Target Information

Target General Information

Top

Target ID

T21945 (Former ID: TTDC00304)

Target Name

Norepinephrine transporter (NET)

Synonyms

Solute carrier family 6 member 2; Sodium-dependent noradrenaline transporter; SLC6A2; NET1; NET; NAT1

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Gene Name

SLC6A2

Target Type

Successful target

[1]

Disease

[+] 11 Target-related Diseases

Acute pain [ICD-11: MG31]

Attention deficit hyperactivity disorder [ICD-11: 6A05]

Chronic pain [ICD-11: MG30]

Corneal disease [ICD-11: 9A76-9A78]

Depression [ICD-11: 6A70-6A7Z]

Glaucoma [ICD-11: 9C61]

Migraine [ICD-11: 8A80]

Nicotine use disorder [ICD-11: 6C4A]

Obesity [ICD-11: 5B80-5B81]

Pain [ICD-11: MG30-MG3Z]

Stomach cancer [ICD-11: 2B72]

Function

Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.

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BioChemical Class

Neurotransmitter:sodium symporter

UniProt ID

SC6A2_HUMAN

Sequence

MLLARMNPQVQPENNGADTGPEQPLRARKTAELLVVKERNGVQCLLAPRDGDAQPRETWG
KKIDFLLSVVGFAVDLANVWRFPYLCYKNGGGAFLIPYTLFLIIAGMPLFYMELALGQYN
REGAATVWKICPFFKGVGYAVILIALYVGFYYNVIIAWSLYYLFSSFTLNLPWTDCGHTW
NSPNCTDPKLLNGSVLGNHTKYSKYKFTPAAEFYERGVLHLHESSGIHDIGLPQWQLLLC
LMVVVIVLYFSLWKGVKTSGKVVWITATLPYFVLFVLLVHGVTLPGASNGINAYLHIDFY
RLKEATVWIDAATQIFFSLGAGFGVLIAFASYNKFDNNCYRDALLTSSINCITSFVSGFA
IFSILGYMAHEHKVNIEDVATEGAGLVFILYPEAISTLSGSTFWAVVFFVMLLALGLDSS
MGGMEAVITGLADDFQVLKRHRKLFTFGVTFSTFLLALFCITKGGIYVLTLLDTFAAGTS
ILFAVLMEAIGVSWFYGVDRFSNDIQQMMGFRPGLYWRLCWKFVSPAFLLFVVVVSIINF
KPLTYDDYIFPPWANWVGWGIALSSMVLVPIYVIYKFLSTQGSLWERLAYGITPENEHHL
VAQRDIRQFQLQHWLAI

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3D Structure

Click to Show 3D Structure of This Target

AlphaFold

Drugs and Modes of Action

Top

Approved Drug(s)

[+] 27 Approved Drugs

Acetaminophen

Drug Info

Approved

Pain

[2], [3], [4]

Amfepramone

Drug Info

Approved

Obesity

[5]

Amitriptyline

Drug Info

Approved

Depression

[6], [7], [8]

Amoxapine

Drug Info

Approved

Major depressive disorder

[7], [9], [10]

Atomoxetine

Drug Info

Approved

Attention deficit hyperactivity disorder

[11], [12]

Bupropion

Drug Info

Approved

Smoking dependence

[7]

Cocaine

Drug Info

Approved

Anaesthesia

[7], [13], [14]

Dasotraline

Drug Info

Approved

Attention deficit hyperactivity disorder

[15]

Desipramine

Drug Info

Approved

Attention deficit hyperactivity disorder

[7], [8], [16]

Desvenalfaxine succinate

Drug Info

Approved

Fibromyalgia

[17]

Duloxetine

Drug Info

Approved

Depression

[18], [8]

Imipramine

Drug Info

Approved

Depression

[7], [8], [19]

Iobenguane I-123

Drug Info

Approved

Neuroendocrine cancer

[20]

Levomilnacipran

Drug Info

Approved

Fibromyalgia

[21], [22]

Maprotiline

Drug Info

Approved

Major depressive disorder

[7]

Mazindol

Drug Info

Approved

Obesity

[23], [24]

Milnacipran

Drug Info

Approved

Depression

[25], [26]

Netarsudil

Drug Info

Approved

Open-angle glaucoma

[27]

Phenmetrazine

Drug Info

Approved

Obesity

[28]

Phentermine

Drug Info

Approved

Obesity

[29], [30]

Protriptyline

Drug Info

Approved

Depression

[7], [8], [31]

Reboxetine

Drug Info

Approved

Depression

[32], [8]

Sibutramine

Drug Info

Approved

Obesity

[33], [30]

Tapentadol hydrochloride

Drug Info

Approved

Acute pain

[20]

Trimipramine

Drug Info

Approved

Major depressive disorder

[7]

Venlafaxine

Drug Info

Approved

Depression

[34], [35]

SPN-812

Drug Info

Phase 4

Attention deficit hyperactivity disorder

[36]

Clinical Trial Drug(s)

[+] 17 Clinical Trial Drugs

Amitifadine

Drug Info

Phase 3

Obesity

[37], [38]

Bicifadine

Drug Info

Phase 3

Neuropathic pain

[39]

Bupropion+naltrexone

Drug Info

Phase 3

Obesity

[40]

Roclatan

Drug Info

Phase 3

Glaucoma/ocular hypertension

[41]

Suronacrine maleate

Drug Info

Phase 3

Cognitive impairment

[42]

18F-LMI-1195

Drug Info

Phase 2

Heart failure

[43]

BLI-1005

Drug Info

Phase 2

Major depressive disorder

[15]

MCT-125

Drug Info

Phase 2

Fatigue

[44]

Metaiodobenzylguanidine I-131

Drug Info

Phase 2

Neuroblastoma

[45]

NS 2359

Drug Info

Phase 2

Cocaine addiction

[15]

PDC-1421

Drug Info

Phase 2

Attention deficit hyperactivity disorder

[46]

Spiroglumide

Drug Info

Phase 2

Stomach disease

[47]

SPN-812

Drug Info

Phase 2

Attention deficit hyperactivity disorder

[48]

TD-9855

Drug Info

Phase 2

Pain

[49]

XEN-2174

Drug Info

Phase 2

Cancer related pain

[50]

BL-1021

Drug Info

Phase 1

Pain

[51]

GSK-1360707

Drug Info

Phase 1

Major depressive disorder

[52]

Discontinued Drug(s)

[+] 10 Discontinued Drugs

DOV-216303

Drug Info

Discontinued in Phase 2

Mood disorder

[26]

Esreboxetine

Drug Info

Discontinued in Phase 2

Fibromyalgia

[53]

Manifaxine

Drug Info

Discontinued in Phase 2

Major depressive disorder

[54]

Napitane mesilate

Drug Info

Discontinued in Phase 2

Major depressive disorder

[55]

NS-2389

Drug Info

Discontinued in Phase 2

Major depressive disorder

[56]

R-sibutramine metabolite

Drug Info

Discontinued in Phase 2

Attention deficit hyperactivity disorder

[26]

Radafaxine

Drug Info

Discontinued in Phase 2

Major depressive disorder

[57]

SPD-473

Drug Info

Discontinued in Phase 2

Mood disorder

[58]

NSD-644

Drug Info

Discontinued in Phase 1

Neurological disorder

[59]

RG-7166

Drug Info

Discontinued in Phase 1

Major depressive disorder

[60]

Mode of Action

[+] 7 Modes of Action

Inhibitor

[+] 207 Inhibitor drugs

Acetaminophen

Drug Info

[61]

Amfepramone

Drug Info

[5], [62]

Amitriptyline

Drug Info

[63], [64]

