Target Validation Information
TTD ID T30082
Target Name Acetylcholinesterase (AChE)
Type of Target
Successful
Drug Potency against Target Ambenonium Drug Info IC50 = 0.698 nM [61]
Edrophonium Drug Info IC50 = 5220 nM [60]
Galantamine Drug Info IC50 = 365 nM [62]
Isoflurophate Drug Info IC50 = 640 nM [65]
Malathion Drug Info IC50 = 2500 nM [63]
Neostigmine Drug Info IC50 = 36 nM [66]
Pyridostigmine Drug Info IC50 = 330 nM [64]
Tacrine Drug Info IC50 = 200 nM [64]
Drug Info IC50 = 0.78 nM [17]
Drug Info IC50 = 230 nM [1]
(-)-huperzine B Drug Info Ki = 334 nM [28]
(-)-Phenserine Drug Info IC50 = 24 nM
(-)-Tolserine Drug Info IC50 = 10.3 nM
(2-Butyryloxy-ethyl)-trimethyl-ammonium iodide Drug Info IC50 = 2.29 nM [56]
(2-Chloro-ethyl)-trimethyl-ammonium chloride Drug Info IC50 = 2.39 nM [56]
(2-Ethoxy-ethyl)-trimethyl-ammonium iodide Drug Info IC50 = 1.16 nM [56]
(2-Mercapto-ethyl)-trimethyl-ammonium iodide Drug Info IC50 = 4.4 nM [56]
(24S)-ethylcholesta-7,9(11),22(E)-triene-3b-ol Drug Info IC50 = 19200 nM [10]
(3-Bromo-propyl)-trimethyl-ammonium Drug Info IC50 = 8.79 nM [56]
(3-Hydroxy-2-methyl-phenyl)-trimethyl-ammonium Drug Info IC50 = 1.92 nM [56]
(3R)-9-amino-3-methyl-1,2,3,4-tetrahydroacridine Drug Info IC50 = 1384 nM [39]
(4-Bromo-butyl)-trimethyl-ammonium Drug Info IC50 = 5.97 nM [56]
(4-Iodo-butyl)-trimethyl-ammonium iodide Drug Info IC50 = 4.71 nM [56]
(5-Bromo-pentyl)-trimethyl-ammonium Drug Info IC50 = 5.34 nM [56]
(RS)-tacrine(10)-hupyridone Drug Info IC50 = 8.8 nM [28]
(S,S)-(-)-bis(10)-hupyridone Drug Info Ki = 0.8 nM [28]
(S,S)-(-)-bis(12)-hupyridone Drug Info Ki = 19.6 nM [28]
1,10-bis(pyridinium)-decane dibromide Drug Info IC50 = 400 nM [44]
1,11-bis(pyridinium)-undecane dibromide Drug Info Ki = 30 nM [44]
1,2-Di(berberine-9-O-yl)ethane dibromide Drug Info IC50 = 320 nM [49]
1,2-NAPHTHOQUINONE Drug Info Ki = 320 nM [22]
1,3-Bis-(3-imidazolidin-2-yl-phenyl)-urea Drug Info IC50 = 590 nM [5]
1,3-Di(berberine-9-O-yl)ethane dibromide Drug Info IC50 = 226 nM [49]
1,4-Di(berberine-9-O-yl)ethane dibromide Drug Info IC50 = 176 nM [49]
1,9-bis(pyridinium)-nonane dibromide Drug Info IC50 = 2000 nM [44]
1-(3-Bromomethyl-phenyl)-2,2,2-trifluoro-ethanone Drug Info IC50 = 360 nM [3]
1-benzene sulfonyl-cis-2,6-dimethyl piperidine Drug Info IC50 = 388 nM [36]
10-Hydroxy-infractopicrin Drug Info IC50 = 12700 nM [46]
2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-imine Drug Info IC50 = 13200 nM [12]
2-Hex-5-enyl-5-non-8-enyl-3,4-dihydro-2H-pyrrole Drug Info Ki = 13000 nM
