Proteins > Sodium-dependent noradrenaline transporter
Page last updated: 2024-08-07 16:15:17
Sodium-dependent noradrenaline transporter
A sodium-dependent noradrenaline transporter that is encoded in the genome of human. [PRO:DNx, UniProtKB:P23975]
Synonyms
Norepinephrine transporter;
NET;
Solute carrier family 6 member 2
Research
Bioassay Publications (172)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 1 (0.58) | 18.7374 |
| 1990's | 6 (3.49) | 18.2507 |
| 2000's | 90 (52.33) | 29.6817 |
| 2010's | 70 (40.70) | 24.3611 |
| 2020's | 5 (2.91) | 2.80 |
Compounds (306)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| quinacrine | Homo sapiens (human) | IC50 | 2.8960 | 1 | 0 |
| quinacrine | Homo sapiens (human) | Ki | 2.8720 | 1 | 0 |
| bupropion | Homo sapiens (human) | IC50 | 2.2003 | 10 | 10 |
| bupropion | Homo sapiens (human) | Ki | 6.9700 | 1 | 1 |
| 3,4-methylenedioxyamphetamine | Homo sapiens (human) | IC50 | 1.2314 | 3 | 3 |
| 3,4-methylenedioxyamphetamine | Homo sapiens (human) | Ki | 0.7040 | 1 | 1 |
| n-methyl-3,4-methylenedioxyamphetamine | Homo sapiens (human) | IC50 | 0.9351 | 3 | 3 |
| n-methyl-3,4-methylenedioxyamphetamine | Homo sapiens (human) | Ki | 0.3980 | 1 | 1 |
| 3-methylcholanthrene | Homo sapiens (human) | IC50 | 29.6500 | 1 | 0 |
| 3-methylcholanthrene | Homo sapiens (human) | Ki | 29.4050 | 1 | 0 |
| 4-nonylphenol | Homo sapiens (human) | IC50 | 1.2540 | 1 | 0 |
| 4-nonylphenol | Homo sapiens (human) | Ki | 1.2440 | 1 | 0 |
| tacrine | Homo sapiens (human) | IC50 | 0.5170 | 1 | 0 |
| tacrine | Homo sapiens (human) | Ki | 0.5130 | 1 | 0 |
| amiodarone | Homo sapiens (human) | IC50 | 2.2710 | 1 | 0 |
| amiodarone | Homo sapiens (human) | Ki | 2.2520 | 1 | 0 |
| amitriptyline | Homo sapiens (human) | IC50 | 1.0324 | 2 | 1 |
| amitriptyline | Homo sapiens (human) | Ki | 0.1775 | 2 | 1 |
| amoxapine | Homo sapiens (human) | IC50 | 0.0130 | 1 | 0 |
| amoxapine | Homo sapiens (human) | Ki | 0.0130 | 1 | 0 |
| astemizole | Homo sapiens (human) | IC50 | 1.3750 | 1 | 0 |
| astemizole | Homo sapiens (human) | Ki | 1.3640 | 1 | 0 |
| bithionol | Homo sapiens (human) | IC50 | 1.2350 | 1 | 0 |
| bithionol | Homo sapiens (human) | Ki | 1.2250 | 1 | 0 |
| butenafine | Homo sapiens (human) | IC50 | 3.9099 | 1 | 0 |
| butenafine | Homo sapiens (human) | Ki | 3.8775 | 1 | 0 |
| candesartan | Homo sapiens (human) | IC50 | 3.0652 | 1 | 0 |
| candesartan | Homo sapiens (human) | Ki | 3.0398 | 1 | 0 |
| carvedilol | Homo sapiens (human) | IC50 | 0.5380 | 1 | 0 |
| carvedilol | Homo sapiens (human) | Ki | 0.5330 | 1 | 0 |
| celecoxib | Homo sapiens (human) | IC50 | 7.3080 | 1 | 0 |
| celecoxib | Homo sapiens (human) | Ki | 7.2470 | 1 | 0 |
| chlorpromazine | Homo sapiens (human) | IC50 | 0.0190 | 1 | 0 |
| chlorpromazine | Homo sapiens (human) | Ki | 0.0190 | 1 | 0 |
| ciglitazone | Homo sapiens (human) | IC50 | 2.2200 | 1 | 0 |
| ciglitazone | Homo sapiens (human) | Ki | 2.2010 | 1 | 0 |
| citalopram | Homo sapiens (human) | IC50 | 2.1960 | 1 | 0 |
| citalopram | Homo sapiens (human) | Ki | 336.1227 | 3 | 2 |
| clomipramine | Homo sapiens (human) | IC50 | 0.0678 | 2 | 1 |
| clomipramine | Homo sapiens (human) | Ki | 0.0700 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | IC50 | 7.9360 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | Ki | 7.8700 | 1 | 0 |
| cyproheptadine | Homo sapiens (human) | IC50 | 0.5640 | 1 | 0 |
| cyproheptadine | Homo sapiens (human) | Ki | 0.4245 | 2 | 1 |
| desipramine | Homo sapiens (human) | IC50 | 0.0031 | 16 | 16 |
| desipramine | Homo sapiens (human) | Ki | 0.0405 | 14 | 15 |
| diphenhydramine | Homo sapiens (human) | IC50 | 3.5420 | 1 | 0 |
| diphenhydramine | Homo sapiens (human) | Ki | 3.5130 | 1 | 0 |
| disulfiram | Homo sapiens (human) | IC50 | 70.3700 | 1 | 0 |
| disulfiram | Homo sapiens (human) | Ki | 69.8120 | 1 | 0 |
| p-chloroamphetamine | Homo sapiens (human) | IC50 | 0.2070 | 1 | 1 |
| domperidone | Homo sapiens (human) | IC50 | 2.6140 | 1 | 0 |
| domperidone | Homo sapiens (human) | Ki | 2.5930 | 1 | 0 |
| doxepin | Homo sapiens (human) | IC50 | 0.0290 | 1 | 0 |
| doxepin | Homo sapiens (human) | Ki | 0.0290 | 1 | 0 |
| ebastine | Homo sapiens (human) | IC50 | 0.4603 | 1 | 0 |
| ebastine | Homo sapiens (human) | Ki | 0.4564 | 1 | 0 |
| econazole | Homo sapiens (human) | IC50 | 2.4350 | 1 | 0 |
| econazole | Homo sapiens (human) | Ki | 2.4150 | 1 | 0 |
| fenofibrate | Homo sapiens (human) | IC50 | 21.4080 | 1 | 0 |
| fenofibrate | Homo sapiens (human) | Ki | 21.2310 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | IC50 | 1.9620 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | Ki | 1.9460 | 1 | 0 |
| fluoxetine | Homo sapiens (human) | IC50 | 2.8332 | 12 | 11 |
| fluoxetine | Homo sapiens (human) | Ki | 1.4009 | 7 | 6 |
| vanoxerine | Homo sapiens (human) | IC50 | 0.5098 | 5 | 4 |
| gbr 12935 | Homo sapiens (human) | IC50 | 0.7130 | 2 | 2 |
| gbr 12935 | Homo sapiens (human) | Ki | 0.6300 | 1 | 1 |
| haloperidol | Homo sapiens (human) | IC50 | 1.8360 | 1 | 0 |
| haloperidol | Homo sapiens (human) | Ki | 3.6600 | 2 | 1 |
| haloprogin | Homo sapiens (human) | IC50 | 2.7700 | 1 | 0 |
| haloprogin | Homo sapiens (human) | Ki | 2.7470 | 1 | 0 |
| imipramine | Homo sapiens (human) | IC50 | 0.0740 | 1 | 1 |
| imipramine | Homo sapiens (human) | Ki | 0.0160 | 1 | 1 |
| ipriflavone | Homo sapiens (human) | IC50 | 2.5125 | 1 | 0 |
| ipriflavone | Homo sapiens (human) | Ki | 2.4917 | 1 | 0 |
| ketanserin | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| ketoconazole | Homo sapiens (human) | IC50 | 24.2030 | 1 | 0 |
| ketoconazole | Homo sapiens (human) | Ki | 24.0030 | 1 | 0 |
| labetalol | Homo sapiens (human) | IC50 | 3.3540 | 1 | 0 |
| labetalol | Homo sapiens (human) | Ki | 3.3260 | 1 | 0 |
| leflunomide | Homo sapiens (human) | IC50 | 4.6300 | 1 | 0 |
| leflunomide | Homo sapiens (human) | Ki | 4.5910 | 1 | 0 |
| maprotiline | Homo sapiens (human) | IC50 | 0.0300 | 1 | 0 |
| maprotiline | Homo sapiens (human) | Ki | 0.0180 | 3 | 2 |
| mazindol | Homo sapiens (human) | IC50 | 0.0029 | 2 | 2 |
| mazindol | Homo sapiens (human) | Ki | 0.0152 | 4 | 4 |
| methapyrilene | Homo sapiens (human) | IC50 | 1.3910 | 1 | 0 |
| methapyrilene | Homo sapiens (human) | Ki | 1.3800 | 1 | 0 |
| methylphenidate | Homo sapiens (human) | IC50 | 0.0610 | 1 | 1 |
| methylphenidate | Homo sapiens (human) | Ki | 0.5000 | 2 | 2 |
| mianserin | Homo sapiens (human) | IC50 | 0.1630 | 1 | 0 |
| mianserin | Homo sapiens (human) | Ki | 0.1610 | 1 | 0 |
| miconazole | Homo sapiens (human) | IC50 | 2.9390 | 1 | 0 |
| miconazole | Homo sapiens (human) | Ki | 2.9150 | 1 | 0 |
| mitotane | Homo sapiens (human) | IC50 | 0.8190 | 1 | 0 |
| mitotane | Homo sapiens (human) | Ki | 0.8120 | 1 | 0 |
| mitoxantrone | Homo sapiens (human) | IC50 | 4.9898 | 1 | 0 |
| mitoxantrone | Homo sapiens (human) | Ki | 4.9485 | 1 | 0 |
| modafinil | Homo sapiens (human) | IC50 | 283.6000 | 1 | 1 |
| nabumetone | Homo sapiens (human) | IC50 | 1.8680 | 1 | 0 |
| nabumetone | Homo sapiens (human) | Ki | 1.8530 | 1 | 0 |
| nisoxetine | Homo sapiens (human) | IC50 | 0.0131 | 9 | 9 |
| nisoxetine | Homo sapiens (human) | Ki | 0.0045 | 3 | 3 |
| nomifensine | Homo sapiens (human) | IC50 | 0.6310 | 1 | 1 |
| nomifensine | Homo sapiens (human) | Ki | 0.0287 | 4 | 4 |
| nortriptyline | Homo sapiens (human) | IC50 | 0.0032 | 1 | 0 |
