Proteins > Sodium-dependent dopamine transporter
Page last updated: 2024-08-07 16:58:55
Sodium-dependent dopamine transporter
A sodium-dependent dopamine transporter that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q01959]
Synonyms
DA transporter;
DAT;
Solute carrier family 6 member 3
Research
Bioassay Publications (169)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 12 (7.10) | 18.2507 |
2000's | 84 (49.70) | 29.6817 |
2010's | 68 (40.24) | 24.3611 |
2020's | 5 (2.96) | 2.80 |
Compounds (177)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
bupropion | Homo sapiens (human) | IC50 | 1.0848 | 13 | 12 |
bupropion | Homo sapiens (human) | Ki | 0.7111 | 3 | 2 |
3,4-methylenedioxyamphetamine | Homo sapiens (human) | IC50 | 2.6486 | 3 | 3 |
3,4-methylenedioxyamphetamine | Homo sapiens (human) | Ki | 2.4250 | 1 | 1 |
n-methyl-3,4-methylenedioxyamphetamine | Homo sapiens (human) | IC50 | 1.7609 | 3 | 3 |
n-methyl-3,4-methylenedioxyamphetamine | Homo sapiens (human) | Ki | 0.8970 | 1 | 1 |
4-nonylphenol | Homo sapiens (human) | IC50 | 1.6490 | 1 | 0 |
4-nonylphenol | Homo sapiens (human) | Ki | 1.3100 | 1 | 0 |
amiodarone | Homo sapiens (human) | IC50 | 2.5050 | 1 | 0 |
amiodarone | Homo sapiens (human) | Ki | 1.9900 | 1 | 0 |
amitriptyline | Homo sapiens (human) | IC50 | 12.5892 | 1 | 1 |
amitriptyline | Homo sapiens (human) | Ki | 6.2030 | 1 | 1 |
amlodipine | Homo sapiens (human) | IC50 | 5.5210 | 1 | 0 |
amlodipine | Homo sapiens (human) | Ki | 4.3870 | 1 | 0 |
astemizole | Homo sapiens (human) | IC50 | 0.9980 | 1 | 0 |
astemizole | Homo sapiens (human) | Ki | 0.7930 | 1 | 0 |
bisacodyl | Homo sapiens (human) | IC50 | 2.2080 | 1 | 0 |
bisacodyl | Homo sapiens (human) | Ki | 1.7550 | 1 | 0 |
bithionol | Homo sapiens (human) | IC50 | 2.1810 | 1 | 0 |
bithionol | Homo sapiens (human) | Ki | 1.7330 | 1 | 0 |
carvedilol | Homo sapiens (human) | IC50 | 0.8450 | 1 | 0 |
carvedilol | Homo sapiens (human) | Ki | 0.6710 | 1 | 0 |
celecoxib | Homo sapiens (human) | IC50 | 2.4310 | 1 | 0 |
celecoxib | Homo sapiens (human) | Ki | 1.9310 | 1 | 0 |
chlorpromazine | Homo sapiens (human) | IC50 | 2.6430 | 1 | 0 |
chlorpromazine | Homo sapiens (human) | Ki | 2.1000 | 1 | 0 |
citalopram | Homo sapiens (human) | Ki | 508.2700 | 2 | 2 |
clebopride | Homo sapiens (human) | Ki | 0.0104 | 1 | 1 |
clomipramine | Homo sapiens (human) | IC50 | 2.7615 | 2 | 1 |
clomipramine | Homo sapiens (human) | Ki | 2.1820 | 1 | 0 |
clotrimazole | Homo sapiens (human) | IC50 | 5.5810 | 1 | 0 |
clotrimazole | Homo sapiens (human) | Ki | 4.4340 | 1 | 0 |
desipramine | Homo sapiens (human) | IC50 | 41.6000 | 5 | 5 |
desipramine | Homo sapiens (human) | Ki | 0.7504 | 2 | 4 |
disulfiram | Homo sapiens (human) | IC50 | 4.6370 | 1 | 0 |
disulfiram | Homo sapiens (human) | Ki | 3.6840 | 1 | 0 |
p-chloroamphetamine | Homo sapiens (human) | IC50 | 0.4240 | 1 | 1 |
doxazosin | Homo sapiens (human) | IC50 | 0.1880 | 1 | 0 |
doxazosin | Homo sapiens (human) | Ki | 0.1490 | 1 | 0 |
ebastine | Homo sapiens (human) | IC50 | 0.0987 | 1 | 0 |
ebastine | Homo sapiens (human) | Ki | 0.0784 | 1 | 0 |
econazole | Homo sapiens (human) | IC50 | 0.8350 | 1 | 0 |
econazole | Homo sapiens (human) | Ki | 0.6630 | 1 | 0 |
fenofibrate | Homo sapiens (human) | IC50 | 8.6330 | 1 | 0 |
fenofibrate | Homo sapiens (human) | Ki | 6.8590 | 1 | 0 |
fluphenazine | Homo sapiens (human) | IC50 | 2.0530 | 1 | 0 |
fluphenazine | Homo sapiens (human) | Ki | 1.6310 | 1 | 0 |
fluoxetine | Homo sapiens (human) | IC50 | 11.7467 | 9 | 9 |
fluoxetine | Homo sapiens (human) | Ki | 4.5250 | 6 | 7 |
vanoxerine | Homo sapiens (human) | IC50 | 0.0424 | 9 | 9 |
vanoxerine | Homo sapiens (human) | Ki | 0.0069 | 7 | 7 |
gbr 12935 | Homo sapiens (human) | IC50 | 0.0180 | 1 | 1 |
gbr 12935 | Homo sapiens (human) | Ki | 0.0383 | 2 | 2 |
haloprogin | Homo sapiens (human) | IC50 | 1.9690 | 1 | 0 |
haloprogin | Homo sapiens (human) | Ki | 1.5650 | 1 | 0 |
imipramine | Homo sapiens (human) | IC50 | 25.6000 | 1 | 1 |
ketoconazole | Homo sapiens (human) | IC50 | 23.5170 | 1 | 0 |
ketoconazole | Homo sapiens (human) | Ki | 18.6850 | 1 | 0 |
labetalol | Homo sapiens (human) | IC50 | 1.6070 | 1 | 0 |
labetalol | Homo sapiens (human) | Ki | 1.2770 | 1 | 0 |
leflunomide | Homo sapiens (human) | IC50 | 2.8840 | 1 | 0 |
leflunomide | Homo sapiens (human) | Ki | 2.2910 | 1 | 0 |
loxapine | Homo sapiens (human) | Ki | 0.0049 | 1 | 1 |
maprotiline | Homo sapiens (human) | IC50 | 2.9100 | 1 | 0 |
maprotiline | Homo sapiens (human) | Ki | 2.3120 | 1 | 0 |
mazindol | Homo sapiens (human) | IC50 | 0.0275 | 6 | 6 |
mazindol | Homo sapiens (human) | Ki | 0.0379 | 7 | 7 |
methapyrilene | Homo sapiens (human) | IC50 | 2.7570 | 1 | 0 |
methapyrilene | Homo sapiens (human) | Ki | 2.1900 | 1 | 0 |
nocodazole | Homo sapiens (human) | IC50 | 6.2320 | 1 | 0 |
nocodazole | Homo sapiens (human) | Ki | 4.9460 | 1 | 0 |
methylphenidate | Homo sapiens (human) | IC50 | 0.0790 | 1 | 1 |
methylphenidate | Homo sapiens (human) | Ki | 0.0720 | 2 | 2 |
miconazole | Homo sapiens (human) | IC50 | 1.7010 | 1 | 0 |
miconazole | Homo sapiens (human) | Ki | 1.3520 | 1 | 0 |
mitotane | Homo sapiens (human) | IC50 | 1.0010 | 1 | 0 |
mitotane | Homo sapiens (human) | Ki | 0.7950 | 1 | 0 |
modafinil | Homo sapiens (human) | IC50 | 6.6660 | 2 | 1 |
modafinil | Homo sapiens (human) | Ki | 4.0946 | 5 | 4 |
nimesulide | Homo sapiens (human) | IC50 | 14.8840 | 1 | 0 |
nimesulide | Homo sapiens (human) | Ki | 11.8260 | 1 | 0 |
nisoxetine | Homo sapiens (human) | IC50 | 1.6500 | 5 | 5 |
nisoxetine | Homo sapiens (human) | Ki | 0.2725 | 2 | 4 |
nomifensine | Homo sapiens (human) | IC50 | 0.0781 | 5 | 5 |
nomifensine | Homo sapiens (human) | Ki | 0.0611 | 5 | 5 |
nortriptyline | Homo sapiens (human) | IC50 | 1.6780 | 1 | 0 |
nortriptyline | Homo sapiens (human) | Ki | 1.3330 | 1 | 0 |
oxybutynin | Homo sapiens (human) | IC50 | 0.0855 | 1 | 0 |
oxybutynin | Homo sapiens (human) | Ki | 0.0679 | 1 | 0 |
pemoline | Homo sapiens (human) | IC50 | 0.5213 | 1 | 0 |
pemoline | Homo sapiens (human) | Ki | 0.4142 | 1 | 0 |
pentamidine | Homo sapiens (human) | IC50 | 3.1590 | 1 | 0 |
pentamidine | Homo sapiens (human) | Ki | 2.5100 | 1 | 0 |
prochlorperazine | Homo sapiens (human) | IC50 | 1.7350 | 1 | 0 |
prochlorperazine | Homo sapiens (human) | Ki | 1.3790 | 1 | 0 |
propafenone | Homo sapiens (human) | IC50 | 1.8680 | 1 | 0 |
propafenone | Homo sapiens (human) | Ki | 1.4840 | 1 | 0 |
pyrilamine | Homo sapiens (human) | IC50 | 0.8790 | 1 | 0 |
pyrilamine | Homo sapiens (human) | Ki | 0.6990 | 1 | 0 |
raloxifene | Homo sapiens (human) | IC50 | 1.8690 | 1 | 0 |
raloxifene | Homo sapiens (human) | Ki | 1.4850 | 1 | 0 |
sibutramine | Homo sapiens (human) | IC50 | 0.6320 | 1 | 0 |
sibutramine | Homo sapiens (human) | Ki | 0.5020 | 1 | 0 |
spiperone | Homo sapiens (human) | Ki | 0.0013 | 1 | 1 |
sulconazole | Homo sapiens (human) | IC50 | 1.7260 | 1 | 0 |
sulconazole | Homo sapiens (human) | Ki | 1.3710 | 1 | 0 |
terfenadine | Homo sapiens (human) | IC50 | 0.2550 | 1 | 0 |
terfenadine | Homo sapiens (human) | Ki | 0.2030 | 1 | 0 |
thioridazine | Homo sapiens (human) | IC50 | 2.3760 | 1 | 0 |
thioridazine | Homo sapiens (human) | Ki | 1.8880 | 1 | 0 |
venlafaxine | Homo sapiens (human) | IC50 | 8.5145 | 6 | 6 |
venlafaxine | Homo sapiens (human) | Ki | 3.2700 | 3 | 3 |
n-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-n-(2-pyridinyl)cyclohexanecarboxamide | Homo sapiens (human) | Ki | 0.0003 | 1 | 3 |
lysergic acid diethylamide | Homo sapiens (human) | Ki | 0.3400 | 1 | 1 |
dextroamphetamine | Homo sapiens (human) | IC50 | 0.2884 | 1 | 1 |
dextroamphetamine | Homo sapiens (human) | Ki | 0.1090 | 1 | 1 |
ethinyl estradiol | Homo sapiens (human) | IC50 | 0.5590 | 1 | 0 |
ethinyl estradiol | Homo sapiens (human) | Ki | 0.4440 | 1 | 0 |
17-alpha-hydroxyprogesterone | Homo sapiens (human) | IC50 | 6.9050 | 1 | 0 |
17-alpha-hydroxyprogesterone | Homo sapiens (human) | Ki | 5.4860 | 1 | 0 |
bisphenol a | Homo sapiens (human) | IC50 | 19.0150 | 1 | 0 |
bisphenol a | Homo sapiens (human) | Ki | 15.1080 | 1 | 0 |
cyclizine | Homo sapiens (human) | IC50 | 0.7630 | 1 | 0 |
cyclizine | Homo sapiens (human) | Ki | 0.6060 | 1 | 0 |
phenothiazine | Homo sapiens (human) | IC50 | 18.6360 | 1 | 0 |
phenothiazine | Homo sapiens (human) | Ki | 14.8070 | 1 | 0 |
dibenzothiazyl disulfide | Homo sapiens (human) | IC50 | 0.2450 | 1 | 0 |
