Page last updated: 2024-08-07 16:06:20
Alpha-2C adrenergic receptor
An alpha-2C adrenergic receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P18825]
Synonyms
Alpha-2 adrenergic receptor subtype C4;
Alpha-2C adrenoreceptor;
Alpha-2C adrenoceptor;
Alpha-2CAR
Research
Bioassay Publications (99)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 11 (11.11) | 18.7374 |
| 1990's | 15 (15.15) | 18.2507 |
| 2000's | 35 (35.35) | 29.6817 |
| 2010's | 31 (31.31) | 24.3611 |
| 2020's | 7 (7.07) | 2.80 |
Compounds (177)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| quinacrine | Homo sapiens (human) | IC50 | 3.8570 | 1 | 0 |
| quinacrine | Homo sapiens (human) | Ki | 0.5600 | 1 | 0 |
| sk&f-38393 | Homo sapiens (human) | Ki | 0.0832 | 1 | 1 |
| 6-fluoronorepinephrine | Homo sapiens (human) | Ki | 0.0120 | 1 | 1 |
| amitriptyline | Homo sapiens (human) | IC50 | 0.0295 | 2 | 1 |
| amitriptyline | Homo sapiens (human) | Ki | 0.0086 | 1 | 0 |
| amlodipine | Homo sapiens (human) | IC50 | 1.8000 | 1 | 0 |
| amlodipine | Homo sapiens (human) | Ki | 0.2610 | 1 | 0 |
| amoxapine | Homo sapiens (human) | IC50 | 3.1740 | 1 | 0 |
| amoxapine | Homo sapiens (human) | Ki | 0.4610 | 1 | 0 |
| apraclonidine | Homo sapiens (human) | IC50 | 0.0040 | 1 | 1 |
| apraclonidine | Homo sapiens (human) | Ki | 0.0300 | 1 | 1 |
| astemizole | Homo sapiens (human) | IC50 | 1.9590 | 1 | 0 |
| astemizole | Homo sapiens (human) | Ki | 0.2850 | 1 | 0 |
| bithionol | Homo sapiens (human) | IC50 | 4.3920 | 1 | 0 |
| bithionol | Homo sapiens (human) | Ki | 0.6380 | 1 | 0 |
| bmy 7378 | Homo sapiens (human) | Ki | 0.1820 | 1 | 1 |
| brimonidine | Homo sapiens (human) | IC50 | 0.0030 | 1 | 1 |
| brimonidine | Homo sapiens (human) | Ki | 0.0156 | 2 | 3 |
| carvedilol | Homo sapiens (human) | IC50 | 0.0900 | 1 | 0 |
| carvedilol | Homo sapiens (human) | Ki | 0.0130 | 1 | 0 |
| chloroquine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| chlorpromazine | Homo sapiens (human) | IC50 | 0.3740 | 1 | 0 |
| chlorpromazine | Homo sapiens (human) | Ki | 0.0540 | 1 | 0 |
| cirazoline | Homo sapiens (human) | Ki | 0.5495 | 2 | 2 |
| cisapride | Homo sapiens (human) | IC50 | 3.2600 | 3 | 2 |
| cisapride | Homo sapiens (human) | Ki | 0.1130 | 1 | 0 |
| clomipramine | Homo sapiens (human) | IC50 | 0.7065 | 2 | 1 |
| clomipramine | Homo sapiens (human) | Ki | 0.2050 | 1 | 0 |
| clonidine | Homo sapiens (human) | IC50 | 0.0115 | 2 | 2 |
| clonidine | Homo sapiens (human) | Ki | 0.0466 | 5 | 5 |
| cyproheptadine | Homo sapiens (human) | IC50 | 1.2750 | 1 | 0 |
| cyproheptadine | Homo sapiens (human) | Ki | 0.1850 | 1 | 0 |
| desipramine | Homo sapiens (human) | IC50 | 0.0002 | 1 | 1 |
| domperidone | Homo sapiens (human) | IC50 | 1.0110 | 1 | 0 |
| domperidone | Homo sapiens (human) | Ki | 0.1470 | 1 | 0 |
| doxazosin | Homo sapiens (human) | Ki | 0.2800 | 1 | 1 |
| doxepin | Homo sapiens (human) | IC50 | 0.5145 | 2 | 1 |
| doxepin | Homo sapiens (human) | Ki | 0.1500 | 1 | 0 |
| droperidol | Homo sapiens (human) | IC50 | 1.7630 | 1 | 0 |
| droperidol | Homo sapiens (human) | Ki | 0.2560 | 1 | 0 |
| ebastine | Homo sapiens (human) | IC50 | 0.2757 | 1 | 0 |
| ebastine | Homo sapiens (human) | Ki | 0.0401 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | IC50 | 0.1540 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | Ki | 0.0220 | 1 | 0 |
| guanfacine | Homo sapiens (human) | IC50 | 6.4470 | 1 | 0 |
| guanfacine | Homo sapiens (human) | Ki | 0.9370 | 1 | 0 |
| haloperidol | Homo sapiens (human) | IC50 | 1.8450 | 1 | 0 |
| haloperidol | Homo sapiens (human) | Ki | 2.6340 | 2 | 1 |
| haloprogin | Homo sapiens (human) | IC50 | 4.0450 | 1 | 0 |
| haloprogin | Homo sapiens (human) | Ki | 0.5880 | 1 | 0 |
| hexachlorophene | Homo sapiens (human) | IC50 | 6.9754 | 1 | 0 |
| hexachlorophene | Homo sapiens (human) | Ki | 1.0135 | 1 | 0 |
| hydroxychloroquine | Homo sapiens (human) | Ki | 15.8489 | 1 | 1 |
| maprotiline | Homo sapiens (human) | IC50 | 3.0440 | 1 | 0 |
| maprotiline | Homo sapiens (human) | Ki | 0.4420 | 1 | 0 |
| mianserin | Homo sapiens (human) | IC50 | 0.0661 | 4 | 3 |
| mianserin | Homo sapiens (human) | Ki | 0.0149 | 2 | 1 |
| mirtazapine | Homo sapiens (human) | IC50 | 0.1995 | 1 | 1 |
| mirtazapine | Homo sapiens (human) | Ki | 0.0180 | 1 | 1 |
| nan 190 | Homo sapiens (human) | Ki | 0.0008 | 1 | 1 |
| naphazoline | Homo sapiens (human) | Ki | 0.0023 | 1 | 1 |