| nortriptyline | Homo sapiens (human) | Ki | 0.0047 | 2 | 1 |
| orphenadrine | Homo sapiens (human) | IC50 | 2.6660 | 1 | 0 |
| orphenadrine | Homo sapiens (human) | Ki | 2.6430 | 1 | 0 |
| oxybutynin | Homo sapiens (human) | IC50 | 2.5951 | 1 | 0 |
| oxybutynin | Homo sapiens (human) | Ki | 2.5737 | 1 | 0 |
| pentamidine | Homo sapiens (human) | IC50 | 2.2140 | 1 | 0 |
| pentamidine | Homo sapiens (human) | Ki | 2.1960 | 1 | 0 |
| perhexiline | Homo sapiens (human) | IC50 | 3.2942 | 1 | 0 |
| perhexiline | Homo sapiens (human) | Ki | 3.2670 | 1 | 0 |
| prochlorperazine | Homo sapiens (human) | IC50 | 0.4000 | 1 | 0 |
| prochlorperazine | Homo sapiens (human) | Ki | 0.3960 | 1 | 0 |
| promazine | Homo sapiens (human) | IC50 | 0.0130 | 1 | 0 |
| promazine | Homo sapiens (human) | Ki | 0.0130 | 1 | 0 |
| promethazine | Homo sapiens (human) | IC50 | 4.2380 | 1 | 0 |
| promethazine | Homo sapiens (human) | Ki | 4.2030 | 1 | 0 |
| propafenone | Homo sapiens (human) | IC50 | 3.0160 | 1 | 0 |
| propafenone | Homo sapiens (human) | Ki | 2.9910 | 1 | 0 |
| propofol | Homo sapiens (human) | IC50 | 9.3930 | 1 | 0 |
| propofol | Homo sapiens (human) | Ki | 9.3160 | 1 | 0 |
| protriptyline | Homo sapiens (human) | IC50 | 0.0049 | 10 | 10 |
| protriptyline | Homo sapiens (human) | Ki | 0.0030 | 5 | 5 |
| raloxifene | Homo sapiens (human) | IC50 | 0.2820 | 1 | 0 |
| raloxifene | Homo sapiens (human) | Ki | 0.2800 | 1 | 0 |
| riluzole | Homo sapiens (human) | IC50 | 1.7330 | 1 | 0 |
| riluzole | Homo sapiens (human) | Ki | 1.7180 | 1 | 0 |
| rolipram | Homo sapiens (human) | Ki | 0.0589 | 1 | 1 |
| sibutramine | Homo sapiens (human) | IC50 | 5.6650 | 1 | 0 |
| sibutramine | Homo sapiens (human) | Ki | 5.6190 | 1 | 0 |
| sulconazole | Homo sapiens (human) | IC50 | 2.0270 | 1 | 0 |
| sulconazole | Homo sapiens (human) | Ki | 2.0100 | 1 | 0 |
| terfenadine | Homo sapiens (human) | IC50 | 1.9280 | 1 | 0 |
| terfenadine | Homo sapiens (human) | Ki | 1.9120 | 1 | 0 |
| thioridazine | Homo sapiens (human) | IC50 | 1.5510 | 1 | 0 |
| thioridazine | Homo sapiens (human) | Ki | 1.5380 | 1 | 0 |
| ultram | Homo sapiens (human) | IC50 | 2.3255 | 2 | 2 |
| venlafaxine | Homo sapiens (human) | IC50 | 2.1114 | 9 | 8 |
| venlafaxine | Homo sapiens (human) | Ki | 1.0912 | 5 | 4 |
| zotepine | Homo sapiens (human) | Ki | 0.0005 | 1 | 1 |
| dextroamphetamine | Homo sapiens (human) | IC50 | 0.6310 | 1 | 1 |
| dextroamphetamine | Homo sapiens (human) | Ki | 0.1010 | 1 | 1 |
| 2-acetylaminofluorene | Homo sapiens (human) | IC50 | 8.5950 | 1 | 0 |
| 2-acetylaminofluorene | Homo sapiens (human) | Ki | 8.5240 | 1 | 0 |
| ethinyl estradiol | Homo sapiens (human) | IC50 | 0.9590 | 1 | 0 |
| ethinyl estradiol | Homo sapiens (human) | Ki | 0.9510 | 1 | 0 |
| mepazine | Homo sapiens (human) | IC50 | 1.8770 | 1 | 0 |
| mepazine | Homo sapiens (human) | Ki | 1.8610 | 1 | 0 |
| mestranol | Homo sapiens (human) | IC50 | 1.3820 | 1 | 0 |
| mestranol | Homo sapiens (human) | Ki | 1.3710 | 1 | 0 |
| n,n'-diphenyl-4-phenylenediamine | Homo sapiens (human) | IC50 | 0.7860 | 1 | 0 |
| n,n'-diphenyl-4-phenylenediamine | Homo sapiens (human) | Ki | 0.7800 | 1 | 0 |
| bisphenol a | Homo sapiens (human) | IC50 | 16.6200 | 1 | 0 |
| bisphenol a | Homo sapiens (human) | Ki | 16.4830 | 1 | 0 |
| phenothiazine | Homo sapiens (human) | IC50 | 0.4610 | 1 | 0 |
| phenothiazine | Homo sapiens (human) | Ki | 0.4570 | 1 | 0 |
| diphenylguanidine | Homo sapiens (human) | IC50 | 1.1520 | 1 | 0 |
| diphenylguanidine | Homo sapiens (human) | Ki | 1.1430 | 1 | 0 |
| monobenzone | Homo sapiens (human) | IC50 | 3.8860 | 1 | 0 |
| monobenzone | Homo sapiens (human) | Ki | 3.8540 | 1 | 0 |
| benzethonium chloride | Homo sapiens (human) | IC50 | 0.9070 | 1 | 0 |
| benzethonium chloride | Homo sapiens (human) | Ki | 0.9000 | 1 | 0 |
| sterogenol | Homo sapiens (human) | IC50 | 2.6530 | 1 | 0 |
| sterogenol | Homo sapiens (human) | Ki | 2.6310 | 1 | 0 |
| indopan | Homo sapiens (human) | IC50 | 3.7154 | 1 | 1 |
| indopan | Homo sapiens (human) | Ki | 5.3210 | 2 | 2 |
| dimenhydrinate | Homo sapiens (human) | IC50 | 2.0370 | 1 | 0 |
| dimenhydrinate | Homo sapiens (human) | Ki | 2.0200 | 1 | 0 |
| amitriptyline hydrochloride | Homo sapiens (human) | IC50 | 0.2000 | 1 | 0 |
| ethylestrenol | Homo sapiens (human) | IC50 | 2.0980 | 1 | 0 |
| ethylestrenol | Homo sapiens (human) | Ki | 2.0800 | 1 | 0 |
| pyrovalerone | Homo sapiens (human) | IC50 | 0.0283 | 1 | 1 |
| pyrovalerone | Homo sapiens (human) | Ki | 0.1950 | 1 | 1 |
| 4-octylphenol | Homo sapiens (human) | IC50 | 61.6470 | 1 | 0 |
| 4-octylphenol | Homo sapiens (human) | Ki | 61.1380 | 1 | 0 |
| n-methyllaurotetanine | Homo sapiens (human) | Ki | 0.9500 | 1 | 1 |
| clemastine | Homo sapiens (human) | IC50 | 3.0860 | 1 | 0 |
| clemastine | Homo sapiens (human) | Ki | 3.0600 | 1 | 0 |
| danazol | Homo sapiens (human) | IC50 | 5.6980 | 1 | 0 |
| danazol | Homo sapiens (human) | Ki | 5.6510 | 1 | 0 |
| metergoline | Homo sapiens (human) | IC50 | 0.3660 | 1 | 0 |
| metergoline | Homo sapiens (human) | Ki | 0.3630 | 1 | 0 |
| dexchlorpheniramine | Homo sapiens (human) | IC50 | 4.9660 | 1 | 0 |
| dexchlorpheniramine | Homo sapiens (human) | Ki | 4.9250 | 1 | 0 |
| penfluridol | Homo sapiens (human) | Ki | 0.5880 | 1 | 1 |
| dobutamine | Homo sapiens (human) | IC50 | 0.3830 | 1 | 0 |
| dobutamine | Homo sapiens (human) | Ki | 0.3800 | 1 | 0 |
| paroxetine | Homo sapiens (human) | IC50 | 0.0930 | 2 | 1 |
| paroxetine | Homo sapiens (human) | Ki | 0.0880 | 2 | 1 |
| bicifadine | Homo sapiens (human) | IC50 | 0.0550 | 1 | 1 |
| lovastatin | Homo sapiens (human) | IC50 | 8.7530 | 1 | 0 |
| lovastatin | Homo sapiens (human) | Ki | 8.6800 | 1 | 0 |
| atomoxetine hydrochloride | Homo sapiens (human) | IC50 | 0.0200 | 1 | 0 |
| atomoxetine | Homo sapiens (human) | IC50 | 0.0042 | 12 | 12 |
| (S)-nomifensine | Homo sapiens (human) | Ki | 0.0127 | 2 | 2 |
| duloxetine | Homo sapiens (human) | IC50 | 0.0886 | 13 | 13 |
| duloxetine | Homo sapiens (human) | Ki | 0.0207 | 9 | 9 |
| fluoxetine hydrochloride | Homo sapiens (human) | IC50 | 4.4100 | 1 | 1 |
| bupropion hydrochloride | Homo sapiens (human) | IC50 | 12.6000 | 1 | 0 |
| venlafaxine hydrochloride | Homo sapiens (human) | IC50 | 2.9466 | 8 | 8 |
| nelfinavir | Homo sapiens (human) | IC50 | 8.8520 | 1 | 0 |
| nelfinavir | Homo sapiens (human) | Ki | 8.7790 | 1 | 0 |
| desipramine hydrochloride | Homo sapiens (human) | IC50 | 0.0063 | 1 | 0 |
| desipramine hydrochloride | Homo sapiens (human) | Ki | 0.0008 | 1 | 1 |
| dopamine hydrochloride | Homo sapiens (human) | IC50 | 20.0000 | 1 | 0 |
| litoxetine | Homo sapiens (human) | IC50 | 3.9500 | 2 | 2 |
| milnacipran | Homo sapiens (human) | IC50 | 5.5000 | 1 | 1 |
| esreboxetine | Homo sapiens (human) | IC50 | 0.0027 | 3 | 3 |
| esreboxetine | Homo sapiens (human) | Ki | 0.0005 | 3 | 3 |
| sertraline | Homo sapiens (human) | IC50 | 0.8783 | 3 | 2 |
| sertraline | Homo sapiens (human) | Ki | 0.9766 | 1 | 0 |
| maprotiline hydrochloride | Homo sapiens (human) | IC50 | 0.0500 | 1 | 0 |
| vanoxerine | Homo sapiens (human) | IC50 | 1.4600 | 2 | 2 |
| cubebin | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| valdecoxib | Homo sapiens (human) | IC50 | 2.9270 | 1 | 0 |
| valdecoxib | Homo sapiens (human) | Ki | 2.9030 | 1 | 0 |
| desloratadine | Homo sapiens (human) | IC50 | 1.1160 | 1 | 0 |
| desloratadine | Homo sapiens (human) | Ki | 1.1070 | 1 | 0 |
