Proteins > 5-hydroxytryptamine receptor 2B
Page last updated: 2024-08-07 16:38:09
5-hydroxytryptamine receptor 2B
A 5-hydroxytryptamine receptor 2B that is encoded in the genome of human. [PRO:WCB, UniProtKB:P41595]
Synonyms
5-HT-2B;
5-HT2B;
Serotonin receptor 2B
Research
Bioassay Publications (118)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 1 (0.85) | 18.7374 |
1990's | 7 (5.93) | 18.2507 |
2000's | 40 (33.90) | 29.6817 |
2010's | 61 (51.69) | 24.3611 |
2020's | 9 (7.63) | 2.80 |
Compounds (222)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
4-iodo-2,5-dimethoxyphenylisopropylamine | Homo sapiens (human) | IC50 | 0.0032 | 6 | 6 |
4-iodo-2,5-dimethoxyphenylisopropylamine | Homo sapiens (human) | Ki | 0.0104 | 5 | 5 |
1-(3-chlorophenyl)piperazine | Homo sapiens (human) | Ki | 0.0244 | 5 | 5 |
methylbufotenin | Homo sapiens (human) | Ki | 0.0520 | 1 | 1 |
alosetron | Homo sapiens (human) | IC50 | 0.1000 | 1 | 0 |
alosetron | Homo sapiens (human) | Ki | 0.0640 | 1 | 0 |
alpha-methylserotonin | Homo sapiens (human) | Ki | 0.0130 | 2 | 2 |
amiodarone | Homo sapiens (human) | IC50 | 0.9230 | 1 | 0 |
amiodarone | Homo sapiens (human) | Ki | 0.5870 | 1 | 0 |
dan 2163 | Homo sapiens (human) | Ki | 0.3162 | 1 | 1 |
amitriptyline | Homo sapiens (human) | IC50 | 0.0700 | 1 | 0 |
amitriptyline | Homo sapiens (human) | Ki | 0.0450 | 1 | 0 |
amoxapine | Homo sapiens (human) | IC50 | 0.0100 | 1 | 0 |
amoxapine | Homo sapiens (human) | Ki | 0.0066 | 1 | 0 |
astemizole | Homo sapiens (human) | IC50 | 0.0120 | 1 | 0 |
astemizole | Homo sapiens (human) | Ki | 0.0075 | 1 | 0 |
azelastine | Homo sapiens (human) | Ki | 0.0200 | 1 | 1 |
benzbromarone | Homo sapiens (human) | IC50 | 1.8040 | 1 | 0 |
benzbromarone | Homo sapiens (human) | Ki | 1.1480 | 1 | 0 |
bithionol | Homo sapiens (human) | IC50 | 6.7890 | 1 | 0 |
bithionol | Homo sapiens (human) | Ki | 4.3200 | 1 | 0 |
buspirone | Homo sapiens (human) | IC50 | 0.7500 | 1 | 0 |
buspirone | Homo sapiens (human) | Ki | 0.4770 | 1 | 0 |
verapamil | Homo sapiens (human) | IC50 | 0.1650 | 1 | 0 |
verapamil | Homo sapiens (human) | Ki | 0.1050 | 1 | 0 |
carvedilol | Homo sapiens (human) | IC50 | 0.0230 | 1 | 0 |
carvedilol | Homo sapiens (human) | Ki | 0.0150 | 1 | 0 |
chloroxylenol | Homo sapiens (human) | IC50 | 1.8560 | 1 | 0 |
chloroxylenol | Homo sapiens (human) | Ki | 1.1810 | 1 | 0 |
chlorpromazine | Homo sapiens (human) | IC50 | 0.1260 | 1 | 0 |
chlorpromazine | Homo sapiens (human) | Ki | 0.0573 | 3 | 2 |
cisapride | Homo sapiens (human) | IC50 | 0.0407 | 3 | 2 |
cisapride | Homo sapiens (human) | Ki | 0.0549 | 2 | 1 |
citalopram | Homo sapiens (human) | IC50 | 1.8390 | 1 | 0 |
citalopram | Homo sapiens (human) | Ki | 1.1710 | 1 | 0 |
clomipramine | Homo sapiens (human) | IC50 | 0.2390 | 1 | 0 |
clomipramine | Homo sapiens (human) | Ki | 0.1520 | 1 | 0 |
clotrimazole | Homo sapiens (human) | IC50 | 11.6040 | 1 | 0 |
clotrimazole | Homo sapiens (human) | Ki | 7.3850 | 1 | 0 |
cyproheptadine | Homo sapiens (human) | IC50 | 0.0094 | 1 | 0 |
cyproheptadine | Homo sapiens (human) | Ki | 0.0060 | 1 | 0 |
dicyclomine | Homo sapiens (human) | IC50 | 1.3010 | 1 | 0 |
dicyclomine | Homo sapiens (human) | Ki | 0.8280 | 1 | 0 |
diphenhydramine | Homo sapiens (human) | IC50 | 1.1180 | 1 | 0 |
diphenhydramine | Homo sapiens (human) | Ki | 0.7110 | 1 | 0 |
disulfiram | Homo sapiens (human) | IC50 | 34.5470 | 1 | 0 |
disulfiram | Homo sapiens (human) | Ki | 21.9840 | 1 | 0 |
domperidone | Homo sapiens (human) | IC50 | 2.6000 | 1 | 0 |
domperidone | Homo sapiens (human) | Ki | 1.6550 | 1 | 0 |
doxazosin | Homo sapiens (human) | IC50 | 0.3680 | 1 | 0 |
doxazosin | Homo sapiens (human) | Ki | 0.2340 | 1 | 0 |
doxepin | Homo sapiens (human) | IC50 | 0.0890 | 1 | 0 |
doxepin | Homo sapiens (human) | Ki | 0.0560 | 1 | 0 |
droperidol | Homo sapiens (human) | IC50 | 1.3420 | 1 | 0 |
droperidol | Homo sapiens (human) | Ki | 0.8540 | 1 | 0 |
ebastine | Homo sapiens (human) | IC50 | 0.3126 | 1 | 0 |
ebastine | Homo sapiens (human) | Ki | 0.1989 | 1 | 0 |
econazole | Homo sapiens (human) | IC50 | 6.8330 | 1 | 0 |
econazole | Homo sapiens (human) | Ki | 4.3480 | 1 | 0 |
fendiline | Homo sapiens (human) | Ki | 3.2170 | 1 | 1 |
fluphenazine | Homo sapiens (human) | IC50 | 0.0390 | 1 | 0 |
