DGIdb - ACHE Gene Record

ACHE 43 Druggable Genome

Alternate Names:

43
ACETYLCHOLINESTERASE (CARTWRIGHT BLOOD GROUP)
ACHE
ACEE
ARACHE
N-ACHE
YT
100740
108
ENSG00000087085
OTTHUMG00000157033
P22303
ACES_HUMAN
acetylcholinesterase
BE0000426
TTDS00140
ACETYLCHOLINESTERASE PRECURSOR (EC 3.1.1.7) (ACHE). [SOURCE:UNIPROT/SWISSPROT;ACC:P22303]
2465
PA20
T30082

Gene Info:

Interpro Acc	IPR002018
Interpro Name	Carboxylesterase, type B
Uniprot Status	Swiss-Prot
Human Readable Name	DRUGGABLE GENOME
Interpro Type	Domain
Uniprot Evidence	1: Evidence at protein level
Interpro Short Name	CarbesteraseB
Target Main Class	Enzymes
Target Subclass	3.1.1.7
Target Class	Enzymes
Target Subclass	EC:3.1.1.7
Gene Biotype	PROTEIN_CODING

(10 More Sources)

Gene Categories: Category Details

CELL SURFACE
DRUGGABLE GENOME

Publications:

Zhang et al., 2009, Neuromuscular blockade, reversal agent use, and operating room time: retrospective analysis of US inpatient surgeries., Curr Med Res Opin
Naves et al., 2001, Repetitive nerve stimulation decreases the acetylcholine content of quanta at the frog neuromuscular junction., J. Physiol. (Lond.)
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Minic et al., 2003, Butyrylcholinesterase and acetylcholinesterase activity and quantal transmitter release at normal and acetylcholinesterase knockout mouse neuromuscular junctions., Br. J. Pharmacol.
Takeuchi et al., 2000, Stimulation by nizatidine, a histamine H(2)-receptor antagonist, of duodenal HCO(3)(-)secretion in rats:relation to anti-cholinesterase activity., World J. Gastroenterol.
Beck et al., 2003, Stress interacts with peripheral cholinesterase inhibitors to cause central nervous system effects., Life Sci.
Trevisani et al., 2000, Neostigmine: safe and effective treatment for acute colonic pseudo-obstruction., Dis. Colon Rectum
Greig et al., 2002, Butyrylcholinesterase: an important new target in Alzheimer's disease therapy., Int Psychogeriatr
Farlow, 2003, Update on rivastigmine., Neurologist
Stahl, 2000, The new cholinesterase inhibitors for Alzheimer's disease, Part 1: their similarities are different., J Clin Psychiatry
Grossberg et al., 2000, Lack of adverse pharmacodynamic drug interactions with rivastigmine and twenty-two classes of medications., Int J Geriatr Psychiatry
Gottwald et al., 1999, Rivastigmine, a brain-region selective acetylcholinesterase inhibitor for treating Alzheimer's disease: review and current status., Expert Opin Investig Drugs
Kennedy et al., 1999, Preferential cerebrospinal fluid acetylcholinesterase inhibition by rivastigmine in humans., J Clin Psychopharmacol
Goldblum et al., 2000, Topical rivastigmine, a selective acetylcholinesterase inhibitor, lowers intraocular pressure in rabbits., J Ocul Pharmacol Ther
Lalli et al., 2008, Rivastigmine in Parkinson's disease dementia., Expert Rev Neurother
Naik et al., 2009, Effects of rivastigmine and donepezil on brain acetylcholine levels in acetylcholinesterase-deficient mice., J Pharm Pharm Sci
Birks et al., 2009, Rivastigmine for Alzheimer's disease., Cochrane Database Syst Rev
Onor et al., 2007, Rivastigmine in the treatment of Alzheimer's disease: an update., Clin Interv Aging
Scacchi R et al., 2009, Variability of AChE, BChE, and ChAT genes in the late-onset form of Alzheimer's disease and relationships with response to treatment with Donepezil and Rivastigmine., Am J Med Genet B Neuropsychiatr Genet
Ashani et al., 1990, Differences in conformational stability between native and phosphorylated acetylcholinesterase as evidenced by a monoclonal antibody., Biochemistry
da Costa et al., 2001, Short- and long-term influences of calcitonin gene-related peptide on the synthesis of acetylcholinesterase in mammalian myotubes., Br. J. Pharmacol.
Malatová et al., 1999, Depression of acetylcholinesterase synthesis following transient cerebral ischemia in rat: pharmacohistochemical and biochemical investigation., Gen. Physiol. Biophys.
Quistad et al., 2000, Phosphoacetylcholinesterase: toxicity of phosphorus oxychloride to mammals and insects that can be attributed to selective phosphorylation of acetylcholinesterase by phosphorodichloridic acid., Chem. Res. Toxicol.
Pang et al., 2003, Rational design of alkylene-linked bis-pyridiniumaldoximes as improved acetylcholinesterase reactivators., Chem. Biol.
Cardoso CL et al., 2004, Indole glucoalkaloids from Chimarrhis turbinata and their evaluation as antioxidant agents and acetylcholinesterase inhibitors., J Nat Prod
Kryger et al., 1999, Structure of acetylcholinesterase complexed with E2020 (Aricept): implications for the design of new anti-Alzheimer drugs., Structure
Davis, 1999, Alzheimer's disease: seeking new ways to preserve brain function. Interview by Alice V. Luddington., Geriatrics
Shepherd et al., Donepezil overdose: a tenfold dosing error., Ann Pharmacother
Repantis et al., 2010, Acetylcholinesterase inhibitors and memantine for neuroenhancement in healthy individuals: a systematic review., Pharmacol. Res.
Kosasa et al., 1999, Effect of donepezil hydrochloride (E2020) on basal concentration of extracellular acetylcholine in the hippocampus of rats., Eur. J. Pharmacol.
Jann, 2000, Rivastigmine, a new-generation cholinesterase inhibitor for the treatment of Alzheimer's disease., Pharmacotherapy
Ki et al., 2010, Donepezil, a potent acetylcholinesterase inhibitor, induces caspase-dependent apoptosis in human promyelocytic leukemia HL-60 cells., Biol. Pharm. Bull.
Sugimoto, 2001, Donepezil hydrochloride: a treatment drug for Alzheimer's disease., Chem Rec
Huang L et al., 2014, Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease., Eur J Med Chem
Monnet-Tschudi et al., 2000, Maturation-dependent effects of chlorpyrifos and parathion and their oxygen analogs on acetylcholinesterase and neuronal and glial markers in aggregating brain cell cultures., Toxicol. Appl. Pharmacol.
Nguyen et al., 1999, Maturation of neuromuscular transmission during early development in zebrafish., J. Neurophysiol.
Tuovinen et al., 1999, Success of pyridostigmine, physostigmine, eptastigmine and phosphotriesterase treatments in acute sarin intoxication., Toxicology
Blasina et al., 2000, Evidence for a noncholinergic function of acetylcholinesterase during development of chicken retina as shown by fasciculin., Cell Tissue Res.
