Target Validation Information
Target ID T21945
Target Name Sodium-dependent noradrenaline transporter
Target Type
Successful
Drug Potency against Target Trimipramine Drug Info IC50 = 1000 nM [553151]
Diethylpropion Drug Info IC50 = 18100 nM [552237]
Reboxetine Drug Info IC50 = 8 nM [552411]
Phenmetrazine Drug Info EC50 = 50 nM [535503]
Desipramine Drug Info IC50 = 3.4 nM [553048]
WAY-256805 Drug Info IC50 = 82 nM [529536]
R-sibutramine metabolite Drug Info Ki = 66 nM [553116]
4-(2-(4-fluorophenoxy)phenyl)piperidine Drug Info Ki = 21 nM [530474]
MDL-28618 Drug Info IC50 = 880 nM [529620]
((3R,4R)-4-(o-tolyloxy)chroman-3-yl)methanamine Drug Info IC50 = 46 nM [529620]
1-(2-(2-chlorophenoxy)pyridin-3-yl)piperazine Drug Info Ki = 747 nM [530596]
4-(2-((3-fluorophenoxy)methyl)phenyl)piperidine Drug Info Ki = 1940 nM [530474]
1-(2-phenoxyphenyl)piperazine Drug Info Ki = 554 nM [530474]
4-(2-(benzyloxy)-6-fluorophenyl)piperidine Drug Info Ki = 9 nM [530474]
2-(2-methoxyphenoxy)-3-(piperidin-4-yl)pyridine Drug Info Ki = 292 nM [530596]
POLYGALATENOSIDE B Drug Info IC50 = 6040 nM [528443]
2-(2,3-Dihydro-1H-indol-5-yl)-1-methyl-ethylamine Drug Info IC50 = 360 nM [533479]
N,N-dimethyl(2-phenoxyphenyl)methanamine Drug Info IC50 = 70 nM [529278]
(R)-1-((S)-morpholin-2-yl)-1,2-diphenylethanol Drug Info Ki = 148 nM [527968]
Mazindol Drug Info ED50 = 1.5 nM [553256]
{2-[3-(Phenylsulfonyl)-1H-indol-4-yl]ethyl}amine Drug Info IC50 = 960 nM [530455]
Duloxetine Drug Info Ki = 4.6 nM [527799]
D-211B Drug Info Ki = 418 nM [529287]
2-((2-iodophenoxy)(phenyl)methyl)morpholine Drug Info Ki = 2.47 nM [528517]
NISOXETINE Drug Info IC50 = 6 nM [529670]
METHYLENEDIOXYAMPHETAMINE Drug Info IC50 = 266 nM [530914]
DOV-216303 Drug Info Ki = 20.3 nM [527289]
1-(3-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 9.4 nM [528036]
PYROVALERONE Drug Info IC50 = 28.3 nM [528036]
DOV 21947 Drug Info Ki = 22.8 nM [552331]
Bupropion Drug Info Ki = 1900 nM [552892]
Nortriptyline Drug Info IC50 = 177 nM [552373]
N-(2-oxazolemethyl)milnacipran Drug Info IC50 = 450 nM [529263]
PF-3409409 Drug Info Ki = 6 nM [530265]
1-(3,4-dichlorophenyl)-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 72.4 nM [531114]
Biphenyl-2-ylmethyl-(S)-pyrrolidin-3-yl-amine Drug Info Ki = 271 nM [529592]
RTI-219 Drug Info IC50 = 750 nM [528932]
(R)-Norfluoxetine Drug Info IC50 = 1995 nM [529814]
Radaxafine HCl Drug Info IC50 = 1400 nM [552753]
3-(1H-indol-1-yl)-N-methyl-3-phenylpropan-1-amine Drug Info IC50 = 47 nM [529764]
2-Amino-1-(4-methylthiophenyl)propane Drug Info IC50 = 2375 nM [530347]
4-(2-(benzyloxy)phenyl)piperidine Drug Info Ki = 76 nM [530474]
2-(N-tert-Butylamino)-3',4'-dichloropropiophenone Drug Info Ki = 5400 nM [530442]
