Page last updated: 2024-08-07 16:47:33

5-hydroxytryptamine receptor 6

A 5-hydroxytryptamine receptor 6 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P50406]

Synonyms

5-HT-6;
5-HT6;
Serotonin receptor 6

Research

Bioassay Publications (140)

TimeframeStudies on this Protein(%)All Drugs %
pre-19901 (0.71)18.7374
1990's2 (1.43)18.2507
2000's50 (35.71)29.6817
2010's62 (44.29)24.3611
2020's25 (17.86)2.80

Compounds (158)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
tryptamineHomo sapiens (human)Ki0.180011
8-hydroxy-2-(di-n-propylamino)tetralinHomo sapiens (human)Ki10.000011
octoclothepineHomo sapiens (human)Ki0.050011
1-(1-naphthyl)piperazineHomo sapiens (human)Ki0.108033
1-(2-methoxyphenyl)piperazineHomo sapiens (human)Ki0.001211
1-(3-chlorophenyl)piperazineHomo sapiens (human)Ki2.024022
2-methyl-5-htHomo sapiens (human)Ki0.164033
5-carboxamidotryptamineHomo sapiens (human)Ki0.860022
methylbufoteninHomo sapiens (human)Ki0.030844
5-methoxytryptamineHomo sapiens (human)Ki0.069022
amiodaroneHomo sapiens (human)IC5019.441010
amiodaroneHomo sapiens (human)Ki9.026010
amitriptylineHomo sapiens (human)IC500.140010
amitriptylineHomo sapiens (human)Ki0.065010
amlodipineHomo sapiens (human)IC502.898010
amlodipineHomo sapiens (human)Ki1.346010
amoxapineHomo sapiens (human)IC500.076010
amoxapineHomo sapiens (human)Ki0.035010
astemizoleHomo sapiens (human)IC503.266010
astemizoleHomo sapiens (human)Ki1.516010
buspironeHomo sapiens (human)Ki0.012011
carvedilolHomo sapiens (human)IC501.519010
carvedilolHomo sapiens (human)Ki0.705010
chlorpromazineHomo sapiens (human)IC500.057010
chlorpromazineHomo sapiens (human)Ki0.041755
clomipheneHomo sapiens (human)Ki1.956011
clomipramineHomo sapiens (human)IC500.245010
clomipramineHomo sapiens (human)Ki0.113021
clotrimazoleHomo sapiens (human)IC5012.543010
clotrimazoleHomo sapiens (human)Ki5.824010
cyproheptadineHomo sapiens (human)IC500.281010
cyproheptadineHomo sapiens (human)Ki0.130010
dapsoneHomo sapiens (human)Ki0.183011
dicyclomineHomo sapiens (human)IC503.065010
dicyclomineHomo sapiens (human)Ki1.423010
disulfiramHomo sapiens (human)IC5016.001010
disulfiramHomo sapiens (human)Ki7.429010
doxepinHomo sapiens (human)IC500.320010
doxepinHomo sapiens (human)Ki0.127021
ebastineHomo sapiens (human)IC502.197410
ebastineHomo sapiens (human)Ki1.020210
econazoleHomo sapiens (human)IC5010.899010
econazoleHomo sapiens (human)Ki5.060010
fluphenazineHomo sapiens (human)IC500.052010
fluphenazineHomo sapiens (human)Ki0.037021
fluoxetineHomo sapiens (human)IC501.661010
fluoxetineHomo sapiens (human)Ki0.771010
fluspirileneHomo sapiens (human)Ki1.188011
flutamideHomo sapiens (human)IC5017.814010
flutamideHomo sapiens (human)Ki8.271010
haloperidolHomo sapiens (human)Ki4.027733
haloproginHomo sapiens (human)IC504.011010
haloproginHomo sapiens (human)Ki1.862010
imipramineHomo sapiens (human)Ki3.730013
ketanserinHomo sapiens (human)Ki2.800011
ketotifenHomo sapiens (human)IC501.141010
ketotifenHomo sapiens (human)Ki0.530010
loxapineHomo sapiens (human)Ki0.032522
maprotilineHomo sapiens (human)IC500.892010
maprotilineHomo sapiens (human)Ki0.414010
methapyrileneHomo sapiens (human)IC503.091010
methapyrileneHomo sapiens (human)Ki1.435010
methiothepinHomo sapiens (human)IC500.030055
methiothepinHomo sapiens (human)Ki0.00141010
mianserinHomo sapiens (human)IC500.085010
mianserinHomo sapiens (human)Ki0.047521
miconazoleHomo sapiens (human)IC5010.887010
miconazoleHomo sapiens (human)Ki5.055010
mitotaneHomo sapiens (human)IC501.402010
mitotaneHomo sapiens (human)Ki0.651010
nortriptylineHomo sapiens (human)IC500.554010
nortriptylineHomo sapiens (human)Ki0.235521
orphenadrineHomo sapiens (human)IC501.121010
orphenadrineHomo sapiens (human)Ki0.521010
oxymetazolineHomo sapiens (human)IC501.670010
oxymetazolineHomo sapiens (human)Ki0.775010
prochlorperazineHomo sapiens (human)IC500.267010
prochlorperazineHomo sapiens (human)Ki0.124010
promazineHomo sapiens (human)IC500.274010
promazineHomo sapiens (human)Ki0.127010
promethazineHomo sapiens (human)IC502.429010
promethazineHomo sapiens (human)Ki1.128010
propafenoneHomo sapiens (human)IC501.863010
propafenoneHomo sapiens (human)Ki0.865010
propranololHomo sapiens (human)IC504.038421
propranololHomo sapiens (human)Ki1.423010
quetiapineHomo sapiens (human)Ki1.400011
quipazineHomo sapiens (human)Ki3.600011
raloxifeneHomo sapiens (human)Ki0.750011
risperidoneHomo sapiens (human)Ki1.212488
spiperoneHomo sapiens (human)Ki1.595022
sulfadimethoxineHomo sapiens (human)IC501.339010
sulfadimethoxineHomo sapiens (human)Ki0.622010
terfenadineHomo sapiens (human)IC501.306010
terfenadineHomo sapiens (human)Ki0.606010
thioridazineHomo sapiens (human)IC500.071010
thioridazineHomo sapiens (human)Ki0.052021
lysergic acid diethylamideHomo sapiens (human)Ki0.006622
mepazineHomo sapiens (human)IC501.837010
mepazineHomo sapiens (human)Ki0.853010
bisphenol aHomo sapiens (human)IC505.420010
bisphenol aHomo sapiens (human)Ki2.516010
rotenoneHomo sapiens (human)IC500.870010
rotenoneHomo sapiens (human)Ki0.404010
ergotamineHomo sapiens (human)IC500.002010
ergotamineHomo sapiens (human)Ki0.000910
methylergonovineHomo sapiens (human)IC500.002510
methylergonovineHomo sapiens (human)Ki0.001210
dibenzothiazyl disulfideHomo sapiens (human)IC505.276010
dibenzothiazyl disulfideHomo sapiens (human)Ki2.450010
yohimbineHomo sapiens (human)IC501.689010
yohimbineHomo sapiens (human)Ki0.784010
indopanHomo sapiens (human)Ki0.910512
dibenzepinHomo sapiens (human)Ki3.300011
methysergideHomo sapiens (human)IC500.162010
methysergideHomo sapiens (human)Ki0.075010
2-bromolysergic acid diethylamideHomo sapiens (human)Ki0.017011
dihydroergotamineHomo sapiens (human)IC500.003210
dihydroergotamineHomo sapiens (human)Ki0.001510
pimozideHomo sapiens (human)Ki0.071011
n-methyllaurotetanineHomo sapiens (human)Ki0.306011
clemastineHomo sapiens (human)IC500.077010
clemastineHomo sapiens (human)Ki0.036010
metergolineHomo sapiens (human)IC500.028010
metergolineHomo sapiens (human)Ki0.013010
lisurideHomo sapiens (human)IC500.012010
lisurideHomo sapiens (human)Ki0.005510
bromocriptineHomo sapiens (human)IC500.022010
bromocriptineHomo sapiens (human)Ki0.030021
penfluridolHomo sapiens (human)Ki1.000011
pergolideHomo sapiens (human)IC500.039010
pergolideHomo sapiens (human)Ki0.018010
ipsapironeHomo sapiens (human)Ki16.800011
sertindoleHomo sapiens (human)Ki0.005011
aripiprazoleHomo sapiens (human)Ki0.264866
ziprasidoneHomo sapiens (human)Ki0.056255
mesulergineHomo sapiens (human)Ki0.776112
ergocornineHomo sapiens (human)IC500.015010
ergocornineHomo sapiens (human)Ki0.007110
gr 127935Homo sapiens (human)Ki10.000011
tryptolineHomo sapiens (human)Ki5.000011
5-methoxy 3-(1,2,3,6-tetrahydro-4-pyridinyl)1h indoleHomo sapiens (human)IC500.079011
pramipexoleHomo sapiens (human)Ki10.000011
desloratadineHomo sapiens (human)IC502.171010
desloratadineHomo sapiens (human)Ki1.008010
alpha-ergocryptineHomo sapiens (human)IC500.016010
alpha-ergocryptineHomo sapiens (human)Ki0.007610
3-(1-methyl-1,2,3,6-tetrahydropyrid-4-yl)indoleHomo sapiens (human)Ki0.098011
harmalanHomo sapiens (human)Ki1.450011
n-demethyllysergic acid diethylamideHomo sapiens (human)IC500.016011
nantenine, (+-)-isomerHomo sapiens (human)Ki0.257011
maduramicinHomo sapiens (human)IC500.001710
maduramicinHomo sapiens (human)Ki0.000810
latrepirdineHomo sapiens (human)IC500.980033
latrepirdineHomo sapiens (human)Ki0.030855
