Target Validation Information
TTD ID T27812
Target Name Serotonin transporter (SERT)
Type of Target
Successful
Drug Potency against Target Drug Info IC50 = 1.5 nM [74]
Drug Info IC50 = 39 nM [74]
Drug Info IC50 = 1.8 nM [74]
Drug Info IC50 = 2700 nM [65]
Drug Info Ki = 22000 nM [71]
Amfepramone Drug Info IC50 = 311000 nM [63]
Cocaine Drug Info IC50 = 480 nM [73]
Dexfenfluramine Drug Info pKi = 5.41 [68]
Escitalopram Drug Info IC50 = 1.5 nM [69]
Fluoxetine Drug Info IC50 = 6.8 nM [74]
Fluvoxamine Drug Info IC50 = 3.8 nM [74]
Paroxetine Drug Info IC50 = 0.29 nM [74]
Sertraline Drug Info IC50 = 0.19 nM [74]
Sibutramine Drug Info IC50 = 477000 nM [62]
Tianeptine Drug Info IC50 = 11320 nM
Trazodone Drug Info IC50 = 0.58 mM [70]
Venlafaxine Drug Info IC50 = 210 nM
Drug Info Ki = 12 nM [67]
Drug Info IC50 = 0.5 nM [61]
Bicifadine Drug Info IC50 = 120 nM [28]
DOV-216303 Drug Info Ki = 13.8 nM [7]
OPC-14523 Drug Info IC50 = 80 nM [64]
R-sibutramine metabolite Drug Info Ki = 5100 nM [72]
YM-992 Drug Info Ki = 21 nM [61]
Drug Info Ki = 60.03 nM [4]
Drug Info IC50 = 14000 nM [56]
Drug Info Ki = 11216 nM [27]
Drug Info Ki = 150 nM [15]
Drug Info Ki = 2.8 nM [48]
Drug Info IC50 = 27 nM [28]
Drug Info Ki = 129 nM [48]
Drug Info Ki = 1.82 nM [4]
Drug Info IC50 = 664 nM [43]
Drug Info Ki = 3750 nM [15]
Drug Info IC50 = 2000 nM [59]
Drug Info Ki = 1.9 nM [2]
Drug Info Ki = 3260 nM [16]
Drug Info Ki = 364 nM [47]
Drug Info Ki = 1140 nM [47]
Drug Info IC50 = 5.4 nM [13]
Drug Info Ki = 1260 nM [50]
Drug Info IC50 = 14000 nM [56]
Drug Info Ki = 3260 nM [16]
Drug Info Ki = 17 nM [47]
Drug Info IC50 = 6900 nM [52]
Drug Info IC50 = 46 nM [11]
Drug Info IC50 = 6.8 nM [45]
Drug Info IC50 = 88 nM [40]
Drug Info IC50 = 664 nM [43]
Drug Info Ki = 1.82 nM [4]
Drug Info IC50 = 13 nM [13]
Drug Info Ki = 60.03 nM [4]
Drug Info IC50 = 230 nM [14]
Drug Info IC50 = 24 nM [39]
Drug Info Ki = 2.8 nM [48]
Drug Info IC50 = 27 nM [28]
Drug Info IC50 = 10000 nM [29]
Drug Info Ki = 150 nM [15]
Drug Info IC50 = 23 nM [14]
Drug Info IC50 = 20 nM [40]
Drug Info Ki = 10 nM [53]
Drug Info Ki = 1.9 nM [2]
Drug Info Ki = 3750 nM [15]
Drug Info Ki = 129 nM [48]
Drug Info IC50 = 660 nM [26]
Drug Info IC50 = 3 nM [44]
Drug Info Ki = 11216 nM [27]
Drug Info IC50 = 2710 nM [21]
Drug Info IC50 = 2000 nM [59]
Drug Info IC50 = 10 nM [44]
((3R,4R)-4-(o-tolyloxy)chroman-3-yl)methanamine Drug Info IC50 = 3800 nM [32]
(+/-)-3-((naphthalen-2-yloxy)methyl)pyrrolidine Drug Info IC50 = 25 nM [40]
(+/-)-nantenine Drug Info Ki = 244 nM [49]
(2R,3R)-iodoreboxetine Drug Info Ki = 646 nM [33]
(2R,3R)-iodoreboxetine Drug Info Ki = 646 nM [33]
(2R,3S)-2-[(2-Iodophenoxy)phenylmethyl]morpholine Drug Info Ki = 51.5 nM [42]
(2R,3S)-2-[(2-Iodophenoxy)phenylmethyl]morpholine Drug Info Ki = 51.5 nM [42]
(2R,3S)-2-[(3-Iodophenoxy)phenylmethyl]morpholine Drug Info Ki = 154 nM [42]
(2R,3S)-2-[(3-Iodophenoxy)phenylmethyl]morpholine Drug Info Ki = 154 nM [42]