| nortriptyline | Homo sapiens (human) | IC50 | 0.1015 | 2 | 1 |
| nortriptyline | Homo sapiens (human) | Ki | 0.0300 | 1 | 0 |
| oxymetazoline | Homo sapiens (human) | IC50 | 2.6330 | 1 | 0 |
| oxymetazoline | Homo sapiens (human) | Ki | 0.1090 | 17 | 20 |
| 4-iodoclonidine | Homo sapiens (human) | IC50 | 0.0015 | 1 | 1 |
| moxonidine | Homo sapiens (human) | Ki | 1.0375 | 2 | 2 |
| prazosin | Homo sapiens (human) | IC50 | 0.6470 | 1 | 0 |
| prazosin | Homo sapiens (human) | Ki | 0.8467 | 14 | 13 |
| prochlorperazine | Homo sapiens (human) | IC50 | 0.0820 | 1 | 0 |
| prochlorperazine | Homo sapiens (human) | Ki | 0.0120 | 1 | 0 |
| promazine | Homo sapiens (human) | IC50 | 0.2530 | 1 | 0 |
| promazine | Homo sapiens (human) | Ki | 0.0370 | 1 | 0 |
| promethazine | Homo sapiens (human) | IC50 | 2.4310 | 1 | 0 |
| promethazine | Homo sapiens (human) | Ki | 0.3530 | 1 | 0 |
| propranolol | Homo sapiens (human) | IC50 | 5.0119 | 1 | 1 |
| quetiapine | Homo sapiens (human) | IC50 | 0.4208 | 1 | 0 |
| quetiapine | Homo sapiens (human) | Ki | 0.4160 | 3 | 2 |
| raloxifene | Homo sapiens (human) | IC50 | 0.7380 | 1 | 0 |
| raloxifene | Homo sapiens (human) | Ki | 0.1070 | 1 | 0 |
| risperidone | Homo sapiens (human) | IC50 | 0.0096 | 1 | 0 |
| risperidone | Homo sapiens (human) | Ki | 0.0035 | 4 | 3 |
| sk&f 29661 | Homo sapiens (human) | Ki | 100.0000 | 2 | 3 |
| sulconazole | Homo sapiens (human) | IC50 | 4.9340 | 1 | 0 |
| sulconazole | Homo sapiens (human) | Ki | 0.7170 | 1 | 0 |
| terazosin | Homo sapiens (human) | IC50 | 6.0420 | 1 | 0 |
| terazosin | Homo sapiens (human) | Ki | 0.3126 | 5 | 4 |
| terfenadine | Homo sapiens (human) | IC50 | 3.7480 | 1 | 0 |
| terfenadine | Homo sapiens (human) | Ki | 0.5450 | 1 | 0 |
| thioridazine | Homo sapiens (human) | IC50 | 0.1710 | 1 | 0 |
| thioridazine | Homo sapiens (human) | Ki | 0.0250 | 1 | 0 |
| ticlopidine | Homo sapiens (human) | IC50 | 1.1750 | 1 | 0 |
| ticlopidine | Homo sapiens (human) | Ki | 0.1710 | 1 | 0 |
| trazodone | Homo sapiens (human) | IC50 | 1.9420 | 1 | 0 |
| trazodone | Homo sapiens (human) | Ki | 0.2820 | 1 | 0 |
| 5-methylurapidil | Homo sapiens (human) | Ki | 0.1310 | 1 | 1 |
| wb 4101 | Homo sapiens (human) | Ki | 0.0008 | 1 | 1 |
| xylometazoline | Homo sapiens (human) | Ki | 0.2955 | 2 | 2 |
| zotepine | Homo sapiens (human) | Ki | 0.5700 | 2 | 2 |
| phentolamine | Homo sapiens (human) | IC50 | 0.1100 | 1 | 0 |
| phentolamine | Homo sapiens (human) | Ki | 0.0274 | 4 | 3 |
| phenylephrine | Homo sapiens (human) | Ki | 0.3900 | 1 | 1 |
| yohimbine hydrochloride | Homo sapiens (human) | IC50 | 0.0271 | 1 | 1 |
| yohimbine hydrochloride | Homo sapiens (human) | Ki | 0.0019 | 1 | 1 |
| ergotamine | Homo sapiens (human) | IC50 | 0.0120 | 1 | 0 |
| ergotamine | Homo sapiens (human) | Ki | 0.0018 | 1 | 0 |
| dibenzothiazyl disulfide | Homo sapiens (human) | IC50 | 1.6580 | 1 | 0 |
| dibenzothiazyl disulfide | Homo sapiens (human) | Ki | 0.2410 | 1 | 0 |
| benzethonium chloride | Homo sapiens (human) | IC50 | 1.9610 | 1 | 0 |
| benzethonium chloride | Homo sapiens (human) | Ki | 0.2850 | 1 | 0 |
| sterogenol | Homo sapiens (human) | IC50 | 1.4970 | 1 | 0 |
| sterogenol | Homo sapiens (human) | Ki | 0.2170 | 1 | 0 |
| yohimbine | Homo sapiens (human) | IC50 | 0.0466 | 5 | 4 |
| yohimbine | Homo sapiens (human) | Ki | 0.0130 | 18 | 19 |
| indopan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| emetine | Homo sapiens (human) | IC50 | 0.1820 | 1 | 0 |
| emetine | Homo sapiens (human) | Ki | 0.0260 | 1 | 0 |
| dihydroergotamine | Homo sapiens (human) | IC50 | 0.0100 | 1 | 0 |
| dihydroergotamine | Homo sapiens (human) | Ki | 0.0015 | 1 | 0 |
| gentian violet | Homo sapiens (human) | IC50 | 1.8840 | 1 | 0 |
| gentian violet | Homo sapiens (human) | Ki | 0.2740 | 1 | 0 |
| naphazoline hydrochloride | Homo sapiens (human) | IC50 | 0.0000 | 1 | 1 |
| 1-naphthylisothiocyanate | Homo sapiens (human) | IC50 | 54.5390 | 1 | 0 |
| 1-naphthylisothiocyanate | Homo sapiens (human) | Ki | 7.9240 | 1 | 0 |
| Berberine chloride (TN) | Homo sapiens (human) | IC50 | 2.8370 | 1 | 0 |
| Berberine chloride (TN) | Homo sapiens (human) | Ki | 0.4120 | 1 | 0 |
| 4-octylphenol | Homo sapiens (human) | IC50 | 14.2340 | 1 | 0 |
| 4-octylphenol | Homo sapiens (human) | Ki | 2.0680 | 1 | 0 |
| n-methyllaurotetanine | Homo sapiens (human) | Ki | 0.9500 | 1 | 1 |
| clemastine | Homo sapiens (human) | IC50 | 0.0950 | 1 | 0 |
