7.67
CHEMBL141502 IC50 = 21.38 nM 7.67
CHEMBL5080111 IC50 = 25.7 nM 7.59
CHEMBL5080111 IC50 = 25.6 nM 7.59
CHEMBL5072502 IC50 = 30.9 nM 7.51
CHEMBL5072502 IC50 = 30.7 nM 7.51
CHEMBL5070312 IC50 = 33.7 nM 7.47
CHEMBL5070312 IC50 = 33.88 nM 7.47
CHEMBL5081920 IC50 = 52.3 nM 7.28
CHEMBL5081920 IC50 = 52.48 nM 7.28
CHEMBL5092272 IC50 = 53.2 nM 7.27
CHEMBL5092272 IC50 = 53.7 nM 7.27
CHEMBL5092694 IC50 = 57.0 nM 7.24
CHEMBL5092694 IC50 = 57.54 nM 7.24
CHEMBL5078976 IC50 = 69.18 nM 7.16
CHEMBL5078976 IC50 = 68.8 nM 7.16
CHEMBL5087002 IC50 = 353.0 nM 6.45
CHEMBL5087002 IC50 = 354.81 nM 6.45