Page last updated: 2024-08-05 14:59:05

serotonergic agonist

An agent that has an affinity for serotonin receptors and is able to mimic the effects of serotonin by stimulating the physiologic activity at the cell receptors. Serotonin agonists are used as antidepressants, anxiolytics, and in the treatment of migraine disorders.

ChEBI ID: 35941

Members (41)

MemberDefinitionClass
1-((4-fluorobenzoylamino)ethyl)-4-(7-methoxy-1-naphthyl)piperazine hydrochlorideA hydrochloride salt that is obtained by reaction of 4-fluoro-N-{2-[4-(7-methoxynaphthalen-1-yl)piperazin-1-yl]ethyl}benzamide with one equivalent of hydrogen chloride. Highly potent selective 5-HT1A receptor full agonist (pKi values are 9.0, 6.6, 7.5, 6.6 and < 6.0 for 5-HT1A, 5-HT1B, 5-HT1C, 5-HT2 and 5-HT3 receptors respectively). Possibly binds between the agonist binding site and the G protein interaction switch site, affecting the activation mechanism, and may display positive cooperativity. Anxiolytic following central administration in vivo.4-fluoro-N-{2-[4-(7-methoxynaphthalen-1-yl)piperazin-1-yl]ethyl}benzamide hydrochloride
1-(2-(4-aminophenyl)ethyl)-4-(3-trifluoromethylphenyl)piperazineA N-arylpiperazine that is piperazine substituted by 2-(4-aminophenyl)ethyl and 3-(trifluoromethyl)phenyl groups at positions 1 and 4, respectively. It is a selective 5-HT1A serotonin receptor agonist and 5-HT1D serotonin receptor antagonist.LY-165163
1-(3-chlorophenyl)piperazineA N-arylpiperazine that is piperazine carrying a 3-chlorophenyl substituent at position 1. It is a metabolite of the antidepressant drug trazodone.1-(3-chlorophenyl)piperazine
1-(3-trifluoromethylphenyl)piperazineA N-arylpiperazine that is piperazine substituted by a 3-(trifluoromethyl)phenyl group at position 1. A serotonergic agonist used as a recreational drug.1-(3-(trifluoromethyl)phenyl)piperazine
1-benzylpiperazineA tertiary amino compound that is piperazine substituted by a benzyl group at position 1. It is a serotonergic agonist used as a recreational drug.1-benzylpiperazine
2-methyl-5-ht2-methylserotonin
5-(nonyloxy)tryptamineA tryptamine derivative that consists of serotonin bearing an additional O-nonyl substituent. 5-HT1B selective agonist, several times more potent than sumatriptan and inactive as a 5-HT1A agonist (Ki at 5-HT1B = 1 nM, selectivity over 5-HT1A > 300-fold).5-nonyloxytryptamine
5-methoxytryptamineA member of the class of tryptamines that is the methyl ether derivative of serotonin.5-methoxytryptamine
almotriptanAn indole compound having a 2-(dimethylamino)ethyl group at the 3-position and a (pyrrolidin-1-ylsulfonyl)methyl group at the 5-position.almotriptan
alpha-methylserotoninalpha-methylserotonin
aripiprazoleAn N-arylpiperazine that is piperazine substituted by a 4-[(2-oxo-1,2,3,4-tetrahydroquinolin-7-yl)oxy]butyl group at position 1 and by a 2,3-dichlorophenyl group at position 4. It is an antipsychotic drug used for the treatment of Schizophrenia, and other mood disorders.aripiprazole
aripiprazole lauroxilA dodecanoate ester obtained by formal condensation of the carboxy group of dodecanoic acid with the hydroxy group of 7-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy}-2-oxo-3,4-dihydroquinolin-1(2H)-yl]methanol. A prodrug for aripiprazole, it is used for treatment of schizophrenia.aripiprazole lauroxil
buspironeAn azaspiro compound that is 8-azaspiro[4.5]decane-7,9-dione substituted at the nitrogen atom by a 4-(piperazin-1-yl)butyl group which in turn is substituted by a pyrimidin-2-yl group at the N(4) position.buspirone
buspirone hydrochlorideA hydrochloride salt resulting from the reaction of equimolar amounts of buspirone and hydrogen chloride.buspirone hydrochloride
cgs 12066A pyrroloquinoxaline that is pyrrolo[1,2-a]quinoxaline bearing additional 4-methylpiperazin-1-yl and trifluoromethyl substituents at positions 4 and 7 respectively. A 5-hydroxytryptamine receptor 1B (5-HT1B) full agonist, 10-fold selective over 5-HT1A and 1000-fold selective over 5-HT2C receptors. Centrally active following systemic administration.4-(4-methylpiperazin-1-yl)-7-(trifluoromethyl)pyrrolo[1,2-a]quinoxaline
