Target Information
Target General Information | Top | |||||
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Target ID |
T55959
(Former ID: TTDS00017)
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Target Name |
Dopamine transporter (DAT)
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Synonyms |
Solute carrier family 6 member 3; Sodium-dependent dopamine transporter; DAT1; DAT; DA transporter
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Gene Name |
SLC6A3
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 6 Target-related Diseases | + | ||||
1 | Attention deficit hyperactivity disorder [ICD-11: 6A05] | |||||
2 | Corneal disease [ICD-11: 9A76-9A78] | |||||
3 | Narcolepsy [ICD-11: 7A20] | |||||
4 | Obesity [ICD-11: 5B80-5B81] | |||||
5 | Parkinsonism [ICD-11: 8A00] | |||||
6 | Bipolar disorder [ICD-11: 6A60] | |||||
Function |
Amine transporter. Terminates the action of dopamine by its high affinity sodium-dependent reuptake into presynaptic terminals.
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BioChemical Class |
Neurotransmitter:sodium symporter
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UniProt ID | ||||||
Sequence |
MSKSKCSVGLMSSVVAPAKEPNAVGPKEVELILVKEQNGVQLTSSTLTNPRQSPVEAQDR
ETWGKKIDFLLSVIGFAVDLANVWRFPYLCYKNGGGAFLVPYLLFMVIAGMPLFYMELAL GQFNREGAAGVWKICPILKGVGFTVILISLYVGFFYNVIIAWALHYLFSSFTTELPWIHC NNSWNSPNCSDAHPGDSSGDSSGLNDTFGTTPAAEYFERGVLHLHQSHGIDDLGPPRWQL TACLVLVIVLLYFSLWKGVKTSGKVVWITATMPYVVLTALLLRGVTLPGAIDGIRAYLSV DFYRLCEASVWIDAATQVCFSLGVGFGVLIAFSSYNKFTNNCYRDAIVTTSINSLTSFSS GFVVFSFLGYMAQKHSVPIGDVAKDGPGLIFIIYPEAIATLPLSSAWAVVFFIMLLTLGI DSAMGGMESVITGLIDEFQLLHRHRELFTLFIVLATFLLSLFCVTNGGIYVFTLLDHFAA GTSILFGVLIEAIGVAWFYGVGQFSDDIQQMTGQRPSLYWRLCWKLVSPCFLLFVVVVSI VTFRPPHYGAYIFPDWANALGWVIATSSMAMVPIYAAYKFCSLPGSFREKLAYAIAPEKD RELVDRGEVRQFTLRHWLKV Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
HIT2.0 ID | T24LWC |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 8 Approved Drugs | + | ||||
1 | Altropane | Drug Info | Approved | Attention deficit hyperactivity disorder | [2] | |
2 | Cocaine | Drug Info | Approved | Anaesthesia | [3], [4], [5] | |
3 | Dasotraline | Drug Info | Approved | Attention deficit hyperactivity disorder | [6] | |
4 | DEXMETHYLPHENIDATE HYDROCHLORIDE | Drug Info | Approved | Attention deficit hyperactivity disorder | [5], [7] | |
5 | Ioflupane i-123 | Drug Info | Approved | Parkinson disease | [8] | |
6 | Methylphenidate | Drug Info | Approved | Attention deficit hyperactivity disorder | [9], [10] | |
7 | Modafinil | Drug Info | Approved | Narcolepsy | [5] | |
8 | Phenmetrazine | Drug Info | Approved | Obesity | [11] | |
Clinical Trial Drug(s) | [+] 8 Clinical Trial Drugs | + | ||||
1 | Amitifadine | Drug Info | Phase 3 | Obesity | [12], [13] | |
2 | Bupropion+naltrexone | Drug Info | Phase 3 | Obesity | [14] | |
3 | NAV5001 | Drug Info | Phase 3 | Dementia | [15] | |
4 | MIN-117 | Drug Info | Phase 2 | Major depressive disorder | [16] | |
5 | NS 2359 | Drug Info | Phase 2 | Cocaine addiction | [6] | |
6 | Spiroglumide | Drug Info | Phase 2 | Stomach disease | [17] | |
7 | GSK-1360707 | Drug Info | Phase 1 | Major depressive disorder | [18] | |
8 | RTI-336 | Drug Info | Phase 1 | Cocaine addiction | [19] | |
Discontinued Drug(s) | [+] 12 Discontinued Drugs | + | ||||
1 | Amineptine | Drug Info | Withdrawn from market | Major depressive disorder | [5] | |