2-Hex-5-enyl-5-non-8-enyl-pyrrolidine Drug Info Ki = 2500 nM
2-Hex-5-enyl-5-nonyl-pyrrolidine Drug Info Ki = 1500 nM
2-morpholino-N-phenethylpyrimidin-4-amine Drug Info IC50 = 4800 nM [50]
2-Propyl-beta-carboline-2-ium iodide Drug Info IC50 = 845 nM [48]
24-ethyl-cholest-7-ene-3,5,6-triol Drug Info Ki = 12600 nM [10]
24-ethylcholest-6-ene-3,5-diol Drug Info Ki = 4000 nM [10]
3,4,5,6-Tetrachloro-[1,2]benzoquinone Drug Info Ki = 1670 nM [9]
3-(2,5-Dioxo-pyrrolidin-1-yl)-benzoic acid Drug Info IC50 = 33.4 nM [4]
3-(2-Diethylamino-acetamino)-rutaecarpine Drug Info IC50 = 372.3 nM [41]
3-(2-Diethylamino-propionamino)-rutaecarpine Drug Info IC50 = 80.2 nM [41]
3-(2-N-Piperidyl-acetamino)-rutaecarpine Drug Info IC50 = 111.4 nM [41]
3-(2-N-Piperidyl-propionamino)-rutaecarpine Drug Info IC50 = 21.4 nM [41]
3-(2-N-Pyrrolyl-acetamino)-rutaecarpine Drug Info IC50 = 131.2 nM [41]
3-(2-N-Pyrrolyl-propionamino)-rutaecarpine Drug Info IC50 = 29.24 nM [41]
3-(3-Carboxy-propionylamino)-benzoic acid Drug Info IC50 = 92.5 nM [4]
3-(4-Benzoylpiperazine-1-carbonyl)coumarin Drug Info IC50 = 15000 nM [31]
3-(4-o-Tolylpiperazine-1-carbonyl)coumarin Drug Info IC50 = 6700 nM [31]
3-(4-Phenylpiperazin-1-carbonyl)coumarin Drug Info IC50 = 9300 nM [31]
3-(dimethylamino)phenyl phenylcarbamate Drug Info IC50 = 2500 nM
3-hydroxy-N,N,N-trimethylbenzenaminium iodide Drug Info IC50 = 12000 nM [30]
3-[2-(1-Benzyl-piperidin-4-yl)-ethyl]-1H-indazole Drug Info IC50 = 120 nM [6]
3-[3-(benzylmethylamino)propoxy]xanthen-9-one Drug Info IC50 = 2680 nM [15]
3-[4-(benzylmethylamino)butoxy]xanthen-9-one Drug Info IC50 = 6250 nM [15]
3-[5-(benzylmethylamino)pentyloxy]xanthen-9-one Drug Info IC50 = 7780 nM [15]
3-[6-(benzylmethylamino)hexyloxy]xanthen-9-one Drug Info IC50 = 2890 nM [15]
3-[7-(benzylmethylamino)-heptyloxy]xanthen-9-one Drug Info IC50 = 2820 nM [15]
3-[8-(benzylmethylamino)octyloxy]xanthen-9-one Drug Info IC50 = 10300 nM [15]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [51]
4-formylphenyl-O-beta-D-ribopyranoside Drug Info Ki = 510 nM [19]
4-formylphenyl-O-beta-Dglucopyranoside Drug Info Ki = 730 nM [19]
4-ISOPROPYLPHENSERINE Drug Info IC50 = 8400 nM [43]
4-[4-(benzhydryloxy)piperidino]butyl benzoate Drug Info IC50 = 1310 nM [20]
4ALPHA-(HYDROXYMETHYL)-4ALPHA-DEMETHYLTERRITREM B Drug Info IC50 = 0.423 nM [57]
5,6-dinitroacenaphthoquinone Drug Info Ki = 903 nM [22]
5-Chloro-1,2,3,4-tetrahydro-acridin-9-ylamine Drug Info IC50 = 36 nM