| clemastine | Homo sapiens (human) | Ki | 0.1189 | 2 | 1 |
| danazol | Homo sapiens (human) | IC50 | 23.7520 | 1 | 0 |
| danazol | Homo sapiens (human) | Ki | 3.4510 | 1 | 0 |
| metergoline | Homo sapiens (human) | IC50 | 0.1890 | 1 | 0 |
| metergoline | Homo sapiens (human) | Ki | 0.0270 | 1 | 0 |
| lisuride | Homo sapiens (human) | IC50 | 0.0043 | 1 | 0 |
| lisuride | Homo sapiens (human) | Ki | 0.0006 | 1 | 0 |
| lofexidine | Homo sapiens (human) | Ki | 0.0692 | 1 | 1 |
| bromocriptine | Homo sapiens (human) | IC50 | 0.5200 | 1 | 0 |
| bromocriptine | Homo sapiens (human) | Ki | 0.0760 | 1 | 0 |
| 1-(2-(2,4-dichlorophenyl)-2-hydroxyethyl)-1h-imidazole | Homo sapiens (human) | Ki | 15.1356 | 1 | 1 |
| indoramin | Homo sapiens (human) | Ki | 0.4760 | 1 | 1 |
| penfluridol | Homo sapiens (human) | Ki | 0.4450 | 1 | 1 |
| closantel | Homo sapiens (human) | IC50 | 7.1000 | 1 | 0 |
| closantel | Homo sapiens (human) | Ki | 1.0000 | 1 | 0 |
| pergolide | Homo sapiens (human) | IC50 | 1.4100 | 1 | 0 |
| pergolide | Homo sapiens (human) | Ki | 0.2050 | 1 | 0 |
| idazoxan | Homo sapiens (human) | IC50 | 0.0537 | 1 | 1 |
| idazoxan | Homo sapiens (human) | Ki | 0.0148 | 4 | 4 |
| ipsapirone | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| sertindole | Homo sapiens (human) | Ki | 1.6800 | 1 | 1 |
| niguldipine | Homo sapiens (human) | Ki | 0.3500 | 2 | 2 |
| aripiprazole | Homo sapiens (human) | Ki | 0.0379 | 1 | 1 |
| irinotecan | Homo sapiens (human) | IC50 | 3.1710 | 1 | 0 |
| irinotecan | Homo sapiens (human) | Ki | 0.4610 | 1 | 0 |
| ziprasidone | Homo sapiens (human) | Ki | 0.3900 | 2 | 2 |
| medetomidine hydrochloride | Homo sapiens (human) | IC50 | 3.3000 | 1 | 1 |
| sertraline | Homo sapiens (human) | IC50 | 4.4770 | 1 | 0 |
| sertraline | Homo sapiens (human) | Ki | 0.6505 | 1 | 0 |
| rilmenidine | Homo sapiens (human) | Ki | 0.0963 | 2 | 2 |
| atipamezole | Homo sapiens (human) | Ki | 0.0042 | 1 | 1 |
| efaroxan | Homo sapiens (human) | Ki | 0.0513 | 1 | 1 |
| ergocornine | Homo sapiens (human) | IC50 | 0.0170 | 1 | 0 |
| ergocornine | Homo sapiens (human) | Ki | 0.0024 | 1 | 0 |
| corynanthine | Homo sapiens (human) | Ki | 0.1610 | 1 | 1 |
| u 74006f | Homo sapiens (human) | IC50 | 7.8980 | 1 | 0 |
| u 74006f | Homo sapiens (human) | Ki | 1.1480 | 1 | 0 |
| gr 127935 | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| rx 821002 | Homo sapiens (human) | Ki | 0.0011 | 2 | 2 |
| pramipexole | Homo sapiens (human) | Ki | 0.0522 | 1 | 1 |
| dx 9065 | Homo sapiens (human) | IC50 | 0.0700 | 1 | 1 |
| sk&f 104078 | Homo sapiens (human) | Ki | 0.0640 | 2 | 2 |
| 7,8-dichloro-1,2,3,4-tetrahydroisoquinoline | Homo sapiens (human) | Ki | 0.0210 | 1 | 1 |
| sk&f 86466 | Homo sapiens (human) | Ki | 0.0183 | 2 | 2 |
| sk&f 104856 | Homo sapiens (human) | Ki | 0.0210 | 1 | 1 |
| tamsulosin | Homo sapiens (human) | Ki | 0.0079 | 1 | 1 |
| sc 53116 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sc 53116 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 4-(benzodioxan-5-yl)-1-(indan-2-yl)piperazine | Homo sapiens (human) | Ki | 0.1445 | 1 | 1 |
| alpha-ergocryptine | Homo sapiens (human) | IC50 | 0.0380 | 1 | 0 |
| alpha-ergocryptine | Homo sapiens (human) | Ki | 0.0055 | 1 | 0 |
| n-demethyllysergic acid diethylamide | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| 3-fluoronorepinephrine | Homo sapiens (human) | Ki | 0.7000 | 1 | 1 |
| nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 0.1810 | 1 | 1 |
| maduramicin | Homo sapiens (human) | IC50 | 1.6100 | 1 | 0 |
| maduramicin | Homo sapiens (human) | Ki | 0.2340 | 1 | 0 |
| fipamezole | Homo sapiens (human) | Ki | 0.0138 | 1 | 1 |
| estradiol 3-benzoate | Homo sapiens (human) | IC50 | 24.6500 | 1 | 0 |
| estradiol 3-benzoate | Homo sapiens (human) | Ki | 3.5820 | 1 | 0 |
| 2-(4-methyl-1-piperazinyl)aniline | Homo sapiens (human) | Ki | 0.2399 | 1 | 1 |
| conessine | Homo sapiens (human) | Ki | 0.0105 | 1 | 2 |
| terconazole | Homo sapiens (human) | IC50 | 0.4180 | 1 | 0 |
| terconazole | Homo sapiens (human) | Ki | 0.0610 | 1 | 0 |
| raubasine | Homo sapiens (human) | Ki | 0.0050 | 1 | 1 |
| dihydroergocristine monomesylate | Homo sapiens (human) | IC50 | 0.0086 | 1 | 0 |
| dihydroergocristine monomesylate | Homo sapiens (human) | Ki | 0.0013 | 1 | 0 |
| diethylstilbestrol | Homo sapiens (human) | IC50 | 15.1510 | 1 | 0 |
| diethylstilbestrol | Homo sapiens (human) | Ki | 2.2010 | 1 | 0 |
| jp-1302 | Homo sapiens (human) | Ki | 0.0280 | 2 | 2 |
| rauwolscine | Homo sapiens (human) | IC50 | 0.0160 | 1 | 1 |
| rauwolscine | Homo sapiens (human) | Ki | 0.0018 | 9 | 10 |
| cannabidiol | Homo sapiens (human) | Ki | 3.7000 | 1 | 1 |
| (1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Homo sapiens (human) | IC50 | 3.4460 | 1 | 0 |
| (1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Homo sapiens (human) | Ki | 0.5007 | 1 | 0 |
| flunarizine | Homo sapiens (human) | IC50 | 0.2220 | 1 | 0 |
| flunarizine | Homo sapiens (human) | Ki | 0.0320 | 1 | 0 |
| benztropine | Homo sapiens (human) | IC50 | 0.3950 | 1 | 0 |
| benztropine | Homo sapiens (human) | Ki | 0.0570 | 1 | 0 |
| cinnarizine | Homo sapiens (human) | IC50 | 0.6520 | 1 | 0 |
| cinnarizine | Homo sapiens (human) | Ki | 0.0950 | 1 | 0 |
| enclomiphene | Homo sapiens (human) | IC50 | 1.4820 | 1 | 0 |
| enclomiphene | Homo sapiens (human) | Ki | 0.2150 | 1 | 0 |
| mitragynine | Homo sapiens (human) | Ki | 2.3200 | 1 | 1 |
| thioperamide | Homo sapiens (human) | Ki | 0.3467 | 1 | 1 |
| 2-(2-benzofuranyl)-2-imidazoline | Homo sapiens (human) | Ki | 26.6091 | 2 | 2 |
| n-(1-methyl-5-indolyl)-n'-(3-methyl-5-isothiazolyl)urea | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| 4-[[(4-methylphenyl)sulfonylamino]methyl]-N-[2-[(phenylmethyl)-propan-2-ylamino]ethyl]benzamide | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| 3-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-1,5-dihydropyrimido[5,4-b]indole-2,4-dione | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| rutin | Homo sapiens (human) | Ki | 9.6370 | 1 | 1 |
| harmine | Homo sapiens (human) | Ki | 0.8100 | 1 | 1 |
| montelukast | Homo sapiens (human) | IC50 | 5.2790 | 1 | 0 |
| montelukast | Homo sapiens (human) | Ki | 0.7670 | 1 | 0 |
| dexmedetomidine | Homo sapiens (human) | Ki | 0.0309 | 1 | 1 |
| l 745870 | Homo sapiens (human) | Ki | 0.2300 | 1 | 1 |
| oxiconazole | Homo sapiens (human) | IC50 | 4.1645 | 1 | 0 |
| oxiconazole | Homo sapiens (human) | Ki | 0.6051 | 1 | 0 |
| guanabenz | Homo sapiens (human) | IC50 | 1.1060 | 1 | 0 |
| guanabenz | Homo sapiens (human) | Ki | 0.1610 | 1 | 0 |
| ciproxifan | Homo sapiens (human) | Ki | 0.0631 | 1 | 1 |
| dexniguldipine | Homo sapiens (human) | Ki | 0.4500 | 1 | 1 |
| vilazodone | Homo sapiens (human) | IC50 | 6.0000 | 1 | 1 |
| n-demethylloperamide | Homo sapiens (human) | Ki | 0.0024 | 1 | 1 |
| pd 144418 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 4-(3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl)-1-(4-fluorophenyl)butan-1-one | Homo sapiens (human) | Ki | 0.0554 | 1 | 2 |
| pnu 96415e | Homo sapiens (human) | Ki | 0.1810 | 1 | 1 |
| st 1936 | Homo sapiens (human) | Ki | 0.3000 | 1 | 1 |
| LSM-1328 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 2-(2-fluoro-5-methylphenyl)-4,5-dihydro-1h-imidazole | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 3-trifluoromethyl-7-bromo-1,2,3,4-tetrahydroisoquinoline | Homo sapiens (human) | Ki | 1,000.0000 | 1 | 1 |
| PB28 | Homo sapiens (human) | Ki | 0.4786 | 1 | 1 |
| sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| pf 04457845 | Homo sapiens (human) | Ki | 0.5980 | 2 | 0 |
| 2-(1-(2-allylphenoxy)ethyl)-4,5-dihydro-1h-imidazole | Homo sapiens (human) | Ki | 0.0851 | 4 | 4 |
| nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 3.1213 | 2 | 4 |
| entecavir | Homo sapiens (human) | Ki | 0.8600 | 1 | 0 |
| clozapine | Homo sapiens (human) | IC50 | 0.0079 | 1 | 0 |
| clozapine | Homo sapiens (human) | Ki | 0.0538 | 4 | 3 |
| olanzapine | Homo sapiens (human) | IC50 | 0.5310 | 1 | 0 |
| olanzapine | Homo sapiens (human) | Ki | 0.1322 | 4 | 3 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| alprenolol | Homo sapiens (human) | Kapp | 0.0200 | 1 | 1 |
| bunolol | Homo sapiens (human) | Kapp | 0.0170 | 1 | 1 |
| pindolol | Homo sapiens (human) | Kapp | 0.0930 | 1 | 1 |
| practolol | Homo sapiens (human) | Kapp | 313.0000 | 1 | 1 |
| prazosin | Homo sapiens (human) | EC40 | 1.3000 | 2 | 3 |
| propranolol | Homo sapiens (human) | Kapp | 0.0180 | 1 | 1 |
| phentolamine | Homo sapiens (human) | Kb | 0.0070 | 1 | 1 |
| metergoline | Homo sapiens (human) | Activity | 0.0300 | 1 | 1 |
| rauwolscine | Homo sapiens (human) | Kb | 0.0018 | 1 | 1 |
Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist.Journal of medicinal chemistry, , Aug-30, Volume: 39, Issue:18, 1996