| desvenlafaxine | Homo sapiens (human) | IC50 | 1.0190 | 2 | 2 |
| desvenlafaxine | Homo sapiens (human) | Ki | 0.6500 | 1 | 1 |
| indatraline | Homo sapiens (human) | Ki | 0.0185 | 2 | 2 |
| vestra | Homo sapiens (human) | IC50 | 0.0050 | 1 | 0 |
| reboxetine | Homo sapiens (human) | IC50 | 0.0018 | 1 | 1 |
| reboxetine | Homo sapiens (human) | Ki | 0.0390 | 1 | 1 |
| nisoxetine hydrochloride | Homo sapiens (human) | IC50 | 0.0050 | 1 | 0 |
| 4-methylthioamphetamine | Homo sapiens (human) | IC50 | 2.3750 | 1 | 1 |
| harmalan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| milnacipran hydrochloride | Homo sapiens (human) | IC50 | 0.0500 | 1 | 0 |
| nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| estradiol 3-benzoate | Homo sapiens (human) | IC50 | 17.2290 | 1 | 0 |
| estradiol 3-benzoate | Homo sapiens (human) | Ki | 17.0870 | 1 | 0 |
| benzatropine methanesulfonate | Homo sapiens (human) | IC50 | 0.3200 | 1 | 0 |
| 1-methyl-6-methoxy-dihydro-beta-carboline | Homo sapiens (human) | Ki | 4.1000 | 1 | 1 |
| hyperforin | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| nortriptyline hydrochloride | Homo sapiens (human) | IC50 | 0.0400 | 1 | 0 |
| terconazole | Homo sapiens (human) | IC50 | 25.3910 | 1 | 0 |
| terconazole | Homo sapiens (human) | Ki | 25.1820 | 1 | 0 |
| hinokinin | Homo sapiens (human) | IC50 | 8.7600 | 1 | 1 |
| resveratrol | Homo sapiens (human) | IC50 | 2.3120 | 1 | 0 |
| resveratrol | Homo sapiens (human) | Ki | 2.2930 | 1 | 0 |
| cocaine | Homo sapiens (human) | IC50 | 1.2861 | 22 | 22 |
| cocaine | Homo sapiens (human) | Ki | 1.6163 | 30 | 32 |
| diethylstilbestrol | Homo sapiens (human) | IC50 | 3.6700 | 1 | 0 |
| diethylstilbestrol | Homo sapiens (human) | Ki | 3.6400 | 1 | 0 |
| cocaine hydrochloride | Homo sapiens (human) | IC50 | 0.6300 | 1 | 0 |
| cocaine hydrochloride | Homo sapiens (human) | Ki | 1.9900 | 2 | 2 |
| (1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Homo sapiens (human) | IC50 | 1.4004 | 1 | 0 |
| (1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Homo sapiens (human) | Ki | 1.3888 | 1 | 0 |
| flunarizine | Homo sapiens (human) | IC50 | 1.3390 | 1 | 0 |
| flunarizine | Homo sapiens (human) | Ki | 1.3280 | 1 | 0 |
| benztropine | Homo sapiens (human) | IC50 | 1.3910 | 1 | 0 |
| benztropine | Homo sapiens (human) | Ki | 1.3790 | 1 | 0 |
| cinnarizine | Homo sapiens (human) | IC50 | 2.8320 | 1 | 0 |
| cinnarizine | Homo sapiens (human) | Ki | 2.8080 | 1 | 0 |
| enclomiphene | Homo sapiens (human) | IC50 | 0.8620 | 1 | 0 |
| enclomiphene | Homo sapiens (human) | Ki | 0.8550 | 1 | 0 |
| terbinafine | Homo sapiens (human) | IC50 | 4.1295 | 1 | 0 |
| terbinafine | Homo sapiens (human) | Ki | 4.0954 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | IC50 | 1.4720 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | Ki | 1.4590 | 1 | 0 |
| 2-[(2-ethoxyphenoxy)-phenylmethyl]morpholine | Homo sapiens (human) | IC50 | 0.0053 | 7 | 7 |
| 2-[(2-ethoxyphenoxy)-phenylmethyl]morpholine | Homo sapiens (human) | Ki | 0.0037 | 3 | 3 |
| vx-745 | Homo sapiens (human) | IC50 | 20.4040 | 1 | 0 |
| vx-745 | Homo sapiens (human) | Ki | 20.2360 | 1 | 0 |
| 4-[[(4-methylphenyl)sulfonylamino]methyl]-N-[2-[(phenylmethyl)-propan-2-ylamino]ethyl]benzamide | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| 3-[bis(4-fluorophenyl)methoxy]-8-methyl-8-azabicyclo[3.2.1]octane | Homo sapiens (human) | Ki | 4.6720 | 2 | 2 |
| bw 723c86 | Homo sapiens (human) | IC50 | 3.6257 | 1 | 0 |
| bw 723c86 | Homo sapiens (human) | Ki | 3.5957 | 1 | 0 |
| kurasoin b | Homo sapiens (human) | Ki | 2.7570 | 1 | 1 |
| harmine | Homo sapiens (human) | Ki | 3.2600 | 1 | 1 |
| montelukast | Homo sapiens (human) | IC50 | 2.6890 | 1 | 0 |
| montelukast | Homo sapiens (human) | Ki | 2.6670 | 1 | 0 |
| caffeic acid phenethyl ester | Homo sapiens (human) | IC50 | 3.7870 | 1 | 0 |
| caffeic acid phenethyl ester | Homo sapiens (human) | Ki | 3.7560 | 1 | 0 |
| lacidipine | Homo sapiens (human) | IC50 | 5.7350 | 1 | 0 |
| lacidipine | Homo sapiens (human) | Ki | 5.6870 | 1 | 0 |
| oxiconazole | Homo sapiens (human) | IC50 | 1.9103 | 1 | 0 |
| oxiconazole | Homo sapiens (human) | Ki | 1.8945 | 1 | 0 |
| pregabalin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| pregabalin | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| gw 1929 | Homo sapiens (human) | IC50 | 40.3080 | 1 | 0 |
| gw 1929 | Homo sapiens (human) | Ki | 39.9750 | 1 | 0 |
| levomilnacipran | Homo sapiens (human) | IC50 | 0.0400 | 2 | 2 |
| vilazodone | Homo sapiens (human) | IC50 | 0.1581 | 1 | 1 |
| nps2143 | Homo sapiens (human) | IC50 | 0.2000 | 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 | 10.0000 | 1 | 1 |
| armodafinil | Homo sapiens (human) | IC50 | 170.0000 | 1 | 1 |
| radafaxine | Homo sapiens (human) | IC50 | 5.0000 | 2 | 2 |
| dov 216303 | Homo sapiens (human) | IC50 | 0.0498 | 5 | 6 |
| dov 216303 | Homo sapiens (human) | Ki | 0.0630 | 1 | 1 |
| rwj 68354 | Homo sapiens (human) | IC50 | 1.0700 | 1 | 0 |
| rwj 68354 | Homo sapiens (human) | Ki | 1.0610 | 1 | 0 |
| o-demethyltramadol | Homo sapiens (human) | IC50 | 10.0000 | 2 | 2 |
| [2-[[2-[(dimethylamino)methyl]phenyl]thio]-5-iodophenyl]methanol | Homo sapiens (human) | Ki | 0.2340 | 2 | 2 |
| 4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| n,n-dimethyl-2-(2-amino-4-methylphenylthio)benzylamine | Homo sapiens (human) | IC50 | 0.1000 | 1 | 1 |
| n,n-dimethyl-2-(2-amino-4-methylphenylthio)benzylamine | Homo sapiens (human) | Ki | 0.2355 | 3 | 3 |
| n,n-dimethyl-2-(2-amino-4-fluorophenylthio)benzylamine | Homo sapiens (human) | Ki | 0.1417 | 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 | 2.4923 | 3 | 3 |
| 1-phenyl-2-(1-pyrrolidinyl)-1-pentanone | Homo sapiens (human) | IC50 | 0.0560 | 1 | 1 |
| 1-phenyl-2-(1-pyrrolidinyl)-1-pentanone | Homo sapiens (human) | Ki | 0.1990 | 1 | 1 |
| naphyrone | Homo sapiens (human) | IC50 | 0.0117 | 1 | 1 |
| naphyrone | Homo sapiens (human) | Ki | 0.1360 | 1 | 1 |
| naluzotan | Homo sapiens (human) | Ki | 2.0000 | 1 | 1 |
| milnacipran | Homo sapiens (human) | IC50 | 0.9621 | 6 | 6 |
| milnacipran | Homo sapiens (human) | Ki | 0.0850 | 1 | 1 |
| dov 21947 | Homo sapiens (human) | IC50 | 0.0471 | 2 | 2 |
| dov 21947 | Homo sapiens (human) | Ki | 0.1055 | 2 | 2 |
| lorcaserin | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 2-((2-((dimethylamino)methyl)phenyl)thio)-5-iodophenylamine | Homo sapiens (human) | Ki | 0.9167 | 3 | 3 |
| sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| srt1720 | Homo sapiens (human) | IC50 | 2.4700 | 1 | 1 |
| cep 26401 | Homo sapiens (human) | IC50 | 17.5000 | 1 | 1 |
| cep 26401 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| win 35,065-2 | Homo sapiens (human) | IC50 | 0.9200 | 2 | 2 |
| win 35,065-2 | Homo sapiens (human) | Ki | 0.5500 | 2 | 2 |
| nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| LSM-2536 | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | IC50 | 42.6579 | 1 | 1 |
| n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 10.6693 | 3 | 3 |
| clozapine | Homo sapiens (human) | IC50 | 1.4700 | 1 | 0 |
| clozapine | Homo sapiens (human) | Ki | 1.4580 | 1 | 0 |
| olanzapine | Homo sapiens (human) | Ki | 0.0040 | 1 | 1 |
| asoxime chloride | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| 3,4-dihydroxyphenylacetic acid | Homo sapiens (human) | EC50 | 28.8950 | 1 | 0 |
