Proteins > 5-hydroxytryptamine receptor 2A
Page last updated: 2024-08-07 16:20:30
5-hydroxytryptamine receptor 2A
A 5-hydroxytryptamine receptor 2A that is encoded in the genome of human. [PRO:WCB, UniProtKB:P28223]
Synonyms
5-HT-2;
5-HT-2A;
Serotonin receptor 2A
Research
Bioassay Publications (264)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 1 (0.38) | 18.7374 |
| 1990's | 23 (8.71) | 18.2507 |
| 2000's | 83 (31.44) | 29.6817 |
| 2010's | 116 (43.94) | 24.3611 |
| 2020's | 41 (15.53) | 2.80 |
Compounds (278)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| quinacrine | Homo sapiens (human) | IC50 | 2.6630 | 1 | 0 |
| quinacrine | Homo sapiens (human) | Ki | 0.7610 | 1 | 0 |
| phenethylamine | Homo sapiens (human) | Ki | 16.8000 | 2 | 2 |
| 4-iodo-2,5-dimethoxyphenylisopropylamine | Homo sapiens (human) | Ki | 1.7233 | 8 | 8 |
| 1-(1-naphthyl)piperazine | Homo sapiens (human) | IC50 | 0.0620 | 1 | 1 |
| 1-(3-chlorophenyl)piperazine | Homo sapiens (human) | Ki | 0.0763 | 7 | 7 |
| 5-(nonyloxy)tryptamine | Homo sapiens (human) | Ki | 0.2600 | 1 | 1 |
| 5-carboxamidotryptamine | Homo sapiens (human) | Ki | 5.0119 | 1 | 1 |
| methylbufotenin | Homo sapiens (human) | Ki | 0.2167 | 3 | 3 |
| 5-methoxytryptamine | Homo sapiens (human) | Ki | 0.1524 | 2 | 2 |
| alpha-methylserotonin | Homo sapiens (human) | Ki | 0.0120 | 1 | 1 |
| amiodarone | Homo sapiens (human) | IC50 | 3.5900 | 1 | 0 |
| amiodarone | Homo sapiens (human) | Ki | 1.0260 | 1 | 0 |
| dan 2163 | Homo sapiens (human) | Ki | 0.6310 | 1 | 1 |
| amitriptyline | Homo sapiens (human) | IC50 | 0.0150 | 1 | 0 |
| amitriptyline | Homo sapiens (human) | Ki | 0.0044 | 1 | 0 |
| amoxapine | Homo sapiens (human) | IC50 | 0.0016 | 1 | 0 |
| amoxapine | Homo sapiens (human) | Ki | 0.0011 | 2 | 1 |
| astemizole | Homo sapiens (human) | IC50 | 0.0200 | 1 | 0 |
| astemizole | Homo sapiens (human) | Ki | 0.0056 | 1 | 0 |
| buspirone | Homo sapiens (human) | IC50 | 2.2860 | 1 | 0 |
| buspirone | Homo sapiens (human) | Ki | 1.5813 | 3 | 2 |
| verapamil | Homo sapiens (human) | IC50 | 0.4420 | 1 | 0 |
| verapamil | Homo sapiens (human) | Ki | 0.1260 | 1 | 0 |
| carvedilol | Homo sapiens (human) | IC50 | 0.4100 | 1 | 0 |
| carvedilol | Homo sapiens (human) | Ki | 0.1170 | 1 | 0 |
| chlorpromazine | Homo sapiens (human) | IC50 | 0.0036 | 2 | 1 |
| chlorpromazine | Homo sapiens (human) | Ki | 0.0062 | 4 | 4 |
| cisapride | Homo sapiens (human) | IC50 | 0.0054 | 3 | 2 |
| cisapride | Homo sapiens (human) | Ki | 0.0037 | 2 | 1 |
| clomipramine | Homo sapiens (human) | IC50 | 0.0670 | 1 | 0 |
| clomipramine | Homo sapiens (human) | Ki | 0.0190 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | IC50 | 11.1420 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | Ki | 3.1830 | 1 | 0 |
| cyproheptadine | Homo sapiens (human) | IC50 | 0.0010 | 1 | 0 |
| cyproheptadine | Homo sapiens (human) | Ki | 0.0013 | 4 | 3 |
| desipramine | Homo sapiens (human) | Ki | 0.0803 | 2 | 2 |
| dicyclomine | Homo sapiens (human) | IC50 | 0.2400 | 1 | 0 |
| dicyclomine | Homo sapiens (human) | Ki | 0.0690 | 1 | 0 |
| diphenidol | Homo sapiens (human) | IC50 | 2.5860 | 1 | 0 |
| diphenidol | Homo sapiens (human) | Ki | 0.7390 | 1 | 0 |
| diphenhydramine | Homo sapiens (human) | IC50 | 1.2950 | 1 | 0 |
| diphenhydramine | Homo sapiens (human) | Ki | 0.3700 | 1 | 0 |
| domperidone | Homo sapiens (human) | IC50 | 0.0370 | 1 | 0 |
| domperidone | Homo sapiens (human) | Ki | 0.0110 | 1 | 0 |
| doxepin | Homo sapiens (human) | IC50 | 0.0380 | 1 | 0 |
| doxepin | Homo sapiens (human) | Ki | 0.0110 | 1 | 0 |
| droperidol | Homo sapiens (human) | IC50 | 0.0026 | 1 | 0 |
| droperidol | Homo sapiens (human) | Ki | 0.0007 | 1 | 0 |
| ebastine | Homo sapiens (human) | IC50 | 0.0904 | 1 | 0 |
| ebastine | Homo sapiens (human) | Ki | 0.0258 | 1 | 0 |
| econazole | Homo sapiens (human) | IC50 | 4.0340 | 1 | 0 |
| econazole | Homo sapiens (human) | Ki | 1.1520 | 1 | 0 |
| fenofibrate | Homo sapiens (human) | IC50 | 2.1180 | 1 | 0 |
| fenofibrate | Homo sapiens (human) | Ki | 0.6050 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | IC50 | 0.0051 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | Ki | 0.0015 | 1 | 0 |
| fluoxetine | Homo sapiens (human) | IC50 | 0.4520 | 2 | 1 |
| fluoxetine | Homo sapiens (human) | Ki | 0.0550 | 1 | 0 |
| guanfacine | Homo sapiens (human) | IC50 | 3.0140 | 1 | 0 |
| guanfacine | Homo sapiens (human) | Ki | 0.8610 | 1 | 0 |
| haloperidol | Homo sapiens (human) | IC50 | 0.1815 | 2 | 1 |
| haloperidol | Homo sapiens (human) | Ki | 0.1263 | 16 | 15 |
| haloprogin | Homo sapiens (human) | IC50 | 2.4210 | 1 | 0 |
| haloprogin | Homo sapiens (human) | Ki | 0.6920 | 1 | 0 |
| hydroxyzine | Homo sapiens (human) | Ki | 0.0500 | 1 | 1 |
| imipramine | Homo sapiens (human) | IC50 | 0.2200 | 1 | 1 |
| imipramine | Homo sapiens (human) | Ki | 0.1270 | 2 | 2 |
| ketanserin | Homo sapiens (human) | IC50 | 0.0184 | 16 | 16 |
| ketanserin | Homo sapiens (human) | Ki | 0.0016 | 12 | 12 |
| ketotifen | Homo sapiens (human) | IC50 | 0.0310 | 1 | 0 |
| ketotifen | Homo sapiens (human) | Ki | 0.0124 | 2 | 1 |
| loxapine | Homo sapiens (human) | Ki | 0.0024 | 1 | 1 |
| 2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one | Homo sapiens (human) | IC50 | 2.7960 | 1 | 0 |
| 2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one | Homo sapiens (human) | Ki | 0.7990 | 1 | 0 |
| maprotiline | Homo sapiens (human) | IC50 | 0.0640 | 1 | 0 |
| maprotiline | Homo sapiens (human) | Ki | 0.0150 | 2 | 1 |
| mescaline | Homo sapiens (human) | Ki | 0.5510 | 1 | 1 |
| methapyrilene | Homo sapiens (human) | IC50 | 0.6280 | 1 | 0 |
| methapyrilene | Homo sapiens (human) | Ki | 0.1800 | 1 | 0 |
| methiothepin | Homo sapiens (human) | Ki | 0.0020 | 1 | 1 |
| metoclopramide | Homo sapiens (human) | IC50 | 3.6750 | 1 | 0 |
| metoclopramide | Homo sapiens (human) | Ki | 1.0500 | 1 | 0 |
| mianserin | Homo sapiens (human) | IC50 | 0.0110 | 3 | 2 |
| mianserin | Homo sapiens (human) | Ki | 0.0070 | 11 | 12 |
| miconazole | Homo sapiens (human) | IC50 | 3.9070 | 1 | 0 |
| miconazole | Homo sapiens (human) | Ki | 1.1160 | 1 | 0 |
| mirtazapine | Homo sapiens (human) | Ki | 0.0386 | 2 | 2 |
| nefazodone | Homo sapiens (human) | Ki | 0.0058 | 1 | 1 |
| nisoxetine | Homo sapiens (human) | Ki | 0.0060 | 1 | 1 |
| nortriptyline | Homo sapiens (human) | IC50 | 0.0510 | 1 | 0 |
| nortriptyline | Homo sapiens (human) | Ki | 0.0150 | 1 | 0 |
| ondansetron | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| orphenadrine | Homo sapiens (human) | IC50 | 0.4360 | 1 | 0 |
| orphenadrine | Homo sapiens (human) | Ki | 0.1250 | 1 | 0 |
| oxymetazoline | Homo sapiens (human) | IC50 | 1.2850 | 1 | 0 |
| oxymetazoline | Homo sapiens (human) | Ki | 0.3670 | 1 | 0 |
| pentamidine | Homo sapiens (human) | IC50 | 1.6390 | 1 | 0 |
| pentamidine | Homo sapiens (human) | Ki | 0.4680 | 1 | 0 |
| prochlorperazine | Homo sapiens (human) | IC50 | 0.0071 | 1 | 0 |
| prochlorperazine | Homo sapiens (human) | Ki | 0.0020 | 1 | 0 |
| promazine | Homo sapiens (human) | IC50 | 0.0230 | 1 | 0 |
| promazine | Homo sapiens (human) | Ki | 0.0067 | 1 | 0 |
| promethazine | Homo sapiens (human) | IC50 | 0.0450 | 2 | 1 |
| promethazine | Homo sapiens (human) | Ki | 0.0190 | 1 | 0 |
| propafenone | Homo sapiens (human) | IC50 | 0.6540 | 1 | 0 |
| propafenone | Homo sapiens (human) | Ki | 0.1870 | 1 | 0 |
| propranolol | Homo sapiens (human) | IC50 | 3.2389 | 2 | 1 |
| propranolol | Homo sapiens (human) | Ki | 0.4190 | 1 | 0 |
| psilocin | Homo sapiens (human) | IC50 | 0.0083 | 1 | 1 |
| pyrilamine | Homo sapiens (human) | IC50 | 0.9970 | 1 | 0 |
| pyrilamine | Homo sapiens (human) | Ki | 0.2850 | 1 | 0 |
| quetiapine | Homo sapiens (human) | IC50 | 0.1178 | 1 | 0 |
| quetiapine | Homo sapiens (human) | Ki | 0.1311 | 9 | 8 |
| raloxifene | Homo sapiens (human) | IC50 | 1.4500 | 1 | 0 |
| raloxifene | Homo sapiens (human) | Ki | 0.4140 | 1 | 0 |
| rbi 257 | Homo sapiens (human) | Ki | 0.2730 | 1 | 1 |
| risperidone | Homo sapiens (human) | IC50 | 0.0016 | 3 | 3 |
| risperidone | Homo sapiens (human) | Ki | 0.0004 | 17 | 16 |
| ritanserin | Homo sapiens (human) | IC50 | 0.0025 | 1 | 3 |
| ritanserin | Homo sapiens (human) | Ki | 0.0004 | 3 | 4 |
| rizatriptan | Homo sapiens (human) | IC50 | 7.9433 | 1 | 1 |
| sb 206553 | Homo sapiens (human) | Ki | 1.8085 | 4 | 4 |
| spiperone | Homo sapiens (human) | Ki | 0.0021 | 3 | 3 |
| imatinib | Homo sapiens (human) | IC50 | 1.8910 | 1 | 0 |
| imatinib | Homo sapiens (human) | Ki | 0.5400 | 1 | 0 |
| sulconazole | Homo sapiens (human) | IC50 | 3.9290 | 1 | 0 |
| sulconazole | Homo sapiens (human) | Ki | 1.1220 | 1 | 0 |
| sumatriptan | Homo sapiens (human) | IC50 | 8.9716 | 2 | 2 |
| sumatriptan | Homo sapiens (human) | Ki | 0.6880 | 2 | 2 |
| terfenadine | Homo sapiens (human) | IC50 | 0.2550 | 1 | 0 |
| terfenadine | Homo sapiens (human) | Ki | 0.0730 | 1 | 0 |
| tetracaine | Homo sapiens (human) | IC50 | 3.4150 | 1 | 0 |
| tetracaine | Homo sapiens (human) | Ki | 0.9760 | 1 | 0 |
| thioridazine | Homo sapiens (human) | IC50 | 0.0044 | 1 | 0 |
| thioridazine | Homo sapiens (human) | Ki | 0.0426 | 2 | 1 |
| trazodone | Homo sapiens (human) | IC50 | 0.1315 | 2 | 1 |
| trazodone | Homo sapiens (human) | Ki | 0.0056 | 1 | 0 |
| zotepine | Homo sapiens (human) | Ki | 0.0012 | 4 | 4 |
| lysergic acid diethylamide | Homo sapiens (human) | Ki | 0.0033 | 5 | 5 |
| reserpine | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| phentolamine | Homo sapiens (human) | IC50 | 0.3590 | 1 | 0 |
| phentolamine | Homo sapiens (human) | Ki | 0.1030 | 1 | 0 |
| apomorphine | Homo sapiens (human) | Ki | 0.1200 | 1 | 1 |
| mepazine | Homo sapiens (human) | IC50 | 0.3850 | 1 | 0 |
| mepazine | Homo sapiens (human) | Ki | 0.1100 | 1 | 0 |
| n,n-dimethyltryptamine | Homo sapiens (human) | Ki | 0.0650 | 1 | 1 |
| cyclizine | Homo sapiens (human) | IC50 | 0.2250 | 1 | 0 |
| cyclizine | Homo sapiens (human) | Ki | 0.0640 | 1 | 0 |
| ergotamine | Homo sapiens (human) | IC50 | 0.0065 | 1 | 0 |
| ergotamine | Homo sapiens (human) | Ki | 0.0019 | 1 | 0 |
| methylergonovine | Homo sapiens (human) | IC50 | 0.0025 | 1 | 0 |
| methylergonovine | Homo sapiens (human) | Ki | 0.0007 | 1 | 0 |
| benzethonium chloride | Homo sapiens (human) | IC50 | 0.1290 | 1 | 0 |
