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Literature summary for 3.4.21.109 extracted from

  • Steinmetzer, T.; Doennecke, D.; Korsonewski, M.; Neuwirth, C.; Steinmetzer, P.; Schulze, A.; Saupe, S.M.; Schweinitz, A.
    Modification of the N-terminal sulfonyl residue in 3-amidinophenylalanine-based matriptase inhibitors (2009), Bioorg. Med. Chem. Lett., 19, 67-73.
    View publication on PubMed
Search for more literature for 3.4.21.109

Application

Application Comment Organism
medicine matriptase may be considered to be a potential target for the development of anti-cancer drugs Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3-[(2S)-2-([[3-(4-aminobutyl)phenyl]sulfonyl]amino)-3-[4-(2-aminoethyl)piperidin-1-yl]-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-([[3-(1H-indol-5-yl)phenyl]sulfonyl]amino)-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-([[3-(2-methylpyrimidin-4-yl)phenyl]sulfonyl]amino)-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-([[3-(6-amino-2,3,4,5-tetrahydropyridin-3-yl)phenyl]sulfonyl]amino)-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-([[3-(6-aminopyridin-3-yl)phenyl]sulfonyl]amino)-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-([[4'-(1-methylethoxy)biphenyl-3-yl]sulfonyl]amino)-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[(biphenyl-3-ylsulfonyl)amino]-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[([3-[(3-aminopropyl)amino]phenyl]sulfonyl)amino]-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(2'-chlorobiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(3',4'-dimethoxybiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(3'-chlorobiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(4'-chlorobiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(4'-ethoxybiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(4'-ethylbiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(4'-methoxybiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-3-oxo-2-[[(3-pyridin-3-ylphenyl)sulfonyl]amino]propyl]benzenecarboximidamide
-
 Homo sapiens
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-3-oxo-2-[[(3-pyridin-4-ylphenyl)sulfonyl]amino]propyl]benzenecarboximidamide
-
 Homo sapiens
ethyl (3-[[(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-(3-carbamimidoylbenzyl)-2-oxoethyl]sulfamoyl]phenyl)carbamate
-
 Homo sapiens
N-(3-[[(1S)-1-[[4-(2-aminoethyl)piperidin-1-yl]carbonyl]-3-phenylpropyl]sulfamoyl]phenyl)-beta-alaninamide
-
 Homo sapiens
N-(3-[[(1S)-1-[[4-(2-aminoethyl)piperidin-1-yl]carbonyl]-4-phenylbutyl]sulfamoyl]phenyl)-beta-alaninamide
-
 Homo sapiens
N-(3-[[(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-(3-carbamimidoylbenzyl)-2-oxoethyl]sulfamoyl]phenyl)-3-hydroxypropanamide
-
 Homo sapiens
N-(3-[[(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-(3-carbamimidoylbenzyl)-2-oxoethyl]sulfamoyl]phenyl)-beta-alaninamide
-
 Homo sapiens
N-(3-[[(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-(3-carbamimidoylbenzyl)-2-oxoethyl]sulfamoyl]phenyl)azetidine-3-carboxamide
-
 Homo sapiens
N-(3-[[(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-(3-carbamimidoylbenzyl)-2-oxoethyl]sulfamoyl]phenyl)propanamide
-
 Homo sapiens
N-[(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-[3-(aminomethyl)benzyl]-2-oxoethyl]-4'-methoxybiphenyl-3-sulfonamide
-
 Homo sapiens
N-[3-([(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-benzyl-2-oxoethyl]sulfamoyl)phenyl]-beta-alaninamide
-
 Homo sapiens
N-[3-([(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-[3-(aminomethyl)benzyl]-2-oxoethyl]sulfamoyl)phenyl]-beta-alaninamide
-
 Homo sapiens
N-[3-([(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-[4-(aminomethyl)benzyl]-2-oxoethyl]sulfamoyl)phenyl]-beta-alaninamide
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
insulin-like growth factor binding protein related protein-1 Homo sapiens IGFBP-rP1 ?
-
 ?
pro-hepatocyte growth factor/scatter factor + H2O Homo sapiens pro-HGF/SF ?
-
 ?
pro-uPA + H2O Homo sapiens
-
 ?
-
 ?
protease-activated receptor-2 Homo sapiens PAR2 ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9Y5Y6
-
-

