Proteins > 5-hydroxytryptamine receptor 2C
Page last updated: 2024-08-07 16:20:39
5-hydroxytryptamine receptor 2C
A 5-hydroxytryptamine receptor 2C that is encoded in the genome of human. [PRO:WCB, UniProtKB:P28335]
Synonyms
5-HT-2C;
5-HT2C;
5-HTR2C;
5-hydroxytryptamine receptor 1C;
5-HT-1C;
5-HT1C;
Serotonin receptor 2C
Research
Bioassay Publications (192)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 2 (1.04) | 18.7374 |
1990's | 22 (11.46) | 18.2507 |
2000's | 74 (38.54) | 29.6817 |
2010's | 78 (40.63) | 24.3611 |
2020's | 16 (8.33) | 2.80 |
Compounds (251)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
tryptamine | Homo sapiens (human) | Ki | 0.0500 | 1 | 1 |
8-hydroxy-2-(di-n-propylamino)tetralin | Homo sapiens (human) | Ki | 11.0250 | 2 | 2 |
4-iodo-2,5-dimethoxyphenylisopropylamine | Homo sapiens (human) | Ki | 0.0018 | 1 | 1 |
octoclothepine | Homo sapiens (human) | Ki | 0.0006 | 1 | 1 |
1-(3-chlorophenyl)piperazine | Homo sapiens (human) | Ki | 0.0146 | 6 | 6 |
4-nonylphenol | Homo sapiens (human) | IC50 | 2.5710 | 1 | 0 |
4-nonylphenol | Homo sapiens (human) | Ki | 1.3470 | 1 | 0 |
5-carboxamidotryptamine | Homo sapiens (human) | Ki | 1.5659 | 2 | 2 |
methylbufotenin | Homo sapiens (human) | IC50 | 0.2500 | 1 | 1 |
methylbufotenin | Homo sapiens (human) | Ki | 0.0420 | 1 | 1 |
5-methoxytryptamine | Homo sapiens (human) | Ki | 0.0450 | 1 | 1 |
alpha-methylserotonin | Homo sapiens (human) | Ki | 0.0245 | 3 | 3 |
amiodarone | Homo sapiens (human) | IC50 | 0.4040 | 1 | 0 |
amiodarone | Homo sapiens (human) | Ki | 0.2120 | 1 | 0 |
amitriptyline | Homo sapiens (human) | IC50 | 0.0060 | 1 | 0 |
amitriptyline | Homo sapiens (human) | Ki | 0.0032 | 1 | 0 |
amoxapine | Homo sapiens (human) | IC50 | 0.0038 | 1 | 0 |
amoxapine | Homo sapiens (human) | Ki | 0.0020 | 1 | 0 |
astemizole | Homo sapiens (human) | IC50 | 0.1790 | 1 | 0 |
astemizole | Homo sapiens (human) | Ki | 0.0940 | 1 | 0 |
azelastine | Homo sapiens (human) | Ki | 0.5012 | 1 | 1 |
bithionol | Homo sapiens (human) | IC50 | 8.7800 | 1 | 0 |
bithionol | Homo sapiens (human) | Ki | 4.5990 | 1 | 0 |
buspirone | Homo sapiens (human) | Ki | 2.2700 | 1 | 1 |
verapamil | Homo sapiens (human) | IC50 | 0.2970 | 1 | 0 |
verapamil | Homo sapiens (human) | Ki | 0.1550 | 1 | 0 |
carvedilol | Homo sapiens (human) | IC50 | 0.1150 | 1 | 0 |
carvedilol | Homo sapiens (human) | Ki | 0.0600 | 1 | 0 |
cgs 12066 | Homo sapiens (human) | IC50 | 68.4825 | 3 | 3 |
chlorpromazine | Homo sapiens (human) | IC50 | 0.0052 | 1 | 0 |
chlorpromazine | Homo sapiens (human) | Ki | 0.0260 | 4 | 4 |
cisapride | Homo sapiens (human) | IC50 | 0.2597 | 3 | 2 |
cisapride | Homo sapiens (human) | Ki | 0.4020 | 1 | 0 |
citalopram | Homo sapiens (human) | IC50 | 0.2970 | 1 | 0 |
citalopram | Homo sapiens (human) | Ki | 0.1560 | 1 | 0 |
clomipramine | Homo sapiens (human) | IC50 | 0.0340 | 1 | 0 |
clomipramine | Homo sapiens (human) | Ki | 0.0180 | 1 | 0 |
clotrimazole | Homo sapiens (human) | IC50 | 14.4720 | 1 | 0 |
clotrimazole | Homo sapiens (human) | Ki | 7.5810 | 1 | 0 |
cyproheptadine | Homo sapiens (human) | IC50 | 0.0024 | 1 | 0 |
cyproheptadine | Homo sapiens (human) | Ki | 0.0061 | 2 | 1 |
dicyclomine | Homo sapiens (human) | IC50 | 0.4680 | 1 | 0 |
dicyclomine | Homo sapiens (human) | Ki | 0.2450 | 1 | 0 |
diphenhydramine | Homo sapiens (human) | IC50 | 0.9800 | 1 | 0 |
diphenhydramine | Homo sapiens (human) | Ki | 0.5130 | 1 | 0 |
domperidone | Homo sapiens (human) | IC50 | 1.3320 | 1 | 0 |
domperidone | Homo sapiens (human) | Ki | 0.6980 | 1 | 0 |
doxazosin | Homo sapiens (human) | IC50 | 0.5440 | 1 | 0 |
doxazosin | Homo sapiens (human) | Ki | 0.2850 | 1 | 0 |
doxepin | Homo sapiens (human) | IC50 | 0.0460 | 1 | 0 |
doxepin | Homo sapiens (human) | Ki | 0.0240 | 1 | 0 |
droperidol | Homo sapiens (human) | IC50 | 0.4540 | 1 | 0 |
droperidol | Homo sapiens (human) | Ki | 0.2380 | 1 | 0 |
ebastine | Homo sapiens (human) | IC50 | 0.2375 | 1 | 0 |
ebastine | Homo sapiens (human) | Ki | 0.1244 | 1 | 0 |
econazole | Homo sapiens (human) | IC50 | 11.9820 | 1 | 0 |
econazole | Homo sapiens (human) | Ki | 6.2760 | 1 | 0 |
fenofibrate | Homo sapiens (human) | IC50 | 2.3710 | 1 | 0 |
fenofibrate | Homo sapiens (human) | Ki | 1.2420 | 1 | 0 |
fluphenazine | Homo sapiens (human) | IC50 | 0.0670 | 1 | 0 |
fluphenazine | Homo sapiens (human) | Ki | 0.0350 | 1 | 0 |
fluoxetine | Homo sapiens (human) | IC50 | 0.1395 | 2 | 1 |
fluoxetine | Homo sapiens (human) | Ki | 0.0620 | 1 | 0 |
