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Information on EC 3.1.1.7 - acetylcholinesterase and Organism(s) Electrophorus electricus and UniProt Accession O42275
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3.1.1.7 acetylcholinesteraseIUBMB Comments
Acts on a variety of acetic esters; also catalyses transacetylations.
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Word Map
- 3.1.1.7
-
cholinergic
- alzheimer
- nerve
- butyrylcholinesterase
-
organophosphate
-
pesticide
- hippocampus
-
neurotoxicity
- dementia
- erythrocyte
- deficit
-
organophosphorus
-
insecticide
-
muscarinic
- donepezil
- synaptic
-
neuroprotective
- cerebral
- acetyltransferase
- fiber
-
maze
- cortical
-
innervation
-
poison
- cholinesterases
-
nicotinic
-
neurotransmitter
- neuromuscular
- neurodegenerative
- atropine
- axon
- oxime
- carbamate
-
chat
-
histochemistry
-
amyloid
-
morris
-
neurochemical
-
monoamine
- synapses
-
intoxication
- chlorpyrifos
- striatum
-
neurotransmission
-
postsynaptic
- forebrain
- carboxylesterase
-
antidote
-
parasympathetic
- biotechnology
- synthesis
- analysis
- pharmacology
- medicine
- diagnostics
-
anticholinergic
- environmental protection
- drug development
The taxonomic range for the selected organisms is: Electrophorus electricus
The expected taxonomic range for this enzyme is: Eukaryota, Bacteria
The expected taxonomic range for this enzyme is: Eukaryota, Bacteria
Synonyms
ache, acetylcholinesterase, acetylcholine esterase, acetyl cholinesterase, hache, eeache, ache1, huache, tcache, membrane-bound acetylcholinesterase, 
more
topSYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
AChE
-
AcCholE
-
-
-
-
acetyl beta-methylcholinesterase
-
-
-
-
acetylcholine esterase
-
-
-
-
acetylcholine hydrolase
-
-
-
-
acetylthiocholinesterase
-
-
-
-
AChE
choline esterase I
-
-
-
-
cholinesterase
-
-
-
-
esterase, acetyl choline
-
-
-
-
true cholinesterase
-
-
-
-
AChE
-
-
-
-
AChE
-
-
REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
acetylcholine + H2O = choline + acetate
the mechanism for AChE-catalyzed hydrolysis of substrate is formation of the first tetrahedral intermediate via nucleophilic attack of the active site serine
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
hydrolysis of carboxylic ester
-
-
-
-
transacetylation
-
-
-
-
PATHWAY SOURCE
PATHWAYS
SYSTEMATIC NAME
IUBMB Comments
acetylcholine acetylhydrolase
Acts on a variety of acetic esters; also catalyses transacetylations.
CAS REGISTRY NUMBER
COMMENTARY
9000-81-1
-
SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
acetylcholine + H2O
choline + acetate
-
-
-
?
acetylthiocholine + H2O
thiocholine + acetate
-
-
-
?
acetylthiocholine + H2O
acetate + thiocholine
-
-
-
-
?
acetylthiocholine + H2O
thiocholine + acetate
-
-
-
-
?
acetylthiocholine iodide + H2O
acetate + thiocholine iodide
-
detection with 5,5'-dithio-bis-2-nitrobenzoic acid, i.e. DTNB
-
-
?
S-acetylthiocholine iodide + H2O
acetate + thiocholine iodide
-
detection with 5,5'-dithio-bis-2-nitrobenzoic acid, i.e. DTNB
-
-
?
acetylcholine + H2O
acetate + choline
-
-
691156, 692653, 692785, 703783, 707691, 707743, 707747, 708106, 708130, 708139, 708326, 708829, 709593
-
-
?
acetylcholine + H2O
acetate + choline
-
acetylcholinesterase plays in vivo a key role in cholinergic transmission by catalysing the rapid hydrolysis of the neurotransmitter acetylcholine into acetate and choline
-
-
?
acetylcholine + H2O
choline + acetate
-
-
-
-
?
additional information
?
-
thiols block the enzymatic etching of gold nanorods(thiocholine on the rate of horseradish peroxidase-catalyzed AuNR etching), application to colorimetric detection of acetylcholinesterase activity and its inhibitors, overview
-
-
?
additional information
?
-
-
complex with fasciculin-2 exhibits hydrolytic activity in a buryrylcholinesterase-like kinetics, the switch appears to be a consequence of steric obstruction, but also the consequence of subtle rapid conformational changes around the catalytic site
-
?
additional information
?
-
-
development of an assay method for quantification of the product of enzymatic reaction using substrate as internal standard, thus eliminating the need for addition of an internal standard, mass spectrometric analysis, overview
-
-
?
additional information
?
-
-
activity detection using a capillary electrophoresis, EMMA, method, screening method development and optimization of experimental conditions, overview
-
-
?
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
acetylcholine + H2O
choline + acetate
-
-
-
?
acetylcholine + H2O
acetate + choline
-
-
-
-
?
acetylcholine + H2O
acetate + choline
-
acetylcholinesterase plays in vivo a key role in cholinergic transmission by catalysing the rapid hydrolysis of the neurotransmitter acetylcholine into acetate and choline
-
-
?
acetylcholine + H2O
choline + acetate
-
-
-
-
?
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(-)-3-O-acetylcassine
a semisynthetic alkaloid structure and stereochemistry by ESI-MS/MS and EI-MS
(-)-3-O-acetylspectaline
a semisynthetic alkaloid structure and stereochemistry by ESI-MS/MS and EI-MS
(-)-cassine
a piperidine alkaloid isolated from Senna spectabilis flowers, structure and stereochemistry by ESI-MS/MS and EI-MS
(-)-spectaline
a piperidine alkaloid isolated from Senna spectabilis flowers, structure and stereochemistry by ESI-MS/MS and EI-MS
(2E)-2-(4-hydroxy-3-methoxybenzylidene)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide
-
(2E)-2-(4-hydroxy-3-methoxybenzylidene)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide
-
(2E)-2-(4-hydroxy-3-methoxybenzylidene)-3-oxo-N-[6-(1,2,3,4-tetrahydroacridin-9-ylamino)hexyl]butanamide
-
(2E)-2-(4-hydroxybenzylidene)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide
-
(2E)-2-(4-hydroxybenzylidene)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide
-
(2E)-2-(4-hydroxybenzylidene)-3-oxo-N-[6-(1,2,3,4-tetrahydroacridin-9-ylamino)hexyl]butanamide
-
(6R,7S)-6-(acetyloxy)-8,8-dimethyl-2-oxo-7,8-dihydro-2H,6H-benzo[1,2-b:5,4-b']dipyran-7-yl (2Z)-2-methylbut-2-enoate
mixed-type inhibition
(6R,7S)-6-hydroxy-8,8-dimethyl-2-oxo-7,8-dihydro-2H,6H-benzo[1,2-b:5,4-b']dipyran-7-yl (2E)-2-methylbut-2-enoate
noncompetitive inhibition
(6R,7S)-6-hydroxy-8,8-dimethyl-2-oxo-7,8-dihydro-2H,6H-benzo[1,2-b:5,4-b']dipyran-7-yl 3-methylbut-2-enoate
mixed-type inhibition
(6R,7S)-6-methoxy-8,8-dimethyl-2-oxo-7,8-dihydro-2H,6H-benzo[1,2-b:5,4-b']dipyran-7-yl 3-methylbut-2-enoate
mixed-type inhibition
(6R,7S)-7-hydroxy-8,8-dimethyl-2-oxo-7,8-dihydro-2H,6H-benzo[1,2-b:5,4-b']dipyran-6-yl 4-methylpent-3-enoate
mixed-type inhibition
1-(2-chloro-benzyl)-2,2-diethyl-2,3-dihydro-1H-quinazolin-4-one
-
1-(2-chloro-benzyl)-2,2-diisobutyl-2,3-dihydro-1H-quinazolin-4-one
-
1-(2-chloro-benzyl)-2,2-dimethyl-2,3-dihydro-1Hquinazolin-4-one
-
1-(2-chloro-benzyl)-2-(4-chloro-phenyl)-2-methyl-2,3-dihydro-1H-quinazolin-4-one
-
1-(2-chloro-benzyl)-2-ethyl-2-methyl-2,3-dihydro-1H-quinazolin-4-one
-
1-(2-chloro-benzyl)-2-isobutyl-2-methyl-2,3-dihydro-1H-quinazolin-4-one
-
1-(2-chloro-benzyl)-2-methyl-2-phenyl-2,3-dihydro-1H-quinazolin-4-one
-
1-(2-chloro-benzyl)-2-methyl-2-propyl-2,3-dihydro-1H-quinazolin-4-one
-
1-(2-fluorobenzyl)-N-[6-(1H-indol-1-yl)hexyl]piperidin-4-amine
-
1-(2-fluorobenzyl)-N-[8-(1H-indol-1-yl)octyl]piperidin-4-amine
-
1-(3-chlorobenzyl)-N-[6-(1H-indol-1-yl)hexyl]piperidin-4-amine
-
1-(3-chlorobenzyl)-N-[8-(1H-indol-1-yl)octyl]piperidin-4-amine
-
1-(4-chloro-benzyl)-2,2-diethyl-2,3-dihydro-1H-quinazolin-4-one
-
1-(4-chloro-benzyl)-2,2-diisobutyl-2,3-dihydro-1H-quinazolin-4-one
-
1-(4-chloro-benzyl)-2-(4-chloro-phenyl)-2-methyl-2,3-dihydro-1H-quinazolin-4-one
-
1-(4-chloro-benzyl)-2-ethyl-2-methyl-2,3-dihydro-1H-quinazolin-4-one
-
1-(4-chloro-benzyl)-2-isobutyl-2-methyl-2,3-dihydro-1H-quinazolin-4-one
-
1-(4-chloro-benzyl)-2-methyl-2-phenyl-2,3-dihydro-1H-quinazolin-4-one
-
1-(4-chloro-benzyl)-2-methyl-2-propyl-2,3-dihydro-1H-quinazolin-4-one
-
1--(4-chloro-benzyl)-2,2-dimethyl-2,3-dihydro-1H-quinazolin-4-one
-
1-benzyl-2-(4-chloro-phenyl)-2-methyl-2,3-dihydro-1H-quinazolin-4-one
-
1-benzyl-2-isobutyl-2-methyl-2,3-dihydro-1H-quinazolin-4-one
-
1-benzyl-N-[3-(2,3-dihydro-1H-indol-1-yl)propyl]piperidin-4-amine
-
1-benzyl-N-[5-(2,3-dihydro-1H-indol-1-yl)pentyl]piperidin-4-amine
-
1-ethyl-2-isobutyl-2-methyl-2,3-dihydro-1H-quinazolin-4-one
-
2-(3-[[1-(2-fluorobenzyl)piperidin-4-yl]amino]propyl)-1H-isoindole-1,3(2H)-dione
-
2-(3-[[1-(3-chlorobenzyl)piperidin-4-yl]amino]propyl)-1H-isoindole-1,3(2H)-dione
-
2-(3-[[1-(4-hydroxybenzyl)piperidin-4-yl]amino]propyl)-1H-isoindole-1,3(2H)-dione
-
2-(3-[[1-(4-methoxybenzyl)piperidin-4-yl]amino]propyl)-1H-isoindole-1,3(2H)-dione
-
2-(4-chloro-phenyl)-1-ethyl-2-methyl-2,3-dihydro-1H-quinazolin-4-one
-
2-(4-hydroxy-3-methoxybenzyl)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide
-
2-(4-hydroxy-3-methoxybenzyl)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide
-
2-(4-hydroxy-3-methoxybenzyl)-3-oxo-N-[6-(1,2,3,4-tetrahydroacridin-9-ylamino)hexyl]butanamide
neuroprotective effect of K3-2 against H2O2-induced toxicity
2-(4-hydroxybenzyl)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide
-
2-(4-hydroxybenzyl)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide
-
2-(4-hydroxybenzyl)-3-oxo-N-[6-(1,2,3,4-tetrahydroacridin-9-ylamino)hexyl]butanamide
-
2-(6-[[1-(2-fluorobenzyl)piperidin-4-yl]amino]hexyl)-1H-isoindole-1,3(2H)-dione
-
2-(6-[[1-(3-chlorobenzyl)piperidin-4-yl]amino]hexyl)-1H-isoindole-1,3(2H)-dione
-
2-(6-[[1-(4-hydroxybenzyl)piperidin-4-yl]amino]hexyl)-1H-isoindole-1,3(2H)-dione
-
2-(6-[[1-(4-methoxybenzyl)piperidin-4-yl]amino]hexyl)-1H-isoindole-1,3(2H)-dione
-
2-(8-[[1-(2-fluorobenzyl)piperidin-4-yl]amino]octyl)-1H-isoindole-1,3(2H)-dione
-
2-(8-[[1-(3-chlorobenzyl)piperidin-4-yl]amino]octyl)-1H-isoindole-1,3(2H)-dione
-
2-(8-[[1-(4-hydroxybenzyl)piperidin-4-yl]amino]octyl)-1H-isoindole-1,3(2H)-dione
-
2-(8-[[1-(4-methoxybenzyl)piperidin-4-yl]amino]octyl)-1H-isoindole-1,3(2H)-dione
-
2-amino-3-((1R)-1-cyclohexyl-2-[(cyclohexylcarbonyl)amino]ethyl)-6-phenoxyquinazolin-3-ium
-
2-oxo-N-[2-(piperidin-1-yl)ethyl]-2H-chromene-3-carboxamide
-
2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydro-1H-inden-1-one
-
2-[(5-acetyl-6-methyl-4-phenyl-1,4-dihydropyrimidin-2-yl)sulfanyl]-N-phenylacetamide
-
2-[3-[(1-benzylpiperidin-4-yl)amino]propyl]-1H-isoindole-1,3(2H)-dione
-
2-[5-[(1-benzylpiperidin-4-yl)amino]pentyl]-1H-isoindole-1,3(2H)-dione
-
