Target Information
Target General Information | Top | |||||
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Target ID |
T27812
(Former ID: TTDC00255)
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Target Name |
Serotonin transporter (SERT)
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Synonyms |
Solute carrier family 6 member 4; HTT; 5HTT; 5HT transporter
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Gene Name |
SLC6A4
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Target Type |
Successful target
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[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.
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BioChemical Class |
Neurotransmitter:sodium symporter
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UniProt ID | ||||||
Sequence |
METTPLNSQKQLSACEDGEDCQENGVLQKVVPTPGDKVESGQISNGYSAVPSPGAGDDTR
HSIPATTTTLVAELHQGERETWGKKVDFLLSVIGYAVDLGNVWRFPYICYQNGGGAFLLP YTIMAIFGGIPLFYMELALGQYHRNGCISIWRKICPIFKGIGYAICIIAFYIASYYNTIM AWALYYLISSFTDQLPWTSCKNSWNTGNCTNYFSEDNITWTLHSTSPAEEFYTRHVLQIH RSKGLQDLGGISWQLALCIMLIFTVIYFSIWKGVKTSGKVVWVTATFPYIILSVLLVRGA TLPGAWRGVLFYLKPNWQKLLETGVWIDAAAQIFFSLGPGFGVLLAFASYNKFNNNCYQD ALVTSVVNCMTSFVSGFVIFTVLGYMAEMRNEDVSEVAKDAGPSLLFITYAEAIANMPAS TFFAIIFFLMLITLGLDSTFAGLEGVITAVLDEFPHVWAKRRERFVLAVVITCFFGSLVT LTFGGAYVVKLLEEYATGPAVLTVALIEAVAVSWFYGITQFCRDVKEMLGFSPGWFWRIC WVAISPLFLLFIICSFLMSPPQLRLFQYNYPYWSIILGYCIGTSSFICIPTYIAYRLIIT PGTFKERIIKSITPETPTEIPCGDIRLNAV Click to Show/Hide
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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 | |||||
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Approved Drug(s) | [+] 19 Approved Drugs | + | ||||
1 | Amfepramone | Drug Info | Approved | Obesity | [13] | |
2 | Chlorphentermine Hydrochloride | Drug Info | Approved | Appetite suppressant | [3] | |
3 | Cocaine | Drug Info | Approved | Anaesthesia | [3], [14], [15] | |
4 | Desvenlafaxine | Drug Info | Approved | Major depressive disorder | [16], [17] | |
5 | Dextromethorphan Polistirex | Drug Info | Approved | Dry cough | [3] | |
6 | Duloxetine | Drug Info | Approved | Depression | [18], [5] | |
7 | Escitalopram | Drug Info | Approved | Major depressive disorder | [3] | |
8 | Fluoxetine | Drug Info | Approved | Depression | [19], [20] | |
9 | Fluvoxamine | Drug Info | Approved | Depression | [21], [22] | |
10 | Levomilnacipran | Drug Info | Approved | Fibromyalgia | [23], [24] | |
11 | Luvox | Drug Info | Approved | Anxiety disorder | [25] | |
12 | Nortriptyline | Drug Info | Approved | Depression | [26], [5] | |
13 | Paroxetine | Drug Info | Approved | Depression | [27], [28] | |
14 | Sertraline | Drug Info | Approved | Depression | [29], [5] | |
15 | Sibutramine | Drug Info | Approved | Obesity | [30], [31] | |
16 | Tianeptine | Drug Info | Approved | Major depressive disorder | [3], [5], [32] | |
17 | Trazodone | Drug Info | Approved | Depression | [33], [5] | |
18 | Venlafaxine | Drug Info | Approved | Depression | [34], [35] | |
19 | Vortioxetine | Drug Info | Approved | Major depressive disorder | [36], [37] | |
Clinical Trial Drug(s) | [+] 15 Clinical Trial Drugs | + | ||||
1 | Amitifadine | Drug Info | Phase 3 | Obesity | [40], [41] | |
2 | Bicifadine | Drug Info | Phase 3 | Neuropathic pain | [42] | |
3 | ITI-007 | Drug Info | Phase 3 | Insomnia | [43], [44] | |
4 | LITOXETINE | Drug Info | Phase 3 | Mood disorder | [45] | |
5 | Brasofensine | Drug Info | Phase 2 | Parkinson disease | [47] | |
6 | CLR-3001 | Drug Info | Phase 2 | Major depressive disorder | [48] | |
7 | DA-8031 | Drug Info | Phase 2 | Premature ejaculation | [49] | |
8 | Lu-AA34893 | Drug Info | Phase 2 | Anxiety disorder | [50] | |
9 | NS 2359 | Drug Info | Phase 2 | Cocaine addiction | [2] | |
10 | TD-9855 | Drug Info | Phase 2 | Pain | [51] | |
11 | AD-337 | Drug Info | Phase 1 | Chemotherapy-induced nausea | [52] | |
12 | BGC-20-1259 | Drug Info | Phase 1 | Parkinson disease | [53] | |
13 | BL-1021 | Drug Info | Phase 1 | Pain | [54] | |
14 | GSK-1360707 | Drug Info | Phase 1 | Major depressive disorder | [55] | |
15 | SEP-228432 | Drug Info | Phase 1 | Neuropathic pain | [56] | |
Discontinued Drug(s) | [+] 12 Discontinued Drugs | + | ||||
1 | Dexfenfluramine | Drug Info | Withdrawn from market | Obesity | [57] | |
2 | ZIMELIDINE | Drug Info | Withdrawn from market | Major depressive disorder | [3] | |
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 | [66], [67] | |
12 | MOXIFETIN HYDROGEN MALEATE | Drug Info | Terminated | Mood disorder | [68] | |
Mode of Action | [+] 5 Modes of Action | + | ||||
Inhibitor | [+] 225 Inhibitor drugs | + | ||||
1 | Amfepramone | Drug Info | [13], [69] | |||
2 | Cocaine | Drug Info | [71] | |||
3 | Duloxetine | Drug Info | [73], [74] | |||
4 | Escitalopram | Drug Info | [75] | |||
5 | Fluvoxamine | Drug Info | [76], [77] | |||
6 | Sertraline | Drug Info | [1], [79] | |||
7 | Tianeptine | Drug Info | [5] | |||
8 | Venlafaxine | Drug Info | [80] | |||
9 | Vortioxetine | Drug Info | [37], [37], [81], [82] | |||
10 | Amitifadine | Drug Info | [83] | |||
11 | CLR-3001 | Drug Info | [87] | |||
12 | DA-8031 | Drug Info | [88] | |||
13 | NS 2359 | Drug Info | [58], [90] | |||
14 | GSK-1360707 | Drug Info | [93] | |||
15 | SEP-228432 | Drug Info | [94] | |||
16 | Citalopram derivative 1 | Drug Info | [95] | |||
17 | Dexfenfluramine | Drug Info | [96] | |||
18 | ZIMELIDINE | Drug Info | [97] | |||
19 | DOV-216303 | Drug Info | [58] | |||
20 | OxycoDex | Drug Info | [66], [67] | |||
21 | SPD-473 | Drug Info | [100] | |||
22 | YM-992 | Drug Info | [101] | |||
23 | RG-7166 | Drug Info | [103] | |||
24 | 6-nitroquipazine | Drug Info | [104] | |||
25 | A-80426 | Drug Info | [105] | |||
26 | ((3R,4R)-4-(o-tolyloxy)chroman-3-yl)methanamine | Drug Info | [107] | |||
27 | (+/-)-3-((naphthalen-2-yloxy)methyl)pyrrolidine | Drug Info | [108] | |||
28 | (+/-)-nantenine | Drug Info | [109] | |||
29 | (2R,3R)-iodoreboxetine | Drug Info | [110] | |||
30 | (2R,3S)-2-[(2-Iodophenoxy)phenylmethyl]morpholine | Drug Info | [111] | |||
31 | (2R,3S)-2-[(3-Iodophenoxy)phenylmethyl]morpholine | Drug Info | [111] | |||
32 | (2R,3S)-2-[(4-Iodophenoxy)phenylmethyl]morpholine | Drug Info | [111] | |||
33 | (2S,3S)-iodoreboxetine | Drug Info | [110] | |||
34 | (cis)-1,6-diphenyl-3-aza-bicyclo[3.1.0]hexane | Drug Info | [112] | |||
35 | (R)-2-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol | Drug Info | [113] | |||
36 | (R)-6-(pyrrolidin-3-ylmethoxy)-2-naphthonitrile | Drug Info | [108] | |||
37 | (R)-DULOXETINE | Drug Info | [114] | |||
38 | (R)-N-isobutyl-N-(pyrrolidin-3-yl)-2-naphthamide | Drug Info | [115] | |||
39 | (R)-N-isopropyl-N-(pyrrolidin-3-yl)-2-naphthamide | Drug Info | [115] | |||
40 | (R)-Norfluoxetine | Drug Info | [116] | |||
41 | (S)-3-(naphthalen-2-ylmethoxy)pyrrolidine | Drug Info | [108] | |||
42 | (S)-6-(pyrrolidin-3-ylmethoxy)-2-naphthonitrile | Drug Info | [108] | |||
43 | (S)-NORDULOXETINE | Drug Info | [117] | |||
44 | (S)-Norfluoxetine | Drug Info | [116] | |||
45 | 1-(1,2-diphenylethyl)piperazine | Drug Info | [118] | |||
46 | 1-(1,4-diphenylbutan-2-yl)piperazine | Drug Info | [119] | |||
47 | 1-(1-(2-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) | Drug Info | [113] | |||
48 | 1-(1-(4-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) | Drug Info | [113] | |||
49 | 1-(1-phenyl-2-(2-propoxyphenyl)ethyl)piperazine | Drug Info | [113] | |||
50 | 1-(1-phenyl-2-(pyridin-4-yl)ethyl)piperazine | Drug Info | [119] | |||
51 | 1-(1-phenyl-2-o-tolylethyl)piperazine | Drug Info | [118] | |||
52 | 1-(2-(2-(DIFLUOROMETHOXY)PHENYL)-1-PHENYLETHYL)PIPERAZINE (ENANTIOMERIC MIX) | Drug Info | [113] | |||
53 | 1-(2-(2-bromophenyl)-1-phenylethyl)piperazine | Drug Info | [118] | |||
54 | 1-(2-(2-ethylphenyl)-1-phenylethyl)piperazine | Drug Info | [118] | |||
55 | 1-(2-(2-fluorobenzyloxy)phenyl)piperazine | Drug Info | [120] | |||
56 | 1-(2-(2-methoxyphenyl)-1-phenylethyl)piperazine | Drug Info | [113] | |||
57 | 1-(2-(3-chlorophenyl)-1-phenylethyl)piperazine | Drug Info | [118] | |||
58 | 1-(2-(3-fluorophenoxy)phenyl)piperazine | Drug Info | [120] | |||
59 | 1-(2-(3-methoxyphenyl)-1-phenylethyl)piperazine | Drug Info | [118] | |||
60 | 1-(2-(4-fluorophenoxy)phenyl)piperazine | Drug Info | [120] | |||
61 | 1-(2-(6-fluoronaphthalen-2-yl)ethyl)piperazine | Drug Info | [108] | |||
62 | 1-(2-(naphthalen-1-yl)-1-phenylethyl)piperazine | Drug Info | [119] | |||
63 | 1-(2-(naphthalen-2-yl)-1-phenylethyl)piperazine | Drug Info | [119] | |||
64 | 1-(2-(phenoxymethyl)phenyl)piperazine | Drug Info | [120] | |||
65 | 1-(2-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | [121] | |||
66 | 1-(2-phenoxyphenyl)piperazine | Drug Info | [120] | |||
67 | 1-(3,4-Dichloro-phenyl)-3-diethylamino-indan-5-ol | Drug Info | [122] | |||
68 | 1-(3,4-Dichloro-phenyl)-3-methylamino-indan-5-ol | Drug Info | [122] | |||
69 | 1-(3-chlorophenyl)-2-(piperidin-1-yl)propan-1-one | Drug Info | [123] | |||
70 | 1-(3-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | [121] | |||
71 | 1-(3-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | [121] | |||
72 | 1-(4-Benzylsulfanyl-phenyl)-propylamine | Drug Info | [124] | |||
73 | 1-(4-bromophenyl)-2-(tert-butylamino)propan-1-one | Drug Info | [125] | |||
74 | 1-(4-bromophenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | [121] | |||
75 | 1-(4-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | [121] | |||
76 | 1-(4-nitrophenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | [121] | |||
77 | 1-(benzofuran-2-yl)-3-aza-bicyclo[3.1.0]hexane | Drug Info | [112] | |||
78 | 1-(naphthalen-2-yl)-3-aza-bicyclo[3.1.0]hexane | Drug Info | [112] | |||
79 | 1-(thiophen-2-yl)-3-aza-bicyclo[3.1.0]hexane | Drug Info | [112] | |||
80 | 1-benzylpiperidine hydrochloride | Drug Info | [126] | |||
81 | 1-Biphenyl-4-yl-3-aza-bicyclo[3.1.0]hexane | Drug Info | [112] | |||
82 | 1-fluoro-5-phenyl-3-aza-bicyclo[3.1.0]hexane | Drug Info | [112] | |||
83 | 1-Methyl-2-(4-phenylsulfanyl-phenyl)-ethylamine | Drug Info | [124] | |||
84 | 1-Methyl-4-p-tolyl-piperidine-4-carbonitrile | Drug Info | [127] | |||
85 | 1-phenyl-3-aza-bicyclo[3.1.0]hexane | Drug Info | [112] | |||
86 | 10R-hydroxylobel-7-ene | Drug Info | [128] | |||
87 | 10R-hydroxylobelane | Drug Info | [128] | |||
88 | 10S-hydroxylobel-7-ene | Drug Info | [128] | |||
89 | 10S-hydroxylobelane | Drug Info | [128] | |||
90 | 1S,2R-milnacipran | Drug Info | [129] | |||
91 | 2-(2'-Aminoethyl)-5-benzyltetrahydrofuran | Drug Info | [130] | |||
92 | 2-(2-chlorophenoxy)-3-(piperidin-4-yl)pyridine | Drug Info | [131] | |||
93 | 2-(2-fluorophenoxy)-3-(piperidin-4-yl)pyridine | Drug Info | [131] | |||
94 | 2-(2-methoxyphenoxy)-3-(piperidin-4-yl)pyridine | Drug Info | [131] | |||
95 | 2-(2-phenyl-2-(piperazin-1-yl)ethyl)benzonitrile | Drug Info | [118] | |||
96 | 2-(3-Methyl-piperazin-1-yl)-6-nitro-quinoline | Drug Info | [132] | |||
97 | 2-(Aminomethyl)-5-(1'-naphthethyl)tetrahydrofuran | Drug Info | [130] | |||
98 | 2-(Aminomethyl)-5-(2'-naphthyl)tetrahydrofuran | Drug Info | [130] | |||
99 | 2-(Aminomethyl)-5-phenethyltetrahydrofuran | Drug Info | [130] | |||
100 | 2-(N-Cyclopropylamino)-3-chloropropiophenone | Drug Info | [123] | |||
101 | 2-(N-tert-Butylamino)-3',4'-dichloropropiophenone | Drug Info | [123] | |||
102 | 2-(tert-butylamino)-1-(3-chlorophenyl)butan-1-one | Drug Info | [125] | |||
103 | 2-(tert-Butylamino)-3',4'-dichlorobutyrophenone | Drug Info | [123] | |||
104 | 2-(tert-Butylamino)-3',4'-dichloropentanophenone | Drug Info | [123] | |||
105 | 2-Amino-1-(4-ethylthiophenyl)butane | Drug Info | [124] | |||
106 | 2-Amino-1-(4-ethylthiophenyl)propane | Drug Info | [124] | |||
107 | 2-Amino-1-(4-methylthiophenyl)butane | Drug Info | [124] | |||
108 | 2-Amino-1-(4-methylthiophenyl)propane | Drug Info | [124] | |||
109 | 2-Aminomethyl-5-(p-bromophenyl)tetrahydrofuran | Drug Info | [130] | |||
110 | 2-Aminomethyl-5-(p-chlorophenyl)tetrahydrofuran | Drug Info | [130] | |||
111 | 2-Aminomethyl-5-(p-methoxyphenyl)tetrahydrofuran | Drug Info | [130] | |||
112 | 2-Aminomethyl-5-(p-t-butylphenyl)tetrahydrofuran | Drug Info | [130] | |||
113 | 2-Aminomethyl-5-(phenyl)tetrahydrofuran | Drug Info | [130] | |||
114 | 2-N,N-Dimethylamino-1-(4-methylthiophenyl)propane | Drug Info | [124] | |||
115 | 2-N-(Isopropyl)amino-1-(4-methylthiophenyl)butane | Drug Info | [124] | |||
116 | 2-N-(n-Propyl)amino-1-(4-methylthiophenyl)butane | Drug Info | [124] | |||
117 | 2-N-Allylamino-1-(4-methylthiophenyl)propan | Drug Info | [124] | |||
118 | 2-N-Cyclopropylamino-1-(4-methylthiophenyl)butane | Drug Info | [124] | |||
119 | 2-N-Ethylamino-1-(4-ethylthiophenyl)butane | Drug Info | [124] | |||