guanfacine | Homo sapiens (human) | IC50 | 1.4530 | 1 | 0 |
guanfacine | Homo sapiens (human) | Ki | 0.7610 | 1 | 0 |
haloperidol | Homo sapiens (human) | IC50 | 6.6735 | 2 | 1 |
haloperidol | Homo sapiens (human) | Ki | 4.7367 | 11 | 10 |
haloprogin | Homo sapiens (human) | IC50 | 2.6020 | 1 | 0 |
haloprogin | Homo sapiens (human) | Ki | 1.3630 | 1 | 0 |
hexachlorophene | Homo sapiens (human) | IC50 | 4.6042 | 1 | 0 |
hexachlorophene | Homo sapiens (human) | Ki | 2.4117 | 1 | 0 |
imipramine | Homo sapiens (human) | Ki | 0.1600 | 1 | 1 |
ketanserin | Homo sapiens (human) | IC50 | 0.0027 | 1 | 1 |
ketanserin | Homo sapiens (human) | Ki | 0.0718 | 2 | 2 |
ketotifen | Homo sapiens (human) | IC50 | 0.1600 | 1 | 0 |
ketotifen | Homo sapiens (human) | Ki | 0.1418 | 2 | 1 |
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one | Homo sapiens (human) | IC50 | 1.0020 | 1 | 0 |
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one | Homo sapiens (human) | Ki | 0.5250 | 1 | 0 |
maprotiline | Homo sapiens (human) | IC50 | 0.0780 | 1 | 0 |
maprotiline | Homo sapiens (human) | Ki | 0.0410 | 1 | 0 |
mescaline | Homo sapiens (human) | Ki | 0.3028 | 1 | 1 |
methapyrilene | Homo sapiens (human) | IC50 | 0.7440 | 1 | 0 |
methapyrilene | Homo sapiens (human) | Ki | 0.3900 | 1 | 0 |
metoclopramide | Homo sapiens (human) | IC50 | 2.3830 | 1 | 0 |
metoclopramide | Homo sapiens (human) | Ki | 1.2480 | 1 | 0 |
mianserin | Homo sapiens (human) | IC50 | 0.0043 | 2 | 1 |
mianserin | Homo sapiens (human) | Ki | 0.0048 | 6 | 7 |
miconazole | Homo sapiens (human) | IC50 | 5.3140 | 1 | 0 |
miconazole | Homo sapiens (human) | Ki | 2.7840 | 1 | 0 |
mirtazapine | Homo sapiens (human) | Ki | 0.0390 | 1 | 1 |
mitoxantrone | Homo sapiens (human) | IC50 | 3.5619 | 1 | 0 |
mitoxantrone | Homo sapiens (human) | Ki | 1.8657 | 1 | 0 |
1-(3-trifluoromethylphenyl)piperazine | Homo sapiens (human) | IC50 | 0.1500 | 1 | 1 |
nifedipine | Homo sapiens (human) | IC50 | 18.2730 | 1 | 0 |
nifedipine | Homo sapiens (human) | Ki | 9.5720 | 1 | 0 |
nortriptyline | Homo sapiens (human) | IC50 | 0.0160 | 1 | 0 |
nortriptyline | Homo sapiens (human) | Ki | 0.0082 | 1 | 0 |
orphenadrine | Homo sapiens (human) | IC50 | 0.5340 | 1 | 0 |
orphenadrine | Homo sapiens (human) | Ki | 0.2800 | 1 | 0 |
oxymetazoline | Homo sapiens (human) | IC50 | 0.5780 | 1 | 0 |
oxymetazoline | Homo sapiens (human) | Ki | 0.3030 | 1 | 0 |
pentamidine | Homo sapiens (human) | IC50 | 3.2780 | 1 | 0 |
pentamidine | Homo sapiens (human) | Ki | 1.7170 | 1 | 0 |
pindolol | Homo sapiens (human) | Ki | 54.0000 | 1 | 1 |
pirenperone | Homo sapiens (human) | Ki | 0.0600 | 1 | 1 |
prochlorperazine | Homo sapiens (human) | IC50 | 0.0780 | 1 | 0 |
prochlorperazine | Homo sapiens (human) | Ki | 0.0410 | 1 | 0 |
promazine | Homo sapiens (human) | IC50 | 0.0990 | 1 | 0 |
promazine | Homo sapiens (human) | Ki | 0.0520 | 1 | 0 |
promethazine | Homo sapiens (human) | IC50 | 0.0120 | 1 | 0 |
promethazine | Homo sapiens (human) | Ki | 0.0065 | 1 | 0 |
propafenone | Homo sapiens (human) | IC50 | 0.3840 | 1 | 0 |
propafenone | Homo sapiens (human) | Ki | 0.2010 | 1 | 0 |
propofol | Homo sapiens (human) | IC50 | 11.5530 | 1 | 0 |
propofol | Homo sapiens (human) | Ki | 6.0510 | 1 | 0 |
propranolol | Homo sapiens (human) | IC50 | 3.6529 | 2 | 1 |
propranolol | Homo sapiens (human) | Ki | 1.2020 | 1 | 0 |
psilocin | Homo sapiens (human) | IC50 | 0.0078 | 1 | 1 |
pyrilamine | Homo sapiens (human) | IC50 | 1.1300 | 1 | 0 |
pyrilamine | Homo sapiens (human) | Ki | 0.5920 | 1 | 0 |
quetiapine | Homo sapiens (human) | IC50 | 3.3008 | 1 | 0 |
quetiapine | Homo sapiens (human) | Ki | 1.7338 | 5 | 4 |
quipazine | Homo sapiens (human) | IC50 | 0.0617 | 2 | 2 |
quipazine | Homo sapiens (human) | Ki | 0.2000 | 1 | 1 |
raloxifene | Homo sapiens (human) | IC50 | 1.1780 | 1 | 0 |
raloxifene | Homo sapiens (human) | Ki | 0.6170 | 1 | 0 |
risperidone | Homo sapiens (human) | IC50 | 0.0057 | 6 | 5 |
risperidone | Homo sapiens (human) | Ki | 0.0271 | 16 | 15 |
ritanserin | Homo sapiens (human) | IC50 | 0.0025 | 1 | 3 |
ritanserin | Homo sapiens (human) | Ki | 0.0009 | 6 | 7 |
rizatriptan | Homo sapiens (human) | IC50 | 8.9716 | 2 | 2 |
sb 206553 | Homo sapiens (human) | IC50 | 0.0094 | 1 | 1 |
sb 206553 | Homo sapiens (human) | Ki | 0.0095 | 4 | 4 |
spiperone | Homo sapiens (human) | Ki | 1.1500 | 1 | 1 |
sulconazole | Homo sapiens (human) | IC50 | 2.7850 | 1 | 0 |
sulconazole | Homo sapiens (human) | Ki | 1.4590 | 1 | 0 |
