Target Validation Information
TTD ID T55959
Target Name Dopamine transporter (DAT)
Type of Target
Successful
Drug Potency against Target Methylphenidate Drug Info Ki = 17 nM [53]
RTI-336 Drug Info IC50 = 4.09 nM [54]
Vanoxerine Drug Info IC50 = 0.8 nM [55]
Drug Info IC50 = 380 nM [20]
Drug Info IC50 = 23 nM [49]
Drug Info IC50 = 97.1 nM [46]
Drug Info IC50 = 2340 nM [46]
Drug Info IC50 = 4.2 nM [46]
Drug Info IC50 = 448 nM [46]
(+/-)-3-((naphthalen-2-yloxy)methyl)pyrrolidine Drug Info IC50 = 1000 nM [29]
(+/-)-threo-3',4'-Dichloromethylphenidate amide Drug Info IC50 = 16.4 nM [46]
(+/-)-threo-3',4'-Dichlororitalinol methyl ether Drug Info IC50 = 1.7 nM [46]
(+/-)-threo-3',5'-Dichloromethylphenidate Drug Info IC50 = 65.6 nM [46]
(+/-)-threo-3',5'-Dimethylmethylphenidate Drug Info IC50 = 4690 nM [46]
(+/-)-threo-3-Fluororitalinol Drug Info IC50 = 281 nM [46]
(+/-)-threo-4'-Ethylmethylphenidate Drug Info IC50 = 737 nM [46]
(+/-)-threo-Benzylphenidate Drug Info IC50 = 1020 nM [46]
(+/-)-threo-Methylphenidate amide Drug Info IC50 = 1730 nM [46]
(+/-)-threo-N-(2-Chlorobenzyl)methylphenidate Drug Info IC50 = 243 nM [46]
(+/-)-threo-N-(2-Methylfuran)methylphenidate Drug Info IC50 = 536 nM [46]
(+/-)-threo-N-(2-Methylpyridine)methylphenidate Drug Info IC50 = 369 nM [46]
(+/-)-threo-N-(2-Methylthiopene)methylphenidate Drug Info IC50 = 224 nM [46]
(+/-)-threo-N-(2-Phenylethyl)methylphenidate Drug Info IC50 = 678 nM [46]
(+/-)-threo-N-(2-Phenylethyl)ritalinol Drug Info IC50 = 1430 nM [46]
(+/-)-threo-N-(3-Chlorobenzyl)methylphenidate Drug Info IC50 = 106 nM [46]
(+/-)-threo-N-(3-Methylfuran)methylphenidate Drug Info IC50 = 459 nM [46]
(+/-)-threo-N-(3-Methylpyridine)methylphenidate Drug Info IC50 = 173 nM [46]
(+/-)-threo-N-(3-Methylthiopene)methylphenidate Drug Info IC50 = 143 nM [46]
(+/-)-threo-N-(3-Phenylpropyl)methylphenidate Drug Info IC50 = 267 nM [46]
(+/-)-threo-N-(3-Phenylpropyl)ritalinol Drug Info IC50 = 194 nM [46]
(+/-)-threo-N-(4-Chlorobenzyl)methylphenidate Drug Info IC50 = 31.2 nM [46]
(+/-)-threo-N-(4-Methoxybenzyl)methylphenidate Drug Info IC50 = 79.1 nM [46]
(+/-)-threo-N-(4-Methylpyridine)methylphenidate Drug Info IC50 = 128 nM [46]
(+/-)-threo-N-(4-Nitrobenzyl)methylphenidate Drug Info IC50 = 113 nM [46]
(+/-)-threo-N-(4-Phenylbutyl)methylphenidate Drug Info IC50 = 205 nM [46]
(+/-)-threo-N-(4-Phenylbutyl)ritalinol Drug Info IC50 = 623 nM [46]
(+/-)-threo-N-(5-Phenylpentyl)methylphenidate Drug Info IC50 = 1570 nM [46]
(+/-)-threo-N-(6-Phenylhexyl)methylphenidate Drug Info IC50 = 656 nM [46]
(+/-)-threo-N-Allylmethylphenidate Drug Info IC50 = 597 nM [46]
(+/-)-threo-N-Benzyl-3',4'-dichlororitalinol Drug Info IC50 = 2.74 nM [46]
(+/-)-threo-N-Benzyl-3'-chloromethylphenidate Drug Info IC50 = 41.2 nM [46]
(+/-)-threo-N-Benzylmethylphenidate amide Drug Info IC50 = 384 nM [46]
