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Assay Detail

CHEMBL2173253

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

Binding
Inhibition of N terminal hexahistidine-tag recombinant human LSD1 expressed in Escherichia coli BL21 (DE3) using histone H3 peptide as substrate preincubated for 5 mins before substrate addition measured for 30 mins by microplate reader analysis
4
Total Activities
2
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

Oncoepigenomics: making histone lysine methylation count.
Decarlo D, Hadden MK.
Eur J Med Chem (2012) 56 : 179 -194
PubMed 22975593 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.66 5.72
Ki 2 5.38 5.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1215658 2 5.72
CHEMBL1797639 2 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1215658 IC50 = 1900.0 nM 5.72
CHEMBL1797639 IC50 = 2500.0 nM 5.60
CHEMBL1215658 Ki = 3100.0 nM 5.51
CHEMBL1797639 Ki = 5700.0 nM 5.24