| n-methyl-3,4-methylenedioxyamphetamine | Homo sapiens (human) | EC50 | 1.0000 | 1 | 1 |
| 6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-10,11-diol | Homo sapiens (human) | EC50 | 3.2930 | 1 | 0 |
| desipramine | Homo sapiens (human) | Kd | 0.0008 | 1 | 1 |
| fluoxetine | Homo sapiens (human) | Kd | 0.2400 | 1 | 1 |
| hexachlorophene | Homo sapiens (human) | EC50 | 19.0950 | 1 | 0 |
| nefazodone | Homo sapiens (human) | Kd | 0.3600 | 1 | 1 |
| masoprocol | Homo sapiens (human) | EC50 | 8.7550 | 1 | 0 |
| protoporphyrin ix | Homo sapiens (human) | EC50 | 8.8870 | 1 | 0 |
| protriptyline | Homo sapiens (human) | Kd | 0.0014 | 1 | 1 |
| venlafaxine | Homo sapiens (human) | Kd | 1.0600 | 1 | 1 |
| viloxazine | Homo sapiens (human) | Kd | 0.1550 | 1 | 1 |
| dextroamphetamine | Homo sapiens (human) | EC50 | 0.2100 | 1 | 1 |
| methylene blue | Homo sapiens (human) | EC50 | 113.8860 | 1 | 0 |
| quinophthalone | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| yohimbine | Homo sapiens (human) | EC50 | 103.4860 | 1 | 0 |
| rhein | Homo sapiens (human) | EC50 | 21.5690 | 1 | 0 |
| methamphetamine | Homo sapiens (human) | EC50 | 0.9200 | 1 | 1 |
| neutral red base | Homo sapiens (human) | EC50 | 14.2540 | 1 | 0 |
| malononitrile dimer | Homo sapiens (human) | EC50 | 168.9080 | 1 | 0 |
| lysergol | Homo sapiens (human) | EC50 | 53.1860 | 1 | 0 |
| isoetharine mesylate | Homo sapiens (human) | EC50 | 125.3760 | 1 | 0 |
| benserazide hydrochloride | Homo sapiens (human) | EC50 | 0.1120 | 1 | 0 |
| l-amphetamine | Homo sapiens (human) | EC50 | 4.9600 | 1 | 1 |
| paroxetine | Homo sapiens (human) | Kd | 0.0400 | 1 | 1 |
| atomoxetine | Homo sapiens (human) | Kd | 0.0020 | 1 | 1 |
| epigallocatechin gallate | Homo sapiens (human) | EC50 | 0.7270 | 1 | 0 |
| dimidium bromide | Homo sapiens (human) | EC50 | 5.3630 | 1 | 0 |
| sertraline | Homo sapiens (human) | Kd | 0.4200 | 1 | 1 |
| methyl fluorone black | Homo sapiens (human) | EC50 | 0.0820 | 1 | 0 |
| agroclavine | Homo sapiens (human) | EC50 | 8.6720 | 1 | 0 |
| 2,4,6-tripyridyl-s-triazine | Homo sapiens (human) | EC50 | 54.5750 | 1 | 0 |
| oxoglaucine | Homo sapiens (human) | EC50 | 0.8340 | 1 | 0 |
| paxilline | Homo sapiens (human) | EC50 | 12.2720 | 1 | 0 |
| pyrophen | Homo sapiens (human) | EC50 | 27.9380 | 1 | 0 |
| sk&f-38393 | Homo sapiens (human) | EC50 | 23.9900 | 1 | 0 |
| 4-methylthioamphetamine | Homo sapiens (human) | EC50 | 34.6737 | 1 | 1 |
| sb 216763 | Homo sapiens (human) | EC50 | 21.5470 | 1 | 0 |
| 4-(2-methyl-5-phenyl-1-pyrrolyl)benzoic acid | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 2-carbazol-9-ylbenzoic acid | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| (R)-Roemerine | Homo sapiens (human) | EC50 | 21.4560 | 1 | 0 |
| oxopurpureine | Homo sapiens (human) | EC50 | 4.8310 | 1 | 0 |
| 3,6-bis(2-pyridyl)-1,2,4,5-tetrazine | Homo sapiens (human) | EC50 | 49.7830 | 1 | 0 |
| 18-Hydroxy-11,17-dimethoxyyohimban-16-carboxylic acid | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| (R)-norlaudanosoline | Homo sapiens (human) | EC50 | 5.4310 | 1 | 0 |
| resveratrol | Homo sapiens (human) | EC50 | 163.1310 | 1 | 0 |
| 2-phenoxy-N-(2-pyridinyl)butanamide | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 2-(N-[2-(1-benzotriazolyl)-1-oxoethyl]-4-methoxyanilino)-N-(2-methylbutan-2-yl)-2-(1-methyl-2-pyrrolyl)acetamide | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 6-hydroxy-1-(3-hydroxypropyl)-4-methyl-2-oxo-5-(1-piperidinylmethyl)-3-pyridinecarbonitrile | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 2-cyano-N-(3-methoxypropyl)-2-[3-(1-pyrrolidinyl)-2-quinoxalinyl]acetamide | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| N-ethyl-2-imino-10-methyl-1-[(4-methylphenyl)methyl]-5-oxo-3-dipyrido[3,4-c-1',2'-f]pyrimidinecarboxamide | Homo sapiens (human) | EC50 | 45.5140 | 1 | 0 |
| 7-(diethylamino)-2-oxo-1-benzopyran-3-carbonitrile | Homo sapiens (human) | EC50 | 62.9660 | 1 | 0 |
| 6-amino-5-(methylamino)-1-(phenylmethyl)pyrimidine-2,4-dione | Homo sapiens (human) | EC50 | 92.0940 | 1 | 0 |
| N'-[(4-chlorophenyl)-oxomethyl]-2-pyrazinecarbohydrazide | Homo sapiens (human) | EC50 | 12.4100 | 1 | 0 |
| 2-bromo-N-(3-methoxyphenyl)benzamide | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 2-phenyl-3-imidazo[1,2-a]pyridinecarboxaldehyde | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 1-[[(1,5-dimethyl-3-pyrazolyl)-oxomethyl]amino]-3-(2-methoxyphenyl)thiourea | Homo sapiens (human) | EC50 | 58.4420 | 1 | 0 |
| 3-(3-formyl-2,5-dimethyl-1-pyrrolyl)-4-methylbenzoic acid methyl ester | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| umi-77 | Homo sapiens (human) | EC50 | 8.1740 | 1 | 0 |
| 7-anilino-1-(4-methylphenyl)-5-oxo-[1,2,4]triazolo[4,3-a]pyrimidine-3-carboxylic acid ethyl ester | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 2-imino-10-methyl-N-[2-(4-morpholinyl)ethyl]-5-oxo-1-(3-pyridinylmethyl)-3-dipyrido[3,4-c-1',2'-f]pyrimidinecarboxamide | Homo sapiens (human) | EC50 | 87.1750 | 1 | 0 |
| 2-[2,5-dimethyl-3-[(2,4,6-trioxo-1,3-diazinan-5-ylidene)methyl]-1-pyrrolyl]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxylic acid ethyl ester | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 2-[[3-(3,4-dimethoxyphenyl)-2-oxo-1-benzopyran-7-yl]oxy]acetamide | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 3-amino-8-methyl-N-[4-(4-morpholinyl)phenyl]-2-thieno[2,3-b]quinolinecarboxamide | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 2-(4-chlorophenoxy)-4-(dimethylamino)-3-pyridinecarbonitrile | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 1,4-benzoquinone guanylhydrazone thiosemicarbazone | Homo sapiens (human) | EC50 | 9.7270 | 1 | 0 |
| 5-bromo-N-(2-fluorophenyl)-6-oxo-3-pyrancarboxamide | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 1-[2-[(2-methylphenyl)methylthio]ethyl]-3-phenylthiourea | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 2,8-dimercapto-6-hydroxypurine | Homo sapiens (human) | EC50 | 8.2950 | 1 | 0 |
| 1,3-benzothiazole-6-carboxylic acid [2-(2-furanyl)-2-oxoethyl] ester | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 5-(methoxymethyl)-2-thiophen-2-yl-1H-pyrazolo[1,5-a]pyrimidin-7-one | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| N'-benzoyl-2-(3-pyridinyl)-4-thiazolecarbohydrazide | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 2-amino-4-(4,5-dimethoxy-2-nitrophenyl)-7,7-dimethyl-5-oxo-6,8-dihydro-4H-1-benzopyran-3-carbonitrile | Homo sapiens (human) | EC50 | 23.0060 | 1 | 0 |
| 2-amino-7-methyl-5-oxo-4-(2,3,4-trimethoxyphenyl)-4,6,7,8-tetrahydro-1-benzopyran-3-carbonitrile | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 2-amino-7-methyl-5-oxo-4-(2,4,5-trimethoxyphenyl)-4,6,7,8-tetrahydro-1-benzopyran-3-carbonitrile | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 1-hexadecyl-3-methylimidazolium bromide | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 2-cyano-N-(phenylmethyl)-2-[3-(1-pyrrolidinyl)-2-quinoxalinyl]acetamide | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 2-benzoyl-N-(6-methoxy-3-pyridinyl)-3,4-dihydro-1H-isoquinoline-3-carboxamide | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 4-(6-bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 4-(6-bromo-1,3-benzodioxol-5-yl)-7,9-dimethyl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 1-[4-(6-bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]ethanone | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| N-[[[(2-hydroxyphenyl)-oxomethyl]hydrazo]-sulfanylidenemethyl]-2-nitrobenzamide | Homo sapiens (human) | EC50 | 32.1900 | 1 | 0 |