| benzethonium chloride | Homo sapiens (human) | Ki | 0.0370 | 1 | 0 |
| sterogenol | Homo sapiens (human) | IC50 | 3.1730 | 1 | 0 |
| sterogenol | Homo sapiens (human) | Ki | 0.9070 | 1 | 0 |
| 2-chloroadenosine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| indopan | Homo sapiens (human) | Ki | 0.3875 | 1 | 2 |
| 2h-benzo(a)quinolizin-2-ol, 2-ethyl-1,3,4,6,7,11b-hexahydro-3-isobutyl-9,10-dimethoxy- | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| dibenzepin | Homo sapiens (human) | Ki | 7.2000 | 1 | 1 |
| methysergide | Homo sapiens (human) | IC50 | 0.0130 | 1 | 0 |
| methysergide | Homo sapiens (human) | Ki | 0.0069 | 2 | 1 |
| dihydroergotamine | Homo sapiens (human) | IC50 | 0.0080 | 1 | 0 |
| dihydroergotamine | Homo sapiens (human) | Ki | 0.0023 | 1 | 0 |
| dimenhydrinate | Homo sapiens (human) | IC50 | 0.6930 | 1 | 0 |
| dimenhydrinate | Homo sapiens (human) | Ki | 0.1980 | 1 | 0 |
| gentian violet | Homo sapiens (human) | IC50 | 2.6270 | 1 | 0 |
| gentian violet | Homo sapiens (human) | Ki | 0.7510 | 1 | 0 |
| 5-fluoro-alpha-methyltryptamine | Homo sapiens (human) | Ki | 0.0631 | 1 | 1 |
| azaperone | Homo sapiens (human) | Ki | 0.0542 | 2 | 4 |
| benperidol | Homo sapiens (human) | Ki | 0.0012 | 1 | 1 |
| glaucine | Homo sapiens (human) | Ki | 0.9660 | 2 | 2 |
| clemastine | Homo sapiens (human) | IC50 | 0.0320 | 1 | 0 |
| clemastine | Homo sapiens (human) | Ki | 0.0092 | 1 | 0 |
| pizotyline | Homo sapiens (human) | Ki | 0.0075 | 1 | 1 |
| danazol | Homo sapiens (human) | IC50 | 8.8500 | 1 | 0 |
| danazol | Homo sapiens (human) | Ki | 2.5280 | 1 | 0 |
| metergoline | Homo sapiens (human) | IC50 | 0.0004 | 1 | 0 |
| metergoline | Homo sapiens (human) | Ki | 0.0001 | 1 | 0 |
| lisuride | Homo sapiens (human) | IC50 | 0.0030 | 1 | 0 |
| lisuride | Homo sapiens (human) | Ki | 0.0009 | 1 | 0 |
| 2,4,5-trimethoxyphenylisopropylamine | Homo sapiens (human) | Ki | 0.6290 | 2 | 2 |
| bromocriptine | Homo sapiens (human) | IC50 | 0.0360 | 1 | 0 |
| bromocriptine | Homo sapiens (human) | Ki | 0.0100 | 1 | 0 |
| dexchlorpheniramine | Homo sapiens (human) | IC50 | 3.6920 | 1 | 0 |
| dexchlorpheniramine | Homo sapiens (human) | Ki | 1.0550 | 1 | 0 |
| penfluridol | Homo sapiens (human) | Ki | 0.3610 | 1 | 1 |
| 5-methoxy-alpha-methyltryptamine | Homo sapiens (human) | Ki | 0.0046 | 1 | 1 |
| butaclamol | Homo sapiens (human) | Ki | 0.0030 | 1 | 1 |
| bopindolol | Homo sapiens (human) | IC50 | 1.5810 | 1 | 0 |
| bopindolol | Homo sapiens (human) | Ki | 0.4520 | 1 | 0 |
| pergolide | Homo sapiens (human) | IC50 | 0.0140 | 1 | 0 |
| pergolide | Homo sapiens (human) | Ki | 0.0039 | 1 | 0 |
| quinpirole | Homo sapiens (human) | Ki | 25.0000 | 1 | 1 |
| gepirone | Homo sapiens (human) | Ki | 3.6300 | 1 | 1 |
| ipsapirone | Homo sapiens (human) | Ki | 14.9800 | 1 | 1 |
| sertindole | Homo sapiens (human) | Ki | 0.0007 | 2 | 2 |
| fananserin | Homo sapiens (human) | Ki | 0.0001 | 3 | 3 |
| aripiprazole | Homo sapiens (human) | IC50 | 1.9450 | 2 | 2 |
| aripiprazole | Homo sapiens (human) | Ki | 0.0140 | 21 | 22 |
| ziprasidone | Homo sapiens (human) | IC50 | 0.0004 | 1 | 1 |
| ziprasidone | Homo sapiens (human) | Ki | 0.0005 | 7 | 7 |
| 2,5-dimethoxy-4-bromoamphetamine | Homo sapiens (human) | Ki | 0.0275 | 3 | 3 |
| 2,5-dimethoxyamphetamine | Homo sapiens (human) | Ki | 2.7055 | 2 | 2 |
| esreboxetine | Homo sapiens (human) | Ki | 0.0003 | 1 | 1 |
| spiramide | Homo sapiens (human) | IC50 | 0.0003 | 1 | 1 |
| sertraline | Homo sapiens (human) | IC50 | 2.7409 | 1 | 0 |
| sertraline | Homo sapiens (human) | Ki | 0.7831 | 1 | 0 |
| mdl 11939 | Homo sapiens (human) | Ki | 0.0025 | 2 | 3 |
| ergocornine | Homo sapiens (human) | IC50 | 0.0280 | 1 | 0 |
| ergocornine | Homo sapiens (human) | Ki | 0.0080 | 1 | 0 |
| 3,3-diphenylpropylamine | Homo sapiens (human) | Ki | 7.5860 | 2 | 3 |
| 2-(4-bromo-2,5-dimethoxyphenyl)ethylamine | Homo sapiens (human) | Ki | 0.0119 | 3 | 3 |
| 5'-n-methylcarboxamideadenosine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| lobeline | Homo sapiens (human) | Ki | 7.4000 | 1 | 1 |
| u 74006f | Homo sapiens (human) | IC50 | 2.0020 | 1 | 0 |
| u 74006f | Homo sapiens (human) | Ki | 0.5720 | 1 | 0 |
| gr 127935 | Homo sapiens (human) | Ki | 0.0293 | 2 | 2 |
| 6-chloro-2-(1-piperazinyl)pyrazine | Homo sapiens (human) | Ki | 20.9465 | 1 | 2 |
| 5-methoxy 3-(1,2,3,6-tetrahydro-4-pyridinyl)1h indole | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| paliperidone | Homo sapiens (human) | IC50 | 0.0052 | 1 | 1 |
| 3-n-methylspiperone | Homo sapiens (human) | Ki | 0.0088 | 1 | 1 |
| sb 204070a | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| n(6)-(3-iodobenzyl)-5'-n-methylcarboxamidoadenosine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| dihydrotetrabenazine | Homo sapiens (human) | Ki | 0.0067 | 1 | 1 |
| desloratadine | Homo sapiens (human) | IC50 | 0.0330 | 1 | 0 |
| desloratadine | Homo sapiens (human) | Ki | 0.0094 | 1 | 0 |
| sc 53116 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sc 53116 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| sonepiprazole | Homo sapiens (human) | Ki | 1.6000 | 1 | 1 |
| l 741626 | Homo sapiens (human) | Ki | 0.6950 | 1 | 1 |
| alpha-ergocryptine | Homo sapiens (human) | IC50 | 0.0470 | 1 | 0 |
| alpha-ergocryptine | Homo sapiens (human) | Ki | 0.0140 | 1 | 0 |
| lubazodone hydrochloride | Homo sapiens (human) | Ki | 0.0860 | 1 | 1 |
| didesipramine | Homo sapiens (human) | Ki | 0.3970 | 1 | 1 |
| n-demethyllysergic acid diethylamide | Homo sapiens (human) | IC50 | 0.0060 | 1 | 1 |
| 5,6,7,8-tetrahydro-4h-isoxazolo(4,5-d)azepin-3-ol | Homo sapiens (human) | Ki | 308.1140 | 1 | 2 |
| piboserod | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 0.8320 | 1 | 1 |
| maduramicin | Homo sapiens (human) | IC50 | 0.0087 | 1 | 0 |
| maduramicin | Homo sapiens (human) | Ki | 0.0025 | 1 | 0 |
| latrepirdine | Homo sapiens (human) | Ki | 0.0617 | 1 | 1 |
| lurasidone | Homo sapiens (human) | Ki | 0.0020 | 1 | 1 |
| sorafenib | Homo sapiens (human) | Ki | 1.9590 | 1 | 1 |
| nafronyloxalate | Homo sapiens (human) | Ki | 0.2938 | 1 | 2 |
| terconazole | Homo sapiens (human) | IC50 | 8.1750 | 1 | 0 |
| terconazole | Homo sapiens (human) | Ki | 2.3360 | 1 | 0 |
| sb 221284 | Homo sapiens (human) | Ki | 0.3981 | 2 | 2 |
| sb 228357 | Homo sapiens (human) | Ki | 0.1259 | 1 | 1 |
| sb 243213 | Homo sapiens (human) | IC50 | 0.0324 | 1 | 1 |
| sb 243213 | Homo sapiens (human) | Ki | 0.1585 | 3 | 3 |
| ergonovine | Homo sapiens (human) | IC50 | 0.0022 | 1 | 0 |
| ergonovine | Homo sapiens (human) | Ki | 0.0006 | 1 | 0 |
| dihydroergocristine monomesylate | Homo sapiens (human) | IC50 | 0.0150 | 1 | 0 |
| dihydroergocristine monomesylate | Homo sapiens (human) | Ki | 0.0042 | 1 | 0 |
| adenosine-5'-(n-ethylcarboxamide) | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| diethylstilbestrol | Homo sapiens (human) | IC50 | 4.7900 | 1 | 0 |
| diethylstilbestrol | Homo sapiens (human) | Ki | 1.3690 | 1 | 0 |
| 3,4,5-trimethoxycinnamic acid | Homo sapiens (human) | IC50 | 10.0000 | 2 | 2 |
| flunarizine | Homo sapiens (human) | IC50 | 0.4070 | 1 | 0 |
| flunarizine | Homo sapiens (human) | Ki | 0.1160 | 1 | 0 |
| benztropine | Homo sapiens (human) | IC50 | 0.0240 | 1 | 0 |
| benztropine | Homo sapiens (human) | Ki | 0.0070 | 1 | 0 |
| cinnarizine | Homo sapiens (human) | IC50 | 0.3600 | 1 | 0 |
| cinnarizine | Homo sapiens (human) | Ki | 0.1030 | 1 | 0 |
| enclomiphene | Homo sapiens (human) | IC50 | 3.3080 | 1 | 0 |
| enclomiphene | Homo sapiens (human) | Ki | 0.9450 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | IC50 | 4.8010 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | Ki | 1.3720 | 1 | 0 |
| dapiprazole | Homo sapiens (human) | IC50 | 0.6060 | 1 | 0 |
| dapiprazole | Homo sapiens (human) | Ki | 0.1730 | 1 | 0 |
| altanserin | Homo sapiens (human) | Ki | 0.0002 | 2 | 2 |
| mitragynine | Homo sapiens (human) | Ki | 5.0100 | 1 | 1 |
| 2-chloro-n(6)-(3-iodobenzyl)adenosine-5'-n-methyluronamide | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| paynantheine | Homo sapiens (human) | Ki | 0.8150 | 1 | 1 |
| bp 897 | Homo sapiens (human) | Ki | 0.8400 | 2 | 2 |
| ym348 | Homo sapiens (human) | Ki | 0.0130 | 2 | 2 |
| ro 60-0175 | Homo sapiens (human) | Ki | 0.0367 | 4 | 4 |
| n-(1-methyl-5-indolyl)-n'-(3-methyl-5-isothiazolyl)urea | Homo sapiens (human) | Ki | 6.3096 | 2 | 2 |
| sb-224289 | Homo sapiens (human) | Ki | 1.5849 | 1 | 1 |
| sb 242084 | Homo sapiens (human) | Ki | 0.1585 | 4 | 4 |
| pd 168,077 | Homo sapiens (human) | Ki | 4.0100 | 1 | 1 |
| ly 367265 | Homo sapiens (human) | Ki | 0.0008 | 2 | 2 |
| genistein | Homo sapiens (human) | IC50 | 10.4690 | 1 | 0 |
| genistein | Homo sapiens (human) | Ki | 2.9910 | 1 | 0 |
| l 745870 | Homo sapiens (human) | Ki | 0.4632 | 4 | 4 |
| mdl 100907 | Homo sapiens (human) | IC50 | 0.0048 | 1 | 2 |
| mdl 100907 | Homo sapiens (human) | Ki | 0.0005 | 8 | 8 |
| sb 200646a | Homo sapiens (human) | Ki | 6.3096 | 2 | 2 |
| sb 258719 | Homo sapiens (human) | Ki | 15.8489 | 1 | 1 |
| sb 271046 | Homo sapiens (human) | Ki | 2.1259 | 2 | 2 |
| oxiconazole | Homo sapiens (human) | IC50 | 4.1630 | 1 | 0 |
| oxiconazole | Homo sapiens (human) | Ki | 1.1894 | 1 | 0 |
| cinanserin | Homo sapiens (human) | Ki | 0.0190 | 4 | 4 |
| guanabenz | Homo sapiens (human) | IC50 | 0.3920 | 1 | 0 |
| guanabenz | Homo sapiens (human) | Ki | 0.1120 | 1 | 0 |
| 1-(3-(5-(1,2,4-triazol-4-yl)-1h-indol-3-yl)propyl)-4-(2-(3-fluorophenyl)ethyl)piperazine | Homo sapiens (human) | IC50 | 0.3700 | 1 | 1 |
| jl 13 compound | Homo sapiens (human) | Ki | 0.2040 | 1 | 1 |
| 1-methyl-d-lysergic acid butanolamide | Homo sapiens (human) | Ki | 0.0016 | 1 | 1 |
| sb 269970 | Homo sapiens (human) | Ki | 6.6683 | 3 | 3 |
| 2-ethyl-5-methoxy-n,n-dimethyltryptamine | Homo sapiens (human) | IC50 | 0.6200 | 1 | 1 |
| n-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide | Homo sapiens (human) | Ki | 7.9433 | 1 | 1 |
| 4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamine | Homo sapiens (human) | Ki | 1.4454 | 1 | 1 |
| cp 293019 | Homo sapiens (human) | IC50 | 0.1500 | 1 | 1 |
| cp 293019 | Homo sapiens (human) | Ki | 0.5000 | 1 | 1 |
| n-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)-4-(pyridin-2-yl)benzamide | Homo sapiens (human) | Ki | 0.0229 | 1 | 1 |