sorafenibHomo sapiens (human)Ki6.213011
1-(benzenesulfonyl)indoleHomo sapiens (human)Ki0.159011
1-methyl-6-methoxy-dihydro-beta-carbolineHomo sapiens (human)Ki1.930011
sb 243213Homo sapiens (human)IC500.667011
ergonovineHomo sapiens (human)IC500.003210
ergonovineHomo sapiens (human)Ki0.001510
dihydroergocristine monomesylateHomo sapiens (human)IC500.042010
dihydroergocristine monomesylateHomo sapiens (human)Ki0.019010
diethylstilbestrolHomo sapiens (human)IC5012.892010
diethylstilbestrolHomo sapiens (human)Ki5.986010
chlorprothixeneHomo sapiens (human)Ki0.003011
3,4,5-trimethoxycinnamic acidHomo sapiens (human)IC5010.000024
2-(2,3-dihydroindol-1-yl)-N,N-dimethylethanamineHomo sapiens (human)Ki5.000011
benztropineHomo sapiens (human)IC502.788010
benztropineHomo sapiens (human)Ki1.294010
enclomipheneHomo sapiens (human)IC501.522010
enclomipheneHomo sapiens (human)Ki0.707010
tamoxifenHomo sapiens (human)IC502.679010
tamoxifenHomo sapiens (human)Ki1.142521
toremifeneHomo sapiens (human)Ki4.125011
rasagilineHomo sapiens (human)Ki0.001411
sb 258585Homo sapiens (human)IC500.019011
sb 258585Homo sapiens (human)Ki0.002522
bw 723c86Homo sapiens (human)IC500.641410
bw 723c86Homo sapiens (human)Ki0.297810
harmineHomo sapiens (human)Ki1.480011
l 745870Homo sapiens (human)Ki1.656211
zuclopenthixolHomo sapiens (human)Ki0.169011
ro 63-0563Homo sapiens (human)Ki0.05851011
ro 4-6790Homo sapiens (human)IC500.026311
ro 4-6790Homo sapiens (human)Ki0.05151111
sb 258719Homo sapiens (human)Ki15.848911
sb 271046Homo sapiens (human)IC500.002011
sb 271046Homo sapiens (human)Ki0.00191819
sb 269970Homo sapiens (human)Ki8.154822
2-ethyl-5-methoxy-n,n-dimethyltryptamineHomo sapiens (human)IC500.085022
2-ethyl-5-methoxy-n,n-dimethyltryptamineHomo sapiens (human)Ki0.02241111
5-methoxy-2-phenyl-n,n-dimethyltryptamineHomo sapiens (human)Ki0.030766
ms-245Homo sapiens (human)Ki0.00422324
n-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamideHomo sapiens (human)Ki0.003077
sb 399885Homo sapiens (human)IC500.097011
sb 399885Homo sapiens (human)Ki0.000755
ro4368554Homo sapiens (human)Ki0.000511
4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamineHomo sapiens (human)IC500.003211
4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamineHomo sapiens (human)Ki0.001044
st 1936Homo sapiens (human)IC500.040011
sb-656104-aHomo sapiens (human)Ki0.851111
5-chloro-2-methyl-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1h-indoleHomo sapiens (human)IC500.007422
way 181187Homo sapiens (human)Ki0.1161911
gsk215083Homo sapiens (human)Ki0.000311
e-6801Homo sapiens (human)Ki0.046277
sb-649915Homo sapiens (human)Ki10.000011
way-208466Homo sapiens (human)Ki0.004844
barettinHomo sapiens (human)Ki10.000011
sb 742457Homo sapiens (human)IC500.026444
sb 742457Homo sapiens (human)Ki0.00131213
naluzotanHomo sapiens (human)Ki5.000011
4-(4-chlorophenyl)sulfonyl-5-(3,4-dihydro-1H-isoquinolin-2-yl)-2-ethylsulfonylthiazoleHomo sapiens (human)Ki0.129333
af 353Homo sapiens (human)Ki100,000.000011
a 803467Homo sapiens (human)IC5010.000011
sam-531Homo sapiens (human)Ki0.001333
sp 203Homo sapiens (human)Ki10.000011
lu ae58054Homo sapiens (human)IC500.513022
lu ae58054Homo sapiens (human)Ki0.0017910
e-55888Homo sapiens (human)Ki1.000011
pf 3246799Homo sapiens (human)IC501.800011
n-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamideHomo sapiens (human)Ki1.571022
n,n-diallyl-5-methoxytryptamineHomo sapiens (human)Ki2.581024
clozapineHomo sapiens (human)IC500.017143
clozapineHomo sapiens (human)Ki0.01701719
olanzapineHomo sapiens (human)IC500.013010
olanzapineHomo sapiens (human)Ki0.01011717
methylaplysinopsinHomo sapiens (human)Ki1.716011
aplysinopsinHomo sapiens (human)Ki8.768011

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
methylbufoteninHomo sapiens (human)Kd0.079411
propranololHomo sapiens (human)EC505.011911
ms-245Homo sapiens (human)Kd0.001311
4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamineHomo sapiens (human)Kd0.003211
st 1936Homo sapiens (human)EC500.044811
way 181187Homo sapiens (human)EC500.006533
e-6801Homo sapiens (human)EC500.000122
way-208466Homo sapiens (human)EC500.007333

Drugs with Other Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
methiothepinHomo sapiens (human)Kb0.003711
mianserinHomo sapiens (human)Kb0.030011
ondansetronHomo sapiens (human)Kb10.000011
metergolineHomo sapiens (human)Activity0.091011
sb 258585Homo sapiens (human)Kb0.000422
sb 271046Homo sapiens (human)Kb0.005811
ms-245Homo sapiens (human)Affinity0.016011
ms-245Homo sapiens (human)Kb0.005811
ms-245Homo sapiens (human)pA20.008911
sb 399885Homo sapiens (human)Kb0.000922
sb 742457Homo sapiens (human)Kb0.001044
lu ae58054Homo sapiens (human)Kb0.004111
clozapineHomo sapiens (human)INH0.006411
norclozapineHomo sapiens (human)INH0.008811

Enables

This protein enables 4 target(s):

TargetCategoryDefinition
histamine receptor activitymolecular functionCombining with histamine to initiate a change in cell activity. Histamine is a physiologically active amine, found in plant and animal tissue and released from mast cells as part of an allergic reaction in humans. [GOC:ai]
protein bindingmolecular functionBinding to a protein. [GOC:go_curators]
neurotransmitter receptor activitymolecular functionCombining with a neurotransmitter and transmitting the signal to initiate a change in cell activity. [GOC:jl, GOC:signaling]
G protein-coupled serotonin receptor activitymolecular functionCombining 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]

Located In

This protein is located in 3 target(s):

TargetCategoryDefinition
plasma membranecellular componentThe membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]
ciliumcellular componentA specialized eukaryotic organelle that consists of a filiform extrusion of the cell surface and of some cytoplasmic parts. Each cilium is largely bounded by an extrusion of the cytoplasmic (plasma) membrane, and contains a regular longitudinal array of microtubules, anchored to a basal body. [GOC:cilia, GOC:curators, GOC:kmv, GOC:vw, ISBN:0198547684, PMID:16824949, PMID:17009929, PMID:20144998]
synapsecellular componentThe 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):

TargetCategoryDefinition
dendritecellular componentA 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 membranecellular componentThe membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]

Involved In

This protein is involved in 6 target(s):

TargetCategoryDefinition
cerebral cortex cell migrationbiological processThe orderly movement of cells from one site to another in the cerebral cortex. [GO_REF:0000021, GOC:cls, GOC:dgh, GOC:dph, GOC:jid]
positive regulation of TOR signalingbiological processAny process that activates or increases the frequency, rate or extent of TOR signaling. [GOC:mah]
G protein-coupled serotonin receptor signaling pathwaybiological processThe series of molecular signals generated as a consequence of a G protein-coupled serotonin receptor binding to one of its physiological ligands. [GOC:mah]
chemical synaptic transmissionbiological processThe 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]
adenylate cyclase-modulating G protein-coupled receptor signaling pathwaybiological processA G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of adenylyl cyclase activity and a subsequent change in the intracellular concentration of cyclic AMP (cAMP). [GOC:mah, GOC:signaling, ISBN:0815316194]
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerbiological processA 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]