sumatriptan | Homo sapiens (human) | IC50 | 5.9835 | 3 | 3 |
terfenadine | Homo sapiens (human) | IC50 | 1.2310 | 1 | 0 |
terfenadine | Homo sapiens (human) | Ki | 0.6450 | 1 | 0 |
tetracaine | Homo sapiens (human) | IC50 | 3.2680 | 1 | 0 |
tetracaine | Homo sapiens (human) | Ki | 1.7120 | 1 | 0 |
thioridazine | Homo sapiens (human) | IC50 | 0.0440 | 1 | 0 |
thioridazine | Homo sapiens (human) | Ki | 0.0230 | 1 | 0 |
trazodone | Homo sapiens (human) | IC50 | 0.0910 | 1 | 0 |
trazodone | Homo sapiens (human) | Ki | 0.0470 | 1 | 0 |
trioxsalen | Homo sapiens (human) | IC50 | 2.3560 | 1 | 0 |
trioxsalen | Homo sapiens (human) | Ki | 1.2340 | 1 | 0 |
zotepine | Homo sapiens (human) | Ki | 0.0029 | 1 | 1 |
lysergic acid diethylamide | Homo sapiens (human) | Ki | 0.0050 | 1 | 1 |
phentolamine | Homo sapiens (human) | IC50 | 0.3960 | 1 | 0 |
phentolamine | Homo sapiens (human) | Ki | 0.2070 | 1 | 0 |
2-acetylaminofluorene | Homo sapiens (human) | IC50 | 2.1430 | 1 | 0 |
2-acetylaminofluorene | Homo sapiens (human) | Ki | 1.1220 | 1 | 0 |
mepazine | Homo sapiens (human) | IC50 | 0.4950 | 1 | 0 |
mepazine | Homo sapiens (human) | Ki | 0.2590 | 1 | 0 |
n,n-dimethyltryptamine | Homo sapiens (human) | Ki | 0.0330 | 1 | 1 |
cyclizine | Homo sapiens (human) | IC50 | 1.0210 | 1 | 0 |
cyclizine | Homo sapiens (human) | Ki | 0.5350 | 1 | 0 |
phenothiazine | Homo sapiens (human) | IC50 | 2.2360 | 1 | 0 |
phenothiazine | Homo sapiens (human) | Ki | 1.1710 | 1 | 0 |
ergotamine | Homo sapiens (human) | IC50 | 0.0560 | 1 | 0 |
ergotamine | Homo sapiens (human) | Ki | 0.0290 | 1 | 0 |
methylergonovine | Homo sapiens (human) | IC50 | 0.0130 | 1 | 0 |
methylergonovine | Homo sapiens (human) | Ki | 0.0066 | 1 | 0 |
benzethonium chloride | Homo sapiens (human) | IC50 | 1.0270 | 1 | 0 |
benzethonium chloride | Homo sapiens (human) | Ki | 0.5380 | 1 | 0 |
sterogenol | Homo sapiens (human) | IC50 | 1.2880 | 1 | 0 |
sterogenol | Homo sapiens (human) | Ki | 0.6740 | 1 | 0 |
indopan | Homo sapiens (human) | Ki | 0.1660 | 1 | 2 |
methysergide | Homo sapiens (human) | IC50 | 0.0021 | 1 | 0 |
methysergide | Homo sapiens (human) | Ki | 0.0018 | 2 | 1 |
bufotenin | Homo sapiens (human) | Ki | 0.0700 | 1 | 1 |
dihydroergotamine | Homo sapiens (human) | IC50 | 0.0900 | 1 | 0 |
dihydroergotamine | Homo sapiens (human) | Ki | 0.0470 | 1 | 0 |
dimenhydrinate | Homo sapiens (human) | IC50 | 0.6340 | 1 | 0 |
dimenhydrinate | Homo sapiens (human) | Ki | 0.3320 | 1 | 0 |
5-fluoro-alpha-methyltryptamine | Homo sapiens (human) | Ki | 0.0100 | 1 | 1 |
azaperone | Homo sapiens (human) | Ki | 1.4446 | 2 | 4 |
n-methyllaurotetanine | Homo sapiens (human) | Ki | 0.9500 | 1 | 1 |
glaucine | Homo sapiens (human) | Ki | 0.3280 | 1 | 1 |
clemastine | Homo sapiens (human) | IC50 | 0.0990 | 1 | 0 |
clemastine | Homo sapiens (human) | Ki | 0.0520 | 1 | 0 |
pizotyline | Homo sapiens (human) | Ki | 0.0014 | 1 | 1 |
metergoline | Homo sapiens (human) | IC50 | 0.0007 | 1 | 0 |
metergoline | Homo sapiens (human) | Ki | 0.0004 | 2 | 1 |
lisuride | Homo sapiens (human) | IC50 | 0.0200 | 1 | 0 |
lisuride | Homo sapiens (human) | Ki | 0.0100 | 1 | 0 |
bromocriptine | Homo sapiens (human) | IC50 | 0.5320 | 1 | 0 |
bromocriptine | Homo sapiens (human) | Ki | 0.2780 | 1 | 0 |
dexchlorpheniramine | Homo sapiens (human) | IC50 | 2.3220 | 1 | 0 |
dexchlorpheniramine | Homo sapiens (human) | Ki | 1.2170 | 1 | 0 |
penfluridol | Homo sapiens (human) | Ki | 0.8810 | 1 | 1 |
5-methoxy-alpha-methyltryptamine | Homo sapiens (human) | Ki | 0.0083 | 2 | 2 |
pergolide | Homo sapiens (human) | IC50 | 0.3790 | 1 | 0 |
pergolide | Homo sapiens (human) | Ki | 0.1990 | 1 | 0 |
sertindole | Homo sapiens (human) | Ki | 0.0008 | 3 | 3 |
fananserin | Homo sapiens (human) | Ki | 0.0010 | 1 | 1 |
aripiprazole | Homo sapiens (human) | IC50 | 1.3800 | 3 | 3 |
aripiprazole | Homo sapiens (human) | Ki | 0.0829 | 7 | 8 |
ziprasidone | Homo sapiens (human) | Ki | 0.0050 | 6 | 6 |
fluoxetine hydrochloride | Homo sapiens (human) | Ki | 0.0720 | 1 | 1 |
sertraline | Homo sapiens (human) | IC50 | 1.0830 | 1 | 0 |
sertraline | Homo sapiens (human) | Ki | 0.5673 | 1 | 0 |
mesulergine | Homo sapiens (human) | IC50 | 0.0019 | 1 | 1 |
mesulergine | Homo sapiens (human) | Ki | 0.0014 | 3 | 3 |
mdl 11939 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
ergocornine | Homo sapiens (human) | IC50 | 0.1040 | 1 | 0 |
ergocornine | Homo sapiens (human) | Ki | 0.0550 | 1 | 0 |
s20098 | Homo sapiens (human) | Ki | 0.6820 | 3 | 3 |