dibenzothiazyl disulfide | Homo sapiens (human) | Ki | 0.1940 | 1 | 0 |
benzethonium chloride | Homo sapiens (human) | IC50 | 1.3650 | 1 | 0 |
benzethonium chloride | Homo sapiens (human) | Ki | 1.0850 | 1 | 0 |
sterogenol | Homo sapiens (human) | IC50 | 6.2790 | 1 | 0 |
sterogenol | Homo sapiens (human) | Ki | 4.9890 | 1 | 0 |
indopan | Homo sapiens (human) | IC50 | 1.8621 | 1 | 1 |
indopan | Homo sapiens (human) | Ki | 5.3330 | 2 | 2 |
dimenhydrinate | Homo sapiens (human) | IC50 | 2.2450 | 1 | 0 |
dimenhydrinate | Homo sapiens (human) | Ki | 1.7840 | 1 | 0 |
gentian violet | Homo sapiens (human) | IC50 | 4.0690 | 1 | 0 |
gentian violet | Homo sapiens (human) | Ki | 3.2330 | 1 | 0 |
pyrovalerone | Homo sapiens (human) | IC50 | 0.0420 | 2 | 2 |
pyrovalerone | Homo sapiens (human) | Ki | 0.0147 | 2 | 2 |
4-octylphenol | Homo sapiens (human) | IC50 | 8.4910 | 1 | 0 |
4-octylphenol | Homo sapiens (human) | Ki | 6.7460 | 1 | 0 |
11-(4-methyl-1-piperazinyl)-5h-dibenzo(b,e)(1,4)diazepine | Homo sapiens (human) | Ki | 0.4200 | 1 | 2 |
2-chloro-11-(4-methyl-1-piperazinyl)-5h-dibenzo(b,e)(1,4)diazepine | Homo sapiens (human) | Ki | 0.0160 | 1 | 2 |
n-methyllaurotetanine | Homo sapiens (human) | Ki | 0.9500 | 1 | 1 |
clemastine | Homo sapiens (human) | IC50 | 0.6780 | 1 | 0 |
clemastine | Homo sapiens (human) | Ki | 0.5380 | 1 | 0 |
danazol | Homo sapiens (human) | IC50 | 6.8420 | 1 | 0 |
danazol | Homo sapiens (human) | Ki | 5.4360 | 1 | 0 |
metergoline | Homo sapiens (human) | IC50 | 0.0630 | 1 | 0 |
metergoline | Homo sapiens (human) | Ki | 0.0500 | 1 | 0 |
1-(3-chloro-5-benzo[b][1]benzoxepinyl)-4-methylpiperazine | Homo sapiens (human) | Ki | 0.0005 | 1 | 1 |
dexchlorpheniramine | Homo sapiens (human) | IC50 | 0.9310 | 1 | 0 |
dexchlorpheniramine | Homo sapiens (human) | Ki | 0.7390 | 1 | 0 |
penfluridol | Homo sapiens (human) | Ki | 1.7140 | 1 | 1 |
flazolone | Homo sapiens (human) | Ki | 5.7000 | 1 | 1 |
dobutamine | Homo sapiens (human) | IC50 | 0.1550 | 1 | 0 |
dobutamine | Homo sapiens (human) | Ki | 0.1230 | 1 | 0 |
closantel | Homo sapiens (human) | IC50 | 4.8000 | 1 | 0 |
closantel | Homo sapiens (human) | Ki | 3.8000 | 1 | 0 |
paroxetine | Homo sapiens (human) | IC50 | 0.6720 | 1 | 0 |
paroxetine | Homo sapiens (human) | Ki | 0.4670 | 2 | 1 |
bicifadine | Homo sapiens (human) | IC50 | 0.9100 | 1 | 1 |
lovastatin | Homo sapiens (human) | IC50 | 10.1040 | 1 | 0 |
lovastatin | Homo sapiens (human) | Ki | 8.0280 | 1 | 0 |
atomoxetine | Homo sapiens (human) | IC50 | 3.0429 | 7 | 7 |
(S)-nomifensine | Homo sapiens (human) | Ki | 0.0250 | 2 | 2 |
duloxetine | Homo sapiens (human) | IC50 | 0.8304 | 9 | 9 |
duloxetine | Homo sapiens (human) | Ki | 0.3563 | 9 | 9 |
fluoxetine hydrochloride | Homo sapiens (human) | IC50 | 18.4000 | 1 | 1 |
venlafaxine hydrochloride | Homo sapiens (human) | IC50 | 9.1250 | 2 | 2 |
trovafloxacin | Homo sapiens (human) | IC50 | 62.1910 | 1 | 0 |
trovafloxacin | Homo sapiens (human) | Ki | 49.4120 | 1 | 0 |
nelfinavir | Homo sapiens (human) | IC50 | 15.5250 | 1 | 0 |
nelfinavir | Homo sapiens (human) | Ki | 12.3350 | 1 | 0 |
dopamine hydrochloride | Homo sapiens (human) | IC50 | 46.0000 | 1 | 0 |
litoxetine | Homo sapiens (human) | IC50 | 4.0000 | 2 | 2 |
milnacipran | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
esreboxetine | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
esreboxetine | Homo sapiens (human) | Ki | 10.9763 | 2 | 2 |
sertraline | Homo sapiens (human) | IC50 | 0.2175 | 3 | 2 |
sertraline | Homo sapiens (human) | Ki | 0.0258 | 1 | 0 |
vanoxerine | Homo sapiens (human) | IC50 | 0.1485 | 4 | 3 |
vanoxerine | Homo sapiens (human) | Ki | 0.0024 | 1 | 1 |
(3h)2-carbomethoxy-3-(4-fluorophenyl)tropane | Homo sapiens (human) | Ki | 0.0242 | 2 | 2 |
cubebin | Homo sapiens (human) | IC50 | 12.0000 | 1 | 1 |
1-(1-(2-benzo(b)thienyl)cyclohexyl)piperidine | Homo sapiens (human) | IC50 | 0.0078 | 7 | 7 |
1-(1-(2-benzo(b)thienyl)cyclohexyl)piperidine | Homo sapiens (human) | Ki | 0.0050 | 4 | 4 |
desloratadine | Homo sapiens (human) | IC50 | 3.8790 | 1 | 0 |
desloratadine | Homo sapiens (human) | Ki | 3.0820 | 1 | 0 |
desvenlafaxine | Homo sapiens (human) | Ki | 0.8540 | 1 | 1 |
rti-coc 32 | Homo sapiens (human) | Ki | 0.0324 | 1 | 1 |
indatraline | Homo sapiens (human) | Ki | 0.0250 | 2 | 2 |
4-methylthioamphetamine | Homo sapiens (human) | IC50 | 3.0730 | 1 | 1 |
dexmethylphenidate | Homo sapiens (human) | IC50 | 0.1560 | 1 | 1 |
dexmethylphenidate | Homo sapiens (human) | Ki | 0.0205 | 2 | 2 |
nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
saquinavir | Homo sapiens (human) | IC50 | 35.0970 | 1 | 0 |
saquinavir | Homo sapiens (human) | Ki | 27.8850 | 1 | 0 |
hyperforin | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
terconazole | Homo sapiens (human) | IC50 | 5.4720 | 1 | 0 |
terconazole | Homo sapiens (human) | Ki | 4.3470 | 1 | 0 |
hinokinin | Homo sapiens (human) | IC50 | 8.3500 | 1 | 1 |
cocaine | Homo sapiens (human) | IC50 | 0.3796 | 34 | 34 |
cocaine | Homo sapiens (human) | Ki | 0.4281 | 30 | 33 |
diethylstilbestrol | Homo sapiens (human) | IC50 | 1.0710 | 1 | 0 |
diethylstilbestrol | Homo sapiens (human) | Ki | 0.8510 | 1 | 0 |
cocaine hydrochloride | Homo sapiens (human) | IC50 | 0.2594 | 3 | 2 |
cocaine hydrochloride | Homo sapiens (human) | Ki | 0.0463 | 1 | 1 |
(1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Homo sapiens (human) | IC50 | 2.5700 | 1 | 0 |
(1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Homo sapiens (human) | Ki | 2.0419 | 1 | 0 |
flunarizine | Homo sapiens (human) | IC50 | 0.5840 | 1 | 0 |
flunarizine | Homo sapiens (human) | Ki | 0.4640 | 1 | 0 |
benztropine | Homo sapiens (human) | IC50 | 0.2948 | 2 | 3 |
benztropine | Homo sapiens (human) | Ki | 0.1930 | 1 | 0 |
cinnarizine | Homo sapiens (human) | IC50 | 1.6410 | 1 | 0 |
cinnarizine | Homo sapiens (human) | Ki | 1.3040 | 1 | 0 |
enclomiphene | Homo sapiens (human) | IC50 | 0.7840 | 1 | 0 |
enclomiphene | Homo sapiens (human) | Ki | 0.6230 | 1 | 0 |
tamoxifen | Homo sapiens (human) | IC50 | 1.8410 | 1 | 0 |
tamoxifen | Homo sapiens (human) | Ki | 1.4620 | 1 | 0 |
2-[(2-ethoxyphenoxy)-phenylmethyl]morpholine | Homo sapiens (human) | IC50 | 25.0000 | 2 | 2 |
2-[(2-ethoxyphenoxy)-phenylmethyl]morpholine | Homo sapiens (human) | Ki | 5.0300 | 4 | 6 |
bp 897 | Homo sapiens (human) | Ki | 0.2100 | 1 | 1 |
vx-745 | Homo sapiens (human) | IC50 | 8.0980 | 1 | 0 |
vx-745 | Homo sapiens (human) | Ki | 6.4340 | 1 | 0 |
3-[bis(4-fluorophenyl)methoxy]-8-methyl-8-azabicyclo[3.2.1]octane | Homo sapiens (human) | Ki | 0.0138 | 1 | 1 |
bw 723c86 | Homo sapiens (human) | IC50 | 2.6846 | 1 | 0 |
bw 723c86 | Homo sapiens (human) | Ki | 2.1330 | 1 | 0 |
genistein | Homo sapiens (human) | IC50 | 16.9180 | 1 | 0 |
genistein | Homo sapiens (human) | Ki | 13.4420 | 1 | 0 |
montelukast | Homo sapiens (human) | IC50 | 2.6010 | 1 | 0 |
montelukast | Homo sapiens (human) | Ki | 2.0670 | 1 | 0 |
fluvoxamine | Homo sapiens (human) | Ki | 0.0015 | 1 | 3 |
oxiconazole | Homo sapiens (human) | IC50 | 2.6555 | 1 | 0 |
oxiconazole | Homo sapiens (human) | Ki | 2.1098 | 1 | 0 |
gw 1929 | Homo sapiens (human) | IC50 | 13.5510 | 1 | 0 |
gw 1929 | Homo sapiens (human) | Ki | 10.7670 | 1 | 0 |
levomilnacipran | Homo sapiens (human) | IC50 | 3.2000 | 2 | 2 |
vilazodone | Homo sapiens (human) | IC50 | 0.2950 | 1 | 1 |
nps2143 | Homo sapiens (human) | IC50 | 0.2000 | 1 | 1 |
armodafinil | Homo sapiens (human) | IC50 | 6.6000 | 1 | 1 |
armodafinil | Homo sapiens (human) | Ki | 0.6470 | 1 | 1 |
radafaxine | Homo sapiens (human) | IC50 | 50.1100 | 2 | 2 |
dov 216303 | Homo sapiens (human) | IC50 | 0.1363 | 5 | 6 |
dov 216303 | Homo sapiens (human) | Ki | 0.2510 | 1 | 1 |
[2-[[2-[(dimethylamino)methyl]phenyl]thio]-5-iodophenyl]methanol | Homo sapiens (human) | Ki | 5.5000 | 2 | 2 |
fauc 346 | Homo sapiens (human) | Ki | 0.0870 | 1 | 1 |
4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
LSM-1328 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
2-carbomethoxy-8-(3-fluoropropyl)-3-(4-iodophenyl)tropane | Homo sapiens (human) | Ki | 0.0282 | 1 | 1 |
n,n-dimethyl-2-(2-amino-4-methylphenylthio)benzylamine | Homo sapiens (human) | IC50 | 0.1000 | 1 | 1 |
n,n-dimethyl-2-(2-amino-4-methylphenylthio)benzylamine | Homo sapiens (human) | Ki | 3.8440 | 3 | 3 |
n,n-dimethyl-2-(2-amino-4-fluorophenylthio)benzylamine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