Radioiodinated p-iodoclonidine: a high-affinity probe for the alpha 2-adrenergic receptor.Journal of medicinal chemistry, , Volume: 30, Issue:7, 1987
Guanidine and 2-aminoimidazoline aromatic derivatives as alpha2-adrenoceptor ligands: searching for structure-activity relationships.Journal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009
Guanidine and 2-aminoimidazoline aromatic derivatives as alpha(2)-adrenoceptor antagonists, 1: toward new antidepressants with heteroatomic linkers.Journal of medicinal chemistry, , Sep-06, Volume: 50, Issue:18, 2007
Synthesis and evaluation of 2-(arylamino)imidazoles as alpha 2-adrenergic agonists.Journal of medicinal chemistry, , Jan-03, Volume: 40, Issue:1, 1997
Radioiodinated p-iodoclonidine: a high-affinity probe for the alpha 2-adrenergic receptor.Journal of medicinal chemistry, , Volume: 30, Issue:7, 1987
[no title available],
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.ACS medicinal chemistry letters, , Sep-12, Volume: 4, Issue:9, 2013
Might adrenergic alpha2C-agonists/alpha2A-antagonists become novel therapeutic tools for pain treatment with morphine?Journal of medicinal chemistry, , Nov-26, Volume: 52, Issue:22, 2009
Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists.Journal of medicinal chemistry, , Feb-09, Volume: 49, Issue:3, 2006
Azaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 14, Issue:22, 2004
[no title available],
Transfer of SAR information from hypotensive indazole to indole derivatives acting at α-adrenergic receptors: In vitro and in vivo studies.European journal of medicinal chemistry, , Jun-10, Volume: 115, 2016
Synthesis and biological evaluation of 2-aryliminopyrrolidines as selective ligands for I1 imidazoline receptors: discovery of new sympatho-inhibitory hypotensive agents with potential beneficial effects in metabolic syndrome.Journal of medicinal chemistry, , Jan-22, Volume: 58, Issue:2, 2015
Methylation of imidazoline related compounds leads to loss of α₂-adrenoceptor affinity. Synthesis and biological evaluation of selective I₁ imidazoline receptor ligands.Bioorganic & medicinal chemistry, , Aug-01, Volume: 20, Issue:15, 2012
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.Journal of medicinal chemistry, , Nov-11, Volume: 53, Issue:21, 2010
alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor.Journal of medicinal chemistry, , Mar-09, Volume: 43, Issue:5, 2000
Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent.Journal of medicinal chemistry, , Mar-15, Volume: 39, Issue:6, 1996
Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist.Journal of medicinal chemistry, , Aug-30, Volume: 39, Issue:18, 1996
2H-[1]benzopyrano[3,4-b]pyridines: synthesis and activity at central monoamine receptors.Journal of medicinal chemistry, , Volume: 32, Issue:3, 1989
Radioiodinated p-iodoclonidine: a high-affinity probe for the alpha 2-adrenergic receptor.Journal of medicinal chemistry, , Volume: 30, Issue:7, 1987
[no title available],
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 2.Bioorganic & medicinal chemistry letters, , Jan-21, Volume: 12, Issue:2, 2002
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 1.Bioorganic & medicinal chemistry letters, , Jan-21, Volume: 12, Issue:2, 2002
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.Journal of medicinal chemistry, , Aug-12, Volume: 42, Issue:16, 1999
[no title available],
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine having highly active and potent central alpha 2-antagonistic activity as potential antidepressants.Bioorganic & medicinal chemistry letters, , Jan-03, Volume: 10, Issue:1, 2000
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 24, Issue:2, 2014
2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: the discovery of alpha1a subtype selective 2'-alkylsulfonyl-substituted analogues.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
Benzylimidazolines as h5-HT1B/1D serotonin receptor ligands: a structure-affinity investigation.Journal of medicinal chemistry, , Jun-18, Volume: 41, Issue:13, 1998
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
[no title available],
Synthesis and biological evaluation of 2-aryliminopyrrolidines as selective ligands for I1 imidazoline receptors: discovery of new sympatho-inhibitory hypotensive agents with potential beneficial effects in metabolic syndrome.Journal of medicinal chemistry, , Jan-22, Volume: 58, Issue:2, 2015
Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent.Journal of medicinal chemistry, , Mar-15, Volume: 39, Issue:6, 1996
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.Journal of medicinal chemistry, , May-12, Volume: 38, Issue:10, 1995
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
2,4-diamino-6,7-dimethoxyquinazolines. 1. 2-[4-(1,4-benzodioxan-2-ylcarbonyl)piperazin-1-yl] derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.Journal of medicinal chemistry, , Volume: 30, Issue:1, 1987
2,4-Diamino-6,7-dimethoxyquinazolines. 2. 2-(4-Carbamoylpiperidino) derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.Journal of medicinal chemistry, , Volume: 30, Issue:6, 1987
[no title available],
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.Journal of medicinal chemistry, , Dec-10, Volume: 58, Issue:23, 2015
Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides.Journal of medicinal chemistry, , Volume: 25, Issue:6, 1982
Cardioselectivity of beta-adrenoceptor blocking agents 1. 1-[(4-Hydroxyphenethyl)amino]-3-(aryloxy)propan-2-ols.Journal of medicinal chemistry, , Volume: 22, Issue:6, 1979
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
[no title available],
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
[no title available],
Inhibitors of phenylethanolamine N-methyltransferase devoid of alpha2-adrenoceptor affinity.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 15, Issue:23, 2005
Molecular recognition of sub-micromolar inhibitors by the epinephrine-synthesizing enzyme phenylethanolamine N-methyltransferase.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
Identification of a dihydropyridine as a potent alpha1a adrenoceptor-selective antagonist that inhibits phenylephrine-induced contraction of the human prostate.Journal of medicinal chemistry, , Jul-02, Volume: 41, Issue:14, 1998
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist Journal of medicinal chemistry, , Sep-26, Volume: 40, Issue:20, 1997
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.Journal of medicinal chemistry, , May-12, Volume: 38, Issue:10, 1995
[no title available],
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
Absolute configuration of glycerol derivatives. 7. Enantiomers of 2-[[[2-(2,6-dimethoxyphenoxy)ethyl]amino]methyl]-1,4-benzodioxane (WB-4101), a potent competitive alpha-adrenergic antagonist.Journal of medicinal chemistry, , Volume: 22, Issue:9, 1979
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
Bioisosteric phentolamine analogs as potent alpha-adrenergic antagonists.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 15, Issue:21, 2005
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
Development of an affinity ligand for purification of alpha 2-adrenoceptors from human platelet membranes.Journal of medicinal chemistry, , Volume: 27, Issue:7, 1984
6-Chloro-2,3,4,5-tetrahydro-3-methyl-1H-3-benzazepine: a potent and selective antagonist of alpha 2-adrenoceptors.Journal of medicinal chemistry, , Volume: 26, Issue:9, 1983
Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides.Journal of medicinal chemistry, , Volume: 25, Issue:6, 1982
[no title available],
Further studies on arylpiperazinyl alkyl pyridazinones: discovery of an exceptionally potent, orally active, antinociceptive agent in thermally induced pain.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
Novel 4-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)methylbenzofuran derivatives as selective alpha(2C)-adrenergic receptor antagonists.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 17, Issue:6, 2007
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.Journal of medicinal chemistry, , 01-09, Volume: 63, Issue:1, 2020
Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.European journal of medicinal chemistry, , Mar-06, Volume: 92, 2015
Novel arylsulfonamide derivatives with 5-HT₆/5-HT₇ receptor antagonism targeting behavioral and psychological symptoms of dementia.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
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
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
Synthesis and biological studies of yohimbine derivatives on human alpha2C-adrenergic receptors.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 15, Issue:11, 2005
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.Journal of medicinal chemistry, , Sep-15, Volume: 38, Issue:19, 1995
