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Literature summary for 3.1.1.7 extracted from

  • Ali, H.M.; Sharaf Eldeen, H.A.; Hikal, M.S.
    Selectivity, acetylcholinesterase inhibition kinetics, and quantitative structure-activity relationships of a series of N-(2-oxido-1,3,2-benzodioxa-phosphol-2-yl) amino acid ethyl or diethyl esters (2005), Pestic. Biochem. Physiol., 83, 58-65.
No PubMed abstract available

Inhibitors

Inhibitors Comment Organism Structure
diethyl (2S)-2-((2-oxido-1,3,2-benzodioxaphosphol-2-yl)amino)pentanedioate 50% inhibition at 0.454 mM Musca domestica
diethyl (2S)-2-((2-oxido-1,3,2-benzodioxaphosphol-2-yl)amino)pentanedioate 50% inhibition at 1.226 mM Oryctolagus cuniculus
diethyl (2S)-2-((2-oxido-1,3,2-benzodioxaphosphol-2-yl)amino)succinate 50% inhibition at 0.651 mM Musca domestica
diethyl (2S)-2-((2-oxido-1,3,2-benzodioxaphosphol-2-yl)amino)succinate 50% inhibition at 0.577 mM Oryctolagus cuniculus
ethyl ((2-oxido-1,3,2-benzodioxaphosphol-2-yl)amino)acetate 50% inhibition at 0.626 mM Musca domestica
ethyl ((2-oxido-1,3,2-benzodioxaphosphol-2-yl)amino)acetate 50% inhibition at 0.460 mM Oryctolagus cuniculus
ethyl (2S)-2-((2-oxido-1,3,2-benzodioxaphosphol-2-yl)amino)-3-phenylpropanoate 50% inhibition at 0.332 mM Musca domestica
ethyl (2S)-2-((2-oxido-1,3,2-benzodioxaphosphol-2-yl)amino)-3-phenylpropanoate 50% inhibition at 0.406 mM Oryctolagus cuniculus
ethyl (2S)-2-((2-oxido-1,3,2-benzodioxaphosphol-2-yl)amino)hexanoate 50% inhibition at 0.321 mM Musca domestica
ethyl (2S)-2-((2-oxido-1,3,2-benzodioxaphosphol-2-yl)amino)hexanoate 50% inhibition at 0.506 mM Oryctolagus cuniculus
ethyl (2S)-2-((2-oxido-1,3,2-benzodioxaphosphol-2-yl)amino)propanoate 50% inhibition at 0.615 mM Musca domestica
ethyl (2S)-2-((2-oxido-1,3,2-benzodioxaphosphol-2-yl)amino)propanoate 50% inhibition at 0.537 mM Oryctolagus cuniculus
ethyl (2S)-3-methyl-2-((2-oxido-1,3,2-benzodioxaphosphol-2-yl)amino)butanoate 50% inhibition at 0.454 mM Musca domestica
ethyl (2S)-3-methyl-2-((2-oxido-1,3,2-benzodioxaphosphol-2-yl)amino)butanoate 50% inhibition at 0.394 mM Oryctolagus cuniculus
ethyl (2S)-3-methyl-2-((2-oxido-1,3,2-benzodioxaphosphol-2-yl)amino)pentanoate 50% inhibition at 0.345 mM Musca domestica
ethyl (2S)-3-methyl-2-((2-oxido-1,3,2-benzodioxaphosphol-2-yl)amino)pentanoate 50% inhibition at 0.387 mM Oryctolagus cuniculus
ethyl (2S)-4-(methylthio)-2-((2-oxido-1,3,2-benzodioxaphosphol-2-yl)amino)butanoate 50% inhibition at 0.386 mM Musca domestica
ethyl (2S)-4-(methylthio)-2-((2-oxido-1,3,2-benzodioxaphosphol-2-yl)amino)butanoate 50% inhibition at 0.551 mM Oryctolagus cuniculus
ethyl (2S)-4-amino-2-((2-oxido-1,3,2-benzodioxaphosphol-2-yl)amino)-4-oxobutanoate 50% inhibition at 0.420 mM Musca domestica
ethyl (2S)-4-amino-2-((2-oxido-1,3,2-benzodioxaphosphol-2-yl)amino)-4-oxobutanoate 50% inhibition at 0.385 mM Oryctolagus cuniculus
ethyl (2S)-4-methyl-2-((2-oxido-1,3,2-benzodioxaphosphol-2-yl)amino)pentanoate 50% inhibition at 0.196 mM Musca domestica
ethyl (2S)-4-methyl-2-((2-oxido-1,3,2-benzodioxaphosphol-2-yl)amino)pentanoate 50% inhibition at 0.427 mM Oryctolagus cuniculus
fenitrothion i.e. O,O-dimethyl-O-(3-methyl-4-nitrophenyl) phosphorothioate, 50% inhibition at 394 mM Musca domestica
fenitrothion i.e. O,O-dimethyl-O-(3-methyl-4-nitrophenyl) phosphorothioate, 50% inhibition at 366 mM Oryctolagus cuniculus
additional information proposed inhibition mechanism for 1,3,2-benzodioxaphopholenes Musca domestica
additional information proposed inhibition mechanism for 1,3,2-benzodioxaphopholenes Oryctolagus cuniculus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0003437
-
acetylthiocholine iodide pH 7.2, 30°C Oryctolagus cuniculus
0.0003437
-
acetylthiocholine iodide pH 7.2, 30°C Musca domestica

Organism

Organism UniProt Comment Textmining
Musca domestica
-
-
-
Oryctolagus cuniculus
-
albino rabbit
-

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
Oryctolagus cuniculus
-
head
-
Musca domestica
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetylthiocholine iodide + H2O
-
Oryctolagus cuniculus thiocholine iodide + acetate
-
?
acetylthiocholine iodide + H2O
-
Musca domestica thiocholine iodide + acetate
-
?