fauc 365 | Homo sapiens (human) | Ki | 3.6000 | 1 | 1 |
meridianin a | Homo sapiens (human) | Ki | 2.3500 | 1 | 1 |
3-amino-4-(2-dimethylaminomethylphenylsulfanyl)benzonitrile | Homo sapiens (human) | Ki | 4.1410 | 3 | 3 |
1-phenyl-2-(1-pyrrolidinyl)-1-pentanone | Homo sapiens (human) | IC50 | 0.0523 | 1 | 1 |
1-phenyl-2-(1-pyrrolidinyl)-1-pentanone | Homo sapiens (human) | Ki | 0.0337 | 1 | 1 |
naphyrone | Homo sapiens (human) | IC50 | 0.0400 | 1 | 1 |
naphyrone | Homo sapiens (human) | Ki | 0.0201 | 1 | 1 |
naluzotan | Homo sapiens (human) | Ki | 2.0000 | 1 | 1 |
mrk 560 | Homo sapiens (human) | Ki | 3.1454 | 2 | 0 |
milnacipran | Homo sapiens (human) | IC50 | 7.0750 | 4 | 4 |
milnacipran | Homo sapiens (human) | Ki | 16.2384 | 2 | 2 |
dov 21947 | Homo sapiens (human) | IC50 | 0.1276 | 2 | 2 |
dov 21947 | Homo sapiens (human) | Ki | 0.1027 | 2 | 2 |
lorcaserin | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
2-((2-((dimethylamino)methyl)phenyl)thio)-5-iodophenylamine | Homo sapiens (human) | Ki | 3.8933 | 3 | 3 |
ncq 298 | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
cep 26401 | Homo sapiens (human) | IC50 | 9.4000 | 1 | 1 |
cep 26401 | Homo sapiens (human) | Ki | 11.0000 | 1 | 1 |
(1R,3S)-3-(4-iodophenyl)-8-methyl-8-azabicyclo[3.2.1]octane-4-carboxylic acid methyl ester | Homo sapiens (human) | IC50 | 0.0012 | 2 | 4 |
win 35,065-2 | Homo sapiens (human) | IC50 | 0.0230 | 2 | 2 |
nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
mk-7246 | Homo sapiens (human) | IC50 | 8.6920 | 1 | 0 |
mk-7246 | Homo sapiens (human) | Ki | 0.3256 | 4 | 0 |
skepinone-l | Homo sapiens (human) | Ki | 10.0000 | 1 | 0 |
n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | IC50 | 32.3594 | 1 | 1 |
n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 10.0701 | 3 | 3 |
clozapine | Homo sapiens (human) | Ki | 0.0210 | 1 | 2 |
Drugs with Activation Measurements
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
mazindol | Homo sapiens (human) | Activity | 0.0221 | 1 | 1 |
atomoxetine | Homo sapiens (human) | IC5 | 0.0480 | 1 | 1 |
esreboxetine | Homo sapiens (human) | IC5 | 10.0000 | 1 | 1 |
Selective deuteration of bupropion slows epimerization and reduces metabolism.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 76, 2022
Design, synthesis and docking study of 4-arylpiperazine carboxamides as monoamine neurotransmitters reuptake inhibitors.Bioorganic & medicinal chemistry, , 08-07, Volume: 26, Issue:14, 2018
Design, synthesis and in vitro activity of 1,4-disubstituted piperazines and piperidines as triple reuptake inhibitors.Bioorganic & medicinal chemistry, , 04-01, Volume: 25, Issue:7, 2017
Triple reuptake inhibitors: Design, synthesis and structure-activity relationship of benzylpiperidine-tetrazoles.Bioorganic & medicinal chemistry, , 10-15, Volume: 25, Issue:20, 2017
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Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation.Journal of medicinal chemistry, , Jun-24, Volume: 53, Issue:12, 2010
A novel photoaffinity ligand for the dopamine transporter based on pyrovalerone.Bioorganic & medicinal chemistry, , Jun-01, Volume: 17, Issue:11, 2009
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[no title available],
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Synthesis and in vitro toxicity of 4-MTA, its characteristic clandestine synthesis byproducts and related sulfur substituted alpha-alkylthioamphetamines.Bioorganic & medicinal chemistry, , Jun-01, Volume: 18, Issue:11, 2010
Synthesis and serotonin transporter activity of sulphur-substituted alpha-alkyl phenethylamines as a new class of anticancer agents.European journal of medicinal chemistry, , Volume: 44, Issue:12, 2009
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Synthesis and serotonin transporter activity of sulphur-substituted alpha-alkyl phenethylamines as a new class of anticancer agents.European journal of medicinal chemistry, , Volume: 44, Issue:12, 2009
A rhodamine-labeled citalopram analogue as a high-affinity fluorescent probe for the serotonin transporter.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
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Pharmacotherapies for treatment of cocaine abuse: preclinical aspects.Journal of medicinal chemistry, , Jul-29, Volume: 42, Issue:15, 1999
Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
Exploration of 3-Aminoazetidines as Triple Reuptake Inhibitors by Bioisosteric Modification of 3-α-Oxyazetidine.ACS medicinal chemistry letters, , Sep-11, Volume: 5, Issue:9, 2014
An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Dual inhibitors of phosphodiesterase-4 and serotonin reuptake.Journal of medicinal chemistry, , Mar-26, Volume: 52, Issue:6, 2009
Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression.Bioorganic & medicinal chemistry, , Jan-01, Volume: 17, Issue:1, 2009
Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with a heterocyclic ring constraint.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 18, Issue:16, 2008
Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI).Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 18, Issue:14, 2008
N-(1,2-diphenylethyl)piperazines: a new class of dual serotonin/noradrenaline reuptake inhibitor.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
Conformationally restricted homotryptamines. 2. Indole cyclopropylmethylamines as selective serotonin reuptake inhibitors.Journal of medicinal chemistry, , Sep-22, Volume: 48, Issue:19, 2005
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
Synthesis of a potent wide-spectrum serotonin-, norepinephrine-, dopamine-reuptake inhibitor (SNDRI) and a species-selective dopamine-reuptake inhibitor based on the gamma-amino alcohol functional group.Bioorganic & medicinal chemistry letters, , Mar-03, Volume: 8, Issue:5, 1998
C-terminal modified Enkephalin-like tetrapeptides with enhanced affinities at the kappa opioid receptor and monoamine transporters.Bioorganic & medicinal chemistry, , 12-01, Volume: 51, 2021
Design, synthesis and in vitro activity of 1,4-disubstituted piperazines and piperidines as triple reuptake inhibitors.Bioorganic & medicinal chemistry, , 04-01, Volume: 25, Issue:7, 2017
Triple reuptake inhibitors: Design, synthesis and structure-activity relationship of benzylpiperidine-tetrazoles.Bioorganic & medicinal chemistry, , 10-15, Volume: 25, Issue:20, 2017
Discovery of imidazo[1,2-a]-, [1,2,4]triazolo[4,3-a]-, and [1,2,4]triazolo[1,5-a]pyridine-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 27, Issue:21, 2017
Development of Novel Alkoxyisoxazoles as Sigma-1 Receptor Antagonists with Antinociceptive Efficacy.Journal of medicinal chemistry, , 07-14, Volume: 59, Issue:13, 2016
Exploration of 3-Aminoazetidines as Triple Reuptake Inhibitors by Bioisosteric Modification of 3-α-Oxyazetidine.ACS medicinal chemistry letters, , Sep-11, Volume: 5, Issue:9, 2014
CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs.Bioorganic & medicinal chemistry, , Oct-01, Volume: 19, Issue:19, 2011
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: deBioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
Synthesis of 1,1-[1-naphthyloxy-2-thiophenyl]-2-methylaminomethylcyclopropanes and their evaluation as inhibitors of serotonin, norepinephrine, and dopamine transporters.Journal of medicinal chemistry, , Oct-08, Volume: 52, Issue:19, 2009
Design and synthesis of 2- and 3-substituted-3-phenylpropyl analogs of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine: role of amino, fluoro, hydroxyl, methoxyl, methyl, mJournal of medicinal chemistry, , May-08, Volume: 51, Issue:9, 2008
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
Piperidine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909): high affinity ligands for the dopamine transporter.Journal of medicinal chemistry, , Sep-12, Volume: 45, Issue:19, 2002
Synthesis, biodistribution, and primate imaging of fluorine-18 labeled 2beta-carbo-1'-fluoro-2-propoxy-3beta-(4-chlorophenyl)tr opanes. Ligands for the imaging of dopamine transporters by positron emission tomography.Journal of medicinal chemistry, , Feb-24, Volume: 43, Issue:4, 2000
Tolerance in the replacement of the benzhydrylic O atom in 4-[2-(diphenylmethoxy)ethyl]-1-benzylpiperidine derivatives by an N atom: development of new-generation potent and selective N-analogue molecules for the dopamine transporter.Journal of medicinal chemistry, , Aug-13, Volume: 41, Issue:17, 1998
