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
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

(9 More Sources)

Gene Categories: Category Details

CELL SURFACE
DRUGGABLE GENOME
ENZYME

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
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.
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.
Ciesielski-Treska et al., 1975, Morphological, histochemical and chromosomal patterns of neuroblastoma parental and purine resistant lines., Neurobiology
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
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
Kari et al., 1985, Effects of the synthetic glucocorticoid betamethasone on the survival of neurons in fetal rabbit brain cell culture., Brain 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.

EDROPHONIUM ACHE

Interaction Score: 17.11

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:
10363282 10421446 10433700 19472276 10103097 11752352 10089512

Sources:
TdgClinicalTrial TEND GuideToPharmacology TTD
NEOSTIGMINE ACHE

Interaction Score: 17.11

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:
19257799 11313435 11752352 12522088 11819669 12726885 10826417

Sources:
TdgClinicalTrial TEND GuideToPharmacology TTD
AMBENONIUM ACHE

Interaction Score: 15.56

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
1588924 5833399 13679187 2857786 11330337 11752352 15982786

Sources:
TdgClinicalTrial TEND TTD
PRALIDOXIME ACHE

Interaction Score: 12.45

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 14529460 19519385 10801325 21438612 22206546

Sources:
DTC GuideToPharmacology
RIVASTIGMINE ACHE

Interaction Score: 7.39

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cholinesterases; ACHE & BCHE inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

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

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB TTD
GALANTAMINE ACHE

Interaction Score: 6.22

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

Sources:
DTC TdgClinicalTrial TEND GuideToPharmacology TTD
ISOFLUROPHATE ACHE

Interaction Score: 6.22

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase inhibitor

Direct Interaction yes

PMIDs:
1692236 11752352 11350858 10378121 10898598 12837382

Sources:
ChemblInteractions TTD
TACRINE ACHE

Interaction Score: 4.67

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Specific Action of the Ligand Inhibition

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

Sources:
DTC TdgClinicalTrial TEND GuideToPharmacology TTD
PHYSOSTIGMINE ACHE

Interaction Score: 3.5

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name physostigmine ,Xalieve

Specific Action of the Ligand Inhibition

PMIDs:
10873710 10368402 10403635 10741458 11141093 11752352

Sources:
TdgClinicalTrial TEND GuideToPharmacology
DONEPEZIL ACHE

Interaction Score: 3.33

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

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

Sources:
DTC TdgClinicalTrial TEND GuideToPharmacology TTD
GALACTITOL ACHE

Interaction Score: 3.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11098845

Sources:
NCI
DESOXYCORDIFOLINE ACHE

Interaction Score: 3.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15568781

Sources:
DTC
ECHOTHIOPHATE ACHE

Interaction Score: 3.11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology
TURBINATINE ACHE

Interaction Score: 3.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15568781

Sources:
DTC
PYRIDOSTIGMINE ACHE

Interaction Score: 2.22

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
10669805 10869589 10366222 11752352 10685600 10814558

Sources:
TdgClinicalTrial TEND GuideToPharmacology TTD
DONEPEZIL HYDROCHLORIDE ACHE

Interaction Score: 1.56

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
AMOCARZINE ACHE

Interaction Score: 1.56

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
DEMECARIUM BROMIDE ACHE

Interaction Score: 1.56

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
EDROPHONIUM CHLORIDE ACHE

Interaction Score: 1.56

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Acetylcholinesterase inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
AMBENONIUM CHLORIDE ACHE

Interaction Score: 1.56

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: 1.56

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: 1.56

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: 1.56

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Acetylcholinesterase inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
ACOTIAMIDE ACHE

Interaction Score: 1.56

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
PHENSERINE ACHE

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name Phenserine

PMIDs:
16248851 17594192

Sources:
TdgClinicalTrial
6-AMINONICOTINAMIDE ACHE

Interaction Score: 1.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
153476

Sources:
NCI
ITOPRIDE ACHE

Interaction Score: 1.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name itopride,Itax

