Proteins > Sodium-dependent serotonin transporter
Page last updated: 2024-08-07 16:29:00
Sodium-dependent serotonin transporter
A sodium-dependent serotonin transporter that is encoded in the genome of human. [PRO:DNx, UniProtKB:P31645]
Synonyms
SERT;
5HT transporter;
5HTT;
Solute carrier family 6 member 4
Research
Bioassay Publications (230)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 1 (0.43) | 18.7374 |
| 1990's | 8 (3.48) | 18.2507 |
| 2000's | 109 (47.39) | 29.6817 |
| 2010's | 98 (42.61) | 24.3611 |
| 2020's | 14 (6.09) | 2.80 |
Compounds (198)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| bupropion | Homo sapiens (human) | IC50 | 61.7750 | 4 | 4 |
| bupropion | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 1-(3-chlorophenyl)piperazine | Homo sapiens (human) | Ki | 0.2710 | 1 | 1 |
| 3,4-methylenedioxyamphetamine | Homo sapiens (human) | IC50 | 2.7129 | 3 | 3 |
| 3,4-methylenedioxyamphetamine | Homo sapiens (human) | Ki | 2.3060 | 1 | 1 |
| n-methyl-3,4-methylenedioxyamphetamine | Homo sapiens (human) | IC50 | 1.1761 | 4 | 4 |
| n-methyl-3,4-methylenedioxyamphetamine | Homo sapiens (human) | Ki | 0.3169 | 3 | 3 |
| 4-nonylphenol | Homo sapiens (human) | IC50 | 3.3800 | 1 | 0 |
| 4-nonylphenol | Homo sapiens (human) | Ki | 1.7950 | 1 | 0 |
| ambroxol | Homo sapiens (human) | IC50 | 3.3910 | 1 | 0 |
| ambroxol | Homo sapiens (human) | Ki | 1.8020 | 1 | 0 |
| amiodarone | Homo sapiens (human) | IC50 | 2.3050 | 1 | 0 |
| amiodarone | Homo sapiens (human) | Ki | 1.2240 | 1 | 0 |
| amitriptyline | Homo sapiens (human) | IC50 | 0.2756 | 2 | 1 |
| amitriptyline | Homo sapiens (human) | Ki | 0.0284 | 5 | 5 |
| amoxapine | Homo sapiens (human) | IC50 | 0.0340 | 1 | 0 |
| amoxapine | Homo sapiens (human) | Ki | 0.0180 | 1 | 0 |
| astemizole | Homo sapiens (human) | IC50 | 1.3180 | 1 | 0 |
| astemizole | Homo sapiens (human) | Ki | 0.7000 | 1 | 0 |
| bromhexine | Homo sapiens (human) | IC50 | 2.0910 | 1 | 0 |
| bromhexine | Homo sapiens (human) | Ki | 1.1110 | 1 | 0 |
| butenafine | Homo sapiens (human) | IC50 | 1.4118 | 1 | 0 |
| butenafine | Homo sapiens (human) | Ki | 0.7500 | 1 | 0 |
| verapamil | Homo sapiens (human) | IC50 | 0.2400 | 1 | 0 |
| verapamil | Homo sapiens (human) | Ki | 0.1270 | 1 | 0 |
| carvedilol | Homo sapiens (human) | IC50 | 0.2210 | 1 | 0 |
| carvedilol | Homo sapiens (human) | Ki | 0.1180 | 1 | 0 |
| celecoxib | Homo sapiens (human) | IC50 | 6.2760 | 1 | 0 |
| celecoxib | Homo sapiens (human) | Ki | 3.3340 | 1 | 0 |
| chlorpromazine | Homo sapiens (human) | IC50 | 0.0795 | 2 | 1 |
| chlorpromazine | Homo sapiens (human) | Ki | 0.0421 | 2 | 1 |
| ciglitazone | Homo sapiens (human) | IC50 | 14.9480 | 1 | 0 |
| ciglitazone | Homo sapiens (human) | Ki | 7.9410 | 1 | 0 |
| cisapride | Homo sapiens (human) | IC50 | 0.3840 | 1 | 0 |
| cisapride | Homo sapiens (human) | Ki | 0.2040 | 1 | 0 |
| citalopram | Homo sapiens (human) | IC50 | 0.0227 | 9 | 8 |
| citalopram | Homo sapiens (human) | Ki | 0.0118 | 8 | 7 |
| clomipramine | Homo sapiens (human) | IC50 | 0.0350 | 2 | 1 |
| clomipramine | Homo sapiens (human) | Ki | 0.0002 | 2 | 1 |
| clotrimazole | Homo sapiens (human) | IC50 | 5.7600 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | Ki | 3.0600 | 1 | 0 |
| cyproheptadine | Homo sapiens (human) | Ki | 4.1000 | 1 | 1 |
| desipramine | Homo sapiens (human) | IC50 | 0.1961 | 4 | 4 |
| desipramine | Homo sapiens (human) | Ki | 0.0200 | 1 | 1 |
| domperidone | Homo sapiens (human) | IC50 | 3.0550 | 1 | 0 |
| domperidone | Homo sapiens (human) | Ki | 1.6230 | 1 | 0 |
| donepezil | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 1 |
| doxazosin | Homo sapiens (human) | IC50 | 2.6880 | 1 | 0 |
| doxazosin | Homo sapiens (human) | Ki | 1.4280 | 1 | 0 |
| doxepin | Homo sapiens (human) | IC50 | 0.0420 | 1 | 0 |
| doxepin | Homo sapiens (human) | Ki | 0.0220 | 1 | 0 |
| ebastine | Homo sapiens (human) | IC50 | 1.2287 | 1 | 0 |
| ebastine | Homo sapiens (human) | Ki | 0.6528 | 1 | 0 |
| econazole | Homo sapiens (human) | IC50 | 0.4230 | 1 | 0 |
| econazole | Homo sapiens (human) | Ki | 0.2250 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | IC50 | 1.4920 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | Ki | 0.7930 | 1 | 0 |
| fluoxetine | Homo sapiens (human) | IC50 | 0.0342 | 34 | 33 |
| fluoxetine | Homo sapiens (human) | Ki | 0.4577 | 14 | 14 |
| vanoxerine | Homo sapiens (human) | IC50 | 1.5513 | 3 | 3 |
| vanoxerine | Homo sapiens (human) | Ki | 0.1280 | 2 | 2 |
| gbr 12935 | Homo sapiens (human) | IC50 | 1.9995 | 2 | 2 |
| gbr 12935 | Homo sapiens (human) | Ki | 1.3550 | 2 | 2 |
| haloperidol | Homo sapiens (human) | IC50 | 3.3860 | 1 | 0 |
| haloperidol | Homo sapiens (human) | Ki | 1.7997 | 3 | 2 |
| haloprogin | Homo sapiens (human) | IC50 | 0.8110 | 1 | 0 |
| haloprogin | Homo sapiens (human) | Ki | 0.4310 | 1 | 0 |
| hexachlorophene | Homo sapiens (human) | IC50 | 4.3494 | 1 | 0 |
| hexachlorophene | Homo sapiens (human) | Ki | 2.3106 | 1 | 0 |
| imipramine | Homo sapiens (human) | IC50 | 0.0074 | 15 | 15 |
| imipramine | Homo sapiens (human) | Ki | 0.0879 | 16 | 16 |
| ketanserin | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| ketoconazole | Homo sapiens (human) | IC50 | 0.5310 | 1 | 0 |
| ketoconazole | Homo sapiens (human) | Ki | 0.2820 | 1 | 0 |
| loperamide | Homo sapiens (human) | IC50 | 2.2020 | 1 | 0 |
| loperamide | Homo sapiens (human) | Ki | 1.1700 | 1 | 0 |
| mazindol | Homo sapiens (human) | IC50 | 0.0740 | 2 | 2 |
| mazindol | Homo sapiens (human) | Ki | 0.0703 | 4 | 4 |
| methapyrilene | Homo sapiens (human) | IC50 | 0.2000 | 1 | 0 |
| methapyrilene | Homo sapiens (human) | Ki | 0.1060 | 1 | 0 |
| methylphenidate | Homo sapiens (human) | IC50 | 5.1000 | 1 | 1 |
| methylphenidate | Homo sapiens (human) | Ki | 37.5000 | 2 | 2 |
| mianserin | Homo sapiens (human) | IC50 | 2.0680 | 1 | 0 |
| mianserin | Homo sapiens (human) | Ki | 1.0980 | 1 | 0 |
| miconazole | Homo sapiens (human) | IC50 | 0.7780 | 1 | 0 |
| miconazole | Homo sapiens (human) | Ki | 0.4140 | 1 | 0 |
| mitotane | Homo sapiens (human) | IC50 | 3.0150 | 1 | 0 |
| mitotane | Homo sapiens (human) | Ki | 1.6010 | 1 | 0 |
| modafinil | Homo sapiens (human) | Ki | 570.0000 | 1 | 1 |
| nefazodone | Homo sapiens (human) | Ki | 0.2900 | 1 | 1 |
| nisoxetine | Homo sapiens (human) | IC50 | 0.8628 | 6 | 6 |
| nisoxetine | Homo sapiens (human) | Ki | 0.1022 | 2 | 2 |
| nomifensine | Homo sapiens (human) | IC50 | 8.7096 | 1 | 1 |
| nomifensine | Homo sapiens (human) | Ki | 1.5652 | 4 | 4 |
| nortriptyline | Homo sapiens (human) | IC50 | 0.0130 | 1 | 0 |
| nortriptyline | Homo sapiens (human) | Ki | 0.0070 | 1 | 0 |
| orphenadrine | Homo sapiens (human) | IC50 | 0.4580 | 1 | 0 |
| orphenadrine | Homo sapiens (human) | Ki | 0.2430 | 1 | 0 |
| primaquine | Homo sapiens (human) | IC50 | 0.0160 | 1 | 0 |
| primaquine | Homo sapiens (human) | Ki | 0.0084 | 1 | 0 |
| prochlorperazine | Homo sapiens (human) | IC50 | 1.1690 | 1 | 0 |
| prochlorperazine | Homo sapiens (human) | Ki | 0.6210 | 1 | 0 |
| promazine | Homo sapiens (human) | IC50 | 0.0860 | 1 | 0 |
| promazine | Homo sapiens (human) | Ki | 0.0460 | 1 | 0 |
| promethazine | Homo sapiens (human) | IC50 | 5.8000 | 2 | 1 |
| promethazine | Homo sapiens (human) | Ki | 2.1300 | 1 | 0 |
| propranolol | Homo sapiens (human) | IC50 | 0.3800 | 1 | 0 |
| propranolol | Homo sapiens (human) | Ki | 0.2020 | 1 | 0 |
| pyrilamine | Homo sapiens (human) | IC50 | 0.0470 | 1 | 0 |