Design and synthesis of 2- and 3-substituted-3-phenylpropyl analogs of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine: role of amino, fluoro, hydroxyl, methoxyl, methyl, mJournal of medicinal chemistry, , May-08, Volume: 51, Issue:9, 2008
Novel 3-aminomethyl- and 4-aminopiperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazines: synthesis and evaluation as dopamine transporter ligands.Journal of medicinal chemistry, , Jan-27, Volume: 43, Issue:2, 2000
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.Journal of medicinal chemistry, , 04-13, Volume: 60, Issue:7, 2017
Discovery of novel selective norepinephrine inhibitors: 1-(2-morpholin-2-ylethyl)-3-aryl-1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxides (WYE-114152).Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
Heterocyclic cycloalkanol ethylamines as norepinephrine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 20, Issue:9, 2010
Discovery of novel selective norepinephrine reuptake inhibitors: 4-[3-aryl-2,2-dioxido-2,1,3-benzothiadiazol-1(3H)-yl]-1-(methylamino)butan-2-ols (WYE-103231).Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
1- or 3-(3-Amino-2-hydroxy-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones: potent, selective, and orally efficacious norepinephrine reuptake inhibitors.Journal of medicinal chemistry, , Sep-24, Volume: 52, Issue:18, 2009
3-(Arylamino)-3-phenylpropan-2-olamines as a new series of dual norepinephrine and serotonin reuptake inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 19, Issue:9, 2009
Synthesis and activity of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 18, Issue:23, 2008
Structure-activity relationships of the cycloalkanol ethylamine scaffold: discovery of selective norepinephrine reuptake inhibitors.Journal of medicinal chemistry, , Jul-10, Volume: 51, Issue:13, 2008
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.Journal of medicinal chemistry, , Sep-12, Volume: 45, Issue:19, 2002
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.Journal of medicinal chemistry, , Sep-12, Volume: 45, Issue:19, 2002
Design and synthesis of 4-heteroaryl 1,2,3,4-tetrahydroisoquinolines as triple reuptake inhibitors.ACS medicinal chemistry letters, , Jul-10, Volume: 5, Issue:7, 2014
Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter.Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
Heterocyclic Analogues of Modafinil as Novel, Atypical Dopamine Transporter Inhibitors.Journal of medicinal chemistry, , 11-22, Volume: 60, Issue:22, 2017
Novel and High Affinity 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors.Journal of medicinal chemistry, , 12-08, Volume: 59, Issue:23, 2016
Elucidation of structural elements for selectivity across monoamine transporters: novel 2-[(diphenylmethyl)sulfinyl]acetamide (modafinil) analogues.Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
[no title available],
Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
Exploration of 3-Aminoazetidines as Triple Reuptake Inhibitors by Bioisosteric Modification of 3-α-Oxyazetidine.ACS medicinal chemistry letters, , Sep-11, Volume: 5, Issue:9, 2014
Exploration of novel 3-substituted azetidine derivatives as triple reuptake inhibitors.Journal of medicinal chemistry, , Sep-27, Volume: 55, Issue:18, 2012
Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with a heterocyclic ring constraint.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 18, Issue:16, 2008
Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI).Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 18, Issue:14, 2008
2-(2-(dimethylaminomethyl)phenoxy)-5-iodophenylamine: an improved serotonin transporter imaging agent.Journal of medicinal chemistry, , Oct-07, Volume: 47, Issue:21, 2004
Synthesis and characterization of iodine-123 labeled 2beta-carbomethoxy-3beta-(4'-((Z)-2-iodoethenyl)phenyl)nortropane. A ligand for in vivo imaging of serotonin transporters by single-photon-emission tomography.Journal of medicinal chemistry, , Mar-13, Volume: 46, Issue:6, 2003
Triple Reuptake Inhibitors as Potential Therapeutics for Depression and Other Disorders: Design Paradigm and Developmental Challenges.Journal of medicinal chemistry, , 03-22, Volume: 61, Issue:6, 2018
Discovery of imidazo[1,2-a]-, [1,2,4]triazolo[4,3-a]-, and [1,2,4]triazolo[1,5-a]pyridine-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 27, Issue:21, 2017
An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Azepines and piperidines with dual norepinephrine dopamine uptake inhibition and antidepressant activity.ACS medicinal chemistry letters, , Jan-10, Volume: 4, Issue:1, 2013
4-Phenyl tetrahydroisoquinolines as dual norepinephrine and dopamine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
Synthesis and pharmacological characterization of bicyclic triple reuptake inhibitor 3-aryl octahydrocyclopenta[c]pyrrole analogues.Journal of medicinal chemistry, , Aug-11, Volume: 54, Issue:15, 2011
Synthesis and pharmacological evaluation of 4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalenyl amines as triple reuptake inhibitors.Bioorganic & medicinal chemistry, , Jan-01, Volume: 19, Issue:1, 2011
Discovery of N-methyl-1-(1-phenylcyclohexyl)ethanamine, a novel triple serotonin, norepinephrine and dopamine reuptake inhibitor.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 21, Issue:5, 2011
The role of receptor binding in drug discovery.Journal of natural products, , Volume: 56, Issue:4, 1993
Triple Reuptake Inhibitors as Potential Therapeutics for Depression and Other Disorders: Design Paradigm and Developmental Challenges.Journal of medicinal chemistry, , 03-22, Volume: 61, Issue:6, 2018
Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds.Journal of medicinal chemistry, , 05-10, Volume: 61, Issue:9, 2018
Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
Discovery of a potent, dual serotonin and norepinephrine reuptake inhibitor.ACS medicinal chemistry letters, , Jun-13, Volume: 4, Issue:6, 2013
An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Synopsis of some recent tactical application of bioisosteres in drug design.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Synthesis and pharmacological evaluation of 3-aryl-3-azolylpropan-1-amines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 20, Issue:18, 2010
Heterocyclic cycloalkanol ethylamines as norepinephrine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 20, Issue:9, 2010
Synthesis of a potent wide-spectrum serotonin-, norepinephrine-, dopamine-reuptake inhibitor (SNDRI) and a species-selective dopamine-reuptake inhibitor based on the gamma-amino alcohol functional group.Bioorganic & medicinal chemistry letters, , Mar-03, Volume: 8, Issue:5, 1998
An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Trace amine-associated receptor 1 is a stereoselective binding site for compounds in the amphetamine class.Bioorganic & medicinal chemistry, , Dec-01, Volume: 19, Issue:23, 2011
A novel photoaffinity ligand for the dopamine transporter based on pyrovalerone.Bioorganic & medicinal chemistry, , Jun-01, Volume: 17, Issue:11, 2009
1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors.Journal of medicinal chemistry, , Feb-23, Volume: 49, Issue:4, 2006
Conformationally restricted homotryptamines. 2. Indole cyclopropylmethylamines as selective serotonin reuptake inhibitors.Journal of medicinal chemistry, , Sep-22, Volume: 48, Issue:19, 2005
Synthesis of a potent wide-spectrum serotonin-, norepinephrine-, dopamine-reuptake inhibitor (SNDRI) and a species-selective dopamine-reuptake inhibitor based on the gamma-amino alcohol functional group.Bioorganic & medicinal chemistry letters, , Mar-03, Volume: 8, Issue:5, 1998
[no title available],
1- or 3-(3-Amino-2-hydroxy-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones: potent, selective, and orally efficacious norepinephrine reuptake inhibitors.Journal of medicinal chemistry, , Sep-24, Volume: 52, Issue:18, 2009
Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with a heterocyclic ring constraint.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 18, Issue:16, 2008
Characterization of thien-2-yl 1S,2R-milnacipran analogues as potent norepinephrine/serotonin transporter inhibitors for the treatment of neuropathic pain.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI).Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 18, Issue:14, 2008
Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 18, Issue:4, 2008
Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with improved pharmaceutical characteristics.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 18, Issue:23, 2008
Structure-activity relationships of chiral selective norepinephrine reuptake inhibitors (sNRI) with increased oxidative stability.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 18, Issue:16, 2008
Identification of 1S,2R-milnacipran analogs as potent norepinephrine and serotonin transporter inhibitors.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 18, Issue:11, 2008
Synthesis of a potent wide-spectrum serotonin-, norepinephrine-, dopamine-reuptake inhibitor (SNDRI) and a species-selective dopamine-reuptake inhibitor based on the gamma-amino alcohol functional group.Bioorganic & medicinal chemistry letters, , Mar-03, Volume: 8, Issue:5, 1998
Azepines and piperidines with dual norepinephrine dopamine uptake inhibition and antidepressant activity.ACS medicinal chemistry letters, , Jan-10, Volume: 4, Issue:1, 2013
4-Phenyl tetrahydroisoquinolines as dual norepinephrine and dopamine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
Exploration of 3-Aminoazetidines as Triple Reuptake Inhibitors by Bioisosteric Modification of 3-α-Oxyazetidine.ACS medicinal chemistry letters, , Sep-11, Volume: 5, Issue:9, 2014
Discovery of a potent, dual serotonin and norepinephrine reuptake inhibitor.ACS medicinal chemistry letters, , Jun-13, Volume: 4, Issue:6, 2013
A novel class of 3-(phenoxy-phenyl-methyl)-pyrrolidines as potent and balanced norepinephrine and serotonin reuptake inhibitors: synthesis and structure-activity relationships.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 23, Issue:5, 2013
Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reducing ion channel activity.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 20, Issue:12, 2010
Heterocyclic cycloalkanol ethylamines as norepinephrine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 20, Issue:9, 2010
N-[(3S)-Pyrrolidin-3-yl]benzamides as novel dual serotonin and noradrenaline reuptake inhibitors: impact of small structural modifications on P-gp recognition and CNS penetration.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 19, Issue:17, 2009
Novel, achiral aminoheterocycles as selective monoamine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 19, Issue:16, 2009
4-Piperidines and 3-pyrrolidines as dual serotonin and noradrenaline reuptake inhibitors: design, synthesis and structure-activity relationships.Bioorganic & medicinal chemistry letters, , May-15, Volume: 19, Issue:10, 2009
Characterization of thien-2-yl 1S,2R-milnacipran analogues as potent norepinephrine/serotonin transporter inhibitors for the treatment of neuropathic pain.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 18, Issue:4, 2008
Design and synthesis of morpholine derivatives. SAR for dual serotonin & noradrenaline reuptake inhibition.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 18, Issue:8, 2008
N-Benzyl-N-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-amines as selective dual serotonin/noradrenaline reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 17, Issue:7, 2007
N-(1,2-diphenylethyl)piperazines: a new class of dual serotonin/noradrenaline reuptake inhibitor.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
Synthesis and biological activity of some known and putative duloxetine metabolites.Bioorganic & medicinal chemistry letters, , Jul-05, Volume: 14, Issue:13, 2004
Duloxetine (Cymbalta), a dual inhibitor of serotonin and norepinephrine reuptake.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 13, Issue:24, 2003
Exploration of substituted arylpiperazine-tetrazoles as promising dual norepinephrine and dopamine reuptake inhibitors.Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Exploration of 3-Aminoazetidines as Triple Reuptake Inhibitors by Bioisosteric Modification of 3-α-Oxyazetidine.ACS medicinal chemistry letters, , Sep-11, Volume: 5, Issue:9, 2014
Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 19, Issue:8, 2009
Design and optimisation of selective serotonin re-uptake inhibitors with high synthetic accessibility: part 2.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 19, Issue:20, 2009
A novel class of 3-(phenoxy-phenyl-methyl)-pyrrolidines as potent and balanced norepinephrine and serotonin reuptake inhibitors: synthesis and structure-activity relationships.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 23, Issue:5, 2013
1- or 3-(3-Amino-2-hydroxy-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones: potent, selective, and orally efficacious norepinephrine reuptake inhibitors.Journal of medicinal chemistry, , Sep-24, Volume: 52, Issue:18, 2009
Synthesis, radiosynthesis, and biological evaluation of carbon-11 and fluorine-18 labeled reboxetine analogues: potential positron emission tomography radioligands for in vivo imaging of the norepinephrine transporter.Journal of medicinal chemistry, , Jan-08, Volume: 52, Issue:1, 2009
Structure-activity relationships of chiral selective norepinephrine reuptake inhibitors (sNRI) with increased oxidative stability.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 18, Issue:16, 2008
Synthesis and pharmacological evaluation of 4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalenyl amines as triple reuptake inhibitors.Bioorganic & medicinal chemistry, , Jan-01, Volume: 19, Issue:1, 2011
Designing rapid onset selective serotonin re-uptake inhibitors. Part 1: Structure-activity relationships of substituted (1S,4S)-4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydro-1-naphthaleneamine.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 16, Issue:5, 2006
Synthesis of a potent wide-spectrum serotonin-, norepinephrine-, dopamine-reuptake inhibitor (SNDRI) and a species-selective dopamine-reuptake inhibitor based on the gamma-amino alcohol functional group.Bioorganic & medicinal chemistry letters, , Mar-03, Volume: 8, Issue:5, 1998
[no title available],
Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 23, Issue:20, 2013
Synthesis and evaluation of novel tropane derivatives as potential PET imaging agents for the dopamine transporter.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 22, Issue:13, 2012
Exploration of novel 3-substituted azetidine derivatives as triple reuptake inhibitors.Journal of medicinal chemistry, , Sep-27, Volume: 55, Issue:18, 2012
[no title available],
[no title available]Journal of medicinal chemistry, , 03-12, Volume: 63, Issue:5, 2020
QSAR study and synthesis of new phenyltropanes as ligands of the dopamine transporter (DAT).Bioorganic & medicinal chemistry, , Feb-15, Volume: 20, Issue:4, 2012
Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHBioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators.Journal of medicinal chemistry, , Aug-11, Volume: 54, Issue:15, 2011
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
Evolution of a Compact Photoprobe for the Dopamine Transporter Based on (±)-threo-Methylphenidate.ACS medicinal chemistry letters, , May-10, Volume: 3, Issue:5, 2012
Azido-iodo-N-benzyl derivatives of threo-methylphenidate (Ritalin, Concerta): Rational design, synthesis, pharmacological evaluation, and dopamine transporter photoaffinity labeling.Bioorganic & medicinal chemistry, , Jan-01, Volume: 19, Issue:1, 2011
[no title available]Journal of medicinal chemistry, , 03-12, Volume: 63, Issue:5, 2020
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.Journal of medicinal chemistry, , 04-13, Volume: 60, Issue:7, 2017
Novel and High Affinity 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors.Journal of medicinal chemistry, , 12-08, Volume: 59, Issue:23, 2016
An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
The synthesis and biological evaluation of 2-(3-methyl or 3-phenylisoxazol-5-yl)-3-aryl-8-thiabicyclo[3.2.1]octanes.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
Synthesis and structure-activity relationship of 3beta-(4-alkylthio, -methylsulfinyl, and -methylsulfonylphenyl)tropane and 3beta-(4-alkylthiophenyl)nortropane derivatives for monoamine transporters.Bioorganic & medicinal chemistry, , Jul-15, Volume: 17, Issue:14, 2009