fluphenazine | Homo sapiens (human) | Ki | 0.0250 | 1 | 0 |
fluspirilene | Homo sapiens (human) | Ki | 0.1514 | 1 | 1 |
guanfacine | Homo sapiens (human) | IC50 | 2.0980 | 1 | 0 |
guanfacine | Homo sapiens (human) | Ki | 1.3350 | 1 | 0 |
haloperidol | Homo sapiens (human) | IC50 | 2.0500 | 1 | 0 |
haloperidol | Homo sapiens (human) | Ki | 0.6625 | 2 | 1 |
hexachlorophene | Homo sapiens (human) | IC50 | 5.6947 | 1 | 0 |
hexachlorophene | Homo sapiens (human) | Ki | 3.6239 | 1 | 0 |
ketanserin | Homo sapiens (human) | IC50 | 0.2900 | 1 | 1 |
ketanserin | Homo sapiens (human) | Ki | 0.1800 | 1 | 1 |
ketotifen | Homo sapiens (human) | IC50 | 0.0460 | 1 | 0 |
ketotifen | Homo sapiens (human) | Ki | 0.0303 | 2 | 1 |
labetalol | Homo sapiens (human) | IC50 | 3.0370 | 1 | 0 |
labetalol | Homo sapiens (human) | Ki | 1.9330 | 1 | 0 |
loperamide | Homo sapiens (human) | IC50 | 4.1050 | 1 | 0 |
loperamide | Homo sapiens (human) | Ki | 2.6130 | 1 | 0 |
loratadine | Homo sapiens (human) | IC50 | 0.2450 | 1 | 0 |
loratadine | Homo sapiens (human) | Ki | 0.1560 | 1 | 0 |
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one | Homo sapiens (human) | IC50 | 36.7070 | 1 | 0 |
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one | Homo sapiens (human) | Ki | 23.3590 | 1 | 0 |
maprotiline | Homo sapiens (human) | IC50 | 0.3360 | 1 | 0 |
maprotiline | Homo sapiens (human) | Ki | 0.2140 | 1 | 0 |
mescaline | Homo sapiens (human) | Ki | 0.7951 | 1 | 1 |
methapyrilene | Homo sapiens (human) | IC50 | 0.8430 | 1 | 0 |
methapyrilene | Homo sapiens (human) | Ki | 0.5370 | 1 | 0 |
nocodazole | Homo sapiens (human) | IC50 | 20.1800 | 1 | 0 |
nocodazole | Homo sapiens (human) | Ki | 12.8450 | 1 | 0 |
metoclopramide | Homo sapiens (human) | IC50 | 0.6300 | 1 | 0 |
metoclopramide | Homo sapiens (human) | Ki | 0.4010 | 1 | 0 |
mexiletine | Homo sapiens (human) | IC50 | 1.1380 | 1 | 0 |
mexiletine | Homo sapiens (human) | Ki | 0.7240 | 1 | 0 |
mianserin | Homo sapiens (human) | IC50 | 0.0073 | 1 | 0 |
mianserin | Homo sapiens (human) | Ki | 0.0046 | 1 | 0 |
miconazole | Homo sapiens (human) | IC50 | 5.5450 | 1 | 0 |
miconazole | Homo sapiens (human) | Ki | 3.5290 | 1 | 0 |
mitotane | Homo sapiens (human) | IC50 | 4.8320 | 1 | 0 |
mitotane | Homo sapiens (human) | Ki | 3.0750 | 1 | 0 |
nortriptyline | Homo sapiens (human) | IC50 | 0.1360 | 1 | 0 |
nortriptyline | Homo sapiens (human) | Ki | 0.0860 | 1 | 0 |
ondansetron | Homo sapiens (human) | IC50 | 0.7170 | 1 | 0 |
ondansetron | Homo sapiens (human) | Ki | 0.4560 | 1 | 0 |
orphenadrine | Homo sapiens (human) | IC50 | 3.3910 | 1 | 0 |
orphenadrine | Homo sapiens (human) | Ki | 2.1580 | 1 | 0 |
oxybutynin | Homo sapiens (human) | IC50 | 0.7920 | 1 | 0 |
oxybutynin | Homo sapiens (human) | Ki | 0.5040 | 1 | 0 |
oxymetazoline | Homo sapiens (human) | IC50 | 3.0560 | 1 | 0 |
oxymetazoline | Homo sapiens (human) | Ki | 1.9450 | 1 | 0 |
prazosin | Homo sapiens (human) | IC50 | 4.1180 | 1 | 0 |
prazosin | Homo sapiens (human) | Ki | 2.6210 | 1 | 0 |
prochlorperazine | Homo sapiens (human) | IC50 | 0.1020 | 1 | 0 |
prochlorperazine | Homo sapiens (human) | Ki | 0.0650 | 1 | 0 |
promazine | Homo sapiens (human) | IC50 | 0.3470 | 1 | 0 |
promazine | Homo sapiens (human) | Ki | 0.2210 | 1 | 0 |
promethazine | Homo sapiens (human) | IC50 | 0.0680 | 1 | 0 |
promethazine | Homo sapiens (human) | Ki | 0.0430 | 1 | 0 |
propafenone | Homo sapiens (human) | IC50 | 0.0920 | 1 | 0 |
propafenone | Homo sapiens (human) | Ki | 0.0580 | 1 | 0 |
propofol | Homo sapiens (human) | IC50 | 5.4990 | 1 | 0 |
propofol | Homo sapiens (human) | Ki | 3.4990 | 1 | 0 |
propranolol | Homo sapiens (human) | IC50 | 2.6769 | 2 | 1 |
propranolol | Homo sapiens (human) | Ki | 0.2180 | 1 | 0 |
psilocin | Homo sapiens (human) | IC50 | 0.0011 | 1 | 1 |
pyrilamine | Homo sapiens (human) | IC50 | 2.7880 | 1 | 0 |
pyrilamine | Homo sapiens (human) | Ki | 1.7740 | 1 | 0 |
quetiapine | Homo sapiens (human) | IC50 | 0.2135 | 1 | 0 |
quetiapine | Homo sapiens (human) | Ki | 0.2024 | 3 | 2 |
raloxifene | Homo sapiens (human) | IC50 | 0.3550 | 1 | 0 |
raloxifene | Homo sapiens (human) | Ki | 0.1475 | 2 | 1 |
risperidone | Homo sapiens (human) | IC50 | 0.0230 | 1 | 0 |
risperidone | Homo sapiens (human) | Ki | 0.0175 | 2 | 1 |
