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Literature summary for 3.4.21.109 extracted from

  • Goswami, R.; Wohlfahrt, G.; Mukherjee, S.; Ghadiyaram, C.; Nagaraj, J.; Satyam, L.K.; Subbarao, K.; Gopinath, S.; Krishnamurthy, N.R.; Subramanya, H.S.; Ramachandra, M.
    Discovery of O-(3-carbamimidoylphenyl)-l-serine amides as matriptase inhibitors using a fragment-linking approach (2015), Bioorg. Med. Chem. Lett., 25, 616-620.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[(naphthalen-2-ylsulfonyl)amino]-3-oxopropoxy]benzenecarboximidamide higher cytotoxic effect, enzyme-bound structure, crystal structure analysis, overview Homo sapiens
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(4-cyclohexylphenyl)sulfonyl]amino]-3-oxopropoxy]benzenecarboximidamide
-
Homo sapiens
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-3-oxo-2-([[2,4,6-tri(propan-2-yl)phenyl]sulfonyl]amino)propoxy]benzenecarboximidamide higher cytotoxic effect Homo sapiens
3-[(2S)-3-[4-(4-aminobutanoyl)piperidin-1-yl]-3-oxo-2-([[2,4,6-tri(propan-2-yl)phenyl]sulfonyl]amino)propoxy]benzenecarboximidamide
-
Homo sapiens
3-[(2S)-3-[4-(b-alanyl)piperidin-1-yl]-3-oxo-2-([[2,4,6-tri(propan-2-yl)phenyl]sulfonyl]amino)propoxy]benzenecarboximidamide
-
Homo sapiens
additional information O-(3-carbamimidoylphenyl)-L-serine amides as matriptase inhibitors, overview. Analysis of cytotoxic effects of inhibitors Homo sapiens
N-(4-aminocyclohexyl)-O-(3-carbamimidoylphenyl)-N2-(naphthalen-2-ylsulfonyl)-L-serinamide
-
Homo sapiens
O-(3-carbamimidoylphenyl)-N-(4-methylcyclohexyl)-N2-(naphthalen-2-ylsulfonyl)-L-serinamide
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9Y5Y6
-
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0001
-
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-3-oxo-2-([[2,4,6-tri(propan-2-yl)phenyl]sulfonyl]amino)propoxy]benzenecarboximidamide pH and temperature not specified in the publication Homo sapiens
0.0003
-
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[(naphthalen-2-ylsulfonyl)amino]-3-oxopropoxy]benzenecarboximidamide pH and temperature not specified in the publication Homo sapiens
0.0003
-
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(4-cyclohexylphenyl)sulfonyl]amino]-3-oxopropoxy]benzenecarboximidamide pH and temperature not specified in the publication Homo sapiens
0.0015
-
3-[(2S)-3-[4-(4-aminobutanoyl)piperidin-1-yl]-3-oxo-2-([[2,4,6-tri(propan-2-yl)phenyl]sulfonyl]amino)propoxy]benzenecarboximidamide pH and temperature not specified in the publication Homo sapiens
0.0017
-
3-[(2S)-3-[4-(b-alanyl)piperidin-1-yl]-3-oxo-2-([[2,4,6-tri(propan-2-yl)phenyl]sulfonyl]amino)propoxy]benzenecarboximidamide pH and temperature not specified in the publication Homo sapiens
0.0037
-
N-(4-aminocyclohexyl)-O-(3-carbamimidoylphenyl)-N2-(naphthalen-2-ylsulfonyl)-L-serinamide pH and temperature not specified in the publication Homo sapiens