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ACHE Gene Record

  • Summary
  • Interactions
  • Claims
  • 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
    ACETYLCHOLINESTERASE PRECURSOR (EC 3.1.1.7) (ACHE). [SOURCE:UNIPROT/SWISSPROT;ACC:P22303]
    2465
    PA20
    T30082
    NM_015831
    NP_056646

    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
    GuideToPharmacology Gene Category Name Acetylcholine turnover
    GuideToPharmacology Gene Category ID 765
    GuideToPharmacology Gene Category Name Hydrolases
    GuideToPharmacology Gene Category ID 799
    (10 More Sources)

    Gene Categories: Category Details

    CELL SURFACE
    DRUGGABLE GENOME
    ENZYME

    Publications:

    Trevisani et al., 2000, Neostigmine: safe and effective treatment for acute colonic pseudo-obstruction., Dis. Colon Rectum
    Naves et al., 2001, Repetitive nerve stimulation decreases the acetylcholine content of quanta at the frog neuromuscular junction., J. Physiol. (Lond.)
    Beck et al., 2003, Stress interacts with peripheral cholinesterase inhibitors to cause central nervous system effects., Life Sci.
    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.
    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.
    Zhang et al., 2009, Neuromuscular blockade, reversal agent use, and operating room time: retrospective analysis of US inpatient surgeries., Curr Med Res Opin
    Gottwald et al., 1999, Rivastigmine, a brain-region selective acetylcholinesterase inhibitor for treating Alzheimer's disease: review and current status., Expert Opin Investig Drugs
    Naik et al., 2009, Effects of rivastigmine and donepezil on brain acetylcholine levels in acetylcholinesterase-deficient mice., J Pharm Pharm Sci
    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
    Lalli et al., 2008, Rivastigmine in Parkinson's disease dementia., Expert Rev Neurother
    Greig et al., 2002, Butyrylcholinesterase: an important new target in Alzheimer's disease therapy., Int Psychogeriatr
    Birks et al., 2009, Rivastigmine for Alzheimer's disease., Cochrane Database Syst Rev
    Grossberg et al., 2000, Lack of adverse pharmacodynamic drug interactions with rivastigmine and twenty-two classes of medications., Int J Geriatr Psychiatry
    Goldblum et al., 2000, Topical rivastigmine, a selective acetylcholinesterase inhibitor, lowers intraocular pressure in rabbits., J Ocul Pharmacol Ther
    Stahl, 2000, The new cholinesterase inhibitors for Alzheimer's disease, Part 1: their similarities are different., J Clin Psychiatry
    Onor et al., 2007, Rivastigmine in the treatment of Alzheimer's disease: an update., Clin Interv Aging
    Kennedy et al., 1999, Preferential cerebrospinal fluid acetylcholinesterase inhibition by rivastigmine in humans., J Clin Psychopharmacol
    Farlow, 2003, Update on rivastigmine., Neurologist
    Pang et al., 2003, Rational design of alkylene-linked bis-pyridiniumaldoximes as improved acetylcholinesterase reactivators., Chem. Biol.
    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.
    Ashani et al., 1990, Differences in conformational stability between native and phosphorylated acetylcholinesterase as evidenced by a monoclonal antibody., Biochemistry
    Cardoso CL et al., 2004, Indole glucoalkaloids from Chimarrhis turbinata and their evaluation as antioxidant agents and acetylcholinesterase inhibitors., J Nat Prod
    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
    Kryger et al., 1999, Structure of acetylcholinesterase complexed with E2020 (Aricept): implications for the design of new anti-Alzheimer drugs., Structure
    Repantis et al., 2010, Acetylcholinesterase inhibitors and memantine for neuroenhancement in healthy individuals: a systematic review., Pharmacol. Res.
    Jann, 2000, Rivastigmine, a new-generation cholinesterase inhibitor for the treatment of Alzheimer's disease., Pharmacotherapy
    Shepherd et al., Donepezil overdose: a tenfold dosing error., Ann Pharmacother
    Kosasa et al., 1999, Effect of donepezil hydrochloride (E2020) on basal concentration of extracellular acetylcholine in the hippocampus of rats., Eur. J. Pharmacol.
    Davis, 1999, Alzheimer's disease: seeking new ways to preserve brain function. Interview by Alice V. Luddington., Geriatrics
    Huang L et al., 2014, Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease., Eur J Med Chem
    Tuovinen et al., 1999, Success of pyridostigmine, physostigmine, eptastigmine and phosphotriesterase treatments in acute sarin intoxication., Toxicology
    Nguyen et al., 1999, Maturation of neuromuscular transmission during early development in zebrafish., J. Neurophysiol.
    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.
    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.
    Papp et al., 2006, Similarities between CSF-brain extracellular transfer and neurofibrillary tangle invasion in Alzheimer's disease., Neurobiol. Aging
    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.
    Hodge et al., 1992, Ambenonium is a rapidly reversible noncovalent inhibitor of acetylcholinesterase, with one of the highest known affinities., Mol. Pharmacol.
    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.
    Webb, 1965, Affinity of benzoquinonium and ambenonium derivatives for the acetylcholine receptor, tested on the electroplax, and for acetylcholinesterase in solution., Biochim. Biophys. Acta
    Du et al., 2004, Development of bivalent acetylcholinesterase inhibitors as potential therapeutic drugs for Alzheimer's disease., Curr. Pharm. Des.
    Wang et al., 1999, Effects of bis(7)-tacrine, a novel anti-Alzheimer's agent, on rat brain AChE., Neuroreport
    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.
    Traykov et al., 1999, In vivo PET study of cerebral [11C] methyl- tetrahydroaminoacridine distribution and kinetics in healthy human subjects., Eur. J. Neurol.
    Ahmed et al., 2006, Inhibition of two different cholinesterases by tacrine., Chem. Biol. Interact.
