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Assay Detail

CHEMBL4619650

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

Binding
Inhibition of N-terminal His-tagged full length human HDAC8 expressed in baculovirus expression system using FAM-RHKK(TF-Ac)-NH2 substrate incubated for 3 hrs by EMSA method
28
Total Activities
28
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

Characterization of Conformationally Constrained Benzanilide Scaffolds for Potent and Selective HDAC8 Targeting.
Hassan MM, Israelian J, Nawar N, Ganda G, Manaswiyoungkul P, Raouf YS, Armstrong D, Sedighi A, Olaoye OO, Erdogan F, Cabral AD, Angeles F, Altintas R, de Araujo ED, Gunning PT.
J Med Chem (2020) 63 : 8634 -8648
PubMed 32672458 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 6.92 8.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2170177 1 8.39
CHEMBL4642821 1 7.63
CHEMBL4638377 1 7.47
CHEMBL4640819 1 7.26
CHEMBL4641613 1 7.21
CHEMBL4643684 1 7.19
CHEMBL4649867 1 7.18
CHEMBL4637798 1 7.18
CHEMBL4642047 1 7.10
CHEMBL4649514 1 7.08
CHEMBL4649651 1 7.05
CHEMBL4642398 1 6.97
CHEMBL4637226 1 6.94
CHEMBL4638505 1 6.92
CHEMBL4643791 1 6.89
CHEMBL4634713 1 6.65
CHEMBL4640205 1 6.58
CHEMBL4640536 1 6.51
CHEMBL4641253 1 6.32
CHEMBL4641390 1 6.19
CHEMBL4636672 1 6.17
CHEMBL4633998 1 6.14
CHEMBL4633453 1 6.08
CHEMBL4646090 1 -
CHEMBL4637127 1 -
CHEMBL4639383 1 -
CHEMBL4644653 1 -
CHEMBL4639051 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2170177 IC50 = 4.03 nM 8.39
CHEMBL4642821 IC50 = 23.4 nM 7.63
CHEMBL4638377 IC50 = 33.7 nM 7.47
CHEMBL4640819 IC50 = 55.3 nM 7.26
CHEMBL4641613 IC50 = 62.3 nM 7.21
CHEMBL4643684 IC50 = 65.1 nM 7.19
CHEMBL4649867 IC50 = 65.5 nM 7.18
CHEMBL4637798 IC50 = 66.0 nM 7.18
CHEMBL4642047 IC50 = 79.8 nM 7.10
CHEMBL4649514 IC50 = 83.5 nM 7.08
CHEMBL4649651 IC50 = 88.5 nM 7.05
CHEMBL4642398 IC50 = 107.0 nM 6.97
CHEMBL4637226 IC50 = 116.0 nM 6.94
CHEMBL4638505 IC50 = 119.0 nM 6.92
CHEMBL4643791 IC50 = 129.0 nM 6.89
CHEMBL4634713 IC50 = 225.0 nM 6.65
CHEMBL4640205 IC50 = 264.0 nM 6.58
CHEMBL4640536 IC50 = 308.0 nM 6.51
CHEMBL4641253 IC50 = 478.0 nM 6.32
CHEMBL4641390 IC50 = 648.0 nM 6.19
CHEMBL4636672 IC50 = 682.0 nM 6.17
CHEMBL4633998 IC50 = 723.0 nM 6.14
CHEMBL4633453 IC50 = 823.0 nM 6.08
CHEMBL4646090 IC50 > 2000.0 nM -
CHEMBL4637127 IC50 > 1000.0 nM -
CHEMBL4639383 IC50 > 1000.0 nM -
CHEMBL4644653 IC50 > 1000.0 nM -
CHEMBL4639051 IC50 > 1000.0 nM -