| pyrilamine | Homo sapiens (human) | Ki | 0.0250 | 1 | 0 |
| quetiapine | Homo sapiens (human) | Ki | 18.0000 | 1 | 1 |
| quipazine | Homo sapiens (human) | Ki | 0.0300 | 1 | 1 |
| 6-nitroquipazine | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
| raloxifene | Homo sapiens (human) | IC50 | 3.5760 | 1 | 0 |
| raloxifene | Homo sapiens (human) | Ki | 1.9000 | 1 | 0 |
| risperidone | Homo sapiens (human) | Ki | 1.4000 | 1 | 1 |
| sibutramine | Homo sapiens (human) | IC50 | 2.0850 | 1 | 0 |
| sibutramine | Homo sapiens (human) | Ki | 1.1080 | 1 | 0 |
| imatinib | Homo sapiens (human) | IC50 | 1.4020 | 1 | 0 |
| imatinib | Homo sapiens (human) | Ki | 0.7450 | 1 | 0 |
| sulconazole | Homo sapiens (human) | IC50 | 0.1410 | 1 | 0 |
| sulconazole | Homo sapiens (human) | Ki | 0.0750 | 1 | 0 |
| thioridazine | Homo sapiens (human) | IC50 | 0.7510 | 1 | 0 |
| thioridazine | Homo sapiens (human) | Ki | 0.3990 | 1 | 0 |
| ultram | Homo sapiens (human) | IC50 | 2.0550 | 3 | 2 |
| ultram | Homo sapiens (human) | Ki | 0.1980 | 1 | 0 |
| trazodone | Homo sapiens (human) | IC50 | 0.1920 | 1 | 0 |
| trazodone | Homo sapiens (human) | Ki | 0.1020 | 1 | 0 |
| venlafaxine | Homo sapiens (human) | IC50 | 0.0578 | 9 | 8 |
| venlafaxine | Homo sapiens (human) | Ki | 0.0417 | 4 | 3 |
| n-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-n-(2-pyridinyl)cyclohexanecarboxamide | Homo sapiens (human) | IC50 | 4.5000 | 1 | 1 |
| estriol | Homo sapiens (human) | IC50 | 10.3360 | 1 | 0 |
| estriol | Homo sapiens (human) | Ki | 5.4910 | 1 | 0 |
| dextroamphetamine | Homo sapiens (human) | IC50 | 16.5959 | 1 | 1 |
| dextroamphetamine | Homo sapiens (human) | Ki | 5.7280 | 1 | 1 |
| estrone | Homo sapiens (human) | IC50 | 5.3010 | 1 | 0 |
| estrone | Homo sapiens (human) | Ki | 2.8160 | 1 | 0 |
| 2-acetylaminofluorene | Homo sapiens (human) | IC50 | 6.0530 | 1 | 0 |
| 2-acetylaminofluorene | Homo sapiens (human) | Ki | 3.2160 | 1 | 0 |
| ethinyl estradiol | Homo sapiens (human) | IC50 | 0.0540 | 1 | 0 |
| ethinyl estradiol | Homo sapiens (human) | Ki | 0.0290 | 1 | 0 |
| norethindrone | Homo sapiens (human) | IC50 | 4.5370 | 1 | 0 |
| norethindrone | Homo sapiens (human) | Ki | 2.4110 | 1 | 0 |
| mestranol | Homo sapiens (human) | IC50 | 0.0410 | 1 | 0 |
| mestranol | Homo sapiens (human) | Ki | 0.0220 | 1 | 0 |
| bisphenol a | Homo sapiens (human) | IC50 | 20.3250 | 1 | 0 |
| bisphenol a | Homo sapiens (human) | Ki | 10.7980 | 1 | 0 |
| benzethonium chloride | Homo sapiens (human) | IC50 | 2.4380 | 1 | 0 |
| benzethonium chloride | Homo sapiens (human) | Ki | 1.2950 | 1 | 0 |
| sterogenol | Homo sapiens (human) | IC50 | 1.6800 | 1 | 0 |
| sterogenol | Homo sapiens (human) | Ki | 0.8920 | 1 | 0 |
| indopan | Homo sapiens (human) | IC50 | 2.3442 | 1 | 1 |
| indopan | Homo sapiens (human) | Ki | 1.0203 | 2 | 3 |
| dibenzepin | Homo sapiens (human) | Ki | 10.9000 | 1 | 1 |
| bufotenin | Homo sapiens (human) | IC50 | 1.2000 | 1 | 1 |
| 1-naphthylisothiocyanate | Homo sapiens (human) | IC50 | 14.2930 | 1 | 0 |
| 1-naphthylisothiocyanate | Homo sapiens (human) | Ki | 7.5930 | 1 | 0 |
| ethylestrenol | Homo sapiens (human) | IC50 | 0.0810 | 1 | 0 |
| ethylestrenol | Homo sapiens (human) | Ki | 0.0430 | 1 | 0 |
| pyrovalerone | Homo sapiens (human) | IC50 | 2.7800 | 1 | 1 |
| pyrovalerone | Homo sapiens (human) | Ki | 3.7700 | 1 | 1 |
| 4-octylphenol | Homo sapiens (human) | IC50 | 6.9730 | 1 | 0 |
| 4-octylphenol | Homo sapiens (human) | Ki | 3.7040 | 1 | 0 |
| n-methyllaurotetanine | Homo sapiens (human) | Ki | 0.9500 | 1 | 1 |
| dexpropranolol | Homo sapiens (human) | IC50 | 0.6120 | 1 | 0 |
| dexpropranolol | Homo sapiens (human) | Ki | 0.3250 | 1 | 0 |
| danazol | Homo sapiens (human) | IC50 | 15.4200 | 1 | 0 |
| danazol | Homo sapiens (human) | Ki | 8.1930 | 1 | 0 |
| metergoline | Homo sapiens (human) | IC50 | 0.5900 | 1 | 0 |
| metergoline | Homo sapiens (human) | Ki | 0.3130 | 1 | 0 |
| dexchlorpheniramine | Homo sapiens (human) | IC50 | 0.0250 | 1 | 0 |
| dexchlorpheniramine | Homo sapiens (human) | Ki | 0.0130 | 1 | 0 |
| penfluridol | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| dobutamine | Homo sapiens (human) | IC50 | 1.8950 | 1 | 0 |
| dobutamine | Homo sapiens (human) | Ki | 1.0060 | 1 | 0 |
| levobunolol | Homo sapiens (human) | IC50 | 4.8980 | 1 | 0 |
| levobunolol | Homo sapiens (human) | Ki | 2.6020 | 1 | 0 |
| 1-methyl-4-phenylpyridinium | Homo sapiens (human) | Ki | 48.0000 | 1 | 1 |
| paroxetine | Homo sapiens (human) | IC50 | 0.0007 | 4 | 3 |
| paroxetine | Homo sapiens (human) | Ki | 0.0002 | 9 | 8 |
| indalpine | Homo sapiens (human) | IC50 | 0.0300 | 1 | 1 |
| bicifadine | Homo sapiens (human) | IC50 | 0.1170 | 1 | 1 |
| atomoxetine | Homo sapiens (human) | IC50 | 0.1434 | 10 | 10 |
| (S)-nomifensine | Homo sapiens (human) | Ki | 1.0675 | 2 | 2 |
| clopidogrel | Homo sapiens (human) | IC50 | 0.5620 | 1 | 0 |
| clopidogrel | Homo sapiens (human) | Ki | 0.2990 | 1 | 0 |
| aripiprazole | Homo sapiens (human) | Ki | 0.6739 | 5 | 5 |
| duloxetine | Homo sapiens (human) | IC50 | 0.0052 | 13 | 13 |
| duloxetine | Homo sapiens (human) | Ki | 0.0027 | 8 | 8 |
| ziprasidone | Homo sapiens (human) | Ki | 0.0662 | 2 | 2 |
| fluoxetine hydrochloride | Homo sapiens (human) | IC50 | 0.1500 | 1 | 1 |
| fluoxetine hydrochloride | Homo sapiens (human) | Ki | 0.0011 | 1 | 1 |
| venlafaxine hydrochloride | Homo sapiens (human) | IC50 | 0.1800 | 8 | 8 |
| litoxetine | Homo sapiens (human) | IC50 | 0.0060 | 2 | 2 |
| milnacipran | Homo sapiens (human) | IC50 | 1.7820 | 2 | 2 |
| milnacipran | Homo sapiens (human) | Ki | 0.0220 | 1 | 1 |
| esreboxetine | Homo sapiens (human) | IC50 | 6.5811 | 2 | 2 |
| esreboxetine | Homo sapiens (human) | Ki | 0.6610 | 1 | 1 |
| n-(3-pyridylmethyl)pyrrolidine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| sertraline | Homo sapiens (human) | IC50 | 0.0016 | 4 | 3 |
| sertraline | Homo sapiens (human) | Ki | 0.0001 | 1 | 0 |
| rivastigmine | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| vanoxerine | Homo sapiens (human) | IC50 | 3.8400 | 2 | 2 |
| gr 127935 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| cubebin | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| mosapride | Homo sapiens (human) | IC50 | 3.8117 | 1 | 0 |
| mosapride | Homo sapiens (human) | Ki | 2.0249 | 1 | 0 |
| desloratadine | Homo sapiens (human) | IC50 | 0.2300 | 1 | 0 |
| desloratadine | Homo sapiens (human) | Ki | 0.1220 | 1 | 0 |
| desvenlafaxine | Homo sapiens (human) | IC50 | 0.0350 | 2 | 2 |
| desvenlafaxine | Homo sapiens (human) | Ki | 0.0150 | 1 | 1 |
| indatraline | Homo sapiens (human) | Ki | 0.0049 | 2 | 2 |
| escitalopram | Homo sapiens (human) | IC50 | 1.5374 | 3 | 3 |
| escitalopram | Homo sapiens (human) | Ki | 1.3154 | 6 | 6 |
| lexapro | Homo sapiens (human) | Ki | 0.0010 | 1 | 1 |
| 4-methylthioamphetamine | Homo sapiens (human) | IC50 | 0.1370 | 2 | 2 |
| 4-methylthioamphetamine | Homo sapiens (human) | Ki | 0.4500 | 1 | 1 |
| 3-(1-methyl-1,2,3,6-tetrahydropyrid-4-yl)indole | Homo sapiens (human) | IC50 | 0.6900 | 1 | 1 |
| lubazodone hydrochloride | Homo sapiens (human) | Ki | 0.0210 | 1 | 1 |
| harmalan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 0.2440 | 1 | 1 |
| mesembrenone | Homo sapiens (human) | Ki | 0.0270 | 1 | 1 |
| estradiol 3-benzoate | Homo sapiens (human) | IC50 | 3.6720 | 1 | 0 |
| estradiol 3-benzoate | Homo sapiens (human) | Ki | 1.9510 | 1 | 0 |
