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.
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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) | [+] 12 Approved Drugs | + | ||||
| 1 | Ambenonium | Drug Info | Approved | Myasthenia gravis | [6] | |
| 2 | Demecarium bromide | Drug Info | Approved | Open-angle glaucoma | [5], [7] | |
| 3 | Donepezil | Drug Info | Approved | Alzheimer disease | [5], [8], [9] | |
| 4 | Edrophonium | Drug Info | Approved | Myasthenia gravis | [10] | |
| 5 | Galantamine | Drug Info | Approved | Alzheimer disease | [11], [12] | |
| 6 | Huperzine A | Drug Info | Approved | Alzheimer disease | [5], [13] | |
| 7 | Isoflurophate | Drug Info | Approved | Glaucoma/ocular hypertension | [14] | |
| 8 | Malathion | Drug Info | Approved | Pediculus capitis infestation | [15] | |
| 9 | Neostigmine | Drug Info | Approved | Myasthenia gravis | [16] | |
| 10 | Pyridostigmine | Drug Info | Approved | Myasthenia gravis | [17] | |
| 11 | Tacrine | Drug Info | Approved | Alzheimer disease | [18], [19] | |
| 12 | YM443 | Drug Info | Approved | Functional dyspepsia | [5] | |
| Clinical Trial Drug(s) | [+] 13 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 | [27] | |
| 7 | R-phenserine | Drug Info | Phase 2 | Cognitive impairment | [28] | |
| 8 | T-82 | Drug Info | Phase 2 | Cognitive impairment | [29] | |
| 9 | Desoxypeganine | Drug Info | Phase 1 | Alcohol dependence | [32] | |
| 10 | GTP-004 | Drug Info | Phase 1 | Myasthenia gravis | [30] | |
| 11 | KW-5092 | Drug Info | Phase 1 | Pain | [33] | |
| 12 | PRX-105 | Drug Info | Phase 1 | Poison intoxication | [34] | |
| 13 | ZT-1 | Drug Info | Phase 1 | Parkinson disease | [35] | |
| Discontinued Drug(s) | [+] 19 Discontinued Drugs | + | ||||
| 1 | VELNACRINE | Drug Info | Discontinued in Phase 3 | Cognitive impairment | [36] | |
| 2 | Zanapezil | Drug Info | Discontinued in Phase 3 | Alzheimer disease | [37] | |
| 3 | Caracemide | Drug Info | Discontinued in Phase 2 | Solid tumour/cancer | [38] | |
| 4 | HP-290 | Drug Info | Discontinued in Phase 2 | Parkinson disease | [39] | |
| 5 | Icopezil maleate | Drug Info | Discontinued in Phase 2 | Cognitive impairment | [40] | |
| 6 | Physostigmine | Drug Info | Discontinued in Phase 2 | Xerostomia | [41], [42] | |
| 7 | S-9977 | Drug Info | Discontinued in Phase 2 | Cognitive impairment | [43] | |
| 8 | SM-10888 | Drug Info | Discontinued in Phase 2 | Cognitive impairment | [44] | |
| 9 | TAK-802 | Drug Info | Discontinued in Phase 2 | Urinary dysfunction | [45] | |
| 10 | ZIFROSILONE | Drug Info | Discontinued in Phase 2 | Cognitive impairment | [46] | |
| 11 | NP-61 | Drug Info | Discontinued in Phase 1 | Alzheimer disease | [47] | |
| 12 | ABS-301 | Drug Info | Terminated | Alzheimer disease | [50] | |
| 13 | CI-1002 | Drug Info | Terminated | Alzheimer disease | [51] | |
| 14 | F-3796 | Drug Info | Terminated | Alzheimer disease | [52] | |
| 15 | FR-152558 | Drug Info | Terminated | Alzheimer disease | [53] | |
| 16 | MF-8615 | Drug Info | Terminated | Alzheimer disease | [54] | |
| 17 | MF268 | Drug Info | Terminated | Alzheimer disease | [55] | |
| 18 | NP-7557 | Drug Info | Terminated | Alzheimer disease | [56] | |