2-[6-[(1-benzylpiperidin-4-yl)amino]hexyl]-1H-isoindole-1,3(2H)-dione
-
2-[8-[(1-benzylpiperidin-4-yl)amino]octyl]-1H-isoindole-1,3(2H)-dione
-
2-[[5-acetyl-6-methyl-4-(4-phenoxyphenyl)-1,4-dihydropyrimidin-2-yl]sulfanyl]-N-phenylacetamide
-
3-oxo-N-[(1,2,3,4-tetrahydroacridin-9-ylamino)methyl]butanamide
-
3-oxo-N-[2-(1,2,3,4-tetrahydroacridin-9-ylamino)ethyl]butanamide
-
3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide
-
3-oxo-N-[5-(1,2,3,4-tetrahydroacridin-9-ylamino)pentyl]butanamide
-
3-[(1S)-1-(dimethylamino)ethyl]phenyl ethyl(methyl)carbamate
-
4-[(4-[[6-(1H-indol-1-yl)hexyl]amino]piperidin-1-yl)methyl]phenol
-
4-[(4-[[8-(1H-indol-1-yl)octyl]amino]piperidin-1-yl)methyl]phenol
-
6,8-dibromo-2-(4-chlorophenyl)-2-methyl-2,3-dihydroquinazolin-4(1H)-one
-
6-formyl umbelliferone
isolated from Angelica decursiva, noncompetitive inhibition
8-formyl umbelliferone
noncompetitive inhibition, forms a hydrogen bond with the Glu199 residue. In addition, residues Trp84, Gly117, Gly118, Phe330, His440, and Gly441 are involved in hydrophobic interactions with the coumarin
ethyl 2-oxo-7-[2-(piperidin-1-yl)ethoxy]-2H-chromene-3-carboxylate
-
ethyl 7-hydroxy-8-(3-methoxyphenyl)-2-oxo-2H-chromene-3-carboxylate
-
N-[4-[4-(1,3-benzothiazol-2-yl)phenoxy]butyl]-6-chloro-1,2,3,4-tetrahydroacridin-9-amine
-
N-[6-(1H-indol-1-yl)hexyl]-1-(4-methoxybenzyl)piperidin-4-amine
-
N-[8-(1H-indol-1-yl)octyl]-1-(4-methoxybenzyl)piperidin-4-amine
-
O-ethyl-S-[2-(diisopropylamino)-ethyl]-methylphosphonothioate
nerve agent VX
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
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
umbelliferone
isolated from Angelica decursiva, forms three hydrogen bonds with the interacting residues Tyr121, Phe288, and Arg289. Residues Phe288 and Arg289 are involved in strong hydrogen bonding interactions with the hydroxyl group at position C-7, and Tyr121 is also involved in hydrogen bonding interactions with the ketone group at position C-2. In particular, important peripheral anionic site (PAS) residues, Trp279 and Tyr334, are involved in hydrogen bonding interactions with umbelliferone
(+)-(1R,3R,6S)-9-benzyl-3-fluoro-2,4-dioxa-9-aza-3-phosphadecalin 3-oxide
-
-
(+)-(1R,3S,6S)-9-benzyl-3-fluoro-2,4-dioxa-9-aza-3-phosphadecalin 3-oxide
-
-
(+)-(1S,3R,6S)-9-benzyl-3-fluoro-2,4-dioxa-9-aza-3-phosphadecalin 3-oxide
-
-
(+)-(1S,3S,6S)-9-benzyl-3-fluoro-2,4-dioxa-9-aza-3-phosphadecalin 3-oxide
-
-
(+)-limonene
-
isolated from the ethanolic extract from the fruits of Pimpinella anisoides
(+)-sabinene
-
isolated from the ethanolic extract from the fruits of Pimpinella anisoides
(-)-(1R,3R,6R)-9-benzyl-3-fluoro-2,4-dioxa-9-aza-3-phosphadecalin 3-oxide
-
-
(-)-(1R,3S,6R)-9-benzyl-3-fluoro-2,4-dioxa-9-aza-3-phosphadecalin 3-oxide
-
-
(-)-(1S,3R,6R)-9-benzyl-3-fluoro-2,4-dioxa-9-aza-3-phosphadecalin 3-oxide
-
-
(-)-(1S,3S,6R)-9-benzyl-3-fluoro-2,4-dioxa-9-aza-3-phosphadecalin 3-oxide
-
-
(-)-3-O-acetyl-spectaline
-
isolated from flowers of Senna spectabilis
(1alpha,3beta,22R)-stigmast-5-ene-1,3,22-triol
-
i.e. haloxysterol A, isolated from Haloxylon recurvum
(1alpha,3beta,22R)-stigmasta-4,6-diene-1,3,22-triol
-
i.e. haloxysterol B, isolated from Haloxylon recurvum
(1alpha,3beta,5alpha,6beta,22R)-stigmastane-1,3,5,6,22-pentol
-
i.e. haloxysterol D, isolated from Haloxylon recurvum
(1S,2S,11bS)-4-[2-(acetyloxy)ethyl]-5-methyl-1,2,3,4,4a,5,6,11b-octahydro[1,3]dioxolo[4,5-j]phenanthridine-1,2-diyl diacetate
-
-
(1S,2S,11bS)-4-[2-(acetyloxy)ethyl]-5-methyl-1,2,4a,5,6,11b-hexahydro[1,3]dioxolo[4,5-j]phenanthridine-1,2-diyl diacetate
-
-
(2-methoxy-7-methyl-2-oxido-2,3,4,5-tetrahydro-1,2-oxaphosphepin-6-yl)methanol
-
-
(22R)-22-hydroxystigmasta-4,9(11)-dien-3-one
-
i.e. haloxysterol C, isolated from Haloxylon recurvum
(24S)-ethylcholesta-7,9(11),22(E)-triene-3beta-ol
-
isolated from Haloxylon recurvum
(2E)-1-(5-chloro-2-hydroxyphenyl)-3-(4-chlorophenyl)prop-2-en-1-one
-
-
(3,4-dimethoxyphenyl)(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-1-yl)methanol
-
-
(3aS,8aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl (2,3-dimethylphenyl)carbamate
-
-
(3aS,8aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl (2,4,6-trimethylphenyl)carbamate
-
-
(3aS,8aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl (2,4-dimethylphenyl)carbamate
-
-
(3aS,8aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl (2,5-dimethylphenyl)carbamate
-
-
(3aS,8aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl (2,6-dimethylphenyl)carbamate
-
-
(3aS,8aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl (2-ethylphenyl)carbamate
-
-
(3aS,8aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl (3,4-dimethylphenyl)carbamate
-
-
(3aS,8aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl (3-methylphenyl)carbamate
-
-
(3aS,8aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl (4-methylphenyl)carbamate
-
-
(3beta,4beta,5beta,6beta,8xi,9xi,14xi,17xi,22R)-4,28-dihydroxy-3-methoxy-1,26-dioxo-5,6:22,26-diepoxyergost-24-en-19-oic acid
-
-
(3beta,4beta,5beta,6beta,8xi,9xi,14xi,17xi,22R)-4,28-dihydroxy-3-methoxy-5,6:22,26-diepoxyergost-24-ene-1,26-dione
-
-
(3beta,4beta,6beta,8xi,9xi,14xi,17xi,22R)-4,6,27-trihydroxy-3-methoxy-22,26-epoxyergost-24-ene-1,26-dione
-
-
(3E)-3-([4-[2-(diethylamino)ethoxy]phenyl]methylidene)-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one
-
-
(3E)-3-([4-[3-(diethylamino)propoxy]phenyl]methylidene)-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one
-
-
(3E)-3-[(4-hydroxy-3,5-dimethoxyphenyl)methylidene]-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one
-
-
(3E)-3-[(4-[2-[diethenyl(methylidene)-l5-azanyl]ethoxy]phenyl)methylidene]-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one
-
-
(3E)-3-[(4-[3-[diethenyl(methylidene)-l5-azanyl]propoxy]phenyl)methylidene]-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one
-
-
(3R,4aS,9bS)-9-(chloromethyl)-9b-[2-[(ethoxycarbonyl)(methyl)amino]ethyl]-6-methoxy-3,4,4a,9b-tetrahydrodibenzo[b,d]furan-3-yl ethyl carbonate
-
-
(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
(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
(4aS,6R,8aS)-3-methoxy-11-methyl-5,6,10,11,13,14-hexahydro-4aH,9H-[1]benzofuro[3a,3,2-gh][3,4]benzoxazonin-6-ol
-
-
(4aS,6R,8aS)-3-methoxy-11-[8-[(4aS,6R,8aS)-3-methoxy-6-methyl-5,6,9,10-tetrahydro-4aH-[1]benzofuro[3a,3,2-ef][2]benzazepin-11(12H)-yl]octyl]-5,6,9,10,11,12-hexahydro-4aH-[1]benzofuro[3a,3,2-ef][2]benzazepin-6-ol
-
-
(4aS,6R,8aS)-3-[[12-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)dodecyl]oxy]-6-hydroxy-11-methyl-5,6,9,10-tetrahydro-4aH-[1]benzofuro[3a,3,2-ef][2]benzazepin-11-ium
-
-
(4aS,6R,8aS)-3-[[8-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)octyl]oxy]-6-hydroxy-11-methyl-5,6,9,10-tetrahydro-4aH-[1]benzofuro[3a,3,2-ef][2]benzazepin-11-ium
-
-
(4aS,6R,8aS)-6-hydroxy-3-methoxy-11-[10-[(4aS,6R,8aS)-3-methoxy-6-methyl-5,6,9,10-tetrahydro-4aH-[1]benzofuro[3a,3,2-ef][2]benzazepin-11(12H)-yl]decyl]-5,6,9,10-tetrahydro-4aH-[1]benzofuro[3a,3,2-ef][2]benzazepin-11-ium
-
-
(4aS,6R,8aS)-6-hydroxy-3-methoxy-11-[8-[(4aS,6R,8aS)-3-methoxy-6-methyl-5,6,9,10-tetrahydro-4aH-[1]benzofuro[3a,3,2-ef][2]benzazepin-11(12H)-yl]octyl]-5,6,9,10-tetrahydro-4aH-[1]benzofuro[3a,3,2-ef][2]benzazepin-11-ium
-
-
(4aS,6R,8aS)-6-hydroxy-3-methyl-11-(10-phenyldecyl)-5,6,9,10-tetrahydro-4aH-[1]benzofuro[3a,3,2-ef][2]benzazepin-11-ium
-
-
(4aS,6R,8aS)-6-hydroxy-3-methyl-11-(8-phenyloctyl)-5,6,9,10-tetrahydro-4aH-[1]benzofuro[3a,3,2-ef][2]benzazepin-11-ium
-
-
(4beta,5beta,6beta,8xi,9xi,14xi,17xi,22R)-4,27-dihydroxy-5,6:22,26-diepoxyergosta-2,24-diene-1,26-dione
-
-
(5alpha,6alpha,7alpha,8xi,9xi,14xi,17xi,22R)-5-hydroxy-20-methyl-6,7:22,26-diepoxyergosta-2,24-diene-1,26-dione
-
-
(E)-1-(2,4-dichlorobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
-
-
(E)-1-(2,6-dichlorobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
-
-
(E)-1-(2-bromobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
-
-
(E)-1-(2-chloro-6-fluorobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
-
-
(E)-1-(2-chlorobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
-
-
(E)-1-(2-fluorobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
-
-
(E)-1-(2-methylbenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
-
-
(E)-1-(2-nitrobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium bromide
-
-
(E)-1-(3,4-dichlorobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
-
-
(E)-1-(3-bromobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
-
-
(E)-1-(3-chlorobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium bromide
-
-
(E)-1-(3-fluorobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
-
-
(E)-1-(3-methoxylbenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
-
-
(E)-1-(3-methylbenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
-
-
(E)-1-(4-bromobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
-
-
(E)-1-(4-chlorobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
-
-
(E)-1-(4-chloromethylbenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
-
-
(E)-1-(4-fluorobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
-
-
(E)-1-(4-methoxybenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
-
-
(E)-1-(4-nitrobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
-
-
(E)-1-(benzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium bromide
-
-
(R)-(+)-endo-2-norbornyl-N-n-butylcarbamate
-
synthesis of enantiomers for stereoselective inhibition of AChE, overview. The S-enantiomer is more potent than the R-enantiomer
(R)-(+)-exo-2-norbornyl-N-n-butylcarbamate
-
synthesis of enantiomers for stereoselective inhibition of AChE, overview. The R-enantiomer is potent, while the S-enantiomer is inactive
(S)-(-)-endo-2-norbornyl-N-n-butylcarbamate
-
synthesis of enantiomers for stereoselective inhibition of AChE, overview. The S-enantiomer is more potent than the R-enantiomer
1,2,11,12-tetramethoxy-7-methyl-5,6-dihydro-4H,8H-pyrido[3,2,1-de]phenanthridinium
-
-
1,2,3,10,11-pentamethoxy-7-(methoxycarbonyl)-5,6-dihydro-4H,8H-pyrido[3,2,1-de]phenanthridinium
-
-
1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydroisoquinoline
-
-
1-methyl-1-[2-oxo-3-(7-oxo-7H-dibenzo[de,h]quinolin-9-yl)propyl]pyrrolidinium
-
-
1-methyl-1-[3-oxo-4-(7-oxo-7H-dibenzo[de,h]quinolin-9-yl)butyl]pyrrolidinium
-
-
1-methyl-1-[4-oxo-5-(7-oxo-7H-dibenzo[de,h]quinolin-9-yl)pentyl]pyrrolidinium
-
-
1-methyl-4,5-dihydro[1,3]dioxolo[4,5-j]pyrrolo[3,2,1-de]phenanthridin-6-ium-2-olate
-
-
13-methyl-5,8-dihydro-6H isoquino[1,2b]quinazolin-13-ium chloride