(+/-)-threo-N-Methyl-30-methylmethylphenidate Drug Info IC50 = 108 nM [46]
(+/-)-threo-N-Propargylmethylphenidate Drug Info IC50 = 821 nM [46]
(1-Phenyl-ethyl)-(2-phenyl-quinazolin-4-yl)-amine Drug Info Ki = 1800 nM [52]
(2R,3R)-iodoreboxetine Drug Info Ki = 716 nM [24]
(2R,3S)-2-[(2-Iodophenoxy)phenylmethyl]morpholine Drug Info Ki = 525.9 nM [32]
(2R,3S)-2-[(3-Iodophenoxy)phenylmethyl]morpholine Drug Info Ki = 1900 nM [32]
(2R,3S)-2-[(4-Iodophenoxy)phenylmethyl]morpholine Drug Info Ki = 2100 nM [32]
(2S,3S)-2-(m-Tolyl)-3,5,5-trimethylmorpholin-2-ol Drug Info IC50 = 2600 nM [44]
(2S,3S)-2-Phenyl-3,5,5-trimethylmorpholin-2-ol Drug Info IC50 = 1065 nM [44]
(2S,3S)-iodoreboxetine Drug Info Ki = 1457 nM [24]
(cis)-1,6-diphenyl-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 8700 nM [20]
(R)-2-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol Drug Info Ki = 2070 nM [43]
(R)-3-(naphthalen-2-ylmethoxy)pyrrolidine Drug Info IC50 = 3800 nM [29]
(R)-DULOXETINE Drug Info IC50 = 660 nM [27]
(R)-N-isobutyl-N-(pyrrolidin-3-yl)-2-naphthamide Drug Info IC50 = 9500 nM [34]
(R)-Norfluoxetine Drug Info IC50 = 7133 nM [26]
(RS/SR)-2-[1-(3,4-dichlorophenyl)butyl]piperidine Drug Info Ki = 43 nM [13]
(RS/SR)-2-[1-(4-chlorophenyl)butyl]piperidine Drug Info IC50 = 450 nM [13]
(RS/SR)-2-[1-(4-chlorophenyl)ethyl]piperidine Drug Info IC50 = 1500 nM [13]
(RS/SR)-2-[1-(4-chlorophenyl)hexyl]piperidine Drug Info IC50 = 650 nM [13]
(RS/SR)-2-[1-(4-chlorophenyl)pentyl]piperidine Drug Info IC50 = 170 nM [13]
(RS/SR)-2-[1-(4-chlorophenyl)propyl]piperidine Drug Info IC50 = 2800 nM [13]
(S)-3-(naphthalen-2-ylmethoxy)pyrrolidine Drug Info IC50 = 15000 nM [29]
(S)-Norfluoxetine Drug Info IC50 = 6488 nM [26]
1-(1,4-diphenylbutan-2-yl)piperazine Drug Info IC50 = 400 nM [8]
1-(1-(4-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info Ki = 2620 nM [43]
1-(1-(benzo[b]thiophen-2-yl)cyclohexyl)piperidine Drug Info IC50 = 12 nM [22]
1-(1-Benzo[b]thiophen-2-yl-cycloheptyl)-azepane Drug Info IC50 = 67 nM [48]
1-(1-Benzo[b]thiophen-2-yl-cyclohexyl)-azepane Drug Info IC50 = 18 nM [48]
1-(1-Benzo[b]thiophen-2-yl-cyclopentyl)-azepane Drug Info IC50 = 21 nM [48]
1-(1-phenyl-2-(2-propoxyphenyl)ethyl)piperazine Drug Info Ki = 1950 nM [43]
1-(2,3-Dihydro-1H-indol-5-ylmethyl)-propylamine Drug Info IC50 = 10000 nM [47]
1-(2-(2-(DIFLUOROMETHOXY)PHENYL)-1-PHENYLETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info Ki = 3160 nM [43]
1-(2-(2-chlorophenyl)-1-phenylethyl)piperazine Drug Info IC50 = 1300 nM [7]
1-(2-(2-methoxyphenyl)-1-phenylethyl)piperazine Drug Info IC50 = 11000 nM [7]
1-(2-(4-fluorophenoxy)phenyl)piperazine Drug Info Ki = 4420 nM [37]
1-(2-(phenoxymethyl)phenyl)piperazine Drug Info Ki = 701 nM [37]
1-(2-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 63 nM [6]
1-(2-phenoxyphenyl)piperazine Drug Info Ki = 4730 nM [37]
1-(3,4-Dichloro-phenyl)-3-diethylamino-indan-5-ol Drug Info Ki = 40 nM [4]
1-(3,4-Dichloro-phenyl)-3-methylamino-indan-5-ol Drug Info Ki = 11 nM [4]
1-(3-bromophenyl)-2-(tert-butylamino)propan-1-one Drug Info IC50 = 511 nM [41]
1-(3-chlorophenyl)-2-(dimethylamino)propan-1-one Drug Info IC50 = 1750 nM [41]
1-(3-chlorophenyl)-2-(piperidin-1-yl)propan-1-one Drug Info IC50 = 852 nM [41]
1-(3-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 52 nM [6]
1-(3-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 62.9 nM [6]
1-(4-aminophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 7 nM [30]
1-(4-bromophenyl)-2-(tert-butylamino)propan-1-one Drug Info IC50 = 689 nM [41]
1-(4-bromophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 39.5 nM [6]
1-(4-fluorophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 185 nM [6]
1-(4-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 32 nM [6]
1-(4-nitrophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 1110 nM [6]
1-(benzofuran-2-yl)-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 330 nM [20]
1-(naphthalen-2-yl)-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 190 nM [20]
1-(thiophen-2-yl)-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 7500 nM [20]
1-Benzo[b]thiophen-2-yl-cycloheptylamine Drug Info IC50 = 416 nM [48]
1-Benzo[b]thiophen-2-yl-cyclohexylamine Drug Info IC50 = 123 nM [48]
1-Benzo[b]thiophen-2-yl-cyclopentylamine Drug Info IC50 = 630 nM [48]
1-benzylpiperidine hydrochloride Drug Info IC50 = 1060 nM [16]
1-Biphenyl-4-yl-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 2300 nM [20]
1-naphthalen-2-yl-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 40 nM [6]
1-phenyl-1-(piperidin-2-yl)propan-2-one Drug Info IC50 = 190 nM [13]
1-phenyl-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 2700 nM [20]
10R-hydroxylobel-7-ene Drug Info Ki = 290 nM [10]
10R-hydroxylobelane Drug Info Ki = 570 nM [10]
10S-hydroxylobel-7-ene Drug Info Ki = 110 nM [10]
10S-hydroxylobelane Drug Info Ki = 1390 nM [10]
1S,2R-milnacipran Drug Info IC50 = 3200 nM [25]
2-((2-iodophenoxy)(phenyl)methyl)morpholine Drug Info Ki = 410 nM [12]
2-((3-iodophenyl)(o-tolyloxy)methyl)morpholine Drug Info Ki = 740 nM [12]
2-(2'-Aminoethyl)-5-benzyltetrahydrofuran Drug Info IC50 = 565 nM [28]
2-(2,3-Dihydro-1H-indol-5-yl)-1-methyl-ethylamine Drug Info IC50 = 3800 nM [47]
2-(2-chlorophenoxy)-3-(piperidin-4-yl)pyridine Drug Info Ki = 5150 nM [39]
2-(2-methoxyphenoxy)-3-(piperidin-4-yl)pyridine Drug Info Ki = 6410 nM [39]
2-(Aminomethyl)-5-(1'-naphthyl)tetrahydrofuran Drug Info IC50 = 463 nM [28]
2-(Aminomethyl)-5-(2'-naphthyl)tetrahydrofuran Drug Info IC50 = 28 nM [28]
2-(Aminomethyl)-5-phenethyltetrahydrofuran Drug Info IC50 = 513 nM [28]
2-(N,N-Diethylamino)-3'-chloropropiophenone Drug Info IC50 = 1744 nM [36]
2-(N-Cyclopentylamino)-3'-bromopropiophenone Drug Info IC50 = 845 nM [41]
2-(N-Cyclopentylamino)-3'-chloropropiophenone Drug Info IC50 = 980 nM [36]
2-(N-Cyclopentylamino)-3'-fluoropropiophenone Drug Info IC50 = 693 nM [41]
2-(N-Cyclopentylamino)-3'-methoxypropiophenone Drug Info IC50 = 2270 nM [41]
2-(N-Cyclopentylamino)-3'-methylpropiophenone Drug Info IC50 = 842 nM [41]
2-(N-Cyclopropylamino)-3-chloropropiophenone Drug Info IC50 = 265 nM [36]
2-(N-Isopropylamino)-3'-chloropropiophenone Drug Info Ki = 3980 nM [36]
2-(N-Pyrrolidinyl)-3'-bromopropiophenone Drug Info IC50 = 750 nM [41]
2-(N-Pyrrolidinyl)-3'-fluoropropiophenone Drug Info IC50 = 156 nM [41]
2-(N-Pyrrolidinyl)-3'-methoxypropiophenone Drug Info IC50 = 452 nM [41]
2-(N-Pyrrolidinyl)-3'-methylpropiophenone Drug Info IC50 = 414 nM [41]
2-(N-Pyrrolidinyl)-3'-nitropropiophenone Drug Info IC50 = 10000 nM [41]
2-(N-tert-Butylamino)-3',4'-dichloropropiophenone Drug Info IC50 = 271 nM [36]
2-(N-tert-Butylamino)-3'-chloroheptanophenone Drug Info Ki = 709 nM [36]
2-(N-tert-Butylamino)-3'-chlorohexanophenone Drug Info IC50 = 69 nM [36]
2-(N-tert-Butylamino)-3'-chlorooctanophenone Drug Info IC50 = 135 nM [36]
2-(N-tert-Butylamino)-3'-chloropentanophenone Drug Info IC50 = 33 nM [36]
2-(N-tert-Butylamino)-4'-chloropropiophenone Drug Info Ki = 2195 nM [36]
2-(N-tert-Butylamino)propiophenone Drug Info Ki = 5730 nM [36]
2-(tert-butylamino)-1-(3-chlorophenyl)butan-1-one Drug Info IC50 = 209 nM [41]
2-(tert-butylamino)-1-m-tolylpropan-1-one Drug Info IC50 = 1470 nM [41]
2-(tert-butylamino)-1-p-tolylpropan-1-one Drug Info IC50 = 1950 nM [41]
2-(tert-Butylamino)-3',4'-dichlorobutyrophenone Drug Info IC50 = 175 nM [36]
2-(tert-Butylamino)-3',4'-dichloropentanophenone Drug Info Ki = 43.7 nM [36]
2-(tert-Butylamino)-3',5'-difluoropropiophenone Drug Info IC50 = 5600 nM [36]
2-(tert-Butylamino)-3'-fluoropropiophenone Drug Info Ki = 4510 nM [36]
2-Amino-1-(4-methylthiophenyl)propane Drug Info IC50 = 3073 nM [33]
2-Aminomethyl-5-(p-bromophenyl)tetrahydrofuran Drug Info IC50 = 167 nM [28]
2-Aminomethyl-5-(p-chlorophenyl)tetrahydrofuran Drug Info IC50 = 313 nM [28]
2-Aminomethyl-5-(p-methoxyphenyl)tetrahydrofuran Drug Info IC50 = 668 nM [28]
2-Aminomethyl-5-(p-t-butylphenyl)tetrahydrofuran Drug Info IC50 = 4301 nM [28]
2-Aminomethyl-5-(phenyl)tetrahydrofuran Drug Info IC50 = 147 nM [28]
2-phenoxy-3-(piperidin-4-yl)pyridine Drug Info Ki = 4310 nM [39]
2-phenylpiperidine hydrochloride Drug Info IC50 = 8800 nM [16]
2pyrrolidin-1-yl-1-phenylpentan-1-one Drug Info IC50 = 52.3 nM [6]
3-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol Drug Info IC50 = 1400 nM [7]
3-(3,4-dichlorophenyl)-2-nortropene Drug Info Ki = 16 nM [38]