Bolognesi et al., 2001, Hexahydrochromeno[4,3-b]pyrrole derivatives as acetylcholinesterase inhibitors., J. Med. Chem.
Hodge et al., 1992, Ambenonium is a rapidly reversible noncovalent inhibitor of acetylcholinesterase, with one of the highest known affinities., Mol. Pharmacol.
Webb, 1965, Affinity of benzoquinonium and ambenonium derivatives for the acetylcholine receptor, tested on the electroplax, and for acetylcholinesterase in solution., Biochim. Biophys. Acta
Bolognesi et al., 2003, Design, synthesis and biological evaluation of ambenonium derivatives as AChE inhibitors., Farmaco
Kenakin et al., 1985, Self-cancellation of drug properties as a mode of organ selectivity: the antimuscarinic effects of ambenonium., J. Pharmacol. Exp. Ther.
Lockhart et al., 2001, Differential inhibition of [3H]-oxotremorine-M and [3H]-quinuclinidyl benzilate binding to muscarinic receptors in rat brain membranes with acetylcholinesterase inhibitors., Naunyn Schmiedebergs Arch. Pharmacol.
Papp et al., 2006, Similarities between CSF-brain extracellular transfer and neurofibrillary tangle invasion in Alzheimer's disease., Neurobiol. Aging
Wang et al., 1999, Effects of bis(7)-tacrine, a novel anti-Alzheimer's agent, on rat brain AChE., Neuroreport
Marco et al., 2003, Recent developments in the synthesis of acetylcholinesterase inhibitors., Mini Rev Med Chem
Krustev et al., 2006, Calcium-independent tacrine-induced relaxation of rat gastric corpus smooth muscles., Can. J. Physiol. Pharmacol.
Du et al., 2004, Development of bivalent acetylcholinesterase inhibitors as potential therapeutic drugs for Alzheimer's disease., Curr. Pharm. Des.
Traykov et al., 1999, In vivo PET study of cerebral [11C] methyl- tetrahydroaminoacridine distribution and kinetics in healthy human subjects., Eur. J. Neurol.
Takatori, 2006, [Mechanisms of neuroprotective effects of therapeutic acetylcholinesterase inhibitors used in treatment of Alzheimer's disease]., Yakugaku Zasshi
Ahmed et al., 2006, Inhibition of two different cholinesterases by tacrine., Chem. Biol. Interact.
Wang et al., 1998, Anticholinesterase effects of huperzine A, E2020, and tacrine in rats., Zhongguo Yao Li Xue Bao
Villarroya et al., 2004, New classes of AChE inhibitors with additional pharmacological effects of interest for the treatment of Alzheimer's disease., Curr. Pharm. Des.
Bag S et al., 2013, Design, synthesis and biological activity of multifunctional α,β-unsaturated carbonyl scaffolds for Alzheimer's disease., Bioorg Med Chem Lett
Olin et al., 2002, Galantamine for Alzheimer's disease., Cochrane Database Syst Rev
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Lilienfeld, 2002, Galantamine--a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer's disease., CNS Drug Rev
Guillou et al., 2000, Potent acetylcholinesterase inhibitors: design, synthesis and structure-activity relationships of alkylene linked bis-galanthamine and galanthamine-galanthaminium salts., Bioorg. Med. Chem. Lett.
Scott et al., 2000, Galantamine: a review of its use in Alzheimer's disease., Drugs
Greenblatt et al., 1999, Structure of acetylcholinesterase complexed with (-)-galanthamine at 2.3 A resolution., FEBS Lett.
Tonkopiĭ et al., 1976, [Interaction of reversible inhibitors with the catalytic centers and allosteric sites of cholinesterases]., Biull Eksp Biol Med
Woodruff-Pak et al., 2002, Nicotinic cholinergic modulation: galantamine as a prototype., CNS Drug Rev
Lilienfeld et al., 2000, Galantamine: additional benefits to patients with Alzheimer's disease., Dement Geriatr Cogn Disord
Blesa, 2000, Galantamine: therapeutic effects beyond cognition., Dement Geriatr Cogn Disord
Hansen et al.
Woodruff-Pak DS et al., 2001, Galantamine: effect on nicotinic receptor binding, acetylcholinesterase inhibition, and learning., Proc Natl Acad Sci U S A
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Robaire et al., 1975, Effects of edrophonium, eserine, decamethonium, d-tubocurarine, and gallamine on the kinetics of membrane-bound and solubilized eel acetylcholinesterase., Mol. Pharmacol.
Hallek et al., 1988, Effects of some mono- and bisquaternary ammonium compounds on the reactivatability of soman-inhibited human acetylcholinesterase in vitro., Biochem. Pharmacol.
Wu et al., 1989, Tacrine protection of acetylcholinesterase from inactivation by diisopropylfluorophosphate: a circular dichroism study., Mol. Pharmacol.
Seto et al., 1988, Structure-activity relationship of reversible cholinesterase inhibitors including paraquat., Arch. Toxicol.
Sinha et al., 1975, Synthesis and biological activity of spin-labeled analogs of biotin, hexamethonium, decamethonium, dichlorisoproterenol, and propranolol., J. Med. Chem.
Durcan et al., 2006, Eosinophil-mediated cholinergic nerve remodeling., Am. J. Respir. Cell Mol. Biol.
Anzai, 2006, [Use of biosensors for detecting organophosphorus agents]., Yakugaku Zasshi
Amenta et al., 2006, Association with the cholinergic precursor choline alphoscerate and the cholinesterase inhibitor rivastigmine: an approach for enhancing cholinergic neurotransmission., Mech. Ageing Dev.
Alkondon et al., 2006, Subtype-specific inhibition of nicotinic acetylcholine receptors by choline: a regulatory pathway., J. Pharmacol. Exp. Ther.
Longobardi et al., 2005, Use of electrochemical biosensor and gas chromatography for determination of dichlorvos in wheat., J. Agric. Food Chem.
Ricordel et al., 2000, [Chemical weapons: antidotes. View about the real means, perspectives]., Ann Pharm Fr
Servatius et al., 2000, Effects of inescapable stress and treatment with pyridostigmine bromide on plasma butyrylcholinesterase and the acoustic startle response in rats., Physiol. Behav.
Drake-Baumann et al., 1999, Effects of exposure to low-dose pyridostigmine on neuromuscular junctions in vitro., Muscle Nerve
Prasad et al., 2000, Interactions of bovine brain tubulin with pyridostigmine bromide and N,N'-diethyl-m-toluamide., Neurochem. Res.
Sinton et al., 2000, Stressful manipulations that elevate corticosterone reduce blood-brain barrier permeability to pyridostigmine in the Rat., Toxicol. Appl. Pharmacol.
