Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T30082
(Former ID: TTDS00140)
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| Target Name |
Acetylcholinesterase (AChE)
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| Synonyms |
YT; N-ACHE; ARACHE
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| Gene Name |
ACHE
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| Target Type |
Successful target
|
[1] | ||||
| Disease | [+] 6 Target-related Diseases | + | ||||
| 1 | Alzheimer disease [ICD-11: 8A20] | |||||
| 2 | Glaucoma [ICD-11: 9C61] | |||||
| 3 | Myasthenia gravis [ICD-11: 8C6Y] | |||||
| 4 | Oesophageal/gastroduodenal disorder [ICD-11: DD90] | |||||
| 5 | Pediculosis [ICD-11: 1G00] | |||||
| 6 | Unspecific substance harmful effect [ICD-11: NE6Z] | |||||
| Function |
Role in neuronal apoptosis. Terminates signal transduction at the neuromuscular junction by rapid hydrolysis of the acetylcholine released into the synaptic cleft.
Click to Show/Hide
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| BioChemical Class |
Carboxylic ester hydrolase
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| UniProt ID | ||||||
| EC Number |
EC 3.1.1.7
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| Sequence |
MRPPQCLLHTPSLASPLLLLLLWLLGGGVGAEGREDAELLVTVRGGRLRGIRLKTPGGPV
SAFLGIPFAEPPMGPRRFLPPEPKQPWSGVVDATTFQSVCYQYVDTLYPGFEGTEMWNPN RELSEDCLYLNVWTPYPRPTSPTPVLVWIYGGGFYSGASSLDVYDGRFLVQAERTVLVSM NYRVGAFGFLALPGSREAPGNVGLLDQRLALQWVQENVAAFGGDPTSVTLFGESAGAASV GMHLLSPPSRGLFHRAVLQSGAPNGPWATVGMGEARRRATQLAHLVGCPPGGTGGNDTEL VACLRTRPAQVLVNHEWHVLPQESVFRFSFVPVVDGDFLSDTPEALINAGDFHGLQVLVG VVKDEGSYFLVYGAPGFSKDNESLISRAEFLAGVRVGVPQVSDLAAEAVVLHYTDWLHPE DPARLREALSDVVGDHNVVCPVAQLAGRLAAQGARVYAYVFEHRASTLSWPLWMGVPHGY EIEFIFGIPLDPSRNYTAEEKIFAQRLMRYWANFARTGDPNEPRDPKAPQWPPYTAGAQQ YVSLDLRPLEVRRGLRAQACAFWNRFLPKLLSATDTLDEAERQWKAEFHRWSSYMVHWKN QFDHYSKQDRCSDL Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| ADReCS ID | BADD_A02356 ; BADD_A02979 | |||||
| HIT2.0 ID | T83YZD | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 15 Approved Drugs | + | ||||
| 1 | Ambenonium | Drug Info | Approved | Myasthenia gravis | [2] | |
| 2 | Demecarium bromide | Drug Info | Approved | Open-angle glaucoma | [3], [4] | |
| 3 | Donepezil | Drug Info | Approved | Alzheimer disease | [4], [5], [6] | |
| 4 | Echothiophate Iodide | Drug Info | Approved | Chronic glaucoma | [7] | |
| 5 | Edrophonium | Drug Info | Approved | Myasthenia gravis | [8] | |
| 6 | Galantamine | Drug Info | Approved | Alzheimer disease | [9], [10] | |
| 7 | Huperzine A | Drug Info | Approved | Alzheimer disease | [4], [11] | |
| 8 | Isoflurophate | Drug Info | Approved | Glaucoma/ocular hypertension | [12] | |
| 9 | Malathion | Drug Info | Approved | Pediculus capitis infestation | [13] | |
| 10 | Neostigmine | Drug Info | Approved | Myasthenia gravis | [14] | |
| 11 | Pralidoxime Chloride | Drug Info | Approved | Poisoning due to pesticides and chemicals | [4] | |
| 12 | Pyridostigmine | Drug Info | Approved | Myasthenia gravis | [15] | |
| 13 | Rivastigmine | Drug Info | Approved | Alzheimer disease | [16], [17] | |
| 14 | Tacrine | Drug Info | Approved | Alzheimer disease | [18], [19] | |
| 15 | YM443 | Drug Info | Approved | Functional dyspepsia | [4] | |
| Clinical Trial Drug(s) | [+] 16 Clinical Trial Drugs | + | ||||
| 1 | (-)-Phenserine | Drug Info | Phase 3 | Alzheimer disease | [20] | |
| 2 | Amocarzine | Drug Info | Phase 3 | Helminth infection | [21] | |
| 3 | Eptastigmine | Drug Info | Phase 3 | Cognitive impairment | [22] | |
| 4 | INM-176 | Drug Info | Phase 3 | Alzheimer disease | [23] | |
| 5 | Suronacrine maleate | Drug Info | Phase 3 | Cognitive impairment | [24] | |
| 6 | Ladostigil | Drug Info | Phase 2 | Alzheimer disease | [25] | |
| 7 | Methanesulfonyl fluoride | Drug Info | Phase 2 | Alzheimer disease | [26] | |
| 8 | R-phenserine | Drug Info | Phase 2 | Cognitive impairment | [27] | |
| 9 | T-82 | Drug Info | Phase 2 | Cognitive impairment | [28] | |
| 10 | CPC-212 | Drug Info | Phase 1 | Alzheimer disease | [29], [30] | |
| 11 | CPC-250 | Drug Info | Phase 1 | Alzheimer disease | [29], [30] | |
| 12 | Desoxypeganine | Drug Info | Phase 1 | Alcohol dependence | [31] | |
| 13 | GTP-004 | Drug Info | Phase 1 | Myasthenia gravis | [29] | |
| 14 | KW-5092 | Drug Info | Phase 1 | Pain | [32] | |
| 15 | PRX-105 | Drug Info | Phase 1 | Poison intoxication | [33] | |
| 16 | ZT-1 | Drug Info | Phase 1 | Parkinson disease | [34] | |
| Discontinued Drug(s) | [+] 19 Discontinued Drugs | + | ||||
| 1 | VELNACRINE | Drug Info | Discontinued in Phase 3 | Cognitive impairment | [35] | |
| 2 | Zanapezil | Drug Info | Discontinued in Phase 3 | Alzheimer disease | [36] | |
| 3 | Caracemide | Drug Info | Discontinued in Phase 2 | Solid tumour/cancer | [37] | |
| 4 | HP-290 | Drug Info | Discontinued in Phase 2 | Parkinson disease | [38] | |
| 5 | Icopezil maleate | Drug Info | Discontinued in Phase 2 | Cognitive impairment | [39] | |
| 6 | Physostigmine | Drug Info | Discontinued in Phase 2 | Xerostomia | [40], [41] | |
| 7 | S-9977 | Drug Info | Discontinued in Phase 2 | Cognitive impairment | [42] | |
| 8 | SM-10888 | Drug Info | Discontinued in Phase 2 | Cognitive impairment | [43] | |
| 9 | TAK-802 | Drug Info | Discontinued in Phase 2 | Urinary dysfunction | [44] | |
| 10 | ZIFROSILONE | Drug Info | Discontinued in Phase 2 | Cognitive impairment | [45] | |
| 11 | NP-61 | Drug Info | Discontinued in Phase 1 | Alzheimer disease | [46] | |
| 12 | ABS-301 | Drug Info | Terminated | Alzheimer disease | [49] | |
| 13 | CI-1002 | Drug Info | Terminated | Alzheimer disease | [50] | |
| 14 | F-3796 | Drug Info | Terminated | Alzheimer disease | [51] | |
| 15 | FR-152558 | Drug Info | Terminated | Alzheimer disease | [52] | |
| 16 | MF-8615 | Drug Info | Terminated | Alzheimer disease | [53] | |
| 17 | MF268 | Drug Info | Terminated | Alzheimer disease | [54] | |
| 18 | NP-7557 | Drug Info | Terminated | Alzheimer disease | [55] | |