5-Hex-5-enyl-2-nonyl-3,4-dihydro-2H-pyrrole Drug Info Ki = 5000 nM
6,8-Dichloro-1,2,3,4-tetrahydro-acridin-9-ylamine Drug Info Ki = 1 nM [2]
6-chlorotacrine hydrochloride Drug Info IC50 = 5.73 nM [37]
6-hydroxy-1,2,9-trimethyl-9H-beta-carbolin-2-ium Drug Info IC50 = 1900 nM [13]
6-hydroxy-1,2-dimethyl-9H-beta-carbolin-2-ium Drug Info IC50 = 1000 nM [13]
6-hydroxy-2,9-dimethyl-9H-beta-carbolin-2-ium Drug Info IC50 = 1800 nM [13]
6-hydroxy-2-methyl-9H-beta-carbolin-2-ium Drug Info IC50 = 4200 nM [13]
6-methoxy-1,2-dimethyl-9H-beta-carbolin-2-ium Drug Info IC50 = 800 nM [13]
6-methoxy-1,9-dimethyl-9H-pyrido[3,4-b]indole Drug Info IC50 = 11800 nM [13]
6-methoxy-2,9-dimethyl-9H-beta-carbolin-2-ium Drug Info IC50 = 1300 nM [13]
6-methoxy-2-methyl-9H-beta-carbolin-2-ium Drug Info IC50 = 2200 nM [13]
6-Methyl-4-(4-benzoylpiperazin-1-yl)coumarin Drug Info IC50 = 7400 nM [31]
6-Methyl-4-(4-o-tolylpiperazin-1-yl)coumarin Drug Info IC50 = 7900 nM [31]
6-Methyl-4-(4-phenylpiperazin-1-yl)coumarin Drug Info IC50 = 4500 nM [31]
7-Chloro-1,2,3,4-tetrahydro-acridin-9-ylamine Drug Info IC50 = 40 nM
7-methoxytacrine Drug Info IC50 = 15000 nM [53]
7-Oxo-7H-dibenzo[de,g]quinoline Drug Info Ki = 14580 nM [34]
8-Chloro-1,2,3,4-tetrahydro-acridin-9-ylamine Drug Info IC50 = 4.43 nM
9-Amino-1,2,3,4-tetrahydro-acridine-1,7-diol Drug Info IC50 = 10600 nM
9-amino-7H-dibenzo[de,h]quinolin-7-one Drug Info Ki = 3860 nM [34]
9-Ethyl-2-methyl-beta-carboline-2-ium iodide Drug Info IC50 = 2567 nM [48]
9-hydrazino-1,2,3,4-tetrahydroacridine Drug Info IC50 = 13000 nM [16]
9-O-[2-(Phenylol-1-yloxy)ethyl]berberine bromide Drug Info IC50 = 224 nM [40]
9-O-[2-(Phenylol-1-yloxy)hexyl]berberine bromide Drug Info IC50 = 520 nM [40]
9-O-[3-(2-Pyridinoxyl)butyl]-berberine bromide Drug Info IC50 = 340 nM [49]
9-O-[3-(4-Bromo-phenoxyl)butyl]-berberine bromide Drug Info IC50 = 743 nM [49]
9-O-[3-(4-Nitro-phenoxyl)butyl]-berberine bromide Drug Info IC50 = 490 nM [49]
9-O-[3-(Phenylamino)propyl]-berberine bromide Drug Info IC50 = 138 nM [49]
9-O-[3-(Phenylol-1-yloxy)propyl]berberine bromide Drug Info IC50 = 123 nM [40]
9-O-[4-(Phenylol-1-yloxy)butyl]berberine bromide Drug Info Ki = 45 nM [40]
9-O-[5-(Phenylol-1-yloxy)pentyl]berberine bromide Drug Info IC50 = 398 nM [40]
Allyl-trimethyl-ammonium Drug Info IC50 = 2.92 nM [56]
AP-2238 Drug Info IC50 = 44 nM [45]
AP-2243 Drug Info IC50 = 18 nM [23]
BENZOQUINONE Drug Info Ki = 955 nM [9]
BIS(12)-HUPERZINE B Drug Info IC50 = 76.2 nM [8]