2 | DOV-216303 | Drug Info | Discontinued in Phase 2 | Mood disorder | [20] | |
3 | Manifaxine | Drug Info | Discontinued in Phase 2 | Major depressive disorder | [21] | |
4 | NS-2389 | Drug Info | Discontinued in Phase 2 | Major depressive disorder | [22] | |
5 | Radafaxine | Drug Info | Discontinued in Phase 2 | Major depressive disorder | [23] | |
6 | SPD-473 | Drug Info | Discontinued in Phase 2 | Mood disorder | [24] | |
7 | KP106 | Drug Info | Discontinued in Phase 1 | Attention deficit hyperactivity disorder | [25] | |
8 | NSD-644 | Drug Info | Discontinued in Phase 1 | Neurological disorder | [26] | |
9 | RG-7166 | Drug Info | Discontinued in Phase 1 | Major depressive disorder | [27] | |
10 | Vanoxerine | Drug Info | Discontinued in Phase 1 | Cocaine addiction | [19] | |
11 | Fluoratec | Drug Info | Terminated | Attention deficit hyperactivity disorder | [28] | |
12 | Seridopidine | Drug Info | Terminated | Neurological disorder | [29] | |
Mode of Action | [+] 6 Modes of Action | + | ||||
Inhibitor | [+] 266 Inhibitor drugs | + | ||||
1 | Altropane | Drug Info | [30] | |||
2 | Cocaine | Drug Info | [31] | |||
3 | Dasotraline | Drug Info | [32] | |||
4 | DEXMETHYLPHENIDATE HYDROCHLORIDE | Drug Info | [33] | |||
5 | Phenmetrazine | Drug Info | [35] | |||
6 | Amitifadine | Drug Info | [36] | |||
7 | Bupropion+naltrexone | Drug Info | [37] | |||
8 | MIN-117 | Drug Info | [6] | |||
9 | NS 2359 | Drug Info | [20], [38] | |||
10 | Spiroglumide | Drug Info | [39] | |||
11 | GSK-1360707 | Drug Info | [40] | |||
12 | Amineptine | Drug Info | [42] | |||
13 | DOV-216303 | Drug Info | [20] | |||
14 | Radafaxine | Drug Info | [23], [45] | |||
15 | SPD-473 | Drug Info | [46] | |||
16 | RG-7166 | Drug Info | [49] | |||
17 | (+/-)-3-((naphthalen-2-yloxy)methyl)pyrrolidine | Drug Info | [52] | |||
18 | (+/-)-threo-3',4'-Dichloromethylphenidate amide | Drug Info | [53] | |||
19 | (+/-)-threo-3',4'-Dichlororitalinol methyl ether | Drug Info | [53] | |||
20 | (+/-)-threo-3',5'-Dichloromethylphenidate | Drug Info | [53] | |||
21 | (+/-)-threo-3',5'-Dimethylmethylphenidate | Drug Info | [53] | |||
22 | (+/-)-threo-3-Fluororitalinol | Drug Info | [53] | |||
23 | (+/-)-threo-4'-Ethylmethylphenidate | Drug Info | [53] | |||
24 | (+/-)-threo-Benzylphenidate | Drug Info | [53] | |||
25 | (+/-)-threo-Methylphenidate amide | Drug Info | [53] | |||
26 | (+/-)-threo-N-(2-Chlorobenzyl)methylphenidate | Drug Info | [53] | |||
27 | (+/-)-threo-N-(2-Methylfuran)methylphenidate | Drug Info | [53] | |||
28 | (+/-)-threo-N-(2-Methylpyridine)methylphenidate | Drug Info | [53] | |||
29 | (+/-)-threo-N-(2-Methylthiopene)methylphenidate | Drug Info | [53] | |||
30 | (+/-)-threo-N-(2-Phenylethyl)methylphenidate | Drug Info | [53] | |||
31 | (+/-)-threo-N-(2-Phenylethyl)ritalinol | Drug Info | [53] | |||
32 | (+/-)-threo-N-(3-Chlorobenzyl)methylphenidate | Drug Info | [53] | |||
33 | (+/-)-threo-N-(3-Methylfuran)methylphenidate | Drug Info | [53] | |||
34 | (+/-)-threo-N-(3-Methylpyridine)methylphenidate | Drug Info | [53] | |||
35 | (+/-)-threo-N-(3-Methylthiopene)methylphenidate | Drug Info | [53] | |||
36 | (+/-)-threo-N-(3-Phenylpropyl)methylphenidate | Drug Info | [53] | |||
37 | (+/-)-threo-N-(3-Phenylpropyl)ritalinol | Drug Info | [53] | |||
38 | (+/-)-threo-N-(4-Chlorobenzyl)methylphenidate | Drug Info | [53] | |||
39 | (+/-)-threo-N-(4-Methoxybenzyl)methylphenidate | Drug Info | [53] | |||
