Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(2-methoxy-7-methyl-2-oxido-2,3,4,5-tetrahydro-1,2-oxaphosphepin-6-yl)methanol | - |
Electrophorus electricus | |
(3R,5aR)-3-methoxy-1-methyl-4,5,5a,6-tetrahydro-3H,8H-furo[3,4-e][1,2]oxaphosphepin-8-one 3-oxide | a diastereoisomeric bicyclic phosphonate analogue | Electrophorus electricus | |
(3S,5aR)-3-methoxy-1-methyl-4,5,5a,6-tetrahydro-3H,8H-furo[3,4-e][1,2]oxaphosphepin-8-one 3-oxide | a diastereoisomeric bicyclic phosphonate analogue | Electrophorus electricus | |
(E)-dimethyl 1-(2-oxodihydrofuran-3(2H)-ylidene)ethyl phosphate | - |
Electrophorus electricus | |
(Z)-dimethyl 1-(2-oxodihydrofuran-3(2H)-ylidene)ethyl phosphate | - |
Electrophorus electricus | |
cyclophostin | a natural AChE inhibitor | Electrophorus electricus | |
diethylfluorophosphate | - |
Electrophorus electricus | |
diisopropylfluorophosphate | - |
Electrophorus electricus | |
methyl (2R,5R)-5-[(benzyloxy)methyl]-2-methoxy-7-methyl-2,3,4,5-tetrahydro-1,2-oxaphosphepine-6-carboxylate 2-oxide | - |
Electrophorus electricus | |
methyl (2S,5R)-5-[(benzyloxy)methyl]-2-methoxy-7-methyl-2,3,4,5-tetrahydro-1,2-oxaphosphepine-6-carboxylate 2-oxide | - |
Electrophorus electricus | |
methyl 1-methoxy-5-methyl-1,2,3,6-tetrahydrophosphinine-4-carboxylate 1-oxide | - |
Electrophorus electricus | |
methyl 2-acetyl-4-(dimethoxyphosphoryl)butanoate | - |
Electrophorus electricus | |
methyl 2-acetyl-5-(dimethoxyphosphoryl)pent-4-enoate | - |
Electrophorus electricus | |
methyl 2-acetyl-5-(dimethoxyphosphoryl)pentanoate | - |
Electrophorus electricus | |
methyl 2-methoxy-7-methyl-2,3,4,5-tetrahydro-1,2-oxaphosphepine-6-carboxylate 2-oxide | - |
Electrophorus electricus | |
additional information | synthesis and kinetic analysis of some phosphonate analogs of cyclophostin as inhibitors of acetylcholinesterase, mechanism of inhibition, overview | Electrophorus electricus | |
paraoxon | - |
Electrophorus electricus | |
soman | - |
Electrophorus electricus | |
Tabun | - |
Electrophorus electricus | |
VX (nerve agent) | - |
Electrophorus electricus |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
acetylcholine + H2O | Electrophorus electricus | - |
acetate + choline | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Electrophorus electricus | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
acetylcholine + H2O | - |
Electrophorus electricus | acetate + choline | - |
? | |
acetylthiocholine + H2O | - |
Electrophorus electricus | acetate + thiocholine | - |
? |
Synonyms | Comment | Organism |
---|---|---|
AChE | - |
Electrophorus electricus |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
25 | - |
irreversible inhibition assay at | Electrophorus electricus |
37 | - |
assay at | Electrophorus electricus |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.5 | - |
irreversible inhibition assay at | Electrophorus electricus |
8 | - |
enzyme assay at | Electrophorus electricus |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0000008 | - |
cyclophostin | pH 7.5, 25°C | Electrophorus electricus | |
0.006 | - |
diisopropylfluorophosphate | pH 7.5, 25°C | Electrophorus electricus | |
0.024 | - |
(3S,5aR)-3-methoxy-1-methyl-4,5,5a,6-tetrahydro-3H,8H-furo[3,4-e][1,2]oxaphosphepin-8-one 3-oxide | pH 7.5, 25°C | Electrophorus electricus | |
0.076 | - |
methyl 2-methoxy-7-methyl-2,3,4,5-tetrahydro-1,2-oxaphosphepine-6-carboxylate 2-oxide | pH 7.5, 25°C | Electrophorus electricus | |
0.14 | - |
(3R,5aR)-3-methoxy-1-methyl-4,5,5a,6-tetrahydro-3H,8H-furo[3,4-e][1,2]oxaphosphepin-8-one 3-oxide | pH 7.5, 25°C | Electrophorus electricus | |
0.31 | - |
methyl 1-methoxy-5-methyl-1,2,3,6-tetrahydrophosphinine-4-carboxylate 1-oxide | pH 7.5, 25°C | Electrophorus electricus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00012 | - |
pH 7.5, 25°C | Electrophorus electricus | diisopropylfluorophosphate | |
0.0003 | - |
pH 7.5, 25°C | Electrophorus electricus | (3S,5aR)-3-methoxy-1-methyl-4,5,5a,6-tetrahydro-3H,8H-furo[3,4-e][1,2]oxaphosphepin-8-one 3-oxide | |
0.003 | - |
pH 7.5, 25°C | Electrophorus electricus | (3R,5aR)-3-methoxy-1-methyl-4,5,5a,6-tetrahydro-3H,8H-furo[3,4-e][1,2]oxaphosphepin-8-one 3-oxide | |
0.005 | - |
pH 7.5, 25°C | Electrophorus electricus | methyl 1-methoxy-5-methyl-1,2,3,6-tetrahydrophosphinine-4-carboxylate 1-oxide | |
0.006 | - |
pH 7.5, 25°C | Electrophorus electricus | methyl (2R,5R)-5-[(benzyloxy)methyl]-2-methoxy-7-methyl-2,3,4,5-tetrahydro-1,2-oxaphosphepine-6-carboxylate 2-oxide | |
0.007 | - |
pH 7.5, 25°C | Electrophorus electricus | methyl 2-methoxy-7-methyl-2,3,4,5-tetrahydro-1,2-oxaphosphepine-6-carboxylate 2-oxide | |
0.035 | - |
pH 7.5, 25°C | Electrophorus electricus | methyl (2S,5R)-5-[(benzyloxy)methyl]-2-methoxy-7-methyl-2,3,4,5-tetrahydro-1,2-oxaphosphepine-6-carboxylate 2-oxide | |
0.07 | - |
pH 7.5, 25°C | Electrophorus electricus | (E)-dimethyl 1-(2-oxodihydrofuran-3(2H)-ylidene)ethyl phosphate | |
0.6 | - |
pH 7.5, 25°C | Electrophorus electricus | (2-methoxy-7-methyl-2-oxido-2,3,4,5-tetrahydro-1,2-oxaphosphepin-6-yl)methanol | |
1 | - |
above, pH 7.5, 25°C | Electrophorus electricus | (Z)-dimethyl 1-(2-oxodihydrofuran-3(2H)-ylidene)ethyl phosphate |