(2R,3S)-2-[(4-Iodophenoxy)phenylmethyl]morpholine Drug Info Ki = 34.5 nM [42]
(2R,3S)-2-[(4-Iodophenoxy)phenylmethyl]morpholine Drug Info Ki = 34.5 nM [42]
(2S,3S)-iodoreboxetine Drug Info Ki = 2793 nM [33]
(2S,3S)-iodoreboxetine Drug Info Ki = 2793 nM [33]
(cis)-1,6-diphenyl-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 240 nM [28]
(cis)-1,6-diphenyl-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 240 nM [28]
(R)-2-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol Drug Info Ki = 8 nM [53]
(R)-6-(pyrrolidin-3-ylmethoxy)-2-naphthonitrile Drug Info IC50 = 42 nM [40]
(R)-DULOXETINE Drug Info Ki = 8.8 nM [37]
(R)-DULOXETINE Drug Info Ki = 8.8 nM [37]
(R)-N-isobutyl-N-(pyrrolidin-3-yl)-2-naphthamide Drug Info IC50 = 5 nM [44]
(R)-N-isopropyl-N-(pyrrolidin-3-yl)-2-naphthamide Drug Info IC50 = 15 nM [44]
(R)-Norfluoxetine Drug Info IC50 = 13 nM [36]
(S)-3-(naphthalen-2-ylmethoxy)pyrrolidine Drug Info IC50 = 23 nM [40]
(S)-6-(pyrrolidin-3-ylmethoxy)-2-naphthonitrile Drug Info IC50 = 37 nM [40]
(S)-NORDULOXETINE Drug Info IC50 = 25.6 nM [45]
(S)-Norfluoxetine Drug Info IC50 = 46 nM [36]
1-(1,2-diphenylethyl)piperazine Drug Info IC50 = 14 nM [13]
1-(1,4-diphenylbutan-2-yl)piperazine Drug Info IC50 = 23 nM [14]
1-(1-(2-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info Ki = 24 nM [53]
1-(1-(4-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info Ki = 24 nM [53]
1-(1-phenyl-2-(2-propoxyphenyl)ethyl)piperazine Drug Info Ki = 18 nM [53]
1-(1-phenyl-2-(pyridin-4-yl)ethyl)piperazine Drug Info IC50 = 38 nM [14]
1-(1-phenyl-2-o-tolylethyl)piperazine Drug Info IC50 = 12 nM [13]
1-(2-(2-(DIFLUOROMETHOXY)PHENYL)-1-PHENYLETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info Ki = 27 nM [53]
1-(2-(2-bromophenyl)-1-phenylethyl)piperazine Drug Info IC50 = 15 nM [13]
1-(2-(2-ethylphenyl)-1-phenylethyl)piperazine Drug Info IC50 = 16 nM [13]
1-(2-(2-fluorobenzyloxy)phenyl)piperazine Drug Info Ki = 978 nM [47]
1-(2-(2-methoxyphenyl)-1-phenylethyl)piperazine Drug Info Ki = 4 nM [53]
1-(2-(3-chlorophenyl)-1-phenylethyl)piperazine Drug Info IC50 = 9.4 nM [13]
1-(2-(3-fluorophenoxy)phenyl)piperazine Drug Info Ki = 3100 nM [47]
1-(2-(3-methoxyphenyl)-1-phenylethyl)piperazine Drug Info IC50 = 25 nM [13]
1-(2-(4-fluorophenoxy)phenyl)piperazine Drug Info Ki = 994 nM [47]
1-(2-(6-fluoronaphthalen-2-yl)ethyl)piperazine Drug Info IC50 = 11 nM [40]
1-(2-(naphthalen-1-yl)-1-phenylethyl)piperazine Drug Info IC50 = 12 nM [14]
1-(2-(naphthalen-2-yl)-1-phenylethyl)piperazine Drug Info IC50 = 17 nM [14]
1-(2-(phenoxymethyl)phenyl)piperazine Drug Info Ki = 780 nM [47]
1-(2-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 2020 nM [11]
1-(2-phenoxyphenyl)piperazine Drug Info Ki = 1880 nM [47]
1-(3,4-Dichloro-phenyl)-3-diethylamino-indan-5-ol Drug Info Ki = 0.7 nM [6]
1-(3,4-Dichloro-phenyl)-3-diethylamino-indan-5-ol Drug Info Ki = 0.7 nM [6]