| 19 | Ro-46-5934 | Drug Info | Terminated | Alzheimer disease | [57] | |
| Preclinical Drug(s) | [+] 1 Preclinical Drugs | + | ||||
| 1 | PHENSERINE TARTRATE | Drug Info | Preclinical | Parkinson disease | [49] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Inhibitor | [+] 262 Inhibitor drugs | + | ||||
| 1 | Ambenonium | Drug Info | [58] | |||
| 2 | Demecarium bromide | Drug Info | [59], [60] | |||
| 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 | [27] | |||
| 16 | R-phenserine | Drug Info | [76] | |||
| 17 | T-82 | Drug Info | [29], [5] | |||
| 18 | GTP-004 | Drug Info | [30] | |||
| 19 | KW-5092 | Drug Info | [33] | |||
| 20 | PRX-105 | Drug Info | [77] | |||
| 21 | ZT-1 | Drug Info | [78], [5] | |||
| 22 | Di-substituted piperidine derivative 2 | Drug Info | [80] | |||
| 23 | Egonol compound 1 | Drug Info | [79] | |||
| 24 | Fluorinated donepezil derivative 2 | Drug Info | [79] | |||
| 25 | Indoline derivative 1 | Drug Info | [80] | |||
| 26 | Isochroman-4-ketone derivative 1 | Drug Info | [80] | |||
| 27 | Lycorine dimer salt derivative 1 | Drug Info | [79] | |||
| 28 | PMID27967267-Compound-12 | Drug Info | [79] | |||
| 29 | PMID27967267-Compound-13 | Drug Info | [79] | |||
| 30 | PMID27967267-Compound-15 | Drug Info | [79] | |||
| 31 | PMID27967267-Compound-3 | Drug Info | [79] | |||
| 32 | PMID27967267-Compound-39 | Drug Info | [79] | |||
| 33 | PMID27967267-Compound-42 | Drug Info | [79] | |||
| 34 | PMID27967267-Compound-7 | Drug Info | [79] | |||
| 35 | PMID27967267-Compound-neostenine | Drug Info | [79] | |||
| 36 | PMID27967267-Compound-stenine | Drug Info | [79] | |||
| 37 | PMID29757691-Compound-2a | Drug Info | [80] | |||
| 38 | PMID29757691-Compound-4 | Drug Info | [80] | |||
| 39 | PMID29757691-Compound-8a | Drug Info | [80] | |||
| 40 | PMID29757691-Compound-8b | Drug Info | [80] | |||
| 41 | PMID29757691-Compound-8d | Drug Info | [80] | |||
| 42 | Quinazoline alkaloid derivative 1 | Drug Info | [80] | |||
| 43 | Tacrine heterodimer derivative 1 | Drug Info | [80] | |||
| 44 | Tacrine-caffeic acid hybrid derivative 1 | Drug Info | [79] | |||
| 45 | Tacrine-caffeic acid hybrid derivative 2 | Drug Info | [79] | |||
| 46 | Tacrine-indole hybrid derivative 1 | Drug Info | [79] | |||
| 47 | Tacrine-indole hybrid derivative 2 | Drug Info | [79] | |||
| 48 | Tacrine-indole hybrid derivative 3 | Drug Info | [79] | |||
| 49 | Tacrine-phenothiazine hybrid derivative 1 | Drug Info | [79] | |||
| 50 | Tetra-hydro-isoquinoline derivative 1 | Drug Info | [80] | |||
| 51 | Tetra-hydro-isoquinoline derivative 2 | Drug Info | [80] | |||
| 52 | Tetra-hydro-isoquinoline derivative 3 | Drug Info | [80] | |||
| 53 | Tetra-hydro-isoquinoline derivative 4 | Drug Info | [80] | |||
| 54 | VELNACRINE | Drug Info | [81] | |||
| 55 | Zanapezil | Drug Info | [82] | |||
| 56 | Caracemide | Drug Info | [83] | |||
| 57 | HP-290 | Drug Info | [84], [73] | |||
| 58 | Icopezil maleate | Drug Info | [85] | |||
| 59 | Physostigmine | Drug Info | [86] | |||
| 60 | S-9977 | Drug Info | [87] | |||
| 61 | SM-10888 | Drug Info | [88] | |||
| 62 | TAK-802 | Drug Info | [89] | |||
| 63 | ZIFROSILONE | Drug Info | [90], [5] | |||
| 64 | NP-61 | Drug Info | [91] | |||