Source Tissue

Source Tissue Comment Organism Textmining
epithelial cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
insulin-like growth factor binding protein related protein-1 IGFBP-rP1 Homo sapiens ?
-
 ?
pro-hepatocyte growth factor/scatter factor + H2O pro-HGF/SF Homo sapiens ?
-
 ?
pro-uPA + H2O
-
 Homo sapiens ?
-
 ?
protease-activated receptor-2 PAR2 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
matriptase
-
 Homo sapiens
MT-SP1
-
 Homo sapiens
ST14
-
 Homo sapiens
TADG-15
-
 Homo sapiens
type II transmembrane protease
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000008
-
 3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-([[3-(6-amino-2,3,4,5-tetrahydropyridin-3-yl)phenyl]sulfonyl]amino)-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
0.000001
-
 3-[(2S)-2-([[3-(4-aminobutyl)phenyl]sulfonyl]amino)-3-[4-(2-aminoethyl)piperidin-1-yl]-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
0.0000016
-
 3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-([[3-(6-aminopyridin-3-yl)phenyl]sulfonyl]amino)-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
0.0000025
-
 3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(4'-ethylbiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
0.000003
-
 N-(3-[[(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-(3-carbamimidoylbenzyl)-2-oxoethyl]sulfamoyl]phenyl)azetidine-3-carboxamide
-
 Homo sapiens
0.0000038
-
 N-(3-[[(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-(3-carbamimidoylbenzyl)-2-oxoethyl]sulfamoyl]phenyl)-beta-alaninamide
-
 Homo sapiens
0.0000054
-
 3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(3',4'-dimethoxybiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
0.000006
-
 3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(4'-ethoxybiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
0.0000067
-
 3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[([3-[(3-aminopropyl)amino]phenyl]sulfonyl)amino]-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
0.000007
-
 3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(4'-methoxybiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
0.000012
-
 3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-([[4'-(1-methylethoxy)biphenyl-3-yl]sulfonyl]amino)-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
0.000013
-
 3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-([[3-(1H-indol-5-yl)phenyl]sulfonyl]amino)-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
0.000026
-
 3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(4'-chlorobiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
0.000028
-
 3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-([[3-(2-methylpyrimidin-4-yl)phenyl]sulfonyl]amino)-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
0.000029
-
 3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(2'-chlorobiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
0.000041
-
 ethyl (3-[[(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-(3-carbamimidoylbenzyl)-2-oxoethyl]sulfamoyl]phenyl)carbamate
-
 Homo sapiens
0.000047
-
 3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-3-oxo-2-[[(3-pyridin-3-ylphenyl)sulfonyl]amino]propyl]benzenecarboximidamide
-
 Homo sapiens
0.000056
-
 N-[3-([(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-[3-(aminomethyl)benzyl]-2-oxoethyl]sulfamoyl)phenyl]-beta-alaninamide
-
 Homo sapiens
0.00006
-
 3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-3-oxo-2-[[(3-pyridin-4-ylphenyl)sulfonyl]amino]propyl]benzenecarboximidamide
-
 Homo sapiens
0.000091
-
 3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(3'-chlorobiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
0.00011
-
 3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[(biphenyl-3-ylsulfonyl)amino]-3-oxopropyl]benzenecarboximidamide
-
 Homo sapiens
0.00012
-
 N-(3-[[(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-(3-carbamimidoylbenzyl)-2-oxoethyl]sulfamoyl]phenyl)-3-hydroxypropanamide
-
 Homo sapiens
0.000145
-
 N-[(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-[3-(aminomethyl)benzyl]-2-oxoethyl]-4'-methoxybiphenyl-3-sulfonamide
-
 Homo sapiens
0.00018
-
 N-(3-[[(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-(3-carbamimidoylbenzyl)-2-oxoethyl]sulfamoyl]phenyl)propanamide
-
 Homo sapiens
0.0028
-
 N-[3-([(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-[4-(aminomethyl)benzyl]-2-oxoethyl]sulfamoyl)phenyl]-beta-alaninamide
-
 Homo sapiens
0.01
-
 N-[3-([(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-benzyl-2-oxoethyl]sulfamoyl)phenyl]-beta-alaninamide
-
 Homo sapiens
1
-
 N-(3-[[(1S)-1-[[4-(2-aminoethyl)piperidin-1-yl]carbonyl]-3-phenylpropyl]sulfamoyl]phenyl)-beta-alaninamide larger than 1 Homo sapiens
1
-
 N-(3-[[(1S)-1-[[4-(2-aminoethyl)piperidin-1-yl]carbonyl]-4-phenylbutyl]sulfamoyl]phenyl)-beta-alaninamide larger than 1 Homo sapiens