ritanserin | Homo sapiens (human) | IC50 | 0.0025 | 1 | 3 |
sb 206553 | Homo sapiens (human) | Ki | 0.0173 | 6 | 7 |
sulconazole | Homo sapiens (human) | IC50 | 3.0200 | 1 | 0 |
sulconazole | Homo sapiens (human) | Ki | 1.9220 | 1 | 0 |
terfenadine | Homo sapiens (human) | IC50 | 0.0480 | 1 | 0 |
terfenadine | Homo sapiens (human) | Ki | 0.0300 | 1 | 0 |
thioridazine | Homo sapiens (human) | IC50 | 0.1290 | 1 | 0 |
thioridazine | Homo sapiens (human) | Ki | 0.0820 | 1 | 0 |
tolnaftate | Homo sapiens (human) | IC50 | 2.0070 | 1 | 0 |
tolnaftate | Homo sapiens (human) | Ki | 1.2770 | 1 | 0 |
trazodone | Homo sapiens (human) | IC50 | 0.1070 | 1 | 0 |
trazodone | Homo sapiens (human) | Ki | 0.0680 | 1 | 0 |
troglitazone | Homo sapiens (human) | IC50 | 1.3120 | 1 | 0 |
troglitazone | Homo sapiens (human) | Ki | 0.8350 | 1 | 0 |
lysergic acid diethylamide | Homo sapiens (human) | Ki | 0.0300 | 1 | 1 |
phentolamine | Homo sapiens (human) | IC50 | 3.8070 | 1 | 0 |
phentolamine | Homo sapiens (human) | Ki | 2.4220 | 1 | 0 |
estrone | Homo sapiens (human) | IC50 | 13.6300 | 1 | 0 |
estrone | Homo sapiens (human) | Ki | 8.6760 | 1 | 0 |
2-acetylaminofluorene | Homo sapiens (human) | IC50 | 3.1700 | 1 | 0 |
2-acetylaminofluorene | Homo sapiens (human) | Ki | 2.0170 | 1 | 0 |
mepazine | Homo sapiens (human) | IC50 | 0.5140 | 1 | 0 |
mepazine | Homo sapiens (human) | Ki | 0.3270 | 1 | 0 |
n,n-dimethyltryptamine | Homo sapiens (human) | Ki | 0.1010 | 1 | 1 |
n,n'-diphenyl-4-phenylenediamine | Homo sapiens (human) | IC50 | 0.1420 | 1 | 0 |
n,n'-diphenyl-4-phenylenediamine | Homo sapiens (human) | Ki | 0.0900 | 1 | 0 |
cyclizine | Homo sapiens (human) | IC50 | 0.3730 | 1 | 0 |
cyclizine | Homo sapiens (human) | Ki | 0.2380 | 1 | 0 |
ergotamine | Homo sapiens (human) | IC50 | 0.0035 | 1 | 0 |
ergotamine | Homo sapiens (human) | Ki | 0.0022 | 1 | 0 |
methylergonovine | Homo sapiens (human) | IC50 | 0.0015 | 1 | 0 |
methylergonovine | Homo sapiens (human) | Ki | 0.0009 | 2 | 1 |
sterogenol | Homo sapiens (human) | IC50 | 5.6900 | 1 | 0 |
sterogenol | Homo sapiens (human) | Ki | 3.6210 | 1 | 0 |
yohimbine | Homo sapiens (human) | IC50 | 0.0740 | 1 | 0 |
yohimbine | Homo sapiens (human) | Ki | 0.0470 | 1 | 0 |
indopan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
methysergide | Homo sapiens (human) | IC50 | 0.0006 | 1 | 0 |
methysergide | Homo sapiens (human) | Ki | 0.0052 | 2 | 2 |
dihydroergotamine | Homo sapiens (human) | IC50 | 0.0068 | 1 | 0 |
dihydroergotamine | Homo sapiens (human) | Ki | 0.0043 | 1 | 0 |
dimenhydrinate | Homo sapiens (human) | IC50 | 1.7240 | 1 | 0 |
dimenhydrinate | Homo sapiens (human) | Ki | 1.0970 | 1 | 0 |
1-naphthylisothiocyanate | Homo sapiens (human) | IC50 | 25.1580 | 1 | 0 |
1-naphthylisothiocyanate | Homo sapiens (human) | Ki | 16.0090 | 1 | 0 |
Berberine chloride (TN) | Homo sapiens (human) | IC50 | 3.4370 | 1 | 0 |
Berberine chloride (TN) | Homo sapiens (human) | Ki | 2.1870 | 1 | 0 |
n-methyllaurotetanine | Homo sapiens (human) | Ki | 0.3230 | 1 | 1 |
glaucine | Homo sapiens (human) | Ki | 0.1190 | 1 | 1 |
dexpropranolol | Homo sapiens (human) | IC50 | 0.4380 | 1 | 0 |
dexpropranolol | Homo sapiens (human) | Ki | 0.2790 | 1 | 0 |
camptothecin | Homo sapiens (human) | IC50 | 0.9700 | 1 | 0 |
camptothecin | Homo sapiens (human) | Ki | 0.6170 | 1 | 0 |
clemastine | Homo sapiens (human) | IC50 | 0.0360 | 1 | 0 |
clemastine | Homo sapiens (human) | Ki | 0.0230 | 1 | 0 |
pizotyline | Homo sapiens (human) | Ki | 0.0020 | 1 | 1 |
metergoline | Homo sapiens (human) | IC50 | 0.0004 | 1 | 0 |
metergoline | Homo sapiens (human) | Ki | 0.0003 | 1 | 0 |
lisuride | Homo sapiens (human) | IC50 | 0.0051 | 1 | 0 |
lisuride | Homo sapiens (human) | Ki | 0.0032 | 1 | 0 |
bromocriptine | Homo sapiens (human) | IC50 | 0.0083 | 1 | 0 |
bromocriptine | Homo sapiens (human) | Ki | 0.0053 | 1 | 0 |
penfluridol | Homo sapiens (human) | Ki | 0.1840 | 1 | 1 |
5-methoxy-alpha-methyltryptamine | Homo sapiens (human) | Ki | 0.0078 | 2 | 2 |
6-fluoromelatonin | Homo sapiens (human) | Ki | 2.4950 | 1 | 1 |
bopindolol | Homo sapiens (human) | IC50 | 1.5230 | 1 | 0 |
bopindolol | Homo sapiens (human) | Ki | 0.9690 | 1 | 0 |
pergolide | Homo sapiens (human) | IC50 | 0.0760 | 1 | 0 |
pergolide | Homo sapiens (human) | Ki | 0.0490 | 1 | 0 |
cabergoline | Homo sapiens (human) | Ki | 0.0014 | 1 | 1 |
aripiprazole | Homo sapiens (human) | Ki | 0.0024 | 3 | 3 |
ziprasidone | Homo sapiens (human) | Ki | 0.0016 | 1 | 1 |
sertraline | Homo sapiens (human) | IC50 | 3.3935 | 1 | 0 |
sertraline | Homo sapiens (human) | Ki | 2.1595 | 1 | 0 |
mesulergine | Homo sapiens (human) | IC50 | 0.0052 | 1 | 1 |
mesulergine | Homo sapiens (human) | Ki | 0.0028 | 1 | 1 |
adrenoglomerulotropin | Homo sapiens (human) | Ki | 0.4910 | 1 | 1 |
ergocornine | Homo sapiens (human) | IC50 | 0.0110 | 1 | 0 |
ergocornine | Homo sapiens (human) | Ki | 0.0069 | 1 | 0 |
u 74006f | Homo sapiens (human) | IC50 | 18.5070 | 1 | 0 |
u 74006f | Homo sapiens (human) | Ki | 11.7770 | 1 | 0 |
way 100635 | Homo sapiens (human) | Ki | 0.0240 | 1 | 1 |
10-hydroxycarbamazepine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
mosapride | Homo sapiens (human) | IC50 | 0.2959 | 1 | 0 |
mosapride | Homo sapiens (human) | Ki | 0.1883 | 1 | 0 |
n(6)-(3-iodobenzyl)-5'-n-methylcarboxamidoadenosine | Homo sapiens (human) | Ki | 1.0800 | 2 | 2 |
desloratadine | Homo sapiens (human) | IC50 | 0.0430 | 1 | 0 |
desloratadine | Homo sapiens (human) | Ki | 0.0280 | 1 | 0 |
sb 200646 | Homo sapiens (human) | Ki | 0.0210 | 1 | 1 |
sc 53116 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
sc 53116 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
alpha-ergocryptine | Homo sapiens (human) | IC50 | 0.0130 | 1 | 0 |
alpha-ergocryptine | Homo sapiens (human) | Ki | 0.0082 | 1 | 0 |
n-demethyllysergic acid diethylamide | Homo sapiens (human) | IC50 | 0.0540 | 1 | 1 |
nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 0.5430 | 2 | 2 |
maduramicin | Homo sapiens (human) | IC50 | 0.0330 | 1 | 0 |
maduramicin | Homo sapiens (human) | Ki | 0.0210 | 1 | 0 |
rs 127445 | Homo sapiens (human) | IC50 | 0.0098 | 2 | 2 |
rs 127445 | Homo sapiens (human) | Ki | 0.0003 | 1 | 1 |
sorafenib | Homo sapiens (human) | Ki | 0.0560 | 1 | 1 |
estradiol 3-benzoate | Homo sapiens (human) | IC50 | 11.5650 | 1 | 0 |
estradiol 3-benzoate | Homo sapiens (human) | Ki | 7.3590 | 1 | 0 |
sb 221284 | Homo sapiens (human) | Ki | 0.0126 | 2 | 2 |
sb 228357 | Homo sapiens (human) | Ki | 0.0100 | 1 | 1 |
sb 243213 | Homo sapiens (human) | Ki | 0.1000 | 3 | 3 |
ergonovine | Homo sapiens (human) | IC50 | 0.0041 | 1 | 0 |
ergonovine | Homo sapiens (human) | Ki | 0.0026 | 1 | 0 |
dihydroergocristine monomesylate | Homo sapiens (human) | IC50 | 0.0066 | 1 | 0 |
dihydroergocristine monomesylate | Homo sapiens (human) | Ki | 0.0042 | 1 | 0 |
tretinoin | Homo sapiens (human) | IC50 | 0.3580 | 1 | 0 |
tretinoin | Homo sapiens (human) | Ki | 0.2280 | 1 | 0 |
diethylstilbestrol | Homo sapiens (human) | IC50 | 3.1400 | 1 | 0 |
diethylstilbestrol | Homo sapiens (human) | Ki | 1.9980 | 1 | 0 |
aclarubicin | Homo sapiens (human) | IC50 | 1.1060 | 1 | 0 |
aclarubicin | Homo sapiens (human) | Ki | 0.7040 | 1 | 0 |
(1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Homo sapiens (human) | IC50 | 0.9390 | 1 | 0 |
(1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Homo sapiens (human) | Ki | 0.5975 | 1 | 0 |
doxepin hydrochloride | Homo sapiens (human) | Ki | 0.0253 | 1 | 1 |
flunarizine | Homo sapiens (human) | IC50 | 1.0880 | 1 | 0 |
flunarizine | Homo sapiens (human) | Ki | 0.6920 | 1 | 0 |
benztropine | Homo sapiens (human) | IC50 | 0.2000 | 1 | 0 |
benztropine | Homo sapiens (human) | Ki | 0.1270 | 1 | 0 |
cinnarizine | Homo sapiens (human) | IC50 | 0.7310 | 1 | 0 |
cinnarizine | Homo sapiens (human) | Ki | 0.4650 | 1 | 0 |
enclomiphene | Homo sapiens (human) | IC50 | 1.3630 | 1 | 0 |
enclomiphene | Homo sapiens (human) | Ki | 0.8670 | 1 | 0 |
tamoxifen | Homo sapiens (human) | IC50 | 2.0840 | 1 | 0 |
tamoxifen | Homo sapiens (human) | Ki | 1.3260 | 1 | 0 |
dapiprazole | Homo sapiens (human) | IC50 | 1.0560 | 1 | 0 |
dapiprazole | Homo sapiens (human) | Ki | 0.6720 | 1 | 0 |
mitragynine | Homo sapiens (human) | Ki | 1.2600 | 1 | 1 |
2-chloro-n(6)-(3-iodobenzyl)adenosine-5'-n-methyluronamide | Homo sapiens (human) | Ki | 2.7700 | 1 | 1 |
paynantheine | Homo sapiens (human) | Ki | 0.0516 | 2 | 2 |
bp 897 | Homo sapiens (human) | Ki | 0.5710 | 3 | 3 |
ym348 | Homo sapiens (human) | Ki | 0.0025 | 1 | 1 |
ro 60-0175 | Homo sapiens (human) | Ki | 0.0051 | 2 | 2 |
4-[[(4-methylphenyl)sulfonylamino]methyl]-N-[2-[(phenylmethyl)-propan-2-ylamino]ethyl]benzamide | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
sb 242084 | Homo sapiens (human) | Ki | 0.1000 | 4 | 4 |
bw 723c86 | Homo sapiens (human) | IC50 | 0.0811 | 1 | 0 |
bw 723c86 | Homo sapiens (human) | Ki | 0.0516 | 1 | 0 |
sb 408124 | Homo sapiens (human) | Ki | 0.3200 | 1 | 1 |
montelukast | Homo sapiens (human) | IC50 | 6.2560 | 1 | 0 |
montelukast | Homo sapiens (human) | Ki | 3.9810 | 1 | 0 |
methysergide maleate | Homo sapiens (human) | Ki | 0.0019 | 1 | 1 |
isotretinoin | Homo sapiens (human) | IC50 | 0.8480 | 1 | 0 |
isotretinoin | Homo sapiens (human) | Ki | 0.5400 | 1 | 0 |
ly 344864 | Homo sapiens (human) | Ki | 0.5000 | 1 | 1 |
l 745870 | Homo sapiens (human) | Ki | 0.6000 | 2 | 2 |
mdl 100907 | Homo sapiens (human) | Ki | 1.2589 | 1 | 1 |
sb 258719 | Homo sapiens (human) | Ki | 5.0119 | 1 | 1 |
sb 271046 | Homo sapiens (human) | Ki | 3.9811 | 1 | 1 |
oxiconazole | Homo sapiens (human) | IC50 | 4.6064 | 1 | 0 |
oxiconazole | Homo sapiens (human) | Ki | 2.9314 | 1 | 0 |
guanabenz | Homo sapiens (human) | IC50 | 0.0970 | 1 | 0 |
guanabenz | Homo sapiens (human) | Ki | 0.0620 | 1 | 0 |
tg4-155 | Homo sapiens (human) | IC50 | 2.6000 | 1 | 1 |
sb 269970 | Homo sapiens (human) | Ki | 6.6683 | 3 | 3 |
sb 334867-a | Homo sapiens (human) | Ki | 3.9811 | 1 | 1 |
n-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide | Homo sapiens (human) | Ki | 3.9811 | 1 | 1 |
4-iodo-2,5-dimethoxyphenylisopropylamine, (r)-isomer | Homo sapiens (human) | Ki | 0.0127 | 3 | 3 |
sb258741 | Homo sapiens (human) | Ki | 2.5119 | 1 | 1 |
slv 313 | Homo sapiens (human) | Ki | 0.0126 | 1 | 1 |
fauc 346 | Homo sapiens (human) | Ki | 0.3500 | 1 | 1 |
pnu 96415e | Homo sapiens (human) | Ki | 0.0696 | 1 | 1 |
st 1936 | Homo sapiens (human) | Ki | 0.2450 | 1 | 1 |
n-(4-((4-(dimethylamino)quinazolin-2-yl)amino)cyclohexyl)-3,4-difluorobenzamide hydrochloride | Homo sapiens (human) | IC50 | 0.0798 | 2 | 2 |
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 | 0.2400 | 1 | 1 |
sb-656104-a | Homo sapiens (human) | Ki | 0.0912 | 1 | 1 |
pimavanserin | Homo sapiens (human) | IC50 | 0.0464 | 1 | 2 |
way 181187 | Homo sapiens (human) | Ki | 0.4298 | 2 | 4 |
2-(4-iodo-2,5-dimethoxyphenyl)-n-(2-methoxybenzyl)ethanamine | Homo sapiens (human) | Ki | 0.0023 | 1 | 1 |
fauc 365 | Homo sapiens (human) | Ki | 2.0000 | 1 | 1 |
sb-649915 | Homo sapiens (human) | Ki | 1.5849 | 1 | 1 |
meridianin a | Homo sapiens (human) | Ki | 0.1500 | 1 | 1 |
sb 215505 | Homo sapiens (human) | IC50 | 0.0385 | 2 | 2 |
mrs 3558 | Homo sapiens (human) | IC50 | 3.2600 | 1 | 1 |
naluzotan | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
prx 08066 | Homo sapiens (human) | IC50 | 0.1368 | 2 | 2 |
prx 08066 | Homo sapiens (human) | Ki | 0.0034 | 1 | 1 |
5-hydroxy-2-(2-phenylethyl)chromone | Homo sapiens (human) | IC50 | 8.9125 | 1 | 1 |
5-hydroxy-2-(2-phenylethyl)chromone | Homo sapiens (human) | Ki | 2.4547 | 1 | 1 |
col-144 | Homo sapiens (human) | Ki | 0.5930 | 1 | 1 |
lorcaserin | Homo sapiens (human) | Ki | 0.1517 | 5 | 5 |
td-5108 | Homo sapiens (human) | Ki | 0.0020 | 1 | 1 |
brexpiprazole | Homo sapiens (human) | Ki | 0.0004 | 1 | 1 |
mitragynine | Homo sapiens (human) | Ki | 0.0655 | 2 | 2 |
sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
lu aa33810 | Homo sapiens (human) | Ki | 0.2450 | 1 | 1 |
pf 04457845 | Homo sapiens (human) | Ki | 1.3437 | 1 | 0 |
e-52862 | Homo sapiens (human) | IC50 | 4.7000 | 1 | 1 |
e-52862 | Homo sapiens (human) | Ki | 0.3280 | 1 | 1 |
nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
skepinone-l | Homo sapiens (human) | Ki | 0.1724 | 1 | 0 |
n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 2.5311 | 2 | 4 |
ogerin | Homo sapiens (human) | Ki | 0.4964 | 1 | 0 |
tg6-10-1 | Homo sapiens (human) | IC50 | 7.5000 | 1 | 1 |
clozapine | Homo sapiens (human) | IC50 | 0.0810 | 2 | 3 |
clozapine | Homo sapiens (human) | Ki | 0.0051 | 3 | 2 |
olanzapine | Homo sapiens (human) | IC50 | 0.0570 | 1 | 0 |
olanzapine | Homo sapiens (human) | Ki | 0.0212 | 2 | 1 |
tegaserod | Homo sapiens (human) | Ki | 0.0020 | 1 | 1 |
methylaplysinopsin | Homo sapiens (human) | Ki | 4.5540 | 1 | 1 |
aplysinopsin | Homo sapiens (human) | Ki | 4.4490 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
ketanserin | Homo sapiens (human) | Kb | 1.9800 | 1 | 1 |
nuciferine | Homo sapiens (human) | Kb | 0.0310 | 1 | 1 |
metergoline | Homo sapiens (human) | Activity | 0.0026 | 1 | 1 |
roemerine | Homo sapiens (human) | Kb | 0.0840 | 1 | 1 |
yil 781 | Homo sapiens (human) | Activity | 1.0000 | 1 | 1 |
Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHBioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 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
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
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
A novel (benzodifuranyl)aminoalkane with extremely potent activity at the 5-HT2A receptor.Journal of medicinal chemistry, , Dec-17, Volume: 41, Issue:26, 1998
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
Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 20, Issue:3, 2010
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
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
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
Serotonin receptor binding affinities of several hallucinogenic phenylalkylamine and N,N-dimethyltryptamine analogues.Journal of medicinal chemistry, , Volume: 21, Issue:8, 1978
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
A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole.Journal of medicinal chemistry, , Sep-11, Volume: 46, Issue:19, 2003
Development, validation, and use of quantitative structure-activity relationship models of 5-hydroxytryptamine (2B) receptor ligands to identify novel receptor binders and putative valvulopathic compounds among common drugs.Journal of medicinal chemistry, , Nov-11, Volume: 53, Issue:21, 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],
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],
Synthesis and evaluation of nuciferine and roemerine enantiomers as 5-HTMedChemComm, , Mar-01, Volume: 9, Issue:3, 2018
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 23, Issue:6, 2013
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
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 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],
Semisynthetic Transformations on (+)-Boldine Reveal a 5-HTJournal of natural products, , 09-23, Volume: 85, Issue:9, 2022
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective DJournal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Pharmacophore-based tailoring of biphenyl amide derivatives as selective 5-hydroxytryptamine 2B receptor antagonists.MedChemComm, , Jun-01, Volume: 9, Issue:6, 2018
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 24, Issue:2, 2014
Development, validation, and use of quantitative structure-activity relationship models of 5-hydroxytryptamine (2B) receptor ligands to identify novel receptor binders and putative valvulopathic compounds among common drugs.Journal of medicinal chemistry, , Nov-11, Volume: 53, Issue:21, 2010
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
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
A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole.Journal of medicinal chemistry, , Sep-11, Volume: 46, Issue:19, 2003
[no title available]European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
Design and synthesis of dual 5-HT1A and 5-HT7 receptor ligands.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
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, , 12-22, Volume: 59, Issue:24, 2016
In vivo phenotypic screening for treating chronic neuropathic pain: modification of C2-arylethynyl group of conformationally constrained A3 adenosine receptor agonists.Journal of medicinal chemistry, , Dec-11, Volume: 57, Issue:23, 2014
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
C4 phenyl aporphines with selective h5-HT(2B) receptor affinity.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 25, Issue:17, 2015
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 20, Issue:2, 2010
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
A new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 19, Issue:8, 2009
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
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