Dual inhibitors of phosphodiesterase-4 and serotonin reuptake.Journal of medicinal chemistry, , Mar-26, Volume: 52, Issue:6, 2009
Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction.Journal of medicinal chemistry, , Nov-12, Volume: 52, Issue:21, 2009
Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression.Bioorganic & medicinal chemistry, , Jan-01, Volume: 17, Issue:1, 2009
2,5-Disubstituted tetrahydrofurans as selective serotonin re-uptake inhibitors.Bioorganic & medicinal chemistry, , Mar-01, Volume: 17, Issue:5, 2009
Inhibition of serotonin and norepinephrine reuptake and inhibition of phosphodiesterase by multi-target inhibitors as potential agents for depression.Bioorganic & medicinal chemistry, , Oct-01, Volume: 17, Issue:19, 2009
Synthesis and receptor binding properties of 2beta-alkynyl and 2beta-(1,2,3-triazol)substituted 3beta-(substituted phenyl)tropane derivatives.Bioorganic & medicinal chemistry, , May-15, Volume: 16, Issue:10, 2008
Design and synthesis of 2- and 3-substituted-3-phenylpropyl analogs of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine: role of amino, fluoro, hydroxyl, methoxyl, methyl, mJournal of medicinal chemistry, , May-08, Volume: 51, Issue:9, 2008
Synthesis, monoamine transporter binding, properties, and functional monoamine uptake activity of 3beta-[4-methylphenyl and 4-chlorophenyl]-2 beta-[5-(substituted phenyl)thiazol-2-yl]tropanes.Journal of medicinal chemistry, , Jul-26, Volume: 50, Issue:15, 2007
Synthesis, inhibition and binding of simple non-nitrogen inhibitors of monoamine transporters.Bioorganic & medicinal chemistry, , Jun-15, Volume: 15, Issue:12, 2007
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:11, 2007
Localization of cocaine analog [125I]RTI 82 irreversible binding to transmembrane domain 6 of the dopamine transporter.The Journal of biological chemistry, , Mar-23, Volume: 282, Issue:12, 2007
Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter.Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
Synthesis and monoamine transporter binding properties of 2,3-cyclo analogues of 3beta-(4'-aminophenyl)-2beta-tropanemethanol.Journal of medicinal chemistry, , Jul-27, Volume: 49, Issue:15, 2006
1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors.Journal of medicinal chemistry, , Feb-23, Volume: 49, Issue:4, 2006
The role of QSAR in dopamine interactions.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 15, Issue:8, 2005
Synthesis and pharmacology of ethylphenidate enantiomers: the human transesterification metabolite of methylphenidate and ethanol.Journal of medicinal chemistry, , Apr-21, Volume: 48, Issue:8, 2005
Synthesis and monoamine transporter binding properties of 2,3-diaryltropanes.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers.Journal of medicinal chemistry, , Dec-02, Volume: 47, Issue:25, 2004
Pharmacophore-based discovery of substituted pyridines as novel dopamine transporter inhibitors.Bioorganic & medicinal chemistry letters, , Feb-10, Volume: 13, Issue:3, 2003
Synthesis and biological activity of 2-carbomethoxy-3-catechol-8-azabicyclo[3.2.1]octanes.Bioorganic & medicinal chemistry letters, , Nov-17, Volume: 13, Issue:22, 2003
Bivalent biogenic amine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Jul-07, Volume: 13, Issue:13, 2003
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.Journal of medicinal chemistry, , Sep-12, Volume: 45, Issue:19, 2002
Discovery of a novel dopamine transporter inhibitor, 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone, as a potential cocaine antagonist through 3D-database pharmacophore searching. Molecular modeling, structure-activity relationshiJournal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Design, synthesis and biological evaluation of 7-azatricyclodecanes: analogues of cocaine.Bioorganic & medicinal chemistry letters, , Feb-07, Volume: 10, Issue:3, 2000
Slow-onset, long-duration 3-(3',4'-dichlorophenyl)-1-indanamine monoamine reuptake blockers as potential medications to treat cocaine abuse.Journal of medicinal chemistry, , Dec-28, Volume: 43, Issue:26, 2000
Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter.Journal of medicinal chemistry, , May-18, Volume: 43, Issue:10, 2000
Novel 3-aminomethyl- and 4-aminopiperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazines: synthesis and evaluation as dopamine transporter ligands.Journal of medicinal chemistry, , Jan-27, Volume: 43, Issue:2, 2000
Design, synthesis, and biological evaluation of novel non-piperazine analogues of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines as dopamine transporter inhibitors.Journal of medicinal chemistry, , Sep-09, Volume: 42, Issue:18, 1999
Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter.Journal of medicinal chemistry, , Mar-20, Volume: 35, Issue:6, 1992
Synthesis, fluorine-18 radiolabeling, and biological evaluation of N-((E)-4-fluorobut-2-en-1-yl)-2beta-carbomethoxy-3beta-(4'-halophenyl)nortropanes: candidate radioligands for in vivo imaging of the brain dopamine transporter with positron emission tomogJournal of medicinal chemistry, , Aug-12, Volume: 53, Issue:15, 2010
Development of 3-phenyltropane analogues with high affinity for the dopamine and serotonin transporters and low affinity for the norepinephrine transporter.Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
Synthesis and monoamine transporter binding properties of 2beta-[3'-(substituted benzyl)isoxazol-5-yl]- and 2beta-[3'-methyl-4'-(substituted phenyl)isoxazol-5-yl]-3beta-(substituted phenyl)tropanes.Bioorganic & medicinal chemistry, , Jul-15, Volume: 16, Issue:14, 2008
[no title available],
Design and synthesis of morpholine derivatives. SAR for dual serotonin & noradrenaline reuptake inhibition.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 18, Issue:8, 2008
[4-(Phenoxy)pyridin-3-yl]methylamines: a new class of selective noradrenaline reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 18, Issue:6, 2008
N-(1,2-diphenylethyl)piperazines: a new class of dual serotonin/noradrenaline reuptake inhibitor.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
Synthesis, radiosynthesis, and biological evaluation of carbon-11 and iodine-123 labeled 2beta-carbomethoxy-3beta-[4'-((Z)-2-haloethenyl)phenyl]tropanes: candidate radioligands for in vivo imaging of the serotonin transporter.Journal of medicinal chemistry, , Feb-26, Volume: 47, Issue:5, 2004
Synthesis and characterization of iodine-123 labeled 2beta-carbomethoxy-3beta-(4'-((Z)-2-iodoethenyl)phenyl)nortropane. A ligand for in vivo imaging of serotonin transporters by single-photon-emission tomography.Journal of medicinal chemistry, , Mar-13, Volume: 46, Issue:6, 2003
Studies on a series of milnacipran analogs containing a heteroaromatic group as potent norepinephrine and serotonin transporter inhibitors.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 18, Issue:11, 2008
Identification of 1S,2R-milnacipran analogs as potent norepinephrine and serotonin transporter inhibitors.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 18, Issue:11, 2008
Structure-Activity Relationships of Novel Thiazole-Based Modafinil Analogues Acting at Monoamine Transporters.Journal of medicinal chemistry, , 01-09, Volume: 63, Issue:1, 2020
Novel and High Affinity 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors.Journal of medicinal chemistry, , 12-08, Volume: 59, Issue:23, 2016
Synthesis of 2-(substituted phenyl)-3,5,5-trimethylmorpholine analogues and their effects on monoamine uptake, nicotinic acetylcholine receptor function, and behavioral effects of nicotine.Journal of medicinal chemistry, , Mar-10, Volume: 54, Issue:5, 2011
Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation.Journal of medicinal chemistry, , Jun-24, Volume: 53, Issue:12, 2010
Triple Reuptake Inhibitors as Potential Therapeutics for Depression and Other Disorders: Design Paradigm and Developmental Challenges.Journal of medicinal chemistry, , 03-22, Volume: 61, Issue:6, 2018
Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
Synthesis and pharmacological evaluation of 4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalenyl amines as triple reuptake inhibitors.Bioorganic & medicinal chemistry, , Jan-01, Volume: 19, Issue:1, 2011
Synthesis and pharmacological evaluation of 3-aryl-3-azolylpropan-1-amines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 20, Issue:18, 2010