1-(3,4-Dichloro-phenyl)-3-methylamino-indan-5-ol Drug Info Ki = 3 nM [6]
1-(3,4-Dichloro-phenyl)-3-methylamino-indan-5-ol Drug Info Ki = 3 nM [6]
1-(3-chlorophenyl)-2-(piperidin-1-yl)propan-1-one Drug Info Ki = 5479 nM [46]
1-(3-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 1070 nM [11]
1-(3-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 4400 nM [11]
1-(4-Benzylsulfanyl-phenyl)-propylamine Drug Info IC50 = 679 nM [43]
1-(4-Benzylsulfanyl-phenyl)-propylamine Drug Info IC50 = 679 nM [43]
1-(4-bromophenyl)-2-(tert-butylamino)propan-1-one Drug Info IC50 = 4508 nM [52]
1-(4-bromophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 1050 nM [11]
1-(4-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 197 nM [11]
1-(4-nitrophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 1110 nM [11]
1-(benzofuran-2-yl)-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 140 nM [28]
1-(benzofuran-2-yl)-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 140 nM [28]
1-(naphthalen-2-yl)-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 50 nM [28]
1-(naphthalen-2-yl)-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 50 nM [28]
1-(thiophen-2-yl)-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 4500 nM [28]
1-(thiophen-2-yl)-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 4500 nM [28]
1-Biphenyl-4-yl-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 160 nM [28]
1-Biphenyl-4-yl-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 160 nM [28]
1-fluoro-5-phenyl-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 2900 nM [28]
1-fluoro-5-phenyl-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 2900 nM [28]
1-Methyl-2-(4-phenylsulfanyl-phenyl)-ethylamine Drug Info IC50 = 14330 nM [43]
1-Methyl-2-(4-phenylsulfanyl-phenyl)-ethylamine Drug Info IC50 = 14330 nM [43]
1-Methyl-4-p-tolyl-piperidine-4-carbonitrile Drug Info Ki = 13700 nM [1]
1-Methyl-4-p-tolyl-piperidine-4-carbonitrile Drug Info Ki = 13700 nM [1]
1-phenyl-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 5200 nM [28]
1-phenyl-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 5200 nM [28]
10R-hydroxylobel-7-ene Drug Info Ki = 7500 nM [15]
10R-hydroxylobel-7-ene Drug Info Ki = 7500 nM [15]
10R-hydroxylobelane Drug Info Ki = 7300 nM [15]
10R-hydroxylobelane Drug Info Ki = 7300 nM [15]
10S-hydroxylobel-7-ene Drug Info Ki = 19000 nM [15]
10S-hydroxylobel-7-ene Drug Info Ki = 19000 nM [15]
10S-hydroxylobelane Drug Info Ki = 4270 nM [15]
10S-hydroxylobelane Drug Info Ki = 4270 nM [15]
1S,2R-milnacipran Drug Info IC50 = 28 nM [35]
1S,2R-milnacipran Drug Info IC50 = 28 nM [35]
2-(2'-Aminoethyl)-5-benzyltetrahydrofuran Drug Info IC50 = 2260 nM [39]
2-(2-chlorophenoxy)-3-(piperidin-4-yl)pyridine Drug Info Ki = 57 nM [50]
2-(2-fluorophenoxy)-3-(piperidin-4-yl)pyridine Drug Info Ki = 728 nM [50]
2-(2-methoxyphenoxy)-3-(piperidin-4-yl)pyridine Drug Info Ki = 610 nM [50]