| 4-iodo-2,5-dimethoxyphenylisopropylamine, (r)-isomer | Homo sapiens (human) | Ki | 0.0037 | 2 | 2 |
| l 772405 | Homo sapiens (human) | IC50 | 1.1000 | 1 | 1 |
| sb258741 | Homo sapiens (human) | Ki | 5.0119 | 1 | 1 |
| slv 313 | Homo sapiens (human) | Ki | 0.2512 | 1 | 1 |
| fauc 346 | Homo sapiens (human) | Ki | 0.2350 | 2 | 2 |
| ngb 2904 | Homo sapiens (human) | Ki | 0.6790 | 1 | 1 |
| 2-(3-chlorobenzyloxy)-6-(piperazin-1-yl)pyrazine | Homo sapiens (human) | Ki | 0.0811 | 1 | 2 |
| 4-(3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl)-1-(4-fluorophenyl)butan-1-one | Homo sapiens (human) | Ki | 0.1586 | 2 | 4 |
| pnu 109291 | Homo sapiens (human) | Ki | 0.1680 | 2 | 2 |
| pnu 96415e | Homo sapiens (human) | Ki | 0.0058 | 1 | 1 |
| 4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| 1-phenyl-3-dimethylamino-1,2,3,4-tetrahydronaphthalene | Homo sapiens (human) | Ki | 0.4700 | 1 | 1 |
| sb-656104-a | Homo sapiens (human) | Ki | 0.0631 | 1 | 1 |
| pimavanserin | Homo sapiens (human) | IC50 | 0.0335 | 5 | 6 |
| pimavanserin | Homo sapiens (human) | Ki | 0.0009 | 2 | 3 |
| 5-chloro-2-methyl-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1h-indole | Homo sapiens (human) | IC50 | 0.2400 | 1 | 1 |
| gsk215083 | Homo sapiens (human) | Ki | 0.0004 | 1 | 1 |
| fauc 365 | Homo sapiens (human) | Ki | 1.0085 | 2 | 2 |
| sb-649915 | Homo sapiens (human) | Ki | 3.1623 | 1 | 1 |
| 11-hydroxy-n-(n-propyl)noraporphine hydrochloride, (r)-isomer | Homo sapiens (human) | Ki | 0.1140 | 1 | 1 |
| way-208466 | Homo sapiens (human) | IC50 | 0.3510 | 1 | 1 |
| 9-(aminomethyl)-9,10-dihydroanthracene | Homo sapiens (human) | Ki | 0.0438 | 8 | 9 |
| n-cyclopropyl adenosine-5'-carboxamide | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 1-(2,4-difluorophenethyl)-4-(4-fluorophenylsulfonyl)piperidine | Homo sapiens (human) | Ki | 0.0004 | 4 | 4 |
| cariprazine | Homo sapiens (human) | Ki | 0.0775 | 6 | 7 |
| barettin | Homo sapiens (human) | Ki | 1.9300 | 1 | 1 |
| sb 742457 | Homo sapiens (human) | Ki | 0.0260 | 1 | 1 |
| naluzotan | Homo sapiens (human) | Ki | 2.0000 | 1 | 1 |
| pg 01037 | Homo sapiens (human) | Ki | 0.0624 | 1 | 1 |
| lorcaserin | Homo sapiens (human) | Ki | 0.6212 | 5 | 5 |
| td-5108 | Homo sapiens (human) | Ki | 0.1000 | 1 | 1 |
| brexpiprazole | Homo sapiens (human) | Ki | 0.0005 | 2 | 2 |
| 4-(4-chlorophenyl)sulfonyl-5-(3,4-dihydro-1H-isoquinolin-2-yl)-2-ethylsulfonylthiazole | Homo sapiens (human) | Ki | 0.3055 | 2 | 2 |
| 2,5-dimethoxy-4-bromoamphetamine, (r)-isomer | Homo sapiens (human) | Ki | 0.0003 | 1 | 1 |
| mitragynine | Homo sapiens (human) | Ki | 1.3200 | 1 | 1 |
| af 353 | Homo sapiens (human) | Ki | 100,000.0000 | 1 | 1 |
| a 803467 | Homo sapiens (human) | IC50 | 2.5000 | 2 | 2 |
| sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| lu ae58054 | Homo sapiens (human) | Ki | 0.7910 | 1 | 1 |
| 2,5-dimethoxy-4-bromoamphetamine, (s)-isomer | Homo sapiens (human) | Ki | 0.0019 | 1 | 1 |
| pf 04457845 | Homo sapiens (human) | Ki | 0.2495 | 2 | 0 |
| e-55888 | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| n-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide | Homo sapiens (human) | Ki | 0.6260 | 1 | 1 |
| nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| skepinone-l | Homo sapiens (human) | Ki | 3.7111 | 1 | 0 |
| n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 2.3083 | 2 | 5 |
| rk 682 | Homo sapiens (human) | IC50 | 17.0000 | 1 | 1 |
| tg6-10-1 | Homo sapiens (human) | IC50 | 75.0000 | 1 | 1 |
| clozapine | Homo sapiens (human) | IC50 | 0.0658 | 3 | 4 |
| clozapine | Homo sapiens (human) | Ki | 0.0156 | 34 | 37 |
| olanzapine | Homo sapiens (human) | IC50 | 0.0380 | 3 | 2 |
| olanzapine | Homo sapiens (human) | Ki | 0.0036 | 21 | 21 |
| tegaserod | Homo sapiens (human) | Ki | 0.1000 | 1 | 1 |
| aplysinopsin | Homo sapiens (human) | Ki | 0.5980 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
Potential modes of interaction of 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives with the 5-HT2A receptor: a ligand structure-affinity relationship, receptor mutagenesis and receptor modeling investigation.Journal of medicinal chemistry, , Nov-13, Volume: 51, Issue:21, 2008
Geometry-affinity relationships of the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene.Journal of medicinal chemistry, , Apr-11, Volume: 45, Issue:8, 2002
The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The "Phenylalkylaminome" with a Focus on Selected Drugs of Abuse.Journal of medicinal chemistry, , 04-13, Volume: 60, Issue:7, 2017
Synthesis and pharmacological evaluation of N-benzyl substituted 4-bromo-2,5-dimethoxyphenethylamines as 5-HT2A/2C partial agonists.Bioorganic & medicinal chemistry, , Jul-15, Volume: 23, Issue:14, 2015
Potential modes of interaction of 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives with the 5-HT2A receptor: a ligand structure-affinity relationship, receptor mutagenesis and receptor modeling investigation.Journal of medicinal chemistry, , Nov-13, Volume: 51, Issue:21, 2008
High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand.Bioorganic & medicinal chemistry, , Jun-01, Volume: 16, Issue:11, 2008
A novel (benzodifuranyl)aminoalkane with extremely potent activity at the 5-HT2A receptor.Journal of medicinal chemistry, , Dec-17, Volume: 41, Issue:26, 1998
[no title available]European journal of medicinal chemistry, , May-05, Volume: 235, 2022
Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5-HTJournal of medicinal chemistry, , 07-27, Volume: 60, Issue:14, 2017
Tetrahydroquinoline-based tricyclic amines as potent and selective agonists of the 5-HTBioorganic & medicinal chemistry letters, , 12-15, Volume: 26, Issue:24, 2016
The influence of 5-HT(2A) activity on a 5-HT(2C) specific in vivo assay used for early identification of multiple acting SERT and 5-HT(2C) receptor ligands.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 26, Issue:3, 2016
Novel pyrimidoazepine analogs as serotonin 5-HT(2A) and 5-HT(2C) receptor ligands for the treatment of obesity.European journal of medicinal chemistry, , Volume: 63, 2013
Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 20, Issue:3, 2010
Design and synthesis of pyridazinone-based 5-HT(2C) agonists.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 19, Issue:19, 2009
Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity.Journal of medicinal chemistry, , Jan-24, Volume: 51, Issue:2, 2008
Discovery of (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol- 6(2H)-one, a selective, orally active agonist of the 5-HT(2C) receptor.Journal of medicinal chemistry, , Mar-22, Volume: 50, Issue:6, 2007
Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.Bioorganic & medicinal chemistry letters, , Volume: 16, Issue:3, 2006
Indoline derivatives as 5-HT(2C) receptor agonists.Bioorganic & medicinal chemistry letters, , May-03, Volume: 14, Issue:9, 2004
Improved Metabolically Stable 5-HT Receptor Modulators and the Development of New Antidepressants.ACS medicinal chemistry letters, , Apr-14, Volume: 13, Issue:4, 2022
The Psychedelic Renaissance: Addressing Potential Adverse Effects in a Therapeutic Setting.ACS medicinal chemistry letters, , Dec-09, Volume: 12, Issue:12, 2021
1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
Influence of amine substituents on 5-HT2A versus 5-HT2C binding of phenylalkyl- and indolylalkylamines.Journal of medicinal chemistry, , Jun-24, Volume: 37, Issue:13, 1994
Serotonin receptor binding affinities of several hallucinogenic phenylalkylamine and N,N-dimethyltryptamine analogues.Journal of medicinal chemistry, , Volume: 21, Issue:8, 1978
Alpha-ethyltryptamines as dual dopamine-serotonin releasers.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 24, Issue:19, 2014
Influence of amine substituents on 5-HT2A versus 5-HT2C binding of phenylalkyl- and indolylalkylamines.Journal of medicinal chemistry, , Jun-24, Volume: 37, Issue:13, 1994
[no title available]Bioorganic & medicinal chemistry letters, , 06-15, Volume: 28, Issue:11, 2018
1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry.Journal of medicinal chemistry, , 03-22, Volume: 61, Issue:6, 2018
Synthesis and serotonin receptor activity of the arylpiperazine alkyl/propoxy derivatives of new azatricycloundecanes.European journal of medicinal chemistry, , Volume: 44, Issue:1, 2009
[no title available],
[no title available]Journal of medicinal chemistry, , 09-09, Volume: 64, Issue:17, 2021
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 24, Issue:2, 2014
Polypharmacology - foe or friend?Journal of medicinal chemistry, , Nov-27, Volume: 56, Issue:22, 2013
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
[no title available],
Discovery of TD-8954, a clinical stage 5-HT(4) receptor agonist with gastrointestinal prokinetic properties.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 23, Issue:14, 2013
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],
Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
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
Influence of chain length and N-alkylation on the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene.Bioorganic & medicinal chemistry letters, , Mar-12, Volume: 11, Issue:5, 2001
[no title available],
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
Influence of chain length and N-alkylation on the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene.Bioorganic & medicinal chemistry letters, , Mar-12, Volume: 11, Issue:5, 2001
[no title available]Journal of medicinal chemistry, , 09-09, Volume: 64, Issue:17, 2021
[no title available]European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Further evaluation of the tropane analogs of haloperidol.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 24, Issue:17, 2014
Synthesis and biological evaluation of a series of aminoalkyl-tetralones and tetralols as dual dopamine/serotonin ligands.European journal of medicinal chemistry, , Volume: 71, 2014
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 19, Issue:21, 2009
Synthesis, binding affinity, and molecular docking analysis of new benzofuranone derivatives as potential antipsychotics.Journal of medicinal chemistry, , Oct-09, Volume: 51, Issue:19, 2008
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 17, Issue:17, 2007