-
-
13-methyl-5,8-dihydro-6H-isoquino[1,2b]quinazolin-13-ium chloride
-
-
2-(dimethylamino)-7-ethyl-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one
-
50% inhibition at 0.011 mM
2-(dimethylamino)-7-isobutyl-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one
-
50% inhibition at 0.00036 mM
2-(dimethylamino)-7-methyl-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one
-
50% inhibition at 0.039 mM
2-amino-7-benzyl-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one
-
50% inhibition at 0.0059 mM
2-amino-7-benzyl-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)thiazin-4-one
-
50% inhibition at 0.0012 mM
2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydro-1H-inden-1-one
-
-
2-[4-(5(6)-chloro-1H-benzo[d]imidazol-2-yl)phenoxy]-N,N-diethylethanamine
-
-
2-[4-(5(6)-chloro-1H-benzo[d]imidazol-2-yl)phenoxy]-N,N-dimethylethanamine
-
-
2-[[2-[(5aS,7R,9aS)-1-formyl-7-hydroxy-4-methoxy-6,7-dihydrodibenzo[b,d]furan-9a(5aH)-yl]ethyl](methyl)amino]butanoic acid
-
-
2-[[2-[(5aS,7R,9aS)-7-hydroxy-1-(hydroxymethyl)-4-methoxy-6,7-dihydrodibenzo[b,d]furan-9a(5aH)-yl]ethyl](methyl)amino]butanoic acid
-
-
24-ethyl-cholest-7-ene-3,5,6-triol
-
isolated from Haloxylon recurvum
3-(4-propoxybenzyl)-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one
-
-
3-(4-[2-[diethenyl(methylidene)-l5-azanyl]ethoxy]benzyl)-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one
-
-
3-(4-[3-[diethenyl(methylidene)-l5-azanyl]propoxy]benzyl)-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one
-
-
3-(9-hydroxy-5,6-dimethyl-7H,9H-pyrano[3,4,5-ij]isoquinolin-9-yl)propane-1,2-diol
-
-
3-(9-methoxy-5,6-dimethyl-7H,9H-pyrano[3,4,5-ij]isoquinolin-9-yl)propane-1,2-diol
-
-
3-hydroxy-2,2,6-trimethyl-3,4,5,6-tetrahydro-2H-pyrano[3,2c] quinoline 5-one
-
isolated from Skimmia laureola
3-N,N-diethylaminophenyl-N'-(1-alkyl) carbamates
-
inhibit quickly by carbamoylation
3-[4-[3-(diethylamino)propoxy]benzyl]-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one
-
-
4-ethyl-5-hexyl-5,6-dihydro[1,3]dioxolo[4,5-j]phenanthridine hydrobromide
-
-
4-nitrophenyl allylcarbamate
-
detailed kinetic analysis and mechanism
4-nitrophenyl benzylcarbamate
-
detailed kinetic analysis and mechanism
4-nitrophenyl butylcarbamate
-
detailed kinetic analysis and mechanism
4-nitrophenyl hexylcarbamate
-
detailed kinetic analysis and mechanism
4-nitrophenyl octylcarbamate
-
detailed kinetic analysis and mechanism
4-nitrophenyl phenylcarbamate
-
detailed kinetic analysis and mechanism
4-nitrophenyl tert-butylcarbamate
-
detailed kinetic analysis and mechanism
4-[2-[4-(5(6)-chloro-1H-benzo[d]imidazol-2-yl)phenoxy]ethyl]morpholine
-
-
4-[2-[4-(5(6)-methyl-1H-benzo[d]imidazol-2-yl)phenoxy]ethyl]morpholine
-
-
5(6)-chloro-2-[4-[2-(piperidin-1-yl)ethoxy]phenyl]-1H-benzo[d]imidazole
-
-
5(6)-chloro-2-[4-[2-(pyrrolidin-1-yl)ethoxy]phenyl]-1H-benzo[d]imidazole
-
-
5(6)-methyl-2-[4-[2-(piperidin-1-yl)ethoxy]phenyl]-1H-benzo[d]imidazole
-
-
5(6)-methyl-2-[4-[2-(pyrrolidin-1-yl)ethoxy]phenyl]-1H-benzo[d]imidazole
-
-
5,6-dimethoxy-9-prop-2-en-1-yl-7H,9H-pyrano[3,4,5-ij]isoquinolin-9-ol
-
-
5alpha,8alpha-epidioxy-(24S)-ethylcholesta-6,9(11),22(E)-triene-3beta-ol
-
isolated from Haloxylon recurvum
7-benzoyl-2-(dimethylamino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one
-
50% inhibition at 0.036 mM
7-benzyl-2-((3,4-dimethoxybenzyl)(methyl)amino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one
-
50% inhibition at 0.00033 mM
7-benzyl-2-(4-benzylpiperazin-1-yl)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one
-
50% inhibition at 0.00132 mM
7-benzyl-2-(benzyl(methyl)amino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one
-
50% inhibition at 0.00084 mM
7-benzyl-2-(benzylamino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one
-
50% inhibition at 0.00286 mM
7-benzyl-2-(benzylamino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)thiazin-4-one
-
50% inhibition at 0.0052 mM
7-benzyl-2-(cyclohexylamino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)thiazin-4-one
-
50% inhibition at 0.00282 mM
7-benzyl-2-(diethylamino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one
-
50% inhibition at 0.00208 mM
7-benzyl-2-(dimethylamino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one
-
50% inhibition at 0.00089 mM
7-benzyl-2-(isopropylamino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one
-
50% inhibition at 0.00074 mM
7-benzyl-2-(isopropylamino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)thiazin-4-one
-
50% inhibition at 0.00058 mM
7-benzyl-2-(phenylamino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one
-
50% inhibition at 0.00094 mM
7-benzyl-2-(phenylamino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)thiazin-4-one
-
50% inhibition at 0.00103 mM
7-benzyl-2-(propan-2-ylamino)-1,2,5,6,7,8-hexahydro-4H-pyrido[4',3':4,5]thieno[2,3-d][1,3]thiazin-4-one
-
the substance acts as a hyperbolic mixed-type inhibitor
7-benzyl-2-morpholin-4-yl-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one
-
50% inhibition at 0.00077 mM
9-(2-oxo-3-pyrrolidin-1-ylpropyl)-7H-dibenzo[de,h]quinolin-7-one
-
-
9-(2-oxo-5-pyrrolidin-1-ylpentyl)-7H-dibenzo[de,h]quinolin-7-one
-
-
9-(4-[[2-(dimethylamino)ethyl]amino]-2-oxobutyl)-7H-dibenzo[de,h]quinolin-7-one
-
-
9-O-[4-(phenylol-1-yloxy)butyl] berberine bromide
-
most potent berberine derivative inhibitor, mixed type inhibition
9-[3-(dimethylamino)-2-oxopropyl]-7H-dibenzo[de,h]quinolin-7-one
-
-
9-[4-[(2-hydroxyethyl)amino]-2-oxobutyl]-7H-dibenzo[de,h]quinolin-7-one
-
-
9-[5-(dimethylamino)-2-oxopentyl]-7H-dibenzo[de,h]quinolin-7-one
-
-
acetonitrile
-
a competitive pseudo-inhibition is observed for 6% acetonitrile
acrifoline
-
isolated from ethanolic extracts of Lycopodium annotinum ssp. alpestre
anhydrolycodoline
-
isolated from ethanolic extracts of Lycopodium annotinum ssp. alpestre
annotine
-
isolated from ethanolic extracts of Lycopodium annotinum ssp. alpestre
annotine N-oxide
-
isolated from ethanolic extracts of Lycopodium annotinum ssp. alpestre
annotinine
-
isolated from ethanolic extracts of Lycopodium annotinum ssp. alpestre
bis-N,N-dimethylfulleropyrrolidinium salts
-
inhibitory activity and mechanism of cationic fulleropyrrolidinium regioisomers, AChE docking parameters, molecular modleing, overview
-
conessimin
-
strong, reversible and noncompetitive inhibition, 98% inhibition at 0.1 mg/ml
coumarin 106
-
exhibits mixed-type AChE inhibition, targets a primary binding site at the active gorge and a secondary peripheral anionic binding site. Analysis of inhibitor binding, overview
diisopropyl phosphorofluoridate
-
synthesis and evaluation of novel bis-pyridinium oximes as reactivators of DFP-inhibited acetylcholinesterase, overview. 1,3-Dimethoxymethyl benzene bis-[4,40-(hydroxyiminomethyl) pyridinium] dichloride and 1,4-dimethoxy but-2-ene bis-[4,40-(hydroxyiminomethyl) pyridinium] dichloride show high efficacy
ethyl [2-[(5aS,7R,9aS)-1-formyl-7-hydroxy-4-methoxy-6,7-dihydrodibenzo[b,d]furan-9a(5aH)-yl]ethyl]methylcarbamate
-
-
ethyl [2-[(5aS,7R,9aS)-7-hydroxy-1-(hydroxymethyl)-4-methoxy-6,7-dihydrodibenzo[b,d]furan-9a(5aH)-yl]ethyl]methylcarbamate
-
-
gallamine
-
inhibition by gallamine follows the steric blockade hypothesis, i.e. only substrate association to as well as substrate-product dissociation from the active site were reduced in the presence of the inhibitor
giganteone C
-
isolated from ethyl acetate and methanol extracts from the leaves and the fruits of Myristica crassa, structure analysis by mass spectrometry
gnidioidine
-
isolated from ethanolic extracts of Lycopodium annotinum ssp. alpestre
lannotinidine D
-
isolated from ethanolic extracts of Lycopodium annotinum ssp. alpestre
lycodoline
-
isolated from ethanolic extracts of Lycopodium annotinum ssp. alpestre
lycofoline
-
isolated from ethanolic extracts of Lycopodium annotinum ssp. alpestre
lycoposerramine M
-
isolated from ethanolic extracts of Lycopodium annotinum ssp. alpestre
maingayone B
-
isolated from ethyl acetate and methanol extracts from the leaves and the fruits of Myristica crassa, structure analysis by mass spectrometry
maingayone C
-
isolated from ethyl acetate and methanol extracts from the leaves and the fruits of Myristica crassa, structure analysis by mass spectrometry
malabaricone A
-
isolated from ethyl acetate and methanol extracts from the leaves and the fruits of Myristica crassa, structure analysis by mass spectrometry
malabaricone B
-
isolated from ethyl acetate and methanol extracts from the leaves and the fruits of Myristica crassa, structure analysis by mass spectrometry
malabaricone C
-
isolated from ethyl acetate and methanol extracts from the leaves and the fruits of Myristica crassa, structure analysis by mass spectrometry
methyl (2R,5R)-5-[(benzyloxy)methyl]-2-methoxy-7-methyl-2,3,4,5-tetrahydro-1,2-oxaphosphepine-6-carboxylate 2-oxide
-
-
methyl (2S,5R)-5-[(benzyloxy)methyl]-2-methoxy-7-methyl-2,3,4,5-tetrahydro-1,2-oxaphosphepine-6-carboxylate 2-oxide
-
-
methyl (3-{4-[({[5-(dimethylamino)naphthalen-1-yl]sulfonyl}amino)methyl]-1H-1,2,3-triazol-1-yl}propyl)phosphonofluoridate
-
-
methyl (3-{4-[({[6-(diethylamino)-2-oxo-2H-chromen-3-yl]carbonyl}amino)methyl]-1H-1,2,3-triazol-1-yl}propyl)phosphonofluoridate
-
-
methyl (4-{4-[({[5-(dimethylamino)naphthalen-1-yl]sulfonyl}amino)methyl]-1H-1,2,3-triazol-1-yl}butyl)phosphonofluoridate
-
-
methyl (4-{4-[({[6-(diethylamino)-2-oxo-2H-chromen-3-yl]carbonyl}amino)methyl]-1H-1,2,3-triazol-1-yl}butyl)phosphonofluoridate
-
-
methyl 1-methoxy-5-methyl-1,2,3,6-tetrahydrophosphinine-4-carboxylate 1-oxide
-
-
methyl 2-methoxy-7-methyl-2,3,4,5-tetrahydro-1,2-oxaphosphepine-6-carboxylate 2-oxide
-
-
methyl [3-(4-{[(4-{(E)-[4-(dimethylamino)phenyl]diazenyl}benzoyl)amino]methyl}-1H-1,2,3-triazol-1-yl)propyl]phosphonofluoridate
-
-
methyl [3-(4-{[(pyren-2-ylsulfonyl)amino]methyl}-1H-1,2,3-triazol-1-yl)propyl]phosphonofluoridate
-
-
methyl [4-(4-{[(4-{(E)-[4-(dimethylamino)phenyl]diazenyl}benzoyl)amino]methyl}-1H-1,2,3-triazol-1-yl)butyl]phosphonofluoridate
-
-
methyl [4-(4-{[(pyren-2-ylsulfonyl)amino]methyl}-1H-1,2,3-triazol-1-yl)butyl]phosphonofluoridate
-
-
methyl {3-[4-({[(6-methoxy-2-oxo-2H-chromen-3-yl)carbonyl]amino}methyl)-1H-1,2,3-triazol-1-yl]propyl}phosphonofluoridate
-
-
methyl {4-[4-({[(6-methoxy-2-oxo-2H-chromen-3-yl)carbonyl]amino}methyl)-1H-1,2,3-triazol-1-yl]butyl}phosphonofluoridate
-
-
N,N,N-trimethyl-2-oxo-3-(7-oxo-7H-dibenzo[de,h]quinolin-9-yl)propan-1-aminium
-
-