120 | 2-N-Ethylamino-1-(4-ethylthiophenyl)propane | Drug Info | [124] | |||
121 | 2-N-Ethylamino-1-(4-methylthiophenyl)butane | Drug Info | [124] | |||
122 | 2-N-Ethylamino-1-(4-methylthiophenyl)propane | Drug Info | [124] | |||
123 | 2-N-Hydroxyamino-1-(4-ethylthiophenyl)butane | Drug Info | [124] | |||
124 | 2-N-Hydroxyamino-1-(4-ethylthiophenyl)propane | Drug Info | [124] | |||
125 | 2-N-Hydroxyamino-1-(4-methylthiophenyl)butane | Drug Info | [124] | |||
126 | 2-N-Hydroxyamino-1-(4-methylthiophenyl)propane | Drug Info | [124] | |||
127 | 2-N-Methylamino-1-(4-ethylthiophenyl)propane | Drug Info | [124] | |||
128 | 2-N-Methylamino-1-(4-methylthiophenyl)butane | Drug Info | [124] | |||
129 | 2-N-Methylamino-1-(4-methylthiophenyl)propane | Drug Info | [124] | |||
130 | 2-N-Propargylamino-1-(4-methylthiophenyl)butane | Drug Info | [124] | |||
131 | 2-N-Propargylamino-1-(4-methylthiophenyl)propane | Drug Info | [124] | |||
132 | 2-Naphthalen-2-ylmethyl-4,5-dihydro-1H-imidazole | Drug Info | [105] | |||
133 | 2-phenoxy-3-(piperidin-4-yl)pyridine | Drug Info | [131] | |||
134 | 3-(1H-indol-1-yl)-N-methyl-3-phenylpropan-1-amine | Drug Info | [133] | |||
135 | 3-(1H-indol-3-yl)-N,N-dimethylpropan-1-amine | Drug Info | [134] | |||
136 | 3-(2-phenyl-2-(piperazin-1-yl)ethyl)benzamide | Drug Info | [118] | |||
137 | 3-(2-phenyl-2-(piperazin-1-yl)ethyl)benzonitrile | Drug Info | [118] | |||
138 | 3-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol | Drug Info | [118] | |||
139 | 3-(3,4-dichlorophenyl)-2-nortropene | Drug Info | [135] | |||
140 | 3-(3-aminocyclopentyl)-1H-indole-5-carbonitrile | Drug Info | [136] | |||
141 | 3-(4-Trifluoromethylphenyl)-2-nortropene | Drug Info | [135] | |||
142 | 3-(piperidin-4-yl)-2-(o-tolyloxy)pyridine | Drug Info | [131] | |||
143 | 3-alpha-Phenylmethoxy-3-beta-phenyl-nortropane | Drug Info | [135] | |||
144 | 3-Bromo-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | [132] | |||
145 | 3-p-Tolyl-8-aza-bicyclo[3.2.1]octane | Drug Info | [137] | |||
146 | 3-Phenyl-2-nortropene | Drug Info | [135] | |||
147 | 3alpha-(bis-chloro-phenylmethoxy)tropane | Drug Info | [138] | |||
148 | 4-((naphthalen-2-yloxy)methyl)piperidine | Drug Info | [108] | |||
149 | 4-(1H-indol-3-yl)-N,N-dimethylcyclohex-3-enamine | Drug Info | [139] | |||
150 | 4-(2-((3-fluorophenoxy)methyl)phenyl)piperidine | Drug Info | [120] | |||
151 | 4-(2-((dimethylamino)methyl)phenoxy)benzonitrile | Drug Info | [140] | |||
152 | 4-(2-(2-fluoro-5-methylphenoxy)phenyl)piperidine | Drug Info | [120] | |||
153 | 4-(2-(2-fluorobenzyloxy)phenyl)piperidine | Drug Info | [120] | |||
154 | 4-(2-(3-chlorophenoxy)phenyl)piperidine | Drug Info | [120] | |||
155 | 4-(2-(3-fluorophenoxy)-4-methylphenyl)piperidine | Drug Info | [120] | |||
156 | 4-(2-(3-fluorophenoxy)phenyl)piperidine | Drug Info | [120] | |||
157 | 4-(2-(4-fluorobenzyloxy)phenyl)piperidine | Drug Info | [120] | |||
158 | 4-(2-(4-fluorophenoxy)-4-methylphenyl)piperidine | Drug Info | [120] | |||
159 | 4-(2-(4-fluorophenoxy)phenyl)piperidine | Drug Info | [120] | |||
160 | 4-(2-(benzyloxy)-3-fluorophenyl)piperidine | Drug Info | [120] | |||
161 | 4-(2-(benzyloxy)-6-fluorophenyl)piperidine | Drug Info | [120] | |||
