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Literature summary for 3.4.21.21 extracted from

  • Parlow, J.J.; Stevens, A.M.; Stegeman, R.A.; Stallings, W.C.; Kurumbail, R.G.; South, M.S.
    Synthesis and crystal structures of substituted benzenes and benzoquinones as tissue factor VIIa inhibitors (2003), J. Med. Chem., 46, 4297-4312.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
sitting-drop vapour-diffusion method Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-(3'-amino-3-fluoro-4-(isopropylamino)-1,1'-biphenyl-2-yl)-N-(4-(amino(imino)methyl)benzyl)acetamide IC50: 340 nM Homo sapiens
2-(3'-amino-4-(benzylamino)-3-fluoro-1,1'-biphenyl-2-yl)-N-(4-(amino(imino)methyl)benzyl)acetamide IC50: 500 nM Homo sapiens
N-(4-(amino(imino)methyl)benzyl)-2-(2,6-difluoro-3-((2-phenylethyl)amino)phenyl)acetamide IC50: 0.0164 mM Homo sapiens
N-(4-(amino(imino)methyl)benzyl)-2-(3-fluoro-4-((2-phenylethyl)amino)-1,1'-biphenyl-2-yl)acetamide IC50: 0.00398 mM Homo sapiens
N-(4-(amino(imino)methyl)benzyl)-2-(3-hydroxy-4-((2-phenylethyl)amino)-1,1'-biphenyl-2-yl)acetamide IC50: 0.0027 mM Homo sapiens
N-(4-(amino(imino)methyl)benzyl)-2-(3-hydroxy-4-(isopropylamino)-1,1'-biphenyl-2-yl)acetamide IC50: 0.0025 mM Homo sapiens
N-(4-(amino(imino)methyl)benzyl)-2-(3-methoxy-4-((2-phenylethyl)amino)-1,1'-biphenyl-2-yl)acetamide IC50: 0.025 mM Homo sapiens
N-(4-(amino(imino)methyl)benzyl)-2-(4-(isopropylamino)-3-methoxy-1,1'-biphenyl-2-yl)acetamide IC50: 0.0147 mM Homo sapiens
N-(4-(amino(imino)methyl)benzyl)-2-(5-(isopropylamino)-3,6-dioxo-2-phenylcyclohexa-1,4-dien-1-yl)acetamide IC50: 0.0028 mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N-methylsulfonyl-D-Phe-Gly-Arg-p-nitroanilide + H2O
-
Homo sapiens N-methylsulfonyl-D-Phe-Gly-Arg + p-nitroaniline
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00034
-
IC50: 340 nM Homo sapiens 2-(3'-amino-3-fluoro-4-(isopropylamino)-1,1'-biphenyl-2-yl)-N-(4-(amino(imino)methyl)benzyl)acetamide
0.0005
-
IC50: 500 nM Homo sapiens 2-(3'-amino-4-(benzylamino)-3-fluoro-1,1'-biphenyl-2-yl)-N-(4-(amino(imino)methyl)benzyl)acetamide
0.0025
-
IC50: 0.0025 mM Homo sapiens N-(4-(amino(imino)methyl)benzyl)-2-(3-hydroxy-4-(isopropylamino)-1,1'-biphenyl-2-yl)acetamide
0.0027
-
IC50: 0.0027 mM Homo sapiens N-(4-(amino(imino)methyl)benzyl)-2-(3-hydroxy-4-((2-phenylethyl)amino)-1,1'-biphenyl-2-yl)acetamide
0.0028
-
IC50: 0.0028 mM Homo sapiens N-(4-(amino(imino)methyl)benzyl)-2-(5-(isopropylamino)-3,6-dioxo-2-phenylcyclohexa-1,4-dien-1-yl)acetamide
0.00398
-
IC50: 0.00398 mM Homo sapiens N-(4-(amino(imino)methyl)benzyl)-2-(3-fluoro-4-((2-phenylethyl)amino)-1,1'-biphenyl-2-yl)acetamide
0.0147
-
IC50: 0.0147 mM Homo sapiens N-(4-(amino(imino)methyl)benzyl)-2-(4-(isopropylamino)-3-methoxy-1,1'-biphenyl-2-yl)acetamide
0.0164
-
IC50: 0.0164 mM Homo sapiens N-(4-(amino(imino)methyl)benzyl)-2-(2,6-difluoro-3-((2-phenylethyl)amino)phenyl)acetamide
0.025
-
IC50: 0.025 mM Homo sapiens N-(4-(amino(imino)methyl)benzyl)-2-(3-methoxy-4-((2-phenylethyl)amino)-1,1'-biphenyl-2-yl)acetamide