40 | (+/-)-threo-N-(4-Methylpyridine)methylphenidate | Drug Info | [53] | |||
41 | (+/-)-threo-N-(4-Nitrobenzyl)methylphenidate | Drug Info | [53] | |||
42 | (+/-)-threo-N-(4-Phenylbutyl)methylphenidate | Drug Info | [53] | |||
43 | (+/-)-threo-N-(4-Phenylbutyl)ritalinol | Drug Info | [53] | |||
44 | (+/-)-threo-N-(5-Phenylpentyl)methylphenidate | Drug Info | [53] | |||
45 | (+/-)-threo-N-(6-Phenylhexyl)methylphenidate | Drug Info | [53] | |||
46 | (+/-)-threo-N-Allylmethylphenidate | Drug Info | [53] | |||
47 | (+/-)-threo-N-Benzyl-3',4'-dichlororitalinol | Drug Info | [53] | |||
48 | (+/-)-threo-N-Benzyl-3'-chloromethylphenidate | Drug Info | [53] | |||
49 | (+/-)-threo-N-Benzylmethylphenidate amide | Drug Info | [53] | |||
50 | (+/-)-threo-N-Methyl-30-methylmethylphenidate | Drug Info | [53] | |||
51 | (+/-)-threo-N-Propargylmethylphenidate | Drug Info | [53] | |||
52 | (1-Phenyl-ethyl)-(2-phenyl-quinazolin-4-yl)-amine | Drug Info | [54] | |||
53 | (2R,3R)-iodoreboxetine | Drug Info | [55] | |||
54 | (2R,3S)-2-[(2-Iodophenoxy)phenylmethyl]morpholine | Drug Info | [56] | |||
55 | (2R,3S)-2-[(3-Iodophenoxy)phenylmethyl]morpholine | Drug Info | [56] | |||
56 | (2R,3S)-2-[(4-Iodophenoxy)phenylmethyl]morpholine | Drug Info | [56] | |||
57 | (2S,3S)-2-(m-Tolyl)-3,5,5-trimethylmorpholin-2-ol | Drug Info | [57] | |||
58 | (2S,3S)-2-Phenyl-3,5,5-trimethylmorpholin-2-ol | Drug Info | [57] | |||
59 | (2S,3S)-iodoreboxetine | Drug Info | [55] | |||
60 | (cis)-1,6-diphenyl-3-aza-bicyclo[3.1.0]hexane | Drug Info | [58] | |||
61 | (R)-2-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol | Drug Info | [59] | |||
62 | (R)-3-(naphthalen-2-ylmethoxy)pyrrolidine | Drug Info | [52] | |||
63 | (R)-DULOXETINE | Drug Info | [60] | |||
64 | (R)-N-isobutyl-N-(pyrrolidin-3-yl)-2-naphthamide | Drug Info | [61] | |||
65 | (R)-Norfluoxetine | Drug Info | [62] | |||
66 | (RS/SR)-2-[1-(3,4-dichlorophenyl)butyl]piperidine | Drug Info | [63] | |||
67 | (RS/SR)-2-[1-(4-chlorophenyl)butyl]piperidine | Drug Info | [63] | |||
68 | (RS/SR)-2-[1-(4-chlorophenyl)ethyl]piperidine | Drug Info | [63] | |||
69 | (RS/SR)-2-[1-(4-chlorophenyl)hexyl]piperidine | Drug Info | [63] | |||
70 | (RS/SR)-2-[1-(4-chlorophenyl)pentyl]piperidine | Drug Info | [63] | |||
71 | (RS/SR)-2-[1-(4-chlorophenyl)propyl]piperidine | Drug Info | [63] | |||
72 | (S)-3-(naphthalen-2-ylmethoxy)pyrrolidine | Drug Info | [52] | |||
73 | (S)-Norfluoxetine | Drug Info | [62] | |||
74 | 1-(1,4-diphenylbutan-2-yl)piperazine | Drug Info | [64] | |||
75 | 1-(1-(4-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) | Drug Info | [59] | |||
76 | 1-(1-(benzo[b]thiophen-2-yl)cyclohexyl)piperidine | Drug Info | [65] | |||
77 | 1-(1-Benzo[b]thiophen-2-yl-cycloheptyl)-azepane | Drug Info | [66] | |||
78 | 1-(1-Benzo[b]thiophen-2-yl-cyclohexyl)-azepane | Drug Info | [66] | |||
79 | 1-(1-Benzo[b]thiophen-2-yl-cyclopentyl)-azepane | Drug Info | [66] | |||
80 | 1-(1-phenyl-2-(2-propoxyphenyl)ethyl)piperazine | Drug Info | [59] | |||
81 | 1-(2,3-Dihydro-1H-indol-5-ylmethyl)-propylamine | Drug Info | [67] | |||
82 | 1-(2-(2-(DIFLUOROMETHOXY)PHENYL)-1-PHENYLETHYL)PIPERAZINE (ENANTIOMERIC MIX) | Drug Info | [59] | |||
83 | 1-(2-(2-chlorophenyl)-1-phenylethyl)piperazine | Drug Info | [68] | |||
84 | 1-(2-(2-methoxyphenyl)-1-phenylethyl)piperazine | Drug Info | [68] | |||
85 | 1-(2-(4-fluorophenoxy)phenyl)piperazine | Drug Info | [69] | |||
86 | 1-(2-(phenoxymethyl)phenyl)piperazine | Drug Info | [69] | |||