| 19 | Ro-46-5934 | Drug Info | Terminated | Alzheimer disease | [56] | |
| Preclinical Drug(s) | [+] 2 Preclinical Drugs | + | ||||
| 1 | PHENSERINE TARTRATE | Drug Info | Preclinical | Parkinson disease | [47] | |
| 2 | SPH-1285 | Drug Info | Preclinical | Alzheimer disease | [48] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Inhibitor | [+] 303 Inhibitor drugs | + | ||||
| 1 | Ambenonium | Drug Info | [57] | |||
| 2 | Demecarium bromide | Drug Info | [58], [59] | |||
| 3 | Edrophonium | Drug Info | [61], [62], [63] | |||
| 4 | Galantamine | Drug Info | [64], [65], [66] | |||
| 5 | Huperzine A | Drug Info | [67] | |||
| 6 | Isoflurophate | Drug Info | [68] | |||
| 7 | Malathion | Drug Info | [69] | |||
| 8 | Neostigmine | Drug Info | [61], [62] | |||
| 9 | Pyridostigmine | Drug Info | [62] | |||
| 10 | Tacrine | Drug Info | [70] | |||
| 11 | (-)-Phenserine | Drug Info | [71] | |||
| 12 | Amocarzine | Drug Info | [72] | |||
| 13 | Eptastigmine | Drug Info | [22], [73] | |||
| 14 | INM-176 | Drug Info | [74] | |||
| 15 | Ladostigil | Drug Info | [25] | |||
| 16 | Methanesulfonyl fluoride | Drug Info | [76] | |||
| 17 | R-phenserine | Drug Info | [77] | |||
| 18 | T-82 | Drug Info | [28], [4] | |||
| 19 | CPC-212 | Drug Info | [29], [30] | |||
| 20 | CPC-250 | Drug Info | [29], [30] | |||
| 21 | GTP-004 | Drug Info | [29] | |||
| 22 | KW-5092 | Drug Info | [32] | |||
| 23 | PRX-105 | Drug Info | [78] | |||
| 24 | ZT-1 | Drug Info | [79], [4] | |||
| 25 | Decyle nelycorine dibromo salt derivative 1 | Drug Info | [81] | |||
| 26 | Di-substituted piperidine derivative 2 | Drug Info | [81] | |||
| 27 | Egonol compound 1 | Drug Info | [80] | |||
| 28 | Fluorinated donepezil derivative 1 | Drug Info | [80] | |||
| 29 | Fluorinated donepezil derivative 2 | Drug Info | [80] | |||
| 30 | Galantamine analog 1 | Drug Info | [80] | |||
| 31 | Indoline derivative 1 | Drug Info | [81] | |||
| 32 | Isochroman-4-ketone derivative 1 | Drug Info | [81] | |||
| 33 | Lycorine dimer salt derivative 1 | Drug Info | [80] | |||
| 34 | PMID27967267-Compound-12 | Drug Info | [80] | |||
| 35 | PMID27967267-Compound-13 | Drug Info | [80] | |||
| 36 | PMID27967267-Compound-14 | Drug Info | [80] | |||
| 37 | PMID27967267-Compound-15 | Drug Info | [80] | |||
| 38 | PMID27967267-Compound-3 | Drug Info | [80] | |||
| 39 | PMID27967267-Compound-39 | Drug Info | [80] | |||
| 40 | PMID27967267-Compound-42 | Drug Info | [80] | |||
| 41 | PMID27967267-Compound-43 | Drug Info | [80] | |||
| 42 | PMID27967267-Compound-7 | Drug Info | [80] | |||
| 43 | PMID27967267-Compound-neostenine | Drug Info | [80] | |||
| 44 | PMID27967267-Compound-neotuberostemonine | Drug Info | [80] | |||
| 45 | PMID27967267-Compound-stenine | Drug Info | [80] | |||
| 46 | PMID29757691-Compound-10 | Drug Info | [81] | |||
| 47 | PMID29757691-Compound-2a | Drug Info | [81] | |||
| 48 | PMID29757691-Compound-2a-i | Drug Info | [81] | |||
| 49 | PMID29757691-Compound-4 | Drug Info | [81] | |||
| 50 | PMID29757691-Compound-7 | Drug Info | [81] | |||
| 51 | PMID29757691-Compound-8a | Drug Info | [81] | |||
| 52 | PMID29757691-Compound-8b | Drug Info | [81] | |||
| 53 | PMID29757691-Compound-8c | Drug Info | [81] | |||
| 54 | PMID29757691-Compound-8d | Drug Info | [81] | |||
| 55 | Quinazoline alkaloid derivative 1 | Drug Info | [81] | |||
| 56 | Tacrine heterodimer derivative 1 | Drug Info | [81] | |||
| 57 | Tacrine-caffeic acid hybrid derivative 1 | Drug Info | [80] | |||
| 58 | Tacrine-caffeic acid hybrid derivative 2 | Drug Info | [80] | |||
| 59 | Tacrine-indole hybrid derivative 1 | Drug Info | [80] | |||
| 60 | Tacrine-indole hybrid derivative 2 | Drug Info | [80] | |||
| 61 | Tacrine-indole hybrid derivative 3 | Drug Info | [80] | |||
| 62 | Tacrine-phenothiazine hybrid derivative 1 | Drug Info | [80] | |||
| 63 | Tetra-hydro-isoquinoline derivative 1 | Drug Info | [81] | |||
| 64 | Tetra-hydro-isoquinoline derivative 2 | Drug Info | [81] | |||
| 65 | Tetra-hydro-isoquinoline derivative 3 | Drug Info | [81] | |||
| 66 | Tetra-hydro-isoquinoline derivative 4 | Drug Info | [81] | |||
| 67 | VELNACRINE | Drug Info | [82] | |||
| 68 | Zanapezil | Drug Info | [83] | |||
| 69 | Caracemide | Drug Info | [84] | |||
| 70 | HP-290 | Drug Info | [85], [73] | |||
| 71 | Icopezil maleate | Drug Info | [86] | |||
| 72 | Physostigmine | Drug Info | [87] | |||
| 73 | S-9977 | Drug Info | [88] | |||
| 74 | SM-10888 | Drug Info | [89] | |||
| 75 | TAK-802 | Drug Info | [90] | |||
| 76 | ZIFROSILONE | Drug Info | [91], [4] | |||
| 77 | NP-61 | Drug Info | [92] | |||
| 78 | PHENSERINE TARTRATE | Drug Info | [77], [4] | |||
| 79 | SPH-1285 | Drug Info | [93] | |||
| 80 | 7-methoxytacrine | Drug Info | [94] | |||
| 81 | F-3796 | Drug Info | [96] | |||
| 82 | FR-152558 | Drug Info | [97] | |||
| 83 | MF-8615 | Drug Info | [98] | |||
| 84 | MF268 | Drug Info | [99] | |||
| 85 | NP-7557 | Drug Info | [100] | |||
| 86 | Ro-46-5934 | Drug Info | [56] | |||
| 87 | (-)-huperzine B | Drug Info | [101] | |||
| 88 | (-)-Tolserine | Drug Info | [71] | |||
| 89 | (1R)-1,2,2-TRIMETHYLPROPYL (S)-METHYLPHOSPHINATE | Drug Info | [99] | |||
| 90 | (2-Butyryloxy-ethyl)-trimethyl-ammonium iodide | Drug Info | [102] | |||
| 91 | (2-Chloro-ethyl)-trimethyl-ammonium chloride | Drug Info | [102] | |||
| 92 | (2-Ethoxy-ethyl)-trimethyl-ammonium iodide | Drug Info | [102] | |||
| 93 | (2-Mercapto-ethyl)-trimethyl-ammonium iodide | Drug Info | [102] | |||
| 94 | (24S)-ethylcholesta-7,9(11),22(E)-triene-3b-ol | Drug Info | [103] | |||
| 95 | (3-Bromo-propyl)-trimethyl-ammonium | Drug Info | [102] | |||
| 96 | (3-Hydroxy-2-methyl-phenyl)-trimethyl-ammonium | Drug Info | [102] | |||
| 97 | (3R)-9-amino-3-methyl-1,2,3,4-tetrahydroacridine | Drug Info | [104] | |||
| 98 | (4-Bromo-butyl)-trimethyl-ammonium | Drug Info | [102] | |||
| 99 | (4-Iodo-butyl)-trimethyl-ammonium iodide | Drug Info | [102] | |||
| 100 | (5-Bromo-pentyl)-trimethyl-ammonium | Drug Info | [102] | |||
| 101 | (R)-tacrine(10)-hupyridone | Drug Info | [99] | |||