BIS(16)-HUPERZINE B Drug Info IC50 = 18.5 nM [8]
BIS(18)-HUPERZINE B Drug Info IC50 = 4.93 nM [8]
BIS(20)-HUPERZINE B Drug Info IC50 = 25.2 nM [8]
BIS(8)-HUPERZINE B Drug Info IC50 = 1020 nM [8]
BIS(9)-HUPERZINE B Drug Info IC50 = 471 nM [8]
Bis-7-tacrine Drug Info IC50 = 1.8 nM [50]
But-3-enyl-trimethyl-ammonium bromide Drug Info IC50 = 8.48 nM [56]
CAPROCTAMINE Drug Info IC50 = 170 nM [33]
Carinatumins B (2) Drug Info IC50 = 7000 nM [18]
CHF-2819 Drug Info IC50 = 5120 nM [11]
CHLORANIL Drug Info Ki = 163 nM [9]
Chlorphrifos oxon Drug Info IC50 = 63 nM [27]
CHOLINE IODIDE Drug Info IC50 = 3.01 nM [56]
Cis-2,6-dimethyl-1-methyl sulfonyl piperidine Drug Info IC50 = 90 nM [36]
CLEBOPRIDE Drug Info IC50 = 890 nM [5]
CORONARIDINE Drug Info IC50 = 8600 nM [54]
CRYPTADINE B Drug Info IC50 = 18500 nM [21]
DECIDIUM Drug Info Ki = 21.3 nM [28]
Dimethyl-pent-4-enyl-ammonium bromide Drug Info IC50 = 1.13 nM [56]
Eptastigmine Drug Info IC50 = 22 nM [52]
Ethyl octylfluorophosphonate Drug Info IC50 = 120 nM [27]
ETHYLPHENSERINE Drug Info IC50 = 10 nM [52]
Galanthamine derivative Drug Info IC50 = 4 nM [28]
GANSTIGMINE Drug Info IC50 = 5120 nM [28]
GENESERINE Drug Info IC50 = 1740 nM [11]
HALOXYSTEROL A Drug Info Ki = 7600 nM [10]
HALOXYSTEROL B Drug Info Ki = 850 nM [10]
Haloxysterol C Drug Info Ki = 1100 nM [10]
Haloxysterol D Drug Info Ki = 17000 nM [10]
Hexyl-trimethyl-ammonium Drug Info IC50 = 8.16 nM [56]
HP-290 Drug Info IC50 = 148 nM [52]
Huprine X Drug Info Ki = 0.13 nM [28]
Huprine Y Drug Info IC50 = 1.84 nM [35]
Icopezil maleate Drug Info IC50 = 0.33 nM [6]
Infractopicrin Drug Info IC50 = 9720 nM [46]
Iso-OMPA Drug Info IC50 = 2500 nM [32]
Isopropyl dodecylfluorophosphonate Drug Info IC50 = 6300 nM [27]
Isosorbide-2-(methylcarbamate)-5-mononitrate Drug Info IC50 = 17200 nM [32]
Isosorbide-di-(4-nitrophenyl carbamate) Drug Info IC50 = 5400 nM [42]
Isosorbide-di-(ethylcarbamate) Drug Info IC50 = 6500 nM [42]
LAWSARITOL Drug Info Ki = 16100 nM [10]
LIPOCRINE Drug Info IC50 = 0.253 nM [38]
LYSICAMINE Drug Info IC50 = 16100 nM
MEMOQUIN Drug Info IC50 = 1.5 nM [38]
MESUAGENIN A Drug Info IC50 = 1060 nM [55]
MESUAGENIN B Drug Info IC50 = 700 nM [55]
Mesuagenin D Drug Info IC50 = 8730 nM [55]
N,N'-(1',10'-decylene)-bis-(-)-nor-MEP Drug Info IC50 = 9.5 nM [25]
N,N'-(1',11'-undecydene)-bis-(-)-nor-MEP Drug Info IC50 = 24 nM [25]
N,N'-(1',12'-dodecydene)-bis-(-)-nor-MEP Drug Info IC50 = 42 nM [25]
N,N'-(1',5'-pentylene)-bis-(-)-nor-MEP Drug Info IC50 = 1000 nM [25]