| 2-imino-1-[(4-methylphenyl)methyl]-5-oxo-N-(2-oxolanylmethyl)-3-dipyrido[1,2-d-3',4'-f]pyrimidinecarboxamide | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 6-amino-2-ethyl-8-[2-(trifluoromethyl)phenyl]-1,6,8,8a-tetrahydroisoquinoline-5,7,7-tricarbonitrile | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 2-(3-ethoxypropylamino)-8-methyl-5-oxo-N-(2-oxolanylmethyl)-3-dipyrido[1,2-pyrimidinecarboxamide | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 5-[(4-fluorophenyl)methylsulfonylmethyl]-N-(2-oxolanylmethyl)-2-furancarboxamide | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 4-[[2-[[cyclohexyl(oxo)methyl]amino]-1-oxo-3-phenylpropyl]amino]-1-piperidinecarboxylic acid ethyl ester | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 4-morpholinecarboxylic acid [4-(2-amino-3-cyano-5-oxo-4,6,7,8-tetrahydro-1-benzopyran-4-yl)-2,6-dimethoxyphenyl] ester | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 4-[3-(1,3-diphenyl-4-pyrazolyl)-5-thiophen-2-yl-3,4-dihydropyrazol-2-yl]-4-oxobutanoic acid | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 6-(5,6-Dihydroxy-4-oxo-2-phenylchromen-7-yl)oxy-3,4,5-trihydroxyoxane-2-carboxylic acid | Homo sapiens (human) | EC50 | 11.8890 | 1 | 0 |
| 4-(3,5-dimethyl-1-piperidinyl)-N-[5-(2-methylpropyl)-1,3,4-thiadiazol-2-yl]-4-oxobutanamide | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| N,6-dimethyl-2-[[[4-[(2-methyl-1-piperidinyl)sulfonyl]phenyl]-oxomethyl]amino]-5,7-dihydro-4H-thieno[2,3-c]pyridine-3-carboxamide | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 5-(3,4-dimethoxyphenyl)-3-(2-furanylmethyl)-4-imino-5H-[1]benzopyrano[2,3-d]pyrimidin-8-ol | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| luteolin | Homo sapiens (human) | EC50 | 31.0000 | 1 | 0 |
| methysergide maleate | Homo sapiens (human) | EC50 | 20.0450 | 1 | 0 |
| myricitrin | Homo sapiens (human) | EC50 | 14.0470 | 1 | 0 |
| rosmarinic acid | Homo sapiens (human) | EC50 | 8.7510 | 1 | 0 |
| 4-[(3aR,4S,9bS)-8-[(4-methoxyphenyl)sulfamoyl]-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-4-yl]benzoic acid | Homo sapiens (human) | EC50 | 7.8780 | 1 | 0 |
| semaxinib | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 2-(4-(dimethylamino)styryl)benzothiazole | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 1,5-dioxo-2,4-dihydropyrrolo[1,2-a]quinazoline-3-carboxylic acid ethyl ester | Homo sapiens (human) | EC50 | 38.8230 | 1 | 0 |
| quinaldine red | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 2',3,4-trihydroxychalcone | Homo sapiens (human) | EC50 | 42.2700 | 1 | 0 |
| 3-amino-5-(4-bromophenyl)-4-pyridazinecarbonitrile | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| cefdinir | Homo sapiens (human) | EC50 | 33.2570 | 1 | 0 |
| altenusin | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 1-(3,4-dimethylphenyl)-2,5-dioxo-3-dipyrido[1,2-d-3',4'-f]pyrimidinecarbonitrile | Homo sapiens (human) | EC50 | 55.7830 | 1 | 0 |
| mdl 105725 | Homo sapiens (human) | EC50 | 13.6670 | 1 | 0 |
| 3-amino-2-cyano-5-(3-methoxyphenyl)-7-methyl-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid methyl ester | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| 2-hydroxyapomorphine, (r)-isomer | Homo sapiens (human) | EC50 | 3.1730 | 1 | 0 |
| N-butyl-N-methyl-4-[(2-methyl-[1,2,4]triazolo[1,5-c]quinazolin-5-yl)hydrazo]-4-oxobutanamide | Homo sapiens (human) | EC50 | 5.3690 | 1 | 0 |
| [5-Chloranyl-3-[(1E,3E)-3,5-dimethylhepta-1,3-dienyl]-7-methyl-6,8-bis(oxidanylidene)isochromen-7-yl] ethanoate | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| N-[3-(diethylamino)propyl]-4-[(2-methyl-[1,2,4]triazolo[1,5-c]quinazolin-5-yl)hydrazo]-4-oxobutanamide | Homo sapiens (human) | EC50 | 0.9300 | 1 | 0 |
| violaceol II | Homo sapiens (human) | EC50 | 12.8910 | 1 | 0 |
| 2-(2-acetyl-3,5-dihydroxyphenyl)acetic acid | Homo sapiens (human) | EC50 | 190.0240 | 1 | 0 |
| cyclopenol | Homo sapiens (human) | EC50 | 35.0840 | 1 | 0 |
| N-[5-[methyl-(3-methylphenyl)sulfamoyl]-1,3,4-thiadiazol-2-yl]-2-furancarboxamide | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
| N-[1-(3-fluorophenyl)-6,6-dimethyl-5,7-dihydro-4H-indazol-4-yl]-2-(2-pyridinylthio)acetamide | Homo sapiens (human) | EC50 | 150.0000 | 1 | 0 |
| 3-[[1-[1-(methylthio)propan-2-yl]-4-piperidinyl]oxy]-N-(2-pyridinylmethyl)benzamide | Homo sapiens (human) | EC50 | 75.4220 | 1 | 0 |
| 2-(4-morpholinyl)-N'-[(2-nitrophenyl)-oxomethyl]-4-thiazolecarbohydrazide | Homo sapiens (human) | EC50 | 0.7310 | 1 | 0 |
| 2-(3,4-dihydro-1H-isoquinolin-2-ylmethyl)-1H-quinazolin-4-one | Homo sapiens (human) | EC50 | 300.0000 | 1 | 0 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| metergoline | Homo sapiens (human) | Activity | 1.1320 | 1 | 1 |
Selective deuteration of bupropion slows epimerization and reduces metabolism.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 76, 2022
Design, synthesis and docking study of 4-arylpiperazine carboxamides as monoamine neurotransmitters reuptake inhibitors.Bioorganic & medicinal chemistry, , 08-07, Volume: 26, Issue:14, 2018
Design, synthesis and in vitro activity of 1,4-disubstituted piperazines and piperidines as triple reuptake inhibitors.Bioorganic & medicinal chemistry, , 04-01, Volume: 25, Issue:7, 2017
Triple reuptake inhibitors: Design, synthesis and structure-activity relationship of benzylpiperidine-tetrazoles.Bioorganic & medicinal chemistry, , 10-15, Volume: 25, Issue:20, 2017
Exploration of substituted arylpiperazine-tetrazoles as promising dual norepinephrine and dopamine reuptake inhibitors.Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
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 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 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
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, 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],
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
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
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
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
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
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
Discovery of novel selective norepinephrine reuptake inhibitors: 4-[3-aryl-2,2-dioxido-2,1,3-benzothiadiazol-1(3H)-yl]-1-(methylamino)butan-2-ols (WYE-103231).Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
1-(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
Heterocyclic cycloalkanol ethylamines as norepinephrine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 20, Issue:9, 2010
Dual acting norepinephrine reuptake inhibitors and 5-HT(2A) receptor antagonists: Identification, synthesis and activity of novel 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles.Bioorganic & medicinal chemistry, , Nov-15, Volume: 17, Issue:22, 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
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
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
1- or 3-(3-Amino-2-hydroxy-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones: potent, selective, and orally efficacious norepinephrine reuptake inhibitors.Journal of medicinal chemistry, , Sep-24, Volume: 52, Issue:18, 2009