| 102 | (RS)-tacrine(10)-hupyridone | Drug Info | [101] | |||
| 103 | (S)-tacrine(10)-hupyridone | Drug Info | [99] | |||
| 104 | (S,S)-(-)-bis(10)-hupyridone | Drug Info | [101] | |||
| 105 | (S,S)-(-)-bis(12)-hupyridone | Drug Info | [101] | |||
| 106 | 1,10-bis(pyridinium)-decane dibromide | Drug Info | [105] | |||
| 107 | 1,11-bis(pyridinium)-undecane dibromide | Drug Info | [105] | |||
| 108 | 1,2-Di(berberine-9-O-yl)ethane dibromide | Drug Info | [106] | |||
| 109 | 1,2-NAPHTHOQUINONE | Drug Info | [107] | |||
| 110 | 1,3-Bis-(3-imidazolidin-2-yl-phenyl)-urea | Drug Info | [108] | |||
| 111 | 1,3-Di(berberine-9-O-yl)ethane dibromide | Drug Info | [106] | |||
| 112 | 1,4-Di(berberine-9-O-yl)ethane dibromide | Drug Info | [106] | |||
| 113 | 1,9-bis(pyridinium)-nonane dibromide | Drug Info | [105] | |||
| 114 | 1-(3-Bromomethyl-phenyl)-2,2,2-trifluoro-ethanone | Drug Info | [109] | |||
| 115 | 1-benzene sulfonyl-cis-2,6-dimethyl piperidine | Drug Info | [110] | |||
| 116 | 1-Deoxy-1-Thio-Heptaethylene Glycol | Drug Info | [99] | |||
| 117 | 1-ETHOXY-2-(2-ETHOXYETHOXY)ETHANE | Drug Info | [99] | |||
| 118 | 10-Hydroxy-infractopicrin | Drug Info | [111] | |||
| 119 | 2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-imine | Drug Info | [112] | |||
| 120 | 2-(Acetylamino)-2-Deoxy-a-D-Glucopyranose | Drug Info | [113] | |||
| 121 | 2-(N-Morpholino)-Ethanesulfonic Acid | Drug Info | [113] | |||
| 122 | 2-Hex-5-enyl-5-non-8-enyl-3,4-dihydro-2H-pyrrole | Drug Info | [114] | |||
| 123 | 2-Hex-5-enyl-5-non-8-enyl-pyrrolidine | Drug Info | [114] | |||
| 124 | 2-Hex-5-enyl-5-nonyl-pyrrolidine | Drug Info | [114] | |||
| 125 | 2-morpholino-N-phenethylpyrimidin-4-amine | Drug Info | [115] | |||
| 126 | 2-Propyl-beta-carboline-2-ium iodide | Drug Info | [116] | |||
| 127 | 24-ethyl-cholest-7-ene-3,5,6-triol | Drug Info | [103] | |||
| 128 | 24-ethylcholest-6-ene-3,5-diol | Drug Info | [103] | |||
| 129 | 3,4,5,6-Tetrachloro-[1,2]benzoquinone | Drug Info | [117] | |||
| 130 | 3,6,9,12,15-Pentaoxaheptadecane | Drug Info | [99] | |||
| 131 | 3,7-BIS(DIMETHYLAMINO)PHENOTHIAZIN-5-IUM | Drug Info | [99] | |||
| 132 | 3-(2,5-Dioxo-pyrrolidin-1-yl)-benzoic acid | Drug Info | [118] | |||
| 133 | 3-(2-Diethylamino-acetamino)-rutaecarpine | Drug Info | [119] | |||
| 134 | 3-(2-Diethylamino-propionamino)-rutaecarpine | Drug Info | [119] | |||
| 135 | 3-(2-N-Piperidyl-acetamino)-rutaecarpine | Drug Info | [119] | |||
| 136 | 3-(2-N-Piperidyl-propionamino)-rutaecarpine | Drug Info | [119] | |||
| 137 | 3-(2-N-Pyrrolyl-acetamino)-rutaecarpine | Drug Info | [119] | |||
| 138 | 3-(2-N-Pyrrolyl-propionamino)-rutaecarpine | Drug Info | [119] | |||
| 139 | 3-(3-Carboxy-propionylamino)-benzoic acid | Drug Info | [118] | |||
| 140 | 3-(4-Benzoylpiperazine-1-carbonyl)coumarin | Drug Info | [120] | |||
| 141 | 3-(4-o-Tolylpiperazine-1-carbonyl)coumarin | Drug Info | [120] | |||
| 142 | 3-(4-Phenylpiperazin-1-carbonyl)coumarin | Drug Info | [120] | |||
| 143 | 3-(dimethylamino)phenyl phenylcarbamate | Drug Info | [71] | |||
| 144 | 3-hydroxy-N,N,N-trimethylbenzenaminium iodide | Drug Info | [121] | |||
| 145 | 3-[(1s)-1-(Dimethylamino)Ethyl]Phenol | Drug Info | [99] | |||
| 146 | 3-[2-(1-Benzyl-piperidin-4-yl)-ethyl]-1H-indazole | Drug Info | [86] | |||
| 147 | 3-[3-(benzylmethylamino)propoxy]xanthen-9-one | Drug Info | [122] | |||
| 148 | 3-[4-(benzylmethylamino)butoxy]xanthen-9-one | Drug Info | [122] | |||
| 149 | 3-[5-(benzylmethylamino)pentyloxy]xanthen-9-one | Drug Info | [122] | |||
| 150 | 3-[6-(benzylmethylamino)hexyloxy]xanthen-9-one | Drug Info | [122] | |||
| 151 | 3-[7-(benzylmethylamino)-heptyloxy]xanthen-9-one | Drug Info | [122] | |||
| 152 | 3-[8-(benzylmethylamino)octyloxy]xanthen-9-one | Drug Info | [122] | |||
| 153 | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [123] | |||
| 154 | 4-formylphenyl-O-beta-D-ribopyranoside | Drug Info | [124] | |||
| 155 | 4-formylphenyl-O-beta-Dglucopyranoside | Drug Info | [124] | |||
| 156 | 4-ISOPROPYLPHENSERINE | Drug Info | [125] | |||
| 157 | 4-[4-(benzhydryloxy)piperidino]butyl benzoate | Drug Info | [126] | |||
| 158 | 4ALPHA-(HYDROXYMETHYL)-4ALPHA-DEMETHYLTERRITREM B | Drug Info | [127] | |||
| 159 | 5,6-dinitroacenaphthoquinone | Drug Info | [107] | |||
| 160 | 5-Chloro-1,2,3,4-tetrahydro-acridin-9-ylamine | Drug Info | [128] | |||
| 161 | 5-Hex-5-enyl-2-nonyl-3,4-dihydro-2H-pyrrole | Drug Info | [114] | |||
| 162 | 6,8-Dichloro-1,2,3,4-tetrahydro-acridin-9-ylamine | Drug Info | [129] | |||
| 163 | 6-chlorotacrine hydrochloride | Drug Info | [130] | |||
| 164 | 6-hydroxy-1,2,9-trimethyl-9H-beta-carbolin-2-ium | Drug Info | [131] | |||
| 165 | 6-hydroxy-1,2-dimethyl-9H-beta-carbolin-2-ium | Drug Info | [131] | |||
| 166 | 6-hydroxy-2,9-dimethyl-9H-beta-carbolin-2-ium | Drug Info | [131] | |||
| 167 | 6-hydroxy-2-methyl-9H-beta-carbolin-2-ium | Drug Info | [131] | |||
| 168 | 6-methoxy-1,2-dimethyl-9H-beta-carbolin-2-ium | Drug Info | [131] | |||
| 169 | 6-methoxy-1,9-dimethyl-9H-pyrido[3,4-b]indole | Drug Info | [131] | |||
| 170 | 6-methoxy-2,9-dimethyl-9H-beta-carbolin-2-ium | Drug Info | [131] | |||
| 171 | 6-methoxy-2-methyl-9H-beta-carbolin-2-ium | Drug Info | [131] | |||
| 172 | 6-Methyl-4-(4-benzoylpiperazin-1-yl)coumarin | Drug Info | [120] | |||
| 173 | 6-Methyl-4-(4-o-tolylpiperazin-1-yl)coumarin | Drug Info | [120] | |||
| 174 | 6-Methyl-4-(4-phenylpiperazin-1-yl)coumarin | Drug Info | [120] | |||
| 175 | 7-Chloro-1,2,3,4-tetrahydro-acridin-9-ylamine | Drug Info | [128] | |||
| 176 | 7-Oxo-7H-dibenzo[de,g]quinoline | Drug Info | [132] | |||
| 177 | 8-Chloro-1,2,3,4-tetrahydro-acridin-9-ylamine | Drug Info | [128] | |||
| 178 | 9-Amino-1,2,3,4-tetrahydro-acridine-1,7-diol | Drug Info | [82] | |||
| 179 | 9-amino-7H-dibenzo[de,h]quinolin-7-one | Drug Info | [132] | |||
| 180 | 9-Ethyl-2-methyl-beta-carboline-2-ium iodide | Drug Info | [116] | |||
| 181 | 9-Ethyl-beta-carboline | Drug Info | [116] | |||
| 182 | 9-hydrazino-1,2,3,4-tetrahydroacridine | Drug Info | [133] | |||
