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Assay Detail

CHEMBL5135589

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

Binding
Inhibition of recombinant human HDAC6 using ZMAL (Z-(Ac)Lys-AMC as substrate incubated for 20 mins and measured by homogenous fluorescence assay
14
Total Activities
14
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

Identification of histone deacetylase 10 (HDAC10) inhibitors that modulate autophagy in transformed cells.
Zeyen P, Zeyn Y, Herp D, Mahmoudi F, Yesiloglu TZ, Erdmann F, Schmidt M, Robaa D, Romier C, Ridinger J, Herbst-Gervasoni CJ, Christianson DW, Oehme I, Jung M, Krämer OH, Sippl W.
Eur J Med Chem (2022) 234 : 114272 -114272
PubMed 35306288 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.20 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27759 ENTINOSTAT 3.0 1 7.47
CHEMBL5208700 1 6.80
CHEMBL5208990 1 6.75
CHEMBL5181507 1 6.68
CHEMBL5203383 1 6.55
CHEMBL5188463 1 6.37
CHEMBL5184762 1 5.85
CHEMBL5201275 1 5.62
CHEMBL5173958 1 5.43
CHEMBL5184156 1 5.36
CHEMBL5207713 1 5.32
CHEMBL5201544 1 -
CHEMBL5188225 1 -
CHEMBL2018302 TUBASTATIN A 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27759 ENTINOSTAT IC50 = 34.0 nM 7.47
CHEMBL5208700 IC50 = 158.0 nM 6.80
CHEMBL5208990 IC50 = 177.0 nM 6.75
CHEMBL5181507 IC50 = 210.0 nM 6.68
CHEMBL5203383 IC50 = 280.0 nM 6.55
CHEMBL5188463 IC50 = 430.0 nM 6.37
CHEMBL5184762 IC50 = 1400.0 nM 5.85
CHEMBL5201275 IC50 = 2420.0 nM 5.62
CHEMBL5173958 IC50 = 3700.0 nM 5.43
CHEMBL5184156 IC50 = 4400.0 nM 5.36
CHEMBL5207713 IC50 = 4800.0 nM 5.32
CHEMBL5201544 IC50 - -
CHEMBL5188225 IC50 - -
CHEMBL2018302 TUBASTATIN A IC50 - -