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics.Bioorganic & medicinal chemistry letters, , Feb-09, Volume: 14, Issue:3, 2004
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic?Bioorganic & medicinal chemistry letters, , May-21, Volume: 11, Issue:10, 2001
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
[no title available],
Polypharmacology - foe or friend?Journal of medicinal chemistry, , Nov-27, Volume: 56, Issue:22, 2013
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
Influence of chain length and N-alkylation on the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene.Bioorganic & medicinal chemistry letters, , Mar-12, Volume: 11, Issue:5, 2001
Therapeutic progression of quinazolines as targeted chemotherapeutic agents.European journal of medicinal chemistry, , Feb-05, Volume: 211, 2021
[no title available]European journal of medicinal chemistry, , Dec-01, Volume: 207, 2020
[no title available]European journal of medicinal chemistry, , Aug-15, Volume: 176, 2019
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
[no title available]European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Synthesis and evaluation of nuciferine and roemerine enantiomers as 5-HTMedChemComm, , Mar-01, Volume: 9, Issue:3, 2018
Synthesis and Discovery of Arylpiperidinylquinazolines: New Inhibitors of the Vesicular Monoamine Transporter.Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
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
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
Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 25, Issue:22, 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
Novel pyrimidoazepine analogs as serotonin 5-HT(2A) and 5-HT(2C) receptor ligands for the treatment of obesity.European journal of medicinal chemistry, , Volume: 63, 2013
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 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
Affinity of aporphines for the human 5-HT2A receptor: insights from homology modeling and molecular docking studies.Bioorganic & medicinal chemistry, , Aug-01, Volume: 18, Issue:15, 2010
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
(+/-)-Nantenine analogs as antagonists at human 5-HT(2A) receptors: C1 and flexible congeners.Bioorganic & medicinal chemistry letters, , May-01, Volume: 19, Issue:9, 2009
Potential modes of interaction of 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives with the 5-HT2A receptor: a ligand structure-affinity relationship, receptor mutagenesis and receptor modeling investigation.Journal of medicinal chemistry, , Nov-13, Volume: 51, Issue:21, 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
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
Multifunctional 6-fluoro-3-[3-(pyrrolidin-1-yl)propyl]-1,2-benzoxazoles targeting behavioral and psychological symptoms of dementia (BPSD).European journal of medicinal chemistry, , Apr-01, Volume: 191, 2020
Synthesis of new 5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HTEuropean journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HTEuropean journal of medicinal chemistry, , Mar-15, Volume: 166, 2019
5-HTBioorganic & medicinal chemistry, , 01-15, Volume: 26, Issue:2, 2018
[no title available]Bioorganic & medicinal chemistry letters, , 06-15, Volume: 28, Issue:11, 2018
Development of selective agents targeting serotonin 5HTMedChemComm, , Aug-01, Volume: 8, Issue:8, 2017
Synthesis of a new series of aryl/heteroarylpiperazinyl derivatives of 8-acetyl-7-hydroxy-4-methylcoumarin with low nanomolar 5-HTEuropean journal of medicinal chemistry, , Sep-08, Volume: 137, 2017
Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
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
[no title available],
Design, synthesis and evaluation of activity and pharmacokinetic profile of new derivatives of xanthone and piperazine in the central nervous system.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 29, Issue:21, 2019
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Novel DEuropean journal of medicinal chemistry, , Mar-15, Volume: 232, 2022
3-Pyrrolidine-indole Derivatives as 5-HT2-Selective Receptor Modulators for the Potential Treatment of Mental Disorders.ACS medicinal chemistry letters, , May-12, Volume: 13, Issue:5, 2022
Improved Metabolically Stable 5-HT Receptor Modulators and the Development of New Antidepressants.ACS medicinal chemistry letters, , Apr-14, Volume: 13, Issue:4, 2022
Restoration of Motor Function Post-Neurological Injury Using Serotonergic Agonist.ACS medicinal chemistry letters, , Sep-08, Volume: 13, Issue:9, 2022
Psilocin Derivatives as Serotonergic Psychedelic Agents for the Treatment of CNS Disorders.ACS medicinal chemistry letters, , Oct-14, Volume: 12, Issue:10, 2021
The Psychedelic Renaissance: Addressing Potential Adverse Effects in a Therapeutic Setting.ACS medicinal chemistry letters, , Dec-09, Volume: 12, Issue:12, 2021
Improved 5-HT2 Selective Receptor Modulators for the Treatment of Psychological Disorders.ACS medicinal chemistry letters, , Dec-09, Volume: 12, Issue:12, 2021
Synthesis and Biological Evaluation of Tryptamines Found in Hallucinogenic Mushrooms: Norbaeocystin, Baeocystin, Norpsilocin, and Aeruginascin.Journal of natural products, , 02-28, Volume: 83, Issue:2, 2020
SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 15, Issue:20, 2005
[no title available]Journal of medicinal chemistry, , 09-09, Volume: 64, Issue:17, 2021
Synthesis and biological investigation of new equatorial (β) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile.Bioorganic & medicinal chemistry, , 09-15, Volume: 24, Issue:18, 2016
New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
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
Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic?Bioorganic & medicinal chemistry letters, , May-21, Volume: 11, Issue:10, 2001
[no title available],
Return of DJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 40, 2021
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.Bioorganic & medicinal chemistry letters, , 10-15, Volume: 30, Issue:20, 2020
Discovery of aryl-piperidine derivatives as potential antipsychotic agents using molecular hybridization strategy.European journal of medicinal chemistry, , May-01, Volume: 193, 2020
[no title available]European journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
[no title available]European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics.Bioorganic & medicinal chemistry, , 09-01, Volume: 25, Issue:17, 2017
Synthesis and biological evaluation of a series of aminoalkyl-tetralones and tetralols as dual dopamine/serotonin ligands.European journal of medicinal chemistry, , Volume: 71, 2014
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
Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.Journal of medicinal chemistry, , Nov-26, Volume: 57, Issue:22, 2014
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 19, Issue:21, 2009
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 17, Issue:17, 2007
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics.Bioorganic & medicinal chemistry letters, , Feb-09, Volume: 14, Issue:3, 2004
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],
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
Identification of a novel DGKα inhibitor for XLP-1 therapy by virtual screening.European journal of medicinal chemistry, , Feb-15, Volume: 164, 2019
Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-103), a novel 5-hydroxytryptamine(2A) receptor inverse agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 317, Issue:2, 2006
Novel and selective 5-HT2C/2B receptor antagonists as potential anxiolytic agents: synthesis, quantitative structure-activity relationships, and molecular modeling of substituted 1-(3-pyridylcarbamoyl)indolines.Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998
6-Chloro-5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]- indoline (SB-242084): the first selective and brain penetrant 5-HT2C receptor antagonist.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
Potent, selective tetrahydro-beta-carboline antagonists of the serotonin 2B (5HT2B) contractile receptor in the rat stomach fundus.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
5-Methyl-1-(3-pyridylcarbamoyl)-1,2,3,5-tetrahydropyrrolo[2,3-f]indole: a novel 5-HT2C/5-HT2B receptor antagonist with improved affinity, selectivity, and oral activity.Journal of medicinal chemistry, , Jul-07, Volume: 38, Issue:14, 1995
Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
Asymmetric total synthesis and identification of tetrahydroprotoberberine derivatives as new antipsychotic agents possessing a dopamine D(1), D(2) and serotonin 5-HT(1A) multi-action profile.Bioorganic & medicinal chemistry, , Feb-15, Volume: 21, Issue:4, 2013
Design, synthesis, and pharmacological evaluation of novel tetrahydroprotoberberine derivatives: selective inhibitors of dopamine D₁ receptor.Bioorganic & medicinal chemistry, , Aug-01, Volume: 20, Issue:15, 2012
Isochroman-6-carboxamides as highly selective 5-HT1D agonists: potential new treatment for migraine without cardiovascular side effects.Journal of medicinal chemistry, , Jun-18, Volume: 41, Issue:13, 1998
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.Journal of medicinal chemistry, , May-12, Volume: 38, Issue:10, 1995
5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist.Journal of medicinal chemistry, , Sep-02, Volume: 37, Issue:18, 1994
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
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
Discovery of β-Arrestin-Biased 25CN-NBOH-Derived 5-HTJournal of medicinal chemistry, , 09-22, Volume: 65, Issue:18, 2022
High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand.Bioorganic & medicinal chemistry, , Jun-01, Volume: 16, Issue:11, 2008
A novel ergot alkaloid as a 5-HT(1A) inhibitor produced by Dicyma sp.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Improved Metabolically Stable 5-HT Receptor Modulators and the Development of New Antidepressants.ACS medicinal chemistry letters, , Apr-14, Volume: 13, Issue:4, 2022
The Psychedelic Renaissance: Addressing Potential Adverse Effects in a Therapeutic Setting.ACS medicinal chemistry letters, , Dec-09, Volume: 12, Issue:12, 2021