Mazzucchelli M et al., 2003, Characterization of the effect of ganstigmine (CHF2819) on amyloid precursor protein metabolism in SH-SY5Y neuroblastoma cells., J Neural Transm (Vienna)
Bartolucci C et al., 2006, Structural determinants of Torpedo californica acetylcholinesterase inhibition by the novel and orally active carbamate based anti-alzheimer drug ganstigmine (CHF-2819)., J Med Chem
Huby et al., 1999, Role of acetylcholinesterase (AChE) secreted by parasitic nematodes on the growth of the cell line from epithelial origin HT29-D4., Parasitology
Luo et al., 1999, Role of edrophonium in prevention of the re-inhibition of acetylcholinesterase by phosphorylated oxime., Chem. Biol. Interact.
Luo et al., 1999, Phosphoryl oxime inhibition of acetylcholinesterase during oxime reactivation is prevented by edrophonium., Biochemistry
Martín-Biosca et al., 2009, Screening of acetylcholinesterase inhibitors by CE after enzymatic reaction at capillary inlet., J Sep Sci
Keymer et al., 1999, Acetylcholinesterase and inhibitors: effects upon normal and regenerating nerves of the rat., Eur. J. Neurosci.
Ravelli et al., 1998, Static Laue diffraction studies on acetylcholinesterase., Acta Crystallogr. D Biol. Crystallogr.
Hatip-Al-Khatib et al., 2005, Effect of oral administration of zanapezil (TAK-147) for 21 days on acetylcholine and monoamines levels in the ventral hippocampus of freely moving rats., Br. J. Pharmacol.
Ciesielski-Treska et al., 1975, Morphological, histochemical and chromosomal patterns of neuroblastoma parental and purine resistant lines., Neurobiology
Duarte et al., 2007, Privileged structures: a useful concept for the rational design of new lead drug candidates., Mini Rev Med Chem
Contreras et al., 1999, Aminopyridazines as acetylcholinesterase inhibitors., J. Med. Chem.
Greig et al., 2005, Anticholinesterase and pharmacokinetic profile of phenserine in healthy elderly human subjects., Curr Alzheimer Res
Klein, 2007, Phenserine., Expert Opin Investig Drugs
Ward et al., 2003, The effects of topical ocular application of 0.25% demecarium bromide on serum acetylcholinesterase levels in normal dogs., Vet Ophthalmol
Choung et al., 2007, A double-blind, randomized, placebo-controlled trial of itopride (100 and 200 mg three times daily) on gastric motor and sensory function in healthy volunteers., Neurogastroenterol. Motil.
Jokanović, 2009, Medical treatment of acute poisoning with organophosphorus and carbamate pesticides., Toxicol. Lett.
Kovacic, 2003, Mechanism of organophosphates (nerve gases and pesticides) and antidotes: electron transfer and oxidative stress., Curr. Med. Chem.
Jokanović et al., 2009, Pyridinium oximes as cholinesterase reactivators. Structure-activity relationship and efficacy in the treatment of poisoning with organophosphorus compounds., Curr. Med. Chem.
Wong et al., 2000, Mechanism of oxime reactivation of acetylcholinesterase analyzed by chirality and mutagenesis., Biochemistry
Kalisiak J et al., 2011, Amidine-oximes: reactivators for organophosphate exposure., J Med Chem
Kalisiak J et al., 2012, Nonquaternary reactivators for organophosphate-inhibited cholinesterases., J Med Chem
Bourgeois et al., 1978, [Effects of chronic paralysis of chick embryo by flaxedil on the development of the neuromuscular junction]., C.R. Hebd. Seances Acad. Sci., Ser. D, Sci. Nat.
Radić et al., 1999, The influence of peripheral site ligands on the reaction of symmetric and chiral organophosphates with wildtype and mutant acetylcholinesterases., Chem. Biol. Interact.
Elsinghorst et al., 2007, First gallamine-tacrine hybrid: design and characterization at cholinesterases and the M2 muscarinic receptor., J. Med. Chem.
Radić et al., 2001, Peripheral site ligands accelerate inhibition of acetylcholinesterase by neutral organophosphates., J Appl Toxicol
Ishitani et al., 1972, Studies on the ultrastructural distribution of H 3 -dimetacrine in rat cerebral cortex., Jpn. J. Pharmacol.
Gupta et al., 1992, Potential of memantine, D-tubocurarine, and atropine in preventing acute toxic myopathy induced by organophosphate nerve agents: soman, sarin, tabun and VX., Neurotoxicology
Golicnik et al., 2002, Acceleration of Drosophila melanogaster acetylcholinesterase methanesulfonylation: peripheral ligand D-tubocurarine enhances the affinity for small methanesulfonylfluoride., Chem. Biol. Interact.
Bianchi et al., 2005, Synthesis of tricyclic analogs of stephaoxocanidine and their evaluation as acetylcholinesterase inhibitors., Bioorg. Med. Chem. Lett.
Kari et al., 1985, Effects of the synthetic glucocorticoid betamethasone on the survival of neurons in fetal rabbit brain cell culture., Brain Res.
Singh et al., 1998, Effects of hexamethonium, phenothiazines, propranolol and ephedrine on acetylcholinesterase carbamylation by physostigmine, aldicarb and carbaryl: interaction between the active site and the functionally distinct peripheral sites in acetylcholinesterase., Comp. Biochem. Physiol. C, Pharmacol. Toxicol. Endocrinol.
Nakamura et al., 1993, Characterization of esterases involved in the hydrolysis of dipivefrin hydrochloride., Ophthalmic Res.
Robinson et al., 1993, Prenatal exposure to methadone delays the development of striatal cholinergic neurons., Brain Res. Dev. Brain Res.
Tsakiris et al., The effect of galactose metabolic disorders on rat brain acetylcholinesterase activity., Z. Naturforsch., C, J. Biosci.
Zeitz et al., 1978, Effects of 6-aminonicotinamide on growth and acetylcholinesterase activity during differentiation of neuroblastoma cells in vitro., Naunyn Schmiedebergs Arch. Pharmacol.
Changeux JP et al., 1969, On the association of tyrocidine with acetylcholinesterase., Proc Natl Acad Sci U S A
Petroianu GA et al., 2005, Weak inhibitors protect cholinesterases from strong inhibitors (paraoxon): in vitro effect of ranitidine., J Appl Toxicol
Kounenis G et al., 1986, The inhibition of acetylcholinesterase by ranitidine: a study on the guinea pig ileum., J Pharmacobiodyn
Laine-Cessac P et al., 1993, Inhibition of cholinesterases by histamine 2 receptor antagonist drugs., Res Commun Chem Pathol Pharmacol
Aono M et al., 1986, Cholinergic effects of histamine-H2 receptor antagonists partly through inhibition of acetylcholinesterase., Gastroenterol Jpn