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
Radioiodinated p-iodoclonidine: a high-affinity probe for the alpha 2-adrenergic receptor.Journal of medicinal chemistry, , Volume: 30, Issue:7, 1987
[no title available],
Benzofuranyl-2-imidazoles as imidazoline IEuropean journal of medicinal chemistry, , Oct-15, Volume: 222, 2021
Favourable involvement of α2A-adrenoreceptor antagonism in the I₂-imidazoline binding sites-mediated morphine analgesia enhancement.Bioorganic & medicinal chemistry, , Apr-01, Volume: 20, Issue:7, 2012
Alpha2-adrenoreceptors profile modulation. 4. From antagonist to agonist behavior.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
Novel 4-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)methylbenzofuran derivatives as selective alpha(2C)-adrenergic receptor antagonists.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 17, Issue:6, 2007
New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine having highly active and potent central alpha 2-antagonistic activity as potential antidepressants.Bioorganic & medicinal chemistry letters, , Jan-03, Volume: 10, Issue:1, 2000
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.Journal of medicinal chemistry, , Sep-15, Volume: 38, Issue:19, 1995
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.Journal of medicinal chemistry, , May-12, Volume: 38, Issue:10, 1995
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
Synthesis and biological evaluation of 2-aryliminopyrrolidines as selective ligands for I1 imidazoline receptors: discovery of new sympatho-inhibitory hypotensive agents with potential beneficial effects in metabolic syndrome.Journal of medicinal chemistry, , Jan-22, Volume: 58, Issue:2, 2015
Methylation of imidazoline related compounds leads to loss of α₂-adrenoceptor affinity. Synthesis and biological evaluation of selective I₁ imidazoline receptor ligands.Bioorganic & medicinal chemistry, , Aug-01, Volume: 20, Issue:15, 2012
[no title available]European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Substituted conformationally restricted guanidine derivatives: Probing the α2-adrenoceptors' binding pocket.European journal of medicinal chemistry, , Nov-10, Volume: 123, 2016
Alpha2-adrenoreceptors profile modulation. 4. From antagonist to agonist behavior.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa.Bioorganic & medicinal chemistry, , Feb-01, Volume: 17, Issue:3, 2009
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.Journal of medicinal chemistry, , Sep-15, Volume: 38, Issue:19, 1995
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist Journal of medicinal chemistry, , Sep-26, Volume: 40, Issue:20, 1997
Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists.Journal of medicinal chemistry, , Feb-09, Volume: 49, Issue:3, 2006
Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 14, Issue:12, 2004
[no title available]European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Novel arylsulfonamide derivatives with 5-HT₆/5-HT₇ receptor antagonism targeting behavioral and psychological symptoms of dementia.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.Journal of medicinal chemistry, , Sep-15, Volume: 38, Issue:19, 1995
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
Return of DJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Return of DJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.ACS medicinal chemistry letters, , Sep-12, Volume: 4, Issue:9, 2013
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.ACS medicinal chemistry letters, , Jul-12, Volume: 3, Issue:7, 2012
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.Journal of medicinal chemistry, , Nov-11, Volume: 53, Issue:21, 2010
Alpha2-adrenoreceptors profile modulation. 4. From antagonist to agonist behavior.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
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
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
[no title available],
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
[no title available],
Enables
This protein enables 6 target(s):
| Target | Category | Definition |
|---|