2-(2-phenyl-2-(piperazin-1-yl)ethyl)benzonitrile Drug Info IC50 = 87 nM [13]
2-(3-Methyl-piperazin-1-yl)-6-nitro-quinoline Drug Info Ki = 22.19 nM [2]
2-(3-Methyl-piperazin-1-yl)-6-nitro-quinoline Drug Info Ki = 22.19 nM [2]
2-(Aminomethyl)-5-(1'-naphthethyl)tetrahydrofuran Drug Info IC50 = 23 nM [39]
2-(Aminomethyl)-5-(2'-naphthyl)tetrahydrofuran Drug Info IC50 = 4 nM [39]
2-(Aminomethyl)-5-phenethyltetrahydrofuran Drug Info IC50 = 129 nM [39]
2-(N-Cyclopropylamino)-3-chloropropiophenone Drug Info Ki = 3420 nM [46]
2-(N-tert-Butylamino)-3',4'-dichloropropiophenone Drug Info Ki = 1480 nM [46]
2-(tert-butylamino)-1-(3-chlorophenyl)butan-1-one Drug Info IC50 = 16000 nM [52]
2-(tert-Butylamino)-3',4'-dichlorobutyrophenone Drug Info IC50 = 790 nM [46]
2-(tert-Butylamino)-3',4'-dichloropentanophenone Drug Info Ki = 842 nM [46]
2-Amino-1-(4-ethylthiophenyl)butane Drug Info IC50 = 1290 nM [43]
2-Amino-1-(4-ethylthiophenyl)butane Drug Info IC50 = 1290 nM [43]
2-Amino-1-(4-ethylthiophenyl)propane Drug Info IC50 = 1403 nM [43]
2-Amino-1-(4-ethylthiophenyl)propane Drug Info IC50 = 1403 nM [43]
2-Amino-1-(4-methylthiophenyl)butane Drug Info IC50 = 611 nM [43]
2-Amino-1-(4-methylthiophenyl)butane Drug Info IC50 = 611 nM [43]
2-Amino-1-(4-methylthiophenyl)propane Drug Info IC50 = 74 nM [43]
2-Amino-1-(4-methylthiophenyl)propane Drug Info IC50 = 74 nM [43]
2-Aminomethyl-5-(p-bromophenyl)tetrahydrofuran Drug Info IC50 = 50 nM [39]
2-Aminomethyl-5-(p-chlorophenyl)tetrahydrofuran Drug Info IC50 = 32 nM [39]
2-Aminomethyl-5-(p-methoxyphenyl)tetrahydrofuran Drug Info IC50 = 617 nM [39]
2-Aminomethyl-5-(p-t-butylphenyl)tetrahydrofuran Drug Info IC50 = 636 nM [39]
2-Aminomethyl-5-(phenyl)tetrahydrofuran Drug Info IC50 = 1714 nM [39]
2-N,N-Dimethylamino-1-(4-methylthiophenyl)propane Drug Info IC50 = 520 nM [43]
2-N,N-Dimethylamino-1-(4-methylthiophenyl)propane Drug Info IC50 = 520 nM [43]
2-N-(Isopropyl)amino-1-(4-methylthiophenyl)butane Drug Info IC50 = 1939 nM [43]
2-N-(Isopropyl)amino-1-(4-methylthiophenyl)butane Drug Info IC50 = 1939 nM [43]
2-N-(n-Propyl)amino-1-(4-methylthiophenyl)butane Drug Info IC50 = 621 nM [43]
2-N-(n-Propyl)amino-1-(4-methylthiophenyl)butane Drug Info IC50 = 621 nM [43]
2-N-Allylamino-1-(4-methylthiophenyl)propan Drug Info IC50 = 524 nM [43]
2-N-Allylamino-1-(4-methylthiophenyl)propan Drug Info IC50 = 524 nM [43]
2-N-Cyclopropylamino-1-(4-methylthiophenyl)butane Drug Info IC50 = 872 nM [43]
2-N-Cyclopropylamino-1-(4-methylthiophenyl)butane Drug Info IC50 = 872 nM [43]
2-N-Ethylamino-1-(4-ethylthiophenyl)butane Drug Info IC50 = 1804 nM [43]
2-N-Ethylamino-1-(4-ethylthiophenyl)butane Drug Info IC50 = 1804 nM [43]
2-N-Ethylamino-1-(4-ethylthiophenyl)propane Drug Info IC50 = 478 nM [43]
2-N-Ethylamino-1-(4-ethylthiophenyl)propane Drug Info IC50 = 478 nM [43]
2-N-Ethylamino-1-(4-methylthiophenyl)butane Drug Info IC50 = 823 nM [43]