| 1-methyl-6-methoxy-dihydro-beta-carboline | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| hyperforin | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| terconazole | Homo sapiens (human) | IC50 | 11.4560 | 1 | 0 |
| terconazole | Homo sapiens (human) | Ki | 6.0860 | 1 | 0 |
| hinokinin | Homo sapiens (human) | IC50 | 175.0000 | 1 | 1 |
| tibolone | Homo sapiens (human) | IC50 | 0.0907 | 1 | 0 |
| tibolone | Homo sapiens (human) | Ki | 0.0482 | 1 | 0 |
| cocaine | Homo sapiens (human) | IC50 | 0.5442 | 23 | 23 |
| cocaine | Homo sapiens (human) | Ki | 0.3792 | 31 | 34 |
| diethylstilbestrol | Homo sapiens (human) | IC50 | 12.4920 | 1 | 0 |
| diethylstilbestrol | Homo sapiens (human) | Ki | 6.6370 | 1 | 0 |
| tropisetron | Homo sapiens (human) | IC50 | 0.4880 | 1 | 0 |
| tropisetron | Homo sapiens (human) | Ki | 0.2590 | 1 | 0 |
| cocaine hydrochloride | Homo sapiens (human) | Ki | 0.0950 | 2 | 2 |
| (1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Homo sapiens (human) | IC50 | 1.2532 | 1 | 0 |
| (1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Homo sapiens (human) | Ki | 0.6658 | 1 | 0 |
| 3,4,5-trimethoxycinnamic acid | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| flunarizine | Homo sapiens (human) | IC50 | 0.4990 | 1 | 0 |
| flunarizine | Homo sapiens (human) | Ki | 0.2650 | 1 | 0 |
| benztropine | Homo sapiens (human) | IC50 | 24.1000 | 1 | 2 |
| cinnarizine | Homo sapiens (human) | IC50 | 1.0900 | 1 | 0 |
| cinnarizine | Homo sapiens (human) | Ki | 0.5790 | 1 | 0 |
| enclomiphene | Homo sapiens (human) | IC50 | 0.6380 | 1 | 0 |
| enclomiphene | Homo sapiens (human) | Ki | 0.3390 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | IC50 | 2.3340 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | Ki | 1.2400 | 1 | 0 |
| 2-[(2-ethoxyphenoxy)-phenylmethyl]morpholine | Homo sapiens (human) | IC50 | 0.3580 | 6 | 6 |
| 2-[(2-ethoxyphenoxy)-phenylmethyl]morpholine | Homo sapiens (human) | Ki | 0.7345 | 4 | 4 |
| sb-224289 | Homo sapiens (human) | IC50 | 4.7000 | 1 | 1 |
| 3-[bis(4-fluorophenyl)methoxy]-8-methyl-8-azabicyclo[3.2.1]octane | Homo sapiens (human) | Ki | 3.2600 | 1 | 1 |
| bw 723c86 | Homo sapiens (human) | IC50 | 4.7850 | 1 | 0 |
| bw 723c86 | Homo sapiens (human) | Ki | 2.5420 | 1 | 0 |
| ly 367265 | Homo sapiens (human) | Ki | 0.0023 | 2 | 2 |
| harmine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| sphingosine 1-phosphate | Homo sapiens (human) | IC50 | 0.0230 | 1 | 1 |
| fluvoxamine | Homo sapiens (human) | IC50 | 0.0038 | 1 | 1 |
| fluvoxamine | Homo sapiens (human) | Ki | 0.2305 | 2 | 2 |
| oxiconazole | Homo sapiens (human) | IC50 | 0.8001 | 1 | 0 |
| oxiconazole | Homo sapiens (human) | Ki | 0.4251 | 1 | 0 |
| dextromethorphan | Homo sapiens (human) | IC50 | 0.0027 | 1 | 0 |
| dextromethorphan | Homo sapiens (human) | Ki | 0.0014 | 1 | 0 |
| (R)-citalopram | Homo sapiens (human) | IC50 | 0.1700 | 1 | 1 |
| clovoxamine | Homo sapiens (human) | Ki | 0.0610 | 1 | 1 |
| levomilnacipran | Homo sapiens (human) | IC50 | 0.3200 | 2 | 2 |
| vilazodone | Homo sapiens (human) | IC50 | 0.0004 | 3 | 3 |
| vilazodone | Homo sapiens (human) | Ki | 0.0012 | 2 | 2 |
| nps2143 | Homo sapiens (human) | IC50 | 0.0020 | 1 | 1 |
| 2-ethyl-5-methoxy-n,n-dimethyltryptamine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 5-methoxy-2-phenyl-n,n-dimethyltryptamine | Homo sapiens (human) | Ki | 4.7000 | 1 | 1 |
| armodafinil | Homo sapiens (human) | IC50 | 232.0000 | 1 | 1 |
| radafaxine | Homo sapiens (human) | IC50 | 50.1935 | 2 | 2 |
| dov 216303 | Homo sapiens (human) | IC50 | 0.1653 | 5 | 6 |
| dov 216303 | Homo sapiens (human) | Ki | 0.0630 | 1 | 1 |
| n-demethylloperamide | Homo sapiens (human) | Ki | 0.0062 | 1 | 1 |
| o-demethyltramadol | Homo sapiens (human) | IC50 | 7.3000 | 2 | 2 |
| [2-[[2-[(dimethylamino)methyl]phenyl]thio]-5-iodophenyl]methanol | Homo sapiens (human) | Ki | 0.0001 | 3 | 3 |
| fty 720p | Homo sapiens (human) | IC50 | 0.0150 | 1 | 1 |
| 4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| vortioxetine | Homo sapiens (human) | Ki | 0.0016 | 1 | 1 |
| n,n-dimethyl-2-(2-amino-4-methylphenylthio)benzylamine | Homo sapiens (human) | Ki | 0.0013 | 6 | 6 |
| n,n-dimethyl-2-(2-amino-4-fluorophenylthio)benzylamine | Homo sapiens (human) | Ki | 0.0015 | 1 | 1 |
| sb-649915 | Homo sapiens (human) | Ki | 0.0063 | 1 | 1 |
| kaspar | Homo sapiens (human) | IC50 | 0.1120 | 1 | 1 |
| 9-(aminomethyl)-9,10-dihydroanthracene | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 3-amino-4-(2-dimethylaminomethylphenylsulfanyl)benzonitrile | Homo sapiens (human) | Ki | 0.0011 | 3 | 3 |
| 1-phenyl-2-(1-pyrrolidinyl)-1-pentanone | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| naphyrone | Homo sapiens (human) | IC50 | 0.0460 | 1 | 1 |
| naphyrone | Homo sapiens (human) | Ki | 0.0331 | 1 | 1 |
| milnacipran | Homo sapiens (human) | IC50 | 0.7046 | 7 | 7 |
| milnacipran | Homo sapiens (human) | Ki | 0.0065 | 1 | 1 |
| dov 21947 | Homo sapiens (human) | IC50 | 0.2119 | 2 | 2 |
| dov 21947 | Homo sapiens (human) | Ki | 0.0806 | 2 | 2 |
| lorcaserin | Homo sapiens (human) | Ki | 2.6060 | 1 | 1 |
| 2-((2-((dimethylamino)methyl)phenyl)thio)-5-iodophenylamine | Homo sapiens (human) | Ki | 0.1682 | 5 | 5 |
| sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| (1R,3S)-3-(4-iodophenyl)-8-methyl-8-azabicyclo[3.2.1]octane-4-carboxylic acid methyl ester | Homo sapiens (human) | IC50 | 0.0030 | 2 | 3 |
| win 35,065-2 | Homo sapiens (human) | IC50 | 1.9600 | 2 | 2 |
| win 35,065-2 | Homo sapiens (human) | Ki | 0.1780 | 2 | 2 |
| nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | IC50 | 8.7096 | 1 | 1 |
| n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 1.0823 | 3 | 4 |
| clozapine | Homo sapiens (human) | IC50 | 0.5460 | 1 | 0 |
| clozapine | Homo sapiens (human) | Ki | 2.0950 | 2 | 1 |
| olanzapine | Homo sapiens (human) | IC50 | 1.0330 | 1 | 0 |
| olanzapine | Homo sapiens (human) | Ki | 7.7745 | 2 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
Nicotinic acetylcholine receptor efficacy and pharmacological properties of 3-(substituted phenyl)-2β-substituted tropanes.Journal of medicinal chemistry, , Dec-09, Volume: 53, Issue:23, 2010
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
Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for smoking cessation.Journal of medicinal chemistry, , Mar-11, Volume: 53, Issue:5, 2010
Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction.Journal of medicinal chemistry, , Nov-12, Volume: 52, Issue:21, 2009
2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy.Journal of medicinal chemistry, , May-08, Volume: 46, Issue:10, 2003
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
Synthesis and serotonin transporter activity of 1,3-bis(aryl)-2-nitro-1-propenes as a new class of anticancer agents.Bioorganic & medicinal chemistry, , Feb-01, Volume: 19, Issue:3, 2011
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
Ethylenedioxy homologs of N-methyl-(3,4-methylenedioxyphenyl)-2-aminopropane (MDMA) and its corresponding cathinone analog methylenedioxymethcathinone: Interactions with transporters for serotonin, dopamine, and norepinephrine.Bioorganic & medicinal chemistry, , Sep-01, Volume: 23, Issue:17, 2015
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
Synthesis and serotonin transporter activity of 1,3-bis(aryl)-2-nitro-1-propenes as a new class of anticancer agents.Bioorganic & medicinal chemistry, , Feb-01, Volume: 19, Issue:3, 2011