Thieno[3,2-b]- and thieno[2,3-b]pyrrole bioisosteric analogues of the hallucinogen and serotonin agonist N,N-dimethyltryptamine.Journal of medicinal chemistry, , Mar-25, Volume: 42, Issue:6, 1999
Alpha-ethyltryptamines as dual dopamine-serotonin releasers.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 24, Issue:19, 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
Alpha-ethyltryptamines as dual dopamine-serotonin releasers.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 24, Issue:19, 2014
Novel agonists of 5HT2C receptors. Synthesis and biological evaluation of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2-b]pyrrol-1-yl)-1-methylethylamines. Improved therapeutics for obsessive compulsive disorder.Journal of medicinal chemistry, , Aug-15, Volume: 40, Issue:17, 1997
Semisynthetic Transformations on (+)-Boldine Reveal a 5-HTJournal of natural products, , 09-23, Volume: 85, Issue:9, 2022
Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors.Journal of natural products, , Apr-24, Volume: 78, Issue:4, 2015
The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The "Phenylalkylaminome" with a Focus on Selected Drugs of Abuse.Journal of medicinal chemistry, , 04-13, Volume: 60, Issue:7, 2017
Potential modes of interaction of 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives with the 5-HT2A receptor: a ligand structure-affinity relationship, receptor mutagenesis and receptor modeling investigation.Journal of medicinal chemistry, , Nov-13, Volume: 51, Issue:21, 2008
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Understanding the structure-activity relationship of the human ether-a-go-go-related gene cardiac K+ channel. A model for bad behavior.Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
N-[(3S)-1-benzylpyrrolidin-3-yl]-(2-thienyl)benzamides: human dopamine D4 ligands with high affinity for the 5-HT2A receptor.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 15, Issue:23, 2005
4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists.Journal of medicinal chemistry, , Jan-17, Volume: 45, Issue:2, 2002
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
Novel DEuropean journal of medicinal chemistry, , Mar-15, Volume: 232, 2022
[no title available]European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
New dual 5-HT1A and 5-HT7 receptor ligands derived from SYA16263.European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
A study of the structure-affinity relationship in SYA16263; is a DBioorganic & medicinal chemistry, , 01-15, Volume: 30, 2021
2-Phenylcyclopropylmethylamine Derivatives as Dopamine DJournal of medicinal chemistry, , 12-09, Volume: 64, Issue:23, 2021
Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 40, 2021
[no title available]European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Synthesis and biological evaluation of a series of novel pyridinecarboxamides as potential multi-receptor antipsychotic drugs.Bioorganic & medicinal chemistry letters, , 02-15, Volume: 28, Issue:4, 2018
[no title available]European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Discovery of G Protein-Biased Dopaminergics with a Pyrazolo[1,5-a]pyridine Substructure.Journal of medicinal chemistry, , 04-13, Volume: 60, Issue:7, 2017
Hydroxy-Substituted Heteroarylpiperazines: Novel Scaffolds for β-Arrestin-Biased DJournal of medicinal chemistry, , 06-08, Volume: 60, Issue:11, 2017
β-Arrestin biased dopamine D2 receptor partial agonists: Synthesis and pharmacological evaluation.Bioorganic & medicinal chemistry, , 10-15, Volume: 25, Issue:20, 2017
Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 26, Issue:13, 2016
Design and synthesis of dual 5-HT1A and 5-HT7 receptor ligands.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 25, Issue:18, 2015
1,4-Disubstituted aromatic piperazines with high 5-HT2A/D2 selectivity: Quantitative structure-selectivity investigations, docking, synthesis and biological evaluation.Bioorganic & medicinal chemistry, , Sep-15, Volume: 23, Issue:18, 2015
Functionally selective dopamine D₂, D₃ receptor partial agonists.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.Journal of medicinal chemistry, , Nov-26, Volume: 57, Issue:22, 2014
Antidepressant and antipsychotic activity of new quinoline- and isoquinoline-sulfonamide analogs of aripiprazole targeting serotonin 5-HT₁A/5-HT₂A/5-HT₇ and dopamine D₂/D₃ receptors.European journal of medicinal chemistry, , Volume: 60, 2013
Design and synthesis of novel arylpiperazine derivatives containing the imidazole core targeting 5-HT(2A) receptor and 5-HT transporter.Journal of medicinal chemistry, , Sep-22, Volume: 54, Issue:18, 2011
Discovery of PF-00217830: aryl piperazine napthyridinones as D2 partial agonists for schizophrenia and bipolar disorder.Bioorganic & medicinal chemistry letters, , May-01, Volume: 21, Issue:9, 2011
6-Alkoxyisoindolin-1-one based dopamine D2 partial agonists as potential antipsychotics.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 20, Issue:19, 2010
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
[no title available]Journal of medicinal chemistry, , Aug-09, Volume: 61, Issue:15, 2018
[no title available]European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Polypharmacology - foe or friend?Journal of medicinal chemistry, , Nov-27, Volume: 56, Issue:22, 2013
1-Aminoindanes as novel motif with potential atypical antipsychotic properties.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 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
The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The "Phenylalkylaminome" with a Focus on Selected Drugs of Abuse.Journal of medicinal chemistry, , 04-13, Volume: 60, Issue:7, 2017
Potential modes of interaction of 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives with the 5-HT2A receptor: a ligand structure-affinity relationship, receptor mutagenesis and receptor modeling investigation.Journal of medicinal chemistry, , Nov-13, Volume: 51, Issue:21, 2008
Influence of amine substituents on 5-HT2A versus 5-HT2C binding of phenylalkyl- and indolylalkylamines.Journal of medicinal chemistry, , Jun-24, Volume: 37, Issue:13, 1994
The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The "Phenylalkylaminome" with a Focus on Selected Drugs of Abuse.Journal of medicinal chemistry, , 04-13, Volume: 60, Issue:7, 2017
Potential modes of interaction of 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives with the 5-HT2A receptor: a ligand structure-affinity relationship, receptor mutagenesis and receptor modeling investigation.Journal of medicinal chemistry, , Nov-13, Volume: 51, Issue:21, 2008
Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
1-Aminomethylbenzocycloalkanes: conformationally restricted hallucinogenic phenethylamine analogues as functionally selective 5-HT2A receptor agonists.Journal of medicinal chemistry, , Sep-21, Volume: 49, Issue:19, 2006
Influence of amine substituents on 5-HT2A versus 5-HT2C binding of phenylalkyl- and indolylalkylamines.Journal of medicinal chemistry, , Jun-24, Volume: 37, Issue:13, 1994
Synthesis of potent and selective serotonin 5-HT1B receptor ligands.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 15, Issue:21, 2005
The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function bJournal of medicinal chemistry, , Apr-09, Volume: 41, Issue:8, 1998
Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
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
Return of DJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 25, Issue:22, 2015
Affinity of aporphines for the human 5-HT2A receptor: insights from homology modeling and molecular docking studies.Bioorganic & medicinal chemistry, , Aug-01, Volume: 18, Issue:15, 2010
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 20, Issue:2, 2010
(+/-)-Nantenine analogs as antagonists at human 5-HT(2A) receptors: C1 and flexible congeners.Bioorganic & medicinal chemistry letters, , May-01, Volume: 19, Issue:9, 2009
Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models.Journal of medicinal chemistry, , Jan-28, Volume: 59, Issue:2, 2016
Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 25, Issue:18, 2015
Novel and selective 5-HT2C/2B receptor antagonists as potential anxiolytic agents: synthesis, quantitative structure-activity relationships, and molecular modeling of substituted 1-(3-pyridylcarbamoyl)indolines.Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998
6-Chloro-5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]- indoline (SB-242084): the first selective and brain penetrant 5-HT2C receptor antagonist.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
Synthesis and structure-activity relationship of 1H-indole-3-carboxylic acid pyridine-3-ylamides: a novel series of 5-HT2C receptor antagonists.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 18, Issue:14, 2008
A series of bisaryl imidazolidin-2-ones has shown to be selective and orally active 5-HT2C receptor antagonists.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 15, Issue:22, 2005
Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent.Journal of medicinal chemistry, , Mar-23, Volume: 43, Issue:6, 2000
1-[2-[(Heteroaryloxy)heteroaryl]carbamoyl]indolines: novel and selective 5-HT2C receptor inverse agonists with potential as antidepressant/anxiolytic agents.Bioorganic & medicinal chemistry letters, , Aug-21, Volume: 10, Issue:16, 2000
Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.European journal of medicinal chemistry, , Jul-01, Volume: 173, 2019
Design, synthesis, and biological evaluation of 3,4,5-trimethoxyphenyl acrylamides as antinarcotic agents.Journal of enzyme inhibition and medicinal chemistry, , Volume: 25, Issue:1, 2010
Total synthesis and evaluation of [18F]MHMZ.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 18, Issue:4, 2008
Synthesis, receptor potency, and selectivity of halogenated diphenylpiperidines as serotonin 5-HT2A ligands for PET or SPECT brain imaging.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
Activity of Journal of medicinal chemistry, , 09-23, Volume: 64, Issue:18, 2021
Activity of Journal of medicinal chemistry, , 09-23, Volume: 64, Issue:18, 2021
Fancy bioisosteres: novel paracyclophane derivatives as super-affinity dopamine D3 receptor antagonists.Journal of medicinal chemistry, , Jun-15, Volume: 49, Issue:12, 2006
Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists.Journal of medicinal chemistry, , Oct-10, Volume: 45, Issue:21, 2002
Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists.Bioorganic & medicinal chemistry, , Feb-15, Volume: 16, Issue:4, 2008
Synthesis and structure-activity relationships of a series of benzazepine derivatives as 5-HT2C receptor agonists.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists.Bioorganic & medicinal chemistry, , Feb-15, Volume: 16, Issue:4, 2008
Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity.Journal of medicinal chemistry, , Jan-24, Volume: 51, Issue:2, 2008
Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.Bioorganic & medicinal chemistry letters, , Volume: 16, Issue:3, 2006
Indoline derivatives as 5-HT(2C) receptor agonists.Bioorganic & medicinal chemistry letters, , May-03, Volume: 14, Issue:9, 2004
Novel agonists of 5HT2C receptors. Synthesis and biological evaluation of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2-b]pyrrol-1-yl)-1-methylethylamines. Improved therapeutics for obsessive compulsive disorder.Journal of medicinal chemistry, , Aug-15, Volume: 40, Issue:17, 1997
Potent, selective tetrahydro-beta-carboline antagonists of the serotonin 2B (5HT2B) contractile receptor in the rat stomach fundus.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
N-(1-methyl-5-indolyl)-N'-(3-methyl-5-isothiazolyl)urea: a novel, high-affinity 5-HT2B receptor antagonist.Journal of medicinal chemistry, , Mar-17, Volume: 38, Issue:6, 1995
The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function bJournal of medicinal chemistry, , Apr-09, Volume: 41, Issue:8, 1998
A series of bisaryl imidazolidin-2-ones has shown to be selective and orally active 5-HT2C receptor antagonists.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 15, Issue:22, 2005
Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent.Journal of medicinal chemistry, , Mar-23, Volume: 43, Issue:6, 2000
1-[2-[(Heteroaryloxy)heteroaryl]carbamoyl]indolines: novel and selective 5-HT2C receptor inverse agonists with potential as antidepressant/anxiolytic agents.Bioorganic & medicinal chemistry letters, , Aug-21, Volume: 10, Issue:16, 2000
6-Chloro-5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]- indoline (SB-242084): the first selective and brain penetrant 5-HT2C receptor antagonist.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
Design and synthesis of novel arylpiperazine derivatives containing the imidazole core targeting 5-HT(2A) receptor and 5-HT transporter.Journal of medicinal chemistry, , Sep-22, Volume: 54, Issue:18, 2011
Arylpiperazine-containing pyrrole 3-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 20, Issue:5, 2010
Return of DJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.Bioorganic & medicinal chemistry letters, , Jun-04, Volume: 11, Issue:11, 2001
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
Synthesis and activity of functionalizable derivatives of the serotonin (5-HT) 5-HTBioorganic & medicinal chemistry letters, , 05-01, Volume: 28, Issue:8, 2018
Non-basic ligands for aminergic GPCRs: the discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists for the treatment of sleep disorders.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 20, Issue:12, 2010
Novel spirotetracyclic zwitterionic dual H(1)/5-HT(2A) receptor antagonists for the treatment of sleep disorders.Journal of medicinal chemistry, , Nov-11, Volume: 53, Issue:21, 2010
Total synthesis and evaluation of [18F]MHMZ.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 18, Issue:4, 2008
4-Fluorosulfonylpiperidines: selective 5-HT2A ligands for the treatment of insomnia.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 15, Issue:16, 2005
4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists.Journal of medicinal chemistry, , Jan-17, Volume: 45, Issue:2, 2002
Synthesis, receptor potency, and selectivity of halogenated diphenylpiperidines as serotonin 5-HT2A ligands for PET or SPECT brain imaging.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
Solid-phase synthesis of 2,3-disubstituted indoles: discovery of a novel, high-affinity, selective h5-HT2A antagonist.Bioorganic & medicinal chemistry letters, , Dec-18, Volume: 10, Issue:24, 2000
N-(1-methyl-5-indolyl)-N'-(3-methyl-5-isothiazolyl)urea: a novel, high-affinity 5-HT2B receptor antagonist.Journal of medicinal chemistry, , Mar-17, Volume: 38, Issue:6, 1995
5-Methyl-1-(3-pyridylcarbamoyl)-1,2,3,5-tetrahydropyrrolo[2,3-f]indole: a novel 5-HT2C/5-HT2B receptor antagonist with improved affinity, selectivity, and oral activity.Journal of medicinal chemistry, , Jul-07, Volume: 38, Issue:14, 1995
Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists.Bioorganic & medicinal chemistry letters, , May-20, Volume: 12, Issue:10, 2002
Discovery of G Protein-Biased Antagonists against 5-HTJournal of medicinal chemistry, , 09-23, Volume: 64, Issue:18, 2021
Synthesis and evaluation of the structural elements in alkylated tetrahydroisoquinolines for binding to CNS receptors.Bioorganic & medicinal chemistry, , 11-15, Volume: 24, Issue:22, 2016
A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phen ol (SB-269970).Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Return of DJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 8, Issue:7, 1998
Activity of Journal of medicinal chemistry, , 09-23, Volume: 64, Issue:18, 2021
1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
1,4-Disubstituted aromatic piperazines with high 5-HT2A/D2 selectivity: Quantitative structure-selectivity investigations, docking, synthesis and biological evaluation.Bioorganic & medicinal chemistry, , Sep-15, Volume: 23, Issue:18, 2015
Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists.Journal of medicinal chemistry, , Oct-10, Volume: 45, Issue:21, 2002
Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Evaluation of the eutomer of 4-{3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl}-1-(4-fluorophenyl)butan-1-one, {(+)-SYA 09}, a pyrrolidine analog of haloperidol.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 16, Issue:12, 2006
Return of DJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HTEuropean journal of medicinal chemistry, , Apr-15, Volume: 234, 2022
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
Design, Synthesis, and Biological Evaluation of New Peripheral 5HTJournal of medicinal chemistry, , 04-23, Volume: 63, Issue:8, 2020
[no title available]Bioorganic & medicinal chemistry letters, , 06-15, Volume: 28, Issue:11, 2018
Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-103), a novel 5-hydroxytryptamine(2A) receptor inverse agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 317, Issue:2, 2006
1,4-Disubstituted aromatic piperazines with high 5-HT2A/D2 selectivity: Quantitative structure-selectivity investigations, docking, synthesis and biological evaluation.Bioorganic & medicinal chemistry, , Sep-15, Volume: 23, Issue:18, 2015
Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists.Journal of medicinal chemistry, , Oct-10, Volume: 45, Issue:21, 2002
Synthesis, structure-affinity relationships, and modeling of AMDA analogs at 5-HT2A and H1 receptors: structural factors contributing to selectivity.Bioorganic & medicinal chemistry, , Sep-15, Volume: 17, Issue:18, 2009
Potential modes of interaction of 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives with the 5-HT2A receptor: a ligand structure-affinity relationship, receptor mutagenesis and receptor modeling investigation.Journal of medicinal chemistry, , Nov-13, Volume: 51, Issue:21, 2008
Methoxy-substituted 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives exhibit differential binding affinities at the 5-HT(2A) receptor.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 18, Issue:19, 2008
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
Geometry-affinity relationships of the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene.Journal of medicinal chemistry, , Apr-11, Volume: 45, Issue:8, 2002
Influence of chain length and N-alkylation on the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene.Bioorganic & medicinal chemistry letters, , Mar-12, Volume: 11, Issue:5, 2001
Non-basic ligands for aminergic GPCRs: the discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists for the treatment of sleep disorders.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 20, Issue:12, 2010
A new class of selective, non-basic 5-HT2A receptor antagonists.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 16, Issue:12, 2006
4-Fluorosulfonylpiperidines: selective 5-HT2A ligands for the treatment of insomnia.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 15, Issue:16, 2005
4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists.Journal of medicinal chemistry, , Jan-17, Volume: 45, Issue:2, 2002
2-Phenylcyclopropylmethylamine Derivatives as Dopamine DJournal of medicinal chemistry, , 12-09, Volume: 64, Issue:23, 2021
[no title available]Bioorganic & medicinal chemistry letters, , 01-01, Volume: 31, 2021
[no title available]European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Development of molecular tools based on the dopamine DBioorganic & medicinal chemistry, , 07-01, Volume: 25, Issue:13, 2017
Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics.European journal of medicinal chemistry, , Nov-10, Volume: 123, 2016
Functionally selective dopamine D₂, D₃ receptor partial agonists.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Discovery of a lead series of potent benzodiazepine 5-HTBioorganic & medicinal chemistry letters, , 03-01, Volume: 30, Issue:5, 2020
Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HTEuropean journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
Design, Synthesis, and Characterization of 4-Undecylpiperidine-2-carboxamides as Positive Allosteric Modulators of the Serotonin (5-HT) 5-HTJournal of medicinal chemistry, , 01-10, Volume: 62, Issue:1, 2019
Identification of fluorinated (R)-(-)-aporphine derivatives as potent and selective ligands at serotonin 5-HTBioorganic & medicinal chemistry letters, , 01-15, Volume: 29, Issue:2, 2019
Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications.Journal of medicinal chemistry, , 07-27, Volume: 60, Issue:14, 2017
Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models.Journal of medicinal chemistry, , Jan-28, Volume: 59, Issue:2, 2016
Design and Discovery of Functionally Selective Serotonin 2C (5-HTJournal of medicinal chemistry, , 11-10, Volume: 59, Issue:21, 2016
Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents.Journal of medicinal chemistry, , Feb-26, Volume: 58, Issue:4, 2015
Synthesis and SAR of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin-5(9bH)-ones as 5-HT2C receptor agonists.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action.Journal of medicinal chemistry, , Apr-09, Volume: 52, Issue:7, 2009
Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity.Journal of medicinal chemistry, , Jan-24, Volume: 51, Issue:2, 2008
Discovery and SAR of new benzazepines as potent and selective 5-HT(2C) receptor agonists for the treatment of obesity.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 15, Issue:5, 2005
Activity of Journal of medicinal chemistry, , 09-23, Volume: 64, Issue:18, 2021
Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain.Journal of medicinal chemistry, , Feb-14, Volume: 51, Issue:3, 2008
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.Proceedings of the National Academy of Sciences of the United States of America, , May-15, Volume: 104, Issue:20, 2007
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
Novel DEuropean journal of medicinal chemistry, , Mar-15, Volume: 232, 2022
Semisynthetic Transformations on (+)-Boldine Reveal a 5-HTJournal of natural products, , 09-23, Volume: 85, Issue:9, 2022
Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 40, 2021
Structural manipulation of aporphines via C10 nitrogenation leads to the identification of new 5-HTBioorganic & medicinal chemistry, , 08-01, Volume: 28, Issue:15, 2020
Discovery of aryl-piperidine derivatives as potential antipsychotic agents using molecular hybridization strategy.European journal of medicinal chemistry, , May-01, Volume: 193, 2020
Identification of C10 nitrogen-containing aporphines with dopamine DBioorganic & medicinal chemistry letters, , 04-15, Volume: 30, Issue:8, 2020
[no title available]Bioorganic & medicinal chemistry letters, , 11-01, Volume: 30, Issue:21, 2020
[no title available]Journal of medicinal chemistry, , Aug-09, Volume: 61, Issue:15, 2018
[no title available]European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Pharmacophore-based tailoring of biphenyl amide derivatives as selective 5-hydroxytryptamine 2B receptor antagonists.MedChemComm, , Jun-01, Volume: 9, Issue:6, 2018
Synthesis and biological investigation of new equatorial (β) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile.Bioorganic & medicinal chemistry, , 09-15, Volume: 24, Issue:18, 2016
New halogenated tris-(phenylalkyl)amines as h5-HT2B receptor ligands.Bioorganic & medicinal chemistry letters, , 07-15, Volume: 26, Issue:14, 2016
Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 25, Issue:18, 2015
Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors.Journal of natural products, , Apr-24, Volume: 78, Issue:4, 2015
Synthesis and biological evaluation of a series of aminoalkyl-tetralones and tetralols as dual dopamine/serotonin ligands.European journal of medicinal chemistry, , Volume: 71, 2014
Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.Journal of medicinal chemistry, , Nov-26, Volume: 57, Issue:22, 2014
Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 24, Issue:2, 2014
Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 19, Issue:21, 2009
Synthesis, binding affinity, and molecular docking analysis of new benzofuranone derivatives as potential antipsychotics.Journal of medicinal chemistry, , Oct-09, Volume: 51, Issue:19, 2008
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 17, Issue:17, 2007
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-103), a novel 5-hydroxytryptamine(2A) receptor inverse agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 317, Issue:2, 2006
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics.Bioorganic & medicinal chemistry letters, , Feb-09, Volume: 14, Issue:3, 2004
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential.Bioorganic & medicinal chemistry letters, , Aug-16, Volume: 14, Issue:16, 2004
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic?Bioorganic & medicinal chemistry letters, , May-21, Volume: 11, Issue:10, 2001
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
[no title available],
[no title available]Journal of medicinal chemistry, , 09-09, Volume: 64, Issue:17, 2021
[no title available]European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
[no title available]Bioorganic & medicinal chemistry letters, , 11-01, Volume: 30, Issue:21, 2020
Synthesis of new 5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HTEuropean journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
2-Aminoimidazole-based antagonists of the 5-HTEuropean journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
[no title available]European journal of medicinal chemistry, , May-15, Volume: 170, 2019
Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HTEuropean journal of medicinal chemistry, , Mar-15, Volume: 166, 2019
[no title available]European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
[no title available]ACS medicinal chemistry letters, , Apr-13, Volume: 8, Issue:4, 2017
Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 25, Issue:18, 2015
Further evaluation of the tropane analogs of haloperidol.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 24, Issue:17, 2014
Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.Journal of medicinal chemistry, , Nov-26, Volume: 57, Issue:22, 2014
Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
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
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
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
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
[no title available],
Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 40, 2021
Enables
This protein enables 10 target(s):
| Target | Category | Definition |
|---|
| Gq/11-coupled serotonin receptor activity | molecular function | Combining with serotonin and transmitting the signal across the membrane by activation of the Gq/11 subunit of an associated cytoplasmic heterotrimeric G protein complex. The Gq/11 subunit subsequently activates phospholipase C and results in an increase in inositol triphosphate (IP3) levels. [GOC:bf, GOC:mah, PMID:18571247, PMID:18703043] |
| virus receptor activity | molecular function | Combining with a virus component and mediating entry of the virus into the cell. [GOC:bf, GOC:dph, PMID:7621403, UniProtKB-KW:KW-1183] |
| G protein-coupled serotonin receptor activity | molecular function | Combining with the biogenic amine serotonin and transmitting the signal across the membrane by activating an associated G-protein. Serotonin (5-hydroxytryptamine) is a neurotransmitter and hormone found in vertebrates and invertebrates. [GOC:ai] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| protein tyrosine kinase activator activity | molecular function | Increases the activity of a protein tyrosine kinase, an enzyme which phosphorylates a tyrosyl phenolic group on a protein. [GOC:ai, ISBN:0198506732] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| protein-containing complex binding | molecular function | Binding to a macromolecular complex. [GOC:jl] |
| serotonin binding | molecular function | Binding to serotonin (5-hydroxytryptamine), a monoamine neurotransmitter occurring in the peripheral and central nervous systems, also having hormonal properties. [GOC:ai] |
| 1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding | molecular function | Binding to the amine 1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine, a serotonin receptor agonist that can act as a psychedelic drug. [GOC:yaf, PMID:19057895] |
| neurotransmitter receptor activity | molecular function | Combining with a neurotransmitter and transmitting the signal to initiate a change in cell activity. [GOC:jl, GOC:signaling] |
Located In
This protein is located in 11 target(s):
| Target | Category | Definition |
|---|
| neurofilament | cellular component | A type of intermediate filament found in the core of neuronal axons. Neurofilaments are heteropolymers composed of three type IV polypeptides: NF-L, NF-M, and NF-H (for low, middle, and high molecular weight). Neurofilaments are responsible for the radial growth of an axon and determine axonal diameter. [ISBN:0198506732, ISBN:0716731363, 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] |
| caveola | cellular component | A membrane raft that forms small pit, depression, or invagination that communicates with the outside of a cell and extends inward, indenting the cytoplasm and the cell membrane. Examples include flask-shaped invaginations of the plasma membrane in adipocytes associated with caveolin proteins, and minute pits or incuppings of the cell membrane formed during pinocytosis. Caveolae may be pinched off to form free vesicles within the cytoplasm. [GOC:mah, ISBN:0721662544, PMID:16645198] |
| 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] |
| cytoplasmic vesicle | cellular component | A vesicle found in the cytoplasm of a cell. [GOC:ai, GOC:mah, GOC:vesicles] |
| 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] |
| neuronal cell body | cellular component | The portion of a neuron that includes the nucleus, but excludes cell projections such as axons and dendrites. [GOC:go_curators] |
| dendritic shaft | cellular component | Cylindric portion of the dendrite, directly stemming from the perikaryon, and carrying the dendritic spines. [GOC:nln] |
| postsynaptic membrane | cellular component | A specialized area of membrane facing the presynaptic membrane on the tip of the nerve ending and separated from it by a minute cleft (the synaptic cleft). Neurotransmitters cross the synaptic cleft and transmit the signal to the postsynaptic membrane. [ISBN:0198506732] |
| cell body fiber | cellular component | A neuron projection that is found in unipolar neurons and corresponds to the region between the cell body and the point at which the single projection branches. [GOC:dos, GOC:mah] |