Amoxapine

Drug Info

[65]

Atomoxetine

Drug Info

[66], [67]

Bupropion

Drug Info

[1]

Cocaine

Drug Info

[68]

Dasotraline

Drug Info

[69]

Desipramine

Drug Info

[61]

Desvenalfaxine succinate

Drug Info

[17]

Duloxetine

Drug Info

[70], [71]

Imipramine

Drug Info

[72], [73]

Iobenguane I-123

Drug Info

[74]

Maprotiline

Drug Info

[75]

Milnacipran

Drug Info

[78]

Phenmetrazine

Drug Info

[80]

Phentermine

Drug Info

[81]

Protriptyline

Drug Info

[82]

Reboxetine

Drug Info

[83]

Trimipramine

Drug Info

[84]

Venlafaxine

Drug Info

[1]

Hypericum

Drug Info

[85]

Amitifadine

Drug Info

[74]

Bupropion+naltrexone

Drug Info

[30]

BLI-1005

Drug Info

[15]

MCT-125

Drug Info

[74]

NS 2359

Drug Info

[26], [92]

PDC-1421

Drug Info

[93]

Spiroglumide

Drug Info

[39]

SPN-812

Drug Info

[15]

XEN-2174

Drug Info

[94]

GSK-1360707

Drug Info

[96]

DOV-216303

Drug Info

[26]

Radafaxine

Drug Info

[57], [102]

SPD-473

Drug Info

[103]

RG-7166

Drug Info

[105]

((3R,4R)-4-(o-tolyloxy)chroman-3-yl)methanamine

Drug Info

[106]

(+/-)-3-((naphthalen-2-yloxy)methyl)pyrrolidine

Drug Info

[107]

(2S,3S)-2-(m-Tolyl)-3,5,5-trimethylmorpholin-2-ol

Drug Info

[108]

(2S,3S)-2-Phenyl-3,5,5-trimethylmorpholin-2-ol

Drug Info

[108]

(R)-1-((S)-morpholin-2-yl)-1,2-diphenylethanol

Drug Info

[109]

(R)-2-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol

Drug Info

[110]

(R)-3-(naphthalen-2-ylmethoxy)pyrrolidine

Drug Info

[107]

(R)-6-(pyrrolidin-3-ylmethoxy)-2-naphthonitrile

Drug Info

[107]

(R)-DULOXETINE

Drug Info

[111]

(R)-N-isobutyl-N-(pyrrolidin-3-yl)-2-naphthamide

Drug Info

[112]

(R)-N-isopropyl-N-(pyrrolidin-3-yl)-2-naphthamide

Drug Info

[112]

(R)-Norfluoxetine

Drug Info

[113]

(S)-3-(naphthalen-2-ylmethoxy)pyrrolidine

Drug Info

[107]

(S)-6-(pyrrolidin-3-ylmethoxy)-2-naphthonitrile

Drug Info

[107]

(S)-N-isobutyl-N-(pyrrolidin-3-yl)-2-naphthamide

Drug Info

[112]

(S)-NORDULOXETINE

Drug Info

[111]

(S)-Norfluoxetine

Drug Info

[113]

1-(1,2-diphenylethyl)piperazine

Drug Info

[114]

1-(1,4-diphenylbutan-2-yl)piperazine

Drug Info

[115]

1-(1-(2-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX)

Drug Info

[110]

1-(1-(4-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX)

Drug Info

[110]

1-(1-phenyl-2-(2-propoxyphenyl)ethyl)piperazine

Drug Info

[110]

1-(1-phenyl-2-o-tolylethyl)piperazine

Drug Info

[114]

1-(2,3-Dihydro-1H-indol-5-ylmethyl)-propylamine

Drug Info

[116]

1-(2-((3-fluorophenoxy)methyl)phenyl)piperazine

Drug Info

[117]