GALANTAMINE HYDROBROMIDE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Acetylcholinesterase inhibitor

Publications:
ECHOTHIOPHATE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:
HEXAFLUORENIUM BROMIDE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Acetylcholinesterase inhibitor

Publications:
PRALIDOXIME CHLORIDE ACHE

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase activator

Direct Interaction yes

Publications:
PYRIDOSTIGMINE BROMIDE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase inhibitor

Direct Interaction yes

Publications:
ECHOTHIOPHATE IODIDE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase inhibitor

Direct Interaction yes

Publications:
AMBENONIUM CHLORIDE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase inhibitor

Direct Interaction yes

Publications:
EDROPHONIUM CHLORIDE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Acetylcholinesterase inhibitor

Publications:
TACRINE HYDROCHLORIDE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cholinesterases; ACHE & BCHE inhibitor

Direct Interaction yes

Publications:
RIVASTIGMINE TARTRATE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cholinesterases; ACHE & BCHE inhibitor

Direct Interaction yes

Publications:
NEOSTIGMINE METHYLSULFATE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase inhibitor

Direct Interaction yes

Publications:
DEMECARIUM BROMIDE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase inhibitor

Direct Interaction yes

Publications:
DONEPEZIL HYDROCHLORIDE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase inhibitor

Direct Interaction yes

Publications:

NEOSTIGMINE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of ACHE activity in human serum.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:

Zhang et al., 2009, Neuromuscular blockade, reversal agent use, and operating room time: retrospective analysis of US inpatient surgeries., Curr Med Res Opin

Naves et al., 2001, Repetitive nerve stimulation decreases the acetylcholine content of quanta at the frog neuromuscular junction., J. Physiol. (Lond.)

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

RIVASTIGMINE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cholinesterases; ACHE & BCHE inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

Publications:

Greig et al., 2002, Butyrylcholinesterase: an important new target in Alzheimer's disease therapy., Int Psychogeriatr

Farlow, 2003, Update on rivastigmine., Neurologist

Stahl, 2000, The new cholinesterase inhibitors for Alzheimer's disease, Part 1: their similarities are different., J Clin Psychiatry

ISOFLUROPHATE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase inhibitor

Direct Interaction yes

Publications:

Ashani et al., 1990, Differences in conformational stability between native and phosphorylated acetylcholinesterase as evidenced by a monoclonal antibody., Biochemistry

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

da Costa et al., 2001, Short- and long-term influences of calcitonin gene-related peptide on the synthesis of acetylcholinesterase in mammalian myotubes., Br. J. Pharmacol.

