Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T27812
(Former ID: TTDC00255)
|
|||||
| Target Name |
Serotonin transporter (SERT)
|
|||||
| Synonyms |
Solute carrier family 6 member 4; HTT; 5HTT; 5HT transporter
Click to Show/Hide
|
|||||
| Gene Name |
SLC6A4
|
|||||
| Target Type |
Successful target
|
[1] | ||||
| Disease | [+] 11 Target-related Diseases | + | ||||
| 1 | Anxiety disorder [ICD-11: 6B00-6B0Z] | |||||
| 2 | Attention deficit hyperactivity disorder [ICD-11: 6A05] | |||||
| 3 | Chronic pain [ICD-11: MG30] | |||||
| 4 | concerning food/fluid intake symptom [ICD-11: MG43] | |||||
| 5 | Corneal disease [ICD-11: 9A76-9A78] | |||||
| 6 | Cough [ICD-11: MD12] | |||||
| 7 | Depression [ICD-11: 6A70-6A7Z] | |||||
| 8 | Migraine [ICD-11: 8A80] | |||||
| 9 | Nicotine use disorder [ICD-11: 6C4A] | |||||
| 10 | Obesity [ICD-11: 5B80-5B81] | |||||
| 11 | Pain [ICD-11: MG30-MG3Z] | |||||
| Function |
Plays a key role in mediating regulation of the availability of serotonin to other receptors of serotonergic systems. Terminates the action of serotonin and recycles it in a sodium-dependent manner. Serotonin transporter whose primary function in the central nervous system involves the regulation of serotonergic signaling via transport of serotonin molecules from the synaptic cleft back into the pre-synaptic terminal for re-utilization.
Click to Show/Hide
|
|||||
| BioChemical Class |
Neurotransmitter:sodium symporter
|
|||||
| UniProt ID | ||||||
| Sequence |
METTPLNSQKQLSACEDGEDCQENGVLQKVVPTPGDKVESGQISNGYSAVPSPGAGDDTR
HSIPATTTTLVAELHQGERETWGKKVDFLLSVIGYAVDLGNVWRFPYICYQNGGGAFLLP YTIMAIFGGIPLFYMELALGQYHRNGCISIWRKICPIFKGIGYAICIIAFYIASYYNTIM AWALYYLISSFTDQLPWTSCKNSWNTGNCTNYFSEDNITWTLHSTSPAEEFYTRHVLQIH RSKGLQDLGGISWQLALCIMLIFTVIYFSIWKGVKTSGKVVWVTATFPYIILSVLLVRGA TLPGAWRGVLFYLKPNWQKLLETGVWIDAAAQIFFSLGPGFGVLLAFASYNKFNNNCYQD ALVTSVVNCMTSFVSGFVIFTVLGYMAEMRNEDVSEVAKDAGPSLLFITYAEAIANMPAS TFFAIIFFLMLITLGLDSTFAGLEGVITAVLDEFPHVWAKRRERFVLAVVITCFFGSLVT LTFGGAYVVKLLEEYATGPAVLTVALIEAVAVSWFYGITQFCRDVKEMLGFSPGWFWRIC WVAISPLFLLFIICSFLMSPPQLRLFQYNYPYWSIILGYCIGTSSFICIPTYIAYRLIIT PGTFKERIIKSITPETPTEIPCGDIRLNAV Click to Show/Hide
|
|||||
| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| ADReCS ID | BADD_A04234 | |||||
| HIT2.0 ID | T25RHJ | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 26 Approved Drugs | + | ||||
| 1 | Acetaminophen | Drug Info | Approved | Pain | [2], [3], [4] | |
| 2 | Amfepramone | Drug Info | Approved | Obesity | [5] | |
| 3 | Amitriptyline | Drug Info | Approved | Depression | [6], [7], [8] | |
| 4 | Bupropion | Drug Info | Approved | Smoking dependence | [7] | |
| 5 | Chlorphentermine Hydrochloride | Drug Info | Approved | Appetite suppressant | [7] | |
| 6 | Citalopram | Drug Info | Approved | Depression | [9], [8] | |
| 7 | Clomipramine | Drug Info | Approved | Depression | [10], [8] | |
| 8 | Cocaine | Drug Info | Approved | Anaesthesia | [7], [11], [12] | |
| 9 | Dasotraline | Drug Info | Approved | Attention deficit hyperactivity disorder | [13] | |
| 10 | Desvenlafaxine | Drug Info | Approved | Major depressive disorder | [14], [15] | |
| 11 | Dextromethorphan Polistirex | Drug Info | Approved | Dry cough | [7] | |
| 12 | Duloxetine | Drug Info | Approved | Depression | [16], [8] | |
| 13 | Escitalopram | Drug Info | Approved | Major depressive disorder | [7] | |
| 14 | Fluoxetine | Drug Info | Approved | Depression | [17], [18] | |
| 15 | Fluvoxamine | Drug Info | Approved | Depression | [19], [20] | |
| 16 | Levomilnacipran | Drug Info | Approved | Fibromyalgia | [21], [22] | |
| 17 | Luvox | Drug Info | Approved | Anxiety disorder | [23] | |
| 18 | Nortriptyline | Drug Info | Approved | Depression | [24], [8] | |
| 19 | Paroxetine | Drug Info | Approved | Depression | [25], [26] | |
| 20 | Sertraline | Drug Info | Approved | Depression | [27], [8] | |
| 21 | Sibutramine | Drug Info | Approved | Obesity | [28], [29] | |
| 22 | Tianeptine | Drug Info | Approved | Major depressive disorder | [7], [8], [30] | |
| 23 | Trazodone | Drug Info | Approved | Depression | [31], [8] | |
| 24 | Venlafaxine | Drug Info | Approved | Depression | [32], [33] | |
| 25 | Vilazodone | Drug Info | Approved | Major depressive disorder | [34], [35] | |
| 26 | Vortioxetine | Drug Info | Approved | Major depressive disorder | [36], [37] | |
| Clinical Trial Drug(s) | [+] 17 Clinical Trial Drugs | + | ||||
| 1 | Amitifadine | Drug Info | Phase 3 | Obesity | [38], [39] | |
| 2 | AVP-786 | Drug Info | Phase 3 | Alzheimer disease | [13], [40], [41] | |
| 3 | Bicifadine | Drug Info | Phase 3 | Neuropathic pain | [42] | |
| 4 | ITI-007 | Drug Info | Phase 3 | Insomnia | [43], [44] | |
| 5 | LITOXETINE | Drug Info | Phase 3 | Mood disorder | [45] | |
| 6 | Brasofensine | Drug Info | Phase 2 | Parkinson disease | [46] | |
| 7 | CLR-3001 | Drug Info | Phase 2 | Major depressive disorder | [47] | |
| 8 | DA-8031 | Drug Info | Phase 2 | Premature ejaculation | [48] | |
| 9 | Lu-AA34893 | Drug Info | Phase 2 | Anxiety disorder | [49] | |
| 10 | MIN-117 | Drug Info | Phase 2 | Major depressive disorder | [50] | |
| 11 | NS 2359 | Drug Info | Phase 2 | Cocaine addiction | [13] | |
| 12 | TD-9855 | Drug Info | Phase 2 | Pain | [51] | |
| 13 | AD-337 | Drug Info | Phase 1 | Chemotherapy-induced nausea | [52] | |
| 14 | BGC-20-1259 | Drug Info | Phase 1 | Parkinson disease | [53] | |
| 15 | BL-1021 | Drug Info | Phase 1 | Pain | [54] | |
| 16 | GSK-1360707 | Drug Info | Phase 1 | Major depressive disorder | [55] | |
| 17 | SEP-228432 | Drug Info | Phase 1 | Neuropathic pain | [56] | |
| Discontinued Drug(s) | [+] 13 Discontinued Drugs | + | ||||
| 1 | Dexfenfluramine | Drug Info | Withdrawn from market | Obesity | [57] | |
| 2 | ZIMELIDINE | Drug Info | Withdrawn from market | Major depressive disorder | [7] | |
| 3 | DOV-216303 | Drug Info | Discontinued in Phase 2 | Mood disorder | [58] | |
| 4 | NS-2389 | Drug Info | Discontinued in Phase 2 | Major depressive disorder | [59] | |
| 5 | OxycoDex | Drug Info | Discontinued in Phase 2 | Pain | [60] | |
| 6 | R-sibutramine metabolite | Drug Info | Discontinued in Phase 2 | Attention deficit hyperactivity disorder | [58] | |
| 7 | SPD-473 | Drug Info | Discontinued in Phase 2 | Mood disorder | [61] | |
| 8 | YM-992 | Drug Info | Discontinued in Phase 2 | Depression | [62] | |
| 9 | NSD-644 | Drug Info | Discontinued in Phase 1 | Neurological disorder | [63] | |
| 10 | RG-7166 | Drug Info | Discontinued in Phase 1 | Major depressive disorder | [64] | |
| 11 | HydrocoDex | Drug Info | Terminated | Pain | [65], [66] | |
| 12 | Irindalone | Drug Info | Terminated | Inflammation | [67] | |
| 13 | MOXIFETIN HYDROGEN MALEATE | Drug Info | Terminated | Mood disorder | [68] | |
| Mode of Action | [+] 5 Modes of Action | + | ||||
| Inhibitor | [+] 262 Inhibitor drugs | + | ||||
| 1 | Acetaminophen | Drug Info | [69] | |||
| 2 | Amfepramone | Drug Info | [5], [70] | |||
| 3 | Amitriptyline | Drug Info | [71], [72] | |||
| 4 | Bupropion | Drug Info | [73] | |||
| 5 | Clomipramine | Drug Info | [76] | |||
| 6 | Cocaine | Drug Info | [77] | |||
| 7 | Dasotraline | Drug Info | [78] | |||
| 8 | Duloxetine | Drug Info | [79], [80] | |||
| 9 | Escitalopram | Drug Info | [81] | |||
| 10 | Fluvoxamine | Drug Info | [82], [83] | |||
| 11 | Sertraline | Drug Info | [1], [85] | |||
| 12 | Tianeptine | Drug Info | [8] | |||
| 13 | Venlafaxine | Drug Info | [73] | |||
| 14 | Vortioxetine | Drug Info | [37], [37], [86], [87] | |||
| 15 | Amitifadine | Drug Info | [88] | |||
| 16 | CLR-3001 | Drug Info | [92] | |||
| 17 | DA-8031 | Drug Info | [93] | |||
| 18 | MIN-117 | Drug Info | [13] | |||
| 19 | NS 2359 | Drug Info | [58], [95] | |||
| 20 | GSK-1360707 | Drug Info | [98] | |||
| 21 | SEP-228432 | Drug Info | [99] | |||
| 22 | Citalopram derivative 1 | Drug Info | [100] | |||
| 23 | Dexfenfluramine | Drug Info | [101] | |||
| 24 | ZIMELIDINE | Drug Info | [102] | |||
| 25 | DOV-216303 | Drug Info | [58] | |||
| 26 | OxycoDex | Drug Info | [65], [66] | |||
| 27 | SPD-473 | Drug Info | [105] | |||
| 28 | YM-992 | Drug Info | [106] | |||
| 29 | RG-7166 | Drug Info | [108] | |||
| 30 | 6-nitroquipazine | Drug Info | [109] | |||
| 31 | A-80426 | Drug Info | [110] | |||
| 32 | Irindalone | Drug Info | [111] | |||
| 33 | ((3R,4R)-4-(o-tolyloxy)chroman-3-yl)methanamine | Drug Info | [113] | |||
| 34 | (+/-)-3-((naphthalen-2-yloxy)methyl)pyrrolidine | Drug Info | [114] | |||
| 35 | (+/-)-nantenine | Drug Info | [115] | |||
| 36 | (2R,3R)-iodoreboxetine | Drug Info | [116] | |||
| 37 | (2R,3S)-2-[(2-Iodophenoxy)phenylmethyl]morpholine | Drug Info | [117] | |||
| 38 | (2R,3S)-2-[(3-Iodophenoxy)phenylmethyl]morpholine | Drug Info | [117] | |||
| 39 | (2R,3S)-2-[(4-Iodophenoxy)phenylmethyl]morpholine | Drug Info | [117] | |||
| 40 | (2S,3S)-iodoreboxetine | Drug Info | [116] | |||
| 41 | (cis)-1,6-diphenyl-3-aza-bicyclo[3.1.0]hexane | Drug Info | [118] | |||
| 42 | (R)-2-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol | Drug Info | [119] | |||
| 43 | (R)-3-(naphthalen-2-ylmethoxy)pyrrolidine | Drug Info | [114] | |||
| 44 | (R)-6-(pyrrolidin-3-ylmethoxy)-2-naphthonitrile | Drug Info | [114] | |||
| 45 | (R)-DULOXETINE | Drug Info | [120] | |||
| 46 | (R)-N-isobutyl-N-(pyrrolidin-3-yl)-2-naphthamide | Drug Info | [121] | |||
| 47 | (R)-N-isopropyl-N-(pyrrolidin-3-yl)-2-naphthamide | Drug Info | [121] | |||
| 48 | (R)-Norfluoxetine | Drug Info | [122] | |||
| 49 | (S)-3-(naphthalen-2-ylmethoxy)pyrrolidine | Drug Info | [114] | |||
| 50 | (S)-6-(pyrrolidin-3-ylmethoxy)-2-naphthonitrile | Drug Info | [114] | |||
| 51 | (S)-N-isobutyl-N-(pyrrolidin-3-yl)-2-naphthamide | Drug Info | [121] | |||
| 52 | (S)-NORDULOXETINE | Drug Info | [123] | |||
| 53 | (S)-Norfluoxetine | Drug Info | [122] | |||
| 54 | 1-(1,2-diphenylethyl)piperazine | Drug Info | [124] | |||
| 55 | 1-(1,3-diphenylpropyl)piperazine | Drug Info | [125] | |||
| 56 | 1-(1,4-diphenylbutan-2-yl)piperazine | Drug Info | [125] | |||
| 57 | 1-(1-(2-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) | Drug Info | [119] | |||
| 58 | 1-(1-(4-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) | Drug Info | [119] | |||
| 59 | 1-(1-phenyl-2-(2-propoxyphenyl)ethyl)piperazine | Drug Info | [119] | |||
| 60 | 1-(1-phenyl-2-(pyridin-2-yl)ethyl)piperazine | Drug Info | [125] | |||
| 61 | 1-(1-phenyl-2-(pyridin-4-yl)ethyl)piperazine | Drug Info | [125] | |||
| 62 | 1-(1-phenyl-2-o-tolylethyl)piperazine | Drug Info | [124] | |||
| 63 | 1-(2-((3-fluorophenoxy)methyl)phenyl)piperazine | Drug Info | [126] | |||
| 64 | 1-(2-(2-(DIFLUOROMETHOXY)PHENYL)-1-PHENYLETHYL)PIPERAZINE (ENANTIOMERIC MIX) | Drug Info | [119] | |||
| 65 | 1-(2-(2-bromophenyl)-1-phenylethyl)piperazine | Drug Info | [124] | |||
| 66 | 1-(2-(2-chlorophenyl)-1-phenylethyl)piperazine | Drug Info | [124] | |||
| 67 | 1-(2-(2-ethoxyphenyl)-1-phenylethyl)piperazine | Drug Info | [124] | |||
| 68 | 1-(2-(2-ethylphenyl)-1-phenylethyl)piperazine | Drug Info | [124] | |||
| 69 | 1-(2-(2-fluorobenzyloxy)phenyl)piperazine | Drug Info | [126] | |||
| 70 | 1-(2-(2-methoxyphenyl)-1-phenylethyl)piperazine | Drug Info | [119] | |||
| 71 | 1-(2-(3-chlorophenyl)-1-phenylethyl)piperazine | Drug Info | [124] | |||
| 72 | 1-(2-(3-fluorophenoxy)phenyl)piperazine | Drug Info | [126] | |||
| 73 | 1-(2-(3-methoxyphenyl)-1-phenylethyl)piperazine | Drug Info | [124] | |||
| 74 | 1-(2-(4-fluorophenoxy)phenyl)piperazine | Drug Info | [126] | |||
| 75 | 1-(2-(6-fluoronaphthalen-2-yl)ethyl)piperazine | Drug Info | [114] | |||
| 76 | 1-(2-(benzyloxy)phenyl)piperazine | Drug Info | [126] | |||
| 77 | 1-(2-(naphthalen-1-yl)-1-phenylethyl)piperazine | Drug Info | [125] | |||
| 78 | 1-(2-(naphthalen-2-yl)-1-phenylethyl)piperazine | Drug Info | [125] | |||
| 79 | 1-(2-(naphthalen-2-yl)ethyl)piperazine | Drug Info | [114] | |||
| 80 | 1-(2-(phenoxymethyl)phenyl)piperazine | Drug Info | [126] | |||
| 81 | 1-(2-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | [127] | |||
| 82 | 1-(2-phenoxyphenyl)piperazine | Drug Info | [126] | |||
| 83 | 1-(3,4-Dichloro-phenyl)-3-diethylamino-indan-5-ol | Drug Info | [128] | |||
| 84 | 1-(3,4-Dichloro-phenyl)-3-methylamino-indan-5-ol | Drug Info | [128] | |||
| 85 | 1-(3-chlorophenyl)-2-(piperidin-1-yl)propan-1-one | Drug Info | [129] | |||
| 86 | 1-(3-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | [127] | |||
| 87 | 1-(3-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | [127] | |||
| 88 | 1-(4-Benzylsulfanyl-phenyl)-propylamine | Drug Info | [130] | |||
| 89 | 1-(4-bromophenyl)-2-(tert-butylamino)propan-1-one | Drug Info | [131] | |||
| 90 | 1-(4-bromophenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | [127] | |||
| 91 | 1-(4-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | [127] | |||
| 92 | 1-(4-nitrophenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | [127] | |||
| 93 | 1-(benzofuran-2-yl)-3-aza-bicyclo[3.1.0]hexane | Drug Info | [118] | |||
| 94 | 1-(naphthalen-2-yl)-3-aza-bicyclo[3.1.0]hexane | Drug Info | [118] | |||
| 95 | 1-(thiophen-2-yl)-3-aza-bicyclo[3.1.0]hexane | Drug Info | [118] | |||
| 96 | 1-benzylpiperidine hydrochloride | Drug Info | [132] | |||
| 97 | 1-Biphenyl-4-yl-3-aza-bicyclo[3.1.0]hexane | Drug Info | [118] | |||
| 98 | 1-fluoro-5-phenyl-3-aza-bicyclo[3.1.0]hexane | Drug Info | [118] | |||