1-(2-(2-(DIFLUOROMETHOXY)PHENYL)-1-PHENYLETHYL)PIPERAZINE (ENANTIOMERIC MIX)

Drug Info

[110]

1-(2-(2-bromophenyl)-1-phenylethyl)piperazine

Drug Info

[114]

1-(2-(2-chlorophenoxy)pyridin-3-yl)piperazine

Drug Info

[118]

1-(2-(2-chlorophenyl)-1-phenylethyl)piperazine

Drug Info

[114]

1-(2-(2-ethoxyphenyl)-1-phenylethyl)piperazine

Drug Info

[114]

1-(2-(2-ethylphenyl)-1-phenylethyl)piperazine

Drug Info

[114]

1-(2-(2-fluorobenzyloxy)phenyl)piperazine

Drug Info

[117]

1-(2-(2-methoxyphenyl)-1-phenylethyl)piperazine

Drug Info

[110]

1-(2-(3-chlorophenyl)-1-phenylethyl)piperazine

Drug Info

[114]

1-(2-(3-fluorophenoxy)phenyl)piperazine

Drug Info

[117]

1-(2-(3-methoxyphenyl)-1-phenylethyl)piperazine

Drug Info

[114]

1-(2-(4-fluorophenoxy)phenyl)piperazine

Drug Info

[117]

1-(2-(6-fluoronaphthalen-2-yl)ethyl)piperazine

Drug Info

[107]

1-(2-(benzyloxy)phenyl)piperazine

Drug Info

[117]

1-(2-(phenoxymethyl)phenyl)piperazine

Drug Info

[117]

1-(2-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one

Drug Info

[119]

1-(2-phenoxyphenyl)piperazine

Drug Info

[117]

1-(3,4-Dichloro-phenyl)-3-diethylamino-indan-5-ol

Drug Info

[120]

1-(3,4-Dichloro-phenyl)-3-methylamino-indan-5-ol

Drug Info

[120]

1-(3-bromophenyl)-2-(tert-butylamino)propan-1-one

Drug Info

[121]

1-(3-chlorophenyl)-2-(dimethylamino)propan-1-one

Drug Info

[121]

1-(3-chlorophenyl)-2-(piperidin-1-yl)propan-1-one

Drug Info

[121]

1-(3-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one

Drug Info

[119]

1-(3-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one

Drug Info

[119]

1-(4-bromophenyl)-2-(tert-butylamino)propan-1-one

Drug Info

[121]

1-(4-bromophenyl)-2-pyrrolidin-1-yl-pentan-1-one

Drug Info

[119]

1-(4-fluorophenyl)-2-pyrrolidin-1-yl-pentan-1-one

Drug Info

[119]

1-(4-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one

Drug Info

[119]

1-(4-nitrophenyl)-2-pyrrolidin-1-yl-pentan-1-one

Drug Info

[119]

1-naphthalen-2-yl-2-pyrrolidin-1-yl-pentan-1-one

Drug Info

[119]

1S,2R-milnacipran

Drug Info

[122]

2-((2-iodophenoxy)(phenyl)methyl)morpholine

Drug Info

[123]

2-((3-iodophenyl)(o-tolyloxy)methyl)morpholine

Drug Info

[123]

2-(2'-Aminoethyl)-5-benzyltetrahydrofuran

Drug Info

[124]

2-(2,3-Dihydro-1H-indol-5-yl)-1-methyl-ethylamine

Drug Info

[116]

2-(2-chlorophenoxy)-3-(piperidin-4-yl)pyridine

Drug Info

[118]

2-(2-fluorophenoxy)-3-(piperidin-4-yl)pyridine

Drug Info

[118]

2-(2-methoxyphenoxy)-3-(piperidin-4-yl)pyridine

Drug Info

[118]

100

2-(2-phenyl-2-(piperazin-1-yl)ethyl)benzonitrile

Drug Info

[114]

101

2-(Aminomethyl)-5-(1'-naphthethyl)tetrahydrofuran

Drug Info

[124]

