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Assay Detail

CHEMBL4703554

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Binding
Inhibition of LSD1 in human NCI-H1417 cells assessed as suppression of GRP mRNA expression incubated for 12 days by qPCR analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type NCI-H1417
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1).
Kanouni T,Severin C,Cho RW,Yuen NY,Xu J,Shi L,Lai C,Del Rosario JR,Stansfield RK,Lawton LN,Hosfield D,O'Connell S,Kreilein MM,Tavares-Greco P,Nie Z,Kaldor SW,Veal JM,Stafford JA,Chen YK
J Med Chem (2020) 63 : 14522 -14529
PubMed 33034194 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 8.22 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4650360 PULRODEMSTAT BESILATE 2.0 1 8.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4650360 PULRODEMSTAT BESILATE EC50 = 6.0 nM 8.22