| 183 | 9-O-[2-(Phenylol-1-yloxy)ethyl]berberine bromide | Drug Info | [134] | |||
| 184 | 9-O-[2-(Phenylol-1-yloxy)hexyl]berberine bromide | Drug Info | [134] | |||
| 185 | 9-O-[3-(2-Pyridinoxyl)butyl]-berberine bromide | Drug Info | [106] | |||
| 186 | 9-O-[3-(4-Bromo-phenoxyl)butyl]-berberine bromide | Drug Info | [106] | |||
| 187 | 9-O-[3-(4-Nitro-phenoxyl)butyl]-berberine bromide | Drug Info | [106] | |||
| 188 | 9-O-[3-(Phenylamino)propyl]-berberine bromide | Drug Info | [106] | |||
| 189 | 9-O-[3-(Phenylol-1-yloxy)propyl]berberine bromide | Drug Info | [134] | |||
| 190 | 9-O-[4-(Phenylol-1-yloxy)butyl]berberine bromide | Drug Info | [134] | |||
| 191 | 9-O-[5-(Phenylol-1-yloxy)pentyl]berberine bromide | Drug Info | [134] | |||
| 192 | Allyl-trimethyl-ammonium | Drug Info | [102] | |||
| 193 | AP-2238 | Drug Info | [135] | |||
| 194 | AP-2243 | Drug Info | [136] | |||
| 195 | BENZOQUINONE | Drug Info | [117] | |||
| 196 | Beta-L-fucose | Drug Info | [137] | |||
| 197 | BIS(12)-HUPERZINE B | Drug Info | [138] | |||
| 198 | Bis(14)-Huperzine B | Drug Info | [138] | |||
| 199 | BIS(16)-HUPERZINE B | Drug Info | [138] | |||
| 200 | BIS(18)-HUPERZINE B | Drug Info | [138] | |||
| 201 | BIS(20)-HUPERZINE B | Drug Info | [138] | |||
| 202 | BIS(8)-HUPERZINE B | Drug Info | [138] | |||
| 203 | BIS(9)-HUPERZINE B | Drug Info | [138] | |||
| 204 | Bis-7-tacrine | Drug Info | [115] | |||
| 205 | But-3-enyl-trimethyl-ammonium bromide | Drug Info | [102] | |||
| 206 | BW284C51 | Drug Info | [139], [140] | |||
| 207 | BZYX | Drug Info | [1] | |||
| 208 | CAPROCTAMINE | Drug Info | [141] | |||
| 209 | Carinatumins B (2) | Drug Info | [142] | |||
| 210 | CHF-2819 | Drug Info | [143] | |||
| 211 | CHLORANIL | Drug Info | [117] | |||
| 212 | Chlorphrifos oxon | Drug Info | [144] | |||
| 213 | CHLORPYRIFOS | Drug Info | [145] | |||
| 214 | CHOLINE IODIDE | Drug Info | [102] | |||
| 215 | Cis-2,6-dimethyl-1-methyl sulfonyl piperidine | Drug Info | [110] | |||
| 216 | CLEBOPRIDE | Drug Info | [108] | |||
| 217 | CORONARIDINE | Drug Info | [146] | |||
| 218 | CRYPTADINE B | Drug Info | [148] | |||
| 219 | DECIDIUM | Drug Info | [101] | |||
| 220 | Dimethyl-pent-4-enyl-ammonium bromide | Drug Info | [102] | |||
| 221 | Ethyl octylfluorophosphonate | Drug Info | [144] | |||
| 222 | ETHYLPHENSERINE | Drug Info | [73] | |||
| 223 | Fucose | Drug Info | [113] | |||
| 224 | Galanthamine derivative | Drug Info | [101] | |||
| 225 | GANSTIGMINE | Drug Info | [101] | |||
| 226 | GENESERINE | Drug Info | [143] | |||
| 227 | HALOXYSTEROL A | Drug Info | [103] | |||
| 228 | HALOXYSTEROL B | Drug Info | [103] | |||
| 229 | Haloxysterol C | Drug Info | [103] | |||
| 230 | Haloxysterol D | Drug Info | [103] | |||
| 231 | Hexyl-trimethyl-ammonium | Drug Info | [102] | |||
| 232 | Huprine X | Drug Info | [101] | |||
| 233 | Huprine Y | Drug Info | [149] | |||
| 234 | Huprine-Tacrine Heterodimer | Drug Info | [150] | |||
| 235 | Infractopicrin | Drug Info | [111] | |||
| 236 | Iso-OMPA | Drug Info | [140] | |||
| 237 | Isopropyl dodecylfluorophosphonate | Drug Info | [144] | |||
| 238 | Isosorbide-2-(methylcarbamate)-5-benzoate | Drug Info | [140] | |||
| 239 | Isosorbide-2-(methylcarbamate)-5-mononitrate | Drug Info | [140] | |||
| 240 | Isosorbide-2-benzylcarbamate-5-cyclopentanoate | Drug Info | [140] | |||
| 241 | Isosorbide-2-benzylcarbamate-5-cyclopropanoate | Drug Info | [140] | |||
| 242 | Isosorbide-2-benzylcarbamate-5-tosylate | Drug Info | [140] | |||
| 243 | Isosorbide-di-(4-nitrophenyl carbamate) | Drug Info | [151] | |||
| 244 | Isosorbide-di-(benzylcarbamate) | Drug Info | [151] | |||
| 245 | Isosorbide-di-(ethylcarbamate) | Drug Info | [151] | |||
| 246 | Isosorbide-di-phenylcarbamate | Drug Info | [151] | |||
| 247 | LAWSARITOL | Drug Info | [103] | |||
| 248 | LIPOCRINE | Drug Info | [152] | |||
| 249 | LYSICAMINE | Drug Info | [153] | |||
| 250 | MEMOQUIN | Drug Info | [152] | |||
| 251 | MESUAGENIN A | Drug Info | [154] | |||
| 252 | MESUAGENIN B | Drug Info | [154] | |||
| 253 | Mesuagenin D | Drug Info | [154] | |||
| 254 | Methyl Phosphinic Acid | Drug Info | [113] | |||
| 255 | Monoisopropylphosphorylserine | Drug Info | [113] | |||
| 256 | N,N'-(1',10'-decylene)-bis-(-)-nor-MEP | Drug Info | [155] | |||
| 257 | N,N'-(1',11'-undecydene)-bis-(-)-nor-MEP | Drug Info | [155] | |||
| 258 | N,N'-(1',12'-dodecydene)-bis-(-)-nor-MEP | Drug Info | [155] | |||
| 259 | N,N'-(1',5'-pentylene)-bis-(-)-nor-MEP | Drug Info | [155] | |||
| 260 | N,N'-(1',6-hexylene)-bis-(-)-nor-MEP | Drug Info | [155] | |||
| 261 | N,N'-(1',7'-heptylene)-bis-(-)-nor-MEP | Drug Info | [155] | |||
| 262 | N,N'-(1',8'-octylene)-bis-(-)-nor-MEP | Drug Info | [155] | |||
| 263 | N,N'-(1',9'-nonylene)-bis-(-)-nor-MEP | Drug Info | [155] | |||
| 264 | N-(14-methylallyl)norgalanthamine | Drug Info | [156] | |||
| 265 | N-ALLYLNORGALANTHAMINE | Drug Info | [156] | |||
| 266 | N-allylnorlitebamine | Drug Info | [157] | |||
| 267 | N-benzyl-2-(pyrrolidin-1-yl)pyrimidin-4-amine | Drug Info | [115] | |||
| 268 | N-benzyl-2-morpholinopyrimidin-4-amine | Drug Info | [115] | |||
| 269 | N-benzyl-2-thiomorpholinopyrimidin-4-amine | Drug Info | [115] | |||
| 270 | N-benzylnorlitebamine | Drug Info | [157] | |||
| 271 | N-butylnorlitebamine | Drug Info | [157] | |||
| 272 | N-isobutylnorlitebamine | Drug Info | [157] | |||
| 273 | N-isopropylnorlitebamine | Drug Info | [157] | |||
| 274 | N-isopropylnorlitebamineN-methoiodide | Drug Info | [157] | |||
| 275 | N-Methyl-1'H-phenothiazine-1'-carboxamide | Drug Info | [158] | |||
| 276 | N-n-dodecyl-7-methoxytacrine hydrochloride | Drug Info | [94] | |||
| 277 | N-n-heptyl-7-methoxytacrine hydrochloride | Drug Info | [94] | |||
| 278 | N-n-hexyl-7-methoxytacrine hydrochloride | Drug Info | [94] | |||
| 279 | N-n-nonyl-7-methoxytacrine hydrochloride | Drug Info | [94] | |||
| 280 | N-n-octyl-7-methoxytacrine hydrochloride | Drug Info | [94] | |||
| 281 | N-n-pentyl-7-methoxytacrine hydrochloride | Drug Info | [94] | |||