3-(4-Chlorophenyl)-2-nortropene Drug Info Ki = 231 nM [38]
3-(4-Fluorophenyl)-2-nortropene Drug Info Ki = 1056 nM [38]
3-(4-Trifluoromethylphenyl)-2-nortropene Drug Info Ki = 1494 nM [38]
3-alpha-Phenylmethoxy-3-beta-phenyl-nortropane Drug Info Ki = 117 nM [38]
3-p-Tolyl-8-aza-bicyclo[3.2.1]octane Drug Info IC50 = 33.6 nM [2]
3-Phenyl-2-nortropene Drug Info Ki = 1222 nM [38]
3alpha-(bis-chloro-phenylmethoxy)tropane Drug Info IC50 = 23.4 nM [11]
4-(2-((3-fluorophenoxy)methyl)phenyl)piperidine Drug Info Ki = 461 nM [37]
4-(2-(2-fluoro-5-methylphenoxy)phenyl)piperidine Drug Info Ki = 1080 nM [37]
4-(2-(2-fluorobenzyloxy)phenyl)piperidine Drug Info Ki = 1810 nM [37]
4-(2-(3-chlorophenoxy)phenyl)piperidine Drug Info Ki = 310 nM [37]
4-(2-(3-fluorophenoxy)-4-methylphenyl)piperidine Drug Info Ki = 1450 nM [37]
4-(2-(3-fluorophenoxy)phenyl)piperidine Drug Info Ki = 166 nM [37]
4-(2-(4-fluorobenzyloxy)phenyl)piperidine Drug Info Ki = 9120 nM [37]
4-(2-(4-fluorophenoxy)-4-methylphenyl)piperidine Drug Info Ki = 1680 nM [37]
4-(2-(4-fluorophenoxy)phenyl)piperidine Drug Info Ki = 13 nM [37]
4-(2-(benzyloxy)-3-fluorophenyl)piperidine Drug Info Ki = 7370 nM [37]
4-(2-(benzyloxy)-6-fluorophenyl)piperidine Drug Info Ki = 1030 nM [37]
4-(2-(benzyloxy)phenyl)piperidine Drug Info Ki = 1000 nM [37]
4-(2-(phenoxymethyl)phenyl)piperidine Drug Info Ki = 396 nM [37]
4-(2-fluoro-6-(2-fluorophenoxy)phenyl)piperidine Drug Info Ki = 278 nM [39]
4-(2-fluoro-6-(3-fluorophenoxy)phenyl)piperidine Drug Info Ki = 139 nM [37]
4-(2-fluoro-6-(4-fluorophenoxy)phenyl)piperidine Drug Info Ki = 6 nM [37]
4-(2-fluoro-6-phenoxyphenyl)piperidine Drug Info Ki = 45 nM [37]
4-(2-phenoxyphenyl)piperidine Drug Info Ki = 284 nM [37]
4-(2-pyrrolidin-1-yl-pentanoyl)benzonitrile Drug Info IC50 = 1000 nM [6]
4-(3-fluoro-2-phenoxyphenyl)piperidine Drug Info Ki = 239 nM [37]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [45]
4-[(diphenylmethyl)amino]-2-phenylquinazoline Drug Info Ki = 530 nM [52]
6-(3-aza-bicyclo[3.1.0]hexan-1-yl)quinoline Drug Info IC50 = 3900 nM [20]
6-(piperidin-4-ylmethoxy)-2-naphthonitrile Drug Info IC50 = 6000 nM [29]
7-(piperidin-4-ylmethoxy)-2-naphthonitrile Drug Info IC50 = 8800 nM [29]
8-Methyl-3-p-tolyl-8-aza-bicyclo[3.2.1]octane Drug Info IC50 = 10.2 nM [2]
8R-hydroxylobel-9-ene Drug Info Ki = 44 nM [40]
8R-hydroxylobelane Drug Info Ki = 1880 nM [10]
8S-hydroxylobel-9-ene Drug Info Ki = 960 nM [10]
8S-hydroxylobelane Drug Info Ki = 1260 nM [10]
AMINOBENZTROPINE Drug Info IC50 = 373 nM [50]
ANOLOBINE Drug Info IC50 = 8100 nM
ANONAINE Drug Info IC50 = 800 nM
ANTIOQUINE Drug Info IC50 = 3400 nM
Benzyl-(2-phenyl-quinazolin-4-yl)-amine Drug Info Ki = 7900 nM [52]
Bip-tyr(3bzl)-thr-pro-lys-thr Drug Info IC50 = 10000 nM [9]
Bip-tyr-ala-pro-lys-thr(obzl)-gly Drug Info IC50 = 11000 nM [9]