| 99 | 1-Methyl-2-(4-phenylsulfanyl-phenyl)-ethylamine | Drug Info | [130] | |||
| 100 | 1-Methyl-4-p-tolyl-piperidine-4-carbonitrile | Drug Info | [133] | |||
| 101 | 1-naphthalen-2-yl-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | [127] | |||
| 102 | 1-phenyl-3-aza-bicyclo[3.1.0]hexane | Drug Info | [118] | |||
| 103 | 10R-hydroxylobel-7-ene | Drug Info | [134] | |||
| 104 | 10R-hydroxylobelane | Drug Info | [134] | |||
| 105 | 10S-hydroxylobel-7-ene | Drug Info | [134] | |||
| 106 | 10S-hydroxylobelane | Drug Info | [134] | |||
| 107 | 1S,2R-milnacipran | Drug Info | [135] | |||
| 108 | 2-(2'-Aminoethyl)-5-benzyltetrahydrofuran | Drug Info | [136] | |||
| 109 | 2-(2-chlorophenoxy)-3-(piperidin-4-yl)pyridine | Drug Info | [137] | |||
| 110 | 2-(2-fluorophenoxy)-3-(piperidin-4-yl)pyridine | Drug Info | [137] | |||
| 111 | 2-(2-methoxyphenoxy)-3-(piperidin-4-yl)pyridine | Drug Info | [137] | |||
| 112 | 2-(2-phenyl-2-(piperazin-1-yl)ethyl)benzonitrile | Drug Info | [124] | |||
| 113 | 2-(3-Methyl-piperazin-1-yl)-6-nitro-quinoline | Drug Info | [138] | |||
| 114 | 2-(Aminomethyl)-5-(1'-naphthethyl)tetrahydrofuran | Drug Info | [136] | |||
| 115 | 2-(Aminomethyl)-5-(1'-naphthyl)tetrahydrofuran | Drug Info | [136] | |||
| 116 | 2-(Aminomethyl)-5-(2'-naphthyl)tetrahydrofuran | Drug Info | [136] | |||
| 117 | 2-(Aminomethyl)-5-phenethyltetrahydrofuran | Drug Info | [136] | |||
| 118 | 2-(N-Cyclopentylamino)-3'-methoxypropiophenone | Drug Info | [131] | |||
| 119 | 2-(N-Cyclopropylamino)-3-chloropropiophenone | Drug Info | [129] | |||
| 120 | 2-(N-tert-Butylamino)-3',4'-dichloropropiophenone | Drug Info | [129] | |||
| 121 | 2-(tert-butylamino)-1-(3-chlorophenyl)butan-1-one | Drug Info | [131] | |||
| 122 | 2-(tert-Butylamino)-3',4'-dichlorobutyrophenone | Drug Info | [129] | |||
| 123 | 2-(tert-Butylamino)-3',4'-dichloropentanophenone | Drug Info | [129] | |||
| 124 | 2-Amino-1-(4-ethylthiophenyl)butane | Drug Info | [130] | |||
| 125 | 2-Amino-1-(4-ethylthiophenyl)propane | Drug Info | [130] | |||
| 126 | 2-Amino-1-(4-methylthiophenyl)butane | Drug Info | [130] | |||
| 127 | 2-Amino-1-(4-methylthiophenyl)propane | Drug Info | [130] | |||
| 128 | 2-Aminomethyl-5-(p-bromophenyl)tetrahydrofuran | Drug Info | [136] | |||
| 129 | 2-Aminomethyl-5-(p-chlorophenyl)tetrahydrofuran | Drug Info | [136] | |||
| 130 | 2-Aminomethyl-5-(p-methoxyphenyl)tetrahydrofuran | Drug Info | [136] | |||
| 131 | 2-Aminomethyl-5-(p-t-butylphenyl)tetrahydrofuran | Drug Info | [136] | |||
| 132 | 2-Aminomethyl-5-(phenyl)tetrahydrofuran | Drug Info | [136] | |||
| 133 | 2-N,N-Dimethylamino-1-(4-methylthiophenyl)propane | Drug Info | [130] | |||
| 134 | 2-N-(Isopropyl)amino-1-(4-methylthiophenyl)butane | Drug Info | [130] | |||
| 135 | 2-N-(n-Propyl)amino-1-(4-methylthiophenyl)butane | Drug Info | [130] | |||
| 136 | 2-N-Allylamino-1-(4-methylthiophenyl)propan | Drug Info | [130] | |||
| 137 | 2-N-Cyclopropylamino-1-(4-methylthiophenyl)butane | Drug Info | [130] | |||
| 138 | 2-N-Ethylamino-1-(4-ethylthiophenyl)butane | Drug Info | [130] | |||
| 139 | 2-N-Ethylamino-1-(4-ethylthiophenyl)propane | Drug Info | [130] | |||
| 140 | 2-N-Ethylamino-1-(4-methylthiophenyl)butane | Drug Info | [130] | |||
| 141 | 2-N-Ethylamino-1-(4-methylthiophenyl)propane | Drug Info | [130] | |||
| 142 | 2-N-Hydroxyamino-1-(4-ethylthiophenyl)butane | Drug Info | [130] | |||
| 143 | 2-N-Hydroxyamino-1-(4-ethylthiophenyl)propane | Drug Info | [130] | |||
| 144 | 2-N-Hydroxyamino-1-(4-methylthiophenyl)butane | Drug Info | [130] | |||
| 145 | 2-N-Hydroxyamino-1-(4-methylthiophenyl)propane | Drug Info | [130] | |||
| 146 | 2-N-Methoxyamino-1-(4-methylthiophenyl)propane | Drug Info | [130] | |||
| 147 | 2-N-Methylamino-1-(4-ethylthiophenyl)propane | Drug Info | [130] | |||
| 148 | 2-N-Methylamino-1-(4-methylthiophenyl)butane | Drug Info | [130] | |||
| 149 | 2-N-Methylamino-1-(4-methylthiophenyl)propane | Drug Info | [130] | |||
| 150 | 2-N-Propargylamino-1-(4-methylthiophenyl)butane | Drug Info | [130] | |||
| 151 | 2-N-Propargylamino-1-(4-methylthiophenyl)propane | Drug Info | [130] | |||
| 152 | 2-Naphthalen-2-ylmethyl-4,5-dihydro-1H-imidazole | Drug Info | [110] | |||
| 153 | 2-phenoxy-3-(piperidin-4-yl)pyridine | Drug Info | [137] | |||
| 154 | 2-[1,4]Diazepan-1-yl-6-nitro-quinoline | Drug Info | [138] | |||
| 155 | 3-(1H-indol-1-yl)-N-methyl-3-phenylpropan-1-amine | Drug Info | [139] | |||
| 156 | 3-(1H-indol-3-yl)-N,N-dimethylpropan-1-amine | Drug Info | [140] | |||
| 157 | 3-(2-phenyl-2-(piperazin-1-yl)ethyl)benzamide | Drug Info | [124] | |||
| 158 | 3-(2-phenyl-2-(piperazin-1-yl)ethyl)benzonitrile | Drug Info | [124] | |||
| 159 | 3-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol | Drug Info | [124] | |||
| 160 | 3-(3,4-dichlorophenyl)-2-nortropene | Drug Info | [141] | |||
| 161 | 3-(3-aminocyclopentyl)-1H-indole-5-carbonitrile | Drug Info | [142] | |||
| 162 | 3-(4-Chlorophenyl)-2-nortropene | Drug Info | [141] | |||
| 163 | 3-(4-Fluorophenyl)-2-nortropene | Drug Info | [141] | |||
| 164 | 3-(4-Trifluoromethylphenyl)-2-nortropene | Drug Info | [141] | |||
| 165 | 3-(piperidin-4-yl)-2-(o-tolyloxy)pyridine | Drug Info | [137] | |||
| 166 | 3-alpha-Phenylmethoxy-3-beta-phenyl-nortropane | Drug Info | [141] | |||
| 167 | 3-Bromo-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | [138] | |||
| 168 | 3-p-Tolyl-8-aza-bicyclo[3.2.1]octane | Drug Info | [143] | |||
| 169 | 3-Phenyl-2-nortropene | Drug Info | [141] | |||
| 170 | 3alpha-(bis-chloro-phenylmethoxy)tropane | Drug Info | [144] | |||
| 171 | 4-((naphthalen-2-yloxy)methyl)piperidine | Drug Info | [114] | |||
| 172 | 4-(1H-indol-3-yl)-N,N-dimethylcyclohex-3-enamine | Drug Info | [145] | |||
| 173 | 4-(2-((3-fluorophenoxy)methyl)phenyl)piperidine | Drug Info | [126] | |||
| 174 | 4-(2-((dimethylamino)methyl)phenoxy)benzonitrile | Drug Info | [146] | |||
| 175 | 4-(2-(2-fluoro-5-methylphenoxy)phenyl)piperidine | Drug Info | [126] | |||
| 176 | 4-(2-(2-fluorobenzyloxy)phenyl)piperidine | Drug Info | [126] | |||
| 177 | 4-(2-(3-chlorophenoxy)phenyl)piperidine | Drug Info | [126] | |||
| 178 | 4-(2-(3-fluorophenoxy)-4-methylphenyl)piperidine | Drug Info | [126] | |||
| 179 | 4-(2-(3-fluorophenoxy)phenyl)piperidine | Drug Info | [126] | |||
| 180 | 4-(2-(4-fluorobenzyloxy)phenyl)piperidine | Drug Info | [126] | |||
| 181 | 4-(2-(4-fluorophenoxy)-4-methylphenyl)piperidine | Drug Info | [126] | |||
| 182 | 4-(2-(4-fluorophenoxy)phenyl)piperidine | Drug Info | [126] | |||
| 183 | 4-(2-(benzyloxy)-3-fluorophenyl)piperidine | Drug Info | [126] | |||
| 184 | 4-(2-(benzyloxy)-6-fluorophenyl)piperidine | Drug Info | [126] | |||
| 185 | 4-(2-(benzyloxy)phenyl)piperidine | Drug Info | [126] | |||