u 74006f | Homo sapiens (human) | IC50 | 0.7180 | 1 | 0 |
u 74006f | Homo sapiens (human) | Ki | 0.3760 | 1 | 0 |
gr 127935 | Homo sapiens (human) | Ki | 0.1050 | 1 | 1 |
6-chloro-2-(1-piperazinyl)pyrazine | Homo sapiens (human) | Ki | 3.3942 | 1 | 2 |
5-methoxy 3-(1,2,3,6-tetrahydro-4-pyridinyl)1h indole | Homo sapiens (human) | IC50 | 0.2950 | 2 | 2 |
5-methoxy 3-(1,2,3,6-tetrahydro-4-pyridinyl)1h indole | Homo sapiens (human) | Ki | 0.4000 | 1 | 1 |
mosapride | Homo sapiens (human) | IC50 | 0.3966 | 1 | 0 |
mosapride | Homo sapiens (human) | Ki | 0.2077 | 1 | 0 |
sb 204070a | Homo sapiens (human) | Ki | 0.1027 | 2 | 2 |
n(6)-(3-iodobenzyl)-5'-n-methylcarboxamidoadenosine | Homo sapiens (human) | Ki | 5.4200 | 2 | 2 |
cp 93129 | Homo sapiens (human) | IC50 | 6.4000 | 1 | 1 |
desloratadine | Homo sapiens (human) | IC50 | 0.0300 | 1 | 0 |
desloratadine | Homo sapiens (human) | Ki | 0.0160 | 1 | 0 |
l 694247 | Homo sapiens (human) | IC50 | 0.3162 | 1 | 1 |
sc 53116 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
sc 53116 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
l 741626 | Homo sapiens (human) | Ki | 6.5700 | 1 | 1 |
alpha-ergocryptine | Homo sapiens (human) | IC50 | 0.1470 | 1 | 0 |
alpha-ergocryptine | Homo sapiens (human) | Ki | 0.0770 | 1 | 0 |
n-methylserotonin | Homo sapiens (human) | Ki | 0.2800 | 1 | 1 |
6-hydroxytryptamine | Homo sapiens (human) | Ki | 5.5000 | 1 | 1 |
harmalan | Homo sapiens (human) | Ki | 1.8600 | 1 | 1 |
n-demethyllysergic acid diethylamide | Homo sapiens (human) | IC50 | 1.2900 | 1 | 1 |
5,6,7,8-tetrahydro-4h-isoxazolo(4,5-d)azepin-3-ol | Homo sapiens (human) | Ki | 308.1140 | 1 | 2 |
atropine | Homo sapiens (human) | IC50 | 1.0120 | 1 | 0 |
atropine | Homo sapiens (human) | Ki | 0.5300 | 1 | 0 |
nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 1.0690 | 1 | 1 |
maduramicin | Homo sapiens (human) | IC50 | 0.0340 | 1 | 0 |
maduramicin | Homo sapiens (human) | Ki | 0.0180 | 1 | 0 |
latrepirdine | Homo sapiens (human) | Ki | 0.0759 | 2 | 2 |
sorafenib | Homo sapiens (human) | Ki | 0.4170 | 1 | 1 |
1-methyl-6-methoxy-dihydro-beta-carboline | Homo sapiens (human) | Ki | 0.9240 | 1 | 1 |
terconazole | Homo sapiens (human) | IC50 | 6.9610 | 1 | 0 |
terconazole | Homo sapiens (human) | Ki | 3.6460 | 1 | 0 |
sb 221284 | Homo sapiens (human) | Ki | 0.0025 | 2 | 2 |
sb 228357 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
sb 228357 | Homo sapiens (human) | Ki | 0.0010 | 1 | 1 |
sb 243213 | Homo sapiens (human) | IC50 | 0.0007 | 1 | 1 |
sb 243213 | Homo sapiens (human) | Ki | 0.0010 | 4 | 4 |
ergonovine | Homo sapiens (human) | IC50 | 0.0210 | 1 | 0 |
ergonovine | Homo sapiens (human) | Ki | 0.0110 | 1 | 0 |
dihydroergocristine monomesylate | Homo sapiens (human) | IC50 | 0.2390 | 1 | 0 |
dihydroergocristine monomesylate | Homo sapiens (human) | Ki | 0.1250 | 1 | 0 |
diethylstilbestrol | Homo sapiens (human) | IC50 | 50.8190 | 1 | 0 |
diethylstilbestrol | Homo sapiens (human) | Ki | 26.6190 | 1 | 0 |
cannabidiol | Homo sapiens (human) | Ki | 1.1000 | 1 | 1 |
3,4,5-trimethoxycinnamic acid | Homo sapiens (human) | IC50 | 2.5000 | 2 | 2 |
flunarizine | Homo sapiens (human) | IC50 | 0.6690 | 1 | 0 |
flunarizine | Homo sapiens (human) | Ki | 0.3510 | 1 | 0 |
benztropine | Homo sapiens (human) | IC50 | 0.0610 | 1 | 0 |
benztropine | Homo sapiens (human) | Ki | 0.0320 | 1 | 0 |
enclomiphene | Homo sapiens (human) | IC50 | 1.2720 | 1 | 0 |
enclomiphene | Homo sapiens (human) | Ki | 0.6660 | 1 | 0 |
4-phenyl-1,2,3,6-tetrahydropyridine hdyrochloride | Homo sapiens (human) | Ki | 7.1800 | 1 | 1 |
tamoxifen | Homo sapiens (human) | IC50 | 0.4600 | 1 | 0 |
tamoxifen | Homo sapiens (human) | Ki | 0.2410 | 1 | 0 |
dapiprazole | Homo sapiens (human) | IC50 | 0.6250 | 1 | 0 |
dapiprazole | Homo sapiens (human) | Ki | 0.3270 | 1 | 0 |
altanserin | Homo sapiens (human) | Ki | 0.0400 | 1 | 1 |
mitragynine | Homo sapiens (human) | Ki | 10.0000 | 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 | 1.7700 | 1 | 1 |
bp 897 | Homo sapiens (human) | Ki | 0.8400 | 2 | 2 |
ym348 | Homo sapiens (human) | Ki | 0.0009 | 2 | 2 |
ro 60-0175 | Homo sapiens (human) | Ki | 0.0080 | 4 | 4 |
sb-224289 | Homo sapiens (human) | Ki | 0.6310 | 1 | 1 |
sb 242084 | Homo sapiens (human) | IC50 | 0.0003 | 1 | 1 |
sb 242084 | Homo sapiens (human) | Ki | 0.0010 | 4 | 4 |
rs 102221 | Homo sapiens (human) | IC50 | 0.0039 | 5 | 5 |
rs 102221 | Homo sapiens (human) | Ki | 0.0015 | 4 | 4 |