N,N'-(1',6-hexylene)-bis-(-)-nor-MEP Drug Info IC50 = 1220 nM [25]
N,N'-(1',7'-heptylene)-bis-(-)-nor-MEP Drug Info IC50 = 270 nM [25]
N,N'-(1',8'-octylene)-bis-(-)-nor-MEP Drug Info IC50 = 79 nM [25]
N,N'-(1',9'-nonylene)-bis-(-)-nor-MEP Drug Info IC50 = 3.9 nM [25]
N-(14-methylallyl)norgalanthamine Drug Info IC50 = 160 nM [26]
N-ALLYLNORGALANTHAMINE Drug Info IC50 = 180 nM [26]
N-allylnorlitebamine Drug Info IC50 = 15800 nM [58]
N-benzyl-2-(pyrrolidin-1-yl)pyrimidin-4-amine Drug Info IC50 = 9800 nM [50]
N-benzyl-2-morpholinopyrimidin-4-amine Drug Info IC50 = 500 nM [50]
N-benzyl-2-thiomorpholinopyrimidin-4-amine Drug Info IC50 = 330 nM [50]
N-benzylnorlitebamine Drug Info IC50 = 10670 nM [58]
N-butylnorlitebamine Drug Info IC50 = 7790 nM [58]
N-isobutylnorlitebamine Drug Info IC50 = 6510 nM [58]
N-isopropylnorlitebamine Drug Info IC50 = 6800 nM [58]
N-isopropylnorlitebamineN-methoiodide Drug Info IC50 = 2790 nM [58]
N-Methyl-1'H-phenothiazine-1'-carboxamide Drug Info Ki = 9360 nM [47]
N-n-dodecyl-7-methoxytacrine hydrochloride Drug Info IC50 = 1000 nM [53]
N-n-heptyl-7-methoxytacrine hydrochloride Drug Info IC50 = 270 nM [53]
N-n-hexyl-7-methoxytacrine hydrochloride Drug Info IC50 = 100 nM [53]
N-n-nonyl-7-methoxytacrine hydrochloride Drug Info IC50 = 1600 nM [53]
N-n-octyl-7-methoxytacrine hydrochloride Drug Info IC50 = 360 nM [53]
N-n-pentyl-7-methoxytacrine hydrochloride Drug Info IC50 = 6700 nM [53]
N-n-propyl-7-methoxytacrine hydrochloride Drug Info IC50 = 9200 nM [53]
N-phenethyl-2-(pyrrolidin-1-yl)pyrimidin-4-amine Drug Info IC50 = 12000 nM [50]
N-propylnorlitebamine Drug Info IC50 = 7210 nM [58]
NSC-23180 Drug Info Ki = 850 nM [22]
PARAOXON Drug Info IC50 = 13 nM [27]
Petrosamine Drug Info IC50 = 91 nM [29]
Pseudocolumbamine trifluoroacetate Drug Info IC50 = 5000 nM
Pseudopalmatine trifluoroacetate Drug Info IC50 = 1800 nM
TASPINE Drug Info IC50 = 330 nM [14]
THIOCTIC ACID Drug Info IC50 = 1 nM [24]
TOLSERINE Drug Info IC50 = 40 nM [52]
Trimethyl-(3-nitro-phenyl)-ammonium iodide Drug Info IC50 = 6.28 nM [56]
Trimethyl-(4-oxo-pentyl)-ammonium iodide Drug Info IC50 = 8.48 nM [56]
TURBINATINE Drug Info IC50 = 1860 nM [7]
VELNACRINE Drug Info IC50 = 1300 nM
Voacangine Drug Info IC50 = 4400 nM [54]
XANTHOSTIGMINE Drug Info IC50 = 20 nM [59]
References
REF 1 Potent acetylcholinesterase inhibitors: design, synthesis and structure-activity relationships of alkylene linked bis-galanthamine and galanthamine... Bioorg Med Chem Lett. 2000 Apr 3;10(7):637-9.
