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Assay Detail

CHEMBL5157486

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

Binding
Inhibition of human HDAC8 (379 to 382 residues) using RHKKAcKAc-AMC fluorogenic peptide as substrate by fluorescence assay
8
Total Activities
8
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

<i>N</i>-Methylpropargylamine-Conjugated Hydroxamic Acids as Dual Inhibitors of Monoamine Oxidase A and Histone Deacetylase for Glioma Treatment.
Mehndiratta S, Qian B, Chuang JY, Liou JP, Shih JC.
J Med Chem (2022) 65 : 2208 -2224
PubMed 35005974 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.24 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5170598 1 7.30
CHEMBL5191350 1 7.10
CHEMBL5182215 1 6.48
CHEMBL5187984 1 5.95
CHEMBL5178014 1 5.93
CHEMBL5193384 1 5.83
CHEMBL5177240 1 5.75
CHEMBL5200566 1 5.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5170598 IC50 = 50.0 nM 7.30
CHEMBL5191350 IC50 = 80.0 nM 7.10
CHEMBL5182215 IC50 = 330.0 nM 6.48
CHEMBL5187984 IC50 = 1120.0 nM 5.95
CHEMBL5178014 IC50 = 1170.0 nM 5.93
CHEMBL5193384 IC50 = 1470.0 nM 5.83
CHEMBL5177240 IC50 = 1780.0 nM 5.75
CHEMBL5200566 IC50 = 2480.0 nM 5.61