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Assay Detail

CHEMBL4158660

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 baculovirus infected Sf9 insect cells using Z(Ac)Lys-AMC as substrate by fluorometric method
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

Characterization of Histone Deacetylase 8 (HDAC8) Selective Inhibition Reveals Specific Active Site Structural and Functional Determinants.
Marek M, Shaik TB, Heimburg T, Chakrabarti A, Lancelot J, Ramos-Morales E, Da Veiga C, Kalinin D, Melesina J, Robaa D, Schmidtkunz K, Suzuki T, Holl R, Ennifar E, Pierce RJ, Jung M, Sippl W, Romier C.
J Med Chem (2018) 61 : 10000 -10016
PubMed 30347148 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.80 7.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4160522 1 7.28
CHEMBL2170177 1 4.32
CHEMBL4176696 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4160522 IC50 = 53.0 nM 7.28
CHEMBL2170177 IC50 = 48200.0 nM 4.32
CHEMBL4176696 IC50 - -