| glutamatergic synapse | cellular component | A synapse that uses glutamate as a neurotransmitter. [GOC:dos] |
Active In
This protein is active in 2 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] |
| dendrite | cellular component | A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| G protein-coupled serotonin receptor complex | cellular component | A protein complex that is capable of G protein-coupled serotonin receptor activity. [GO_REF:0000088, GOC:bhm, GOC:TermGenie] |
Involved In
This protein is involved in 40 target(s):
| Target | Category | Definition |
|---|
| temperature homeostasis | biological process | A homeostatic process in which an organism modulates its internal body temperature. [GOC:jl] |
| positive regulation of cytokine production involved in immune response | biological process | Any process that activates or increases the frequency, rate, or extent of cytokine production that contributes to an immune response. [GOC:add] |
| glycolytic process | biological process | The chemical reactions and pathways resulting in the breakdown of a carbohydrate into pyruvate, with the concomitant production of a small amount of ATP and the reduction of NAD(P) to NAD(P)H. Glycolysis begins with the metabolism of a carbohydrate to generate products that can enter the pathway and ends with the production of pyruvate. Pyruvate may be converted to acetyl-coenzyme A, ethanol, lactate, or other small molecules. [GOC:bf, GOC:dph, ISBN:0201090910, ISBN:0716720094, ISBN:0879010479, Wikipedia:Glycolysis] |
| intracellular calcium ion homeostasis | biological process | A homeostatic process involved in the maintenance of a steady state level of calcium ions within a cell. [GOC:ceb, GOC:mah] |
| activation of phospholipase C activity | biological process | The initiation of the activity of the inactive enzyme phospolipase C as the result of The series of molecular signals generated as a consequence of a G protein-coupled receptor binding to its physiological ligand. [GOC:dph, GOC:mah, GOC:tb, PMID:8280098] |
| positive regulation of cytosolic calcium ion concentration | biological process | Any process that increases the concentration of calcium ions in the cytosol. [GOC:ai] |
| memory | biological process | The activities involved in the mental information processing system that receives (registers), modifies, stores, and retrieves informational stimuli. The main stages involved in the formation and retrieval of memory are encoding (processing of received information by acquisition), storage (building a permanent record of received information as a result of consolidation) and retrieval (calling back the stored information and use it in a suitable way to execute a given task). [GOC:curators, ISBN:0582227089] |
| positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
| response to xenobiotic stimulus | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus from a xenobiotic, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:jl, GOC:krc] |
| positive regulation of phosphatidylinositol biosynthetic process | biological process | Any process that increases the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of phosphatidylinositol. [GOC:dph, GOC:tb, GOC:vw] |
| regulation of dopamine secretion | biological process | Any process that modulates the frequency, rate or extent of the regulated release of dopamine. [GOC:ef] |
| artery smooth muscle contraction | biological process | A process in which force is generated within smooth muscle tissue, resulting in a change in muscle geometry. This process occurs in the artery. Force generation involves a chemo-mechanical energy conversion step that is carried out by the actin/myosin complex activity, which generates force through ATP hydrolysis. The artery is a vessel carrying blood away from the heart. [GOC:mtg_muscle, MA:0000708, MSH:D001158] |
| urinary bladder smooth muscle contraction | biological process | A process in which force is generated within smooth muscle tissue, resulting in a change in muscle geometry. This process occurs in the urinary bladder. Force generation involves a chemo-mechanical energy conversion step that is carried out by the actin/myosin complex activity, which generates force through ATP hydrolysis. The urinary bladder is a musculomembranous sac along the urinary tract. [GOC:mr, GOC:mtg_muscle, PMID:11768524, PMID:18276178, PMID:538956] |
| positive regulation of heat generation | biological process | Any process that activates or increases the rate or extent of heat generation. [GOC:dph, GOC:mah, GOC:tb] |
| negative regulation of potassium ion transport | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the directed movement of potassium ions (K+) into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:jl] |
| phosphatidylinositol 3-kinase/protein kinase B signal transduction | biological process | An intracellular signaling cassette that starts with phosphatidylinositol 3-kinase (PI3K) activation, production of phosphatidylinositol 3-phosphate (PI3P), activation of PDK1, which recruits and ending with the activation of protein kinase B (PKB, also known as Akt). PI3K is activated by cell surface receptors. Note that PTEN is an inhibitor of the pathway. [PMID:20517722, PMID:22952397] |
| positive regulation of neuron apoptotic process | biological process | Any process that activates or increases the frequency, rate or extent of cell death of neurons by apoptotic process. [GOC:go_curators, GOC:mtg_apoptosis] |
| protein localization to cytoskeleton | biological process | A process in which a protein is transported to, or maintained in, a location within the cytoskeleton. [GOC:jl] |
| positive regulation of fat cell differentiation | biological process | Any process that activates or increases the frequency, rate or extent of adipocyte differentiation. [GOC:go_curators] |
| positive regulation of glycolytic process | biological process | Any process that activates or increases the frequency, rate or extent of glycolysis. [GOC:go_curators] |
| positive regulation of vasoconstriction | biological process | Any process that activates or increases the frequency, rate or extent of vasoconstriction. [GOC:go_curators] |
| symbiont entry into host cell | biological process | The process by which a symbiont breaches the plasma membrane or cell envelope and enters the host cell. The process ends when the symbiont or its genome is released into the host cell. [GOC:jl] |
| sensitization | biological process | An increased in a behavioral response to a repeated stimulus. For example, a shock to the tail of the marine snail Aplysia, to which the snail responds by withdrawing its gill, will result in increased gill withdrawal the next time the skin is touched. [ISBN:0582227089] |
| behavioral response to cocaine | biological process | Any process that results in a change in the behavior of an organism as a result of a cocaine stimulus. [GOC:jid] |
| positive regulation of inflammatory response | biological process | Any process that activates or increases the frequency, rate or extent of the inflammatory response. [GOC:ai] |
| positive regulation of peptidyl-tyrosine phosphorylation | biological process | Any process that activates or increases the frequency, rate or extent of the phosphorylation of peptidyl-tyrosine. [GOC:ai] |
| detection of temperature stimulus involved in sensory perception of pain | biological process | The series of events involved in the perception of pain in which a temperature stimulus is received and converted into a molecular signal. [GOC:ai, GOC:dos] |
| detection of mechanical stimulus involved in sensory perception of pain | biological process | The series of events involved in the perception of pain in which a mechanical stimulus is received and converted into a molecular signal. [GOC:ai, GOC:dos] |
| release of sequestered calcium ion into cytosol | biological process | The process in which calcium ions sequestered in the endoplasmic reticulum, Golgi apparatus or mitochondria are released into the cytosolic compartment. [GOC:dph, GOC:hjd, GOC:mtg_lung, PMID:1814929] |
| negative regulation of synaptic transmission, glutamatergic | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of glutamatergic synaptic transmission, the process of communication from a neuron to another neuron across a synapse using the neurotransmitter glutamate. [GOC:ai] |
| positive regulation of ERK1 and ERK2 cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the ERK1 and ERK2 cascade. [GOC:mah] |
| G protein-coupled serotonin receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of a G protein-coupled serotonin receptor binding to one of its physiological ligands. [GOC:mah] |
| presynaptic modulation of chemical synaptic transmission | biological process | Any process, acting in the presynapse that results in modulation of chemical synaptic transmission. [GOC:dos] |
| positive regulation of execution phase of apoptosis | biological process | Any process that activates or increases the frequency, rate or extent of execution phase of apoptosis. [GOC:mtg_apoptosis, GOC:TermGenie] |
| positive regulation of platelet aggregation | biological process | Any process that activates or increases the frequency, rate or extent of platelet aggregation. Platelet aggregation is the adhesion of one platelet to one or more other platelets via adhesion molecules. [GOC:fj, GOC:TermGenie] |
| positive regulation of DNA biosynthetic process | biological process | Any process that activates or increases the frequency, rate or extent of DNA biosynthetic process. [GOC:obol] |
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of a nucleotide cyclase activity and a subsequent change in the concentration of a cyclic nucleotide. [GOC:mah, GOC:signaling, ISBN:0815316194] |
| phospholipase C-activating serotonin receptor signaling pathway | biological process | A phospholipase C-activating receptor G protein-coupled receptor signaling pathway initiated by serotonin binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb] |
| serotonin receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of a serotonin receptor binding to one of its physiological ligands. [GOC:mah] |
| 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] |