87 | 1-(2-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | [70] | |||
88 | 1-(2-phenoxyphenyl)piperazine | Drug Info | [69] | |||
89 | 1-(3,4-Dichloro-phenyl)-3-diethylamino-indan-5-ol | Drug Info | [71] | |||
90 | 1-(3,4-Dichloro-phenyl)-3-methylamino-indan-5-ol | Drug Info | [71] | |||
91 | 1-(3-bromophenyl)-2-(tert-butylamino)propan-1-one | Drug Info | [72] | |||
92 | 1-(3-chlorophenyl)-2-(dimethylamino)propan-1-one | Drug Info | [72] | |||
93 | 1-(3-chlorophenyl)-2-(piperidin-1-yl)propan-1-one | Drug Info | [72] | |||
94 | 1-(3-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | [70] | |||
95 | 1-(3-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | [70] | |||
96 | 1-(4-aminophenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | [73] | |||
97 | 1-(4-bromophenyl)-2-(tert-butylamino)propan-1-one | Drug Info | [72] | |||
98 | 1-(4-bromophenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | [70] | |||
99 | 1-(4-fluorophenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | [70] | |||
100 | 1-(4-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | [70] | |||
101 | 1-(4-nitrophenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | [70] | |||
102 | 1-(benzofuran-2-yl)-3-aza-bicyclo[3.1.0]hexane | Drug Info | [58] | |||
103 | 1-(naphthalen-2-yl)-3-aza-bicyclo[3.1.0]hexane | Drug Info | [58] | |||
104 | 1-(thiophen-2-yl)-3-aza-bicyclo[3.1.0]hexane | Drug Info | [58] | |||
105 | 1-Benzo[b]thiophen-2-yl-cycloheptylamine | Drug Info | [66] | |||
106 | 1-Benzo[b]thiophen-2-yl-cyclohexylamine | Drug Info | [66] | |||
107 | 1-Benzo[b]thiophen-2-yl-cyclopentylamine | Drug Info | [66] | |||
108 | 1-benzylpiperidine hydrochloride | Drug Info | [33] | |||
109 | 1-Biphenyl-4-yl-3-aza-bicyclo[3.1.0]hexane | Drug Info | [58] | |||
110 | 1-naphthalen-2-yl-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | [70] | |||
111 | 1-phenyl-1-(piperidin-2-yl)propan-2-one | Drug Info | [63] | |||
112 | 1-phenyl-3-aza-bicyclo[3.1.0]hexane | Drug Info | [58] | |||
113 | 10R-hydroxylobel-7-ene | Drug Info | [74] | |||
114 | 10R-hydroxylobelane | Drug Info | [74] | |||
115 | 10S-hydroxylobel-7-ene | Drug Info | [74] | |||
116 | 10S-hydroxylobelane | Drug Info | [74] | |||
117 | 1S,2R-milnacipran | Drug Info | [75] | |||
118 | 2-((2-iodophenoxy)(phenyl)methyl)morpholine | Drug Info | [76] | |||
119 | 2-((3-iodophenyl)(o-tolyloxy)methyl)morpholine | Drug Info | [76] | |||
120 | 2-(2'-Aminoethyl)-5-benzyltetrahydrofuran | Drug Info | [77] | |||
121 | 2-(2,3-Dihydro-1H-indol-5-yl)-1-methyl-ethylamine | Drug Info | [67] | |||
122 | 2-(2-chlorophenoxy)-3-(piperidin-4-yl)pyridine | Drug Info | [78] | |||
123 | 2-(2-methoxyphenoxy)-3-(piperidin-4-yl)pyridine | Drug Info | [78] | |||
124 | 2-(Aminomethyl)-5-(1'-naphthyl)tetrahydrofuran | Drug Info | [77] | |||
125 | 2-(Aminomethyl)-5-(2'-naphthyl)tetrahydrofuran | Drug Info | [77] | |||
126 | 2-(Aminomethyl)-5-phenethyltetrahydrofuran | Drug Info | [77] | |||
127 | 2-(N,N-Diethylamino)-3'-chloropropiophenone | Drug Info | [79] | |||
128 | 2-(N-Cyclopentylamino)-3'-bromopropiophenone | Drug Info | [72] | |||
129 | 2-(N-Cyclopentylamino)-3'-chloropropiophenone | Drug Info | [79] | |||
130 | 2-(N-Cyclopentylamino)-3'-fluoropropiophenone | Drug Info | [72] | |||
131 | 2-(N-Cyclopentylamino)-3'-methoxypropiophenone | Drug Info | [72] | |||
132 | 2-(N-Cyclopentylamino)-3'-methylpropiophenone | Drug Info | [72] | |||