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
Carbon-11 labeled indolylpropylamine analog as a new potential PET agent for imaging of the serotonin transporter.Bioorganic & medicinal chemistry, , Jun-15, Volume: 16, Issue:12, 2008
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
Development of Novel Alkoxyisoxazoles as Sigma-1 Receptor Antagonists with Antinociceptive Efficacy.Journal of medicinal chemistry, , 07-14, Volume: 59, Issue:13, 2016
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 24, Issue:2, 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
[no title available],
Polypharmacology - foe or friend?Journal of medicinal chemistry, , Nov-27, Volume: 56, Issue:22, 2013
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
[no title available],
The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
Tuning the activity of known drugs via the introduction of halogen atoms, a case study of SERT ligands - Fluoxetine and fluvoxamine.European journal of medicinal chemistry, , Aug-05, Volume: 220, 2021
Synthesis, in vitro evaluation and molecular docking of a new class of indolylpropyl benzamidopiperazines as dual AChE and SERT ligands for Alzheimer's disease.European journal of medicinal chemistry, , Jul-15, Volume: 198, 2020
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics.Bioorganic & medicinal chemistry letters, , 04-15, Volume: 30, Issue:8, 2020
Design, synthesis and evaluation of vilazodone-tacrine hybrids as multitarget-directed ligands against depression with cognitive impairment.Bioorganic & medicinal chemistry, , 07-23, Volume: 26, Issue:12, 2018
X-ray structure based evaluation of analogs of citalopram: Compounds with increased affinity and selectivity compared with R-citalopram for the allosteric site (S2) on hSERT.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 27, Issue:3, 2017
Design and synthesis of 1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile (citalopram) analogues as novel probes for the serotonin transporter S1 and S2 binding sites.Journal of medicinal chemistry, , Dec-12, Volume: 56, Issue:23, 2013
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
Synthesis and serotonin transporter activity of 1,3-bis(aryl)-2-nitro-1-propenes as a new class of anticancer agents.Bioorganic & medicinal chemistry, , Feb-01, Volume: 19, Issue:3, 2011
3-(4-(6-Fluoroalkoxy-3,4-dihydroisoquinoline-2(1H)-yl)cyclohexyl)-1H-indole-5-carbonitriles for SERT imaging: chemical synthesis, evaluation in vitro and radiofluorination.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 18, Issue:16, 2008
Carbon-11 labeled indolylpropylamine analog as a new potential PET agent for imaging of the serotonin transporter.Bioorganic & medicinal chemistry, , Jun-15, Volume: 16, Issue:12, 2008
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
[no title available],
Reengineered tricyclic anti-cancer agents.Bioorganic & medicinal chemistry, , Oct-01, Volume: 23, Issue:19, 2015
3-(4-Piperidinylalkyl)indoles, selective inhibitors of neuronal 5-hydroxytryptamine uptake.Journal of medicinal chemistry, , Volume: 23, Issue:12, 1980
[no title available],
Basic N-interlinked imipramines show apoptotic activity against malignant cells including Burkitt's lymphoma.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 23, Issue:5, 2013
Diaryldiamines with dual inhibition of the histamine H(3) receptor and the norepinephrine transporter and the efficacy of 4-(3-(methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in pain.Journal of medicinal chemistry, , Nov-11, Volume: 53, Issue:21, 2010
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:11, 2007
LeuT-desipramine structure reveals how antidepressants block neurotransmitter reuptake.Science (New York, N.Y.), , Sep-07, Volume: 317, Issue:5843, 2007
Tuning the activity of known drugs via the introduction of halogen atoms, a case study of SERT ligands - Fluoxetine and fluvoxamine.European journal of medicinal chemistry, , Aug-05, Volume: 220, 2021
Evaluation of anti-depressant effects of phthalazinone-based triple-acting small molecules against 5-HTBioorganic & medicinal chemistry letters, , 02-15, Volume: 30, Issue:4, 2020
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
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
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 23, 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
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
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
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
NO-SSRIs: Nitric Oxide Chimera Drugs Incorporating a Selective Serotonin Reuptake Inhibitor.ACS medicinal chemistry letters, , Sep-08, Volume: 2, Issue:9, 2011
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
1-(Indolin-1-yl)-1-phenyl-3-propan-2-olamines as potent and selective norepinephrine reuptake inhibitors.Journal of medicinal chemistry, , Mar-11, Volume: 53, Issue:5, 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
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
Synthesis and hSERT activity of homotryptamine analogs. Part 6: [3+2] dipolar cycloaddition of 3-vinylindoles.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 20, Issue:3, 2010
Heterocyclic cycloalkanol ethylamines as norepinephrine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 20, Issue:9, 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
Dual inhibitors of phosphodiesterase-4 and serotonin reuptake.Journal of medicinal chemistry, , Mar-26, Volume: 52, Issue:6, 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
Structure-activity relationships of the 1-amino-3-(1H-indol-1-yl)-3-phenylpropan-2-ol series of monoamine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 19, Issue:19, 2009
Discovery of a new series of monoamine reuptake inhibitors, the 1-amino-3-(1H-indol-1-yl)-3-phenylpropan-2-ols.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 19, Issue:17, 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 activity of 1-(3-amino-1-phenylpropyl)indolin-2-ones: a new class of selective norepinephrine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 18, Issue:18, 2008
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
Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI).Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 18, Issue:14, 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
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
Advances toward new antidepressants with dual serotonin transporter and 5-HT1A receptor affinity within a class of 3-aminochroman derivatives. Part 2.Journal of medicinal chemistry, , Nov-13, Volume: 51, Issue:21, 2008
Multi-target-directed ligands to combat neurodegenerative diseases.Journal of medicinal chemistry, , Feb-14, Volume: 51, Issue:3, 2008
Dual serotonin transporter/histamine H3 ligands: Optimization of the H3 pharmacophore.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 17, Issue:3, 2007
Benzylamine histamine H(3) antagonists and serotonin reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 17, Issue:17, 2007
Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 17, Issue:4, 2007
Novel naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 17, Issue:9, 2007
Synthesis and biological evaluation of novel compounds within a class of 3-aminochroman derivatives with dual 5-HT1A receptor and serotonin transporter affinity.Journal of medicinal chemistry, , Jul-27, Volume: 49, Issue:15, 2006
Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
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
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
Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines.Journal of medicinal chemistry, , Jul-15, Volume: 47, Issue:15, 2004
2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.Journal of medicinal chemistry, , Mar-09, Volume: 43, Issue:5, 2000
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],
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 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
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
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
Design and synthesis of a biotinylated dopamine transporter ligand for the purification and labeling of dopaminergic neurons.Bioorganic & medicinal chemistry letters, , Feb-03, Volume: 8, Issue:3, 1998
Further evaluation of the tropane analogs of haloperidol.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 24, Issue:17, 2014
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
[no title available],
Synthesis, crystal structure and biological activity of novel analogues of tricyclic drugs.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 30, Issue:21, 2020
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
[no title available]European journal of medicinal chemistry, , Aug-15, Volume: 176, 2019
[no title available]European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Novel 3-(1,2,3,6-Tetrahydropyridin-4-yl)-1H-indole-Based Multifunctional Ligands with Antipsychotic-Like, Mood-Modulating, and Procognitive Activity.Journal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Discovery of SMP-304, a novel benzylpiperidine derivative with serotonin transporter inhibitory activity and 5-HTBioorganic & medicinal chemistry, , 01-01, Volume: 25, 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 inhibitory evaluation of 3-linked imipramines for the exploration of the S2 site of the human serotonin transporter.Bioorganic & medicinal chemistry, , 06-15, Volume: 24, Issue:12, 2016
Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.European journal of medicinal chemistry, , Mar-06, Volume: 92, 2015
Novel arylsulfonamide derivatives with 5-HT₆/5-HT₇ receptor antagonism targeting behavioral and psychological symptoms of dementia.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Polypharmacology - foe or friend?Journal of medicinal chemistry, , Nov-27, Volume: 56, Issue:22, 2013
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
Basic N-interlinked imipramines show apoptotic activity against malignant cells including Burkitt's lymphoma.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 23, Issue:5, 2013
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
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
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
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
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:11, 2007
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Structural determinants for high 5-HT(2A) receptor affinity of spiro[9,10-dihydroanthracene]-9,3(')-pyrrolidine (SpAMDA).Bioorganic & medicinal chemistry letters, , May-03, Volume: 14, Issue:9, 2004
The role of receptor binding in drug discovery.Journal of natural products, , Volume: 56, Issue:4, 1993
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
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
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
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
Design and synthesis of novel arylpiperazine derivatives containing the imidazole core targeting 5-HT(2A) receptor and 5-HT transporter.Journal of medicinal chemistry, , Sep-22, Volume: 54, Issue:18, 2011
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
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 activity of 1-(3-amino-1-phenylpropyl)indolin-2-ones: a new class of selective norepinephrine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 18, Issue:18, 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
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
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
Azepines and piperidines with dual norepinephrine dopamine uptake inhibition and antidepressant activity.ACS medicinal chemistry letters, , Jan-10, Volume: 4, Issue:1, 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
4-Phenyl tetrahydroisoquinolines as dual norepinephrine and dopamine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
In vitro and in vivo evaluation of O-alkyl derivatives of tramadol.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 18, Issue:5, 2008
Derivatives of tramadol for increased duration of effect.Bioorganic & medicinal chemistry letters, , Volume: 16, Issue:3, 2006
[no title available],
Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds.Journal of medicinal chemistry, , 05-10, Volume: 61, Issue:9, 2018
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
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
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
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],
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
Tuning the activity of known drugs via the introduction of halogen atoms, a case study of SERT ligands - Fluoxetine and fluvoxamine.European journal of medicinal chemistry, , Aug-05, Volume: 220, 2021
Discovery of SMP-304, a novel benzylpiperidine derivative with serotonin transporter inhibitory activity and 5-HTBioorganic & medicinal chemistry, , 01-01, Volume: 25, Issue:1, 2017
Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists-serotonin reuptake transporter inhibitors for the treatment of depression.Bioorganic & medicinal chemistry, , Apr-15, Volume: 21, Issue:8, 2013
Synthesis and activity of 1-(3-amino-1-phenylpropyl)indolin-2-ones: a new class of selective norepinephrine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 18, Issue:18, 2008
3-(4-(6-Fluoroalkoxy-3,4-dihydroisoquinoline-2(1H)-yl)cyclohexyl)-1H-indole-5-carbonitriles for SERT imaging: chemical synthesis, evaluation in vitro and radiofluorination.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 18, Issue:16, 2008
Carbon-11 labeled indolylpropylamine analog as a new potential PET agent for imaging of the serotonin transporter.Bioorganic & medicinal chemistry, , Jun-15, Volume: 16, Issue:12, 2008
1-Aminocyclopentane-1,2,4-tricarboxylic acids screening on glutamatergic and serotonergic systems.Bioorganic & medicinal chemistry, , Dec-15, Volume: 15, Issue:24, 2007
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
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
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 activity of 1-(3-amino-1-phenylpropyl)indolin-2-ones: a new class of selective norepinephrine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 18, Issue:18, 2008
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
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
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
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
New dual 5-HT1A and 5-HT7 receptor ligands derived from SYA16263.European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
A study of the structure-affinity relationship in SYA16263; is a DBioorganic & medicinal chemistry, , 01-15, Volume: 30, 2021
