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Literature summary for 1.14.99.66 extracted from

  • Duan, Y.; Qin, W.; Suo, F.; Zhai, X.; Guan, Y.; Wang, X.; Zheng, Y.; Liu, H.
    Design, synthesis and in vitro evaluation of stilbene derivatives as novel LSD1 inhibitors for AML therapy (2018), Bioorg. Med. Chem., 26, 6000-6014 .
    View publication on PubMed
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Crystallization (Commentary)

Crystallization (Comment) Organism
molecular docking of inhibitor 3-[(E)-2-[2-(5-fluoro-2-hydroxyphenyl)pyridin-4-yl]ethenyl]N'-hydroxybenzene-1-carboximidamide. Compound can be well docked into the FAD binding site of LSD1 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3-[(E)-2-[2-(5-fluoro-2-hydroxyphenyl)pyridin-4-yl]ethenyl]N'-hydroxybenzene-1-carboximidamide potently inhibits LSD1 in a reversible and FAD competitive manner. Compound is capable of upregulating the expression of the surrogate cellular biomarker CD86 in THP-1 human leukemia cells and shows good inhibition against THP-1 and MOLM-13 cells with IC50 values of 5.76 and 8.34 microM Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
nucleus
-
 Homo sapiens 5634
-

Organism

Organism UniProt Comment Textmining
Homo sapiens O60341
-
-

Source Tissue

Source Tissue Comment Organism Textmining
MOLM-13 cell
-
 Homo sapiens
-
MV-4-11 cell
-
 Homo sapiens
-
THP-1 cell
-
 Homo sapiens
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.283
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 3-[(E)-2-[2-(5-fluoro-2-hydroxyphenyl)pyridin-4-yl]ethenyl]N'-hydroxybenzene-1-carboximidamide