Bip-tyr-thr-ala-pro-phe Drug Info IC50 = 900 nM [9]
Bip-tyr-thr-pro-ala-thr(obzl)-gly Drug Info IC50 = 1700 nM [9]
Bip-tyr-thr-pro-lys-thr Drug Info IC50 = 19000 nM [9]
Bip-tyr-thr-pro-lys-thr(obzl)-gly Drug Info IC50 = 1800 nM [9]
Bip-tyr-thr-pro-thr(obzl)-gly Drug Info IC50 = 300 nM [9]
Biphenyl-2-ylmethyl-(S)-pyrrolidin-3-yl-amine Drug Info Ki = 2470 nM [23]
Cis-3-phenoxy-2,3-dihydro-1H-inden-1-amine Drug Info IC50 = 2000 nM [21]
COCAINE.HCL Drug Info IC50 = 404 nM [16]
COCLAURINE Drug Info IC50 = 14100 nM
D-166A Drug Info Ki = 82.9 nM [19]
D-211A Drug Info Ki = 41.8 nM [19]
D-211B Drug Info Ki = 8.63 nM [19]
D-254C Drug Info Ki = 10.6 nM [19]
D-257A Drug Info Ki = 204 nM [19]
D-257C Drug Info Ki = 66.5 nM [19]
Difluorobenztropine Drug Info Ki = 4.11 nM [11]
DIMETHYLGRISABINE Drug Info IC50 = 1100 nM
Erythro-3,4-dichloromethylphenidate hydrochloride Drug Info IC50 = 317 nM [16]
GB-12819 Drug Info Ki = 595 nM [3]
HOMOAROMOLINE Drug Info IC50 = 10900 nM
ISOPILINE Drug Info IC50 = 2500 nM
ISOTETRANDRINE Drug Info IC50 = 4200 nM
LITOXETINE Drug Info IC50 = 6700 nM [34]
Methyl 2-(naphthalen-2-yl)benzoate Drug Info Ki = 4060 nM [15]
METHYLENEDIOXYAMPHETAMINE Drug Info IC50 = 890 nM [42]
METHYLENEDIOXYMETHAMPHETAMINE Drug Info IC50 = 1442 nM [33]
N,Ndimethyl milnacipran Drug Info IC50 = 4500 nM [18]
N-Benzylmethylphenidate Drug Info IC50 = 52.9 nM [46]
NISOXETINE Drug Info IC50 = 2400 nM [21]
NORBOLDINE Drug Info IC50 = 16500 nM
NORSTEPHALAGINE Drug Info IC50 = 1400 nM
O-methyldauricine Drug Info IC50 = 5800 nM
OBABERINE Drug Info IC50 = 3900 nM
Para-chloroamphetamine Drug Info IC50 = 424 nM [33]
PF-18298 Drug Info Ki = 544 nM [43]
PF-3409409 Drug Info Ki = 2290 nM [31]
PF-526014 Drug Info Ki = 2650 nM [43]
PSEUDOCOCAINE Drug Info Ki = 13800 nM [1]
PYROVALERONE Drug Info IC50 = 32 nM [30]
R-226161 Drug Info Ki = 583 nM [14]
R-NORDULOXETINE Drug Info Ki = 3549 nM [35]
RTI-219 Drug Info IC50 = 5.7 nM [17]
SECOCULARIDINE Drug Info IC50 = 13400 nM
Threo-1-aza-5-phenyl[4.4.0]decane hydrochloride Drug Info IC50 = 244 nM [16]
Threo-3,4-dichlororitalinol hydrochloride Drug Info IC50 = 22.5 nM [16]
Threo-N-ethylritalinol hydrochloride Drug Info IC50 = 10400 nM [16]
Threo-ritalinol hydrochloride Drug Info IC50 = 1520 nM [16]
Threo-ritalinol methyl ether hydrochloride Drug Info IC50 = 281 nM [16]
Trans-3-(o-tolyloxy)-2,3-dihydro-1H-inden-1-amine Drug Info IC50 = 600 nM [21]
WIN-35065 Drug Info IC50 = 23 nM [17]
WIN-35066-2 Drug Info IC50 = 23 nM [5]
[3-(3,4-Dichloro-phenyl)-indan-1-yl]-methyl-amine Drug Info Ki = 2 nM [4]
[3H]WIN35428 Drug Info IC50 = 21 nM [49]
[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 IC50 = 616 nM [51]
References
REF 1 Synthesis of 8-Oxa analogues of norcocaine endowed with interesting cocaine-like activity. Bioorg Med Chem Lett. 1999 Jul 5;9(13):1831-6.