162 | 4-(2-(benzyloxy)phenyl)piperidine | Drug Info | [120] | |||
163 | 4-(2-fluoro-6-(3-fluorophenoxy)phenyl)piperidine | Drug Info | [120] | |||
164 | 4-(2-fluoro-6-(4-fluorophenoxy)phenyl)piperidine | Drug Info | [120] | |||
165 | 4-(2-fluoro-6-phenoxyphenyl)piperidine | Drug Info | [120] | |||
166 | 4-(2-phenoxyphenyl)piperidine | Drug Info | [120] | |||
167 | 4-(3-fluoro-2-phenoxyphenyl)piperidine | Drug Info | [120] | |||
168 | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [141] | |||
169 | 4-Allyl-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | [142] | |||
170 | 4-Benzyl-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | [142] | |||
171 | 4-Bromo-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | [142] | |||
172 | 4-Chloro-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | [142] | |||
173 | 4-Furan-2-yl-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | [142] | |||
174 | 4-Iodo-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | [142] | |||
175 | 6,6-dimethyl-1-phenyl-3-aza-bicyclo[3.1.0]hexane | Drug Info | [112] | |||
176 | 6,8-Dinitro-2-piperazin-1-yl-quinoline | Drug Info | [132] | |||
177 | 6-(3-aza-bicyclo[3.1.0]hexan-1-yl)quinoline | Drug Info | [112] | |||
178 | 6-(piperidin-4-ylmethoxy)-2-naphthonitrile | Drug Info | [108] | |||
179 | 6-Bromo-2-piperazin-1-yl-quinoline | Drug Info | [132] | |||
180 | 6-Chloro-2-piperazin-1-yl-quinoline | Drug Info | [132] | |||
181 | 6-Iodo-2-piperazin-1-yl-quinoline | Drug Info | [132] | |||
182 | 7-(piperidin-4-ylmethoxy)-2-naphthonitrile | Drug Info | [108] | |||
183 | 8-Methyl-3-p-tolyl-8-aza-bicyclo[3.2.1]octane | Drug Info | [137] | |||
184 | 8R-hydroxylobel-9-ene | Drug Info | [143] | |||
185 | 8S-hydroxylobelane | Drug Info | [128] | |||
186 | Beta-methoxyamphetamine | Drug Info | [144], [124] | |||
187 | Biphenyl-2-ylmethyl-(S)-pyrrolidin-3-yl-amine | Drug Info | [145] | |||
188 | COCAINE.HCL | Drug Info | [126] | |||
189 | Cyclohexyl-(3,4-dichloro-phenyl)-acetonitrile | Drug Info | [146] | |||
190 | Cyclopentyl-(3,4-dichloro-phenyl)-acetonitrile | Drug Info | [146] | |||
191 | D-211A | Drug Info | [147] | |||
192 | D-211B | Drug Info | [147] | |||
193 | D-254C | Drug Info | [147] | |||
194 | D-257A | Drug Info | [147] | |||
195 | D-257C | Drug Info | [147] | |||
196 | Erythro-3,4-dichloromethylphenidate hydrochloride | Drug Info | [126] | |||
197 | Isobutyl-(4-methyl-benzyl)-piperidin-4-yl-amine | Drug Info | [148] | |||
198 | JNJ-28583867 | Drug Info | [149] | |||
199 | KF-A5 | Drug Info | [150] | |||
200 | KF-A6 | Drug Info | [150] | |||
201 | MDL-28618 | Drug Info | [107] | |||
202 | METHYLENEDIOXYAMPHETAMINE | Drug Info | [124] | |||
203 | METHYLENEDIOXYMETHAMPHETAMINE | Drug Info | [151], [124] | |||
204 | N*1*-(6-Nitro-quinolin-2-yl)-ethane-1,2-diamine | Drug Info | [132] | |||
205 | N-(2-oxazolemethyl)milnacipran | Drug Info | [153] | |||
206 | N-(piperidin-4-yl)-N-propyl-2-naphthamide | Drug Info | [115] | |||
207 | N-benzyl-N-isobutylpiperidin-4-amine | Drug Info | [148] | |||
208 | NISOXETINE | Drug Info | [114] | |||
209 | norzotepine | Drug Info | [154] | |||
210 | O-DESMETHYL TRAMADOL | Drug Info | [155] | |||