2-(2-chlorophenoxy)-3-(piperidin-4-yl)pyridine Drug Info Ki = 74 nM [530596]
4-(2-fluoro-6-(3-fluorophenoxy)phenyl)piperidine Drug Info Ki = 18 nM [530474]
2-(tert-butylamino)-1-(3-chlorophenyl)butan-1-one Drug Info IC50 = 607 nM [530728]
1-(3-bromophenyl)-2-(tert-butylamino)propan-1-one Drug Info IC50 = 5600 nM [530728]
2-(N-Cyclopentylamino)-3'-fluoropropiophenone Drug Info IC50 = 2850 nM [530728]
4-(2-(3-fluorophenoxy)phenyl)piperidine Drug Info Ki = 11 nM [530474]
(S)-6-(pyrrolidin-3-ylmethoxy)-2-naphthonitrile Drug Info IC50 = 200 nM [530012]
2-Aminomethyl-5-(p-t-butylphenyl)tetrahydrofuran Drug Info IC50 = 2322 nM [529955]
Trans-3-(o-tolyloxy)-2,3-dihydro-1H-inden-1-amine Drug Info IC50 = 840 nM [529530]
2-((3-iodophenyl)(o-tolyloxy)methyl)morpholine Drug Info Ki = 27.6 nM [528517]
2-(N-tert-Butylamino)propiophenone Drug Info Ki = 5700 nM [530442]
2-(N-tert-Butylamino)-3'-chloropentanophenone Drug Info IC50 = 472 nM [530442]
2-(N-Pyrrolidinyl)-3'-methoxypropiophenone Drug Info IC50 = 718 nM [530728]
2-(N-tert-Butylamino)-3'-chlorooctanophenone Drug Info IC50 = 4890 nM [530442]
WIN_35428 Drug Info IC50 = 1230 nM [534240]
1-(1-phenyl-2-(2-propoxyphenyl)ethyl)piperazine Drug Info Ki = 31 nM [530918]
(S)-NORDULOXETINE Drug Info IC50 = 445 nM [530368]
3-(2-phenyl-2-(piperazin-1-yl)ethyl)benzonitrile Drug Info IC50 = 300 nM [528224]
4-(2-fluoro-6-(2-fluorophenoxy)phenyl)piperidine Drug Info Ki = 32 nM [530596]
2-(2-phenyl-2-(piperazin-1-yl)ethyl)benzonitrile Drug Info IC50 = 73 nM [528224]
1-(2-(2-(DIFLUOROMETHOXY)PHENYL)-1-PHENYLETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info Ki = 180 nM [530918]
2-(2-fluorophenoxy)-3-(piperidin-4-yl)pyridine Drug Info Ki = 536 nM [530596]
2-(Aminomethyl)-5-phenethyltetrahydrofuran Drug Info IC50 = 360 nM [529955]
2-Aminomethyl-5-(phenyl)tetrahydrofuran Drug Info IC50 = 23 nM [529955]
(S)-3-(naphthalen-2-ylmethoxy)pyrrolidine Drug Info IC50 = 2900 nM [530012]
1-(2-(3-chlorophenyl)-1-phenylethyl)piperazine Drug Info IC50 = 54 nM [528224]
1-(2-(phenoxymethyl)phenyl)piperazine Drug Info Ki = 183 nM [530474]
1-(4-fluorophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 171 nM [528036]
1-(2-(4-fluorophenoxy)phenyl)piperazine Drug Info Ki = 1710 nM [530474]
1-(2-(2-bromophenyl)-1-phenylethyl)piperazine Drug Info IC50 = 35 nM [528224]
2-(N-Pyrrolidinyl)-3'-methylpropiophenone Drug Info IC50 = 577 nM [530728]
1-(3-chlorophenyl)-2-(piperidin-1-yl)propan-1-one Drug Info IC50 = 2520 nM [530728]
1-(2-(2-fluorobenzyloxy)phenyl)piperazine Drug Info Ki = 526 nM [530474]
1-(1,4-diphenylbutan-2-yl)piperazine Drug Info IC50 = 48 nM [528226]
3-(piperidin-4-yl)-2-(o-tolyloxy)pyridine Drug Info Ki = 330 nM [530596]
1-(2-(3-methoxyphenyl)-1-phenylethyl)piperazine Drug Info IC50 = 130 nM [528224]
4-(2-(3-fluorophenoxy)-4-methylphenyl)piperidine Drug Info Ki = 170 nM [530474]
4-(2-fluoro-6-phenoxyphenyl)piperidine Drug Info Ki = 170 nM [530474]
4-(2-(4-fluorophenoxy)-4-methylphenyl)piperidine Drug Info Ki = 115 nM [530474]
4-(2-(3-chlorophenoxy)phenyl)piperidine Drug Info Ki = 13 nM [530474]
1-(3,4-Dichloro-phenyl)-3-diethylamino-indan-5-ol Drug Info Ki = 1330 nM [527062]
2-(N-Pyrrolidinyl)-3'-fluoropropiophenone Drug Info IC50 = 135 nM [530728]
AMIFLAMINE Drug Info IC50 = 650 nM [533479]
1-(4-bromophenyl)-2-(tert-butylamino)propan-1-one Drug Info IC50 = 2540 nM [530728]
2-(tert-butylamino)-1-p-tolylpropan-1-one Drug Info IC50 = 2350 nM [530728]
1-(3-chlorophenyl)-2-(dimethylamino)propan-1-one Drug Info IC50 = 1520 nM [530728]
PF-526014 Drug Info Ki = 12 nM [530918]
Bicifadine Drug Info IC50 = 55 nM [529523]
1-(2-((3-fluorophenoxy)methyl)phenyl)piperazine Drug Info Ki = 104 nM [530474]
(R)-DULOXETINE Drug Info IC50 = 13.2 nM [530368]
1-(2-(2-chlorophenyl)-1-phenylethyl)piperazine Drug Info IC50 = 22 nM [528224]
4-(2-(phenoxymethyl)phenyl)piperidine Drug Info Ki = 1710 nM [530474]
Para-chloroamphetamine Drug Info IC50 = 207 nM [530347]
3-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol Drug Info IC50 = 14 nM [528224]
METHYLENEDIOXYMETHAMPHETAMINE Drug Info IC50 = 405 nM [530347]
1-(1-phenyl-2-o-tolylethyl)piperazine Drug Info IC50 = 90 nM [528224]
2-Aminomethyl-5-(p-bromophenyl)tetrahydrofuran Drug Info IC50 = 59 nM [529955]
1-(1,2-diphenylethyl)piperazine Drug Info IC50 = 39 nM [528224]
1-(4-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 46.5 nM [528036]
1-(3,4-Dichloro-phenyl)-3-methylamino-indan-5-ol Drug Info Ki = 24 nM [527062]
1-(2-(2-ethoxyphenyl)-1-phenylethyl)piperazine Drug Info IC50 = 16 nM [528224]
2-(Aminomethyl)-5-(2'-naphthyl)tetrahydrofuran Drug Info IC50 = 58 nM [529955]
4-(2-fluoro-6-(4-fluorophenoxy)phenyl)piperidine Drug Info Ki = 97 nM [530474]
1-naphthalen-2-yl-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 11.7 nM [528036]
3-p-Tolyl-8-aza-bicyclo[3.2.1]octane Drug Info Ki = 5.2 nM [525906]
4-(2-(2-fluorobenzyloxy)phenyl)piperidine Drug Info Ki = 34 nM [530474]
1-(2-(2-ethylphenyl)-1-phenylethyl)piperazine Drug Info IC50 = 72 nM [528224]
2-(Aminomethyl)-5-(1'-naphthyl)tetrahydrofuran Drug Info IC50 = 210 nM [529955]
(R)-N-isopropyl-N-(pyrrolidin-3-yl)-2-naphthamide Drug Info IC50 = 7500 nM [530367]
(R)-N-isobutyl-N-(pyrrolidin-3-yl)-2-naphthamide Drug Info IC50 = 1200 nM [530367]
2-(tert-Butylamino)-3',4'-dichlorobutyrophenone Drug Info IC50 = 135 nM [530442]