| 186 | 4-(2-(phenoxymethyl)phenyl)piperidine | Drug Info | [126] | |||
| 187 | 4-(2-fluoro-6-(2-fluorophenoxy)phenyl)piperidine | Drug Info | [137] | |||
| 188 | 4-(2-fluoro-6-(3-fluorophenoxy)phenyl)piperidine | Drug Info | [126] | |||
| 189 | 4-(2-fluoro-6-(4-fluorophenoxy)phenyl)piperidine | Drug Info | [126] | |||
| 190 | 4-(2-fluoro-6-phenoxyphenyl)piperidine | Drug Info | [126] | |||
| 191 | 4-(2-phenoxyphenyl)piperidine | Drug Info | [126] | |||
| 192 | 4-(3-fluoro-2-phenoxyphenyl)piperidine | Drug Info | [126] | |||
| 193 | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [147] | |||
| 194 | 4-Allyl-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | [148] | |||
| 195 | 4-Benzyl-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | [148] | |||
| 196 | 4-Bromo-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | [148] | |||
| 197 | 4-Chloro-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | [148] | |||
| 198 | 4-Furan-2-yl-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | [148] | |||
| 199 | 4-Iodo-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | [148] | |||
| 200 | 6,6-dimethyl-1-phenyl-3-aza-bicyclo[3.1.0]hexane | Drug Info | [118] | |||
| 201 | 6,8-Dinitro-2-piperazin-1-yl-quinoline | Drug Info | [138] | |||
| 202 | 6-(3-aza-bicyclo[3.1.0]hexan-1-yl)quinoline | Drug Info | [118] | |||
| 203 | 6-(piperidin-4-ylmethoxy)-2-naphthonitrile | Drug Info | [114] | |||
| 204 | 6-Bromo-2-piperazin-1-yl-quinoline | Drug Info | [138] | |||
| 205 | 6-Chloro-2-piperazin-1-yl-quinoline | Drug Info | [138] | |||
| 206 | 6-Iodo-2-piperazin-1-yl-quinoline | Drug Info | [138] | |||
| 207 | 6-Nitro-2-piperazin-1-yl-4-vinyl-quinoline | Drug Info | [148] | |||
| 208 | 6-Nitro-4-phenyl-2-piperazin-1-yl-quinoline | Drug Info | [148] | |||
| 209 | 7-(piperidin-4-ylmethoxy)-2-naphthonitrile | Drug Info | [114] | |||
| 210 | 8-Methyl-3-p-tolyl-8-aza-bicyclo[3.2.1]octane | Drug Info | [143] | |||
| 211 | 8R-hydroxylobel-9-ene | Drug Info | [149] | |||
| 212 | 8R-hydroxylobelane | Drug Info | [134] | |||
| 213 | 8S-hydroxylobel-9-ene | Drug Info | [134] | |||
| 214 | 8S-hydroxylobelane | Drug Info | [134] | |||
| 215 | Beta-methoxyamphetamine | Drug Info | [150], [130] | |||
| 216 | Biphenyl-2-ylmethyl-(S)-pyrrolidin-3-yl-amine | Drug Info | [151] | |||
| 217 | COCAINE.HCL | Drug Info | [132] | |||
| 218 | Cyclohexyl-(3,4-dichloro-phenyl)-acetonitrile | Drug Info | [152] | |||
| 219 | Cyclopentyl-(3,4-dichloro-phenyl)-acetonitrile | Drug Info | [152] | |||
| 220 | D-166A | Drug Info | [153] | |||
| 221 | D-211A | Drug Info | [153] | |||
| 222 | D-211B | Drug Info | [153] | |||
| 223 | D-254C | Drug Info | [153] | |||
| 224 | D-257A | Drug Info | [153] | |||
| 225 | D-257C | Drug Info | [153] | |||
| 226 | Difluorobenztropine | Drug Info | [144] | |||
| 227 | Erythro-3,4-dichloromethylphenidate hydrochloride | Drug Info | [132] | |||
| 228 | Isobutyl-(4-methyl-benzyl)-piperidin-4-yl-amine | Drug Info | [154] | |||
| 229 | JNJ-28583867 | Drug Info | [155] | |||
| 230 | KF-A5 | Drug Info | [156] | |||
| 231 | KF-A6 | Drug Info | [156] | |||
| 232 | MDL-28618 | Drug Info | [113] | |||
| 233 | METHYLENEDIOXYAMPHETAMINE | Drug Info | [130] | |||
| 234 | METHYLENEDIOXYMETHAMPHETAMINE | Drug Info | [157], [130] | |||
| 235 | N*1*-(6-Nitro-quinolin-2-yl)-ethane-1,2-diamine | Drug Info | [138] | |||
| 236 | N,N-dimethyl(2-phenoxyphenyl)methanamine | Drug Info | [159] | |||
| 237 | N-(2-oxazolemethyl)milnacipran | Drug Info | [160] | |||
| 238 | N-(piperidin-4-yl)-N-propyl-2-naphthamide | Drug Info | [121] | |||
| 239 | N-benzyl-N-isobutylpiperidin-4-amine | Drug Info | [154] | |||
| 240 | N-cyclobutyl-N-(piperidin-4-yl)-2-naphthamide | Drug Info | [121] | |||
| 241 | NISOXETINE | Drug Info | [120] | |||
| 242 | norzotepine | Drug Info | [161] | |||
| 243 | O-DESMETHYL TRAMADOL | Drug Info | [162] | |||
| 244 | Para-chloroamphetamine | Drug Info | [130] | |||
| 245 | PF-18298 | Drug Info | [119] | |||
| 246 | PF-3409409 | Drug Info | [163] | |||
| 247 | PF-526014 | Drug Info | [119] | |||
| 248 | PYROVALERONE | Drug Info | [127] | |||
| 249 | QUIPAZINE | Drug Info | [138] | |||
| 250 | R-226161 | Drug Info | [164] | |||
| 251 | R-NORDULOXETINE | Drug Info | [123] | |||
| 252 | RTI-219 | Drug Info | [165] | |||
| 253 | S-34324 | Drug Info | [166] | |||
| 254 | S33005 | Drug Info | [106] | |||
| 255 | TEFLUDAZINE | Drug Info | [167] | |||
| 256 | Threo-1-aza-5-phenyl[4.4.0]decane hydrochloride | Drug Info | [132] | |||
| 257 | Threo-3,4-dichlororitalinol hydrochloride | Drug Info | [132] | |||
| 258 | Trans-3-(o-tolyloxy)-2,3-dihydro-1H-inden-1-amine | Drug Info | [168] | |||
| 259 | WIN-35065 | Drug Info | [165] | |||
| 260 | WIN-35066-2 | Drug Info | [169] | |||
| 261 | [3-(3,4-Dichloro-phenyl)-indan-1-yl]-methyl-amine | Drug Info | [128] | |||
| 262 | [3H]WIN35428 | Drug Info | [170] | |||
| Modulator | [+] 25 Modulator drugs | + | ||||
| 1 | Chlorphentermine Hydrochloride | Drug Info | [74] | |||
| 2 | Citalopram | Drug Info | [75] | |||
| 3 | Desvenlafaxine | Drug Info | [15] | |||
| 4 | Dextromethorphan Polistirex | Drug Info | [75] | |||
| 5 | Fluoxetine | Drug Info | [75] | |||
| 6 | Levomilnacipran | Drug Info | [22] | |||
| 7 | Luvox | Drug Info | [84] | |||
| 8 | Nortriptyline | Drug Info | [75] | |||
| 9 | Paroxetine | Drug Info | [75] | |||
| 10 | Sibutramine | Drug Info | [75] | |||
| 11 | Trazodone | Drug Info | [75] | |||
| 12 | Vilazodone | Drug Info | [35] | |||
| 13 | AVP-786 | Drug Info | [65], [66] | |||
| 14 | Bicifadine | Drug Info | [89] | |||
| 15 | LITOXETINE | Drug Info | [91] | |||
| 16 | Brasofensine | Drug Info | [46] | |||
| 17 | Lu-AA34893 | Drug Info | [94] | |||
| 18 | TD-9855 | Drug Info | [51] | |||
| 19 | AD-337 | Drug Info | [84] | |||
| 20 | BGC-20-1259 | Drug Info | [96] | |||
| 21 | BL-1021 | Drug Info | [97] | |||
| 22 | NS-2389 | Drug Info | [103] | |||
| 23 | R-sibutramine metabolite | Drug Info | [104] | |||
| 24 | HydrocoDex | Drug Info | [65], [66] | |||
| 25 | MMDA | Drug Info | [158] | |||
| Antagonist | [+] 1 Antagonist drugs | + | ||||
| 1 | ITI-007 | Drug Info | [90] | |||
| Activator | [+] 1 Activator drugs | + | ||||
| 1 | NSD-644 | Drug Info | [107] | |||
| Binder | [+] 1 Binder drugs | + | ||||
| 1 | CX-1001 | Drug Info | [88] | |||
| Cell-based Target Expression Variations | Top | |||||
|---|---|---|---|---|---|---|
| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Paroxetine | Ligand Info | |||||
| Structure Description | X-ray structure of the ts3 human serotonin transporter complexed with paroxetine at the central site | PDB:5I6X | ||||
