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Assay Detail

CHEMBL1799129

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

Binding
Inhibition of human LSD1
6
Total Activities
6
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

Enantioselective synthesis of tranylcypromine analogues as lysine demethylase (LSD1) inhibitors.
Benelkebir H, Hodgkinson C, Duriez PJ, Hayden AL, Bulleid RA, Crabb SJ, Packham G, Ganesan A.
Bioorg Med Chem (2011) 19 : 3709 -3716
PubMed 21382717 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.35 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1795979 1 5.70
CHEMBL1795980 1 5.70
CHEMBL1795981 1 5.70
CHEMBL1795978 1 5.22
CHEMBL1795977 1 5.10
CHEMBL3989843 TRANYLCYPROMINE 4.0 1 4.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1795979 Ki = 2000.0 nM 5.70
CHEMBL1795980 Ki = 2000.0 nM 5.70
CHEMBL1795981 Ki = 2000.0 nM 5.70
CHEMBL1795978 Ki = 6000.0 nM 5.22
CHEMBL1795977 Ki = 8000.0 nM 5.10
CHEMBL3989843 TRANYLCYPROMINE Ki = 21000.0 nM 4.68