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Literature summary for 3.4.21.75 extracted from

  • Worachartcheewan, A.; Nantasenamat, C.; Naenna, T.; Isarankura-Na-Ayudhya, C.; Prachayasittikul, V.
    Modeling the activity of furin inhibitors using artificial neural network (2009), Eur. J. Med. Chem., 44, 1664-1673.
    View publication on PubMed

Application

Application Comment Organism
drug development good prospect of using quantitative structure-activity relationship models for the rational design of novel therapeutic furin inhibitors toward anthrax and furin-dependent diseases synthetic construct

Inhibitors

Inhibitors Comment Organism Structure
(1R,3S,4S,6R)-4-(2-carbamimidoylhydrazinyl)-6-guanidinocyclohexane-1,3-diyl bis(3-guanidinophenylcarbamate)
-
synthetic construct
(1R,3S,4S,6R)-4-(2-carbamimidoylhydrazinyl)-6-guanidinocyclohexane-1,3-diyl bis(4-guanidinophenylcarbamate)
-
synthetic construct
1-[(1R,2R,4S,5S)-2,4-bis(4-carbamimidamidophenoxy)-5-[(4-carbamimidamidophenyl)amino]cyclohexyl]guanidine
-
synthetic construct
1-[4-([(1S,2S,4R,5R)-5-carbamimidamido-2,4-bis[(4-carbamimidamidonaphthalen-1-yl)oxy]cyclohexyl]amino)naphthalen-1-yl]guanidine
-
synthetic construct
2-((1S,2S,4R,5R)-2,4-bis(2,4-diguanidinophenoxy)-5-guanidinocyclohexyl)hydrazinecarboximidamide
-
synthetic construct
2-((1S,2S,4R,5R)-2-(2,4-diguanidinophenoxy)-5-guanidino-4-(4-guanidinonaphthalen-1-yloxy)cyclohexyl)hydrazinecarboximidamide
-
synthetic construct
2-((1S,2S,4R,5R)-2-(2,4-diguanidinophenoxy)-5-guanidino-4-(4-guanidinophenoxy)cyclohexyl)hydrazinecarboximidamide
-
synthetic construct
2-((1S,2S,4R,5R)-2-(2-amino-4-guanidinophenoxy)-5-guanidino-4-(4-guanidinonaphthalen-1-yloxy)cyclohexyl)hydrazinecarboximidamide
-
synthetic construct
2-((1S,2S,4R,5R)-5-guanidino-2,4-bis(4-guanidinonaphthalen-1-yloxy)cyclohexyl)hydrazinecarboximidamide
-
synthetic construct
2-((1S,2S,4R,5R)-5-guanidino-2,4-bis(4-guanidinophenoxy)cyclohexyl)hydrazinecarboximidamide
-
synthetic construct
2-((1S,2S,4R,5R)-5-guanidino-2,4-bis(5-guanidinopyridin-2-yloxy)cyclohexyl)hydrazinecarboximidamide
-
synthetic construct
2-((1S,2S,4R,5R)-5-guanidino-4-(4-guanidinonaphthalen-1-yloxy)-2-(4-guanidinophenoxy)cyclohexyl)hydrazinecarboximidamide
-
synthetic construct
additional information compounds 2-((1S,2S,4R,5R)-5-guanidino-2,4-bis(2-guanidinophenoxy)cyclohexyl)hydrazinecarboximidamide, 2-((1S,2S,4R,5R)-5-guanidino-2,4-bis(3-guanidinopyridin-2-yloxy)cyclohexyl)hydrazinecarboximidamide, 2-((1S,2S,4R,5R)-5-guanidino-2,4-bis(3-guanidinopyridin-4-yloxy)cyclohexyl)hydrazinecarboximidamide, 2-((1S,2S,4R,5R)-2,4-bis(2-amino-1H-benzo[d]imidazol-6-yloxy)-5-guanidinocyclohexyl)hydrazinecarboximidamide, 2-((1S,2S,4R,5R)-5-guanidino-2,4-bis(pyridin-2-yloxy)cyclohexyl)hydrazinecarboximidamide and (1R,3S,4S,6R)-4-(2-carbamimidoylhydrazinyl)-6-guanidinocyclohexane-1,3-diyl bis(2-guanidinophenylcarbamate) do not inhibit synthetic construct

Organism

Organism UniProt Comment Textmining
synthetic construct
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
anthrax protective antigen + H2O
-
synthetic construct ?
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000006
-
2-((1S,2S,4R,5R)-5-guanidino-4-(4-guanidinonaphthalen-1-yloxy)-2-(4-guanidinophenoxy)cyclohexyl)hydrazinecarboximidamide
-
synthetic construct
0.000012
-
2-((1S,2S,4R,5R)-5-guanidino-2,4-bis(4-guanidinophenoxy)cyclohexyl)hydrazinecarboximidamide
-
synthetic construct
0.000022
-
2-((1S,2S,4R,5R)-2-(2-amino-4-guanidinophenoxy)-5-guanidino-4-(4-guanidinonaphthalen-1-yloxy)cyclohexyl)hydrazinecarboximidamide
-
synthetic construct
0.000042
-
2-((1S,2S,4R,5R)-5-guanidino-2,4-bis(5-guanidinopyridin-2-yloxy)cyclohexyl)hydrazinecarboximidamide
-
synthetic construct
0.000046
-
1-[(1R,2R,4S,5S)-2,4-bis(4-carbamimidamidophenoxy)-5-[(4-carbamimidamidophenyl)amino]cyclohexyl]guanidine
-
synthetic construct
0.000069
-
2-((1S,2S,4R,5R)-5-guanidino-2,4-bis(4-guanidinonaphthalen-1-yloxy)cyclohexyl)hydrazinecarboximidamide
-
synthetic construct
0.000089
-
2-((1S,2S,4R,5R)-2-(2,4-diguanidinophenoxy)-5-guanidino-4-(4-guanidinophenoxy)cyclohexyl)hydrazinecarboximidamide
-
synthetic construct
0.000169
-
2-((1S,2S,4R,5R)-2,4-bis(2,4-diguanidinophenoxy)-5-guanidinocyclohexyl)hydrazinecarboximidamide
-
synthetic construct
0.000404
-
2-((1S,2S,4R,5R)-2-(2,4-diguanidinophenoxy)-5-guanidino-4-(4-guanidinonaphthalen-1-yloxy)cyclohexyl)hydrazinecarboximidamide
-
synthetic construct
0.000423
-
1-[4-([(1S,2S,4R,5R)-5-carbamimidamido-2,4-bis[(4-carbamimidamidonaphthalen-1-yl)oxy]cyclohexyl]amino)naphthalen-1-yl]guanidine
-
synthetic construct
0.000812
-
(1R,3S,4S,6R)-4-(2-carbamimidoylhydrazinyl)-6-guanidinocyclohexane-1,3-diyl bis(4-guanidinophenylcarbamate)
-
synthetic construct
0.001768
-
(1R,3S,4S,6R)-4-(2-carbamimidoylhydrazinyl)-6-guanidinocyclohexane-1,3-diyl bis(3-guanidinophenylcarbamate)
-
synthetic construct