| Method | X-ray diffraction | Resolution | 3.14 Å | Mutation | Yes | [171] |
| PDB Sequence |
GSQGERETWG
83 KKVDFLLSVI93 GYAVDLGNVW103 RFPYICAQNG113 GGAFLLPYTI123 MAIFGGIPLF 133 YMELALGQYH143 RNGCISIWRK153 ICPIFKGIGY163 AICIIAFYIA173 SYYNTIMAWA 183 LYYLISSFTD193 QLPWTSCKNS203 WNTGNCTNYF213 SEDNITWTLH223 STSPAEEFYT 233 RHVLQIHRSK243 GLQDLGGISW253 QLALCIMLIF263 TVIYFSIWKG273 VKTSGKVVWV 283 TATFPYIALS293 VLLVRGATLP303 GAWRGVLFYL313 KPNWQKLLET323 GVWIDAAAQI 333 FFSLGPGFGV343 LLAFASYNKF353 NNNCYQDALV363 TSVVNCMTSF373 VSGFVIFTVL 383 GYMAEMRNED393 VSEVAKDAGP403 SLLFITYAEA413 IANMPASTFF423 AIIFFLMLIT 433 LGLDSSFAGL443 EGVITAVLDE453 FPHVWAKRRE463 RFVLAVVITC473 FFGSLVTLTF 483 GGAYVVKLLE493 EYATGPAVLT503 VALIEAVAVS513 WFYGITQFCR523 DVKEMLGFSP 533 GWFWRICWVA543 ISPLFLLFII553 ASFLMSPPQL563 RLFQYNYPYW573 SIILGYAIGT 583 SSFICIPTYI593 AYRLIITPGT603 FKERIIKSIT613 PETP
|
|||||
|
|
TYR95
3.187
ALA96
3.157
VAL97
4.680
ASP98
3.088
ASN101
4.996
ILE168
4.867
ALA169
3.444
ILE172
3.234
ALA173
4.020
TYR176
3.733
PHE335
3.239
|
|||||
| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: Escitalopram | Ligand Info | |||||
| Structure Description | X-ray structure of the ts3 human serotonin transporter complexed with s-citalopram at the central site | PDB:5I71 | ||||
| Method | X-ray diffraction | Resolution | 3.15 Å | Mutation | Yes | [171] |
| PDB Sequence |
GSQGERETWG
83 KKVDFLLSVI93 GYAVDLGNVW103 RFPYICAQNG113 GGAFLLPYTI123 MAIFGGIPLF 133 YMELALGQYH143 RNGCISIWRK153 ICPIFKGIGY163 AICIIAFYIA173 SYYNTIMAWA 183 LYYLISSFTD193 QLPWTSCKNS203 WNTGNCTNYF213 SEDNITWTLH223 STSPAEEFYT 233 RHVLQIHRSK243 GLQDLGGISW253 QLALCIMLIF263 TVIYFSIWKG273 VKTSGKVVWV 283 TATFPYIALS293 VLLVRGATLP303 GAWRGVLFYL313 KPNWQKLLET323 GVWIDAAAQI 333 FFSLGPGFGV343 LLAFASYNKF353 NNNCYQDALV363 TSVVNCMTSF373 VSGFVIFTVL 383 GYMAEMRNED393 VSEVAKDAGP403 SLLFITYAEA413 IANMPASTFF423 AIIFFLMLIT 433 LGLDSSFAGL443 EGVITAVLDE453 FPHVWAKRRE463 RFVLAVVITC473 FFGSLVTLTF 483 GGAYVVKLLE493 EYATGPAVLT503 VALIEAVAVS513 WFYGITQFCR523 DVKEMLGFSP 533 GWFWRICWVA543 ISPLFLLFII553 ASFLMSPPQL563 RLFQYNYPYW573 SIILGYAIGT 583 SSFICIPTYI593 AYRLIITPGT603 FKERIIKSIT613 PE
|
|||||
|
|
TYR95
3.241
ALA96
2.873
VAL97
4.796
ASP98
3.007
ASN101
4.894
ALA169
4.107
ILE172
3.427
ALA173
3.646
TYR175
3.961
TYR176
4.155
PHE335
2.918
|
|||||
| 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
|
|
|
There is no similarity protein (E value < 0.005) for this target
|
|
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 |
|---|---|---|---|
| Synaptic vesicle cycle | hsa04721 | Affiliated Target |
|
| Class: Organismal Systems => Nervous system | Pathway Hierarchy | ||
| Serotonergic synapse | hsa04726 | Affiliated Target |
|
| Class: Organismal Systems => Nervous system | Pathway Hierarchy | ||
| Degree | 2 | Degree centrality | 2.15E-04 | Betweenness centrality | 8.36E-06 |
|---|---|---|---|---|---|
| Closeness centrality | 1.74E-01 | Radiality | 1.28E+01 | Clustering coefficient | 0.00E+00 |
| Neighborhood connectivity | 1.80E+01 | Topological coefficient | 5.00E-01 | Eccentricity | 13 |
| 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-interacting Proteins | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 1 KEGG Pathways | + | ||||
| 1 | Serotonergic synapse | |||||
| NetPath Pathway | [+] 1 NetPath Pathways | + | ||||
| 1 | TCR Signaling Pathway | |||||
| Panther Pathway | [+] 4 Panther Pathways | + | ||||
| 1 | 5HT1 type receptor mediated signaling pathway | |||||
| 2 | 5HT2 type receptor mediated signaling pathway | |||||
| 3 | 5HT3 type receptor mediated signaling pathway | |||||
| 4 | 5HT4 type receptor mediated signaling pathway | |||||
| WikiPathways | [+] 5 WikiPathways | + | ||||
| 1 | Monoamine Transport | |||||
| 2 | SIDS Susceptibility Pathways | |||||
| 3 | NRF2 pathway | |||||
| 4 | Synaptic Vesicle Pathway | |||||
| 5 | Serotonin Transporter Activity | |||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Psychopharmacological treatment of dermatological patients--when simply talking does not help. J Dtsch Dermatol Ges. 2007 Dec;5(12):1101-6. | |||||
| REF 2 | The Diversion of Ultram, Ultracet, and generic tramadol HCL. J Addict Dis. 2006;25(2):53-8. | |||||
| REF 3 | 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: 5239). | |||||
| REF 4 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 018337. | |||||
| REF 5 | Pharmacotherapy for obesity. Drugs. 2005;65(10):1391-418. | |||||
| REF 6 | 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: 200). | |||||
| REF 7 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 8 | Emerging treatments for depression. Expert Opin Pharmacother. 2006 Dec;7(17):2323-39. | |||||
| 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: 7547). | |||||
| REF 10 | 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: 2398). | |||||
| 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: 2286). | |||||
| REF 12 | Drug information of Cocaine, 2008. eduDrugs. | |||||
| REF 13 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 14 | 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: 7158). | |||||
| REF 15 | 2008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6. | |||||
| 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: 202). | |||||
| REF 17 | 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: 203). | |||||
| REF 18 | Anti-obesity drugs and neural circuits of feeding. Trends Pharmacol Sci. 2008 Apr;29(4):208-17. | |||||
| REF 19 | 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: 7189). | |||||
| REF 20 | Autism spectrum disorders: emerging pharmacotherapy. Expert Opin Emerg Drugs. 2005 Aug;10(3):521-36. | |||||
| REF 21 | 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: 7435). | |||||
| REF 22 | Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92. | |||||
| REF 23 | ClinicalTrials.gov (NCT00743834) Cost-Effectiveness of Adding Web-Based Cognitive-Behavioral Therapy (CBT) to Luvox CR for Obsessive Compulsive Disorder (OCD). U.S. National Institutes of Health. | |||||
| REF 24 | 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: 2404). | |||||
| REF 25 | 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: 4790). | |||||
| REF 26 | Emerging drug therapies in Huntington's disease. Expert Opin Emerg Drugs. 2009 Jun;14(2):273-97. | |||||
| REF 27 | 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: 4798). | |||||
| REF 28 | 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: 2586). | |||||
| REF 29 | Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50. | |||||
| REF 30 | 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: 7558). | |||||
| REF 31 | 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: 213). | |||||