| alpha2-adrenergic receptor activity | molecular function | Combining with epinephrine or norepinephrine to initiate a change in cell activity via activation of a G protein, with pharmacological characteristics of alpha2-adrenergic receptors; the activity involves transmitting the signal to the Gi alpha subunit of a heterotrimeric G protein. [GOC:cb, GOC:mah, IUPHAR_GPCR:1274] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| alpha-2A adrenergic receptor binding | molecular function | Binding to an alpha-2A adrenergic receptor. [GOC:mah, GOC:nln] |
| protein homodimerization activity | molecular function | Binding to an identical protein to form a homodimer. [GOC:jl] |
| protein heterodimerization activity | molecular function | Binding to a nonidentical protein to form a heterodimer. [GOC:ai] |
| epinephrine binding | molecular function | Binding to epinephrine, a hormone produced by the medulla of the adrenal glands that increases heart activity, improves the power and prolongs the action of muscles, and increases the rate and depth of breathing. It is synthesized by the methylation of norepinephrine. [GOC:ai] |
Located In
This protein is located in 3 target(s):
| Target | Category | Definition |
|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| endosome | cellular component | A vacuole to which materials ingested by endocytosis are delivered. [ISBN:0198506732, PMID:19696797] |
| 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] |
Active In
This protein is active in 1 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] |
Involved In
This protein is involved in 13 target(s):
| Target | Category | Definition |
|---|
| regulation of smooth muscle contraction | biological process | Any process that modulates the frequency, rate or extent of smooth muscle contraction. [GOC:go_curators] |
| G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
| cell-cell signaling | biological process | Any process that mediates the transfer of information from one cell to another. This process includes signal transduction in the receiving cell and, where applicable, release of a ligand and any processes that actively facilitate its transport and presentation to the receiving cell. Examples include signaling via soluble ligands, via cell adhesion molecules and via gap junctions. [GOC:dos, GOC:mah] |
| negative regulation of norepinephrine secretion | biological process | Any process that decreases the frequency, rate or extent of the regulated release of norepinephrine. [GOC:dph, GOC:tb] |
| regulation of vasoconstriction | biological process | Any process that modulates the frequency, rate or extent of reductions in the diameter of blood vessels. [GOC:jl] |
| platelet activation | biological process | A series of progressive, overlapping events triggered by exposure of the platelets to subendothelial tissue. These events include shape change, adhesiveness, aggregation, and release reactions. When carried through to completion, these events lead to the formation of a stable hemostatic plug. [http://www.graylab.ac.uk/omd/] |
| activation of protein kinase B activity | biological process | Any process that initiates the activity of the inactive enzyme protein kinase B. [GOC:pg] |
| negative regulation of epinephrine secretion | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the regulated release of epinephrine. [GOC:vk] |
| receptor transactivation | biological process | The process in which a receptor is activated by another receptor. Receptor transactivation can occur through different mechanisms and includes cross-talk between signaling pathways where one receptor activates a receptor for a different ligand, and also activation of subunits within a receptor oligomer. [GOC:al, GOC:bf, GOC:BHF, PMID:16870826, PMID:21063387] |
| positive regulation of MAPK cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the MAPK cascade. [GOC:go_curators] |
| positive regulation of neuron differentiation | biological process | Any process that activates or increases the frequency, rate or extent of neuron differentiation. [GOC:go_curators] |
| adrenergic receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by a ligand binding to an adrenergic receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:BHF] |
| adenylate cyclase-activating adrenergic receptor signaling pathway | biological process | An adenylate cyclase-activating G protein-coupled receptor signaling pathway initiated by a ligand binding to an adrenergic receptor on the surface of the target cell, and ending with the regulation of a downstream cellular process. [GOC:BHF, GOC:mah, GOC:signaling] |