bw 723c86 | Homo sapiens (human) | IC50 | 0.2043 | 1 | 0 |
bw 723c86 | Homo sapiens (human) | Ki | 0.1070 | 1 | 0 |
harmine | Homo sapiens (human) | Ki | 9.3400 | 1 | 1 |
genistein | Homo sapiens (human) | IC50 | 14.9100 | 1 | 0 |
genistein | Homo sapiens (human) | Ki | 7.8060 | 1 | 0 |
methysergide maleate | Homo sapiens (human) | Ki | 0.0008 | 1 | 1 |
amentoflavone | Homo sapiens (human) | Ki | 2.5550 | 1 | 1 |
ly 344864 | Homo sapiens (human) | Ki | 0.5000 | 1 | 1 |
l 745870 | Homo sapiens (human) | Ki | 3.7333 | 3 | 3 |
mdl 100907 | Homo sapiens (human) | Ki | 0.0924 | 5 | 5 |
sb 200646a | Homo sapiens (human) | Ki | 0.1238 | 2 | 2 |
sb 258719 | Homo sapiens (human) | Ki | 15.8489 | 1 | 1 |
sb 271046 | Homo sapiens (human) | Ki | 1.0179 | 3 | 4 |
cinanserin | Homo sapiens (human) | Ki | 0.2000 | 1 | 1 |
guanabenz | Homo sapiens (human) | IC50 | 0.2040 | 1 | 0 |
guanabenz | Homo sapiens (human) | Ki | 0.1070 | 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 | 9.0000 | 1 | 1 |
sb 269970 | Homo sapiens (human) | Ki | 6.6683 | 3 | 3 |
sb 334867-a | Homo sapiens (human) | Ki | 3.1059 | 2 | 2 |
2-ethyl-5-methoxy-n,n-dimethyltryptamine | Homo sapiens (human) | IC50 | 5.5000 | 1 | 1 |
n-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide | Homo sapiens (human) | Ki | 5.0119 | 1 | 1 |
4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
rwj 68354 | Homo sapiens (human) | IC50 | 1.2370 | 1 | 0 |
rwj 68354 | Homo sapiens (human) | Ki | 0.6480 | 1 | 0 |
n-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)-4-(pyridin-2-yl)benzamide | Homo sapiens (human) | Ki | 0.0527 | 1 | 1 |
4-iodo-2,5-dimethoxyphenylisopropylamine, (r)-isomer | Homo sapiens (human) | Ki | 0.0040 | 2 | 2 |
s 21007 | Homo sapiens (human) | IC50 | 1.8621 | 2 | 2 |
sb258741 | Homo sapiens (human) | Ki | 5.0119 | 1 | 1 |
fauc 346 | Homo sapiens (human) | Ki | 0.3500 | 1 | 1 |
ngb 2904 | Homo sapiens (human) | Ki | 0.4110 | 1 | 1 |
2-(3-chlorobenzyloxy)-6-(piperazin-1-yl)pyrazine | Homo sapiens (human) | Ki | 0.0065 | 2 | 3 |
4-(3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl)-1-(4-fluorophenyl)butan-1-one | Homo sapiens (human) | Ki | 2.4250 | 2 | 4 |
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 | 0.4300 | 1 | 1 |
sb-656104-a | Homo sapiens (human) | Ki | 0.2692 | 1 | 1 |
pimavanserin | Homo sapiens (human) | IC50 | 0.0464 | 1 | 2 |
pimavanserin | Homo sapiens (human) | Ki | 0.0012 | 2 | 3 |
tert-butyl peroxybenzoate | Homo sapiens (human) | Ki | 0.0850 | 1 | 1 |
way 163909 | Homo sapiens (human) | Ki | 0.0102 | 2 | 2 |
5-chloro-2-methyl-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1h-indole | Homo sapiens (human) | IC50 | 0.4500 | 1 | 1 |
way 181187 | Homo sapiens (human) | Ki | 0.3463 | 2 | 4 |
2-(4-iodo-2,5-dimethoxyphenyl)-n-(2-methoxybenzyl)ethanamine | Homo sapiens (human) | Ki | 0.0070 | 1 | 1 |
fauc 365 | Homo sapiens (human) | Ki | 2.0000 | 1 | 1 |
sb-649915 | Homo sapiens (human) | Ki | 7.9433 | 1 | 1 |
way-208466 | Homo sapiens (human) | IC50 | 0.6440 | 1 | 1 |
9-(aminomethyl)-9,10-dihydroanthracene | Homo sapiens (human) | Ki | 0.0430 | 1 | 1 |
meridianin a | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
1-(2,4-difluorophenethyl)-4-(4-fluorophenylsulfonyl)piperidine | Homo sapiens (human) | Ki | 0.0788 | 4 | 4 |
cariprazine | Homo sapiens (human) | Ki | 0.1989 | 1 | 2 |
barettin | Homo sapiens (human) | Ki | 0.3400 | 1 | 1 |
naphyrone | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
naluzotan | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
pg 01037 | Homo sapiens (human) | Ki | 0.0470 | 1 | 1 |
vabicaserin | Homo sapiens (human) | Ki | 0.0030 | 1 | 1 |
col-144 | Homo sapiens (human) | Ki | 0.5940 | 1 | 1 |
lassbio-579 | Homo sapiens (human) | Ki | 8.5350 | 2 | 2 |
lorcaserin | Homo sapiens (human) | Ki | 0.0713 | 7 | 7 |
td-5108 | Homo sapiens (human) | Ki | 0.1000 | 1 | 1 |
octoclothepine, (s)-isomer | Homo sapiens (human) | Ki | 0.0029 | 1 | 1 |
mitragynine | Homo sapiens (human) | Ki | 5.4300 | 1 | 1 |
a 803467 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
lu ae58054 | Homo sapiens (human) | Ki | 0.2506 | 1 | 2 |
yil 781 | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
pf 04457845 | Homo sapiens (human) | Ki | 1.6594 | 1 | 0 |
pf 3246799 | Homo sapiens (human) | Ki | 0.1700 | 2 | 2 |
nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 3.4837 | 2 | 4 |
clozapine | Homo sapiens (human) | IC50 | 0.0658 | 3 | 4 |
clozapine | Homo sapiens (human) | Ki | 0.0154 | 23 | 25 |