| REF 32 | 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: 7321). | |||||
| REF 33 | Desvenlafaxine in the treatment of major depressive disorder. Neuropsychiatr Dis Treat. 2009;5:127-36. | |||||
| REF 34 | 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: 7427). | |||||
| REF 35 | 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4. | |||||
| REF 36 | 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: 7351). | |||||
| REF 37 | Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651. | |||||
| REF 38 | DOV 216,303, a "triple" reuptake inhibitor: safety, tolerability, and pharmacokinetic profile. J Clin Pharmacol. 2004 Dec;44(12):1360-7. | |||||
| REF 39 | Preclinical and clinical pharmacology of DOV 216,303, a "triple" reuptake inhibitor. CNS Drug Rev. 2006 Summer;12(2):123-34. | |||||
| REF 40 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 41 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 42 | Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26. | |||||
| REF 43 | ClinicalTrials.gov (NCT02469155) A Trial to Assess the Antipsychotic Efficacy of ITI-007 Over 6 Weeks of Treatment. | |||||
| REF 44 | Clinical pipeline report, company report or official report of Intra-Cellular Therapies. | |||||
| 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 800001264) | |||||
| REF 46 | Brasofensine NeuroSearch. Curr Opin Investig Drugs. 2000 Dec;1(4):504-7. | |||||
| 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 800032468) | |||||
| REF 48 | ClinicalTrials.gov (NCT01798667) Clinical Trial to Evaluate the Efficacy and Safety of DA-8031 in Male Patients With Premature Ejaculation. U.S. National Institutes of Health. | |||||
| REF 49 | ClinicalTrials.gov (NCT00622245) Efficacy and Safety of Lu AA34893 in Patients With Bipolar Depression. U.S. National Institutes of Health. | |||||
| REF 50 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800037483) | |||||
| REF 51 | Preclinical to clinical translation of CNS transporter occupancy of TD-9855, a novel norepinephrine and serotonin reuptake inhibitor. Int J Neuropsychopharmacol. 2014 Dec 13;18(2). pii: pyu027. | |||||
| REF 52 | Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006 Mar;11(1):137-51. | |||||
| REF 53 | Pharmacological characterization of RS-1259, an orally active dual inhibitor of acetylcholinesterase and serotonin transporter, in rodents: possible treatment of Alzheimer's disease. J Pharmacol Sci.2003 Sep;93(1):95-105. | |||||
| REF 54 | ClinicalTrials.gov (NCT01121380) A Study Intended to Evaluate Safety, Tolerability and Pharmacokinetics (PK) Parameters of BL-1021. U.S. National Institutes of Health. | |||||
| REF 55 | ClinicalTrials.gov (NCT01153802) An Open Label Positron Emission Tomography Study in Healthy Male Subjects to Investigate Brain DAT and SERT Occupancy,Pharmacokinetics and Safety of Single Oral Dosesof GSK1360707, Using 11C- PE2I and 11C-DASB as PET Ligands. U.S. National Institutes of Health. | |||||
| REF 56 | ClinicalTrials.gov (NCT01531972) A Phase 1, Open-Label, Single-photon Emission Computed Tomography (SPECT) Study to Evaluate Serotonin and Dopamine Transporter Occupancy After Multiple Dose Administration of SEP-228432 to Achieve Steady State in Healthy Subjects. U.S. National Institutes of Health. | |||||
| REF 57 | Obesity: pathophysiology and clinical management. Curr Med Chem. 2009;16(4):506-21. | |||||
| REF 58 | Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. | |||||
| REF 59 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009012) | |||||
| REF 60 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017613) | |||||
| REF 61 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010517) | |||||
| REF 62 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008166) | |||||
| REF 63 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027571) | |||||
| REF 64 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031598) | |||||
| REF 65 | Antitussives and substance abuse. Subst Abuse Rehabil. 2013 Nov 6;4:75-82. | |||||
| REF 66 | Dextromethorphan antagonizes the acute depletion of brain serotonin by p-chloroamphetamine and H75/12 in rats. Brain Res. 1992 Oct 30;594(2):323-6. | |||||
| REF 67 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000378) | |||||
| REF 68 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001731) | |||||
| REF 69 | Augmentation effect of combination therapy of aripiprazole and antidepressants on forced swimming test in mice. Psychopharmacology (Berl). 2009 Sep;206(1):97-107. | |||||
| REF 70 | Phentermine and anaesthesia. Anaesth Intensive Care. 2005 Aug;33(4):525-7. | |||||
| REF 71 | Treatment of comorbid pain with serotonin norepinephrine reuptake inhibitors. CNS Spectr. 2008 Jul;13(7 Suppl 11):22-6. | |||||
| REF 72 | A non-selective (amitriptyline), but not a selective (citalopram), serotonin reuptake inhibitor is effective in the prophylactic treatment of chronic tension-type headache. J Neurol Neurosurg Psychiatry. 1996 Sep;61(3):285-90. | |||||
| REF 73 | Clinically relevant drug interactions with new generation antidepressants and antipsychotics. Ther Umsch. 2009 Jun;66(6):485-92. | |||||
| REF 74 | Aminorex, fenfluramine, and chlorphentermine are serotonin transporter substrates.Implications for primary pulmonary hypertension.Circulation.1999 Aug 24;100(8):869-75. | |||||
| REF 75 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
| REF 76 | Efficacy of treatments for patients with obsessive-compulsive disorder: a systematic review. J Am Acad Nurse Pract. 2009 Apr;21(4):207-13. | |||||
| REF 77 | Differential involvement of the norepinephrine, serotonin and dopamine reuptake transporter proteins in cocaine-induced taste aversion. Pharmacol Biochem Behav. 2009 Jul;93(1):75-81. | |||||
| REF 78 | Dasotraline for the Treatment of Attention-Deficit/Hyperactivity Disorder: A Randomized, Double-Blind, Placebo-Controlled, Proof-of-Concept Trial in Adults. Neuropsychopharmacology. 2015 Nov;40(12):2745-52. | |||||
| REF 79 | Multi-target therapeutics: when the whole is greater than the sum of the parts. Drug Discov Today. 2007 Jan;12(1-2):34-42. | |||||
| REF 80 | Duloxetine for the treatment of generalized anxiety disorder: a review. Neuropsychiatr Dis Treat. 2009;5:23-31. | |||||
| REF 81 | Antidepressants and sleep: a review. Perspect Psychiatr Care. 2009 Jul;45(3):191-7. | |||||
| REF 82 | Changes of functional MRI findings in a patient whose pathological gambling improved with fluvoxamine. Yonsei Med J. 2009 Jun 30;50(3):441-4. | |||||
| REF 83 | Placebo controlled double-blind trial of fluvoxamine maleate in the obese. J Psychosom Res. 1986;30(2):143-6. | |||||
| REF 84 | Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41. | |||||
