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Literature summary for 3.4.21.7 extracted from

  • Teno, N.; Gohda, K.; Wanaka, K.; Sueda, T.; Tsuda, Y.
    Identification of novel plasmin inhibitors possessing nitrile moiety as warhead (2011), Bioorg. Med. Chem. Lett., 21, 6305-6309.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
D-Ile-Phe-Lys-CN
-
Homo sapiens
D-Ile-Phe-Lys-NH2
-
Homo sapiens
additional information preparation and analysis of lysine-nitrile derivatives having a trisubstituted benzene for inhibitory activities against plasmin and the highly homologous plasma kallikrein and urokinase. Development of specific and selective inhibitors based on 9, overview. No inhibition by N-[(1S)-5-amino-1-cyanopentyl]-3-([3-[1-(4-fluorobenzyl)-1H-indol-3-yl]propanoyl]amino)-4-methoxybenzamide Homo sapiens
N-[(1S)-5-amino-1-cyanopentyl]-3-([3-[1-(4-fluorobenzyl)-1H-indol-3-yl]propanoyl]amino)-4-(pyridin-4-ylmethoxy)benzamide molecular modeling Homo sapiens
N-[(1S)-5-amino-1-cyanopentyl]-3-[(naphthalen-1-ylacetyl)amino]-4-(pyridin-4-ylmethoxy)benzamide
-
Homo sapiens
N-[(1S)-5-amino-1-cyanopentyl]-3-[(naphthalen-2-ylacetyl)amino]-4-(pyridin-4-ylmethoxy)benzamide
-
Homo sapiens
N-[(1S)-5-amino-1-cyanopentyl]-3-[[(4-fluorophenyl)acetyl]amino]-4-(pyridin-4-ylmethoxy)benzamide
-
Homo sapiens
N-[(1S)-5-amino-1-cyanopentyl]-3-[[3-(1H-indol-3-yl)propanoyl]amino]-4-(pyridin-4-ylmethoxy)benzamide
-
Homo sapiens
N-[(1S)-5-amino-1-cyanopentyl]-4-(pyridin-4-ylmethoxy)benzamide
-
Homo sapiens
tert-butyl 3-(3-[[5-[[(1S)-5-amino-1-cyanopentyl]carbamoyl]-2-(pyridin-4-ylmethoxy)phenyl]amino]-3-oxopropyl)-1H-indole-1-carboxylate
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.078
-
pH and temperature not specified in the publication Homo sapiens D-Ile-Phe-Lys-CN
0.14
-
pH and temperature not specified in the publication Homo sapiens N-[(1S)-5-amino-1-cyanopentyl]-3-([3-[1-(4-fluorobenzyl)-1H-indol-3-yl]propanoyl]amino)-4-(pyridin-4-ylmethoxy)benzamide
0.22
-
pH and temperature not specified in the publication Homo sapiens N-[(1S)-5-amino-1-cyanopentyl]-3-[(naphthalen-2-ylacetyl)amino]-4-(pyridin-4-ylmethoxy)benzamide
0.22
-
pH and temperature not specified in the publication Homo sapiens tert-butyl 3-(3-[[5-[[(1S)-5-amino-1-cyanopentyl]carbamoyl]-2-(pyridin-4-ylmethoxy)phenyl]amino]-3-oxopropyl)-1H-indole-1-carboxylate
0.24
-
pH and temperature not specified in the publication Homo sapiens N-[(1S)-5-amino-1-cyanopentyl]-4-(pyridin-4-ylmethoxy)benzamide
0.29
-
pH and temperature not specified in the publication Homo sapiens D-Ile-Phe-Lys-NH2
0.37
-
pH and temperature not specified in the publication Homo sapiens N-[(1S)-5-amino-1-cyanopentyl]-3-[[3-(1H-indol-3-yl)propanoyl]amino]-4-(pyridin-4-ylmethoxy)benzamide
0.57
-
pH and temperature not specified in the publication Homo sapiens N-[(1S)-5-amino-1-cyanopentyl]-3-[(naphthalen-1-ylacetyl)amino]-4-(pyridin-4-ylmethoxy)benzamide
0.59
-
pH and temperature not specified in the publication Homo sapiens N-[(1S)-5-amino-1-cyanopentyl]-3-[[(4-fluorophenyl)acetyl]amino]-4-(pyridin-4-ylmethoxy)benzamide