REF 2 Novel and potent tacrine-related hetero- and homobivalent ligands for acetylcholinesterase and butyrylcholinesterase. Bioorg Med Chem Lett. 2001 Jul 9;11(13):1779-82.
REF 3 A structure-based design approach to the development of novel, reversible AChE inhibitors. J Med Chem. 2001 Sep 27;44(20):3203-15.
REF 4 Synthesis, anticholinesterase activity and structure-activity relationships of m-Aminobenzoic acid derivatives. Bioorg Med Chem Lett. 2003 May 19;13(10):1825-7.
REF 5 Efficient method for high-throughput virtual screening based on flexible docking: discovery of novel acetylcholinesterase inhibitors. J Med Chem. 2004 Sep 23;47(20):4818-28.
REF 6 A docking score function for estimating ligand-protein interactions: application to acetylcholinesterase inhibition. J Med Chem. 2004 Oct 21;47(22):5492-500.
REF 7 Indole glucoalkaloids from Chimarrhis turbinata and their evaluation as antioxidant agents and acetylcholinesterase inhibitors. J Nat Prod. 2004 Nov;67(11):1882-5.
REF 8 Bis-huperzine B: highly potent and selective acetylcholinesterase inhibitors. J Med Chem. 2005 Feb 10;48(3):655-7.
REF 9 Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases. J Med Chem. 2005 Apr 21;48(8):2906-15.
REF 10 Isolation and cholinesterase-inhibition studies of sterols from Haloxylon recurvum. Bioorg Med Chem Lett. 2006 Feb;16(3):573-80.
REF 11 Structural determinants of Torpedo californica acetylcholinesterase inhibition by the novel and orally active carbamate based anti-alzheimer drug g... J Med Chem. 2006 Aug 24;49(17):5051-8.
REF 12 Homobivalent quinazolinimines as novel nanomolar inhibitors of cholinesterases with dirigible selectivity toward butyrylcholinesterase. J Med Chem. 2006 Sep 7;49(18):5411-3.
REF 13 6-Hydroxy- and 6-methoxy-beta-carbolines as acetyl- and butyrylcholinesterase inhibitors. Bioorg Med Chem Lett. 2006 Nov 15;16(22):5840-3.
REF 14 Taspine: bioactivity-guided isolation and molecular ligand-target insight of a potent acetylcholinesterase inhibitor from Magnolia x soulangiana. J Nat Prod. 2006 Sep;69(9):1341-6.
REF 15 Cholinesterase inhibitors: SAR and enzyme inhibitory activity of 3-[omega-(benzylmethylamino)alkoxy]xanthen-9-ones. Bioorg Med Chem. 2007 Jan 1;15(1):575-85.
REF 16 Novel heterobivalent tacrine derivatives as cholinesterase inhibitors with notable selectivity toward butyrylcholinesterase. J Med Chem. 2006 Dec 14;49(25):7540-4.
REF 17 Binding of 13-amidohuprines to acetylcholinesterase: exploring the ligand-induced conformational change of the gly117-gly118 peptide bond in the ox... J Med Chem. 2006 Nov 16;49(23):6833-40.
REF 18 Carinatumins A-C, new alkaloids from Lycopodium carinatum inhibiting acetylcholinesterase. Bioorg Med Chem. 2007 Feb 15;15(4):1703-7.
REF 19 Synthesis and biological evaluation of helicid analogues as novel acetylcholinesterase inhibitors. Eur J Med Chem. 2008 Jan;43(1):166-73.
REF 20 Synthesis, in vitro assay, and molecular modeling of new piperidine derivatives having dual inhibitory potency against acetylcholinesterase and Abe... Bioorg Med Chem. 2007 Oct 15;15(20):6596-607.
REF 21 Cryptadines A and B, novel C27N3-type pentacyclic alkaloids from Lycopodium cryptomerinum. Bioorg Med Chem. 2007 Dec 15;15(24):7803-8.
REF 22 Planarity and constraint of the carbonyl groups in 1,2-diones are determinants for selective inhibition of human carboxylesterase 1. J Med Chem. 2007 Nov 15;50(23):5727-34.