DONEPEZIL ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:

Kryger et al., 1999, Structure of acetylcholinesterase complexed with E2020 (Aricept): implications for the design of new anti-Alzheimer drugs., Structure

Davis, 1999, Alzheimer's disease: seeking new ways to preserve brain function. Interview by Alice V. Luddington., Geriatrics

Shepherd et al., Donepezil overdose: a tenfold dosing error., Ann Pharmacother

PHYSOSTIGMINE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name physostigmine ,Xalieve

Specific Action of the Ligand Inhibition

Publications:

Monnet-Tschudi et al., 2000, Maturation-dependent effects of chlorpyrifos and parathion and their oxygen analogs on acetylcholinesterase and neuronal and glial markers in aggregating brain cell cultures., Toxicol. Appl. Pharmacol.

Nguyen et al., 1999, Maturation of neuromuscular transmission during early development in zebrafish., J. Neurophysiol.

Tuovinen et al., 1999, Success of pyridostigmine, physostigmine, eptastigmine and phosphotriesterase treatments in acute sarin intoxication., Toxicology

AMBENONIUM ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Hodge et al., 1992, Ambenonium is a rapidly reversible noncovalent inhibitor of acetylcholinesterase, with one of the highest known affinities., Mol. Pharmacol.

Webb, 1965, Affinity of benzoquinonium and ambenonium derivatives for the acetylcholine receptor, tested on the electroplax, and for acetylcholinesterase in solution., Biochim. Biophys. Acta

Bolognesi et al., 2003, Design, synthesis and biological evaluation of ambenonium derivatives as AChE inhibitors., Farmaco

TACRINE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Specific Action of the Ligand Inhibition

Publications:

Wang et al., 1999, Effects of bis(7)-tacrine, a novel anti-Alzheimer's agent, on rat brain AChE., Neuroreport

Marco et al., 2003, Recent developments in the synthesis of acetylcholinesterase inhibitors., Mini Rev Med Chem

Davis, 1999, Alzheimer's disease: seeking new ways to preserve brain function. Interview by Alice V. Luddington., Geriatrics

GALANTAMINE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name galantamine hydrobromide,Razadyne, Reminyl

Novel drug target Established target

Specific Action of the Ligand Inhibition

Publications:

Bag S et al., 2013, Design, synthesis and biological activity of multifunctional α,β-unsaturated carbonyl scaffolds for Alzheimer's disease., Bioorg Med Chem Lett

Olin et al., 2002, Galantamine for Alzheimer's disease., Cochrane Database Syst Rev

Stahl, 2000, The new cholinesterase inhibitors for Alzheimer's disease, Part 1: their similarities are different., J Clin Psychiatry

DECAMETHONIUM ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Robaire et al., 1975, Effects of edrophonium, eserine, decamethonium, d-tubocurarine, and gallamine on the kinetics of membrane-bound and solubilized eel acetylcholinesterase., Mol. Pharmacol.

Hallek et al., 1988, Effects of some mono- and bisquaternary ammonium compounds on the reactivatability of soman-inhibited human acetylcholinesterase in vitro., Biochem. Pharmacol.

Wu et al., 1989, Tacrine protection of acetylcholinesterase from inactivation by diisopropylfluorophosphate: a circular dichroism study., Mol. Pharmacol.

CHOLINE ACHE

Interaction Types & Directionality:

product of

Interaction Info:

Publications:

Durcan et al., 2006, Eosinophil-mediated cholinergic nerve remodeling., Am. J. Respir. Cell Mol. Biol.

Anzai, 2006, [Use of biosensors for detecting organophosphorus agents]., Yakugaku Zasshi

Amenta et al., 2006, Association with the cholinergic precursor choline alphoscerate and the cholinesterase inhibitor rivastigmine: an approach for enhancing cholinergic neurotransmission., Mech. Ageing Dev.

PYRIDOSTIGMINE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

antagonist (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:

Ricordel et al., 2000, [Chemical weapons: antidotes. View about the real means, perspectives]., Ann Pharm Fr

Servatius et al., 2000, Effects of inescapable stress and treatment with pyridostigmine bromide on plasma butyrylcholinesterase and the acoustic startle response in rats., Physiol. Behav.

Drake-Baumann et al., 1999, Effects of exposure to low-dose pyridostigmine on neuromuscular junctions in vitro., Muscle Nerve

EDROPHONIUM ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Details of the Assay for Interaction Using the chloride salt

Publications:

Huby et al., 1999, Role of acetylcholinesterase (AChE) secreted by parasitic nematodes on the growth of the cell line from epithelial origin HT29-D4., Parasitology

Luo et al., 1999, Role of edrophonium in prevention of the re-inhibition of acetylcholinesterase by phosphorylated oxime., Chem. Biol. Interact.

Luo et al., 1999, Phosphoryl oxime inhibition of acetylcholinesterase during oxime reactivation is prevented by edrophonium., Biochemistry

MINAPRINE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Duarte et al., 2007, Privileged structures: a useful concept for the rational design of new lead drug candidates., Mini Rev Med Chem

Contreras et al., 1999, Aminopyridazines as acetylcholinesterase inhibitors., J. Med. Chem.

DEMECARIUM ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Ward et al., 2003, The effects of topical ocular application of 0.25% demecarium bromide on serum acetylcholinesterase levels in normal dogs., Vet Ophthalmol

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

ITOPRIDE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name itopride,Itax

Novel drug target Established target

Publications:

Choung et al., 2007, A double-blind, randomized, placebo-controlled trial of itopride (100 and 200 mg three times daily) on gastric motor and sensory function in healthy volunteers., Neurogastroenterol. Motil.

PRALIDOXIME ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

activator (activating)

Interaction Info:

Details of the Assay for Interaction Inhibition of human recombinant AChE by modified Ellman's method.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:

Jokanović, 2009, Medical treatment of acute poisoning with organophosphorus and carbamate pesticides., Toxicol. Lett.

