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Literature summary for 1.14.99.66 extracted from
- Histone H3 peptides incorporating modified lysine residues as lysine-specific demethylase 1 inhibitors (2018), Bioorg. Med. Chem. Lett., 28, 167-169 .
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| additional information | trans-2-phenylcyclopropylamine-modified peptides containing a longer side chain, which can react with FAD in the active site, are potent LSD1-selective inhibitors | Homo sapiens | |
| PCPA-Lys-4 H3-11 | 11-mer histone H3 peptide because the 11-mer bearing a trans-2-phenylcyclopropylamine moiety at Lys-4 | Homo sapiens |  |
| PCPA-Orn-4 H3-11 | 11-mer histone H3 peptide because the 11-mer bearing a trans-2-phenylcyclopropylamine moiety at Orn-4 | Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | O60341 | - |
- |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| FAD | - |
Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.000154 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | PCPA-Lys-4 H3-11 | |
| 0.00018 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | PCPA-Orn-4 H3-11 | |
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