Design and synthesis of dual 5-HT1A and 5-HT7 receptor ligands.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
Design and synthesis of novel arylpiperazine derivatives containing the imidazole core targeting 5-HT(2A) receptor and 5-HT transporter.Journal of medicinal chemistry, , Sep-22, Volume: 54, Issue:18, 2011
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
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
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
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
Novel, achiral aminoheterocycles as selective monoamine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 19, Issue:16, 2009
Synthesis and activity of 1-(3-amino-1-phenylpropyl)indolin-2-ones: a new class of selective norepinephrine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 18, Issue:18, 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
Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 18, Issue:4, 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
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
Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
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
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
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
Design, synthesis, and systematic evaluation of 4-arylpiperazine- and 4-benzylpiperidine napthyl ethers as inhibitors of monoamine neurotransmitters reuptake.Bioorganic & medicinal chemistry, , 11-01, Volume: 26, Issue:20, 2018
Design, synthesis and docking study of 4-arylpiperazine carboxamides as monoamine neurotransmitters reuptake inhibitors.Bioorganic & medicinal chemistry, , 08-07, Volume: 26, Issue:14, 2018
Triple reuptake inhibitors: Design, synthesis and structure-activity relationship of benzylpiperidine-tetrazoles.Bioorganic & medicinal chemistry, , 10-15, Volume: 25, Issue:20, 2017
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
Design, synthesis, and biological evaluation of arylpiperazine-benzylpiperidines with dual serotonin and norepinephrine reuptake inhibitory activities.Bioorganic & medicinal chemistry, , May-01, Volume: 24, Issue:9, 2016
Exploration of substituted arylpiperazine-tetrazoles as promising dual norepinephrine and dopamine reuptake inhibitors.Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Design and synthesis of 4-benzylpiperidine carboxamides as dual serotonin and norepinephrine reuptake inhibitors.Bioorganic & medicinal chemistry, , Oct-01, Volume: 23, Issue:19, 2015
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 optimisation of selective serotonin re-uptake inhibitors with high synthetic accessibility: part 2.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 19, Issue:20, 2009
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
Discovery of SMP-304, a novel benzylpiperidine derivative with serotonin transporter inhibitory activity and 5-HTBioorganic & medicinal chemistry, , 01-01, Volume: 25, Issue:1, 2017
Identification of 1S,2R-milnacipran analogs as potent norepinephrine and serotonin transporter inhibitors.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 18, Issue:11, 2008
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
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
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
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
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
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
Exploration of novel 3-substituted azetidine derivatives as triple reuptake inhibitors.Journal of medicinal chemistry, , Sep-27, Volume: 55, Issue:18, 2012
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 a potent, dual serotonin and norepinephrine reuptake inhibitor.ACS medicinal chemistry letters, , Jun-13, Volume: 4, Issue:6, 2013
Clickable photoaffinity ligands for the human serotonin transporter based on the selective serotonin reuptake inhibitor (S)-citalopram.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 28, Issue:21, 2018
X-ray structure based evaluation of analogs of citalopram: Compounds with increased affinity and selectivity compared with R-citalopram for the allosteric site (S2) on hSERT.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 27, Issue:3, 2017
Novel Azido-Iodo Photoaffinity Ligands for the Human Serotonin Transporter Based on the Selective Serotonin Reuptake Inhibitor (S)-Citalopram.Journal of medicinal chemistry, , Jul-23, Volume: 58, Issue:14, 2015
Novel and high affinity fluorescent ligands for the serotonin transporter based on (s)-citalopram.ACS medicinal chemistry letters, , Jun-12, Volume: 5, Issue:6, 2014
Design and synthesis of 1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile (citalopram) analogues as novel probes for the serotonin transporter S1 and S2 binding sites.Journal of medicinal chemistry, , Dec-12, Volume: 56, Issue:23, 2013
Potent dihydroquinolinone dopamine D2 partial agonist/serotonin reuptake inhibitors for the treatment of schizophrenia.Bioorganic & medicinal chemistry letters, , May-01, Volume: 20, Issue:9, 2010
Tetrahydrocarbazole-based serotonin reuptake inhibitor/dopamine D2 partial agonists for the potential treatment of schizophrenia.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 19, Issue:19, 2009
Synthesis and serotonin transporter activity of 1,3-bis(aryl)-2-nitro-1-propenes as a new class of anticancer agents.Bioorganic & medicinal chemistry, , Feb-01, Volume: 19, Issue:3, 2011
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
Synthesis and Discovery of Arylpiperidinylquinazolines: New Inhibitors of the Vesicular Monoamine Transporter.Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
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
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
2,5-Disubstituted tetrahydrofurans as selective serotonin re-uptake inhibitors.Bioorganic & medicinal chemistry, , Mar-01, Volume: 17, Issue:5, 2009
Dual inhibitors of phosphodiesterase-4 and serotonin reuptake.Journal of medicinal chemistry, , Mar-26, Volume: 52, Issue:6, 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 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
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 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
Synthesis, inhibition and binding of simple non-nitrogen inhibitors of monoamine transporters.Bioorganic & medicinal chemistry, , Jun-15, Volume: 15, Issue:12, 2007
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
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
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:11, 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
Synthesis and monoamine transporter binding properties of 2,3-diaryltropanes.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 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
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
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 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
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
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
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
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
1-(Indolin-1-yl)-1-phenyl-3-propan-2-olamines as potent and selective norepinephrine reuptake inhibitors.Journal of medicinal chemistry, , Mar-11, Volume: 53, Issue:5, 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 1-(3-amino-1-phenylpropyl)indolin-2-ones: a new class of selective norepinephrine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 18, Issue:18, 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