REF 23 Multi-target-directed coumarin derivatives: hAChE and BACE1 inhibitors as potential anti-Alzheimer compounds. Bioorg Med Chem Lett. 2008 Jan 1;18(1):423-6.
REF 24 Multi-target-directed ligands to combat neurodegenerative diseases. J Med Chem. 2008 Feb 14;51(3):347-72.
REF 25 Bis-(-)-nor-meptazinols as novel nanomolar cholinesterase inhibitors with high inhibitory potency on amyloid-beta aggregation. J Med Chem. 2008 Apr 10;51(7):2027-36.
REF 26 N-Alkylated galanthamine derivatives: Potent acetylcholinesterase inhibitors from Leucojum aestivum. Bioorg Med Chem Lett. 2008 Apr 1;18(7):2263-6.
REF 27 Activation of the endocannabinoid system by organophosphorus nerve agents. Nat Chem Biol. 2008 Jun;4(6):373-8.
REF 28 Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely... J Med Chem. 2008 Jun 12;51(11):3154-70.
REF 29 Petrosamine, a potent anticholinesterase pyridoacridine alkaloid from a Thai marine sponge Petrosia n. sp. Bioorg Med Chem. 2008 Jul 1;16(13):6560-7.
REF 30 Homo- and hetero-bivalent edrophonium-like ammonium salts as highly potent, dual binding site AChE inhibitors. Bioorg Med Chem. 2008 Aug 1;16(15):7450-6.
REF 31 Design, synthesis, and acetylcholinesterase inhibitory activity of novel coumarin analogues. Bioorg Med Chem. 2008 Sep 1;16(17):8011-21.
REF 32 Isosorbide-2-carbamate esters: potent and selective butyrylcholinesterase inhibitors. J Med Chem. 2008 Oct 23;51(20):6400-9.
REF 33 Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inne... J Med Chem. 2008 Nov 27;51(22):7308-12.
REF 34 Synthesis, biological evaluation and molecular modeling of oxoisoaporphine and oxoaporphine derivatives as new dual inhibitors of acetylcholinester... Eur J Med Chem. 2009 Jun;44(6):2523-32.
REF 35 Synthesis and structure-activity relationship of Huprine derivatives as human acetylcholinesterase inhibitors. Bioorg Med Chem. 2009 Jul 1;17(13):4523-36.
REF 36 Active site directed docking studies: synthesis and pharmacological evaluation of cis-2,6-dimethyl piperidine sulfonamides as inhibitors of acetylc... Eur J Med Chem. 2009 Oct;44(10):4057-62.
REF 37 Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds. J Med Chem. 2009 Sep 10;52(17):5365-79.
REF 38 Toward a rational design of multitarget-directed antioxidants: merging memoquin and lipoic acid molecular frameworks. J Med Chem. 2009 Dec 10;52(23):7883-6.
REF 39 Synthesis and AChE inhibitory activity of new chiral tetrahydroacridine analogues from terpenic cyclanones. Eur J Med Chem. 2010 Feb;45(2):526-35.
REF 40 Synthesis, biological evaluation, and molecular modeling of berberine derivatives as potent acetylcholinesterase inhibitors. Bioorg Med Chem. 2010 Feb;18(3):1244-51.
REF 41 Synthesis and evaluation of novel rutaecarpine derivatives and related alkaloids derivatives as selective acetylcholinesterase inhibitors. Eur J Med Chem. 2010 Apr;45(4):1415-23.
REF 42 Isosorbide-based cholinesterase inhibitors; replacement of 5-ester groups leading to increased stability. Bioorg Med Chem. 2010 Feb;18(3):1045-53.
REF 43 Design, synthesis, evaluation and QSAR analysis of N(1)-substituted norcymserine derivatives as selective butyrylcholinesterase inhibitors. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1718-20.
REF 44 Preparation and in vitro screening of symmetrical bispyridinium cholinesterase inhibitors bearing different connecting linkage-initial study for My... Bioorg Med Chem Lett. 2010 Mar 1;20(5):1763-6.