1-(2-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 19.7 nM [528036]
PF-18298 Drug Info Ki = 21 nM [530918]
(R)-2-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol Drug Info Ki = 58 nM [530918]
S-34324 Drug Info Ki = 365 nM [527481]
Imipramine Drug Info pKi < 5 [552587]
[3-(3,4-Dichloro-phenyl)-indan-1-yl]-methyl-amine Drug Info Ki = 11 nM [527062]
D-211A Drug Info Ki = 388 nM [529287]
D-257A Drug Info Ki = 954 nM [529287]
R-NORDULOXETINE Drug Info IC50 = 188 nM [530368]
DIFLUOROBENZTROPINE Drug Info Ki = 844 nM [528473]
1-(2-(3-fluorophenoxy)phenyl)piperazine Drug Info Ki = 1720 nM [530474]
1-(3-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 81 nM [528036]
4-(3-fluoro-2-phenoxyphenyl)piperidine Drug Info Ki = 1370 nM [530474]
1-(2-(benzyloxy)phenyl)piperazine Drug Info Ki = 168 nM [530474]
2-Aminomethyl-5-(p-chlorophenyl)tetrahydrofuran Drug Info IC50 = 61 nM [529955]
4-(2-(benzyloxy)-3-fluorophenyl)piperidine Drug Info Ki = 9 nM [530474]
2-(N-Cyclopentylamino)-3'-bromopropiophenone Drug Info IC50 = 2530 nM [530728]
3alpha-(bis-chloro-phenylmethoxy)tropane Drug Info Ki = 2980 nM [528473]
2-(tert-butylamino)-1-m-tolylpropan-1-one Drug Info IC50 = 6200 nM [530728]
2-(2'-Aminoethyl)-5-benzyltetrahydrofuran Drug Info IC50 = 347 nM [529955]
2-(N-Cyclopentylamino)-3'-methoxypropiophenone Drug Info IC50 = 8200 nM [530728]
N-benzyl-N-isobutylpiperidin-4-amine Drug Info Ki = 91 nM [528048]
Isobutyl-(4-methyl-benzyl)-piperidin-4-yl-amine Drug Info Ki = 69 nM [528048]
1-(2-(2-methoxyphenyl)-1-phenylethyl)piperazine Drug Info Ki = 18 nM [530918]
7-(piperidin-4-ylmethoxy)-2-naphthonitrile Drug Info IC50 = 4400 nM [530012]
2-(N,N-Diethylamino)-3'-chloropropiophenone Drug Info Ki = 4476 nM [530442]
2-(N-tert-Butylamino)-3'-chloroheptanophenone Drug Info Ki = 4300 nM [530442]
2-(tert-Butylamino)-3',4'-dichloropentanophenone Drug Info IC50 = 43 nM [530442]
2-(N-tert-Butylamino)-3'-chlorohexanophenone Drug Info Ki = 3190 nM [530442]
2-(N-Cyclopropylamino)-3-chloropropiophenone Drug Info Ki = 4000 nM [530442]
2-(N-Pyrrolidinyl)-3'-nitropropiophenone Drug Info IC50 = 4100 nM [530728]
2-phenoxy-3-(piperidin-4-yl)pyridine Drug Info Ki = 2440 nM [530596]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [531079]
2-(N-Cyclopentylamino)-3'-methylpropiophenone Drug Info IC50 = 8700 nM [530728]
1-(2,3-Dihydro-1H-indol-5-ylmethyl)-propylamine Drug Info IC50 = 500 nM [533479]
1-(4-bromophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 83 nM [528036]
2-(N-Cyclopentylamino)-3'-chloropropiophenone Drug Info Ki = 5700 nM [530442]
(+/-)-3-((naphthalen-2-yloxy)methyl)pyrrolidine Drug Info IC50 = 1400 nM [530012]
4-(2-phenoxyphenyl)piperidine Drug Info Ki = 416 nM [530474]