N,N,N-trimethyl-3-oxo-4-(7-oxo-7H-dibenzo[de,h]quinolin-9-yl)butan-1-aminium
-
-
N,N,N-trimethyl-4-oxo-5-(7-oxo-7H-dibenzo[de,h]quinolin-9-yl)pentan-1-aminium
-
-
N,N-diethyl-2-[4-(5(6)-methyl-1H-benzo[d]imidazol-2-yl)phenoxy]ethanamine
-
-
N,N-dimethyl-2-[4-(5(6)-methyl-1H-benzo[d]imidazol-2-yl)phenoxy]ethanamine
-
-
N-(2-phenylethyl)-N-[(12Z)-7,8,9,10-tetrahydroazepino [2,1b]quinazolin-12(6H)-ylidene]amine
-
-
N-[2-[4-(1H-benzo[d]imidazol-2-yl)phenoxy]ethyl]-N-isopropylpropan-2-amine
-
-
N-[2-[4-(5(6)-chloro-1H-benzo[d]imidazol-2-yl)phenoxy]ethyl]-N-isopropylpropan-2-amine
-
-
paraoxon-methyl
-
inhibition mechanism and reactivation of paraoxon-methyl-inhibited AChE by pyridine-2-aldoxime methochloride, overview
polyamidoamine dendrimer PAMAM G3.5
-
0.1 mM, 75% residual activity due to changes in enzyme conformation
-
polyamidoamine dendrimer PAMAM G4
-
0.1 mM, 40% residual activity due to changes in enzyme conformation
-
polyamidoamine dendrimer PAMAM-OH G4
-
0.1 mM, 85% residual activity due to changes in enzyme conformation
-
serpentine
-
isolated from aqueous extracts of Catharanthus roseus roots
trans-anethole
-
isolated from the ethanolic extract from the fruits of Pimpinella anisoides
Triton X-100
-
uncompetitive inhibition at 0.01%, below the critical micelle concentration, and above at concentration higher than 0.013%
galantamine
galantamine competes with the substrate for binding to the active site of enzyme AChE in a reversible manner, inhibitory mechanism, overview
carvacrol
-
in vitro inhibition, compound of the essential oil of Thymus vulgaris
galanthamine
-
a naturally occurring alkaloid and a drug for the treatment of mild to moderate Alzheimer's disease
paraoxon
-
an organophosphate compound, a quasi-irreversible AChE inhibitor
tacrine
-
a mixed-type inhibitor with a strong noncompetitive component, completely blocks deacylation of the acyl-enzyme
tacrine
-
i.e. 9-amino-1,2,3,4-tetrahydroacridine hydrochloride, 54.2% inhibition at 0.1 mM, mixed-type inhibition
thymohydroquinone
-
high in vitro inhibition, compound of the essential oil of Thymus vulgaris
Thymol
-
in vitro inhibition, compound of the essential oil of Thymus vulgaris
thymoquinone
-
in vitro inhibition, compound of the essential oil of Thymus vulgaris
additional information
design, synthesis, and biological evaluation of multifunctional tacrine-curcumin hybrids as cholinesterase inhibitors with metal ions-chelating and neuroprotective properties, overview. The hybrid compounds show good cholinesterase inhibitory activity, some of the compounds exhibited different selectivity on acetylcholinesterase or butyrylcholinesterase due to the structural difference. Structure-activity relationships, molecular modelling, overview
-
additional information
designed and molecular recognition studies of coumarin-based inhibitors towards acetylcholinesterase (AChE), molecular docking simulations, dissociation constant and bound conformations of these inhibitors within the inhibitor-AChE complex, overview. The docking simulations mimic NMR results
-
additional information
evaluation of a combination of both anticholinesterase and beta-amyloid anti-aggregation activities in one molecule, and therapeutic potential in vivo. Design and synthesis of 28 compounds as derivatives of donepezil that contain the N-benzylpiperidine moiety combined with the phthalimide or indole moieties. No or poor inhibition by 23, 27, 28, 30, 38, 39, 40, and 41
-
additional information
evaluation of the potential of six dihydroxanthyletin-type coumarins, isolated from Angelica decursiva, to inhibit acetylcholinesterase (AChE), butyrylcholinesterase (BChE, EC 3.1.1.8), and beta-site amyloid precursor protein cleaving enzyme 1 (BACE1, EC 3.4.23.46). AChE protein-ligand docking studies, overview
-
additional information
mass spectrometric analysis and inhibitory potency of homologous piperidine alkaloids as acetylcholinesterase inhibitors, overview. Besides other aspects, the 2-methyl-3-hydroxypiperidine moiety is an important interaction site for the observed activity
-
additional information
molecular docking, modelling, overview
-
additional information
synthesis, crystal structure determination, biological screening, and docking studies of N1-substituted derivatives of 2,3-dihydroquinazolin-4(1H)-one as inhibitors of cholinesterases, structure-activity relationships, overview
-
additional information
thiols block the enzymatic etching of gold nanorods(thiocholine on the rate of horseradish peroxidase-catalyzed AuNR etching), application to colorimetric detection of acetylcholinesterase activity and its inhibitors, method, detailed overview
-
additional information
-
inhibition of enzyme activity after exposure to cellular phone irradiation for more than 10 min. Irradiation induces formation of a enzyme hydrogel from the assembly of highly hydrated protein molecules
-
additional information
-
proposed mechanism for enzyme inhibition by N-butylcarbamates and detailed kinetics of inhibition
-
additional information
-
some inhibitors fullfill the competitive inhibition model with irreversible reaction between enzyme and inhibitor, but e.g. not galantamin
-
additional information
-
the enzyme is not affected by ethanol concentrations up to 500 mM
-
additional information
-
binding structures and inhibitory potencies of isosorbide di-esters, that are mixed inhibitors of the enzyme forming a ternary enzyme-inhibitor-substrate complex, molecular modelling, overview. The di-esters dock within the butyrylcholinesterase gorge in a very different manner, with the ester side chain at the 5-position occupying the acyl pocket at residues Leu286 and Val288, and the 2-ester binding to Trp82. The carbonyl group of the 2-ester is susceptible to nucleophilic attack by Ser198 of the catalytic triad. The larger residues of the acyl pocket in acetylcholinesterase prevent binding in this manner
-
additional information
-
inhibitor screening by solid-phase extraction-liquid chromatography/electrospray ionisation-octopole-orthogonal acceleration time-of-flight-mass spectrometry and novel thin-layer chromatography-based bioautography, overview
-
additional information
-
potency and mechanism of diverse enzyme inhibitors, corydaline and ribalinine, isolated from Skimmia laureola, are specific for acetylcholinesterase, overview
-
additional information
-
selectivity and inhibitory potency of isaindigotone derivatives for inhibition of AChE
-
additional information
-
acetylcholinesterase inhibition induced by endogenous neurotoxin with an enzyme-semiconductor photoelectrochemical system, method development and evaluation, overview
-
additional information
-
adsorption and inhibition of AChE by eight nanoparticles, SiO2, TiO2, Al2O3, Al, Cu, Cu-C (carbon-coated copper), multiwalled carbon nanotubes (MWCNT) and single-walled carbon nanotubes (SWCNT), adsorption and inhibition rates of AChE by different nanoparticles, overview
-
additional information
-
chromophore-linked fluorophosphonate inhibitors show bimolecular inhibition constants ranging from 0.3 * 105 M/min to 10.4 * 105 M/min
-
additional information
-
commercially available essential oils extracted from Artemisia dracunculus L., Inula graveolens L., Lavandula officinalis Chaix, and Ocimum sanctum L. show inhibitory activity on the enzyme, with highest inhibitory activity of Artemisia dracunculus oil with an IC50 of 0.058 mg/ml, overview
-
additional information
-
comparison of bisquaternary pyridinium oximes in in vitro reactivation paraoxon-inhibited and tabun-inhibited acetylcholinesterase from Electrophorus electricus and Homo sapiens, overview. Effects on reactivation potency of compounds bearing aliphatic linkers and heteroaromatic linkers, kinetics, overview
-
additional information
-
descending order of inhibitory potency is tacrine, edrophonium, neostigmine, eserine, pyridostigmine
-
additional information
-
ethanolic extract from the fruits of Pimpinella anisoides, an aromatic plant and a spice, exhibits activity against AChE with an IC50 value of 0.2275 mg/ml, chemical composition of the extract, GC analysis, overview
-
additional information
-
extracts of Achyrocline tomentosa, Eupatorium viscidum, Ruprechtia apetala, Trichocline reptans, and Zanthoxylum coco present strong inhibition of AChE, higher than 80% at 1 mg/mL. The extracts from Ruprechtia apetala and Trichocline reptans are the most potent, showing complete inhibition of the enzyme with IC50 values 0.0779 and 0.1118 mg/mL, respectively, overview. Acetylcholinesterase inhibitory activity of organic and aqueous fractions obtained from extracts of diverse other plants of central Argentina, overview. IC50 value of Achyrocline tomentosa extract is 0.485 mg/ml, of Eupatorium viscidum is 0.479 mg/ml, and 0.158 mg/ml for extract of Zanthoxylum coco
-
additional information
-
inhibitor analysis using capillary electrophoresis with contactless conductivity detection, method development, overview
-
additional information
-
inhibitor design and evaluation using cardanol derivatives and the B3LYP method, structures with substitution by N,N-dimethycarbamoyl, N,N-dimethylamine, and pyrrolidine groups are better correlated to rivastigmine, and represent possible AChE inhibitors against Alzheimer's disease, overview. Cardanol is a non-isoprenoid phenolic lipid of cashew Anacardium occidentale nut-shell liquid
-
additional information
-
interaction of acetylcholinesterase with acetonitrile and tacrine or gallamine results in a 7-10fold increase in the KI values, whereas the principal mode of inhibition is not affected by the organic solvent
-
additional information
-
isolation of acetylcholinesterase inhibitory activity of lycopodane-type alkaloids from the Icelandic Lycopodium annotinum ssp. alpestre, NMR structure determination, and molecular modelling of interactions of the alkaloids with the enzyme, overview
-
additional information
-
Mg2+ ameliorates inhibitory effects of AChE inhibitors
-
additional information
-
no inhibition by (S)-(-)-exo-2-norbornyl-N-n-butylcarbamate at 0.01 mM. Optically pure2-norbornyl-N-n-butylcarbamate enantiomers are synthesized from condensations of optically pure (R)-(1)-exo-, (S)-(2)-exo-, (R)-(1)-endo-, and (S)-(2)-endo-2-norborneols with n-butyl isocyanate, respectively. Molecular modeling, overview
-
additional information
-
synthesis and biological evaluation of berberine derivatives as potent acetylcholinesterase inhibitors, kinetic and molecular modeling studies, overview