102

2-(Aminomethyl)-5-(1'-naphthyl)tetrahydrofuran

Drug Info

[124]

103

2-(Aminomethyl)-5-(2'-naphthyl)tetrahydrofuran

Drug Info

[124]

104

2-(Aminomethyl)-5-phenethyltetrahydrofuran

Drug Info

[124]

105

2-(N,N-Diethylamino)-3'-chloropropiophenone

Drug Info

[125]

106

2-(N-Cyclopentylamino)-3'-bromopropiophenone

Drug Info

[121]

107

2-(N-Cyclopentylamino)-3'-chloropropiophenone

Drug Info

[125]

108

2-(N-Cyclopentylamino)-3'-fluoropropiophenone

Drug Info

[121]

109

2-(N-Cyclopentylamino)-3'-methoxypropiophenone

Drug Info

[121]

110

2-(N-Cyclopentylamino)-3'-methylpropiophenone

Drug Info

[121]

111

2-(N-Cyclopropylamino)-3-chloropropiophenone

Drug Info

[125]

112

2-(N-Pyrrolidinyl)-3'-bromopropiophenone

Drug Info

[121]

113

2-(N-Pyrrolidinyl)-3'-fluoropropiophenone

Drug Info

[121]

114

2-(N-Pyrrolidinyl)-3'-methoxypropiophenone

Drug Info

[121]

115

2-(N-Pyrrolidinyl)-3'-methylpropiophenone

Drug Info

[121]

116

2-(N-Pyrrolidinyl)-3'-nitropropiophenone

Drug Info

[121]

117

2-(N-tert-Butylamino)-3',4'-dichloropropiophenone

Drug Info

[125]

118

2-(N-tert-Butylamino)-3'-chloroheptanophenone

Drug Info

[125]

119

2-(N-tert-Butylamino)-3'-chlorohexanophenone

Drug Info

[125]

120

2-(N-tert-Butylamino)-3'-chlorooctanophenone

Drug Info

[125]

121

2-(N-tert-Butylamino)-3'-chloropentanophenone

Drug Info

[125]

122

2-(N-tert-Butylamino)propiophenone

Drug Info

[125]

123

2-(tert-butylamino)-1-(3-chlorophenyl)butan-1-one

Drug Info

[121]

124

2-(tert-butylamino)-1-m-tolylpropan-1-one

Drug Info

[121]

125

2-(tert-butylamino)-1-p-tolylpropan-1-one

Drug Info

[121]

126

2-(tert-Butylamino)-3',4'-dichlorobutyrophenone

Drug Info

[125]

127

2-(tert-Butylamino)-3',4'-dichloropentanophenone

Drug Info

[125]

128

2-Amino-1-(4-methylthiophenyl)propane

Drug Info

[126]

129

2-Aminomethyl-5-(p-bromophenyl)tetrahydrofuran

Drug Info

[124]

130

2-Aminomethyl-5-(p-chlorophenyl)tetrahydrofuran

Drug Info

[124]

131

2-Aminomethyl-5-(p-methoxyphenyl)tetrahydrofuran

Drug Info

[124]

132

2-Aminomethyl-5-(p-t-butylphenyl)tetrahydrofuran

Drug Info

[124]

133

2-Aminomethyl-5-(phenyl)tetrahydrofuran

Drug Info

[124]

134

2-phenoxy-3-(piperidin-4-yl)pyridine

Drug Info

[118]

135

2pyrrolidin-1-yl-1-phenylpentan-1-one

Drug Info

[119]

136

3-(1H-indol-1-yl)-N-methyl-3-phenylpropan-1-amine

Drug Info

[127]

137

3-(2-phenyl-2-(piperazin-1-yl)ethyl)benzonitrile

Drug Info

[114]

138

3-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol

Drug Info

[114]

139

3-(3'-furyl)-aniline

Drug Info

[128]