Synthesis and 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
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
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
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 of 11C-labelled (R)-OHDMI and CFMME and their evaluation as candidate radioligands for imaging central norepinephrine transporters with PET.Bioorganic & medicinal chemistry, , Jan-15, Volume: 15, Issue:2, 2007
Antidepressant principles of the roots of Polygala tenuifolia.Journal of natural products, , Volume: 69, Issue:9, 2006
The role of receptor binding in drug discovery.Journal of natural products, , Volume: 56, Issue:4, 1993
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
Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Dual inhibitors of phosphodiesterase-4 and serotonin reuptake.Journal of medicinal chemistry, , Mar-26, Volume: 52, Issue:6, 2009
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
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
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
N-(1,2-diphenylethyl)piperazines: a new class of dual serotonin/noradrenaline reuptake inhibitor.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
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],
Design, synthesis and in vitro activity of 1,4-disubstituted piperazines and piperidines as triple reuptake inhibitors.Bioorganic & medicinal chemistry, , 04-01, Volume: 25, Issue:7, 2017
Triple reuptake inhibitors: Design, synthesis and structure-activity relationship of benzylpiperidine-tetrazoles.Bioorganic & medicinal chemistry, , 10-15, Volume: 25, Issue:20, 2017
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
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
[no title available],
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
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:11, 2007
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
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
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
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
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
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 characterization of bicyclic triple reuptake inhibitor 3-aryl octahydrocyclopenta[c]pyrrole analogues.Journal of medicinal chemistry, , Aug-11, Volume: 54, Issue:15, 2011
Dual acting norepinephrine reuptake inhibitors and 5-HT(2A) receptor antagonists: Identification, synthesis and activity of novel 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles.Bioorganic & medicinal chemistry, , Nov-15, Volume: 17, Issue:22, 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
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
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
An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Azepines and piperidines with dual norepinephrine dopamine uptake inhibition and antidepressant activity.ACS medicinal chemistry letters, , Jan-10, Volume: 4, Issue:1, 2013
4-Phenyl tetrahydroisoquinolines as dual norepinephrine and dopamine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHBioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
First-in-class, dual-action, 3,5-disubstituted indole derivatives having human nitric oxide synthase (nNOS) and norepinephrine reuptake inhibitory (NERI) activity for the treatment of neuropathic pain.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
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
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
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
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
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
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
Discovery of a potent, dual serotonin and norepinephrine reuptake inhibitor.ACS medicinal chemistry letters, , Jun-13, Volume: 4, Issue:6, 2013
Synopsis of some recent tactical application of bioisosteres in drug design.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Heterocyclic cycloalkanol ethylamines as norepinephrine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 20, Issue:9, 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
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
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
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],
Structure-activity relationships of norepinephrine reuptake inhibitors with benzothiadiazine dioxide or dihydrosulfostyril cores.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 20, 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
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
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
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
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
Identification of 1S,2R-milnacipran analogs as potent norepinephrine and serotonin transporter inhibitors.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 18, Issue:11, 2008
Structure-activity relationships of chiral selective norepinephrine reuptake inhibitors (sNRI) with increased oxidative stability.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 18, Issue:16, 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
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
Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
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
Discovery of a potent, dual serotonin and norepinephrine reuptake inhibitor.ACS medicinal chemistry letters, , Jun-13, Volume: 4, Issue:6, 2013
4-Phenyl tetrahydroisoquinolines as dual norepinephrine and dopamine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
Heterocyclic cycloalkanol ethylamines as norepinephrine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 20, Issue:9, 2010
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
N-[(3S)-Pyrrolidin-3-yl]benzamides as novel dual serotonin and noradrenaline reuptake inhibitors: impact of small structural modifications on P-gp recognition and CNS penetration.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 19, Issue:17, 2009
Novel, achiral aminoheterocycles as selective monoamine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 19, Issue:16, 2009
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
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
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 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
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
Design and synthesis of morpholine derivatives. SAR for dual serotonin & noradrenaline reuptake inhibition.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 18, Issue:8, 2008
N-Benzyl-N-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-amines as selective dual serotonin/noradrenaline reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 17, Issue:7, 2007
N-(1,2-diphenylethyl)piperazines: a new class of dual serotonin/noradrenaline reuptake inhibitor.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
Synthesis and biological activity of some known and putative duloxetine metabolites.Bioorganic & medicinal chemistry letters, , Jul-05, Volume: 14, Issue:13, 2004
Duloxetine (Cymbalta), a dual inhibitor of serotonin and norepinephrine reuptake.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 13, Issue:24, 2003