Kovacic, 2003, Mechanism of organophosphates (nerve gases and pesticides) and antidotes: electron transfer and oxidative stress., Curr. Med. Chem.

Jokanović et al., 2009, Pyridinium oximes as cholinesterase reactivators. Structure-activity relationship and efficacy in the treatment of poisoning with organophosphorus compounds., Curr. Med. Chem.

GALLAMINE TRIETHIODIDE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Seto et al., 1988, Structure-activity relationship of reversible cholinesterase inhibitors including paraquat., Arch. Toxicol.

Bourgeois et al., 1978, [Effects of chronic paralysis of chick embryo by flaxedil on the development of the neuromuscular junction]., C.R. Hebd. Seances Acad. Sci., Ser. D, Sci. Nat.

Robaire et al., 1975, Effects of edrophonium, eserine, decamethonium, d-tubocurarine, and gallamine on the kinetics of membrane-bound and solubilized eel acetylcholinesterase., Mol. Pharmacol.

DIMETACRINE ACHE

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Ishitani et al., 1972, Studies on the ultrastructural distribution of H 3 -dimetacrine in rat cerebral cortex., Jpn. J. Pharmacol.

TUBOCURARINE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Gupta et al., 1992, Potential of memantine, D-tubocurarine, and atropine in preventing acute toxic myopathy induced by organophosphate nerve agents: soman, sarin, tabun and VX., Neurotoxicology

Radić et al., 1999, The influence of peripheral site ligands on the reaction of symmetric and chiral organophosphates with wildtype and mutant acetylcholinesterases., Chem. Biol. Interact.

Golicnik et al., 2002, Acceleration of Drosophila melanogaster acetylcholinesterase methanesulfonylation: peripheral ligand D-tubocurarine enhances the affinity for small methanesulfonylfluoride., Chem. Biol. Interact.

DIPIVEFRIN ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Nakamura et al., 1993, Characterization of esterases involved in the hydrolysis of dipivefrin hydrochloride., Ophthalmic Res.
TYROTHRICIN ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Changeux JP et al., 1969, On the association of tyrocidine with acetylcholinesterase., Proc Natl Acad Sci U S A

RANITIDINE ACHE

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Petroianu GA et al., 2005, Weak inhibitors protect cholinesterases from strong inhibitors (paraoxon): in vitro effect of ranitidine., J Appl Toxicol

Kounenis G et al., 1986, The inhibition of acetylcholinesterase by ranitidine: a study on the guinea pig ileum., J Pharmacobiodyn

Laine-Cessac P et al., 1993, Inhibition of cholinesterases by histamine 2 receptor antagonist drugs., Res Commun Chem Pathol Pharmacol

ACOTIAMIDE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name acotiamide hydrochloride, YM-443, Z-338

Novel drug target Established target

Publications:
LATREPIRDINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name Dimebon

Publications:
TURBINATINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Cardoso CL et al., 2004, Indole glucoalkaloids from Chimarrhis turbinata and their evaluation as antioxidant agents and acetylcholinesterase inhibitors., J Nat Prod

PROPIDIUM ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

GANSTIGMINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Mazzucchelli M et al., 2003, Characterization of the effect of ganstigmine (CHF2819) on amyloid precursor protein metabolism in SH-SY5Y neuroblastoma cells., J Neural Transm (Vienna)

Bartolucci C et al., 2006, Structural determinants of Torpedo californica acetylcholinesterase inhibition by the novel and orally active carbamate based anti-alzheimer drug ganstigmine (CHF-2819)., J Med Chem

ZANAPEZIL ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Hatip-Al-Khatib et al., 2005, Effect of oral administration of zanapezil (TAK-147) for 21 days on acetylcholine and monoamines levels in the ventral hippocampus of freely moving rats., Br. J. Pharmacol.

THIOGUANINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Ciesielski-Treska et al., 1975, Morphological, histochemical and chromosomal patterns of neuroblastoma parental and purine resistant lines., Neurobiology

PHENSERINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name Phenserine

Publications:

Greig et al., 2005, Anticholinesterase and pharmacokinetic profile of phenserine in healthy elderly human subjects., Curr Alzheimer Res

Klein, 2007, Phenserine., Expert Opin Investig Drugs

ACETYLCHOLINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

BETAMETHASONE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Kari et al., 1985, Effects of the synthetic glucocorticoid betamethasone on the survival of neurons in fetal rabbit brain cell culture., Brain Res.

EPHEDRINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Singh et al., 1998, Effects of hexamethonium, phenothiazines, propranolol and ephedrine on acetylcholinesterase carbamylation by physostigmine, aldicarb and carbaryl: interaction between the active site and the functionally distinct peripheral sites in acetylcholinesterase., Comp. Biochem. Physiol. C, Pharmacol. Toxicol. Endocrinol.

8-AZAGUANINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Ciesielski-Treska et al., 1975, Morphological, histochemical and chromosomal patterns of neuroblastoma parental and purine resistant lines., Neurobiology
DESOXYCORDIFOLINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Cardoso CL et al., 2004, Indole glucoalkaloids from Chimarrhis turbinata and their evaluation as antioxidant agents and acetylcholinesterase inhibitors., J Nat Prod
METHADONE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Robinson et al., 1993, Prenatal exposure to methadone delays the development of striatal cholinergic neurons., Brain Res. Dev. Brain Res.
GALACTITOL ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Tsakiris et al., The effect of galactose metabolic disorders on rat brain acetylcholinesterase activity., Z. Naturforsch., C, J. Biosci.
6-AMINONICOTINAMIDE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Zeitz et al., 1978, Effects of 6-aminonicotinamide on growth and acetylcholinesterase activity during differentiation of neuroblastoma cells in vitro., Naunyn Schmiedebergs Arch. Pharmacol.
EPTASTIGMINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
TRIMEDOXIME ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
TOLSERINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
CORONARIDINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
CLEBOPRIDE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
LYSICAMINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
CHLORANIL ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL516841 ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL463083 ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL136229 ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
XANTHOSTIGMINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
PARAOXON ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
LAWSARITOL ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL433282 ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL603711 ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL464944 ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
LADOSTIGIL ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
INFRACTOPICRIN ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
OBIDOXIME ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL244416 ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
BENZOQUINONE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL463500 ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL465346 ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
ETHYLPHENSERINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
TASPINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
TETRAISOPROPYL PYROPHOSPHORAMIDE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
CHLORPYRIFOS ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
GENESERINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
DECIDIUM ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
PETROSAMINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
CAPROCTAMINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
VOACANGINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL75121 ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
MALATHION ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
MEMOQUIN ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL539624 ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL517486 ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
AMOCARZINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL32823 ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL465347 ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL589071 ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
SKIMMIANINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
4-ISOPROPYLPHENSERINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
N-ALLYLNORGALANTHAMINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
LIPOCRINE ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL135503 ACHE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Ensembl: ENSG00000087085
- Version: 101_38
Alternate Names:

ACHE Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
RussLampel: ENSG00000087085
- Version: 26-July-2011
Alternate Names:

ENSG00000087085 Ensembl Gene Id

ACHE Display Id

ACETYLCHOLINESTERASE PRECURSOR (EC 3.1.1.7) (ACHE). [SOURCE:UNIPROT/SWISSPROT;ACC:P22303] Description

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
TEND: P22303
- Version: 01-August-2011
Alternate Names:

P22303 Uniprot Accession

ENSG00000087085 Ensembl Gene Id

43 Entrez Gene Id

Gene Info:

Target Main Class Enzymes

Target Subclass 3.1.1.7

Publications:
HopkinsGroom: P22303
- Version: 11-September-2012
Alternate Names:

ACHE Uniprot Gene Name

43 Entrez Gene Id

P22303 Uniprot Accession

Gene Info:

Interpro Acc IPR002018

Interpro Name Carboxylesterase, type B

Uniprot Status Swiss-Prot

Gene Categories:

DRUGGABLE GENOME

Publications:
TdgClinicalTrial: P22303
- Version: January-2014
Alternate Names:

ACHE Gene Symbol

Gene Info:

Target Subclass EC:3.1.1.7

Target Class Enzymes

Publications:

PharmGKB: ACHE

Version: 18-August-2020

Alternate Names:

PA20 PharmGKB ID

Gene Info:

Publications:

Scacchi R et al., 2009, Variability of AChE, BChE, and ChAT genes in the late-onset form of Alzheimer's disease and relationships with response to treatment with Donepezil and Rivastigmine., Am J Med Genet B Neuropsychiatr Genet

DrugBank: BE0000426

Version: 5.1.7

Alternate Names:

ACHE DrugBank Gene Name

P22303 UniProt Accession

43 Entrez Gene Id

Gene Info:

Publications:

Alkondon et al., 2006, Subtype-specific inhibition of nicotinic acetylcholine receptors by choline: a regulatory pathway., J. Pharmacol. Exp. Ther.

Anzai, 2006, [Use of biosensors for detecting organophosphorus agents]., Yakugaku Zasshi

Longobardi et al., 2005, Use of electrochemical biosensor and gas chromatography for determination of dichlorvos in wheat., J. Agric. Food Chem.

NCI: ACHE

Version: 14-September-2017

Alternate Names:

Gene Info:

Publications:

Ciesielski-Treska et al., 1975, Morphological, histochemical and chromosomal patterns of neuroblastoma parental and purine resistant lines., Neurobiology

Tsakiris et al., The effect of galactose metabolic disorders on rat brain acetylcholinesterase activity., Z. Naturforsch., C, J. Biosci.

Abou-Bedair et al., 2002, Comparison of hypoxic cell radiosensitizers, KIN-804, KIN-844, KIN-806 and TX-1877, on brain and liver metabolizing capacities in mice bearing Ehrlich ascites carcinoma., Biol. Pharm. Bull.

DTC: ACHE

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Cardoso CL et al., 2004, Indole glucoalkaloids from Chimarrhis turbinata and their evaluation as antioxidant agents and acetylcholinesterase inhibitors., J Nat Prod

Huang L et al., 2014, Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease., Eur J Med Chem

Kalisiak J et al., 2012, Nonquaternary reactivators for organophosphate-inhibited cholinesterases., J Med Chem

HingoraniCasas: ENSG00000087085
- Version: 31-May-2017
Alternate Names:

ENSG00000087085 Gene Symbol

ACHE Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: ACHE
- Version: chembl_23
Alternate Names:

ACHE GENE_SYMBOL

Acetylcholinesterase UNIPROT

AChE UNIPROT

Gene Info:

Publications:
GuideToPharmacologyInteractions: ENSG00000087085
- Version: 20-July-2020
Alternate Names:

acetylcholinesterase (Cartwright blood group) GuideToPharmacology Name

P22303 UniProtKB ID

Gene Info:

Publications:
TTD: Acetylcholinesterase
- Version: 2020.06.01
Alternate Names:

AChE TTD Gene Abbreviation

T30082 TTD Target ID

Gene Info:

Publications:
GO: ACHE
- Version: 05-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CELL SURFACE

Publications:

Direct Interaction	yes
Mechanism of Interaction	Acetylcholinesterase inhibitor

Direct Interaction?	False
Endogenous Drug?	False
Specific Action of the Ligand	Inhibition

Mechanism of Interaction	Acetylcholinesterase activator
Direct Interaction	yes

Mechanism of Interaction	Cholinesterases; ACHE & BCHE inhibitor
Direct Interaction	yes

Details of the Assay for Interaction	Inhibition of ACHE activity in human serum.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Direct Interaction?	True
Endogenous Drug?	False
Specific Action of the Ligand	Inhibition

Novel drug target	Established target
Trial Name	physostigmine ,Xalieve
Specific Action of the Ligand	Inhibition

Trial Name	galantamine hydrobromide,Razadyne, Reminyl
Novel drug target	Established target
Specific Action of the Ligand	Inhibition

Details of the Assay for Interaction	Inhibition of human recombinant AChE by modified Ellman's method.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Trial Name	acotiamide hydrochloride, YM-443, Z-338
Novel drug target	Established target

ENSG00000087085	Ensembl Gene Id
ACHE	Display Id
ACETYLCHOLINESTERASE PRECURSOR (EC 3.1.1.7) (ACHE). [SOURCE:UNIPROT/SWISSPROT;ACC:P22303]	Description

P22303	Uniprot Accession
ENSG00000087085	Ensembl Gene Id
43	Entrez Gene Id

ACHE	Uniprot Gene Name
43	Entrez Gene Id
P22303	Uniprot Accession

ACHE	DrugBank Gene Name
P22303	UniProt Accession
43	Entrez Gene Id

acetylcholinesterase (Cartwright blood group)	GuideToPharmacology Name
P22303	UniProtKB ID

ACHE Gene Record

ACHE 43 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Acetylcholinesterase inhibitor

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand Inhibition

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Acetylcholinesterase inhibitor

Publications:

Interaction Types & Directionality: activator (activating)

Interaction Info: Mechanism of Interaction Acetylcholinesterase activator Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Acetylcholinesterase inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Acetylcholinesterase inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Acetylcholinesterase inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Acetylcholinesterase inhibitor

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cholinesterases; ACHE & BCHE inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cholinesterases; ACHE & BCHE inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Acetylcholinesterase inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Acetylcholinesterase inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Acetylcholinesterase inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Inhibition of ACHE activity in human serum. Specific Action of the Ligand Inhibition Endogenous Drug? False

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cholinesterases; ACHE & BCHE inhibitor Direct Interaction yes Specific Action of the Ligand Inhibition

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Acetylcholinesterase inhibitor Direct Interaction yes

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? True Endogenous Drug? False Specific Action of the Ligand Inhibition

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Novel drug target Established target Trial Name physostigmine ,Xalieve Specific Action of the Ligand Inhibition

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Novel drug target Established target Trial Name - Specific Action of the Ligand Inhibition

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name galantamine hydrobromide,Razadyne, Reminyl Novel drug target Established target Specific Action of the Ligand Inhibition

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Interaction Types & Directionality: product of

Interaction Info:

Interaction Types & Directionality: inhibitor (inhibitory) antagonist (inhibitory)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand Inhibition

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target Details of the Assay for Interaction Using the chloride salt

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications: Duarte et al., 2007, Privileged structures: a useful concept for the rational design of new lead drug candidates., Mini Rev Med Chem Contreras et al., 1999, Aminopyridazines as acetylcholinesterase inhibitors., J. Med. Chem.

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications: Ward et al., 2003, The effects of topical ocular application of 0.25% demecarium bromide on serum acetylcholinesterase levels in normal dogs., Vet Ophthalmol Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name itopride,Itax Novel drug target Established target

Publications: Choung et al., 2007, A double-blind, randomized, placebo-controlled trial of itopride (100 and 200 mg three times daily) on gastric motor and sensory function in healthy volunteers., Neurogastroenterol. Motil.

Interaction Types & Directionality: inhibitor (inhibitory) activator (activating)

Interaction Info: Details of the Assay for Interaction Inhibition of human recombinant AChE by modified Ellman's method. Specific Action of the Ligand Inhibition Endogenous Drug? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Acetylcholinesterase inhibitor

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Acetylcholinesterase inhibitor

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase activator

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Acetylcholinesterase inhibitor

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cholinesterases; ACHE & BCHE inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cholinesterases; ACHE & BCHE inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of ACHE activity in human serum.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cholinesterases; ACHE & BCHE inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name physostigmine ,Xalieve

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name galantamine hydrobromide,Razadyne, Reminyl

Novel drug target Established target

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

product of

Interaction Types & Directionality:

inhibitor (inhibitory)

antagonist (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Details of the Assay for Interaction Using the chloride salt

Interaction Types & Directionality:

inhibitor (inhibitory)

Publications:

Duarte et al., 2007, Privileged structures: a useful concept for the rational design of new lead drug candidates., Mini Rev Med Chem

Contreras et al., 1999, Aminopyridazines as acetylcholinesterase inhibitors., J. Med. Chem.

Interaction Types & Directionality:

inhibitor (inhibitory)

Publications:

Ward et al., 2003, The effects of topical ocular application of 0.25% demecarium bromide on serum acetylcholinesterase levels in normal dogs., Vet Ophthalmol

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name itopride,Itax

Novel drug target Established target

Publications:

Choung et al., 2007, A double-blind, randomized, placebo-controlled trial of itopride (100 and 200 mg three times daily) on gastric motor and sensory function in healthy volunteers., Neurogastroenterol. Motil.

Interaction Types & Directionality:

inhibitor (inhibitory)

activator (activating)

Interaction Info:

Details of the Assay for Interaction Inhibition of human recombinant AChE by modified Ellman's method.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

antagonist (inhibitory)

Publications:

Ishitani et al., 1972, Studies on the ultrastructural distribution of H 3 -dimetacrine in rat cerebral cortex., Jpn. J. Pharmacol.

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Publications:

Nakamura et al., 1993, Characterization of esterases involved in the hydrolysis of dipivefrin hydrochloride., Ophthalmic Res.

Interaction Types & Directionality:

inhibitor (inhibitory)

Publications:

Changeux JP et al., 1969, On the association of tyrocidine with acetylcholinesterase., Proc Natl Acad Sci U S A

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name acotiamide hydrochloride, YM-443, Z-338

Novel drug target Established target