REF 45 Targeting Alzheimer's disease: Novel indanone hybrids bearing a pharmacophoric fragment of AP2238. Bioorg Med Chem. 2010 Mar 1;18(5):1749-60.
REF 46 Acetylcholinesterase inhibitors from the toadstool Cortinarius infractus. Bioorg Med Chem. 2010 Mar 15;18(6):2173-2177.
REF 47 Differential binding of phenothiazine urea derivatives to wild-type human cholinesterases and butyrylcholinesterase mutants. Bioorg Med Chem. 2010 Mar 15;18(6):2232-2244.
REF 48 Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents. J Med Chem. 2010 May 13;53(9):3611-7.
REF 49 Synthesis and biological evaluation of a new series of berberine derivatives as dual inhibitors of acetylcholinesterase and butyrylcholinesterase. Bioorg Med Chem. 2010 Jun 15;18(12):4475-84.
REF 50 Design, synthesis and evaluation of 2,4-disubstituted pyrimidines as cholinesterase inhibitors. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3606-9.
REF 51 Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
REF 52 Novel carbamates as orally active acetylcholinesterase inhibitors found to improve scopolamine-induced cognition impairment: pharmacophore-based vi... J Med Chem. 2010 Sep 9;53(17):6490-505.
REF 53 Synthesis and in vitro evaluation of N-alkyl-7-methoxytacrine hydrochlorides as potential cholinesterase inhibitors in Alzheimer disease. Bioorg Med Chem Lett. 2010 Oct 15;20(20):6093-5.
REF 54 Indole alkaloids from Ervatamia hainanensis with potent acetylcholinesterase inhibition activities. Bioorg Med Chem Lett. 2010 Nov 1;20(21):6185-7.
REF 55 4-Phenylcoumarins from Mesua elegans with acetylcholinesterase inhibitory activity. Bioorg Med Chem. 2010 Nov 15;18(22):7873-7.
REF 56 Structure-based alignment and comparative molecular field analysis of acetylcholinesterase inhibitors. J Med Chem. 1996 Dec 20;39(26):5064-71.
REF 57 Structure and anti-acetylcholinesterase activity of 4 alpha-(hydroxymethyl)-4 alpha-demethylterritrem B. J Nat Prod. 1997 Aug;60(8):842-3.
REF 58 Litebamine N-homologues: preparation and anti-acetylcholinesterase activity. J Nat Prod. 1998 Jan;61(1):46-50.
REF 59 Acetylcholinesterase inhibitors: synthesis and structure-activity relationships of omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)- methyl]aminoalkox... J Med Chem. 1998 Oct 8;41(21):3976-86.
REF 60 Determination of inhibitors' potency (IC50) by a direct high-performance liquid chromatographic method on an immobilised acetylcholinesterase column. J Chromatogr B Biomed Sci Appl. 2001 Apr 5;753(2):375-83.
REF 61 Design, synthesis and biological evaluation of ambenonium derivatives as AChE inhibitors. Farmaco. 2003 Sep;58(9):917-28.
REF 62 Brain levels and acetylcholinesterase inhibition with galantamine and donepezil in rats, mice, and rabbits. Brain Res. 2005 Feb 8;1033(2):186-93.
REF 63 Malathion, carbofuran and paraquat inhibit Bungarus sindanus (krait) venom acetylcholinesterase and human serum butyrylcholinesterase in vitro. Ecotoxicology. 2007 May;16(4):363-9.
REF 64 Pretreatment for acute exposure to diisopropylfluorophosphate: in vivo efficacy of various acetylcholinesterase inhibitors. J Appl Toxicol. 2011 Aug;31(6):515-23.
REF 65 The role of non-critical binding proteins in the sensitivity of acetylcholinesterase from different species to diisopropyl fluorophosphate (DFP), in vitro. Life Sci. 1982 Jul 12;31(2):139-49.
REF 66 Inhibitory effects of KW-5092, a novel gastroprokinetic agent, on the activity of acetylcholinesterase in guinea pig ileum. Jpn J Pharmacol. 1994 Dec;66(4):397-403.

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