2-Aminomethyl-5-(p-methoxyphenyl)tetrahydrofuran Drug Info IC50 = 92 nM [529955]
4-(2-(2-fluoro-5-methylphenoxy)phenyl)piperidine Drug Info Ki = 3 nM [530474]
(S)-N-isobutyl-N-(pyrrolidin-3-yl)-2-naphthamide Drug Info IC50 = 24 nM [530367]
2pyrrolidin-1-yl-1-phenylpentan-1-one Drug Info IC50 = 56 nM [528036]
2-(Aminomethyl)-5-(1'-naphthethyl)tetrahydrofuran Drug Info IC50 = 3420 nM [529955]
4-(2-(4-fluorobenzyloxy)phenyl)piperidine Drug Info Ki = 162 nM [530474]
6-(piperidin-4-ylmethoxy)-2-naphthonitrile Drug Info IC50 = 1900 nM [530012]
LITOXETINE Drug Info IC50 = 1400 nM [530367]
(R)-6-(pyrrolidin-3-ylmethoxy)-2-naphthonitrile Drug Info IC50 = 772 nM [530012]
1-(2-(6-fluoronaphthalen-2-yl)ethyl)piperazine Drug Info IC50 = 10500 nM [530012]
1-(1-(2-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info Ki = 17 nM [530918]
Levomilnacipran Drug Info IC50 = 100 nM [527799]
2-(N-Pyrrolidinyl)-3'-bromopropiophenone Drug Info IC50 = 1180 nM [530728]
D-257C Drug Info Ki = 319 nM [529287]
1S,2R-milnacipran Drug Info IC50 = 40 nM [529776]
(2S,3S)-2-(m-Tolyl)-3,5,5-trimethylmorpholin-2-ol Drug Info IC50 = 1130 nM [530946]
D-166A Drug Info Ki = 730 nM [529287]
D-254C Drug Info Ki = 170 nM [529287]
1-(4-nitrophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 531 nM [528036]
Reboxetine Drug Info Ki = 1.04 nM [529855]
(S)-Norfluoxetine Drug Info IC50 = 2806 nM [529814]
1-(1-(4-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info Ki = 30 nM [530918]
Desvenalfaxine succinate Drug Info Ki = 558.4 nM [552594]
WIN-35065-2 Drug Info IC50 = 920 nM [534240]
KF-A5 Drug Info IC50 = 9100 nM [529032]
Phentermine Drug Info EC50 = 39.4 nM [552643]
Venlafaxine Drug Info Ki = 640 nM [537564]
WIN-35066-2 Drug Info Ki = 550 nM [527309]
(2S,3S)-2-Phenyl-3,5,5-trimethylmorpholin-2-ol Drug Info IC50 = 550 nM [530946]
Cis-3-phenoxy-2,3-dihydro-1H-inden-1-amine Drug Info IC50 = 5000 nM [529530]
4-((naphthalen-2-yloxy)methyl)piperidine Drug Info IC50 = 1800 nM [530012]
(R)-3-(naphthalen-2-ylmethoxy)pyrrolidine Drug Info IC50 = 1200 nM [530012]
8-Methyl-3-p-tolyl-8-aza-bicyclo[3.2.1]octane Drug Info Ki = 160 nM [525906]
Action against Disease Model Sibutramine Uptake of 3H-dopamine in rat whole brain synaptosomes IC50: 2000 nM [552433] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations Extracellular clearance rate pof NET prolonged (sixfold);Amplitude of stimulated release of NET decreased by 55%;Basal extracellular of NET elevated twofold;Tissue content of NET decreased by 55%-75%;Synthesis rate of NET elevated by 70%;Postsynaptic receptors of NET is down-regulated [529536]
References
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