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Assay Detail

CHEMBL5339141

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

Binding
Inhibition of LSD1 (unknown origin)
4
Total Activities
4
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

Design, synthesis, and structure-activity relationship of TAK-418 and its derivatives as a novel series of LSD1 inhibitors with lowered risk of hematological side effects.
Hattori Y, Matsumoto S, Morimoto S, Daini M, Toyofuku M, Matsuda S, Baba R, Murakami K, Iwatani M, Oki H, Iwasaki S, Matsumiya K, Tominari Y, Kimura H, Ito M.
Eur J Med Chem (2022) 239 : 114522 -114522
PubMed 35749987 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.73 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5433883 1 9.00
CHEMBL5439167 1 8.85
CHEMBL5286191 1 8.54
CHEMBL3775474 1 8.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5433883 IC50 = 1.0 nM 9.00
CHEMBL5439167 IC50 = 1.4 nM 8.85
CHEMBL5286191 IC50 = 2.9 nM 8.54
CHEMBL3775474 IC50 = 2.9 nM 8.54