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Literature summary for 3.4.21.5 extracted from

  • Hanessian, S.; Simard, D.; Bayrakdarian, M.; Therrien, E.; Nilsson, I.; Fjellstroem, O.
    Design, synthesis, and thrombin-inhibitory activity of pyridin-2-ones as P2/P3 core motifs (2008), Bioorg. Med. Chem. Lett., 18, 1972-1976.
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
N-(4-carbamimidoylbenzyl)-2-(1-[[(4-chloro-2-methoxyphenyl)sulfonyl]amino]-4-methyl-2-oxo-1,2-dihydropyridin-3-yl)acetamide 13fold selectivity for thrombim over trypsin Homo sapiens
N-(4-carbamimidoylbenzyl)-2-(1-[[2-(2,5-dimethylphenyl)ethyl]amino]-4-methyl-2-oxo-1,2-dihydropyridin-3-yl)acetamide 23fold selectivity for thrombim over trypsin Homo sapiens
N-(4-carbamimidoylbenzyl)-2-(4-methyl-1-[[2-(2-methylphenyl)ethyl]amino]-2-oxo-1,2-dihydropyridin-3-yl)acetamide 42fold selectivity for thrombim over trypsin Homo sapiens
N-(4-carbamimidoylbenzyl)-2-[4-methyl-2-oxo-1-[(2-phenylethyl)amino]-1,2-dihydropyridin-3-yl]acetamide 16fold selectivity for thrombim over trypsin Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.023
-
-
 Homo sapiens N-(4-carbamimidoylbenzyl)-2-(4-methyl-1-[[2-(2-methylphenyl)ethyl]amino]-2-oxo-1,2-dihydropyridin-3-yl)acetamide
0.091
-
-
 Homo sapiens N-(4-carbamimidoylbenzyl)-2-[4-methyl-2-oxo-1-[(2-phenylethyl)amino]-1,2-dihydropyridin-3-yl]acetamide
0.092
-
-
 Homo sapiens N-(4-carbamimidoylbenzyl)-2-(1-[[2-(2,5-dimethylphenyl)ethyl]amino]-4-methyl-2-oxo-1,2-dihydropyridin-3-yl)acetamide
0.307
-
-
 Homo sapiens N-(4-carbamimidoylbenzyl)-2-(1-[[(4-chloro-2-methoxyphenyl)sulfonyl]amino]-4-methyl-2-oxo-1,2-dihydropyridin-3-yl)acetamide