    Marco et al., 2003, Recent developments in the synthesis of acetylcholinesterase inhibitors., Mini Rev Med Chem
    Wang et al., 1998, Anticholinesterase effects of huperzine A, E2020, and tacrine in rats., Zhongguo Yao Li Xue Bao
    Takatori, 2006, [Mechanisms of neuroprotective effects of therapeutic acetylcholinesterase inhibitors used in treatment of Alzheimer's disease]., Yakugaku Zasshi
    Krustev et al., 2006, Calcium-independent tacrine-induced relaxation of rat gastric corpus smooth muscles., Can. J. Physiol. Pharmacol.
    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
    Greenblatt et al., 1999, Structure of acetylcholinesterase complexed with (-)-galanthamine at 2.3 A resolution., FEBS Lett.
    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.
    Woodruff-Pak DS et al., 2001, Galantamine: effect on nicotinic receptor binding, acetylcholinesterase inhibition, and learning., Proc Natl Acad Sci U S A
    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
    Olin et al., 2002, Galantamine for Alzheimer's disease., Cochrane Database Syst Rev
    Lilienfeld et al., 2000, Galantamine: additional benefits to patients with Alzheimer's disease., Dement Geriatr Cogn Disord
    Scott et al., 2000, Galantamine: a review of its use in Alzheimer's disease., Drugs
    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
    Hansen et al.
    Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
    Blesa, 2000, Galantamine: therapeutic effects beyond cognition., Dement Geriatr Cogn Disord
    Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
    Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
    Sinha et al., 1975, Synthesis and biological activity of spin-labeled analogs of biotin, hexamethonium, decamethonium, dichlorisoproterenol, and propranolol., J. Med. Chem.
    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.
    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.
    Seto et al., 1988, Structure-activity relationship of reversible cholinesterase inhibitors including paraquat., Arch. Toxicol.
    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.
    Anzai, 2006, [Use of biosensors for detecting organophosphorus agents]., Yakugaku Zasshi
    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.
    Durcan et al., 2006, Eosinophil-mediated cholinergic nerve remodeling., Am. J. Respir. Cell Mol. Biol.
    Prasad et al., 2000, Interactions of bovine brain tubulin with pyridostigmine bromide and N,N'-diethyl-m-toluamide., Neurochem. Res.
    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.
    Ricordel et al., 2000, [Chemical weapons: antidotes. View about the real means, perspectives]., Ann Pharm Fr
    Sinton et al., 2000, Stressful manipulations that elevate corticosterone reduce blood-brain barrier permeability to pyridostigmine in the Rat., Toxicol. Appl. Pharmacol.
    Drake-Baumann et al., 1999, Effects of exposure to low-dose pyridostigmine on neuromuscular junctions in vitro., Muscle Nerve
    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
    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)
    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.
    Martín-Biosca et al., 2009, Screening of acetylcholinesterase inhibitors by CE after enzymatic reaction at capillary inlet., J Sep Sci
    Luo et al., 1999, Phosphoryl oxime inhibition of acetylcholinesterase during oxime reactivation is prevented by edrophonium., Biochemistry
    Luo et al., 1999, Role of edrophonium in prevention of the re-inhibition of acetylcholinesterase by phosphorylated oxime., Chem. Biol. Interact.
    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
    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.
    Klein, 2007, Phenserine., Expert Opin Investig Drugs
    Greig et al., 2005, Anticholinesterase and pharmacokinetic profile of phenserine in healthy elderly human subjects., Curr Alzheimer Res
    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.
    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.
    Kalisiak J et al., 2012, Nonquaternary reactivators for organophosphate-inhibited cholinesterases., J Med Chem
    Kalisiak J et al., 2011, Amidine-oximes: reactivators for organophosphate exposure., J Med Chem
    Kovacic, 2003, Mechanism of organophosphates (nerve gases and pesticides) and antidotes: electron transfer and oxidative stress., Curr. Med. Chem.
    Wong et al., 2000, Mechanism of oxime reactivation of acetylcholinesterase analyzed by chirality and mutagenesis., Biochemistry
    Elsinghorst et al., 2007, First gallamine-tacrine hybrid: design and characterization at cholinesterases and the M2 muscarinic receptor., J. Med. Chem.
    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.
    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., 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.
    Golicnik et al., 2002, Acceleration of Drosophila melanogaster acetylcholinesterase methanesulfonylation: peripheral ligand D-tubocurarine enhances the affinity for small methanesulfonylfluoride., Chem. Biol. Interact.
    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
    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.
    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.
    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
    Kounenis G et al., 1986, The inhibition of acetylcholinesterase by ranitidine: a study on the guinea pig ileum., J Pharmacobiodyn
    Petroianu GA et al., 2005, Weak inhibitors protect cholinesterases from strong inhibitors (paraoxon): in vitro effect of ranitidine., J Appl Toxicol
    Changeux JP et al., 1969, On the association of tyrocidine with acetylcholinesterase., Proc Natl Acad Sci U S A
    He et al., 2007, Study on dual-site inhibitors of acetylcholinesterase: Highly potent derivatives of bis- and bifunctional huperzine B., Bioorg. Med. Chem.
    Zangara, 2003, The psychopharmacology of huperzine A: an alkaloid with cognitive enhancing and neuroprotective properties of interest in the treatment of Alzheimer's disease., Pharmacol. Biochem. Behav.
  • NEOSTIGMINE   ACHE