| REF 85 | Methadone: from pharmacokinetic profile to clinical pharmacology. Encephale. 2006 Jul-Aug;32(4 Pt 1):478-86. | |||||
| REF 86 | Vortioxetine (Lu AA21004), a novel multimodal antidepressant, enhances memory in rats. Pharmacol Biochem Behav. 2013 Apr;105:41-50. | |||||
| REF 87 | A double-blind, randomized, placebo-controlled, active reference study of Lu AA21004 in patients with major depressive disorder. Int J Neuropsychopharmacol. 2012 Jun;15(5):589-600. | |||||
| REF 88 | 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: 928). | |||||
| REF 89 | Preclinical Evaluation of the Abuse Potential of the Analgesic Bicifadine | |||||
| REF 90 | Clinical pipeline report, company report or official report of Intra-Cellular Therapies, Inc. | |||||
| REF 91 | Litoxetine: a selective 5-HT uptake inhibitor with concomitant 5-HT3 receptor antagonist and antiemetic properties. Eur J Pharmacol. 1993 Mar 2;232(2-3):139-45. | |||||
| REF 92 | Clinical pipeline report, company report or official report of Clera Inc. | |||||
| REF 93 | Effect of DA-8031, a novel oral compound for premature ejaculation, on male rat sexual behavior. Int J Urol. 2014 Mar;21(3):325-9. | |||||
| REF 94 | Encyclopedia of Psychopharmacology. Ian Stolerman. 2010. Page(105). | |||||
| REF 95 | Emerging drugs for attention-deficit/hyperactivity disorder. Expert Opin Emerg Drugs. 2007 Sep;12(3):423-34. | |||||
| REF 96 | Bifeprunox: a partial agonist at dopamine D2 and serotonin 1A receptors, influences nicotine-seeking behaviour in response to drug-associated stimuli in rats.Addict Biol.2012 Mar;17(2):274-86. | |||||
| REF 97 | Company report (BioLineRx) | |||||
| REF 98 | Monoamine transporter occupancy of a novel triple reuptake inhibitor in baboons and humans using positron emission tomography. J Pharmacol Exp Ther. 2013 Aug;346(2):311-7. | |||||
| REF 99 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028715) | |||||
| REF 100 | Progress in the development of histamine H3 receptor antagonists/inverse agonists: a patent review (2013-2017).Expert Opin Ther Pat. 2018 Mar;28(3):175-196. | |||||
| REF 101 | Serotonergic drugs : effects on appetite expression and use for the treatment of obesity. Drugs. 2007;67(1):27-55. | |||||
| REF 102 | Nontricyclic antidepressant agents derived from cis- and trans-1-amino-4-aryltetralins. J Med Chem. 1984 Nov;27(11):1508-15. | |||||
| REF 103 | Clinical pipeline report, company report or official report of Neurosearch. | |||||
| REF 104 | Monoamine reuptake site occupancy of sibutramine: Relationship to antidepressant-like and thermogenic effects in rats.Eur J Pharmacol.2014 Aug 15;737:47-56. | |||||
| REF 105 | Dopamine uptake inhibitor-induced rotation in 6-hydroxydopamine-lesioned rats involves both D1 and D2 receptors but is modulated through 5-hydroxyt... J Pharmacol Exp Ther. 2005 Mar;312(3):1124-31. | |||||
| REF 106 | Serotonin reuptake inhibitors: the corner stone in treatment of depression for half a century--a medicinal chemistry survey. Curr Top Med Chem. 2006;6(17):1801-23. | |||||
| REF 107 | NSD-644: Phase I started.NeuroSearch A/S (CSE:NEUR), Ballerup, Denmark, GlaxoSmithKline plc (LSE:GSK; GSK), London, U.K. | |||||
| REF 108 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031598) | |||||
| REF 109 | Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 5: 2'-Substituted 6-nitroquipazines. Bioorg Med Chem. 2007 May 15;15(10):3499-504. | |||||
| REF 110 | Structure-activity studies for a novel series of N-(arylethyl)-N-(1,2,3,4-tetrahydronaphthalen-1-ylmethyl)-N-methylamine s possessing dual 5-HT upt... J Med Chem. 1997 Mar 28;40(7):1049-62. | |||||
| REF 111 | Antihypertensive activity in a series of 1-piperazino-3-phenylindans with potent 5-HT2-antagonistic activity. J Med Chem. 1988 Dec;31(12):2247-56. | |||||
| REF 112 | Moxidectin causes adult worm mortality of human lymphatic filarial parasite Brugia malayi in rodent models. Folia Parasitol (Praha). 2014 Dec;61(6):561-70. | |||||
| REF 113 | Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with a heterocyclic ring constraint. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4495-8. | |||||
| REF 114 | Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2329-32. | |||||
| REF 115 | Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. | |||||
| REF 116 | New iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter. Bioorg Med Chem Lett. 2008 Sep 15;18(18):4940-3. | |||||
| REF 117 | Design and synthesis of (2R,3S)-iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter. Bioorg Med Chem Lett. 2009 Sep 1;19(17):4996-8. | |||||
| REF 118 | Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors. Bioorg Med Chem Lett. 2008 Jul 1;18(13):3682-6. | |||||
| REF 119 | Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reduc... Bioorg Med Chem Lett. 2010 Jun 15;20(12):3788-92. | |||||
| REF 120 | 1-Naphthyl and 4-indolyl arylalkylamines as selective monoamine reuptake inhibitors. Bioorg Med Chem Lett. 2009 Jan 1;19(1):58-61. | |||||
| REF 121 | Bioorg Med Chem Lett. 2009 Oct 15;19(20):5893-7. Epub 2009 Aug 21.Design and optimisation of selective serotonin re-uptake inhibitors with high synthetic accessibility: part 2. | |||||
| REF 122 | Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression. Bioorg Med Chem. 2009 Jan 1;17(1):337-43. | |||||
| REF 123 | Inhibition of serotonin and norepinephrine reuptake and inhibition of phosphodiesterase by multi-target inhibitors as potential agents for depression. Bioorg Med Chem. 2009 Oct 1;17(19):6890-7. | |||||
| REF 124 | N-(1,2-diphenylethyl)piperazines: a new class of dual serotonin/noradrenaline reuptake inhibitor. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4345-8. | |||||
| REF 125 | Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4349-53. | |||||
| REF 126 | Discovery and pharmacological characterization of aryl piperazine and piperidine ethers as dual acting norepinephrine reuptake inhibitors and 5-HT1... Bioorg Med Chem Lett. 2009 Dec 1;19(23):6604-7. | |||||
| REF 127 | 1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors. J Med Chem. 2006 Feb 23;49(4):1420-32. | |||||
| REF 128 | Synthesis and pharmacological evaluation of 3-(3,4-dichlorophenyl)-1-indanamine derivatives as nonselective ligands for biogenic amine transporters. J Med Chem. 2004 May 6;47(10):2624-34. | |||||
| REF 129 | Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction. J Med Chem. 2009 Nov 12;52(21):6768-81. | |||||
| REF 130 | Synthesis and serotonin transporter activity of sulphur-substituted alpha-alkyl phenethylamines as a new class of anticancer agents. Eur J Med Chem. 2009 Dec;44(12):4862-88. | |||||