2-N-Ethylamino-1-(4-methylthiophenyl)butane Drug Info IC50 = 823 nM [43]
2-N-Ethylamino-1-(4-methylthiophenyl)propane Drug Info IC50 = 963 nM [43]
2-N-Ethylamino-1-(4-methylthiophenyl)propane Drug Info IC50 = 963 nM [43]
2-N-Hydroxyamino-1-(4-ethylthiophenyl)butane Drug Info IC50 = 1446 nM [43]
2-N-Hydroxyamino-1-(4-ethylthiophenyl)butane Drug Info IC50 = 1446 nM [43]
2-N-Hydroxyamino-1-(4-ethylthiophenyl)propane Drug Info IC50 = 625 nM [43]
2-N-Hydroxyamino-1-(4-ethylthiophenyl)propane Drug Info IC50 = 625 nM [43]
2-N-Hydroxyamino-1-(4-methylthiophenyl)butane Drug Info IC50 = 598 nM [43]
2-N-Hydroxyamino-1-(4-methylthiophenyl)butane Drug Info IC50 = 598 nM [43]
2-N-Hydroxyamino-1-(4-methylthiophenyl)propane Drug Info IC50 = 436 nM [43]
2-N-Hydroxyamino-1-(4-methylthiophenyl)propane Drug Info IC50 = 436 nM [43]
2-N-Methylamino-1-(4-ethylthiophenyl)propane Drug Info IC50 = 724 nM [43]
2-N-Methylamino-1-(4-ethylthiophenyl)propane Drug Info IC50 = 724 nM [43]
2-N-Methylamino-1-(4-methylthiophenyl)butane Drug Info IC50 = 437 nM [43]
2-N-Methylamino-1-(4-methylthiophenyl)butane Drug Info IC50 = 437 nM [43]
2-N-Methylamino-1-(4-methylthiophenyl)propane Drug Info IC50 = 417 nM [43]
2-N-Methylamino-1-(4-methylthiophenyl)propane Drug Info IC50 = 417 nM [43]
2-N-Propargylamino-1-(4-methylthiophenyl)butane Drug Info IC50 = 399 nM [43]
2-N-Propargylamino-1-(4-methylthiophenyl)butane Drug Info IC50 = 399 nM [43]
2-N-Propargylamino-1-(4-methylthiophenyl)propane Drug Info IC50 = 688 nM [43]
2-N-Propargylamino-1-(4-methylthiophenyl)propane Drug Info IC50 = 688 nM [43]
2-Naphthalen-2-ylmethyl-4,5-dihydro-1H-imidazole Drug Info IC50 = 887 nM [60]
2-Naphthalen-2-ylmethyl-4,5-dihydro-1H-imidazole Drug Info IC50 = 887 nM [60]
2-phenoxy-3-(piperidin-4-yl)pyridine Drug Info Ki = 1890 nM [50]
3-(1H-indol-1-yl)-N-methyl-3-phenylpropan-1-amine Drug Info IC50 = 327 nM [34]
3-(1H-indol-3-yl)-N,N-dimethylpropan-1-amine Drug Info IC50 = 58 nM [22]
3-(2-phenyl-2-(piperazin-1-yl)ethyl)benzamide Drug Info IC50 = 210 nM [13]
3-(2-phenyl-2-(piperazin-1-yl)ethyl)benzonitrile Drug Info IC50 = 4 nM [13]
3-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol Drug Info IC50 = 9.5 nM [13]
3-(3,4-dichlorophenyl)-2-nortropene Drug Info Ki = 0.3 nM [48]
3-(3,4-dichlorophenyl)-2-nortropene Drug Info Ki = 0.3 nM [48]
3-(3-aminocyclopentyl)-1H-indole-5-carbonitrile Drug Info IC50 = 32 nM [55]
3-(4-Trifluoromethylphenyl)-2-nortropene Drug Info Ki = 1.8 nM [48]
3-(4-Trifluoromethylphenyl)-2-nortropene Drug Info Ki = 1.8 nM [48]
3-(piperidin-4-yl)-2-(o-tolyloxy)pyridine Drug Info Ki = 292 nM [50]
3-alpha-Phenylmethoxy-3-beta-phenyl-nortropane Drug Info Ki = 247 nM [48]
3-alpha-Phenylmethoxy-3-beta-phenyl-nortropane Drug Info Ki = 247 nM [48]
3-Bromo-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 12.62 nM [2]
3-Bromo-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 12.62 nM [2]