140

3-(piperidin-4-yl)-2-(o-tolyloxy)pyridine

Drug Info

[118]

141

3-p-Tolyl-8-aza-bicyclo[3.2.1]octane

Drug Info

[129]

142

3alpha-(bis-chloro-phenylmethoxy)tropane

Drug Info

[130]

143

4-((naphthalen-2-yloxy)methyl)piperidine

Drug Info

[107]

144

4-(1H-indol-3-yl)-N,N-dimethylcyclohex-3-enamine

Drug Info

[131]

145

4-(2-((3-fluorophenoxy)methyl)phenyl)piperidine

Drug Info

[117]

146

4-(2-(2-fluoro-5-methylphenoxy)phenyl)piperidine

Drug Info

[117]

147

4-(2-(2-fluorobenzyloxy)phenyl)piperidine

Drug Info

[117]

148

4-(2-(3-chlorophenoxy)phenyl)piperidine

Drug Info

[117]

149

4-(2-(3-fluorophenoxy)-4-methylphenyl)piperidine

Drug Info

[117]

150

4-(2-(3-fluorophenoxy)phenyl)piperidine

Drug Info

[117]

151

4-(2-(4-fluorobenzyloxy)phenyl)piperidine

Drug Info

[117]

152

4-(2-(4-fluorophenoxy)-4-methylphenyl)piperidine

Drug Info

[117]

153

4-(2-(4-fluorophenoxy)phenyl)piperidine

Drug Info

[117]

154

4-(2-(benzyloxy)-3-fluorophenyl)piperidine

Drug Info

[117]

155

4-(2-(benzyloxy)-6-fluorophenyl)piperidine

Drug Info

[117]

156

4-(2-(benzyloxy)phenyl)piperidine

Drug Info

[117]

157

4-(2-(phenoxymethyl)phenyl)piperidine

Drug Info

[117]

158

4-(2-fluoro-6-(2-fluorophenoxy)phenyl)piperidine

Drug Info

[118]

159

4-(2-fluoro-6-(3-fluorophenoxy)phenyl)piperidine

Drug Info

[117]

160

4-(2-fluoro-6-(4-fluorophenoxy)phenyl)piperidine

Drug Info

[117]

161

4-(2-fluoro-6-phenoxyphenyl)piperidine

Drug Info

[117]

162

4-(2-phenoxyphenyl)piperidine

Drug Info

[117]

163

4-(3'-furyl)-aniline

Drug Info

[128]

164

4-(3-fluoro-2-phenoxyphenyl)piperidine

Drug Info

[117]

165

4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one

Drug Info

[132]

166

6-(piperidin-4-ylmethoxy)-2-naphthonitrile

Drug Info

[107]

167

7-(piperidin-4-ylmethoxy)-2-naphthonitrile

Drug Info

[107]

168

8-Methyl-3-p-tolyl-8-aza-bicyclo[3.2.1]octane

Drug Info

[129]

169

AMIFLAMINE

Drug Info

[116]

170

Biphenyl-2-ylmethyl-(S)-pyrrolidin-3-yl-amine

Drug Info

[133]

171

Cis-3-phenoxy-2,3-dihydro-1H-inden-1-amine

Drug Info

[134]

172

D-166A

Drug Info

[135]

173

D-211A

Drug Info

[135]

174

D-211B

Drug Info

[135]

175

D-254C

Drug Info

[135]

176

D-257A

Drug Info

[135]

177

D-257C

Drug Info

[135]

178

Difluorobenztropine

Drug Info

[130]

179

Isobutyl-(4-methyl-benzyl)-piperidin-4-yl-amine

Drug Info

[136]

180

KF-A5

Drug Info

[137]

181

MDL-28618

Drug Info

[106]

182

METHYLENEDIOXYAMPHETAMINE

Drug Info

[138]