133 | 2-(N-Cyclopropylamino)-3-chloropropiophenone | Drug Info | [79] | |||
134 | 2-(N-Isopropylamino)-3'-chloropropiophenone | Drug Info | [79] | |||
135 | 2-(N-Pyrrolidinyl)-3'-bromopropiophenone | Drug Info | [72] | |||
136 | 2-(N-Pyrrolidinyl)-3'-fluoropropiophenone | Drug Info | [72] | |||
137 | 2-(N-Pyrrolidinyl)-3'-methoxypropiophenone | Drug Info | [72] | |||
138 | 2-(N-Pyrrolidinyl)-3'-methylpropiophenone | Drug Info | [72] | |||
139 | 2-(N-Pyrrolidinyl)-3'-nitropropiophenone | Drug Info | [72] | |||
140 | 2-(N-tert-Butylamino)-3',4'-dichloropropiophenone | Drug Info | [79] | |||
141 | 2-(N-tert-Butylamino)-3'-chloroheptanophenone | Drug Info | [79] | |||
142 | 2-(N-tert-Butylamino)-3'-chlorohexanophenone | Drug Info | [79] | |||
143 | 2-(N-tert-Butylamino)-3'-chlorooctanophenone | Drug Info | [79] | |||
144 | 2-(N-tert-Butylamino)-3'-chloropentanophenone | Drug Info | [79] | |||
145 | 2-(N-tert-Butylamino)-4'-chloropropiophenone | Drug Info | [79] | |||
146 | 2-(N-tert-Butylamino)propiophenone | Drug Info | [79] | |||
147 | 2-(tert-butylamino)-1-(3-chlorophenyl)butan-1-one | Drug Info | [72] | |||
148 | 2-(tert-butylamino)-1-m-tolylpropan-1-one | Drug Info | [72] | |||
149 | 2-(tert-butylamino)-1-p-tolylpropan-1-one | Drug Info | [72] | |||
150 | 2-(tert-Butylamino)-3',4'-dichlorobutyrophenone | Drug Info | [79] | |||
151 | 2-(tert-Butylamino)-3',4'-dichloropentanophenone | Drug Info | [79] | |||
152 | 2-(tert-Butylamino)-3',5'-difluoropropiophenone | Drug Info | [79] | |||
153 | 2-(tert-Butylamino)-3'-fluoropropiophenone | Drug Info | [79] | |||
154 | 2-Amino-1-(4-methylthiophenyl)propane | Drug Info | [80] | |||
155 | 2-Aminomethyl-5-(p-bromophenyl)tetrahydrofuran | Drug Info | [77] | |||
156 | 2-Aminomethyl-5-(p-chlorophenyl)tetrahydrofuran | Drug Info | [77] | |||
157 | 2-Aminomethyl-5-(p-methoxyphenyl)tetrahydrofuran | Drug Info | [77] | |||
158 | 2-Aminomethyl-5-(p-t-butylphenyl)tetrahydrofuran | Drug Info | [77] | |||
159 | 2-Aminomethyl-5-(phenyl)tetrahydrofuran | Drug Info | [77] | |||
160 | 2-phenoxy-3-(piperidin-4-yl)pyridine | Drug Info | [78] | |||
161 | 2-phenylpiperidine hydrochloride | Drug Info | [33] | |||
162 | 2pyrrolidin-1-yl-1-phenylpentan-1-one | Drug Info | [70] | |||
163 | 3-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol | Drug Info | [68] | |||
164 | 3-(3,4-dichlorophenyl)-2-nortropene | Drug Info | [81] | |||
165 | 3-(4-Chlorophenyl)-2-nortropene | Drug Info | [81] | |||
166 | 3-(4-Fluorophenyl)-2-nortropene | Drug Info | [81] | |||
167 | 3-(4-Trifluoromethylphenyl)-2-nortropene | Drug Info | [81] | |||
168 | 3-alpha-Phenylmethoxy-3-beta-phenyl-nortropane | Drug Info | [81] | |||
169 | 3-p-Tolyl-8-aza-bicyclo[3.2.1]octane | Drug Info | [82] | |||
170 | 3-Phenyl-2-nortropene | Drug Info | [81] | |||
171 | 3alpha-(bis-chloro-phenylmethoxy)tropane | Drug Info | [83] | |||
172 | 4-(1H-indol-3-yl)-N,N-dimethylcyclohex-3-enamine | Drug Info | [84] | |||
173 | 4-(2-((3-fluorophenoxy)methyl)phenyl)piperidine | Drug Info | [69] | |||
174 | 4-(2-(2-fluoro-5-methylphenoxy)phenyl)piperidine | Drug Info | [69] | |||
175 | 4-(2-(2-fluorobenzyloxy)phenyl)piperidine | Drug Info | [69] | |||
176 | 4-(2-(3-chlorophenoxy)phenyl)piperidine | Drug Info | [69] | |||
177 | 4-(2-(3-fluorophenoxy)-4-methylphenyl)piperidine | Drug Info | [69] | |||
178 | 4-(2-(3-fluorophenoxy)phenyl)piperidine | Drug Info | [69] | |||