Design, synthesis and docking study of 4-arylpiperazine carboxamides as monoamine neurotransmitters reuptake inhibitors.Bioorganic & medicinal chemistry, , 08-07, Volume: 26, Issue:14, 2018
Design, synthesis, and 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 in vitro activity of 1,4-disubstituted piperazines and piperidines as triple reuptake inhibitors.Bioorganic & medicinal chemistry, , 04-01, Volume: 25, Issue:7, 2017
Triple reuptake inhibitors: Design, synthesis and structure-activity relationship of benzylpiperidine-tetrazoles.Bioorganic & medicinal chemistry, , 10-15, Volume: 25, Issue:20, 2017
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
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
Dual acting norepinephrine reuptake inhibitors and 5-HT(2A) receptor antagonists: Identification, synthesis and activity of novel 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles.Bioorganic & medicinal chemistry, , Nov-15, Volume: 17, Issue:22, 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
Synthesis, radiosynthesis, and biological evaluation of carbon-11 and fluorine-18 labeled reboxetine analogues: potential positron emission tomography radioligands for in vivo imaging of the norepinephrine transporter.Journal of medicinal chemistry, , Jan-08, Volume: 52, Issue:1, 2009
Structure-activity relationships of chiral selective norepinephrine reuptake inhibitors (sNRI) with increased oxidative stability.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 18, Issue:16, 2008
Synthesis and pharmacological evaluation of 4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalenyl amines as triple reuptake inhibitors.Bioorganic & medicinal chemistry, , Jan-01, Volume: 19, Issue:1, 2011
Designing rapid onset selective serotonin re-uptake inhibitors. Part 1: Structure-activity relationships of substituted (1S,4S)-4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydro-1-naphthaleneamine.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 16, Issue:5, 2006
Synthesis of a potent wide-spectrum serotonin-, norepinephrine-, dopamine-reuptake inhibitor (SNDRI) and a species-selective dopamine-reuptake inhibitor based on the gamma-amino alcohol functional group.Bioorganic & medicinal chemistry letters, , Mar-03, Volume: 8, Issue:5, 1998
[no title available],
Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
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
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
Synthesis and structure-activity relationship of 3beta-(4-alkylthio, -methylsulfinyl, and -methylsulfonylphenyl)tropane and 3beta-(4-alkylthiophenyl)nortropane derivatives for monoamine transporters.Bioorganic & medicinal chemistry, , Jul-15, Volume: 17, Issue:14, 2009
Dual inhibitors of phosphodiesterase-4 and serotonin reuptake.Journal of medicinal chemistry, , Mar-26, Volume: 52, Issue:6, 2009
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
2,5-Disubstituted tetrahydrofurans as selective serotonin re-uptake inhibitors.Bioorganic & medicinal chemistry, , Mar-01, Volume: 17, Issue:5, 2009
Synthesis and receptor binding properties of 2beta-alkynyl and 2beta-(1,2,3-triazol)substituted 3beta-(substituted phenyl)tropane derivatives.Bioorganic & medicinal chemistry, , May-15, Volume: 16, Issue:10, 2008
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:11, 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
Synthesis, inhibition and binding of simple non-nitrogen inhibitors of monoamine transporters.Bioorganic & medicinal chemistry, , Jun-15, Volume: 15, Issue:12, 2007
Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter.Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
Development of peptidic dopamine transporter inhibitors via aromatic modification-mediated conformational restriction.Journal of medicinal chemistry, , Jul-13, Volume: 49, Issue:14, 2006
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
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
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
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
Development of 3-phenyltropane analogues with high affinity for the dopamine and serotonin transporters and low affinity for the norepinephrine transporter.Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
Synthesis and monoamine transporter binding properties of 2beta-[3'-(substituted benzyl)isoxazol-5-yl]- and 2beta-[3'-methyl-4'-(substituted phenyl)isoxazol-5-yl]-3beta-(substituted phenyl)tropanes.Bioorganic & medicinal chemistry, , Jul-15, Volume: 16, Issue:14, 2008
[no title available],
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
[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
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
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
N-(1,2-diphenylethyl)piperazines: a new class of dual serotonin/noradrenaline reuptake inhibitor.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
Synthesis, radiosynthesis, and biological evaluation of carbon-11 and iodine-123 labeled 2beta-carbomethoxy-3beta-[4'-((Z)-2-haloethenyl)phenyl]tropanes: candidate radioligands for in vivo imaging of the serotonin transporter.Journal of medicinal chemistry, , Feb-26, Volume: 47, Issue:5, 2004
N-8-Substituted benztropinamine analogs as selective dopamine transporter ligands.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 15, Issue:24, 2005
Novel N-substituted 3 alpha-[bis(4'-fluorophenyl)methoxy]tropane analogues: selective ligands for the dopamine transporter.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
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
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
Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 18, Issue:13, 2008
Novel 3,3-disubstituted pyrrolidines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 18, Issue:23, 2008
2-(2-(dimethylaminomethyl)phenoxy)-5-iodophenylamine: an improved serotonin transporter imaging agent.Journal of medicinal chemistry, , Oct-07, Volume: 47, Issue:21, 2004
A new single-photon emission computed tomography imaging agent for serotonin transporters: [123I]IDAM, 5-iodo-2-((2-((dimethylamino)methyl)phenyl)thio)benzyl alcohol.Journal of medicinal chemistry, , Feb-11, Volume: 42, Issue:3, 1999
Docking study, synthesis, and in vitro evaluation of fluoro-MADAM derivatives as SERT ligands for PET imaging.Bioorganic & medicinal chemistry, , Oct-01, Volume: 16, Issue:19, 2008
Synthesis and in vitro evaluation of novel derivatives of diphenylsulfide as serotonin transporter ligands.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 16, Issue:5, 2006
Synthesis, in vitro characterization, and radiolabeling of N,N-dimethyl-2-(2'-amino-4'-substituted-phenylthio)benzylamines: potential candidates as selective serotonin transporter radioligands.Journal of medicinal chemistry, , Jun-30, Volume: 48, Issue:13, 2005
Fluorinated diaryl sulfides as serotonin transporter ligands: synthesis, structure-activity relationship study, and in vivo evaluation of fluorine-18-labeled compounds as PET imaging agents.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
Fluorinated diaryl sulfides as serotonin transporter ligands: synthesis, structure-activity relationship study, and in vivo evaluation of fluorine-18-labeled compounds as PET imaging agents.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
2-(2-(dimethylaminomethyl)phenoxy)-5-iodophenylamine: an improved serotonin transporter imaging agent.Journal of medicinal chemistry, , Oct-07, Volume: 47, Issue:21, 2004