211 | Para-chloroamphetamine | Drug Info | [124] | |||
212 | PF-18298 | Drug Info | [113] | |||
213 | PF-3409409 | Drug Info | [156] | |||
214 | PYROVALERONE | Drug Info | [121] | |||
215 | QUIPAZINE | Drug Info | [132] | |||
216 | R-226161 | Drug Info | [157] | |||
217 | S-34324 | Drug Info | [158] | |||
218 | S33005 | Drug Info | [101] | |||
219 | TEFLUDAZINE | Drug Info | [159] | |||
220 | Threo-1-aza-5-phenyl[4.4.0]decane hydrochloride | Drug Info | [126] | |||
221 | Threo-3,4-dichlororitalinol hydrochloride | Drug Info | [126] | |||
222 | WIN-35065 | Drug Info | [160] | |||
223 | WIN-35066-2 | Drug Info | [161] | |||
224 | [3-(3,4-Dichloro-phenyl)-indan-1-yl]-methyl-amine | Drug Info | [122] | |||
225 | [3H]WIN35428 | Drug Info | [162] | |||
Modulator | [+] 22 Modulator drugs | + | ||||
1 | Chlorphentermine Hydrochloride | Drug Info | [70] | |||
2 | Desvenlafaxine | Drug Info | [17] | |||
3 | Dextromethorphan Polistirex | Drug Info | [72] | |||
4 | Fluoxetine | Drug Info | [72] | |||
5 | Levomilnacipran | Drug Info | [24] | |||
6 | Luvox | Drug Info | [78] | |||
7 | Nortriptyline | Drug Info | [72] | |||
8 | Paroxetine | Drug Info | [72] | |||
9 | Sibutramine | Drug Info | [72] | |||
10 | Trazodone | Drug Info | [72] | |||
11 | Bicifadine | Drug Info | [84] | |||
12 | LITOXETINE | Drug Info | [86] | |||
13 | Brasofensine | Drug Info | [47] | |||
14 | Lu-AA34893 | Drug Info | [89] | |||
15 | TD-9855 | Drug Info | [51] | |||
16 | AD-337 | Drug Info | [78] | |||
17 | BGC-20-1259 | Drug Info | [91] | |||
18 | BL-1021 | Drug Info | [92] | |||
19 | NS-2389 | Drug Info | [98] | |||
20 | R-sibutramine metabolite | Drug Info | [99] | |||
21 | HydrocoDex | Drug Info | [66], [67] | |||
22 | MMDA | Drug Info | [152] | |||
Antagonist | [+] 1 Antagonist drugs | + | ||||
1 | ITI-007 | Drug Info | [85] | |||
Activator | [+] 1 Activator drugs | + | ||||
1 | NSD-644 | Drug Info | [102] | |||
Binder | [+] 1 Binder drugs | + | ||||
1 | CX-1001 | Drug Info | [83] |
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 | [163] |
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 | [163] |
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 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 3 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 4 | 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). | |||||
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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: 2398). | |||||
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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: 203). | |||||
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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: 4790). | |||||
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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: 2586). | |||||
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REF 33 | 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 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: 7321). | |||||
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REF 39 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
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