3-p-Tolyl-8-aza-bicyclo[3.2.1]octane Drug Info Ki = 46 nM [3]
3-p-Tolyl-8-aza-bicyclo[3.2.1]octane Drug Info Ki = 46 nM [3]
3-Phenyl-2-nortropene Drug Info Ki = 176 nM [48]
3-Phenyl-2-nortropene Drug Info Ki = 176 nM [48]
3alpha-(bis-chloro-phenylmethoxy)tropane Drug Info Ki = 1640 nM [16]
3alpha-(bis-chloro-phenylmethoxy)tropane Drug Info Ki = 1640 nM [16]
4-((naphthalen-2-yloxy)methyl)piperidine Drug Info IC50 = 8 nM [40]
4-(1H-indol-3-yl)-N,N-dimethylcyclohex-3-enamine Drug Info IC50 = 3.1 nM [18]
4-(2-((3-fluorophenoxy)methyl)phenyl)piperidine Drug Info Ki = 49 nM [47]
4-(2-((dimethylamino)methyl)phenoxy)benzonitrile Drug Info IC50 = 60 nM [30]
4-(2-(2-fluoro-5-methylphenoxy)phenyl)piperidine Drug Info Ki = 26 nM [47]
4-(2-(2-fluorobenzyloxy)phenyl)piperidine Drug Info Ki = 56 nM [47]
4-(2-(3-chlorophenoxy)phenyl)piperidine Drug Info Ki = 211 nM [47]
4-(2-(3-fluorophenoxy)-4-methylphenyl)piperidine Drug Info Ki = 2 nM [47]
4-(2-(3-fluorophenoxy)phenyl)piperidine Drug Info Ki = 901 nM [47]
4-(2-(4-fluorobenzyloxy)phenyl)piperidine Drug Info Ki = 274 nM [47]
4-(2-(4-fluorophenoxy)-4-methylphenyl)piperidine Drug Info Ki = 427 nM [47]
4-(2-(4-fluorophenoxy)phenyl)piperidine Drug Info Ki = 319 nM [47]
4-(2-(benzyloxy)-3-fluorophenyl)piperidine Drug Info Ki = 2970 nM [47]
4-(2-(benzyloxy)-6-fluorophenyl)piperidine Drug Info Ki = 28 nM [47]
4-(2-(benzyloxy)phenyl)piperidine Drug Info Ki = 74 nM [47]
4-(2-fluoro-6-(3-fluorophenoxy)phenyl)piperidine Drug Info Ki = 1040 nM [47]
4-(2-fluoro-6-(4-fluorophenoxy)phenyl)piperidine Drug Info Ki = 157 nM [47]
4-(2-fluoro-6-phenoxyphenyl)piperidine Drug Info Ki = 706 nM [47]
4-(2-phenoxyphenyl)piperidine Drug Info Ki = 1760 nM [47]
4-(3-fluoro-2-phenoxyphenyl)piperidine Drug Info Ki = 2330 nM [47]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [54]
4-Allyl-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 1.67 nM [4]
4-Allyl-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 1.67 nM [4]
4-Benzyl-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 126.86 nM [4]
4-Benzyl-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 126.86 nM [4]
4-Bromo-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 0.37 nM [4]
4-Bromo-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 0.37 nM [4]
4-Furan-2-yl-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 5.23 nM [4]
4-Furan-2-yl-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 5.23 nM [4]
4-Iodo-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 1.73 nM [4]
4-Iodo-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 1.73 nM [4]
6,6-dimethyl-1-phenyl-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 1800 nM [28]
6,6-dimethyl-1-phenyl-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 1800 nM [28]
6,8-Dinitro-2-piperazin-1-yl-quinoline Drug Info Ki = 312.85 nM [2]
6,8-Dinitro-2-piperazin-1-yl-quinoline Drug Info Ki = 312.85 nM [2]