olanzapine | Homo sapiens (human) | IC50 | 0.0210 | 1 | 0 |
olanzapine | Homo sapiens (human) | Ki | 0.0083 | 9 | 8 |
tegaserod | Homo sapiens (human) | Ki | 0.1000 | 1 | 1 |
methylaplysinopsin | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
aplysinopsin | Homo sapiens (human) | Ki | 12.2255 | 2 | 2 |
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
4-iodo-2,5-dimethoxyphenylisopropylamine | Homo sapiens (human) | EC50 | 0.0457 | 1 | 1 |
1-(3-chlorophenyl)piperazine | Homo sapiens (human) | EC50 | 0.0466 | 10 | 10 |
methylbufotenin | Homo sapiens (human) | Kd | 0.0794 | 1 | 1 |
methiothepin | Homo sapiens (human) | EC50 | 0.0004 | 1 | 1 |
propranolol | Homo sapiens (human) | EC50 | 5.0119 | 1 | 1 |
psilocin | Homo sapiens (human) | EC50 | 0.0300 | 1 | 1 |
mecoprop | Homo sapiens (human) | EC50 | 0.1200 | 1 | 1 |
indopan | Homo sapiens (human) | EC50 | 0.1071 | 1 | 2 |
psilocybin | Homo sapiens (human) | EC50 | 0.5060 | 1 | 1 |
lisuride | Homo sapiens (human) | EC50 | 0.0246 | 1 | 0 |
bromocriptine | Homo sapiens (human) | EC50 | 1.5849 | 1 | 0 |
pergolide | Homo sapiens (human) | EC50 | 0.2188 | 1 | 0 |
6-chloro-2-(1-piperazinyl)pyrazine | Homo sapiens (human) | EC50 | 0.0946 | 2 | 4 |
Serotonin hydrochloride | Homo sapiens (human) | EC50 | 0.0003 | 1 | 2 |
5,6,7,8-tetrahydro-4h-isoxazolo(4,5-d)azepin-3-ol | Homo sapiens (human) | EC50 | 1,000.0000 | 1 | 2 |
5-hydroxytryptophan | Homo sapiens (human) | EC50 | 0.0002 | 1 | 2 |
4-phenyl-1,2,3,6-tetrahydropyridine hdyrochloride | Homo sapiens (human) | EC50 | 2.4500 | 1 | 1 |
ym348 | Homo sapiens (human) | EC50 | 0.0010 | 1 | 1 |
ro 60-0175 | Homo sapiens (human) | EC50 | 0.0230 | 4 | 4 |
norfenfluramine | Homo sapiens (human) | EC50 | 0.0251 | 1 | 1 |
2-(3-chlorobenzyloxy)-6-(piperazin-1-yl)pyrazine | Homo sapiens (human) | EC50 | 0.0040 | 3 | 5 |
way 163909 | Homo sapiens (human) | EC50 | 0.0080 | 2 | 2 |
vabicaserin | Homo sapiens (human) | EC50 | 0.0080 | 2 | 2 |
lorcaserin | Homo sapiens (human) | EC50 | 0.0222 | 15 | 22 |
pf 3246799 | Homo sapiens (human) | EC50 | 0.0972 | 4 | 4 |
n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | EC50 | 0.0094 | 1 | 2 |
clozapine | Homo sapiens (human) | EC50 | 0.2500 | 1 | 0 |
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
ketanserin | Homo sapiens (human) | Kb | 0.1120 | 1 | 1 |
lg 100268 | Homo sapiens (human) | Synergy | 0.0069 | 1 | 1 |
sb 206553 | Homo sapiens (human) | Kb | 0.0023 | 1 | 1 |
nuciferine | Homo sapiens (human) | Kb | 0.0364 | 1 | 1 |
roemerine | Homo sapiens (human) | Kb | 0.0151 | 1 | 1 |
nrx 194204 | Homo sapiens (human) | Synergy | 0.0019 | 1 | 1 |
way 163909 | Homo sapiens (human) | K | 0.0090 | 2 | 2 |
vabicaserin | Homo sapiens (human) | K | 0.0055 | 2 | 2 |
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Discovery of a novel azepine series of potent and selective 5-HT2C agonists as potential treatments for urinary incontinence.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 19, Issue:17, 2009
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Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole.Journal of medicinal chemistry, , Volume: 33, Issue:8, 1990
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 24, Issue:2, 2014
CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs.Bioorganic & medicinal chemistry, , Oct-01, Volume: 19, Issue:19, 2011
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
[no title available],
Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists.Journal of medicinal chemistry, , Feb-09, Volume: 49, Issue:3, 2006
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[no title available],
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
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
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
New serotonin 5-HT(2A), 5-HT(2B), and 5-HT(2C) receptor antagonists: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo and heterocycloalkanones.Journal of medicinal chemistry, , Jan-03, Volume: 45, Issue:1, 2002
Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic?Bioorganic & medicinal chemistry letters, , May-21, Volume: 11, Issue:10, 2001
Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics.Journal of medicinal chemistry, , Nov-30, Volume: 43, Issue:24, 2000
Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical anJournal of medicinal chemistry, , Jul-29, Volume: 42, Issue:15, 1999
Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics.Journal of medicinal chemistry, , Jun-04, Volume: 41, Issue:12, 1998
[no title available],
Synthesis and evaluation of nuciferine and roemerine enantiomers as 5-HTMedChemComm, , Mar-01, Volume: 9, Issue:3, 2018
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New serotonin 5-HT(2A), 5-HT(2B), and 5-HT(2C) receptor antagonists: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo and heterocycloalkanones.Journal of medicinal chemistry, , Jan-03, Volume: 45, Issue:1, 2002
Central serotonin receptors as targets for drug research.Journal of medicinal chemistry, , Volume: 30, Issue:1, 1987
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 1.Bioorganic & medicinal chemistry letters, , Jan-21, Volume: 12, Issue:2, 2002
New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands.Journal of medicinal chemistry, , Mar-14, Volume: 40, Issue:6, 1997
Central serotonin receptors as targets for drug research.Journal of medicinal chemistry, , Volume: 30, Issue:1, 1987
[no title available],
3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole.Journal of medicinal chemistry, , Volume: 33, Issue:8, 1990
Improved 5-HT2 Selective Receptor Modulators for the Treatment of Psychological Disorders.ACS medicinal chemistry letters, , Dec-09, Volume: 12, Issue:12, 2021
SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 15, Issue:20, 2005
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
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],
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.Journal of medicinal chemistry, , Jun-06, Volume: 40, Issue:12, 1997
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
Central serotonin receptors as targets for drug research.Journal of medicinal chemistry, , Volume: 30, Issue:1, 1987
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
Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics.Bioorganic & medicinal chemistry letters, , 04-15, Volume: 30, Issue:8, 2020
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
Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics.Bioorganic & medicinal chemistry, , 09-01, Volume: 25, Issue:17, 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
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
Novel 7-phenylsulfanyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indoles as dual serotonin 5-HT2C and 5-HT6 receptor ligands.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 20, Issue:18, 2010
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
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
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
New serotonin 5-HT(2A), 5-HT(2B), and 5-HT(2C) receptor antagonists: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo and heterocycloalkanones.Journal of medicinal chemistry, , Jan-03, Volume: 45, Issue:1, 2002
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics.Journal of medicinal chemistry, , Nov-30, Volume: 43, Issue:24, 2000
Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical anJournal of medicinal chemistry, , Jul-29, Volume: 42, Issue:15, 1999
[no title available],
Semisynthetic Transformations on (+)-Boldine Reveal a 5-HTJournal of natural products, , 09-23, Volume: 85, Issue:9, 2022
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
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Activity of Journal of medicinal chemistry, , 09-23, Volume: 64, Issue:18, 2021
Selective 5-HT2C receptor agonists: Design and synthesis of pyridazine-fused azepines.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 26, Issue:16, 2016
Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT₂C) receptor agonists with exquisite functional selectivity over 5-HT₂A and 5-HT₂B receptors.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence.Bioorganic & medicinal chemistry letters, , May-01, Volume: 21, Issue:9, 2011
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
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
Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579.European journal of medicinal chemistry, , Volume: 66, 2013
Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound.European journal of medicinal chemistry, , Volume: 62, 2013
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
Novel 7-phenylsulfanyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indoles as dual serotonin 5-HT2C and 5-HT6 receptor ligands.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 20, Issue:18, 2010
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