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
[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
Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
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
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
Design and synthesis of novel arylpiperazine derivatives containing the imidazole core targeting 5-HT(2A) receptor and 5-HT transporter.Journal of medicinal chemistry, , Sep-22, Volume: 54, Issue:18, 2011
Arylpiperazine-containing pyrrole 3-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 20, Issue:5, 2010
Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 14, Issue:12, 2004
Synthesis of para-alkyl aryl amide analogues of sphingosine-1-phosphate: discovery of potent S1P receptor agonists.Bioorganic & medicinal chemistry letters, , Oct-20, Volume: 13, Issue:20, 2003
Tuning the activity of known drugs via the introduction of halogen atoms, a case study of SERT ligands - Fluoxetine and fluvoxamine.European journal of medicinal chemistry, , Aug-05, Volume: 220, 2021
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
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
Identification of 1S,2R-milnacipran analogs as potent norepinephrine and serotonin transporter inhibitors.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 18, Issue:11, 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
The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
Discovery of novel dual RAGE/SERT inhibitors for the potential treatment of the comorbidity of Alzheimer's disease and depression.European journal of medicinal chemistry, , Jun-05, Volume: 236, 2022
[no title available]European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Design, synthesis and evaluation of vilazodone-tacrine hybrids as multitarget-directed ligands against depression with cognitive impairment.Bioorganic & medicinal chemistry, , 07-23, Volume: 26, Issue:12, 2018
Benzothiazoles as probes for the 5HT1A receptor and the serotonin transporter (SERT): a search for new dual-acting agents as potential antidepressants.European journal of medicinal chemistry, , Volume: 53, 2012
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
A new single-photon emission computed tomography (SPECT) imaging agent for serotonin transporters: [(125)I]Flip-IDAM, (2-((2-((dimethylamino)methyl)-4-iodophenyl)thio)phenyl)methanol.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 23, Issue:3, 2013
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
Synthesis and in vitro evaluation of fluorinated diphenyloxide derivatives and sulfur analogs as serotonin transporter ligands.Bioorganic & medicinal chemistry, , Jan-01, Volume: 18, Issue:1, 2010
3-(4-(6-Fluoroalkoxy-3,4-dihydroisoquinoline-2(1H)-yl)cyclohexyl)-1H-indole-5-carbonitriles for SERT imaging: chemical synthesis, evaluation in vitro and radiofluorination.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 18, Issue:16, 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
Identification of 1S,2R-milnacipran analogs as potent norepinephrine and serotonin transporter inhibitors.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 18, Issue:11, 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
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
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
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
A new single-photon emission computed tomography (SPECT) imaging agent for serotonin transporters: [(125)I]Flip-IDAM, (2-((2-((dimethylamino)methyl)-4-iodophenyl)thio)phenyl)methanol.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 23, Issue:3, 2013
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
New PET imaging agent for the serotonin transporter: [(18)F]ACF (2-[(2-amino-4-chloro-5-fluorophenyl)thio]-N,N-dimethyl-benzenmethanamine).Journal of medicinal chemistry, , Oct-10, Volume: 45, Issue:21, 2002
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 14 target(s):
| Target | Category | Definition |
|---|
| integrin binding | molecular function | Binding to an integrin. [GOC:ceb] |
| monoatomic cation channel activity | molecular function | Enables the energy-independent passage of monoatomic cations across a lipid bilayer down a concentration gradient. [GOC:def, GOC:dph, GOC:mtg_transport, GOC:pr, ISBN:0815340729] |
| 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] |
| serotonin:sodium:chloride 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: serotonin(out) + Na+(out) + Cl-(out) = serotonin(in) + Na+(in)+ Cl-(in). [PMID:21752877, PMID:22519513] |
| 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] |
| antiporter activity | molecular function | Enables the active transport of a solute across a membrane by a mechanism whereby two or more species are transported in opposite directions in a tightly coupled process not directly linked to a form of energy other than chemiosmotic energy. The reaction is: solute A(out) + solute B(in) = solute A(in) + solute B(out). [GOC:mtg_transport, ISBN:0815340729, PMID:10839820] |
| syntaxin-1 binding | molecular function | Binding to a syntaxin-1 SNAP receptor. [GOC:ai] |
| cocaine binding | molecular function | Binding to cocaine (2-beta-carbomethoxy-3-beta-benzoxytropane), an alkaloid obtained from dried leaves of the South American shrub Erythroxylon coca or by chemical synthesis. [GOC:jl, ISBN:0198506732] |
| sodium ion binding | molecular function | Binding to a sodium ion (Na+). [GOC:mah] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| nitric-oxide synthase binding | molecular function | Binding to nitric-oxide synthase. [GOC:ai] |
| actin filament binding | molecular function | Binding to an actin filament, also known as F-actin, a helical filamentous polymer of globular G-actin subunits. [ISBN:0198506732] |
| serotonin binding | molecular function | Binding to serotonin (5-hydroxytryptamine), a monoamine neurotransmitter occurring in the peripheral and central nervous systems, also having hormonal properties. [GOC:ai] |
Located In
This protein is located in 9 target(s):
| Target | Category | Definition |
|---|
| 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] |
| focal adhesion | cellular component | A cell-substrate junction that anchors the cell to the extracellular matrix and that forms a point of termination of actin filaments. In insects focal adhesion has also been referred to as hemi-adherens junction (HAJ). [GOC:aruk, GOC:bc, ISBN:0124325653, ISBN:0815316208, PMID:10419689, PMID:12191915, PMID:15246682, PMID:1643657, PMID:16805308, PMID:19197329, PMID:23033047, PMID:26923917, PMID:28796323, PMID:8314002] |
| endosome membrane | cellular component | The lipid bilayer surrounding an endosome. [GOC:mah] |
| endomembrane system | cellular component | A collection of membranous structures involved in transport within the cell. The main components of the endomembrane system are endoplasmic reticulum, Golgi bodies, vesicles, cell membrane and nuclear envelope. Members of the endomembrane system pass materials through each other or though the use of vesicles. [GOC:lh] |
| 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] |
| 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] |
| synapse | cellular component | The junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110] |
