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Assay Detail

CHEMBL3776819

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

Binding
Inhibition of GST-tagged human LSD1 (172 to 833 residues) expressed in Escherichia coli C43(DE3) pLysS using biotinylated histone H3 mono methylated K4 peptide as substrate preincubated for 60 mins followed by substrate addition measured after 5 mins by time-resolved 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

Lysine-specific histone demethylase 1A (CHEMBL6136)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Cyclopropanamine Compounds and Use Thereof.
Blass B.
ACS Med Chem Lett (2016) 7 : 10 -11
PubMed 26819657 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.67 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3775312 1 6.75
CHEMBL3774654 1 6.68
CHEMBL3775480 1 6.64
CHEMBL3775248 1 6.62
CHEMBL3775474 1 -
CHEMBL3774809 1 -
CHEMBL3775711 1 -
CHEMBL3775351 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3775312 IC50 = 180.0 nM 6.75
CHEMBL3774654 IC50 = 210.0 nM 6.68
CHEMBL3775480 IC50 = 230.0 nM 6.64
CHEMBL3775248 IC50 = 240.0 nM 6.62
CHEMBL3775474 IC50 < 100.0 nM -
CHEMBL3774809 IC50 < 100.0 nM -
CHEMBL3775711 IC50 < 100.0 nM -
CHEMBL3775351 IC50 < 100.0 nM -