183

METHYLENEDIOXYMETHAMPHETAMINE

Drug Info

[126], [139]

184

N,N-dimethyl(2-phenoxyphenyl)methanamine

Drug Info

[141]

185

N-(2-oxazolemethyl)milnacipran

Drug Info

[142]

186

N-benzyl-N-isobutylpiperidin-4-amine

Drug Info

[136]

187

N-desalkylquetiapine

Drug Info

[143]

188

NISOXETINE

Drug Info

[144]

189

norzotepine

Drug Info

[145]

190

Para-chloroamphetamine

Drug Info

[126]

191

PF-18298

Drug Info

[110]

192

PF-3409409

Drug Info

[146]

193

PF-526014

Drug Info

[110]

194

POLYGALATENOSIDE B

Drug Info

[147]

195

PTI-601

Drug Info

[74]

196

PYROVALERONE

Drug Info

[119]

197

R-NORDULOXETINE

Drug Info

[111]

198

RTI-219

Drug Info

[148]

199

S-34324

Drug Info

[149]

200

S33005

Drug Info

[150]

201

Trans-3-(o-tolyloxy)-2,3-dihydro-1H-inden-1-amine

Drug Info

[134]

202

WAY-256805

Drug Info

[151]

203

WIN-35066-2

Drug Info

[152]

204

[3-(3,4-Dichloro-phenyl)-indan-1-yl]-methyl-amine

Drug Info

[120]

205

[3H]nisoxetine

Drug Info

[74]

206

[3H]WIN35428

Drug Info

[153]

207

{2-[3-(Phenylsulfonyl)-1H-indol-4-yl]ethyl}amine

Drug Info

[154]

Modulator

[+] 16 Modulator drugs

Levomilnacipran

Drug Info

[22]

Mazindol

Drug Info

[76], [77]

Netarsudil

Drug Info

[79]

Sibutramine

Drug Info

[77]

Tapentadol hydrochloride

Drug Info

[20]

Bicifadine

Drug Info

[87]

Roclatan

Drug Info

[88]

Suronacrine maleate

Drug Info

[89]

Metaiodobenzylguanidine I-131

Drug Info

[91]

TD-9855

Drug Info

[49]

BL-1021

Drug Info

[95]

Manifaxine

Drug Info

[98]

Napitane mesilate

Drug Info

[99]

NS-2389

Drug Info

[100]

R-sibutramine metabolite

Drug Info

[101]

MMDA

Drug Info

[140]

Antagonist

[+] 1 Antagonist drugs

SPN-812

Drug Info

[86]

Enhancer

[+] 1 Enhancer drugs

18F-LMI-1195

Drug Info

[90]

Blocker

[+] 1 Blocker drugs

Esreboxetine

Drug Info

[97]

Activator

[+] 1 Activator drugs

NSD-644

Drug Info

[104]

Agonist

[+] 1 Agonist drugs

TQ-1017

Drug Info

[7]

Cell-based Target Expression Variations

Top

Cell-based Target Expression Variations

Cell-based Target Expression Variations Info

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). Human Similarity Proteins Human Pathway Affiliation

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).

Human Similarity Proteins

Human Pathway Affiliation

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

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

Co-Targets Info

Target Poor or Non Binders

Top

Target Poor or Non Binders

Target Poor or Non Binders Info

Target Profiles in Patients

Top

Target Expression
Profile (TEP)

Target Expression Profile Info

Target Affiliated Biological Pathways

Top

Panther Pathway

[+] 1 Panther Pathways

Adrenaline and noradrenaline biosynthesis

Reactome

[+] 1 Reactome Pathways

Na+/Cl- dependent neurotransmitter transporters

WikiPathways

[+] 3 WikiPathways

Monoamine Transport

NRF2 pathway

Transport of glucose and other sugars, bile salts and organic acids, metal ions and amine compounds

Target-Related Models and Studies

Top

Target Validation

Target Validation Info

References

Top

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