6-(3-aza-bicyclo[3.1.0]hexan-1-yl)quinoline Drug Info IC50 = 640 nM [28]
6-(3-aza-bicyclo[3.1.0]hexan-1-yl)quinoline Drug Info IC50 = 640 nM [28]
6-(piperidin-4-ylmethoxy)-2-naphthonitrile Drug Info IC50 = 15 nM [40]
6-Bromo-2-piperazin-1-yl-quinoline Drug Info Ki = 0.91 nM [2]
6-Bromo-2-piperazin-1-yl-quinoline Drug Info Ki = 0.91 nM [2]
6-Chloro-2-piperazin-1-yl-quinoline Drug Info Ki = 1.68 nM [2]
6-Chloro-2-piperazin-1-yl-quinoline Drug Info Ki = 1.68 nM [2]
6-Iodo-2-piperazin-1-yl-quinoline Drug Info Ki = 6.6 nM [2]
6-Iodo-2-piperazin-1-yl-quinoline Drug Info Ki = 6.6 nM [2]
6-nitroquipazine Drug Info Ki = 0.24 nM [17]
6-nitroquipazine Drug Info Ki = 0.24 nM [17]
7-(piperidin-4-ylmethoxy)-2-naphthonitrile Drug Info IC50 = 3 nM [40]
8-Methyl-3-p-tolyl-8-aza-bicyclo[3.2.1]octane Drug Info Ki = 390 nM [3]
8-Methyl-3-p-tolyl-8-aza-bicyclo[3.2.1]octane Drug Info Ki = 390 nM [3]
8R-hydroxylobel-9-ene Drug Info Ki = 860 nM [51]
8R-hydroxylobel-9-ene Drug Info Ki = 860 nM [51]
8S-hydroxylobelane Drug Info Ki = 2220 nM [15]
8S-hydroxylobelane Drug Info Ki = 2220 nM [15]
A-80426 Drug Info IC50 = 13.1 nM [60]
A-80426 Drug Info IC50 = 13.1 nM [60]
Beta-methoxyamphetamine Drug Info IC50 = 173 nM [43]
Beta-methoxyamphetamine Drug Info IC50 = 173 nM [43]
Biphenyl-2-ylmethyl-(S)-pyrrolidin-3-yl-amine Drug Info Ki = 1070 nM [31]
COCAINE.HCL Drug Info Ki = 306 nM [20]
COCAINE.HCL Drug Info Ki = 306 nM [20]
Cyclohexyl-(3,4-dichloro-phenyl)-acetonitrile Drug Info IC50 = 8000 nM [5]
Cyclohexyl-(3,4-dichloro-phenyl)-acetonitrile Drug Info IC50 = 8000 nM [5]
Cyclopentyl-(3,4-dichloro-phenyl)-acetonitrile Drug Info IC50 = 10000 nM [5]
Cyclopentyl-(3,4-dichloro-phenyl)-acetonitrile Drug Info IC50 = 10000 nM [5]
D-211A Drug Info Ki = 11884 nM [27]
D-211A Drug Info Ki = 11884 nM [27]
D-211B Drug Info Ki = 1484 nM [27]
D-211B Drug Info Ki = 1484 nM [27]
D-254C Drug Info Ki = 1391 nM [27]
D-254C Drug Info Ki = 1391 nM [27]
D-257A Drug Info Ki = 12904 nM [27]
D-257A Drug Info Ki = 12904 nM [27]
D-257C Drug Info Ki = 7414 nM [27]
D-257C Drug Info Ki = 7414 nM [27]
Erythro-3,4-dichloromethylphenidate hydrochloride Drug Info Ki = 2570 nM [20]
Erythro-3,4-dichloromethylphenidate hydrochloride Drug Info Ki = 2570 nM [20]
Isobutyl-(4-methyl-benzyl)-piperidin-4-yl-amine Drug Info Ki = 0.99 nM [12]
JNJ-28583867 Drug Info Ki = 3.7 nM [24]
KF-A5 Drug Info IC50 = 7800 nM [23]
KF-A6 Drug Info IC50 = 3500 nM [23]
LITOXETINE Drug Info IC50 = 5.9 nM [44]
MDL-28618 Drug Info IC50 = 190 nM [32]
METHYLENEDIOXYAMPHETAMINE Drug Info IC50 = 478 nM [43]
METHYLENEDIOXYAMPHETAMINE Drug Info IC50 = 478 nM [43]
METHYLENEDIOXYMETHAMPHETAMINE Drug Info IC50 = 1060 nM [43]
METHYLENEDIOXYMETHAMPHETAMINE Drug Info IC50 = 1060 nM [43]
N*1*-(6-Nitro-quinolin-2-yl)-ethane-1,2-diamine Drug Info Ki = 164.3 nM [2]
N*1*-(6-Nitro-quinolin-2-yl)-ethane-1,2-diamine Drug Info Ki = 164.3 nM [2]
