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Assay Detail

CHEMBL5157487

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

Binding
Inhibition of human LSD1 assessed as demethylase activity of LSD1 using Histone H3(1-21)K4me2 peptide as substrate incubated for 30 mins followed by substrate addition by amplex red dye based HRP-coupled assay
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Lysine-specific histone demethylase 1A (CHEMBL6136)
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
Activity 2 - -
EC50 2 5.11 5.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5178014 1 5.22
CHEMBL5191350 1 5.00
CHEMBL5182215 1 -
CHEMBL5200566 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5178014 EC50 = 6000.0 nM 5.22
CHEMBL5191350 EC50 = 10000.0 nM 5.00
CHEMBL5182215 Activity - -
CHEMBL5200566 Activity - -