Novel drug target Established target

PMIDs:
17300287

Sources:
TdgClinicalTrial
NEOSTIGMINE METHYLSULFATE ACHE

Interaction Score: 0.78

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: 0.78

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: 0.78

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cholinesterases; ACHE & BCHE inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PYRIDOSTIGMINE BROMIDE ACHE

Interaction Score: 0.78

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: 0.78

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Acetylcholinesterase inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
EPTASTIGMINE ACHE

Interaction Score: 0.78

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
8-AZAGUANINE ACHE

Interaction Score: 0.52

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
1207869

Sources:
NCI
LADOSTIGIL ACHE

Interaction Score: 0.52

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
BETAMETHASONE ACHE

Interaction Score: 0.35

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
3896398

Sources:
NCI
SKIMMIANINE ACHE

Interaction Score: 0.31

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
MALATHION ACHE

Interaction Score: 0.31

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
LATREPIRDINE ACHE

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name Dimebon

PMIDs:
None found

Sources:
TdgClinicalTrial
THIOGUANINE ACHE

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
1207869

Sources:
NCI
METHADONE ACHE

Interaction Score: 0.11

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

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: 01-May-2021
Alternate Names:

Gene Info:

Gene Categories:

CELL SURFACE

Publications:

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

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

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

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

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

Mechanism of Interaction	Acetylcholinesterase inhibitor
Direct Interaction	yes

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

Mechanism of Interaction	Acetylcholinesterase activator
Direct Interaction	yes

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

activator (activating)
inhibitor (inhibitory)

antagonist (inhibitory)
inhibitor (inhibitory)

P22303	Uniprot Accession
ENSG00000087085	Ensembl Gene Id
43	Entrez Gene Id

ACHE	Uniprot Gene Name
43	Entrez Gene Id
P22303	Uniprot Accession

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

ACHE Gene Record

ACHE 43 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

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: 10363282 10421446 10433700 19472276 10103097 11752352 10089512

Sources: TdgClinicalTrial TEND GuideToPharmacology TTD

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: 19257799 11313435 11752352 12522088 11819669 12726885 10826417

Sources: TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 1588924 5833399 13679187 2857786 11330337 11752352 15982786

Sources: TdgClinicalTrial TEND TTD

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 14529460 19519385 10801325 21438612 22206546

Sources: DTC GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

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

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

Sources: TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB TTD

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

Sources: DTC TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Acetylcholinesterase inhibitor Direct Interaction yes

PMIDs: 1692236 11752352 11350858 10378121 10898598 12837382

Sources: ChemblInteractions TTD

Interaction Types & Directionality: inhibitor (inhibitory)

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

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

Sources: DTC TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 10873710 10368402 10403635 10741458 11141093 11752352

Sources: TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

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

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

Sources: DTC TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 11098845

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15568781

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15568781

Sources: DTC

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

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

PMIDs: 10669805 10869589 10366222 11752352 10685600 10814558

Sources: TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Acetylcholinesterase inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Acetylcholinesterase inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Acetylcholinesterase inhibitor

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:
10363282 10421446 10433700 19472276 10103097 11752352 10089512

Sources:
TdgClinicalTrial TEND GuideToPharmacology TTD

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:
19257799 11313435 11752352 12522088 11819669 12726885 10826417

Sources:
TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
1588924 5833399 13679187 2857786 11330337 11752352 15982786

Sources:
TdgClinicalTrial TEND TTD

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 14529460 19519385 10801325 21438612 22206546

Sources:
DTC GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cholinesterases; ACHE & BCHE inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

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

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB TTD

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

Sources:
DTC TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase inhibitor

Direct Interaction yes

PMIDs:
1692236 11752352 11350858 10378121 10898598 12837382

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Specific Action of the Ligand Inhibition

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

Sources:
DTC TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name physostigmine ,Xalieve

Specific Action of the Ligand Inhibition

PMIDs:
10873710 10368402 10403635 10741458 11141093 11752352

Sources:
TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

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

Sources:
DTC TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality:

n/a

PMIDs:
11098845

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
15568781

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
15568781

Sources:
DTC

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
10669805 10869589 10366222 11752352 10685600 10814558

Sources:
TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Acetylcholinesterase inhibitor

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Acetylcholinesterase inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions