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Assay Detail

CHEMBL4193702

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

Binding
Inhibition of recombinant HDAC8 (unknown origin) expressed in Escherichia coli using fluor de Lys(R) as substrate pretreated for 5 mins followed by substrate addition measured after 35 mins by fluorescence assay
21
Total Activities
21
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 8 (CHEMBL3192)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, Synthesis, and Biological Evaluation of Tetrahydroisoquinoline-Based Histone Deacetylase 8 Selective Inhibitors.
Taha TY, Aboukhatwa SM, Knopp RC, Ikegaki N, Abdelkarim H, Neerasa J, Lu Y, Neelarapu R, Hanigan TW, Thatcher GRJ, Petukhov PA.
ACS Med Chem Lett (2017) 8 : 824 -829
PubMed 28835796 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.18 8.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2170177 1 8.18
CHEMBL4209843 1 7.36
CHEMBL4208780 1 7.26
CHEMBL4218293 1 7.09
CHEMBL4206571 1 6.96
CHEMBL4214404 1 6.72
CHEMBL4218825 1 6.68
CHEMBL4213891 1 6.47
CHEMBL4206987 1 6.41
CHEMBL4211873 1 6.32
CHEMBL4210933 1 6.02
CHEMBL4208365 1 5.85
CHEMBL4208901 1 5.75
CHEMBL4213297 1 5.72
CHEMBL4217705 1 5.72
CHEMBL4212751 1 5.40
CHEMBL4209492 1 5.17
CHEMBL4216233 1 5.00
CHEMBL4206055 1 4.72
CHEMBL4204967 1 4.72
CHEMBL4078522 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2170177 IC50 = 6.6 nM 8.18
CHEMBL4209843 IC50 = 44.0 nM 7.36
CHEMBL4208780 IC50 = 55.0 nM 7.26
CHEMBL4218293 IC50 = 82.0 nM 7.09
CHEMBL4206571 IC50 = 110.0 nM 6.96
CHEMBL4214404 IC50 = 190.0 nM 6.72
CHEMBL4218825 IC50 = 210.0 nM 6.68
CHEMBL4213891 IC50 = 340.0 nM 6.47
CHEMBL4206987 IC50 = 390.0 nM 6.41
CHEMBL4211873 IC50 = 480.0 nM 6.32
CHEMBL4210933 IC50 = 950.0 nM 6.02
CHEMBL4208365 IC50 = 1400.0 nM 5.85
CHEMBL4208901 IC50 = 1800.0 nM 5.75
CHEMBL4213297 IC50 = 1900.0 nM 5.72
CHEMBL4217705 IC50 = 1900.0 nM 5.72
CHEMBL4212751 IC50 = 4000.0 nM 5.40
CHEMBL4209492 IC50 = 6700.0 nM 5.17
CHEMBL4216233 IC50 = 10000.0 nM 5.00
CHEMBL4206055 IC50 = 19000.0 nM 4.72
CHEMBL4204967 IC50 = 19000.0 nM 4.72
CHEMBL4078522 IC50 > 100000.0 nM -