179 | 4-(2-(4-fluorobenzyloxy)phenyl)piperidine | Drug Info | [69] | |||
180 | 4-(2-(4-fluorophenoxy)-4-methylphenyl)piperidine | Drug Info | [69] | |||
181 | 4-(2-(4-fluorophenoxy)phenyl)piperidine | Drug Info | [69] | |||
182 | 4-(2-(benzyloxy)-3-fluorophenyl)piperidine | Drug Info | [69] | |||
183 | 4-(2-(benzyloxy)-6-fluorophenyl)piperidine | Drug Info | [69] | |||
184 | 4-(2-(benzyloxy)phenyl)piperidine | Drug Info | [69] | |||
185 | 4-(2-(phenoxymethyl)phenyl)piperidine | Drug Info | [69] | |||
186 | 4-(2-fluoro-6-(2-fluorophenoxy)phenyl)piperidine | Drug Info | [78] | |||
187 | 4-(2-fluoro-6-(3-fluorophenoxy)phenyl)piperidine | Drug Info | [69] | |||
188 | 4-(2-fluoro-6-(4-fluorophenoxy)phenyl)piperidine | Drug Info | [69] | |||
189 | 4-(2-fluoro-6-phenoxyphenyl)piperidine | Drug Info | [69] | |||
190 | 4-(2-phenoxyphenyl)piperidine | Drug Info | [69] | |||
191 | 4-(2-pyrrolidin-1-yl-pentanoyl)benzonitrile | Drug Info | [70] | |||
192 | 4-(3-fluoro-2-phenoxyphenyl)piperidine | Drug Info | [69] | |||
193 | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [85] | |||
194 | 4-[(diphenylmethyl)amino]-2-phenylquinazoline | Drug Info | [54] | |||
195 | 6-(3-aza-bicyclo[3.1.0]hexan-1-yl)quinoline | Drug Info | [58] | |||
196 | 6-(piperidin-4-ylmethoxy)-2-naphthonitrile | Drug Info | [52] | |||
197 | 7-(piperidin-4-ylmethoxy)-2-naphthonitrile | Drug Info | [52] | |||
198 | 8-Methyl-3-p-tolyl-8-aza-bicyclo[3.2.1]octane | Drug Info | [82] | |||
199 | 8R-hydroxylobel-9-ene | Drug Info | [86] | |||
200 | 8R-hydroxylobelane | Drug Info | [74] | |||
201 | 8S-hydroxylobel-9-ene | Drug Info | [74] | |||
202 | 8S-hydroxylobelane | Drug Info | [74] | |||
203 | AMINOBENZTROPINE | Drug Info | [87] | |||
204 | ANOLOBINE | Drug Info | [88] | |||
205 | ANONAINE | Drug Info | [88] | |||
206 | ANTIOQUINE | Drug Info | [88] | |||
207 | Benzyl-(2-phenyl-quinazolin-4-yl)-amine | Drug Info | [54] | |||
208 | Bip-tyr(3bzl)-thr-pro-lys-thr | Drug Info | [90] | |||
209 | Bip-tyr-ala-pro-lys-thr(obzl)-gly | Drug Info | [90] | |||
210 | Bip-tyr-thr-ala-pro-phe | Drug Info | [90] | |||
211 | Bip-tyr-thr-pro-ala-thr(obzl)-gly | Drug Info | [90] | |||
212 | Bip-tyr-thr-pro-lys-thr | Drug Info | [90] | |||
213 | Bip-tyr-thr-pro-lys-thr(obzl)-gly | Drug Info | [90] | |||
214 | Bip-tyr-thr-pro-thr(obzl)-gly | Drug Info | [90] | |||
215 | Biphenyl-2-ylmethyl-(S)-pyrrolidin-3-yl-amine | Drug Info | [91] | |||
216 | Cis-3-phenoxy-2,3-dihydro-1H-inden-1-amine | Drug Info | [92] | |||
217 | COCAINE.HCL | Drug Info | [33] | |||
218 | COCLAURINE | Drug Info | [88] | |||
219 | D-166A | Drug Info | [93] | |||
220 | D-211A | Drug Info | [93] | |||
221 | D-211B | Drug Info | [93] | |||
222 | D-254C | Drug Info | [93] | |||
223 | D-257A | Drug Info | [93] | |||
224 | D-257C | Drug Info | [93] | |||
225 | Difluorobenztropine | Drug Info | [83] | |||
226 | DIMETHYLGRISABINE | Drug Info | [88] | |||
227 | Erythro-3,4-dichloromethylphenidate hydrochloride | Drug Info | [33] | |||
228 | GB-12819 | Drug Info | [94] | |||
229 | HOMOAROMOLINE | Drug Info | [88] | |||
230 | Indatraline | Drug Info | [95] | |||
231 | ISOPILINE | Drug Info | [88] | |||
232 | ISOTETRANDRINE | Drug Info | [88] | |||
233 | Methyl 2-(naphthalen-2-yl)benzoate | Drug Info | [96] | |||
234 | METHYLENEDIOXYAMPHETAMINE | Drug Info | [97] | |||
235 | METHYLENEDIOXYMETHAMPHETAMINE | Drug Info | [80], [98] | |||
236 | N,Ndimethyl milnacipran | Drug Info | [100] | |||