REF 2 3alpha-(4-Substituted phenyl)nortropane-2beta-carboxylic acid methyl esters show selective binding at the norepinephrine transporter. Bioorg Med Chem Lett. 2000 Nov 6;10(21):2445-7.
REF 3 Synthesis and dopamine transporter binding affinities of 3alpha-benzyl-8-(diarylmethoxyethyl)-8-azabicyclo[3.2.1]octanes. Bioorg Med Chem Lett. 2002 Sep 2;12(17):2387-90.
REF 4 Synthesis and pharmacological evaluation of 3-(3,4-dichlorophenyl)-1-indanamine derivatives as nonselective ligands for biogenic amine transporters. J Med Chem. 2004 May 6;47(10):2624-34.
REF 5 Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl e... J Med Chem. 2004 Dec 2;47(25):6401-9.
REF 6 1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors. J Med Chem. 2006 Feb 23;49(4):1420-32.
REF 7 N-(1,2-diphenylethyl)piperazines: a new class of dual serotonin/noradrenaline reuptake inhibitor. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4345-8.
REF 8 Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4349-53.
REF 9 Development of peptidic dopamine transporter inhibitors via aromatic modification-mediated conformational restriction. J Med Chem. 2006 Jul 13;49(14):4048-51.
REF 10 Des-keto lobeline analogs with increased potency and selectivity at dopamine and serotonin transporters. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5018-21.
REF 11 Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogue... J Med Chem. 2006 Oct 19;49(21):6391-9.
REF 12 Development of SPECT imaging agents for the norepinephrine transporters: [123I]INER. Bioorg Med Chem Lett. 2007 Jan 15;17(2):533-7.
REF 13 Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter. J Med Chem. 2007 Jan 25;50(2):219-32.
REF 14 Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-a... Bioorg Med Chem. 2007 Jun 1;15(11):3649-60.
REF 15 Synthesis, inhibition and binding of simple non-nitrogen inhibitors of monoamine transporters. Bioorg Med Chem. 2007 Jun 15;15(12):4159-74.
REF 16 Synthesis and pharmacology of site-specific cocaine abuse treatment agents: restricted rotation analogues of methylphenidate. J Med Chem. 2007 May 31;50(11):2718-31.
REF 17 Synthesis, monoamine transporter binding, properties, and functional monoamine uptake activity of 3beta-[4-methylphenyl and 4-chlorophenyl]-2 beta-... J Med Chem. 2007 Jul 26;50(15):3686-95.
REF 18 Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1346-9.
REF 19 Further structural optimization of cis-(6-benzhydryl-piperidin-3-yl)-benzylamine and 1,4-diazabicyclo[3.3.1]nonane derivatives by introducing an ex... Bioorg Med Chem. 2008 Mar 15;16(6):2769-78.
REF 20 Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors. Bioorg Med Chem Lett. 2008 Jul 1;18(13):3682-6.
REF 21 Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI). Bioorg Med Chem Lett. 2008 Jul 15;18(14):4224-7.
REF 22 Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. J Med Chem. 2008 Jul 24;51(14):4150-69.
REF 23 Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modu... Bioorg Med Chem Lett. 2008 Aug 1;18(15):4355-9.
REF 24 New iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter. Bioorg Med Chem Lett. 2008 Sep 15;18(18):4940-3.
REF 25 Characterization of thien-2-yl 1S,2R-milnacipran analogues as potent norepinephrine/serotonin transporter inhibitors for the treatment of neuropath... J Med Chem. 2008 Nov 27;51(22):7265-72.
REF 26 Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression. Bioorg Med Chem. 2009 Jan 1;17(1):337-43.
REF 27 1-Naphthyl and 4-indolyl arylalkylamines as selective monoamine reuptake inhibitors. Bioorg Med Chem Lett. 2009 Jan 1;19(1):58-61.
REF 28 2,5-Disubstituted tetrahydrofurans as selective serotonin re-uptake inhibitors. Bioorg Med Chem. 2009 Mar 1;17(5):2047-68.
REF 29 Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2329-32.
REF 30 A novel photoaffinity ligand for the dopamine transporter based on pyrovalerone. Bioorg Med Chem. 2009 Jun 1;17(11):3770-4.
REF 31 Design, synthesis and evaluation of N-[(3S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more po... Bioorg Med Chem Lett. 2009 Aug 15;19(16):4579-83.