| 282 | N-n-propyl-7-methoxytacrine hydrochloride | Drug Info | [94] | |||
| 283 | N-phenethyl-2-(pyrrolidin-1-yl)pyrimidin-4-amine | Drug Info | [115] | |||
| 284 | N-propylnorlitebamine | Drug Info | [157] | |||
| 285 | NSC-23180 | Drug Info | [107] | |||
| 286 | OBIDOXIME | Drug Info | [145] | |||
| 287 | PARAOXON | Drug Info | [144] | |||
| 288 | Petrosamine | Drug Info | [159] | |||
| 289 | Propidium | Drug Info | [113] | |||
| 290 | Pseudocolumbamine trifluoroacetate | Drug Info | [153] | |||
| 291 | Pseudopalmatine trifluoroacetate | Drug Info | [153] | |||
| 292 | TACRINE(8)-4-AMINOQUINOLINE | Drug Info | [99] | |||
| 293 | TASPINE | Drug Info | [160] | |||
| 294 | TERRITREM B | Drug Info | [161] | |||
| 295 | Tetraethylene Glycol | Drug Info | [113] | |||
| 296 | THIOCTIC ACID | Drug Info | [162] | |||
| 297 | TOLSERINE | Drug Info | [73] | |||
| 298 | TRIMEDOXIME | Drug Info | [145] | |||
| 299 | Trimethyl-(3-nitro-phenyl)-ammonium iodide | Drug Info | [102] | |||
| 300 | Trimethyl-(4-oxo-pentyl)-ammonium iodide | Drug Info | [102] | |||
| 301 | TURBINATINE | Drug Info | [163] | |||
| 302 | Voacangine | Drug Info | [146] | |||
| 303 | XANTHOSTIGMINE | Drug Info | [164] | |||
| Modulator | [+] 11 Modulator drugs | + | ||||
| 1 | Donepezil | Drug Info | [1] | |||
| 2 | Echothiophate Iodide | Drug Info | [60] | |||
| 3 | Pralidoxime Chloride | Drug Info | [60] | |||
| 4 | Rivastigmine | Drug Info | [1] | |||
| 5 | YM443 | Drug Info | [4] | |||
| 6 | Suronacrine maleate | Drug Info | [75] | |||
| 7 | Desoxypeganine | Drug Info | [31] | |||
| 8 | ABS-301 | Drug Info | [95] | |||
| 9 | CI-1002 | Drug Info | [50] | |||
| 10 | CP-126998 | Drug Info | [147] | |||
| 11 | NPRx-30 | Drug Info | [1] | |||
| Reactivator | [+] 8 Reactivator drugs | + | ||||
| 1 | 2-PAM derivative 1 | Drug Info | [80] | |||
| 2 | 4-PAM derivative 1 | Drug Info | [80] | |||
| 3 | Amidine oxime derivative 1 | Drug Info | [80] | |||
| 4 | PMID27967267-Compound-47 | Drug Info | [80] | |||
| 5 | PMID27967267-Compound-48 | Drug Info | [80] | |||
| 6 | PMID27967267-Compound-49 | Drug Info | [80] | |||
| 7 | PMID27967267-Compound-51 | Drug Info | [80] | |||
| 8 | PMID27967267-Compound-52 | Drug Info | [80] | |||
| Activator | [+] 1 Activator drugs | + | ||||
| 1 | MMB-4 | Drug Info | [1] | |||
| Chemical Structure based Activity Landscape of Target | Top |
|---|---|
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
|
|
||
| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
|
|
||
| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
|
|
||
| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-regulating microRNAs | ||||||
| Target-regulating Transcription Factors | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 2 KEGG Pathways | + | ||||
| 1 | Glycerophospholipid metabolism | |||||
| 2 | Cholinergic synapse | |||||
| Panther Pathway | [+] 3 Panther Pathways | + | ||||
| 1 | Muscarinic acetylcholine receptor 1 and 3 signaling pathway | |||||
| 2 | Muscarinic acetylcholine receptor 2 and 4 signaling pathway | |||||
| 3 | Nicotinic acetylcholine receptor signaling pathway | |||||
| Pathwhiz Pathway | [+] 1 Pathwhiz Pathways | + | ||||
| 1 | Phospholipid Biosynthesis | |||||
| PID Pathway | [+] 1 PID Pathways | + | ||||
| 1 | ATF-2 transcription factor network | |||||
| WikiPathways | [+] 4 WikiPathways | + | ||||
| 1 | Monoamine Transport | |||||
| 2 | Biogenic Amine Synthesis | |||||
| 3 | Acetylcholine Synthesis | |||||
| 4 | Integrated Pancreatic Cancer Pathway | |||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| Target QSAR Model | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2465). | |||||
| REF 2 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 010155. | |||||
| REF 3 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 011860. | |||||
| REF 4 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 5 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6599). | |||||
| REF 6 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001402) | |||||
| REF 7 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 011963. | |||||
| REF 8 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040131. | |||||
| REF 9 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6693). | |||||
| REF 10 | Novel pharmacological targets for the treatment of Parkinson's disease. Nat Rev Drug Discov. 2006 Oct;5(10):845-54. | |||||
| REF 11 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000687) | |||||
| REF 12 | Anaesthetic drugs: linking molecular actions to clinical effects. Curr Pharm Des. 2006;12(28):3665-79. | |||||
| REF 13 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 078743. | |||||
| REF 14 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 15 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040457. | |||||
| REF 16 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6602). | |||||
| REF 17 | ClinicalTrials.gov (NCT00948766) Effects of Rivastigmine Patch on Activities of Daily Living and Cognition in Patients With Severe Dementia of the Alzheimer's Type (ACTION) (Study Protocol CENA713DUS44, NCT00948766) and a 24 Week Open-label Extension to Study CENA713DUS44. U.S. National Institutes of Health. | |||||
| REF 18 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6687). | |||||
| REF 19 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
| REF 20 | Neurotrophic and neuroprotective actions of (-)- and (+)-phenserine, candidate drugs for Alzheimer's disease. PLoS One. 2013;8(1):e54887. | |||||
| REF 21 | The safety and efficacy of amocarzine in African onchocerciasis and the influence of ivermectin on the clinical and parasitological response to treatment. Ann Trop Med Parasitol. 1997 Apr;91(3):281-96. | |||||
| REF 22 | Eptastigmine: ten years of pharmacology, toxicology, pharmacokinetic, and clinical studies. CNS Drug Rev. 2001 Winter;7(4):369-86. | |||||
| REF 23 | ClinicalTrials.gov (NCT01245530) An Efficacy and Safety Study of INM-176 for the Treatment of Patients With Alzheimer Type Dementia. U.S. National Institutes of Health. | |||||