237 | N-Benzylmethylphenidate | Drug Info | [53] | |||
238 | NISOXETINE | Drug Info | [92] | |||
239 | NORBOLDINE | Drug Info | [88] | |||
240 | NORSTEPHALAGINE | Drug Info | [88] | |||
241 | O-2442 | Drug Info | [36] | |||
242 | O-methyldauricine | Drug Info | [88] | |||
243 | OBABERINE | Drug Info | [88] | |||
244 | Para-chloroamphetamine | Drug Info | [80] | |||
245 | PF-18298 | Drug Info | [59] | |||
246 | PF-3409409 | Drug Info | [101] | |||
247 | PF-526014 | Drug Info | [59] | |||
248 | PMID25037917C58 | Drug Info | [102] | |||
249 | PSEUDOCOCAINE | Drug Info | [103] | |||
250 | PYROVALERONE | Drug Info | [73] | |||
251 | R-226161 | Drug Info | [104] | |||
252 | R-NORDULOXETINE | Drug Info | [105] | |||
253 | RTI-219 | Drug Info | [106] | |||
254 | SECOCULARIDINE | Drug Info | [88] | |||
255 | Threo-1-aza-5-phenyl[4.4.0]decane hydrochloride | Drug Info | [33] | |||
256 | Threo-3,4-dichlororitalinol hydrochloride | Drug Info | [33] | |||
257 | Threo-N-ethylritalinol hydrochloride | Drug Info | [33] | |||
258 | Threo-ritalinol hydrochloride | Drug Info | [33] | |||
259 | Threo-ritalinol methyl ether hydrochloride | Drug Info | [33] | |||
260 | Trans-3-(o-tolyloxy)-2,3-dihydro-1H-inden-1-amine | Drug Info | [92] | |||
261 | WIN-35065 | Drug Info | [106] | |||
262 | WIN-35066-2 | Drug Info | [107] | |||
263 | [3-(3,4-Dichloro-phenyl)-indan-1-yl]-methyl-amine | Drug Info | [71] | |||
264 | [3H]GBR12935 | Drug Info | [108] | |||
265 | [3H]WIN35428 | Drug Info | [108], [109] | |||
266 | [N-[2-[(3'-N'-PROPYL-3''ALPHA-(BIS(4-FLUORORPHENYL)METHOXY)TROPANE-2''BETA-CARBOXYLIC ACID METHYL ESTER)(2-MERCAPTOETHYL)AMINO]ACETYL]-2-AMINOETHANETHIOLATO]RHENIUM(V) OXIDE (DIASTEREOMERIC MIX) | Drug Info | [110] | |||
Modulator | [+] 9 Modulator drugs | + | ||||
1 | Ioflupane i-123 | Drug Info | [5] | |||
2 | Modafinil | Drug Info | [34] | |||
3 | NAV5001 | Drug Info | [30] | |||
4 | RTI-336 | Drug Info | [41] | |||
5 | Manifaxine | Drug Info | [43] | |||
6 | NS-2389 | Drug Info | [44] | |||
7 | Fluoratec | Drug Info | [50] | |||
8 | Seridopidine | Drug Info | [51] | |||
9 | MMDA | Drug Info | [99] | |||
Blocker | [+] 2 Blocker drugs | + | ||||
1 | Methylphenidate | Drug Info | [1] | |||
2 | Vanoxerine | Drug Info | [19] | |||
Agonist | [+] 1 Agonist drugs | + | ||||
1 | KP106 | Drug Info | [47] | |||
Activator | [+] 1 Activator drugs | + | ||||
1 | NSD-644 | Drug Info | [48] | |||
Antagonist | [+] 1 Antagonist drugs | + | ||||
1 | Beta-methoxyamphetamine | Drug Info | [89] |
Cell-based Target Expression Variations | Top | |||||
---|---|---|---|---|---|---|
Cell-based Target Expression Variations |
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 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 Pathway Affiliation
Biological Network Descriptors
|
There is no similarity protein (E value < 0.005) for this target
|
KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
---|---|---|---|
Synaptic vesicle cycle | hsa04721 | Affiliated Target |
|
Class: Organismal Systems => Nervous system | Pathway Hierarchy | ||
Dopaminergic synapse | hsa04728 | Affiliated Target |
|
Class: Organismal Systems => Nervous system | Pathway Hierarchy |
Degree | 5 | Degree centrality | 5.37E-04 | Betweenness centrality | 1.40E-04 |
---|---|---|---|---|---|
Closeness centrality | 2.03E-01 | Radiality | 1.35E+01 | Clustering coefficient | 1.00E-01 |