| 65 | PHENSERINE TARTRATE | Drug Info | [76], [5] | |||
| 66 | 7-methoxytacrine | Drug Info | [92] | |||
| 67 | F-3796 | Drug Info | [94] | |||
| 68 | FR-152558 | Drug Info | [95] | |||
| 69 | MF-8615 | Drug Info | [96] | |||
| 70 | MF268 | Drug Info | [97] | |||
| 71 | NP-7557 | Drug Info | [98] | |||
| 72 | Ro-46-5934 | Drug Info | [57] | |||
| 73 | (-)-huperzine B | Drug Info | [99] | |||
| 74 | (-)-Tolserine | Drug Info | [71] | |||
| 75 | (1R)-1,2,2-TRIMETHYLPROPYL (S)-METHYLPHOSPHINATE | Drug Info | [97] | |||
| 76 | (2-Butyryloxy-ethyl)-trimethyl-ammonium iodide | Drug Info | [100] | |||
| 77 | (2-Chloro-ethyl)-trimethyl-ammonium chloride | Drug Info | [100] | |||
| 78 | (2-Ethoxy-ethyl)-trimethyl-ammonium iodide | Drug Info | [100] | |||
| 79 | (2-Mercapto-ethyl)-trimethyl-ammonium iodide | Drug Info | [100] | |||
| 80 | (24S)-ethylcholesta-7,9(11),22(E)-triene-3b-ol | Drug Info | [101] | |||
| 81 | (3-Bromo-propyl)-trimethyl-ammonium | Drug Info | [100] | |||
| 82 | (3-Hydroxy-2-methyl-phenyl)-trimethyl-ammonium | Drug Info | [100] | |||
| 83 | (3R)-9-amino-3-methyl-1,2,3,4-tetrahydroacridine | Drug Info | [102] | |||
| 84 | (4-Bromo-butyl)-trimethyl-ammonium | Drug Info | [100] | |||
| 85 | (4-Iodo-butyl)-trimethyl-ammonium iodide | Drug Info | [100] | |||
| 86 | (5-Bromo-pentyl)-trimethyl-ammonium | Drug Info | [100] | |||
| 87 | (R)-tacrine(10)-hupyridone | Drug Info | [97] | |||
| 88 | (RS)-tacrine(10)-hupyridone | Drug Info | [99] | |||
| 89 | (S)-tacrine(10)-hupyridone | Drug Info | [97] | |||
| 90 | (S,S)-(-)-bis(12)-hupyridone | Drug Info | [99] | |||
| 91 | 1,11-bis(pyridinium)-undecane dibromide | Drug Info | [103] | |||
| 92 | 1,2-Di(berberine-9-O-yl)ethane dibromide | Drug Info | [104] | |||
| 93 | 1,3-Bis-(3-imidazolidin-2-yl-phenyl)-urea | Drug Info | [105] | |||
| 94 | 1,3-Di(berberine-9-O-yl)ethane dibromide | Drug Info | [104] | |||
| 95 | 1,4-Di(berberine-9-O-yl)ethane dibromide | Drug Info | [104] | |||
| 96 | 1,9-bis(pyridinium)-nonane dibromide | Drug Info | [103] | |||
| 97 | 1-(3-Bromomethyl-phenyl)-2,2,2-trifluoro-ethanone | Drug Info | [106] | |||
| 98 | 1-benzene sulfonyl-cis-2,6-dimethyl piperidine | Drug Info | [107] | |||
| 99 | 1-Deoxy-1-Thio-Heptaethylene Glycol | Drug Info | [97] | |||
| 100 | 1-ETHOXY-2-(2-ETHOXYETHOXY)ETHANE | Drug Info | [97] | |||
| 101 | 10-Hydroxy-infractopicrin | Drug Info | [108] | |||
| 102 | 2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-imine | Drug Info | [109] | |||
| 103 | 2-(Acetylamino)-2-Deoxy-a-D-Glucopyranose | Drug Info | [110] | |||
| 104 | 2-(N-Morpholino)-Ethanesulfonic Acid | Drug Info | [110] | |||
| 105 | 2-Hex-5-enyl-5-non-8-enyl-3,4-dihydro-2H-pyrrole | Drug Info | [111] | |||
| 106 | 2-Hex-5-enyl-5-non-8-enyl-pyrrolidine | Drug Info | [111] | |||
| 107 | 2-Hex-5-enyl-5-nonyl-pyrrolidine | Drug Info | [111] | |||
| 108 | 2-morpholino-N-phenethylpyrimidin-4-amine | Drug Info | [112] | |||
| 109 | 2-Propyl-beta-carboline-2-ium iodide | Drug Info | [113] | |||
| 110 | 24-ethyl-cholest-7-ene-3,5,6-triol | Drug Info | [101] | |||
| 111 | 3,4,5,6-Tetrachloro-[1,2]benzoquinone | Drug Info | [114] | |||
| 112 | 3,6,9,12,15-Pentaoxaheptadecane | Drug Info | [97] | |||
| 113 | 3,7-BIS(DIMETHYLAMINO)PHENOTHIAZIN-5-IUM | Drug Info | [97] | |||
| 114 | 3-(2,5-Dioxo-pyrrolidin-1-yl)-benzoic acid | Drug Info | [115] | |||
| 115 | 3-(2-Diethylamino-acetamino)-rutaecarpine | Drug Info | [116] | |||
| 116 | 3-(2-Diethylamino-propionamino)-rutaecarpine | Drug Info | [116] | |||
| 117 | 3-(2-N-Piperidyl-acetamino)-rutaecarpine | Drug Info | [116] | |||
| 118 | 3-(2-N-Piperidyl-propionamino)-rutaecarpine | Drug Info | [116] | |||
| 119 | 3-(2-N-Pyrrolyl-acetamino)-rutaecarpine | Drug Info | [116] | |||
| 120 | 3-(2-N-Pyrrolyl-propionamino)-rutaecarpine | Drug Info | [116] | |||
| 121 | 3-(3-Carboxy-propionylamino)-benzoic acid | Drug Info | [115] | |||
| 122 | 3-(4-o-Tolylpiperazine-1-carbonyl)coumarin | Drug Info | [117] | |||
| 123 | 3-(4-Phenylpiperazin-1-carbonyl)coumarin | Drug Info | [117] | |||
| 124 | 3-(dimethylamino)phenyl phenylcarbamate | Drug Info | [71] | |||
| 125 | 3-hydroxy-N,N,N-trimethylbenzenaminium iodide | Drug Info | [118] | |||
| 126 | 3-[(1s)-1-(Dimethylamino)Ethyl]Phenol | Drug Info | [97] | |||
| 127 | 3-[2-(1-Benzyl-piperidin-4-yl)-ethyl]-1H-indazole | Drug Info | [85] | |||
| 128 | 3-[3-(benzylmethylamino)propoxy]xanthen-9-one | Drug Info | [119] | |||
| 129 | 3-[4-(benzylmethylamino)butoxy]xanthen-9-one | Drug Info | [119] | |||
| 130 | 3-[5-(benzylmethylamino)pentyloxy]xanthen-9-one | Drug Info | [119] | |||
| 131 | 3-[6-(benzylmethylamino)hexyloxy]xanthen-9-one | Drug Info | [119] | |||
| 132 | 3-[7-(benzylmethylamino)-heptyloxy]xanthen-9-one | Drug Info | [119] | |||
| 133 | 3-[8-(benzylmethylamino)octyloxy]xanthen-9-one | Drug Info | [119] | |||
| 134 | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [120] | |||
| 135 | 4-formylphenyl-O-beta-D-ribopyranoside | Drug Info | [121] | |||
| 136 | 4-formylphenyl-O-beta-Dglucopyranoside | Drug Info | [121] | |||
| 137 | 4-ISOPROPYLPHENSERINE | Drug Info | [122] | |||
| 138 | 4-[4-(benzhydryloxy)piperidino]butyl benzoate | Drug Info | [123] | |||
| 139 | 4ALPHA-(HYDROXYMETHYL)-4ALPHA-DEMETHYLTERRITREM B | Drug Info | [124] | |||
| 140 | 5-Chloro-1,2,3,4-tetrahydro-acridin-9-ylamine | Drug Info | [125] | |||
| 141 | 5-Hex-5-enyl-2-nonyl-3,4-dihydro-2H-pyrrole | Drug Info | [111] | |||
| 142 | 6,8-Dichloro-1,2,3,4-tetrahydro-acridin-9-ylamine | Drug Info | [126] | |||
| 143 | 6-chlorotacrine hydrochloride | Drug Info | [127] | |||
| 144 | 6-hydroxy-1,2,9-trimethyl-9H-beta-carbolin-2-ium | Drug Info | [128] | |||
| 145 | 6-hydroxy-1,2-dimethyl-9H-beta-carbolin-2-ium | Drug Info | [128] | |||
| 146 | 6-hydroxy-2,9-dimethyl-9H-beta-carbolin-2-ium | Drug Info | [128] | |||
| 147 | 6-hydroxy-2-methyl-9H-beta-carbolin-2-ium | Drug Info | [128] | |||
| 148 | 6-methoxy-1,2-dimethyl-9H-beta-carbolin-2-ium | Drug Info | [128] | |||
| 149 | 6-methoxy-2,9-dimethyl-9H-beta-carbolin-2-ium | Drug Info | [128] | |||
| 150 | 6-Methyl-4-(4-benzoylpiperazin-1-yl)coumarin | Drug Info | [117] | |||
| 151 | 6-Methyl-4-(4-o-tolylpiperazin-1-yl)coumarin | Drug Info | [117] | |||
| 152 | 6-Methyl-4-(4-phenylpiperazin-1-yl)coumarin | Drug Info | [117] | |||
| 153 | 7-Chloro-1,2,3,4-tetrahydro-acridin-9-ylamine | Drug Info | [125] | |||
| 154 | 7-Oxo-7H-dibenzo[de,g]quinoline | Drug Info | [129] | |||