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
Development, validation, and use of quantitative structure-activity relationship models of 5-hydroxytryptamine (2B) receptor ligands to identify novel receptor binders and putative valvulopathic compounds among common drugs.Journal of medicinal chemistry, , Nov-11, Volume: 53, Issue:21, 2010
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 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
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
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
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
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
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
A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole.Journal of medicinal chemistry, , Sep-11, Volume: 46, Issue:19, 2003
Thieno[2,3-d]pyrimidine as a promising scaffold in medicinal chemistry: Recent advances.Bioorganic & medicinal chemistry, , 04-01, Volume: 27, Issue:7, 2019
A new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 19, Issue:8, 2009
Discovery of a lead series of potent benzodiazepine 5-HTBioorganic & medicinal chemistry letters, , 03-01, Volume: 30, Issue:5, 2020
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
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
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
Design and Discovery of Functionally Selective Serotonin 2C (5-HTJournal of medicinal chemistry, , 11-10, Volume: 59, Issue:21, 2016
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
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
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
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
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
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
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],
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 alpha-subunit binding | molecular function | Binding to a G-protein alpha subunit. The alpha subunit binds a guanine nucleotide. [GOC:hjd] |
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] |
GTPase activator activity | molecular function | Binds to and increases the activity of a GTPase, an enzyme that catalyzes the hydrolysis of GTP. [GOC:mah] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
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] |
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 4 target(s):
Target | Category | Definition |
nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
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 |
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] |
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] |
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 37 target(s):
Target | Category | Definition |
neural crest cell migration | biological process | The characteristic movement of cells from the dorsal ridge of the neural tube to a variety of locations in a vertebrate embryo. [GOC:ascb_2009, GOC:dph, GOC:tb, ISBN:0878932437] |
positive regulation of cytokine production | biological process | Any process that activates or increases the frequency, rate or extent of production of a cytokine. [GOC:add, ISBN:0781735149] |
positive regulation of endothelial cell proliferation | biological process | Any process that activates or increases the rate or extent of endothelial cell proliferation. [GOC:add] |
G protein-coupled receptor internalization | biological process | The process that results in the uptake of a G protein-coupled receptor into an endocytic vesicle. [PMID:8396717] |
heart morphogenesis | biological process | The developmental process in which the heart is generated and organized. The heart is a hollow, muscular organ, which, by contracting rhythmically, keeps up the circulation of the blood. [GOC:dph, GOC:isa_complete] |
cardiac muscle hypertrophy | biological process | The enlargement or overgrowth of all or part of the heart muscle due to an increase in size of cardiac muscle cells without cell division. [GOC:mtg_heart] |
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] |
G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
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] |