Neighborhood connectivity | 1.86E+01 | Topological coefficient | 2.07E-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-regulating microRNAs | ||||||
Target-interacting Proteins |
Target Profiles in Patients | Top | |||||
---|---|---|---|---|---|---|
Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
---|---|---|---|---|---|---|
KEGG Pathway | [+] 5 KEGG Pathways | + | ||||
1 | Dopaminergic synapse | |||||
2 | Parkinson's disease | |||||
3 | Cocaine addiction | |||||
4 | Amphetamine addiction | |||||
5 | Alcoholism | |||||
Panther Pathway | [+] 3 Panther Pathways | + | ||||
1 | Adrenaline and noradrenaline biosynthesis | |||||
2 | Parkinson disease | |||||
3 | Dopamine receptor mediated signaling pathway | |||||
PID Pathway | [+] 1 PID Pathways | + | ||||
1 | Alpha-synuclein signaling | |||||
Reactome | [+] 1 Reactome Pathways | + | ||||
1 | Na+/Cl- dependent neurotransmitter transporters | |||||
WikiPathways | [+] 6 WikiPathways | + | ||||
1 | Monoamine Transport | |||||
2 | NRF2 pathway | |||||
3 | Dopaminergic Neurogenesis | |||||
4 | Parkinsons Disease Pathway | |||||
5 | Transport of glucose and other sugars, bile salts and organic acids, metal ions and amine compounds | |||||
6 | Neurotransmitter Clearance In The Synaptic Cleft |
Target-Related Models and Studies | Top | |||||
---|---|---|---|---|---|---|
Target Validation |
References | Top | |||||
---|---|---|---|---|---|---|
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REF 26 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027571) | |||||
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REF 29 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011877) | |||||
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REF 34 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
REF 35 | Interaction of the anorectic medication, phendimetrazine, and its metabolites with monoamine transporters in rat brain. Eur J Pharmacol. 2002 Jun 28;447(1):51-7. | |||||
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. (Target id: 927). | |||||
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REF 38 | Emerging drugs for attention-deficit/hyperactivity disorder. Expert Opin Emerg Drugs. 2007 Sep;12(3):423-34. | |||||
REF 39 | Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26. | |||||
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REF 41 | Development of the dopamine transporter selective RTI-336 as a pharmacotherapy for cocaine abuse.AAPS J.2006 Mar 24;8(1):E196-203. | |||||
REF 42 | Amineptine in the treatment of amphetamine withdrawal: a placebo-controlled, randomised, double-blind study. J Med Assoc Thai. 1997 Sep;80(9):587-92. | |||||
REF 43 | Pharmacogenetics and obesity: common gene variants influence weight loss response of the norepinephrine/dopamine transporter inhibitor GW320659 in obese subjects. Pharmacogenet Genomics. 2005 Dec;15(12):883-9. | |||||
REF 44 | Clinical pipeline report, company report or official report of Neurosearch. | |||||
REF 45 | Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. | |||||
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REF 47 | Treating Attention-Deficit/Hyperactivity Disorder in Adults: Focus on Once-Daily Medications. Prim Care Companion CNS Disord 2011. | |||||
REF 48 | NSD-644: Phase I started.NeuroSearch A/S (CSE:NEUR), Ballerup, Denmark, GlaxoSmithKline plc (LSE:GSK; GSK), London, U.K. | |||||
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