| REF 24 | Handbook of Dementing Illnesses, Morris John. Page(570). | |||||
| REF 25 | Ladostigil: a novel multimodal neuroprotective drug with cholinesterase and brain-selective monoamine oxidase inhibitory activities for Alzheimer's disease treatment. Curr Drug Targets. 2012 Apr;13(4):483-94. | |||||
| REF 26 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033430) | |||||
| REF 27 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021506) | |||||
| REF 28 | Effects of T-82, a novel acetylcholinesterase inhibitor, on impaired learning and memory in passive avoidance task in rats. Eur J Pharmacol. 2003 Mar 28;465(1-2):97-103. | |||||
| REF 29 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 30 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 31 | Phase I clinical trial with desoxypeganine, a new cholinesterase and selective MAO-A inhibitor: tolerance and pharmacokinetics study of escalating single oral doses. Methods Find Exp Clin Pharmacol. 2008 Mar;30(2):141-7. | |||||
| REF 32 | Oral administration of KW-5092, a novel gastroprokinetic agent with acetylcholinesterase inhibitory and acetylcholine release enhancing activities, causes a dose-dependent increase in the blood acetylcholine content of beagle dogs. Neurosci Lett. 1997 Mar 28;225(1):25-8. | |||||
| REF 33 | ClinicalTrials.gov (NCT01093859) An Exploratory Phase 1 Microdose Study of PRX-105. U.S. National Institutes of Health. | |||||
| REF 34 | Phase I study on the pharmacokinetics and tolerance of ZT-1, a prodrug of huperzine A, for the treatment of Alzheimer's disease. Acta Pharmacol Sin. 2013 Jul;34(7):976-82. | |||||
| REF 35 | Velnacrine for Alzheimer's disease. Cochrane Database Syst Rev. 2004;(2):CD004748. | |||||
| REF 36 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004496) | |||||
| REF 37 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000740) | |||||
| REF 38 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006532) | |||||
| REF 39 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006556) | |||||
| REF 40 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6598). | |||||
| REF 41 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028816) | |||||
| REF 42 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001724) | |||||
| REF 43 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001320) | |||||
| REF 44 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020145) | |||||
| REF 45 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001855) | |||||
| REF 46 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028783) | |||||
| REF 47 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012344) | |||||
| REF 48 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015422) | |||||
| REF 49 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007119) | |||||
| REF 50 | PD 142676 (CI 1002), a novel anticholinesterase and muscarinic antagonist. Mol Neurobiol. 1994 Aug-Dec;9(1-3):93-106. | |||||
| REF 51 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004498) | |||||
| REF 52 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006757) | |||||
| REF 53 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006922) | |||||
| REF 54 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007171) | |||||
| REF 55 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017551) | |||||
| REF 56 | A novel acetylcholinesterase inhibitor, Ro 46-5934, which interacts with muscarinic M2 receptors. Biochem Soc Trans. 1994 Aug;22(3):755-8. | |||||
| REF 57 | Alpha6-containing nicotinic acetylcholine receptors dominate the nicotine control of dopamine neurotransmission in nucleus accumbens. Neuropsychopharmacology. 2008 Aug;33(9):2158-66. | |||||
| REF 58 | The effects of topical ocular application of 0.25% demecarium bromide on serum acetylcholinesterase levels in normal dogs. Vet Ophthalmol. 2003 Mar;6(1):23-5. | |||||
| REF 59 | Neuromuscular blocking agents and axial teratogenesis in the avian embryo. Can axial morphogenetic disorders by explained by pharmacological action upon muscle tissue Teratology. 1981 Apr;23(2):259-71. | |||||
| REF 60 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
| REF 61 | Screening of acetylcholinesterase inhibitors by CE after enzymatic reaction at capillary inlet. J Sep Sci. 2009 May;32(10):1748-56. | |||||
| REF 62 | Neuromuscular blockade, reversal agent use, and operating room time: retrospective analysis of US inpatient surgeries. Curr Med Res Opin. 2009 Apr;25(4):943-50. | |||||
| REF 63 | Stabilization of Torpedo californica acetylcholinesterase by reversible inhibitors. Biochemistry. 2009 Jan 27;48(3):563-74. | |||||
| REF 64 | [From symptomatic to disease modifying therapy Recent developments in the pharmacotherapy of Alzheimer's disease]. Fortschr Neurol Psychiatr. 2009 Jun;77(6):326-33. | |||||
| REF 65 | Effects of cholinesterase inhibition on brain white matter volume in Alzheimer's disease. Neuroreport. 2009 Feb 18;20(3):285-8. | |||||
| REF 66 | Acetylcholinesterase inhibitors enhance cognitive functions in rats following hypobaric hypoxia. Behav Brain Res. 2009 Oct 12;203(1):1-14. | |||||
| REF 67 | Huperzine A attenuates cognitive deficits and brain injury in neonatal rats after hypoxia-ischemia. Brain Res. 2002 Sep 13;949(1-2):162-70. | |||||
| REF 68 | Rational design of alkylene-linked bis-pyridiniumaldoximes as improved acetylcholinesterase reactivators. Chem Biol. 2003 Jun;10(6):491-502. | |||||
| REF 69 | Acetylcholinesterase activity in Corbicula fluminea Mull., as a biomarker of organophosphate pesticide pollution in Pinacanauan River, Philippines. Environ Monit Assess. 2010 Jun;165(1-4):331-40. | |||||
| REF 70 | Evidence that the clinical effects of cholinesterase inhibitors are related to potency and targeting of action. Int J Clin Pract Suppl. 2002 Jun;(127):6-19. | |||||
| REF 71 | Long-acting anticholinesterases for myasthenia gravis: synthesis and activities of quaternary phenylcarbamates of neostigmine, pyridostigmine and physostigmine. Bioorg Med Chem. 2010 Jul 1;18(13):4687-93. | |||||