| 155 | 9-amino-7H-dibenzo[de,h]quinolin-7-one | Drug Info | [129] | |||
| 156 | 9-Ethyl-beta-carboline | Drug Info | [113] | |||
| 157 | 9-hydrazino-1,2,3,4-tetrahydroacridine | Drug Info | [130] | |||
| 158 | 9-O-[2-(Phenylol-1-yloxy)ethyl]berberine bromide | Drug Info | [131] | |||
| 159 | 9-O-[2-(Phenylol-1-yloxy)hexyl]berberine bromide | Drug Info | [131] | |||
| 160 | 9-O-[3-(2-Pyridinoxyl)butyl]-berberine bromide | Drug Info | [104] | |||
| 161 | 9-O-[3-(4-Nitro-phenoxyl)butyl]-berberine bromide | Drug Info | [104] | |||
| 162 | 9-O-[3-(Phenylamino)propyl]-berberine bromide | Drug Info | [104] | |||
| 163 | 9-O-[4-(Phenylol-1-yloxy)butyl]berberine bromide | Drug Info | [131] | |||
| 164 | 9-O-[5-(Phenylol-1-yloxy)pentyl]berberine bromide | Drug Info | [131] | |||
| 165 | Allyl-trimethyl-ammonium | Drug Info | [100] | |||
| 166 | AP-2238 | Drug Info | [132] | |||
| 167 | AP-2243 | Drug Info | [133] | |||
| 168 | BENZOQUINONE | Drug Info | [114] | |||
| 169 | Beta-L-fucose | Drug Info | [134] | |||
| 170 | BIS(12)-HUPERZINE B | Drug Info | [135] | |||
| 171 | Bis(14)-Huperzine B | Drug Info | [135] | |||
| 172 | BIS(16)-HUPERZINE B | Drug Info | [135] | |||
| 173 | BIS(18)-HUPERZINE B | Drug Info | [135] | |||
| 174 | BIS(20)-HUPERZINE B | Drug Info | [135] | |||
| 175 | BIS(8)-HUPERZINE B | Drug Info | [135] | |||
| 176 | Bis-7-tacrine | Drug Info | [112] | |||
| 177 | But-3-enyl-trimethyl-ammonium bromide | Drug Info | [100] | |||
| 178 | BW284C51 | Drug Info | [136], [137] | |||
| 179 | BZYX | Drug Info | [1] | |||
| 180 | CAPROCTAMINE | Drug Info | [138] | |||
| 181 | Carinatumins B (2) | Drug Info | [139] | |||
| 182 | CHF-2819 | Drug Info | [140] | |||
| 183 | CHLORANIL | Drug Info | [114] | |||
| 184 | CHLORPYRIFOS | Drug Info | [141] | |||
| 185 | CHOLINE IODIDE | Drug Info | [100] | |||
| 186 | Cis-2,6-dimethyl-1-methyl sulfonyl piperidine | Drug Info | [107] | |||
| 187 | CLEBOPRIDE | Drug Info | [105] | |||
| 188 | CORONARIDINE | Drug Info | [142] | |||
| 189 | CRYPTADINE B | Drug Info | [144] | |||
| 190 | DECIDIUM | Drug Info | [99] | |||
| 191 | Dimethyl-pent-4-enyl-ammonium bromide | Drug Info | [100] | |||
| 192 | Ethyl octylfluorophosphonate | Drug Info | [145] | |||
| 193 | Fucose | Drug Info | [110] | |||
| 194 | Galanthamine derivative | Drug Info | [99] | |||
| 195 | GANSTIGMINE | Drug Info | [99] | |||
| 196 | GENESERINE | Drug Info | [140] | |||
| 197 | HALOXYSTEROL A | Drug Info | [101] | |||
| 198 | Haloxysterol C | Drug Info | [101] | |||
| 199 | Haloxysterol D | Drug Info | [101] | |||
| 200 | Hexyl-trimethyl-ammonium | Drug Info | [100] | |||
| 201 | Huprine X | Drug Info | [99] | |||
| 202 | Huprine Y | Drug Info | [146] | |||
| 203 | Huprine-Tacrine Heterodimer | Drug Info | [147] | |||
| 204 | Iso-OMPA | Drug Info | [137] | |||
| 205 | Isopropyl dodecylfluorophosphonate | Drug Info | [145] | |||
| 206 | Isosorbide-2-(methylcarbamate)-5-benzoate | Drug Info | [137] | |||
| 207 | Isosorbide-2-(methylcarbamate)-5-mononitrate | Drug Info | [137] | |||
| 208 | Isosorbide-2-benzylcarbamate-5-cyclopentanoate | Drug Info | [137] | |||
| 209 | Isosorbide-2-benzylcarbamate-5-cyclopropanoate | Drug Info | [137] | |||
| 210 | Isosorbide-di-(4-nitrophenyl carbamate) | Drug Info | [148] | |||
