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Assay Detail

CHEMBL4253684

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Binding
Inhibition of LSD1 (unknown origin)
14
Total Activities
14
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

Structure-activity studies on N-Substituted tranylcypromine derivatives lead to selective inhibitors of lysine specific demethylase 1 (LSD1) and potent inducers of leukemic cell differentiation.
Schulz-Fincke J, Hau M, Barth J, Robaa D, Willmann D, Kürner A, Haas J, Greve G, Haydn T, Fulda S, Lübbert M, Lüdeke S, Berg T, Sippl W, Schüle R, Jung M.
Eur J Med Chem (2018) 144 : 52 -67
PubMed 29247860 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.44 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3104250 1 7.89
CHEMBL3926080 1 7.75
CHEMBL4289507 1 7.70
CHEMBL3651585 1 7.16
CHEMBL4291413 1 7.05
CHEMBL4284293 1 7.05
CHEMBL4290752 1 7.01
CHEMBL3415352 1 6.19
CHEMBL3621615 1 5.92
CHEMBL3775735 1 5.77
CHEMBL1797705 1 5.72
CHEMBL4285048 1 5.43
CHEMBL257990 (+)-TRANYLCYPROMINE 1 5.20
CHEMBL2426136 NAMOLINE 1 4.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3104250 IC50 = 13.0 nM 7.89
CHEMBL3926080 IC50 = 18.0 nM 7.75
CHEMBL4289507 IC50 = 20.0 nM 7.70
CHEMBL3651585 IC50 = 70.0 nM 7.16
CHEMBL4291413 IC50 = 90.0 nM 7.05
CHEMBL4284293 IC50 = 90.0 nM 7.05
CHEMBL4290752 IC50 = 98.0 nM 7.01
CHEMBL3415352 IC50 = 650.0 nM 6.19
CHEMBL3621615 IC50 = 1200.0 nM 5.92
CHEMBL3775735 IC50 = 1700.0 nM 5.77
CHEMBL1797705 IC50 = 1900.0 nM 5.72
CHEMBL4285048 IC50 = 3700.0 nM 5.43
CHEMBL257990 (+)-TRANYLCYPROMINE IC50 = 6300.0 nM 5.20
CHEMBL2426136 NAMOLINE IC50 = 51000.0 nM 4.29