protein kinase C-activating G protein-coupled receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of a G protein-coupled receptor binding to its physiological ligand, where the pathway proceeds with activation of protein kinase C (PKC). PKC is activated by second messengers including diacylglycerol (DAG). [GOC:mah, GOC:signaling] |
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] |
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] |
neural crest cell differentiation | biological process | The process in which a relatively unspecialized cell acquires specialized features of a neural crest cell. [GOC:dh, GOC:ef] |
intestine 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 intestine. 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 intestine is the section of the alimentary canal from the stomach to the anal canal. It includes the large intestine and small intestine. [GOC:mtg_muscle, MA:0001539, MSH:D007422] |
phosphorylation | biological process | The process of introducing a phosphate group into a molecule, usually with the formation of a phosphoric ester, a phosphoric anhydride or a phosphoric amide. [ISBN:0198506732] |
calcium-mediated signaling | biological process | Any intracellular signal transduction in which the signal is passed on within the cell via calcium ions. [GOC:signaling] |
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] |
vasoconstriction | biological process | A decrease in the diameter of blood vessels, especially arteries, due to constriction of smooth muscle cells that line the vessels, and usually causing an increase in blood pressure. [GOC:pr, ISBN:0192800752] |
negative regulation of apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
positive regulation of canonical NF-kappaB signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of a canonical NF-kappaB signaling cascade. [GOC:jl] |
positive regulation of MAP kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of MAP kinase activity. [GOC:dph, GOC:go_curators] |
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] |
embryonic morphogenesis | biological process | The process in which anatomical structures are generated and organized during the embryonic phase. The embryonic phase begins with zygote formation. The end of the embryonic phase is organism-specific. For example, it would be at birth for mammals, larval hatching for insects and seed dormancy in plants. [GOC:jid, GOC:mtg_sensu] |
regulation of behavior | biological process | Any process that modulates the frequency, rate or extent of behavior, the internally coordinated responses (actions or inactions) of whole living organisms (individuals or groups) to internal or external stimuli. [GOC:go_curators, GOC:pr] |
positive regulation of nitric-oxide synthase activity | biological process | Any process that activates or increases the activity of the enzyme nitric-oxide synthase. [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 cell division | biological process | Any process that activates or increases the frequency, rate or extent of cell division. [GOC:ai] |
ERK1 and ERK2 cascade | biological process | A MAPK cascade containing at least the ERK1 or ERK2 MAP kinases. It starts with the activation of a MAP3K, and the consecutive activation of a MPK2K and of ERK1 or ERK2. The cascade can also contain an additional tier: the upstream MAP4K. The kinases in each tier phosphorylate and activate the kinase in the downstream tier. The ERK1/ERK2 cascade is activated by mitogens, growth factors, G protein-coupled receptors, and results in cellular responses such as cell proliferation, cell differentiation and development. [PMID:20811974, PMID:23125017, PMID:28903453] |
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] |
protein kinase C signaling | biological process | A series of reactions, mediated by the intracellular serine/threonine kinase protein kinase C, which occurs as a result of a single trigger reaction or compound. [GOC:BHF, GOC:mah] |
cellular response to temperature stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a temperature stimulus. [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] |
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] |
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] |