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Literature summary for 3.1.1.7 extracted from

  • Gholivand, K.; Mojahed, F.; Salehi, M.; Naderi-Manesh, H.; Khajeh, K.
    Synthesis, characterization and inhibitory potency of two oxono and thiono analogues of phosphoramidate compounds on acetylcholinesterase (2006), J. Enzyme Inhib. Med. Chem., 21, 521-525.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
benzoyl phosphoramidic dichloride
-
Homo sapiens
N-benzoyl N',N'-(tert-butybenzyl) phosphoramidic chloride 26% reactivation of enzyme activity by pralidoxime, 4% by obidoxime Homo sapiens
N-benzoyl N',N'-(tert-butybenzyl) thiophosphoramidic chloride 22% reactivation of enzyme activity by pralidoxime, 3% by obidoxime Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
erythrocyte
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetylthiocholine + H2O
-
Homo sapiens thiocholine + acetate
-
?

Synonyms

Synonyms Comment Organism
AChE
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0232
-
N-benzoyl N',N'-(tert-butybenzyl) phosphoramidic chloride pH 7.4, 25°C Homo sapiens
0.0442
-
N-benzoyl N',N'-(tert-butybenzyl) thiophosphoramidic chloride pH 7.4, 25°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.567
-
pH 7.4, 25°C, purified enzyme Homo sapiens N-benzoyl N',N'-(tert-butybenzyl) phosphoramidic chloride
2.986
-
pH 7.4, 25°C, purified enzyme Homo sapiens N-benzoyl N',N'-(tert-butybenzyl) thiophosphoramidic chloride
2.34
-
pH 7.4, 25°C, crude enzyme Homo sapiens N-benzoyl N',N'-(tert-butybenzyl) phosphoramidic chloride
4.64
-
pH 7.4, 25°C, crude enzyme Homo sapiens N-benzoyl N',N'-(tert-butybenzyl) thiophosphoramidic chloride