REF 32 Design and synthesis of (2R,3S)-iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter. Bioorg Med Chem Lett. 2009 Sep 1;19(17):4996-8.
REF 33 Synthesis and serotonin transporter activity of sulphur-substituted alpha-alkyl phenethylamines as a new class of anticancer agents. Eur J Med Chem. 2009 Dec;44(12):4862-88.
REF 34 Bioorg Med Chem Lett. 2009 Oct 15;19(20):5893-7. Epub 2009 Aug 21.Design and optimisation of selective serotonin re-uptake inhibitors with high synthetic accessibility: part 2.
REF 35 Inhibition of serotonin and norepinephrine reuptake and inhibition of phosphodiesterase by multi-target inhibitors as potential agents for depression. Bioorg Med Chem. 2009 Oct 1;17(19):6890-7.
REF 36 Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction. J Med Chem. 2009 Nov 12;52(21):6768-81.
REF 37 Discovery and pharmacological characterization of aryl piperazine and piperidine ethers as dual acting norepinephrine reuptake inhibitors and 5-HT1... Bioorg Med Chem Lett. 2009 Dec 1;19(23):6604-7.
REF 38 Synthesis and monoamine transporter affinity of 3alpha-arylmethoxy-3beta-arylnortropanes. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6865-8.
REF 39 Design, synthesis, and pharmacological evaluation of phenoxy pyridyl derivatives as dual norepinephrine reuptake inhibitors and 5-HT1A partial agon... Bioorg Med Chem Lett. 2010 Feb 1;20(3):1114-7.
REF 40 Lobeline esters as novel ligands for neuronal nicotinic acetylcholine receptors and neurotransmitter transporters. Bioorg Med Chem. 2010 Jan 15;18(2):640-9.
REF 41 Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for smoking cessation. J Med Chem. 2010 Mar 11;53(5):2204-14.
REF 42 Synthesis and in vitro toxicity of 4-MTA, its characteristic clandestine synthesis byproducts and related sulfur substituted alpha-alkylthioampheta... Bioorg Med Chem. 2010 Jun 1;18(11):4009-31.
REF 43 Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reduc... Bioorg Med Chem Lett. 2010 Jun 15;20(12):3788-92.
REF 44 Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation. J Med Chem. 2010 Jun 24;53(12):4731-48.
REF 45 Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
REF 46 Quantitative structure-activity relationship studies of threo-methylphenidate analogs. Bioorg Med Chem. 2010 Oct 15;18(20):7221-38.
REF 47 Selective monoamine oxidase inhibitors. 3. Cyclic compounds related to 4-aminophenethylamine. Preparation and neuron-selective action of some 5-(2-... J Med Chem. 1986 Aug;29(8):1406-12.
REF 48 Synthesis and biological evaluation of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine homologues at dopamine-uptake and phencyclidine- and sigma-bin... J Med Chem. 1993 Apr 30;36(9):1188-93.
REF 49 3 alpha-(4'-substituted phenyl)tropane-2 beta-carboxylic acid methyl esters: novel ligands with high affinity and selectivity at the dopamine trans... J Med Chem. 1996 Oct 11;39(21):4139-41.
REF 50 3'-Chloro-3 alpha-(diphenylmethoxy)tropane but not 4'-chloro-3 alpha-(diphenylmethoxy)tropane produces a cocaine-like behavioral profile. J Med Chem. 1997 Mar 14;40(6):851-7.
REF 51 A technetium-99m SPECT imaging agent which targets the dopamine transporter in primate brain. J Med Chem. 1997 Jun 6;40(12):1835-44.
REF 52 Identification of a novel partial inhibitor of dopamine transporter among 4-substituted 2-phenylquinazolines. Bioorg Med Chem Lett. 2002 Aug 19;12(16):2225-8.
REF 53 Therapeutic potential of monoamine transporter substrates. Curr Top Med Chem. 2006;6(17):1845-59.
REF 54 Effects of dopamine transporter selective 3-phenyltropane analogs on locomotor activity, drug discrimination, and cocaine self-administration after... Eur J Pharmacol. 2006 Dec 28;553(1-3):149-56.
REF 55 Vanoxerine, a new drug for terminating atrial fibrillation and flutter. J Cardiovasc Electrophysiol. 2010 Mar;21(3):311-9.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.