    Interaction Score: 10.02

    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

    PMIDs:
    10826417 11313435 12726885 11819669 11752352 12522088 19257799


    Sources:
    TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology

  • AMBENONIUM   ACHE

    Interaction Score: 9.19

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    15982786 13679187 2857786 1588924 11752352 11330337 5833399


    Sources:
    TEND TdgClinicalTrial TTD DrugBank

  • EDROPHONIUM   ACHE

    Interaction Score: 5.01

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    10103097 10089512 19472276 10433700 11752352 10421446 10363282


    Sources:
    TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology

  • RIVASTIGMINE   ACHE

    Interaction Score: 4.18

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    11139819 19470293 18780301 18671661 12636181 19370562 10713582 10673128 11078030 18044073 11752352 10587286 14587496


    Sources:
    TEND PharmGKB TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

  • PRALIDOXIME   ACHE

    Interaction Score: 3.76

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

    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

    PMIDs:
    19651196 19519385 22206546 21438612 14529460 10801325


    Sources:
    DTC DrugBank GuideToPharmacology

  • GALANTAMINE   ACHE

    Interaction Score: 3.51

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    23540646 10606746 10762042 11172080 12177686 12137632 10971048 11129124 1026294 12481195 11078030 20480924 10592235 11752352 10971049


    Sources:
    TEND DTC TdgClinicalTrial TTD DrugBank GuideToPharmacology

  • CHEMBL490866   ACHE

    Interaction Score: 3.34

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235 17139284 17016423


    Sources:
    DrugBank

  • CHEMBL455333   ACHE

    Interaction Score: 3.34

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235 17139284 17016423


    Sources:
    DrugBank

  • CHEMBL117651   ACHE

    Interaction Score: 3.34

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235 17139284 17016423


    Sources:
    DrugBank

  • CHEMBL395280   ACHE

    Interaction Score: 2.51

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    10592235 12895686


    Sources:
    DrugBank

  • HUPERZINE B   ACHE

    Interaction Score: 2.51

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235 17126020


    Sources:
    DrugBank

  • GANSTIGMINE   ACHE

    Interaction Score: 2.51

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16913695 12898348


    Sources:
    DrugBank

  • ISOFLUROPHATE   ACHE

    Interaction Score: 2.51

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Acetylcholinesterase inhibitor
    Direct Interaction yes