-
additional information
-
synthesis and inhibitory potencies of 2(2-alkoxyphenyl)-1H-imidazoles and benzyl[1-(1H-imidazol-4(5)-yl)ethyl]carbamate compounds, inhibition mechanism, overview
-
additional information
-
synthesis and kinetic analysis of some phosphonate analogs of cyclophostin as inhibitors of acetylcholinesterase, mechanism of inhibition, overview
-
additional information
-
total alkaloidal extract from the seeds of Holarrhen antidysenterica strongly inhibit the enzyme with an IC50 value of 0.0061 mg/ml
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0644 - 0.0809
bis-N,N-dimethylfulleropyrrolidinium salts
-
pH 7.2
-
1.372
acetylthiocholine
-
25°C, pH 8.0, preparation exposed to cellular phone irradiation for 20 min
2.48 - 9.55
acetylthiocholine iodide
-
pH 7.4, 35°C, poly-acrylonitrile-membrane immobilized enzymes
additional information
additional information
Michaelis-Menten kinetics
-
additional information
additional information
Michaelis-Menten kinetic analysis and modelling with increasing pH of the reaction mixture with substrate acetlycholine and acetylthiocholine, deteiled overview
-
additional information
additional information
-
Michaelis-Menten kinetics of soluble and immobilized enzymes, overview
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.00544
(6R,7S)-6-(acetyloxy)-8,8-dimethyl-2-oxo-7,8-dihydro-2H,6H-benzo[1,2-b:5,4-b']dipyran-7-yl (2Z)-2-methylbut-2-enoate
pH 8.0, 22°C
0.01102
(6R,7S)-6-hydroxy-8,8-dimethyl-2-oxo-7,8-dihydro-2H,6H-benzo[1,2-b:5,4-b']dipyran-7-yl (2E)-2-methylbut-2-enoate
pH 8.0, 22°C
0.00744
(6R,7S)-6-hydroxy-8,8-dimethyl-2-oxo-7,8-dihydro-2H,6H-benzo[1,2-b:5,4-b']dipyran-7-yl 3-methylbut-2-enoate
pH 8.0, 22°C
0.00472
(6R,7S)-6-methoxy-8,8-dimethyl-2-oxo-7,8-dihydro-2H,6H-benzo[1,2-b:5,4-b']dipyran-7-yl 3-methylbut-2-enoate
pH 8.0, 22°C
0.00489
(6R,7S)-7-hydroxy-8,8-dimethyl-2-oxo-7,8-dihydro-2H,6H-benzo[1,2-b:5,4-b']dipyran-6-yl 4-methylpent-3-enoate
pH 8.0, 22°C
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
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
0.00059
7-benzyl-2-(propan-2-ylamino)-1,2,5,6,7,8-hexahydro-4H-pyrido[4',3':4,5]thieno[2,3-d][1,3]thiazin-4-one
-
in presence of acetonitrile at 6% v/v
0.000045
9-O-[4-(phenylol-1-yloxy)butyl] berberine bromide
-
pH 8.0, 37°C
0.0156 - 0.0314
bis-N,N-dimethylfulleropyrrolidinium salts
-
pH 7.2
-
0.31
methyl 1-methoxy-5-methyl-1,2,3,6-tetrahydrophosphinine-4-carboxylate 1-oxide
-
pH 7.5, 25°C
0.076
methyl 2-methoxy-7-methyl-2,3,4,5-tetrahydro-1,2-oxaphosphepine-6-carboxylate 2-oxide
-
pH 7.5, 25°C
0.0031
neostigmine bromide
-
pH 7.0, 30°C, substrate acetylthiocholine
0.0047
neostigmine bromide
-
pH 7.0, 30°C, substrate propionylthiocholine
additional information
additional information
inhibition kinetics
-
additional information
additional information
-
inhibition kinetics
-
additional information
additional information
-
inhibition kinetics, overview
-
additional information
additional information
-
inhibition kinetics, value of carbamoylation inhibition
-
additional information
additional information
-
inhibition kinetics of 2(2-alkoxyphenyl)-1H-imidazoles and benzyl[1-(1H-imidazol-4(5)-yl)ethyl]carbamate compounds, overview
-
additional information
additional information
-
inhibition mechanism analysis and kinetics, overview
-
additional information
additional information
-
inhibition rate constants, overview
-
additional information
additional information
-
nonlinear Michaelis-Menten inhibition kinetics, detailed overview
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.00126
(2E)-2-(4-hydroxy-3-methoxybenzylidene)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide
Electrophorus electricus
pH 8.0, 37°C
0.0021
(2E)-2-(4-hydroxy-3-methoxybenzylidene)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide
Electrophorus electricus
pH 8.0, 37°C
0.00029
(2E)-2-(4-hydroxy-3-methoxybenzylidene)-3-oxo-N-[6-(1,2,3,4-tetrahydroacridin-9-ylamino)hexyl]butanamide
Electrophorus electricus
pH 8.0, 37°C
0.00964
(2E)-2-(4-hydroxybenzylidene)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide
Electrophorus electricus
pH 8.0, 37°C
0.0038
(2E)-2-(4-hydroxybenzylidene)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide
Electrophorus electricus
pH 8.0, 37°C
0.00295
(2E)-2-(4-hydroxybenzylidene)-3-oxo-N-[6-(1,2,3,4-tetrahydroacridin-9-ylamino)hexyl]butanamide
Electrophorus electricus
pH 8.0, 37°C
0.00371
(6R,7S)-6-(acetyloxy)-8,8-dimethyl-2-oxo-7,8-dihydro-2H,6H-benzo[1,2-b:5,4-b']dipyran-7-yl (2Z)-2-methylbut-2-enoate
Electrophorus electricus
pH 8.0, 22°C
0.00109
(6R,7S)-6-hydroxy-8,8-dimethyl-2-oxo-7,8-dihydro-2H,6H-benzo[1,2-b:5,4-b']dipyran-7-yl (2E)-2-methylbut-2-enoate
Electrophorus electricus
pH 8.0, 22°C
0.00184
(6R,7S)-6-hydroxy-8,8-dimethyl-2-oxo-7,8-dihydro-2H,6H-benzo[1,2-b:5,4-b']dipyran-7-yl 3-methylbut-2-enoate
Electrophorus electricus
pH 8.0, 22°C
0.0029
(6R,7S)-6-methoxy-8,8-dimethyl-2-oxo-7,8-dihydro-2H,6H-benzo[1,2-b:5,4-b']dipyran-7-yl 3-methylbut-2-enoate
Electrophorus electricus
pH 8.0, 22°C
0.00401
(6R,7S)-7-hydroxy-8,8-dimethyl-2-oxo-7,8-dihydro-2H,6H-benzo[1,2-b:5,4-b']dipyran-6-yl 4-methylpent-3-enoate
Electrophorus electricus
pH 8.0, 22°C
0.0391
1,2,2-triethyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0217
1,2-diethyl-2-methyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0038
1-(2-chloro-benzyl)-2,2-diethyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0132
1-(2-chloro-benzyl)-2,2-diisobutyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0132
1-(2-chloro-benzyl)-2,2-dimethyl-2,3-dihydro-1Hquinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0193
1-(2-chloro-benzyl)-2-(4-chloro-phenyl)-2-methyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.013
1-(2-chloro-benzyl)-2-ethyl-2-methyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0229
1-(2-chloro-benzyl)-2-isobutyl-2-methyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0218
1-(2-chloro-benzyl)-2-methyl-2-phenyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.001
1-(2-chloro-benzyl)-2-methyl-2-propyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.05322
1-(2-fluorobenzyl)-N-[6-(1H-indol-1-yl)hexyl]piperidin-4-amine
Electrophorus electricus
pH 8.0, 25°C
0.02168
1-(2-fluorobenzyl)-N-[8-(1H-indol-1-yl)octyl]piperidin-4-amine
Electrophorus electricus
pH 8.0, 25°C
0.04741
1-(3-chlorobenzyl)-N-[6-(1H-indol-1-yl)hexyl]piperidin-4-amine
Electrophorus electricus
pH 8.0, 25°C
0.0261
1-(3-chlorobenzyl)-N-[8-(1H-indol-1-yl)octyl]piperidin-4-amine
Electrophorus electricus
pH 8.0, 25°C
0.0041
1-(4-chloro-benzyl)-2,2-diethyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.6
1-(4-chloro-benzyl)-2,2-diisobutyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0012
1-(4-chloro-benzyl)-2-(4-chloro-phenyl)-2-methyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0073
1-(4-chloro-benzyl)-2-ethyl-2-methyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0092
1-(4-chloro-benzyl)-2-isobutyl-2-methyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0194
1-(4-chloro-benzyl)-2-methyl-2-phenyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0024
1-(4-chloro-benzyl)-2-methyl-2-propyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0024
1--(4-chloro-benzyl)-2,2-dimethyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0018
1-benzyl-2,2-diethyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0008
1-benzyl-2,2-diisobutyl-2,3-dihydro-1Hquinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0064
1-benzyl-2,2-dimethyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0094
1-benzyl-2-(4-chloro-phenyl)-2-methyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0118
1-benzyl-2-ethyl-2-methyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0017
1-benzyl-2-isobutyl-2-methyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0167
1-benzyl-2-methyl-2-phenyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0053
1-benzyl-2-methyl-2-propyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.07011
1-benzyl-N-[5-(2,3-dihydro-1H-indol-1-yl)pentyl]piperidin-4-amine
Electrophorus electricus
pH 8.0, 25°C
0.042
1-benzyl-N-[6-(1H-indol-1-yl)hexyl]piperidin-4-amine
Electrophorus electricus
pH 8.0, 25°C
0.02961
1-benzyl-N-[8-(1H-indol-1-yl)octyl]piperidin-4-amine
Electrophorus electricus
pH 8.0, 25°C
0.0161
1-ethyl-2,2-diisobutyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0338
1-ethyl-2,2-dimethyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0432
1-ethyl-2-isobutyl-2-methyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0186
1-ethyl-2-methyl-2-phenyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.0323
1-ethyl-2-methyl-2-propyl -2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.02308
2-(3-[[1-(2-fluorobenzyl)piperidin-4-yl]amino]propyl)-1H-isoindole-1,3(2H)-dione
Electrophorus electricus
pH 8.0, 25°C
0.06833
2-(3-[[1-(3-chlorobenzyl)piperidin-4-yl]amino]propyl)-1H-isoindole-1,3(2H)-dione
Electrophorus electricus
pH 8.0, 25°C
0.00452
2-(3-[[1-(4-hydroxybenzyl)piperidin-4-yl]amino]propyl)-1H-isoindole-1,3(2H)-dione
Electrophorus electricus
pH 8.0, 25°C
0.0232
2-(4-chloro-phenyl)-1-ethyl-2-methyl-2,3-dihydro-1H-quinazolin-4-one
Electrophorus electricus
pH and temperature not specified in the publication
0.00571
2-(4-hydroxy-3-methoxybenzyl)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide
Electrophorus electricus
pH 8.0, 37°C
0.00368
2-(4-hydroxy-3-methoxybenzyl)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide
Electrophorus electricus
pH 8.0, 37°C
0.00008
2-(4-hydroxy-3-methoxybenzyl)-3-oxo-N-[6-(1,2,3,4-tetrahydroacridin-9-ylamino)hexyl]butanamide
Electrophorus electricus
pH 8.0, 37°C
0.00876
2-(4-hydroxybenzyl)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide
Electrophorus electricus
pH 8.0, 37°C
0.00199
2-(4-hydroxybenzyl)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide
Electrophorus electricus
pH 8.0, 37°C
0.00013
2-(4-hydroxybenzyl)-3-oxo-N-[6-(1,2,3,4-tetrahydroacridin-9-ylamino)hexyl]butanamide
Electrophorus electricus
pH 8.0, 37°C
0.0853
2-(6-[[1-(2-fluorobenzyl)piperidin-4-yl]amino]hexyl)-1H-isoindole-1,3(2H)-dione
Electrophorus electricus
pH 8.0, 25°C
0.05441
2-(6-[[1-(3-chlorobenzyl)piperidin-4-yl]amino]hexyl)-1H-isoindole-1,3(2H)-dione
Electrophorus electricus
pH 8.0, 25°C
0.02977
2-(6-[[1-(4-hydroxybenzyl)piperidin-4-yl]amino]hexyl)-1H-isoindole-1,3(2H)-dione
Electrophorus electricus
pH 8.0, 25°C
0.04339
2-(8-[[1-(2-fluorobenzyl)piperidin-4-yl]amino]octyl)-1H-isoindole-1,3(2H)-dione