| REF 72 | Activity, mechanism of action and pharmacokinetics of 2-tert-butylbenzothiazole and CGP 6140 (amocarzine) antifilarial drugs. Acta Trop. 1992 Aug;51(3-4):195-211. | |||||
| REF 73 | 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 74 | The memory ameliorating effects of INM-176, an ethanolic extract of Angelica gigas, against scopolamine- or Abeta(1-42)-induced cognitive dysfunction in mice. J Ethnopharmacol. 2012 Sep 28;143(2):611-20. | |||||
| REF 75 | Potential clinical use of an adrenergic/cholinergic agent (HP 128) in the treatment of Alzheimer's disease. Ann N Y Acad Sci. 1991;640:263-7. | |||||
| REF 76 | A randomized phase I study of methanesulfonyl fluoride, an irreversible cholinesterase inhibitor, for the treatment of Alzheimer's disease. Br J Clin Pharmacol. 2013 May;75(5):1231-9. | |||||
| REF 77 | An overview of phenserine tartrate, a novel acetylcholinesterase inhibitor for the treatment of Alzheimer's disease. Curr Alzheimer Res. 2005 Jul;2(3):281-90. | |||||
| REF 78 | Preclinical and first-in-human evaluation of PRX-105, a PEGylated, plant-derived, recombinant human acetylcholinesterase-R. Toxicol Appl Pharmacol. 2015 Sep 15;287(3):202-9. | |||||
| REF 79 | A sensitive method for the determination of the novel cholinesterase inhibitor ZT-1 and its active metabolite huperzine A in rat blood using liquid chromatography/tandem mass spectrometry. Rapid Commun Mass Spectrom. 2004;18(6):651-6. | |||||
| REF 80 | Recent advances in acetylcholinesterase Inhibitors and Reactivators: an update on the patent literature (2012-2015).Expert Opin Ther Pat. 2017 Apr;27(4):455-476. | |||||
| REF 81 | A patent review of butyrylcholinesterase inhibitors and reactivators 2010-2017.Expert Opin Ther Pat. 2018 Jun;28(6):455-465. | |||||
| REF 82 | Synthesis and biological activity of putative mono-hydroxylated metabolites of velnacrine, Bioorg. Med. Chem. Lett. 2(8):865-870 (1992). | |||||
| REF 83 | 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. 2005 Aug;145(8):1035-44. | |||||
| REF 84 | Biochemical pharmacology of N-acetyl-N-(methylcarbamoyloxy)-N'-methylurea (caracemide; NSC-253272). Biochem Pharmacol. 1986 Aug 15;35(16):2781-7. | |||||
| REF 85 | NXX-066 in patients with Alzheimer's disease: a bridging study. Life Sci. 1999;64(14):1215-21. | |||||
| REF 86 | A docking score function for estimating ligand-protein interactions: application to acetylcholinesterase inhibition. J Med Chem. 2004 Oct 21;47(22):5492-500. | |||||
| REF 87 | The effects of physostigmine on acetylcholinesterase activity of CSF plasma and brain. A comparison of intravenous and intraventricular administration in beagle dogs. Neuropharmacology. 1986 Oct;25(10):1167-77. | |||||
| REF 88 | Xanthine derivatives IBMX and S-9977-2 potentiate transmission at an Aplysia central cholinergic synapse. Brain Res. 1992 Jul 17;586(1):78-85. | |||||
| REF 89 | Pharmacological and biochemical assessment of SM-10888, a novel cholinesterase inhibitor. Jpn J Pharmacol. 1990 Jun;53(2):145-55. | |||||
| REF 90 | Effects of TAK-802, a novel acetylcholinesterase inhibitor, on distension-induced rhythmic bladder contractions in rats and guinea pigs. Eur J Pharmacol. 2004 Feb 6;485(1-3):299-305. | |||||
| REF 91 | Acetylcholinesterase inhibition by zifrosilone: pharmacokinetics and pharmacodynamics. Clin Pharmacol Ther. 1995 Jul;58(1):54-61. | |||||
| REF 92 | Potent beta-amyloid modulators. Neurodegener Dis. 2008;5(3-4):153-6. | |||||
| REF 93 | Galantamine, a cholinesterase inhibitor that allosterically modulates nicotinic receptors: effects on the course of Alzheimer's disease. Biol Psychiatry. 2001 Feb 1;49(3):289-99. | |||||
| REF 94 | 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 95 | Novel tacrine analogues for potential use against Alzheimer's disease: potent and selective acetylcholinesterase inhibitors and 5-HT uptake inhibitors. J Med Chem. 1997 Oct 24;40(22):3516-23. | |||||
| REF 96 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004498) | |||||
| REF 97 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006757) | |||||
| REF 98 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006922) | |||||
| REF 99 | The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. | |||||
| REF 100 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017551) | |||||
| REF 101 | 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 102 | Structure-based alignment and comparative molecular field analysis of acetylcholinesterase inhibitors. J Med Chem. 1996 Dec 20;39(26):5064-71. | |||||
| REF 103 | Isolation and cholinesterase-inhibition studies of sterols from Haloxylon recurvum. Bioorg Med Chem Lett. 2006 Feb;16(3):573-80. | |||||
| REF 104 | Synthesis and AChE inhibitory activity of new chiral tetrahydroacridine analogues from terpenic cyclanones. Eur J Med Chem. 2010 Feb;45(2):526-35. | |||||
| REF 105 | 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 106 | 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 107 | 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 108 | 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 109 | A structure-based design approach to the development of novel, reversible AChE inhibitors. J Med Chem. 2001 Sep 27;44(20):3203-15. | |||||
| REF 110 | 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 111 | Acetylcholinesterase inhibitors from the toadstool Cortinarius infractus. Bioorg Med Chem. 2010 Mar 15;18(6):2173-2177. | |||||
| REF 112 | Homobivalent quinazolinimines as novel nanomolar inhibitors of cholinesterases with dirigible selectivity toward butyrylcholinesterase. J Med Chem. 2006 Sep 7;49(18):5411-3. | |||||
| REF 113 | How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | |||||
| REF 114 | Acetylcholinesterase inhibition by alkaloids of the ant's venom Monomorium minutum, Bioorg. Med. Chem. Lett. 5(11):1131-1132 (1995). | |||||