Novel radiotracers for imaging the serotonin transporter by positron emission tomography: synthesis, radiosynthesis, and in vitro and ex vivo evaluation of (11)C-labeled 2-(phenylthio)araalkylamines.Journal of medicinal chemistry, , Aug-10, Volume: 43, Issue:16, 2000
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
Discovery of a potent, dual serotonin and norepinephrine reuptake inhibitor.ACS medicinal chemistry letters, , Jun-13, Volume: 4, Issue:6, 2013
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
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
Synthesis and pharmacological investigation of aralkyl diamine derivatives as potential triple reuptake inhibitors.European journal of medicinal chemistry, , Oct-30, Volume: 86, 2014
1-(Aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes and 6-(aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes: a new series of potent and selective triple reuptake inhibitors.Journal of medicinal chemistry, , Mar-25, Volume: 53, Issue:6, 2010
6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane: a new potent and selective triple reuptake inhibitor.Journal of medicinal chemistry, , Jul-08, Volume: 53, Issue:13, 2010
Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 18, Issue:13, 2008
Synthesis, in vitro characterization, and radiolabeling of N,N-dimethyl-2-(2'-amino-4'-substituted-phenylthio)benzylamines: potential candidates as selective serotonin transporter radioligands.Journal of medicinal chemistry, , Jun-30, Volume: 48, Issue:13, 2005
Fluorinated diaryl sulfides as serotonin transporter ligands: synthesis, structure-activity relationship study, and in vivo evaluation of fluorine-18-labeled compounds as PET imaging agents.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
2-(2-(dimethylaminomethyl)phenoxy)-5-iodophenylamine: an improved serotonin transporter imaging agent.Journal of medicinal chemistry, , Oct-07, Volume: 47, Issue:21, 2004
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 10 target(s):
| Target | Category | Definition |
|---|
| actin binding | molecular function | Binding to monomeric or multimeric forms of actin, including actin filaments. [GOC:clt] |
| 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] |
| neurotransmitter:sodium symporter activity | molecular function | Enables the transfer of a solute or solutes from one side of a membrane to the other according to the reaction: neurotransmitter(out) + Na+(out) = neurotransmitter(in) + Na+(in). [TC:2.A.22.-.-] |
| dopamine:sodium symporter activity | molecular function | Enables the transfer of a solute or solutes from one side of a membrane to the other according to the reaction: dopamine(out) + Na+(out) + Cl-(out)= dopamine(in) + Na+(in) + Cl-(in). [PMID:21752877, PMID:22519513, TC:2.A.22.1.3] |
| norepinephrine:sodium symporter activity | molecular function | Enables the transfer of a solute or solutes from one side of a membrane to the other according to the reaction: norepinephrine(out) + Na+(out) + Cl-(out) = norepinephrine(in) + Na+(in) + Cl-(in). [PMID:21752877, PMID:22519513, TC:2.A.22.1.2] |
| 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] |
| alpha-tubulin binding | molecular function | Binding to the microtubule constituent protein alpha-tubulin. [GOC:jl] |
| metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
| beta-tubulin binding | molecular function | Binding to the microtubule constituent protein beta-tubulin. [GOC:krc] |
Located In
This protein is located in 3 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] |
| cell surface | cellular component | The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
Active In
This protein is active in 4 target(s):
| Target | Category | Definition |
|---|
| neuronal cell body membrane | cellular component | The plasma membrane of a neuron cell body - excludes the plasma membrane of cell projections such as axons and dendrites. [GOC:jl] |
| presynaptic membrane | cellular component | A specialized area of membrane of the axon terminal that faces the plasma membrane of the neuron or muscle fiber with which the axon terminal establishes a synaptic junction; many synaptic junctions exhibit structural presynaptic characteristics, such as conical, electron-dense internal protrusions, that distinguish it from the remainder of the axon plasma membrane. [GOC:jl, ISBN:0815316194] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| axon | cellular component | The long process of a neuron that conducts nerve impulses, usually away from the cell body to the terminals and varicosities, which are sites of storage and release of neurotransmitter. [GOC:nln, ISBN:0198506732] |
Involved In
This protein is involved in 10 target(s):
| Target | Category | Definition |
|---|
| neurotransmitter transport | biological process | The directed movement of a neurotransmitter into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. Neurotransmitters are any chemical substance that is capable of transmitting (or inhibiting the transmission of) a nerve impulse from a neuron to another cell. [GOC:ai] |
| chemical synaptic transmission | biological process | The vesicular release of classical neurotransmitter molecules from a presynapse, across a chemical synapse, the subsequent activation of neurotransmitter receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:jl, MeSH:D009435] |
| 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 pain | 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 pain stimulus. Pain stimuli cause activation of nociceptors, peripheral receptors for pain, include receptors which are sensitive to painful mechanical stimuli, extreme heat or cold, and chemical stimuli. [GOC:jid, PMID:10203867, PMID:12723742, PMID:12843304, Wikipedia:Pain] |
| norepinephrine uptake | biological process | The directed movement of norepinephrine into a cell, typically presynaptic neurons or glial cells. Norepinephrine (3,4-dihydroxyphenyl-2-aminoethanol) is a hormone secreted by the adrenal medulla and a neurotransmitter in the sympathetic peripheral nervous system and in some tracts of the CNS. It is also the biosynthetic precursor of epinephrine. [GOC:ai] |
| neuron cellular homeostasis | biological process | The cellular homeostatic process that preserves a neuron in a stable, differentiated functional and structural state. [GOC:BHF, GOC:mah] |
| amino acid transport | biological process | The directed movement of amino acids, organic acids containing one or more amino substituents, into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:ai] |
| norepinephrine transport | biological process | The directed movement of norepinephrine into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. Norepinephrine (3,4-dihydroxyphenyl-2-aminoethanol) is a hormone secreted by the adrenal medulla and a neurotransmitter in the sympathetic peripheral nervous system and in some tracts of the CNS. It is also the biosynthetic precursor of epinephrine. [GOC:ai, ISBN:0198506732] |
| dopamine uptake involved in synaptic transmission | biological process | The directed movement of dopamine into a presynaptic neuron or glial cell. In this context, dopamine is a catecholamine neurotransmitter and a metabolic precursor of noradrenaline and adrenaline. [GOC:ai] |
| 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] |