Electrophorus electricus
pH 8.0, 25°C
0.02354
2-(8-[[1-(4-hydroxybenzyl)piperidin-4-yl]amino]octyl)-1H-isoindole-1,3(2H)-dione
Electrophorus electricus
pH 8.0, 25°C
43.34
2-(8-[[1-(4-methoxybenzyl)piperidin-4-yl]amino]octyl)-1H-isoindole-1,3(2H)-dione
Electrophorus electricus
pH 8.0, 25°C
0.00811
2-[3-[(1-benzylpiperidin-4-yl)amino]propyl]-1H-isoindole-1,3(2H)-dione
Electrophorus electricus
pH 8.0, 25°C
0.06903
2-[5-[(1-benzylpiperidin-4-yl)amino]pentyl]-1H-isoindole-1,3(2H)-dione
Electrophorus electricus
pH 8.0, 25°C
0.04536
2-[6-[(1-benzylpiperidin-4-yl)amino]hexyl]-1H-isoindole-1,3(2H)-dione
Electrophorus electricus
pH 8.0, 25°C
0.01767
2-[8-[(1-benzylpiperidin-4-yl)amino]octyl]-1H-isoindole-1,3(2H)-dione
Electrophorus electricus
pH 8.0, 25°C
0.00046
3-oxo-N-[(1,2,3,4-tetrahydroacridin-9-ylamino)methyl]butanamide
Electrophorus electricus
pH 8.0, 37°C
0.00024
3-oxo-N-[2-(1,2,3,4-tetrahydroacridin-9-ylamino)ethyl]butanamide
Electrophorus electricus
pH 8.0, 37°C
0.00009
3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide
Electrophorus electricus
pH 8.0, 37°C
0.00057
3-oxo-N-[5-(1,2,3,4-tetrahydroacridin-9-ylamino)pentyl]butanamide
Electrophorus electricus
pH 8.0, 37°C
0.6
(2-methoxy-7-methyl-2-oxido-2,3,4,5-tetrahydro-1,2-oxaphosphepin-6-yl)methanol
Electrophorus electricus
-
pH 7.5, 25°C
0.000023
(3aS,8aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl (2,3-dimethylphenyl)carbamate
Electrophorus electricus
-
-
0.000014
(3aS,8aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl (2,4-dimethylphenyl)carbamate
Electrophorus electricus
-
-
0.000026
(3aS,8aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl (2,5-dimethylphenyl)carbamate
Electrophorus electricus
-
-
0.00001
(3aS,8aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl (2-ethylphenyl)carbamate
Electrophorus electricus
-
-
0.48
(3E)-3-([4-[2-(diethylamino)ethoxy]phenyl]methylidene)-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one
Electrophorus electricus
-
-
2.41
(3E)-3-([4-[3-(diethylamino)propoxy]phenyl]methylidene)-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one
Electrophorus electricus
-
-
0.16
(3E)-3-[(4-[2-[diethenyl(methylidene)-l5-azanyl]ethoxy]phenyl)methylidene]-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one
Electrophorus electricus
-
-
0.72
(3E)-3-[(4-[3-[diethenyl(methylidene)-l5-azanyl]propoxy]phenyl)methylidene]-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one
Electrophorus electricus
-
-
0.003
(3R,5aR)-3-methoxy-1-methyl-4,5,5a,6-tetrahydro-3H,8H-furo[3,4-e][1,2]oxaphosphepin-8-one 3-oxide
Electrophorus electricus
-
pH 7.5, 25°C
0.0003
(3S,5aR)-3-methoxy-1-methyl-4,5,5a,6-tetrahydro-3H,8H-furo[3,4-e][1,2]oxaphosphepin-8-one 3-oxide
Electrophorus electricus
-
pH 7.5, 25°C
0.00023
(4aS,6R,8aS)-3-methoxy-11-[8-[(4aS,6R,8aS)-3-methoxy-6-methyl-5,6,9,10-tetrahydro-4aH-[1]benzofuro[3a,3,2-ef][2]benzazepin-11(12H)-yl]octyl]-5,6,9,10,11,12-hexahydro-4aH-[1]benzofuro[3a,3,2-ef][2]benzazepin-6-ol
Electrophorus electricus
-
-
0.000016
(4aS,6R,8aS)-6-hydroxy-3-methoxy-11-[10-[(4aS,6R,8aS)-3-methoxy-6-methyl-5,6,9,10-tetrahydro-4aH-[1]benzofuro[3a,3,2-ef][2]benzazepin-11(12H)-yl]decyl]-5,6,9,10-tetrahydro-4aH-[1]benzofuro[3a,3,2-ef][2]benzazepin-11-ium
Electrophorus electricus
-
-
0.000022
(4aS,6R,8aS)-6-hydroxy-3-methoxy-11-[8-[(4aS,6R,8aS)-3-methoxy-6-methyl-5,6,9,10-tetrahydro-4aH-[1]benzofuro[3a,3,2-ef][2]benzazepin-11(12H)-yl]octyl]-5,6,9,10-tetrahydro-4aH-[1]benzofuro[3a,3,2-ef][2]benzazepin-11-ium
Electrophorus electricus
-
-
0.0002576
(E)-1-(2,4-dichlorobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
Electrophorus electricus
-
at pH 8.0 and 25°C
0.000017
(E)-1-(2,6-dichlorobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
Electrophorus electricus
-
at pH 8.0 and 25°C
0.00000146
(E)-1-(2-bromobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
Electrophorus electricus
-
at pH 8.0 and 25°C
0.0000041
(E)-1-(2-chloro-6-fluorobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
Electrophorus electricus
-
at pH 8.0 and 25°C
0.00000044
(E)-1-(2-chlorobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
Electrophorus electricus
-
at pH 8.0 and 25°C
0.00000125
(E)-1-(2-fluorobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
Electrophorus electricus
-
at pH 8.0 and 25°C
0.0000153
(E)-1-(2-methylbenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
Electrophorus electricus
-
at pH 8.0 and 25°C
0.000214
(E)-1-(2-nitrobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium bromide
Electrophorus electricus
-
at pH 8.0 and 25°C
0.0000294
(E)-1-(3,4-dichlorobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
Electrophorus electricus
-
at pH 8.0 and 25°C
0.0000103
(E)-1-(3-bromobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
Electrophorus electricus
-
at pH 8.0 and 25°C
0.0000049
(E)-1-(3-chlorobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium bromide
Electrophorus electricus
-
at pH 8.0 and 25°C
0.0000128
(E)-1-(3-fluorobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
Electrophorus electricus
-
at pH 8.0 and 25°C
0.0000066
(E)-1-(3-methoxylbenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
Electrophorus electricus
-
at pH 8.0 and 25°C
0.0000052
(E)-1-(3-methylbenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
Electrophorus electricus
-
at pH 8.0 and 25°C
0.0006534
(E)-1-(4-bromobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
Electrophorus electricus
-
at pH 8.0 and 25°C
0.00059
(E)-1-(4-chlorobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
Electrophorus electricus
-
at pH 8.0 and 25°C
0.0001034
(E)-1-(4-chloromethylbenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
Electrophorus electricus
-
at pH 8.0 and 25°C
0.000677
(E)-1-(4-fluorobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
Electrophorus electricus
-
at pH 8.0 and 25°C
0.000677
(E)-1-(4-methoxybenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
Electrophorus electricus
-
at pH 8.0 and 25°C
0.000744
(E)-1-(4-nitrobenzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium chloride
Electrophorus electricus
-
at pH 8.0 and 25°C
0.0000471
(E)-1-(benzyl)-4-((2-oxoindolin-3-ylidene)methyl)pyridinium bromide
Electrophorus electricus
-
at pH 8.0 and 25°C
0.07
(E)-dimethyl 1-(2-oxodihydrofuran-3(2H)-ylidene)ethyl phosphate
Electrophorus electricus
-
pH 7.5, 25°C
1
(R)-(+)-fenthion sulfoxide
Electrophorus electricus
-
above, pH 7.5, 25°C, recombinant enzyme
1
(rac) fenthion sulfoxide
Electrophorus electricus
-
above, pH 7.5, 25°C, recombinant enzyme
1
(S)-(+)-fenthion sulfoxide
Electrophorus electricus
-
above, pH 7.5, 25°C, recombinant enzyme
1
(Z)-dimethyl 1-(2-oxodihydrofuran-3(2H)-ylidene)ethyl phosphate
Electrophorus electricus
-
above, pH 7.5, 25°C
0.105
1,5,6-trimethyl-9-oxo-7H,9H-pyrano[3,4,5-ij]isoquinolin-1-ium
Electrophorus electricus
-
-
0.01564
2-[4-(1H-benzo[d]imidazol-2-yl)phenoxy]-N,N-diethylethanamine
Electrophorus electricus
-
at pH 8.0 and 20°C
0.01312
2-[4-(1H-benzo[d]imidazol-2-yl)phenoxy]-N,N-dimethylethanamine
Electrophorus electricus
-
at pH 8.0 and 20°C
0.0035
2-[4-(5(6)-chloro-1H-benzo[d]imidazol-2-yl)phenoxy]-N,N-diethylethanamine
Electrophorus electricus
-
at pH 8.0 and 20°C
0.00268
2-[4-(5(6)-chloro-1H-benzo[d]imidazol-2-yl)phenoxy]-N,N-dimethylethanamine
Electrophorus electricus
-
at pH 8.0 and 20°C
0.00108
2-[4-[2-(piperidin-1-yl)ethoxy]phenyl]-1H-benzo[d]-imidazole
Electrophorus electricus
-
at pH 8.0 and 20°C
0.00305
2-[4-[2-(pyrrolidin-1-yl)ethoxy]phenyl]-1H-benzo[d]-imidazole
Electrophorus electricus
-
at pH 8.0 and 20°C
1.62
3-(4-propoxybenzyl)-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one
Electrophorus electricus
-
-
0.75
3-(4-[2-[diethenyl(methylidene)-l5-azanyl]ethoxy]benzyl)-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one
Electrophorus electricus
-
-
5.58
3-(4-[3-[diethenyl(methylidene)-l5-azanyl]propoxy]benzyl)-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one
Electrophorus electricus
-
-
8.95
3-[4-[3-(diethylamino)propoxy]benzyl]-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one
Electrophorus electricus
-
-
0.01459
4-(5-chloro-1H-benzimidazol-2-yl)phenol
Electrophorus electricus
-
at pH 8.0 and 20°C
0.01593
4-(5-methyl-1H-benzimidazol-2-yl)phenol
Electrophorus electricus
-
at pH 8.0 and 20°C
0.00000289
4-ethenyl-5-methyl-5,6-dihydro[1,3]dioxolo[4,5-j]phenanthridine
Electrophorus electricus
-
-
0.01879
4-[2-[4-(1H-benzo[d]imidazol-2-yl)phenoxy]ethyl]morpholine
Electrophorus electricus
-
at pH 8.0 and 20°C
0.01105
4-[2-[4-(5(6)-chloro-1H-benzo[d]imidazol-2-yl)phenoxy]ethyl]morpholine
Electrophorus electricus
-
at pH 8.0 and 20°C
0.1
4-[2-[4-(5(6)-methyl-1H-benzo[d]imidazol-2-yl)phenoxy]ethyl]morpholine
Electrophorus electricus
-
IC50 above 0.1 mM, at pH 8.0 and 20°C
0.00061
5(6)-chloro-2-[4-[2-(piperidin-1-yl)ethoxy]phenyl]-1H-benzo[d]imidazole
Electrophorus electricus
-
at pH 8.0 and 20°C
0.00324
5(6)-chloro-2-[4-[2-(pyrrolidin-1-yl)ethoxy]phenyl]-1H-benzo[d]imidazole
Electrophorus electricus
-
at pH 8.0 and 20°C
0.00084
5(6)-methyl-2-[4-[2-(piperidin-1-yl)ethoxy]phenyl]-1H-benzo[d]imidazole
Electrophorus electricus
-
at pH 8.0 and 20°C
0.00134
5(6)-methyl-2-[4-[2-(pyrrolidin-1-yl)ethoxy]phenyl]-1H-benzo[d]imidazole
Electrophorus electricus
-
at pH 8.0 and 20°C
0.00123
9-O-[2-(9H-carbazole-4-yloxy)ethyl] berberine bromide
Electrophorus electricus
-
pH 8.0, 37°C
0.000375
9-O-[2-(benzotriazole-1-yloxy)ethyl] berberine bromide
Electrophorus electricus
-
pH 8.0, 37°C
0.000224
9-O-[2-(phenylol-1-yloxy)ethyl] berberine bromide
Electrophorus electricus
-
pH 8.0, 37°C
0.000052
9-O-[2-(phenylol-1-yloxy)hexyl] berberine bromide
Electrophorus electricus
-
pH 8.0, 37°C
0.00112
9-O-[3-(9H-carbazole-4-yloxy)propyl] berberine bromide
Electrophorus electricus
-
pH 8.0, 37°C
0.000359
9-O-[3-(benzotriazole-1-yloxy)propyl] berberine bromide
Electrophorus electricus
-
pH 8.0, 37°C
0.000123
9-O-[3-(phenylol-1-yloxy)propyl] berberine bromide
Electrophorus electricus
-
pH 8.0, 37°C
0.000856
9-O-[4-(9H-carbazole-4-yloxy)butyl] berberine bromide
Electrophorus electricus
-
pH 8.0, 37°C
0.000224
9-O-[4-(benzotriazole-1-yloxy)butyl] berberine bromide
Electrophorus electricus
-
pH 8.0, 37°C
0.000097
9-O-[4-(phenylol-1-yloxy)butyl] berberine bromide
Electrophorus electricus
-
pH 8.0, 37°C
0.00168
9-O-[5-(9H-carbazole-4-yloxy)butyl] berberine bromide
Electrophorus electricus
-
pH 8.0, 37°C
0.00028
9-O-[5-(benzotriazole-1-yloxy)pentyl] berberine bromide
Electrophorus electricus
-
pH 8.0, 37°C
0.000398