Novel 3,3-disubstituted pyrrolidines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 18, Issue:23, 2008
Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 18, Issue:13, 2008
2-(2-(dimethylaminomethyl)phenoxy)-5-iodophenylamine: an improved serotonin transporter imaging agent.Journal of medicinal chemistry, , Oct-07, Volume: 47, Issue:21, 2004
A new single-photon emission computed tomography imaging agent for serotonin transporters: [123I]IDAM, 5-iodo-2-((2-((dimethylamino)methyl)phenyl)thio)benzyl alcohol.Journal of medicinal chemistry, , Feb-11, Volume: 42, Issue:3, 1999
Docking study, synthesis, and in vitro evaluation of fluoro-MADAM derivatives as SERT ligands for PET imaging.Bioorganic & medicinal chemistry, , Oct-01, Volume: 16, Issue:19, 2008
Synthesis and in vitro evaluation of novel derivatives of diphenylsulfide as serotonin transporter ligands.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 16, Issue:5, 2006
Synthesis, in vitro characterization, and radiolabeling of N,N-dimethyl-2-(2'-amino-4'-substituted-phenylthio)benzylamines: potential candidates as selective serotonin transporter radioligands.Journal of medicinal chemistry, , Jun-30, Volume: 48, Issue:13, 2005
Fluorinated diaryl sulfides as serotonin transporter ligands: synthesis, structure-activity relationship study, and in vivo evaluation of fluorine-18-labeled compounds as PET imaging agents.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
Fluorinated diaryl sulfides as serotonin transporter ligands: synthesis, structure-activity relationship study, and in vivo evaluation of fluorine-18-labeled compounds as PET imaging agents.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
2-(2-(dimethylaminomethyl)phenoxy)-5-iodophenylamine: an improved serotonin transporter imaging agent.Journal of medicinal chemistry, , Oct-07, Volume: 47, Issue:21, 2004
Novel radiotracers for imaging the serotonin transporter by positron emission tomography: synthesis, radiosynthesis, and in vitro and ex vivo evaluation of (11)C-labeled 2-(phenylthio)araalkylamines.Journal of medicinal chemistry, , Aug-10, Volume: 43, Issue:16, 2000
Discovery of a potent, dual serotonin and norepinephrine reuptake inhibitor.ACS medicinal chemistry letters, , Jun-13, Volume: 4, Issue:6, 2013
A novel class of 3-(phenoxy-phenyl-methyl)-pyrrolidines as potent and balanced norepinephrine and serotonin reuptake inhibitors: synthesis and structure-activity relationships.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 23, Issue:5, 2013
Characterization of thien-2-yl 1S,2R-milnacipran analogues as potent norepinephrine/serotonin transporter inhibitors for the treatment of neuropathic pain.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Studies on a series of milnacipran analogs containing a heteroaromatic group as potent norepinephrine and serotonin transporter inhibitors.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 18, Issue:11, 2008
Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 18, Issue:4, 2008
Identification of 1S,2R-milnacipran analogs as potent norepinephrine and serotonin transporter inhibitors.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 18, Issue:11, 2008
Synthesis and pharmacological investigation of aralkyl diamine derivatives as potential triple reuptake inhibitors.European journal of medicinal chemistry, , Oct-30, Volume: 86, 2014
1-(Aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes and 6-(aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes: a new series of potent and selective triple reuptake inhibitors.Journal of medicinal chemistry, , Mar-25, Volume: 53, Issue:6, 2010
6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane: a new potent and selective triple reuptake inhibitor.Journal of medicinal chemistry, , Jul-08, Volume: 53, Issue:13, 2010
Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 18, Issue:13, 2008
Synthesis, in vitro characterization, and radiolabeling of N,N-dimethyl-2-(2'-amino-4'-substituted-phenylthio)benzylamines: potential candidates as selective serotonin transporter radioligands.Journal of medicinal chemistry, , Jun-30, Volume: 48, Issue:13, 2005
Fluorinated diaryl sulfides as serotonin transporter ligands: synthesis, structure-activity relationship study, and in vivo evaluation of fluorine-18-labeled compounds as PET imaging agents.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
2-(2-(dimethylaminomethyl)phenoxy)-5-iodophenylamine: an improved serotonin transporter imaging agent.Journal of medicinal chemistry, , Oct-07, Volume: 47, Issue:21, 2004
The discovery of an unusually selective and novel cocaine analog: difluoropine. Synthesis and inhibition of binding at cocaine recognition sites.Journal of medicinal chemistry, , Jun-24, Volume: 37, Issue:13, 1994
Enantioselectivity of cocaine recognition sites: binding of (1S)- and (1R)-2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane (beta-CIT) to monoamine transporters.Journal of medicinal chemistry, , Jun-25, Volume: 36, Issue:13, 1993
Synthesis and monoamine transporter binding properties of 2,3-diaryltropanes.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers.Journal of medicinal chemistry, , Dec-02, Volume: 47, Issue:25, 2004
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 26, Issue:3, 2016
An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Enables
This protein enables 13 target(s):
Target | Category | Definition |
protease binding | molecular function | Binding to a protease or a peptidase. [GOC:hjd] |
signaling receptor binding | molecular function | Binding to one or more specific sites on a receptor molecule, a macromolecule that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:bf, GOC:ceb, ISBN:0198506732] |
neurotransmitter transmembrane transporter activity | molecular function | Enables the directed movement of a neurotransmitter into, out of or within a cell, or between cells. Neurotransmitters are any chemical substance that is capable of transmitting (or inhibiting the transmission of) a nerve impulse from a neuron to another cell. [GOC:ai, ISBN:0198506732] |
dopamine:sodium symporter activity | molecular function | Enables the transfer of a solute or solutes from one side of a membrane to the other according to the reaction: dopamine(out) + Na+(out) + Cl-(out)= dopamine(in) + Na+(in) + Cl-(in). [PMID:21752877, PMID:22519513, TC:2.A.22.1.3] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
monoamine transmembrane transporter activity | molecular function | Enables the transfer of monoamines, organic compounds that contain one amino group that is connected to an aromatic ring by an ethylene group (-CH2-CH2-), from one side of a membrane to the other. [GOC:mah] |
dopamine binding | molecular function | Binding to dopamine, a catecholamine neurotransmitter formed by aromatic-L-amino-acid decarboxylase from 3,4-dihydroxy-L-phenylalanine. [ISBN:0198506732] |
amine binding | molecular function | Binding to an amine, a weakly basic organic compound that contains an amino or a substituted amino group. [GOC:jl] |
protein-containing complex binding | molecular function | Binding to a macromolecular complex. [GOC:jl] |
metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
protein phosphatase 2A binding | molecular function | Binding to protein phosphatase 2A. [GOC:ai] |
heterocyclic compound binding | molecular function | Binding to heterocyclic compound. [GOC:TermGenie] |
norepinephrine:sodium symporter activity | molecular function | Enables the transfer of a solute or solutes from one side of a membrane to the other according to the reaction: norepinephrine(out) + Na+(out) + Cl-(out) = norepinephrine(in) + Na+(in) + Cl-(in). [PMID:21752877, PMID:22519513, TC:2.A.22.1.2] |
Located In
This protein is located in 11 target(s):
Target | Category | Definition |
cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
cell surface | cellular component | The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm] |
membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
axon | cellular component | The long process of a neuron that conducts nerve impulses, usually away from the cell body to the terminals and varicosities, which are sites of storage and release of neurotransmitter. [GOC:nln, ISBN:0198506732] |
neuron projection | cellular component | A prolongation or process extending from a nerve cell, e.g. an axon or dendrite. [GOC:jl, http://www.cogsci.princeton.edu/~wn/] |