| 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] |
| serotonergic synapse | cellular component | A synapse that uses serotonin as a neurotransmitter. [GOC:dos] |
Active In
This protein is active in 3 target(s):
| Target | Category | Definition |
|---|
| synapse | cellular component | The junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110] |
| 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] |
| 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/] |
Involved In
This protein is involved in 30 target(s):
| Target | Category | Definition |
|---|
| response to hypoxia | 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 indicating lowered oxygen tension. Hypoxia, defined as a decline in O2 levels below normoxic levels of 20.8 - 20.95%, results in metabolic adaptation at both the cellular and organismal level. [GOC:hjd] |
| 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] |
| response to nutrient | 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 nutrient stimulus. [GOC:go_curators] |
| memory | biological process | The activities involved in the mental information processing system that receives (registers), modifies, stores, and retrieves informational stimuli. The main stages involved in the formation and retrieval of memory are encoding (processing of received information by acquisition), storage (building a permanent record of received information as a result of consolidation) and retrieval (calling back the stored information and use it in a suitable way to execute a given task). [GOC:curators, ISBN:0582227089] |
| circadian rhythm | biological process | Any biological process in an organism that recurs with a regularity of approximately 24 hours. [GOC:bf, GOC:go_curators] |
| 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 toxic substance | 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 toxic stimulus. [GOC:lr] |
| positive regulation of gene expression | biological process | Any process that increases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
| positive regulation of serotonin secretion | biological process | Any process that activates or increases the frequency, rate or extent of the regulated release of serotonin. [GOC:ef] |
| negative regulation of cerebellar granule cell precursor proliferation | biological process | The process that stops, prevents or reduces the rate or extent of granule cell precursor proliferation. [GO_REF:0000021, GOC:cls, GOC:dgh, GOC:dph, GOC:jid, PMID:15157725] |
| negative regulation of synaptic transmission, dopaminergic | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of dopaminergic synaptic transmission, the process of communication from a neuron to another neuron across a synapse using the neurotransmitter dopamine. [GOC:mah] |
| response to estradiol | 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 stimulus by estradiol, a C18 steroid hormone hydroxylated at C3 and C17 that acts as a potent estrogen. [GOC:mah, ISBN:0911910123] |
| social behavior | biological process | Behavior directed towards society, or taking place between members of the same species. Occurs predominantly, or only, in individuals that are part of a group. [GOC:jh2, PMID:12848939, Wikipedia:Social_behavior] |
| vasoconstriction | biological process | A decrease in the diameter of blood vessels, especially arteries, due to constriction of smooth muscle cells that line the vessels, and usually causing an increase in blood pressure. [GOC:pr, ISBN:0192800752] |
| sperm ejaculation | biological process | The expulsion of seminal fluid, thick white fluid containing spermatozoa, from the male genital tract. [GOC:jl, http://www.cogsci.princeton.edu/~wn/] |
| negative regulation of neuron differentiation | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of neuron differentiation. [GOC:go_curators] |
| positive regulation of cell cycle | biological process | Any process that activates or increases the rate or extent of progression through the cell cycle. [GOC:go_curators] |
| negative regulation of organ growth | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of growth of an organ of an organism. [GOC:bf, GOC:tb] |
| behavioral response to cocaine | biological process | Any process that results in a change in the behavior of an organism as a result of a cocaine stimulus. [GOC:jid] |
| enteric nervous system development | biological process | The process whose specific outcome is the progression of the enteric nervous system over time, from its formation to the mature structure. The enteric nervous system is composed of two ganglionated neural plexuses in the gut wall which form one of the three major divisions of the autonomic nervous system. The enteric nervous system innervates the gastrointestinal tract, the pancreas, and the gallbladder. It contains sensory neurons, interneurons, and motor neurons. Thus the circuitry can autonomously sense the tension and the chemical environment in the gut and regulate blood vessel tone, motility, secretions, and fluid transport. The system is itself governed by the central nervous system and receives both parasympathetic and sympathetic innervation. [FMA:66070, GOC:jid, GOC:sr] |
| brain morphogenesis | biological process | The process in which the anatomical structures of the brain are generated and organized. The brain is one of the two components of the central nervous system and is the center of thought and emotion. It is responsible for the coordination and control of bodily activities and the interpretation of information from the senses (sight, hearing, smell, etc.). [GOC:dgh, GOC:jid] |
| serotonin uptake | biological process | The directed movement of serotonin into a cell, typically presynaptic neurons or glial cells. Serotonin (5-hydroxytryptamine) is a monoamine neurotransmitter occurring in the peripheral and central nervous systems. [GOC:ai] |
| membrane depolarization | biological process | The process in which membrane potential decreases with respect to its steady-state potential, usually from negative potential to a more positive potential. For example, the initial depolarization during the rising phase of an action potential is in the direction from the negative steady-state resting potential towards the positive membrane potential that will be the peak of the action potential. [GOC:dh, Wikipedia:Depolarization] |
| platelet aggregation | biological process | The adhesion of one platelet to one or more other platelets via adhesion molecules. [GOC:BHF, GOC:vk] |
| cellular response to retinoic acid | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a retinoic acid stimulus. [GOC:mah] |
| cellular response to cGMP | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cGMP (cyclic GMP, guanosine 3',5'-cyclophosphate) stimulus. [GOC:mah] |
| regulation of thalamus size | biological process | Any process that modulates the size of the thalamus. The thalamus is a part of the diencephalon that is composed of the dorsal thalamus and the ventral thalamus. [GOC:dph, GOC:tb] |
| conditioned place preference | biological process | The associative learning process by which an animal learns and remembers an association between a neutral, unchanging environment and a putatively rewarding, internal state produced by a xenobiotic or drug. [PMID:21549821] |
| 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] |
| 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] |