9-O-[5-(phenylol-1-yloxy)pentyl] berberine bromide
Electrophorus electricus
-
pH 8.0, 37°C
0.0021
9-O-[6-(9H-carbazole-4-yloxy)butyl] berberine bromide
Electrophorus electricus
-
pH 8.0, 37°C
0.000515
9-O-[6-(benzotriazole-1-yloxy)hexyl] berberine bromide
Electrophorus electricus
-
pH 8.0, 37°C
0.028
conarrhimin
Electrophorus electricus
-
in 0.1 M sodium phosphate buffer, pH 8.0, at 37°C
0.004
conessimin
Electrophorus electricus
-
in 0.1 M sodium phosphate buffer, pH 8.0, at 37°C
0.0016
hookerianamide-F
Electrophorus electricus
-
in 0.1 M sodium phosphate buffer, pH 8.0, at 37°C
0.3
isoconessimine
Electrophorus electricus
-
IC50 above 0.3 mM, in 0.1 M sodium phosphate buffer, pH 8.0, at 37°C
0.006
methyl (2R,5R)-5-[(benzyloxy)methyl]-2-methoxy-7-methyl-2,3,4,5-tetrahydro-1,2-oxaphosphepine-6-carboxylate 2-oxide
Electrophorus electricus
-
pH 7.5, 25°C
0.035
methyl (2S,5R)-5-[(benzyloxy)methyl]-2-methoxy-7-methyl-2,3,4,5-tetrahydro-1,2-oxaphosphepine-6-carboxylate 2-oxide
Electrophorus electricus
-
pH 7.5, 25°C
0.005
methyl 1-methoxy-5-methyl-1,2,3,6-tetrahydrophosphinine-4-carboxylate 1-oxide
Electrophorus electricus
-
pH 7.5, 25°C
0.007
methyl 2-methoxy-7-methyl-2,3,4,5-tetrahydro-1,2-oxaphosphepine-6-carboxylate 2-oxide
Electrophorus electricus
-
pH 7.5, 25°C
0.00234
N,N-diethyl-2-[4-(5(6)-methyl-1H-benzo[d]imidazol-2-yl)phenoxy]ethanamine
Electrophorus electricus
-
at pH 8.0 and 20°C
0.00506
N,N-dimethyl-2-[4-(5(6)-methyl-1H-benzo[d]imidazol-2-yl)phenoxy]ethanamine
Electrophorus electricus
-
at pH 8.0 and 20°C
0.00119
N-[2-[4-(1H-benzo[d]imidazol-2-yl)phenoxy]ethyl]-N-isopropylpropan-2-amine
Electrophorus electricus
-
at pH 8.0 and 20°C
0.00058
N-[2-[4-(5(6)-chloro-1H-benzo[d]imidazol-2-yl)phenoxy]ethyl]-N-isopropylpropan-2-amine
Electrophorus electricus
-
at pH 8.0 and 20°C
0.0015
sarcovagenine-C
Electrophorus electricus
-
in 0.1 M sodium phosphate buffer, pH 8.0, at 37°C
0.0022
sarcovagine-D
Electrophorus electricus
-
in 0.1 M sodium phosphate buffer, pH 8.0, at 37°C
0.00006
huperzine A
Electrophorus electricus
-
in 0.1 M sodium phosphate buffer, pH 8.0, at 37°C
additional information
additional information
Electrophorus electricus
-
IC50s: for 1,8-cineole 0.015 mg/ml, for alpha-pinene 0.022 mg/ml, for eugenol 0.48 mg/ml, for alpha-terpineol 1.3 mg/ml, for terpinen-4-ol 3.2 mg/ml, at 37°C, pH not specified in the publication
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
additional information
-
AChE activity of the soluble enzyme form and in the insoluble enzyme form with all the three types of modified poly-acrylonitrile membranes, overview
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
7.5
8
-
assay at
pH RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
4.8 - 9.8
at this pH range, the enzyme activity forms a sigmoid increasing curve with maximum catalytic activity at pH 8.0-9.5
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
22
25
37
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
physiological function
the enzyme acetylcholinesterase (AChE) exists mainly in the synaptic clefts (between nerves and skeletal muscle) and the central nervous system (CNS) of living organisms, and is mostly responsible for proper muscle functioning as well as signal transmissions. AChE hydrolyzes ACh into choline and acetate ion at synapses with a very fast functioning rate, resulting in the loss of stimulatory activity
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable).
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable). ACES_ELEEL
633
1
71815
Swiss-Prot
Secretory Pathway (Reliability: 1)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
?
-
enzyme exists as a mixture of 88 kDa dimers consisting of disulfide-linked 42- to 44-kDa polypeptides and a 42- to 44-kDa monomer, SDS-PAGE
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
additional information
-
AChE immobilization on two different composite membranes constituted by a chemically modified poly-acrylonitrile membrane plus a layer of tethered chitosan of different molecular weight, 10 kDa or 400 kDa, or directly on a chemically modified poly-acrylonitrile membrane with NaOH and ethylenediamine without chitosan, method development and enzyme activities, the best performance is obtained by the modified poly-acrylonitrile membrane having the chitosan with the lower molecular weight, overview
additional information
-
AChE is covalently linked to one side of Au-TiO2-modified Ti foil using glutaraldehyde as a bridging reagent for measurement of enzyme inhibition using this an enzyme-semiconductor photoelectrochemical system, overview. Determination of morphologies of the TiO2 nanotubes and modified nanotubes using a field-emission scanning electron microscope, overview. Method development and evaluation, overview
additional information
-
covalent AChE immobilization on chromatographic resin aminopropyl silica using glutaraldehyde, evaluation of enzyme inhibition in presence and absence of Mg2+, overview. Method evaluation, overview
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
drug development
acetylcholinesterase, butyrylcholinesterase and beta-amyloid are the predominant biological targets in the search for anti-Alzheimer's agents
medicine
acetylcholinesterase (AChE) inhibition is the standard therapy for Alzheimer's disease (AD), a late-onset neurodegenerative pathology that impacts an individual's memory, motor coordination, and cognition in a progressive and eventually lethal manner. Alzheimer's disease has huge socioeconomic impact, and healthcare research in the twenty-first century has prioritized the development of therapeutic alternatives to treat this condition
analysis
diagnostics
-
AChE activity can be used as a biomarker of neurotoxic metal elements, such as lead, cadmium and copper
drug development
-
AChE is an important drug target and its inhibitors prove useful in the symptomatic treatment of Alzheimer's disease
analysis
-
development of sensors for direct detection of organophosphates
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Webb, G.
Acetylcholinesterase: characterization of native and proteolytically derived forms and identification of structural protein components
Can. J. Biochem.
56
1124-1132
1978
Electrophorus electricus
Stojan, J.; Zorko, M.
Kinetic characterization of all steps of the interaction between acetylcholinesterase and eserine
Biochim. Biophys. Acta
1337
75-84
1997
Electrophorus electricus
Singh, A.K.; Flounders, A.W.; Volponi, J.V.; Ashley, C.S.; Wally, K.; Schoeniger, J.S.
Development of sensors for direct detection of organophosphates. Part I: Immobilization, characterization and stabilization of acetylcholinesterases and organophosphate hydrolase on silica supports
Biosens. Bioelectron.
14
703-713
1999
Electrophorus electricus
Villatte, F.; Marcel, V.; Estrada-Mondaca, S.; Fournier, D.
Engineering sensitive acetylcholinesterase for detection of organophosphate and carbamate insecticides
Biosens. Bioelectron.
13
157-164
1998
Caenorhabditis elegans, Drosophila melanogaster, Electrophorus electricus, Torpedo sp.
Golicnik, M.; Stojan, J.
Multi-step analysis as a tool for kinetic parameter estimation and mechanism discrimination in the reaction between tight-binding fasciculin 2 and electric eel acetylcholinesterase
Biochim. Biophys. Acta
1597
164-172
2002
Electrophorus electricus
Shcharbin, D.; Jokiel, M.; Klajnert, B.; Bryszewska, M.
Effect of dendrimers on pure acetylcholinesterase activity and structure
Bioelectrochemistry
68
56-59
2006
Electrophorus electricus
Barteri, M.; Pala, A.; Rotella, S.
Structural and kinetic effects of mobile phone microwaves on acetylcholinesterase activity
Biophys. Chem.
113
245-253
2005
Electrophorus electricus
Zhan, C.G.; Gao, D.
Catalytic mechanism and energy barriers for butyrylcholinesterase-catalyzed hydrolysis of cocaine
Biophys. J.
89
3863-3872
2005
Electrophorus electricus
Lin, G.; Liao, W.C.; Chan, C.H.; Wu, Y.H.; Tsai, H.J.; Hsieh, C.W.
Quantitative structure-activity relationships for the pre-steady state acetylcholinesterase inhibition by carbamates
J. Biochem. Mol. Toxicol.
18
353-360
2004
Electrophorus electricus
Chiou, S.Y.; Lai, G.W.; Tsai, Y.H.; Lee, Y.R.; Lin, L.Y.; Lin, G.L.
Kinetics and mechanisms of acetylcholinesterase and butyrylcholinesterase inhibition by cardiovascular drugs and benzodiazepines
J. Chin. Chem. Soc.
52
843-848
2005
Electrophorus electricus
-
Lin, G.; Liu, Y.C.; Lin, Y.F.; Wu, Y.G.
Ortho effects in quantitative structure-activity relationships for acetylcholinesterase inhibition by aryl carbamates
J. Enzyme Inhib. Med. Chem.
19
395-401
2004
Electrophorus electricus
Pietsch, M.; Gutschow, M.
Synthesis of tricyclic 1,3-oxazin-4-ones and kinetic analysis of cholesterol esterase and acetylcholinesterase inhibition
J. Med. Chem.
48
8270-8288
2005
Electrophorus electricus
Gadepalli, R.S.; Rimoldi, J.M.; Fronczek, F.R.; Nillos, M.; Gan, J.; Deng, X.; Rodriguez-Fuentes, G.; Schlenk, D.
Synthesis of fenthion sulfoxide and fenoxon sulfoxide enantiomers: effect of sulfur chirality on acetylcholinesterase activity
Chem. Res. Toxicol.
20
257-262
2007
Electrophorus electricus, Homo sapiens
Pastorin, G.; Marchesan, S.; Hoebeke, J.; Da Ros, T.; Ehret-Sabatier, L.; Briand, J.P.; Prato, M.; Bianco, A.
Design and activity of cationic fullerene derivatives as inhibitors of acetylcholinesterase
Org. Biomol. Chem.
4
2556-2562
2006
Electrophorus electricus
Jukic, M.; Politeo, O.; Maksimovic, M.; Milos, M.; Milos, M.
In vitro acetylcholinesterase inhibitory properties of thymol, carvacrol and their derivatives thymoquinone and thymohydroquinone
Phytother. Res.
21
259-261
2007
Electrophorus electricus
Zdrazilova, P.; Stepankova, S.; Komersova, A.; Vranova, M.; Komers, K.; Cegan, A.
Kinetics of 13 new cholinesterase inhibitors
Z. Naturforsch. C
61
611-617
2006
Bos taurus, Electrophorus electricus
Zimmermann, M.; Westwell, M.S.; Greenfield, S.A.
Impact of detergents on the activity of acetylcholinesterase and on the effectiveness of its inhibitors
Biol. Chem.
390
19-26
2009
Electrophorus electricus
Pan, L.; Tan, J.H.; Hou, J.Q.; Huang, S.L.; Gu, L.Q.; Huang, Z.S.
Design, synthesis and evaluation of isaindigotone derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors
Bioorg. Med. Chem. Lett.
18
3790-3793
2008
Electrophorus electricus
Carolan, C.G.; Gaynor, J.M.; Dillon, G.P.; Khan, D.; Ryder, S.A.; Reidy, S.; Gilmer, J.F.
Novel isosorbide di-ester compounds as inhibitors of acetylcholinesterase
Chem. Biol. Interact.