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
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
New serotonin 5-HT(2A), 5-HT(2B), and 5-HT(2C) receptor antagonists: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo and heterocycloalkanones.Journal of medicinal chemistry, , Jan-03, Volume: 45, Issue:1, 2002
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
Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics.Journal of medicinal chemistry, , Nov-30, Volume: 43, Issue:24, 2000
Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical anJournal of medicinal chemistry, , Jul-29, Volume: 42, Issue:15, 1999
Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics.Journal of medicinal chemistry, , Jun-04, Volume: 41, Issue:12, 1998
[no title available],
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
Novel 7-phenylsulfanyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indoles as dual serotonin 5-HT2C and 5-HT6 receptor ligands.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 20, Issue:18, 2010
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
[no title available],
In vitro structure-activity relationships of aplysinopsin analogs and their in vivo evaluation in the chick anxiety-depression model.Bioorganic & medicinal chemistry, , Nov-15, Volume: 21, Issue:22, 2013
Synthesis and structure-affinity relationships of novel small molecule natural product derivatives capable of discriminating between serotonin 5-HT1A, 5-HT2A, 5-HT2C receptor subtypes.Bioorganic & medicinal chemistry, , Jul-01, Volume: 18, Issue:13, 2010
Enables
This protein enables 7 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] |
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] |
identical protein binding | molecular function | Binding to an identical protein or proteins. [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 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] |
synapse | cellular component | The junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110] |
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 19 target(s):
Target | Category | Definition |
behavioral fear response | biological process | An acute behavioral change resulting from a perceived external threat. [GOC:dph, PMID:9920659] |
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] |
phospholipase C-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of phospholipase C (PLC) and a subsequent increase in the intracellular concentration of inositol trisphosphate (IP3) and diacylglycerol (DAG). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, 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] |
locomotory behavior | biological process | The specific movement from place to place of an organism in response to external or internal stimuli. Locomotion of a whole organism in a manner dependent upon some combination of that organism's internal state and external conditions. [GOC:dph] |
feeding behavior | biological process | Behavior associated with the intake of food. [GOC:mah] |
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] |
cGMP-mediated signaling | biological process | An intracellular signaling cassette that starts with production of cyclic GMP (cGMP), and ends with activation of downstream effectors that further transmit the signal within the cell. [GOC:signaling] |
regulation of nervous system process | biological process | Any process that modulates the frequency, rate or extent of a neurophysiological process, an organ system process carried out by any of the organs or tissues of the nervous system. [GOC:dph, GOC:mah, GOC:tb] |
regulation of appetite | biological process | Any process which modulates appetite, the desire or physical craving for food. [GOC:add] |
regulation of corticotropin-releasing hormone secretion | biological process | Any process that modulates the frequency, rate or extent of corticotropin-releasing hormone secretion. [GOC:go_curators, PMID:11027914] |
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 calcium-mediated signaling | biological process | Any process that activates or increases the frequency, rate or extent of calcium-mediated signaling. [GOC:ai] |
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] |
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] |
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] |
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] |
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] |