N-(2-oxazolemethyl)milnacipran Drug Info IC50 = 1600 nM [25]
N-(piperidin-4-yl)-N-propyl-2-naphthamide Drug Info IC50 = 28.3 nM [44]
N-benzyl-N-isobutylpiperidin-4-amine Drug Info Ki = 8.4 nM [12]
NISOXETINE Drug Info Ki = 277 nM [37]
NISOXETINE Drug Info Ki = 277 nM [37]
O-DESMETHYL TRAMADOL Drug Info IC50 = 4600 nM [10]
Para-chloroamphetamine Drug Info IC50 = 182 nM [43]
Para-chloroamphetamine Drug Info IC50 = 182 nM [43]
PF-18298 Drug Info Ki = 6 nM [53]
PF-3409409 Drug Info Ki = 224 nM [41]
PYROVALERONE Drug Info IC50 = 2780 nM [11]
QUIPAZINE Drug Info Ki = 63 nM [2]
QUIPAZINE Drug Info Ki = 63 nM [2]
R-226161 Drug Info Ki = 1.2 nM [19]
Reboxetine Drug Info Ki = 661 nM [38]
S-34324 Drug Info Ki = 77 nM [9]
TEFLUDAZINE Drug Info IC50 = 7000 nM [57]
TEFLUDAZINE Drug Info IC50 = 7000 nM [57]
Threo-1-aza-5-phenyl[4.4.0]decane hydrochloride Drug Info Ki = 5140 nM [20]
Threo-1-aza-5-phenyl[4.4.0]decane hydrochloride Drug Info Ki = 5140 nM [20]
Threo-3,4-dichlororitalinol hydrochloride Drug Info Ki = 276 nM [20]
Threo-3,4-dichlororitalinol hydrochloride Drug Info Ki = 276 nM [20]
WIN-35065 Drug Info Ki = 1900 nM [21]
WIN-35065 Drug Info Ki = 1900 nM [21]
WIN-35066-2 Drug Info Ki = 178 nM [8]
ZIMELIDINE Drug Info IC50 = 4500 nM [58]
ZIMELIDINE Drug Info IC50 = 4500 nM [58]
[3-(3,4-Dichloro-phenyl)-indan-1-yl]-methyl-amine Drug Info Ki = 3 nM [6]
[3-(3,4-Dichloro-phenyl)-indan-1-yl]-methyl-amine Drug Info Ki = 3 nM [6]
[3H]WIN35428 Drug Info IC50 = 5060 nM [59]
[3H]WIN35428 Drug Info IC50 = 5060 nM [59]
Action against Disease Model Drug Info EMD 68843 (vilazodone) is a novel compound with combined high affinity and selectivity for the 5-hydroxytryptamine (5-HT) transporter and 5-HT(1A) receptors. In Sf9 cells, EMD 68843 increased guanosine 5'-O-(3-[(35)S]thiotriphosphate) binding to 69% of the magnitude of the full 5-HT(1A) receptor agonist R-(1)-trans-8-hydroxy-2-[N-n-propyl-N-(39-iodo-29-propenyl)] aminotetralin (8-OH-PIPAT), indicating that it is a partial agonist at 5-HT(1A) receptors. Acute, systemic administration of EMD 68843 produced a larger maximal increase of extracellular 5-HT than the SSRI fluoxetine in both the ventral hippocampus (HPv) (558 versus 274%) and the frontal cortex (FC) (527 versus 165%). Regional differences in the response to the two drugs were also observed. These effects maybe attributed to the differential regulation of 5-HT release in the HPv and FC by 5-HT(1A) autoreceptors. When challenged with the 5-HT(1A) receptor agonist 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT), EMD 68843-induced increases in extracellular 5-HT were greatly reduced in the HPv but to a lesser extent in the FC. In behavioral studies, EMD 68843 produced antidepressant-like effects in the forced swimming test in both rats and mice but only within a narrow dosage range. Like fluoxetine, [66]
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