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Literature summary extracted from

  • Mohammed, A.; Sneathen, J.; Frojen, S.G.; Kuo, L.; Dupureur, C.M.
    Stereospecific cholinesterase inhibition by O,S-diethylphenylphosphonothioate (2017), Bioorg. Med. Chem., 25, 3053-3058 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.1.7 cyclophostin
-
 Electrophorus electricus
3.1.1.7 cyclophostin
-
 Homo sapiens
3.1.1.7 leptophos
-
 Electrophorus electricus
3.1.1.7 leptophos
-
 Homo sapiens
3.1.1.7 methamidophos
-
 Electrophorus electricus
3.1.1.7 methamidophos
-
 Homo sapiens
3.1.1.7 O-ethyl-S-[2-(diisopropylamino)-ethyl]-methylphosphonothioate nerve agent VX Electrophorus electricus
3.1.1.7 O-ethyl-S-[2-(diisopropylamino)-ethyl]-methylphosphonothioate nerve agent VX Homo sapiens
3.1.1.7 paraoxon
-
 Electrophorus electricus
3.1.1.7 paraoxon
-
 Homo sapiens
3.1.1.7 R-DEPP O,S-diethylphenylphosphonothioate, both S- and R-DEPP are poor inhibitors of eel AChE, stereospecific inhibition kinetics and stereospecificity of the chiral nerve agent derivative. Kinetic analysis of S-DEPP with cholinesterases Electrophorus electricus
3.1.1.7 R-DEPP O,S-diethylphenylphosphonothioate, stereospecific inhibition kinetics and stereospecificity of the chiral nerve agent derivative O,S-diethylphenylphosphonothioate. Chemical modification by DEPP, a measurable amount of the enzyme-phosphonate adduct does not undergo aging Homo sapiens
3.1.1.7 S-DEPP O,S-diethylphenylphosphonothioate, both S- and R-DEPP are poor inhibitors of eel AChE, stereospecific inhibition kinetics and stereospecificity of the chiral nerve agent derivative Electrophorus electricus
3.1.1.7 S-DEPP O,S-diethylphenylphosphonothioate, stereospecific inhibition kinetics and stereospecificity of the chiral nerve agent derivative O,S-diethylphenylphosphonothioate. Chemical modification by DEPP, a measurable amount of the enzyme-phosphonate adduct does not undergo aging. Pralidoxime, a common rescue agent, affects a modest recovery of eqBChE from treatment with S-DEPP. S-DEPP inhibition is practically irreversible. Kinetic analysis of S-DEPP with cholinesterases Homo sapiens
3.1.1.7 sarin
-
 Electrophorus electricus
3.1.1.7 sarin
-
 Homo sapiens
3.1.1.7 soman
-
 Electrophorus electricus
3.1.1.7 soman
-
 Homo sapiens
3.1.1.7 Tabun
-
 Electrophorus electricus
3.1.1.7 Tabun
-
 Homo sapiens
3.1.1.7 thiomethylcyclosarin
-
 Electrophorus electricus
3.1.1.7 thiomethylcyclosarin
-
 Homo sapiens
3.1.1.7 thiomethylsarin
-
 Electrophorus electricus
3.1.1.7 thiomethylsarin
-
 Homo sapiens
3.1.1.7 thiomethylsoman
-
 Electrophorus electricus
3.1.1.7 thiomethylsoman
-
 Homo sapiens
3.1.1.8 cyclophostin
-
 Equus caballus
3.1.1.8 leptophos
-
 Equus caballus
3.1.1.8 methamidophos
-
 Equus caballus
3.1.1.8 O-ethyl-S-2-diisopropylaminoethylmethylphosphonothiolate
-
 Equus caballus
3.1.1.8 paraoxon
-
 Equus caballus
3.1.1.8 R-DEPP O,R-diethylphenylphosphonothioate, stereospecific inhibition kinetics and stereospecificity of the chiral nerve agent derivative O,R-diethylphenylphosphonothioate. Chemical modification by DEPP, a measurable amount of the enzyme-phosphonate adduct does not undergo aging Equus caballus
3.1.1.8 S-DEPP O,S-diethylphenylphosphonothioate, stereospecific inhibition kinetics and stereospecificity of the chiral nerve agent derivative O,S-diethylphenylphosphonothioate. Chemical modification by DEPP, a measurable amount of the enzyme-phosphonate adduct does not undergo aging. Pralidoxime, a common rescue agent, affects a modest recovery of eqBChE from treatment with S-DEPP. S-DEPP inhibition is practically irreversible. Kinetic analysis of S-DEPP with cholinesterases Equus caballus
3.1.1.8 sarin
-
 Equus caballus
3.1.1.8 soman
-
 Equus caballus
3.1.1.8 Tabun
-
 Equus caballus
3.1.1.8 thiomethylcyclosarin
-
 Equus caballus
3.1.1.8 thiomethylsarin
-
 Equus caballus
3.1.1.8 thiomethylsoman
-
 Equus caballus

Organism

EC Number Organism UniProt Comment Textmining
3.1.1.7 Electrophorus electricus O42275
-
-
3.1.1.7 Homo sapiens P22303
-
-
3.1.1.8 Equus caballus P81908
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.1.1.7 commercial preparation
-
 Homo sapiens
-
3.1.1.7 commercial preparation
-
 Electrophorus electricus
-
3.1.1.8 commercial preparation
-
 Equus caballus
-
3.1.1.8 serum
-
 Equus caballus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.1.7 acetylthiocholine + H2O
-
 Homo sapiens thiocholine + acetate
-
 ?
3.1.1.7 acetylthiocholine + H2O
-
 Electrophorus electricus thiocholine + acetate
-
 ?
3.1.1.8 butyrylthiocholine + H2O
-
 Equus caballus thiocholine + butyrate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.1.1.7 AChE
-
 Electrophorus electricus
3.1.1.7 eeAChE
-
 Electrophorus electricus
3.1.1.7 hAChE
-
 Homo sapiens
3.1.1.8 butyrylcholinesterase
-
 Equus caballus
3.1.1.8 eqBChE
-
 Equus caballus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.1.1.7 25
-
 assay at Homo sapiens
3.1.1.7 25
-
 assay at Electrophorus electricus
3.1.1.8 25
-
 assay at Equus caballus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.1.1.7 8
-
 assay at Homo sapiens
3.1.1.7 8
-
 assay at Electrophorus electricus
3.1.1.8 8
-
 assay at Equus caballus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.1.1.7 0.008
-
 S-DEPP pH 8.0, 25°C Homo sapiens
3.1.1.7 0.15
-
 R-DEPP pH 8.0, 25°C Homo sapiens
3.1.1.8 0.007
-
 S-DEPP pH 8.0, 25°C Equus caballus
3.1.1.8 0.15
-
 R-DEPP pH 8.0, 25°C Equus caballus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.1.1.7 0.145
-
 pH 8.0, 25°C Electrophorus electricus S-DEPP
3.1.1.7 0.165
-
 pH 8.0, 25°C Electrophorus electricus R-DEPP