    PMIDs:
    12837382 11350858 10378121 10898598 11752352 1692236


    Sources:
    TTD DrugBank ChemblInteractions

  • TACRINE   ACHE

    Interaction Score: 2.27

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    15544504 10208549 15544507 10210906 16860785 10513568 10024872 25282266 12871155 10375753 11752352 16880719 17218977


    Sources:
    TEND DTC TdgClinicalTrial TTD DrugBank GuideToPharmacology

  • CHEMBL1082738   ACHE

    Interaction Score: 1.67

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235


    Sources:
    DrugBank

  • CHEMBL1235106   ACHE

    Interaction Score: 1.67

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235


    Sources:
    DrugBank

  • CHEMBL107316   ACHE

    Interaction Score: 1.67

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235


    Sources:
    DrugBank

  • CHEMBL483716   ACHE

    Interaction Score: 1.67

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235


    Sources:
    DrugBank

  • TYROTHRICIN   ACHE

    Interaction Score: 1.67

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    5257018


    Sources:
    DrugBank

  • GALACTITOL   ACHE

    Interaction Score: 1.67

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11098845


    Sources:
    NCI

  • DESOXYCORDIFOLINE   ACHE

    Interaction Score: 1.67

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15568781


    Sources:
    DTC

  • ZANAPEZIL   ACHE

    Interaction Score: 1.67

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15951830


    Sources:
    DrugBank

  • TURBINATINE   ACHE

    Interaction Score: 1.67

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15568781


    Sources:
    DTC

  • PHYSOSTIGMINE   ACHE

    Interaction Score: 1.39

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    10403635 10368402 10873710 11752352 10741458 11141093


    Sources:
    TEND TdgClinicalTrial DrugBank GuideToPharmacology

  • DEMECARIUM   ACHE

    Interaction Score: 1.25

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    12641839 11752352


    Sources:
    DrugBank

  • PYRIDOSTIGMINE   ACHE

    Interaction Score: 1.15

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

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

    PMIDs:
    10685600 10869589 10669805 11752352 10814558 10366222


    Sources:
    TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology

  • PROPIDIUM   ACHE

    Interaction Score: 1.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235 17139284 17016423


    Sources:
    DrugBank

  • DONEPEZIL   ACHE

    Interaction Score: 1.03

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    20522977 11893059 10368299 20193764 10641971 10466911 10513568 10024872 25282266 11752352


    Sources:
    TEND DTC TdgClinicalTrial TTD DrugBank GuideToPharmacology

  • DONEPEZIL HYDROCHLORIDE   ACHE

    Interaction Score: 0.84

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Acetylcholinesterase inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • AMOCARZINE   ACHE

    Interaction Score: 0.84

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • DEMECARIUM BROMIDE   ACHE

    Interaction Score: 0.84

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Acetylcholinesterase inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • DIMETACRINE   ACHE

    Interaction Score: 0.84

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    4539395


    Sources:
    DrugBank

  • EDROPHONIUM CHLORIDE   ACHE

    Interaction Score: 0.84

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Acetylcholinesterase inhibitor

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ITOPRIDE   ACHE

    Interaction Score: 0.84

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    17300287


    Sources:
    TdgClinicalTrial DrugBank

  • AMBENONIUM CHLORIDE   ACHE

    Interaction Score: 0.84

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Acetylcholinesterase inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ECHOTHIOPHATE IODIDE   ACHE

    Interaction Score: 0.84

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Acetylcholinesterase inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • PRALIDOXIME CHLORIDE   ACHE

    Interaction Score: 0.84

    Interaction Types & Directionality:
    activator (activating)

    Interaction Info:
    Mechanism of Interaction Acetylcholinesterase activator
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • HEXAFLUORENIUM BROMIDE   ACHE

    Interaction Score: 0.84

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Acetylcholinesterase inhibitor

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ECHOTHIOPHATE   ACHE

    Interaction Score: 0.84

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology ChemblInteractions

  • DECAMETHONIUM   ACHE

    Interaction Score: 0.84

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    239236 3345199 2913485 1207670 3190453


    Sources:
    DrugBank

  • ACOTIAMIDE   ACHE

    Interaction Score: 0.84

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • CHOLINE SALICYLATE   ACHE

    Interaction Score: 0.72

    Interaction Types & Directionality:
    product of

    Interaction Info:

    PMIDs:
    16297435 17139155 16565162 16302752 16456188


    Sources:
    DrugBank

  • CHEMBL1234669   ACHE

    Interaction Score: 0.67

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235 17139284 17016423


    Sources:
    DrugBank

  • TUBOCURARINE   ACHE

    Interaction Score: 0.63

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    11823003 10421444 1475066 15878275 11920914


    Sources:
    DrugBank

  • CHOLINE   ACHE

    Interaction Score: 0.63

    Interaction Types & Directionality:
    product of

    Interaction Info:

    PMIDs:
    16297435 17139155 16565162 16302752 16456188


    Sources:
    DrugBank

  • 6-AMINONICOTINAMIDE   ACHE

    Interaction Score: 0.56

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    153476


    Sources:
    NCI

  • PHENSERINE   ACHE

    Interaction Score: 0.56

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Novel drug target Established target
    Trial Name Phenserine

    PMIDs:
    17594192 16248851


    Sources:
    TdgClinicalTrial DrugBank

  • GALLAMINE TRIETHIODIDE   ACHE

    Interaction Score: 0.49

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    17944454 10421444 1207670 3190453 417864 11920914


    Sources:
    DrugBank

  • NEOSTIGMINE METHYLSULFATE   ACHE

    Interaction Score: 0.42

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Acetylcholinesterase inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • RIVASTIGMINE TARTRATE   ACHE

    Interaction Score: 0.42

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • TACRINE HYDROCHLORIDE   ACHE

    Interaction Score: 0.42

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ACETYLCHOLINE   ACHE

    Interaction Score: 0.42

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235 17139284 17016423


    Sources:
    DrugBank

  • PYRIDOSTIGMINE BROMIDE   ACHE

    Interaction Score: 0.42

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Acetylcholinesterase inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • GALANTAMINE HYDROBROMIDE   ACHE

    Interaction Score: 0.42

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Acetylcholinesterase inhibitor

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • EPTASTIGMINE   ACHE

    Interaction Score: 0.42

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • RANITIDINE   ACHE

    Interaction Score: 0.28

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    8095733 2874096 3559884 15669026


    Sources:
    DrugBank

  • DIPIVEFRIN   ACHE

    Interaction Score: 0.28

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    8446367


    Sources:
    DrugBank

  • LADOSTIGIL   ACHE

    Interaction Score: 0.28

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • MINAPRINE   ACHE

    Interaction Score: 0.28

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    18045214 10052979


    Sources:
    DrugBank

  • CHEMBL1234276   ACHE

    Interaction Score: 0.26

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235 17139284 17016423


    Sources:
    DrugBank

  • 8-AZAGUANINE   ACHE

    Interaction Score: 0.24

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    1207869


    Sources:
    NCI

  • BETAMETHASONE   ACHE

    Interaction Score: 0.19

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    3896398


    Sources:
    NCI

  • SKIMMIANINE   ACHE

    Interaction Score: 0.17

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • METHYLENE BLUE   ACHE

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235


    Sources:
    DrugBank

  • MALATHION   ACHE

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • LATREPIRDINE   ACHE

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Novel drug target Established target
    Trial Name Dimebon

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • THIOGUANINE   ACHE

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    1207869


    Sources:
    NCI

  • METHADONE   ACHE

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    8149590


    Sources:
    NCI

  • 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:

  • GuideToPharmacology: 43

    • Version: 29-September-2020

    Alternate Names:
    108 HUGO Gene ID
    108 HUGO Gene Symbol
    acetylcholinesterase (Cartwright blood group) HUGO Gene Name

    Gene Info:
    GuideToPharmacology Gene Category Name Acetylcholine turnover
    GuideToPharmacology Gene Category ID 765
    GuideToPharmacology Gene Category Name Hydrolases

    Gene Categories:
    ENZYME

    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:
    Rosenberry TL et al., 2008, Monitoring the reaction of carbachol with acetylcholinesterase by thioflavin T fluorescence and acetylthiocholine hydrolysis., Chem Biol Interact
    Nakamura et al., 1993, Characterization of esterases involved in the hydrolysis of dipivefrin hydrochloride., Ophthalmic Res.
    Elsinghorst et al., 2007, First gallamine-tacrine hybrid: design and characterization at cholinesterases and the M2 muscarinic receptor., J. Med. 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:

  • 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:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21