Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4158667

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

Binding
Inhibition of human His-thioredoxin-tagged HDAC8 mL6/L179I mutant expressed in Escherichia coli BL21 (DE3) cells using Fluor de Lys (R)-HDAC8 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
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Histone deacetylase 8 (CHEMBL3192)
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 6.30 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2105763 QUISINOSTAT 2.0 1 6.77
CHEMBL2178342 1 6.13
CHEMBL2170177 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2105763 QUISINOSTAT IC50 = 169.0 nM 6.77
CHEMBL2178342 IC50 = 746.0 nM 6.13
CHEMBL2170177 IC50 = 1000.0 nM 6.00