| REF 131 | Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for smoking cessation. J Med Chem. 2010 Mar 11;53(5):2204-14. | |||||
| REF 132 | Synthesis and pharmacology of site-specific cocaine abuse treatment agents: restricted rotation analogues of methylphenidate. J Med Chem. 2007 May 31;50(11):2718-31. | |||||
| REF 133 | Synthesis, dopamine and serotonin transporter binding affinities of novel analogues of meperidine. Bioorg Med Chem Lett. 1999 Dec 6;9(23):3273-6. | |||||
| REF 134 | Des-keto lobeline analogs with increased potency and selectivity at dopamine and serotonin transporters. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5018-21. | |||||
| REF 135 | Characterization of thien-2-yl 1S,2R-milnacipran analogues as potent norepinephrine/serotonin transporter inhibitors for the treatment of neuropath... J Med Chem. 2008 Nov 27;51(22):7265-72. | |||||
| REF 136 | 2,5-Disubstituted tetrahydrofurans as selective serotonin re-uptake inhibitors. Bioorg Med Chem. 2009 Mar 1;17(5):2047-68. | |||||
| REF 137 | Design, synthesis, and pharmacological evaluation of phenoxy pyridyl derivatives as dual norepinephrine reuptake inhibitors and 5-HT1A partial agon... Bioorg Med Chem Lett. 2010 Feb 1;20(3):1114-7. | |||||
| REF 138 | Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 1. Bioorg Med Chem Lett. 2000 Jul 17;10(14):1559-62. | |||||
| REF 139 | Synthesis and activity of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6067-70. | |||||
| REF 140 | Conformationally restricted homotryptamines. Part 4: Heterocyclic and naphthyl analogs of a potent selective serotonin reuptake inhibitor. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5647-51. | |||||
| REF 141 | Synthesis and monoamine transporter affinity of 3alpha-arylmethoxy-3beta-arylnortropanes. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6865-8. | |||||
| REF 142 | Conformationally restricted homotryptamines. Part 7: 3-cis-(3-aminocyclopentyl)indoles as potent selective serotonin reuptake inhibitors. J Med Chem. 2010 Nov 11;53(21):7564-72. | |||||
| REF 143 | 3alpha-(4-Substituted phenyl)nortropane-2beta-carboxylic acid methyl esters show selective binding at the norepinephrine transporter. Bioorg Med Chem Lett. 2000 Nov 6;10(21):2445-7. | |||||
| REF 144 | Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogue... J Med Chem. 2006 Oct 19;49(21):6391-9. | |||||
| REF 145 | Conformationally restricted homotryptamines 3. Indole tetrahydropyridines and cyclohexenylamines as selective serotonin reuptake inhibitors. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3099-104. | |||||
| REF 146 | Designing rapid onset selective serotonin re-uptake inhibitors. 2: structure-activity relationships of substituted (aryl)benzylamines. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4018-21. | |||||
| REF 147 | 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 148 | Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 2: 4-substituted 6-nitroquipazines. Bioorg Med Chem Lett. 2002 Mar 11;12(5):811-5. | |||||
| REF 149 | Lobeline esters as novel ligands for neuronal nicotinic acetylcholine receptors and neurotransmitter transporters. Bioorg Med Chem. 2010 Jan 15;18(2):640-9. | |||||
| REF 150 | Differential behavioural and neurochemical effects of para-methoxyamphetamine and 3,4-methylenedioxymethamphetamine in the rat. Prog Neuropsychopharmacol Biol Psychiatry. 2000 Aug;24(6):955-77. | |||||
| REF 151 | Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modu... Bioorg Med Chem Lett. 2008 Aug 1;18(15):4355-9. | |||||
| REF 152 | Synthesis and evaluation of dopamine and serotonin transporter inhibition by oxacyclic and carbacyclic analogues of methylphenidate. J Med Chem. 2003 Apr 10;46(8):1538-45. | |||||
| REF 153 | Further structural optimization of cis-(6-benzhydryl-piperidin-3-yl)-benzylamine and 1,4-diazabicyclo[3.3.1]nonane derivatives by introducing an ex... Bioorg Med Chem. 2008 Mar 15;16(6):2769-78. | |||||
| REF 154 | N-Alkyl-N-arylmethylpiperidin-4-amines: novel dual inhibitors of serotonin and norepinephrine reuptake. Bioorg Med Chem Lett. 2006 May 15;16(10):2714-8. | |||||
| REF 155 | Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors. Bioorg Med Chem Lett. 2008 Jan 1;18(1):39-43. | |||||
| REF 156 | Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. Antimicrob Agents Chemother. 2007 Nov;51(11):4133-40. | |||||
| REF 157 | The origin of MDMA (ecstasy) revisited: the true story reconstructed from the original documents. Addiction. 2006 Sep;101(9):1241-5. | |||||
| REF 158 | How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | |||||
| REF 159 | 1-(2-Phenoxyphenyl)methanamines: SAR for dual serotonin/noradrenaline reuptake inhibition, metabolic stability and hERG affinity. Bioorg Med Chem Lett. 2008 Jan 15;18(2):596-9. | |||||
| REF 160 | Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1346-9. | |||||
| REF 161 | Norzotepine, a major metabolite of zotepine, exerts atypical antipsychotic-like and antidepressant-like actions through its potent inhibition of norepinephrine reuptake. J Pharmacol Exp Ther. 2010 Jun;333(3):772-81. | |||||
| REF 162 | Derivatives of tramadol for increased duration of effect. Bioorg Med Chem Lett. 2006 Feb;16(3):691-4. | |||||
| REF 163 | Design, synthesis and evaluation of N-[(3S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more po... Bioorg Med Chem Lett. 2009 Aug 15;19(16):4579-83. | |||||
| REF 164 | Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-a... Bioorg Med Chem. 2007 Jun 1;15(11):3649-60. | |||||
| REF 165 | Synthesis, monoamine transporter binding, properties, and functional monoamine uptake activity of 3beta-[4-methylphenyl and 4-chlorophenyl]-2 beta-... J Med Chem. 2007 Jul 26;50(15):3686-95. | |||||
| REF 166 | Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking... J Med Chem. 2005 Mar 24;48(6):2054-71. | |||||
| REF 167 | Neuroleptic activity and dopamine-uptake inhibition in 1-piperazino-3-phenylindans. J Med Chem. 1983 Jul;26(7):935-47. | |||||
| REF 168 | Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI). Bioorg Med Chem Lett. 2008 Jul 15;18(14):4224-7. | |||||
| REF 169 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl e... J Med Chem. 2004 Dec 2;47(25):6401-9. | |||||
| REF 170 | 3 alpha-(4'-substituted phenyl)tropane-2 beta-carboxylic acid methyl esters: novel ligands with high affinity and selectivity at the dopamine trans... J Med Chem. 1996 Oct 11;39(21):4139-41. | |||||
| REF 171 | X-ray structures and mechanism of the human serotonin transporter. Nature. 2016 Apr 21;532(7599):334-9. | |||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.