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Literature summary for 3.4.21.21 extracted from

  • Kolesnikov, A.; Rai, R.; Young, W.B.; Mordenti, J.; Liu, L.; Torkelson, S.; Shrader, W.D.; Leahy, E.M.; Hu, H.; Gjerstad, E.; Janc, J.; Katz, B.A.; Sprengeler, P.A.
    Factor VIIa inhibitors: improved pharmacokinetic parameters (2006), Bioorg. Med. Chem. Lett., 16, 2243-2246.
    View publication on PubMed

Application

Application Comment Organism
drug development treatment of thromboembolic disease Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
([5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]methyl)propanedioic acid
-
Rattus norvegicus
2-([5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-5'-fluoro-2',6-dihydroxybiphenyl-3-yl]methyl)butanedioic acid
-
Rattus norvegicus
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-5'-fluoro-2',6-dihydroxybiphenyl-3-yl]butanedioic acid
-
Rattus norvegicus
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]butanedioic acid
-
Rattus norvegicus
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]pentanedioic acid
-
Rattus norvegicus
2-[5-(5-carbamimidoyl-1H-indol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]butanedioic acid
-
Rattus norvegicus
3-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]pentanedioic acid
-
Rattus norvegicus
3-[5-(5-carbamimidoyl-1H-indol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]pentanedioic acid
-
Rattus norvegicus
dimethyl (4-hydroxybenzyl)propanedioate
-
Rattus norvegicus
dimethyl 2-(4-hydroxybenzyl)butanedioate
-
Rattus norvegicus
dimethyl 2-(4-hydroxyphenyl)butanedioate
-
Rattus norvegicus
dimethyl 2-(4-hydroxyphenyl)pentanedioate
-
Rattus norvegicus
dimethyl 3-(4-hydroxyphenyl)pentanedioate
-
Rattus norvegicus
[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-5'-fluoro-2',6-dihydroxybiphenyl-3-yl]acetic acid
-
Rattus norvegicus
[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]acetic acid
-
Rattus norvegicus
[5-(5-carbamimidoyl-1H-indol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]acetic acid
-
Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
factor X + H2O
-
Rattus norvegicus factor Xa
-
?

Synonyms

Synonyms Comment Organism
factor VIIa/tissue factor complex
-
Rattus norvegicus
fVIIa/TF
-
Rattus norvegicus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000001
-
2-[5-(5-carbamimidoyl-1H-indol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]butanedioic acid
-
Rattus norvegicus
0.000002
-
[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-5'-fluoro-2',6-dihydroxybiphenyl-3-yl]acetic acid
-
Rattus norvegicus
0.000003
-
[5-(5-carbamimidoyl-1H-indol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]acetic acid
-
Rattus norvegicus
0.000004
-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-5'-fluoro-2',6-dihydroxybiphenyl-3-yl]butanedioic acid
-
Rattus norvegicus
0.000004
-
2-([5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-5'-fluoro-2',6-dihydroxybiphenyl-3-yl]methyl)butanedioic acid
-
Rattus norvegicus
0.000013
-
3-[5-(5-carbamimidoyl-1H-indol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]pentanedioic acid
-
Rattus norvegicus
0.000015
-
[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]acetic acid
-
Rattus norvegicus
0.000017
-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]pentanedioic acid
-
Rattus norvegicus
0.000021
-
([5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]methyl)propanedioic acid
-
Rattus norvegicus
0.000022
-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]butanedioic acid
-
Rattus norvegicus
0.000036
-
3-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]pentanedioic acid
-
Rattus norvegicus