| REF 115 | Design, synthesis and evaluation of 2,4-disubstituted pyrimidines as cholinesterase inhibitors. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3606-9. | |||||
| REF 116 | Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents. J Med Chem. 2010 May 13;53(9):3611-7. | |||||
| REF 117 | 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 118 | Synthesis, anticholinesterase activity and structure-activity relationships of m-Aminobenzoic acid derivatives. Bioorg Med Chem Lett. 2003 May 19;13(10):1825-7. | |||||
| REF 119 | 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 120 | Design, synthesis, and acetylcholinesterase inhibitory activity of novel coumarin analogues. Bioorg Med Chem. 2008 Sep 1;16(17):8011-21. | |||||
| REF 121 | 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 122 | 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 123 | 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 124 | Synthesis and biological evaluation of helicid analogues as novel acetylcholinesterase inhibitors. Eur J Med Chem. 2008 Jan;43(1):166-73. | |||||
| REF 125 | 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 126 | 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 127 | Structure and anti-acetylcholinesterase activity of 4 alpha-(hydroxymethyl)-4 alpha-demethylterritrem B. J Nat Prod. 1997 Aug;60(8):842-3. | |||||
| REF 128 | The synthesis and in vitro acetylcholinesterase and butyrylcholinesterase inhibitory activity of tacrine (Cognex ) derivaties, Bioorg. Med. Chem. Lett. 2(8):861-864 (1992). | |||||
| REF 129 | 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 130 | 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 131 | 6-Hydroxy- and 6-methoxy-beta-carbolines as acetyl- and butyrylcholinesterase inhibitors. Bioorg Med Chem Lett. 2006 Nov 15;16(22):5840-3. | |||||
| REF 132 | 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 133 | Novel heterobivalent tacrine derivatives as cholinesterase inhibitors with notable selectivity toward butyrylcholinesterase. J Med Chem. 2006 Dec 14;49(25):7540-4. | |||||
| REF 134 | Synthesis, biological evaluation, and molecular modeling of berberine derivatives as potent acetylcholinesterase inhibitors. Bioorg Med Chem. 2010 Feb;18(3):1244-51. | |||||
| REF 135 | Targeting Alzheimer's disease: Novel indanone hybrids bearing a pharmacophoric fragment of AP2238. Bioorg Med Chem. 2010 Mar 1;18(5):1749-60. | |||||
| REF 136 | 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 137 | DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-41. | |||||
| REF 138 | Bis-huperzine B: highly potent and selective acetylcholinesterase inhibitors. J Med Chem. 2005 Feb 10;48(3):655-7. | |||||
| REF 139 | Cholinesterases: new roles in brain function and in Alzheimer's disease. Neurochem Res. 2003 Apr;28(3-4):515-22. | |||||
| REF 140 | Isosorbide-2-carbamate esters: potent and selective butyrylcholinesterase inhibitors. J Med Chem. 2008 Oct 23;51(20):6400-9. | |||||
| REF 141 | 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 142 | Carinatumins A-C, new alkaloids from Lycopodium carinatum inhibiting acetylcholinesterase. Bioorg Med Chem. 2007 Feb 15;15(4):1703-7. | |||||
| REF 143 | 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 144 | Activation of the endocannabinoid system by organophosphorus nerve agents. Nat Chem Biol. 2008 Jun;4(6):373-8. | |||||
| REF 145 | Synthesis of the novel series of bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against chlorpy... Bioorg Med Chem Lett. 2006 Feb;16(3):622-7. | |||||
| REF 146 | Indole alkaloids from Ervatamia hainanensis with potent acetylcholinesterase inhibition activities. Bioorg Med Chem Lett. 2010 Nov 1;20(21):6185-7. | |||||
| REF 147 | PET imaging of brain acetylcholinesterase using [11C]CP-126,998, a brain selective enzyme inhibitor. Synapse. 2002 Jul;45(1):1-9. | |||||
| REF 148 | Cryptadines A and B, novel C27N3-type pentacyclic alkaloids from Lycopodium cryptomerinum. Bioorg Med Chem. 2007 Dec 15;15(24):7803-8. | |||||
| REF 149 | Synthesis and structure-activity relationship of Huprine derivatives as human acetylcholinesterase inhibitors. Bioorg Med Chem. 2009 Jul 1;17(13):4523-36. | |||||
| REF 150 | Synthesis and pharmacological evaluation of huprine-tacrine heterodimers: subnanomolar dual binding site acetylcholinesterase inhibitors. J Med Chem. 2005 Mar 24;48(6):1701-4. | |||||
| REF 151 | Isosorbide-based cholinesterase inhibitors; replacement of 5-ester groups leading to increased stability. Bioorg Med Chem. 2010 Feb;18(3):1045-53. | |||||
| REF 152 | 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 153 | Characterization of Acetylcholinesterase Inhibitory Constituents from Annona glabra Assisted by HPLC Microfractionation. J Nat Prod. 2010 Oct 22;73(10):1632-5. | |||||
| REF 154 | 4-Phenylcoumarins from Mesua elegans with acetylcholinesterase inhibitory activity. Bioorg Med Chem. 2010 Nov 15;18(22):7873-7. | |||||
| REF 155 | 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 156 | N-Alkylated galanthamine derivatives: Potent acetylcholinesterase inhibitors from Leucojum aestivum. Bioorg Med Chem Lett. 2008 Apr 1;18(7):2263-6. | |||||
| REF 157 | Litebamine N-homologues: preparation and anti-acetylcholinesterase activity. J Nat Prod. 1998 Jan;61(1):46-50. | |||||
| REF 158 | 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 159 | 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 160 | 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 161 | Acetylcholinesterase inhibition by territrem B derivatives. J Nat Prod. 1995 Jun;58(6):857-62. | |||||
| REF 162 | Multi-target-directed ligands to combat neurodegenerative diseases. J Med Chem. 2008 Feb 14;51(3):347-72. | |||||
| REF 163 | Indole glucoalkaloids from Chimarrhis turbinata and their evaluation as antioxidant agents and acetylcholinesterase inhibitors. J Nat Prod. 2004 Nov;67(11):1882-5. | |||||
| REF 164 | 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. | |||||
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