| 211 | Isosorbide-di-(benzylcarbamate) | Drug Info | [148] | |||
| 212 | Isosorbide-di-(ethylcarbamate) | Drug Info | [148] | |||
| 213 | Isosorbide-di-phenylcarbamate | Drug Info | [148] | |||
| 214 | LIPOCRINE | Drug Info | [149] | |||
| 215 | LYSICAMINE | Drug Info | [150] | |||
| 216 | MEMOQUIN | Drug Info | [149] | |||
| 217 | MESUAGENIN A | Drug Info | [151] | |||
| 218 | MESUAGENIN B | Drug Info | [151] | |||
| 219 | Mesuagenin D | Drug Info | [151] | |||
| 220 | Methyl Phosphinic Acid | Drug Info | [110] | |||
| 221 | N,N'-(1',10'-decylene)-bis-(-)-nor-MEP | Drug Info | [152] | |||
| 222 | N,N'-(1',11'-undecydene)-bis-(-)-nor-MEP | Drug Info | [152] | |||
| 223 | N,N'-(1',12'-dodecydene)-bis-(-)-nor-MEP | Drug Info | [152] | |||
| 224 | N,N'-(1',5'-pentylene)-bis-(-)-nor-MEP | Drug Info | [152] | |||
| 225 | N,N'-(1',7'-heptylene)-bis-(-)-nor-MEP | Drug Info | [152] | |||
| 226 | N,N'-(1',9'-nonylene)-bis-(-)-nor-MEP | Drug Info | [152] | |||
| 227 | N-(14-methylallyl)norgalanthamine | Drug Info | [153] | |||
| 228 | N-ALLYLNORGALANTHAMINE | Drug Info | [153] | |||
| 229 | N-allylnorlitebamine | Drug Info | [154] | |||
| 230 | N-benzyl-2-thiomorpholinopyrimidin-4-amine | Drug Info | [112] | |||
| 231 | N-benzylnorlitebamine | Drug Info | [154] | |||
| 232 | N-butylnorlitebamine | Drug Info | [154] | |||
| 233 | N-isobutylnorlitebamine | Drug Info | [154] | |||
| 234 | N-isopropylnorlitebamine | Drug Info | [154] | |||
| 235 | N-isopropylnorlitebamineN-methoiodide | Drug Info | [154] | |||
| 236 | N-Methyl-1'H-phenothiazine-1'-carboxamide | Drug Info | [155] | |||
| 237 | N-n-dodecyl-7-methoxytacrine hydrochloride | Drug Info | [92] | |||
| 238 | N-n-heptyl-7-methoxytacrine hydrochloride | Drug Info | [92] | |||
| 239 | N-n-hexyl-7-methoxytacrine hydrochloride | Drug Info | [92] | |||
| 240 | N-n-nonyl-7-methoxytacrine hydrochloride | Drug Info | [92] | |||
| 241 | N-n-octyl-7-methoxytacrine hydrochloride | Drug Info | [92] | |||
| 242 | N-n-pentyl-7-methoxytacrine hydrochloride | Drug Info | [92] | |||
| 243 | N-n-propyl-7-methoxytacrine hydrochloride | Drug Info | [92] | |||
| 244 | N-propylnorlitebamine | Drug Info | [154] | |||
| 245 | NSC-23180 | Drug Info | [156] | |||
| 246 | OBIDOXIME | Drug Info | [141] | |||
| 247 | PARAOXON | Drug Info | [145] | |||
| 248 | Petrosamine | Drug Info | [157] | |||
| 249 | Propidium | Drug Info | [110] | |||
| 250 | Pseudocolumbamine trifluoroacetate | Drug Info | [150] | |||
| 251 | Pseudopalmatine trifluoroacetate | Drug Info | [150] | |||
| 252 | TACRINE(8)-4-AMINOQUINOLINE | Drug Info | [97] | |||
| 253 | TASPINE | Drug Info | [158] | |||
| 254 | TERRITREM B | Drug Info | [159] | |||
| 255 | Tetraethylene Glycol | Drug Info | [110] | |||
| 256 | THIOCTIC ACID | Drug Info | [160] | |||
| 257 | TOLSERINE | Drug Info | [73] | |||
| 258 | TRIMEDOXIME | Drug Info | [141] | |||
| 259 | Trimethyl-(3-nitro-phenyl)-ammonium iodide | Drug Info | [100] | |||
| 260 | Trimethyl-(4-oxo-pentyl)-ammonium iodide | Drug Info | [100] | |||
| 261 | TURBINATINE | Drug Info | [161] | |||
| 262 | Voacangine | Drug Info | [142] | |||
| Modulator | [+] 8 Modulator drugs | + | ||||
