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Literature summary for 3.4.21.5 extracted from

  • Ilas, J.; Tomasic, T.; Kikelj, D.
    Novel potent and selective thrombin inhibitors based on a central 1,4-benzoxazin-3(4H)-one scaffold (2008), J. Med. Chem., 51, 2863-2867.
    View publication on PubMed
Search for more literature for 3.4.21.5

Inhibitors

Inhibitors Comment Organism Structure
3-(benzyl(2-(4-carbamimidoylbenzyl)-4-methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-7-yl)amino)-3-oxopropanoic acid 112400fold selectivity for thrombin over trypsin, 52450fold selectivitiy for thrombin over factor Xa Homo sapiens
3-(benzyl(2-(4-carbamimidoylbenzyl)-4-methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-7-yl)amino)-4-oxobutanoic acid 1131fold selectivity for thrombin over trypsin, 2427fold selectivitiy for thrombin over factor Xa Homo sapiens
ethyl 2-(benzyl(2-(4-carbamimidoylbenzyl)-4-methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-7-yl)amino)-2-oxoacetate 1188fold selectivity for thrombin over trypsin, 537fold selectivitiy for thrombin over factor Xa Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000026
-
 3-(benzyl(2-(4-carbamimidoylbenzyl)-4-methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-7-yl)amino)-3-oxopropanoic acid
-
 Homo sapiens
0.0000036
-
 ethyl 2-(benzyl(2-(4-carbamimidoylbenzyl)-4-methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-7-yl)amino)-2-oxoacetate
-
 Homo sapiens
0.0000065
-
 3-(benzyl(2-(4-carbamimidoylbenzyl)-4-methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-7-yl)amino)-4-oxobutanoic acid
-
 Homo sapiens