neuronal cell body | cellular component | The portion of a neuron that includes the nucleus, but excludes cell projections such as axons and dendrites. [GOC:go_curators] |
axon terminus | cellular component | Terminal inflated portion of the axon, containing the specialized apparatus necessary to release neurotransmitters. The axon terminus is considered to be the whole region of thickening and the terminal button is a specialized region of it. [GOC:dph, GOC:jl] |
membrane raft | cellular component | Any of the small (10-200 nm), heterogeneous, highly dynamic, sterol- and sphingolipid-enriched membrane domains that compartmentalize cellular processes. Small rafts can sometimes be stabilized to form larger platforms through protein-protein and protein-lipid interactions. [PMID:16645198, PMID:20044567] |
postsynaptic membrane | cellular component | A specialized area of membrane facing the presynaptic membrane on the tip of the nerve ending and separated from it by a minute cleft (the synaptic cleft). Neurotransmitters cross the synaptic cleft and transmit the signal to the postsynaptic membrane. [ISBN:0198506732] |
dopaminergic synapse | cellular component | A synapse that uses dopamine as a neurotransmitter. [GOC:dos] |
Active In
This protein is active in 4 target(s):
Target | Category | Definition |
axon | cellular component | The long process of a neuron that conducts nerve impulses, usually away from the cell body to the terminals and varicosities, which are sites of storage and release of neurotransmitter. [GOC:nln, ISBN:0198506732] |
presynaptic membrane | cellular component | A specialized area of membrane of the axon terminal that faces the plasma membrane of the neuron or muscle fiber with which the axon terminal establishes a synaptic junction; many synaptic junctions exhibit structural presynaptic characteristics, such as conical, electron-dense internal protrusions, that distinguish it from the remainder of the axon plasma membrane. [GOC:jl, ISBN:0815316194] |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
neuronal cell body membrane | cellular component | The plasma membrane of a neuron cell body - excludes the plasma membrane of cell projections such as axons and dendrites. [GOC:jl] |
Part Of
This protein is part of 1 target(s):
Target | Category | Definition |
flotillin complex | cellular component | A protein complex that contains flotillin-1 and flotillin-2, and may contain associated proteins. Flotillins associate into membrane microdomains resembling caveolae. [PMID:17206938, PMID:17600709] |
Involved In
This protein is involved in 25 target(s):
Target | Category | Definition |
neurotransmitter transport | biological process | The directed movement of a neurotransmitter into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. Neurotransmitters are any chemical substance that is capable of transmitting (or inhibiting the transmission of) a nerve impulse from a neuron to another cell. [GOC:ai] |
lactation | biological process | The regulated release of milk from the mammary glands and the period of time that a mother lactates to feed her young. [ISBN:0198506732] |
sensory perception of smell | biological process | The series of events required for an organism to receive an olfactory stimulus, convert it to a molecular signal, and recognize and characterize the signal. Olfaction involves the detection of chemical composition of an organism's ambient medium by chemoreceptors. This is a neurological process. [GOC:ai] |
locomotory behavior | biological process | The specific movement from place to place of an organism in response to external or internal stimuli. Locomotion of a whole organism in a manner dependent upon some combination of that organism's internal state and external conditions. [GOC:dph] |
response to xenobiotic stimulus | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus from a xenobiotic, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:jl, GOC:krc] |
response to iron ion | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an iron ion stimulus. [GOC:sm] |
dopamine transport | biological process | The directed movement of dopamine into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. Dopamine is a catecholamine neurotransmitter and a metabolic precursor of noradrenaline and adrenaline. [GOC:ai] |
adenohypophysis development | biological process | The progression of the adenohypophysis over time from its initial formation until its mature state. The adenohypophysis is the anterior part of the pituitary. It secretes a variety of hormones and its function is regulated by the hypothalamus. [GO_REF:0000021, GOC:cls, GOC:dgh, GOC:dph, GOC:jid] |
response to nicotine | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a nicotine stimulus. [GOC:bf, GOC:ef, ISBN:0198506732, ISBN:0582227089] |
positive regulation of multicellular organism growth | biological process | Any process that activates or increases the frequency, rate or extent of growth of an organism to reach its usual body size. [GOC:dph, GOC:go_curators, GOC:tb] |
regulation of dopamine metabolic process | biological process | Any process that modulates the frequency, rate or extent of the chemical reactions and pathways involving dopamine. [GOC:go_curators] |
response to cocaine | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cocaine stimulus. Cocaine is a crystalline alkaloid obtained from the leaves of the coca plant. [GOC:ef, GOC:jl] |
dopamine biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of dopamine, a catecholamine neurotransmitter and a metabolic precursor of noradrenaline and adrenaline. [GOC:jl, ISBN:0198506732] |
dopamine catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of dopamine, a catecholamine neurotransmitter and a metabolic precursor of noradrenaline and adrenaline. [GOC:jl, ISBN:0198506732] |
response to ethanol | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an ethanol stimulus. [GOC:go_curators] |
cognition | biological process | The operation of the mind by which an organism becomes aware of objects of thought or perception; it includes the mental activities associated with thinking, learning, and memory. [ISBN:0721619908] |
dopamine uptake involved in synaptic transmission | biological process | The directed movement of dopamine into a presynaptic neuron or glial cell. In this context, dopamine is a catecholamine neurotransmitter and a metabolic precursor of noradrenaline and adrenaline. [GOC:ai] |
response to cAMP | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cAMP (cyclic AMP, adenosine 3',5'-cyclophosphate) stimulus. [GOC:ai] |
norepinephrine uptake | biological process | The directed movement of norepinephrine into a cell, typically presynaptic neurons or glial cells. Norepinephrine (3,4-dihydroxyphenyl-2-aminoethanol) is a hormone secreted by the adrenal medulla and a neurotransmitter in the sympathetic peripheral nervous system and in some tracts of the CNS. It is also the biosynthetic precursor of epinephrine. [GOC:ai] |
prepulse inhibition | biological process | The process in which a startle magnitude is reduced when the startling stimulus is preceded by a low-intensity prepulse. [GOC:dph, PMID:10341260] |
dopamine uptake | biological process | The directed movement of dopamine into a cell. [GOC:dph, GOC:tb] |
hyaloid vascular plexus regression | biological process | The developmental process in which the hyaloid vascular plexus is destroyed as a part of its normal progression. [GOC:hjd, PMID:18841878] |
amino acid transport | biological process | The directed movement of amino acids, organic acids containing one or more amino substituents, into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:ai] |
norepinephrine transport | biological process | The directed movement of norepinephrine into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. Norepinephrine (3,4-dihydroxyphenyl-2-aminoethanol) is a hormone secreted by the adrenal medulla and a neurotransmitter in the sympathetic peripheral nervous system and in some tracts of the CNS. It is also the biosynthetic precursor of epinephrine. [GOC:ai, ISBN:0198506732] |
sodium ion transmembrane transport | biological process | A process in which a sodium ion is transported from one side of a membrane to the other by means of some agent such as a transporter or pore. [GOC:vw] |