| 1 | Donepezil | Drug Info | [1] | |||
| 2 | YM443 | Drug Info | [5] | |||
| 3 | Suronacrine maleate | Drug Info | [75] | |||
| 4 | Desoxypeganine | Drug Info | [32] | |||
| 5 | ABS-301 | Drug Info | [93] | |||
| 6 | CI-1002 | Drug Info | [51] | |||
| 7 | CP-126998 | Drug Info | [143] | |||
| 8 | NPRx-30 | Drug Info | [1] | |||
| Reactivator | [+] 7 Reactivator drugs | + | ||||
| 1 | 2-PAM derivative 1 | Drug Info | [79] | |||
| 2 | 4-PAM derivative 1 | Drug Info | [79] | |||
| 3 | Amidine oxime derivative 1 | Drug Info | [79] | |||
| 4 | PMID27967267-Compound-47 | Drug Info | [79] | |||
| 5 | PMID27967267-Compound-48 | Drug Info | [79] | |||
| 6 | PMID27967267-Compound-49 | Drug Info | [79] | |||
| 7 | PMID27967267-Compound-52 | Drug Info | [79] | |||
| Activator | [+] 1 Activator drugs | + | ||||
| 1 | MMB-4 | Drug Info | [1] | |||
| Cell-based Target Expression Variations | Top | |||||
|---|---|---|---|---|---|---|
| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Galantamine | Ligand Info | |||||
| Structure Description | Crystal Structure of Recombinant Human Acetylcholinesterase in Complex with (-)-galantamine | PDB:4EY6 | ||||
| Method | X-ray diffraction | Resolution | 2.40 Å | Mutation | No | [162] |
| PDB Sequence |
EDAELLVTVR
13 GGRLRGIRLK23 TPGGPVSAFL33 GIPFAEPPMG43 PRRFLPPEPK53 QPWSGVVDAT 63 TFQSVCYQYV73 DTLYPGFEGT83 EMWNPNRELS93 EDCLYLNVWT103 PYPRPTSPTP 113 VLVWIYGGGF123 YSGASSLDVY133 DGRFLVQAER143 TVLVSMNYRV153 GAFGFLALPG 163 SREAPGNVGL173 LDQRLALQWV183 QENVAAFGGD193 PTSVTLFGES203 AGAASVGMHL 213 LSPPSRGLFH223 RAVLQSGAPN233 GPWATVGMGE243 ARRRATQLAH253 LVGCPNDTEL 269 VACLRTRPAQ279 VLVNHEWHVL289 PQESVFRFSF299 VPVVDGDFLS309 DTPEALINAG 319 DFHGLQVLVG329 VVKDEGSYFL339 VYGAPGFSKD349 NESLISRAEF359 LAGVRVGVPQ 369 VSDLAAEAVV379 LHYTDWLHPE389 DPARLREALS399 DVVGDHNVVC409 PVAQLAGRLA 419 AQGARVYAYV429 FEHRASTLSW439 PLWMGVPHGY449 EIEFIFGIPL459 DPSRNYTAEE 469 KIFAQRLMRY479 WANFARTGDP489 NEPRDPQWPP502 YTAGAQQYVS512 LDLRPLEVRR 522 GLRAQACAFW532 NRFLPKLLSA542
|
|||||
|
|
||||||
| Ligand Name: BW284C51 | Ligand Info | |||||
| Structure Description | Binary complex of native hAChE with BW284c51 | PDB:6O50 | ||||
| Method | X-ray diffraction | Resolution | 2.35 Å | Mutation | No | [163] |
| PDB Sequence |
EDAELLVTVR
13 GGRLRGIRLK23 TPGGPVSAFL33 GIPFAEPPMG43 PRRFLPPEPK53 QPWSGVVDAT 63 TFQSVCYQYV73 DTLYPGFEGT83 EMWNPNRELS93 EDCLYLNVWT103 PYPRPTSPTP 113 VLVWIYGGGF123 YSGASSLDVY133 DGRFLVQAER143 TVLVSMNYRV153 GAFGFLALPG 163 SREAPGNVGL173 LDQRLALQWV183 QENVAAFGGD193 PTSVTLFGES203 AGAASVGMHL 213 LSPPSRGLFH223 RAVLQSGAPN233 GPWATVGMGE243 ARRRATQLAH253 LVGCPPGGTG 263 GNDTELVACL273 RTRPAQVLVN283 HEWHVLPQES293 VFRFSFVPVV303 DGDFLSDTPE 313 ALINAGDFHG323 LQVLVGVVKD333 EGSYFLVYGA343 PGFSKDNESL353 ISRAEFLAGV 363 RVGVPQVSDL373 AAEAVVLHYT383 DWLHPEDPAR393 LREALSDVVG403 DHNVVCPVAQ 413 LAGRLAAQGA423 RVYAYVFEHR433 ASTLSWPLWM443 GVPHGYEIEF453 IFGIPLDPSR 463 NYTAEEKIFA473 QRLMRYWANF483 ARTGDPNEPR493 DPKAPQWPPY503 TAGAQQYVSL 513 DLRPLEVRRG523 LRAQACAFWN533 RFLPKLLSAT543
|
|||||
|
|
TYR72
3.307
ASP74
4.815
LEU76
3.455
TRP86
3.338
GLY120
4.092
GLY121
4.029
GLY122
4.287
TYR124
3.526
SER125
4.840
TYR133
4.155
GLU202
2.924
|
|||||
| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
|---|---|
|
Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Tissue Distribution
Human Pathway Affiliation
Biological Network Descriptors
|
|
| Protein Name | Pfam ID | Percentage of Identity (%) | E value |
|---|---|---|---|
| Arylacetamide deacetylase (AADAC) | 28.889 (39/135) | 3.00E-03 |
|
Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
|
| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
|---|---|---|---|
| Glycerophospholipid metabolism | hsa00564 | Affiliated Target |
|
| Class: Metabolism => Lipid metabolism | Pathway Hierarchy | ||
| Cholinergic synapse | hsa04725 | Affiliated Target |
|
| Class: Organismal Systems => Nervous system | Pathway Hierarchy | ||
| Degree | 2 | Degree centrality | 2.15E-04 | Betweenness centrality | 7.27E-05 |
|---|---|---|---|---|---|
| Closeness centrality | 2.02E-01 | Radiality | 1.35E+01 | Clustering coefficient | 0.00E+00 |
| Neighborhood connectivity | 2.50E+01 | Topological coefficient | 5.00E-01 | Eccentricity | 12 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| 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 | 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 3 | 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 4 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 011963. | |||||
| REF 5 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 6 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 010155. | |||||
| REF 7 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 011860. | |||||
| REF 8 | 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 9 | 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 10 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040131. | |||||
| REF 11 | 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 12 | Novel pharmacological targets for the treatment of Parkinson's disease. Nat Rev Drug Discov. 2006 Oct;5(10):845-54. | |||||
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| REF 17 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040457. | |||||
| 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). | |||||
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| REF 22 | Eptastigmine: ten years of pharmacology, toxicology, pharmacokinetic, and clinical studies. CNS Drug Rev. 2001 Winter;7(4):369-86. | |||||
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| REF 24 | Handbook of Dementing Illnesses, Morris John. Page(570). | |||||
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| REF 29 | 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 30 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 31 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 32 | 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. | |||||
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| REF 34 | ClinicalTrials.gov (NCT01093859) An Exploratory Phase 1 Microdose Study of PRX-105. U.S. National Institutes of Health. | |||||
| REF 35 | 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 36 | Velnacrine for Alzheimer's disease. Cochrane Database Syst Rev. 2004;(2):CD004748. | |||||
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| 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 800006532) | |||||
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