175
293-297
2008
Electrophorus electricus
Loizzo, M.R.; Tundis, R.; Menichini, F.; Menichini, F.
Natural products and their derivatives as cholinesterase inhibitors in the treatment of neurodegenerative disorders: an update
Curr. Med. Chem.
15
1209-1228
2008
Electrophorus electricus, Homo sapiens
Acharya, J.; Gupta, A.K.; Dubey, D.K.; Raza, S.K.
Synthesis and evaluation of novel bis-pyridinium oximes as reactivators of DFP-inhibited acetylcholinesterase
Eur. J. Med. Chem.
44
1335-1340
2008
Electrophorus electricus
Gabrovska, K.; Marinov, I.; Godjevargova, T.; Portaccio, M.; Lepore, M.; Grano, V.; Diano, N.; Mita, D.G.
The influence of the support nature on the kinetics parameters, inhibition constants and reactivation of immobilized acetylcholinesterase
Int. J. Biol. Macromol.
43
339-345
2008
Electrophorus electricus
Xu, Z.; Yao, S.; Wei, Y.; Zhou, J.; Zhang, L.; Wang, C.; Guo, Y.
Monitoring enzyme reaction and screening of inhibitors of acetylcholinesterase by quantitative matrix-assisted laser desorption/ionization fourier transform mass spectrometry
J. Am. Soc. Mass Spectrom.
19
1849-1855
2008
Electrophorus electricus
Mroczek, T.
Highly efficient, selective and sensitive molecular screening of acetylcholinesterase inhibitors of natural origin by solid-phase extraction-liquid chromatography/electrospray ionisation-octopole-orthogonal acceleration time-of-flight-mass spectrometry an
J. Chromatogr. A
1216
2519-2528
2009
Electrophorus electricus
Fallarero, A.; Oinonen, P.; Gupta, S.; Blom, P.; Galkin, A.; Mohan, C.G.; Vuorela, P.M.
Inhibition of acetylcholinesterase by coumarins: the case of coumarin 106
Pharmacol. Res.
58
215-221
2008
Electrophorus electricus
Maia, A.; Schmitz-Afonso, I.; Martin, M.T.; Awang, K.; Laprevote, O.; Gueritte, F.; Litaudon, M.
Acylphenols from Myristica crassa as new acetylcholinesterase inhibitors
Planta Med.
74
1457-1462
2008
Electrophorus electricus
Menichini, F.; Tundis, R.; Loizzo, M.; Bonesi, M.; Marrelli, M.; Statti, G.; Menichini, F.; Conforti, F.
Acetylcholinesterase and butyrylcholinesterase inhibition of ethanolic extract and monoterpenes from Pimpinella anisoides V Brig. (Apiaceae)
Fitoterapia
80
297-300
2009
Electrophorus electricus
Guo, L.; Suarez, A.I.; Braden, M.R.; Gerdes, J.M.; Thompson, C.M.
Inhibition of acetylcholinesterase by chromophore-linked fluorophosphonates
Bioorg. Med. Chem. Lett.
20
1194-1197
2010
Electrophorus electricus, Mus musculus
Huang, L.; Shi, A.; He, F.; Li, X.
Synthesis, biological evaluation, and molecular modeling of berberine derivatives as potent acetylcholinesterase inhibitors
Bioorg. Med. Chem.
18
1244-1251
2010
Electrophorus electricus
Dutta, S.; Malla, R.K.; Bandyopadhyay, S.; Spilling, C.D.; Dupureur, C.M.
Synthesis and kinetic analysis of some phosphonate analogs of cyclophostin as inhibitors of human acetylcholinesterase
Bioorg. Med. Chem.
18
2265-2274
2010
Electrophorus electricus
Bharate, S.B.; Guo, L.; Reeves, T.E.; Cerasoli, D.M.; Thompson, C.M.
Bisquaternary pyridinium oximes: Comparison of in vitro reactivation potency of compounds bearing aliphatic linkers and heteroaromatic linkers for paraoxon-inhibited electric eel and recombinant human acetylcholinesterase
Bioorg. Med. Chem.
18
787-794
2010
Electrophorus electricus, Homo sapiens
Kovarova, M.; Komers, K.; Stepankova, S.; Cegan, A.
Inhibition of acetylcholinesterase by 14 achiral and five chiral imidazole derivates
Biores. Technol.
101
6281-6283
2010
Electrophorus electricus
Zhu, W.; An, Y.R.; Luo, X.M.; Wang, F.; Zheng, J.H.; Tang, L.L.; Wang, Q.J.; Zhang, Z.H.; Zhang, W.; Jin, L.T.
Study on acetylcholinesterase inhibition induced by endogenous neurotoxin with an enzyme-semiconductor photoelectrochemical system
Chem. Commun. (Camb. )
2009
2682-2684
2009
Electrophorus electricus
Wang, Z.; Zhao, J.; Li, F.; Gao, D.; Xing, B.
Adsorption and inhibition of acetylcholinesterase by different nanoparticles
Chemosphere
77
67-73
2009
Electrophorus electricus
Chiou, S.Y.; Huang, C.F.; Yeh, S.J.; Chen, I.R.; Lin, G.
Synthesis of enantiomers of exo-2-norbornyl-N-n-butylcarbamate and endo-2-norbornyl-N-n-butylcarbamate for stereoselective inhibition of acetylcholinesterase
Chirality
22
267-274
2010
Electrophorus electricus
Schuchert-Shi, A.; Hauser, P.C.
Study of acetylcholinesterase inhibitors using CE with contactless conductivity detection
Electrophoresis
30
3442-3448
2009
Electrophorus electricus
Lv, W.; Xue, Y.
Prediction of acetylcholinesterase inhibitors and characterization of correlative molecular descriptors by machine learning methods
Eur. J. Med. Chem.
45
1167-1172
2010
Electrophorus electricus
Pietsch, M.; Christian, L.; Inhester, T.; Petzold, S.; Guetschow, M.
Kinetics of inhibition of acetylcholinesterase in the presence of acetonitrile
FEBS J.
276
2292-2307
2009
Electrophorus electricus
Dohi, S.; Terasaki, M.; Makino, M.
Acetylcholinesterase inhibitory activity and chemical composition of commercial essential oils
J. Agric. Food Chem.
57
4313-4318
2009
Electrophorus electricus
Serrano, M.A.; Pivatto, M.; Francisco, W.; Danuello, A.; Regasini, L.O.; Lopes, E.M.; Lopes, M.N.; Young, M.C.; Bolzani, V.S.
Acetylcholinesterase inhibitory pyridine alkaloids of the leaves of Senna multijuga
J. Nat. Prod.
73
482-484
2010
Electrophorus electricus
Halldorsdottir, E.S.; Jaroszewski, J.W.; Olafsdottir, E.S.
Acetylcholinesterase inhibitory activity of lycopodane-type alkaloids from the Icelandic Lycopodium annotinum ssp. alpestre
Phytochemistry
71
149-157
2010
Electrophorus electricus
Pereira, D.M.; Ferreres, F.; Oliveira, J.M.; Gaspar, L.; Faria, J.; Valentao, P.; Sottomayor, M.; Andrade, P.B.
Pharmacological effects of Catharanthus roseus root alkaloids in acetylcholinesterase inhibition and cholinergic neurotransmission
Phytomedicine
17
646-652
2009
Electrophorus electricus, Rattus norvegicus
Carpinella, M.C.; Andrione, D.G.; Ruiz, G.; Palacios, S.M.
Screening for acetylcholinesterase inhibitory activity in plant extracts from Argentina
Phytother. Res.
24
259-263
2010
Electrophorus electricus
Ibrahim, F.; Guillaume, Y.C.; Thomassin, M.; Andre, C.
Magnesium effect on the acetylcholinesterase inhibition mechanism: a molecular chromatographic approach
Talanta
79
804-809
2009
Electrophorus electricus
Lorenzetto, P.; Wächter, M.; Ruedi, P.
Synthesis and characterization of enantiomerically pure cis- and trans-3-fluoro-2,4-dioxa-9-aza-3-phosphadecalin 3-oxides as acetylcholine mimetics and inhibitors of acetylcholinesterase
Helv. Chim. Acta
94
746-767
2011
Electrophorus electricus
-
Alpan, A.S.; Parlar, S.; Carlino, L.; Tarikogullari, A.H.; Alptuezuen, V.; Guenes, H.S.
Synthesis, biological activity and molecular modeling studies on 1H-benzimidazole derivatives as acetylcholinesterase inhibitors
Bioorg. Med. Chem.
21
4928-4937
2013
Electrophorus electricus, Homo sapiens
Akrami, H.; Mirjalili, B.F.; Khoobi, M.; Nadri, H.; Moradi, A.; Sakhteman, A.; Emami, S.; Foroumadi, A.; Shafiee, A.
Indolinone-based acetylcholinesterase inhibitors: Synthesis, biological activity and molecular modeling
Eur. J. Med. Chem.
84
375-381
2014
Electrophorus electricus
Yang, Z.D.; Duan, D.Z.; Xue, W.W.; Yao, X.J.; Li, S.
Steroidal alkaloids from Holarrhena antidysenterica as acetylcholinesterase inhibitors and the investigation for structure-activity relationships
Life Sci.
90
929-933
2012
Electrophorus electricus
Saa, L.; Grinyte, R.; Sanchez-Iglesias, A.; Liz-Marzan, L.M.; Pavlov, V.
Blocked enzymatic etching of gold nanorods application to colorimetric detection of acetylcholinesterase activity and its inhibitors
ACS Appl. Mater. Interfaces
8
11139-11146
2016
Electrophorus electricus (O42275)
Ali, M.Y.; Seong, S.H.; Jung, H.A.; Jannat, S.; Choi, J.S.
Kinetics and molecular docking of dihydroxanthyletin-type coumarins from Angelica decursiva that inhibit cholinesterase and BACE1
Arch. Pharm. Res.
41
753-764
2018
Electrophorus electricus (O42275)
Sultana, N.; Sarfraz, M.; Tanoli, S.T.; Akram, M.S.; Sadiq, A.; Rashid, U.; Tariq, M.I.
Synthesis, crystal structure determination, biological screening and docking studies of N1-substituted derivatives of 2,3-dihydroquinazolin-4(1H)-one as inhibitors of cholinesterases
Bioorg. Chem.
72
256-267
2017
Electrophorus electricus (O42275)
Wieckowska, A.; Wieckowski, K.; Bajda, M.; Brus, B.; Salat, K.; Czerwinska, P.; Gobec, S.; Filipek, B.; Malawska, B.
Synthesis of new N-benzylpiperidine derivatives as cholinesterase inhibitors with beta-amyloid anti-aggregation properties and beneficial effects on memory in vivo
Bioorg. Med. Chem.
23
2445-2457
2015
Electrophorus electricus (O42275)
Liu, Z.; Fang, L.; Zhang, H.; Gou, S.; Chen, L.
Design, synthesis and biological evaluation of multifunctional tacrine-curcumin hybrids as new cholinesterase inhibitors with metal ions-chelating and neuroprotective property
Bioorg. Med. Chem.
25
2387-2398
2017
Electrophorus electricus (O42275)
Mohammed, A.; Sneathen, J.; Frojen, S.G.; Kuo, L.; Dupureur, C.M.
Stereospecific cholinesterase inhibition by O,S-diethylphenylphosphonothioate
Bioorg. Med. Chem.
25
3053-3058
2017
Electrophorus electricus (O42275), Homo sapiens (P22303), Homo sapiens
Tanoli, N.U.; Tanoli, S.A.K.; Ferreira, A.G.; Mehmood, M.; Gul, S.; Monteiro, J.L.; Vieira, L.C.C.; Venancio, T.; Correa, A.G.; Ul-Haq, Z.
Characterization of the interactions between coumarin-derivatives and acetylcholinesterase examination by NMR and docking simulations
J. Mol. Model.
24
207
2018
Electrophorus electricus (O42275)
Ali, M.Y.; Seong, S.H.; Reddy, M.R.; Seo, S.Y.; Choi, J.S.; Jung, H.A.
Kinetics and molecular docking studies of 6-formyl umbelliferone isolated from Angelica decursiva as an inhibitor of cholinesterase and BACE1
Molecules
22
1604-1616
2017
Electrophorus electricus (O42275)
Freitas, T.R.; Danuello, A.; Viegas Junior, C.; Bolzani, V.S.; Pivatto, M.
Mass spectrometry for characterization of homologous piperidine alkaloids and their activity as acetylcholinesterase inhibitors
Rapid Commun. Mass Spectrom.
32
1303-1310
2018
Electrophorus electricus (O42275)
Komersova, A.; Kovarova, M.; Komers, K.; Lochar, V.; Cegan, A.
Why is the hydrolytic activity of acetylcholinesterase pH dependent? Kinetic study of acetylcholine and acetylthiocholine hydrolysis catalyzed by acetylcholinesterase from electric eel
Z. Naturforsch. C
73
345-351
2018
Electrophorus electricus (O42275)
-
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