cgs 12066bA maleate salt that is the dimaleate salt of 4-(4-methylpiperazin-1-yl)-7-(trifluoromethyl)pyrrolo[1,2-a]quinoxaline. A 5-hydroxytryptamine receptor 1B (5-HT1B) full agonist, 10-fold selective over 5-HT1A and 1000-fold selective over 5-HT2C receptors. Centrally active following systemic administration.4-(4-methylpiperazin-1-yl)-7-(trifluoromethyl)pyrrolo[1,2-a]quinoxaline dimaleate
dexfenfluramineThe S-enantiomer of fenfluramine. It stimulates the release of serotonin and selectively inhibits its reuptake, but unlike fenfluramine it does not possess catecholamine agonist activity. It was formerly given by mouth as the hydrochloride in the treatment of obesity, but, like fenfluramine, was withdrawn wolrdwide following reports of valvular heart defects.(S)-fenfluramine
dexfenfluramine hydrochlorideThe hydrochloride salt of (S)-fenfluramine. It stimulates the release of serotonin and selectively inhibits its reuptake, but unlike the racemate it does not possess catecholamine agonist activity. It was formerly given by mouth in the treatment of obesity, but, like the racemate, was withdrawn wolrdwide following reports of valvular heart defects.(S)-fenfluramine hydrochloride
dihydroergotamineErgotamine in which a single bond replaces the double bond between positions 9 and 10. A semisynthetic ergot alkaloid with weaker oxytocic and vasoconstrictor properties than ergotamine, it is used (as the methanesulfonic or tartaric acid salts) for the treatment of migraine and orthostatic hypotension.dihydroergotamine
dihydroergotamine mesylateThe methanesulfonic acid salt of dihydroergotamine, a semisynthetic ergot alkaloid with weaker oxytocic and vasoconstrictor properties than ergotamine. Both the mesylate and the tartrate salts are used for the treatment of migraine and orthostatic hypotension.dihydroergotamine mesylate
eletriptanAn N-alkylpyrrolidine, that is N-methylpyrrolidine in which the pro-R hydrogen at position 2 is replaced by a {5-[2-(phenylsulfonyl)ethyl]-1H-indol-3-yl}methyl group.eletriptan
ergotamineA peptide ergot alkaloid that is dihydroergotamine in which a double bond replaces the single bond between positions 9 and 10.ergotamine
fenfluramineA secondary amino compound that is 1-phenyl-propan-2-amine in which one of the meta-hydrogens is substituted by trifluoromethyl, and one of the hydrogens attached to the nitrogen is substituted by an ethyl group. It binds to the serotonin reuptake pump, causing inhbition of serotonin uptake and release of serotonin. The resulting increased levels of serotonin lead to greater serotonin receptor activation which in turn lead to enhancement of serotoninergic transmission in the centres of feeding behavior located in the hypothalamus. This suppresses the appetite for carbohydrates. Fenfluramine was used as the hydrochloride for treatment of diabetes and obesity. It was withdrawn worldwide after reports of heart valve disease and pulmonary hypertension.fenfluramine
flibanserinAn N-alkylpiperazine that is 1-[2-(1,3-dihydro-2-oxobenzimidazol-1-yl)ethyl]piperazine in which the remaining amino proton is replaced by a 3-(trifluoromethyl)phenyl group. A multifunctional serotonin agonist and antagonist which is used for the treatment of pre-menopausal women with hypoactive sexual desire disorder.flibanserin
lisuridelisuride
lysergic acid diethylamideAn ergoline alkaloid arising from formal condensation of lysergic acid with diethylamine.lysergic acid diethylamide
n-methylquipazineAn aminoquinoline that consists of quinoline in which the hydrogen at position 2 is substituted by a 4-methylpiperazin-1-yl group. A 5-HT3 agonist. Has almost the same affinity for 5-HT3 sites as quipazine but unlike the latter, does not bind to 5-HT1B sites.N-methylquipazine
naratriptannaratriptan
psilocinA tryptamine alkaloid that is N,N-dimethyltryptamine carrying an additional hydroxy substituent at position 4. A hallucinogenic alkaloid isolated in trace amounts from Psilocybe mushrooms (also known as Teonanacatl or "magic mushrooms").psilocin
psilocybinA tryptamine alkaloid that is N,N-dimethyltryptamine carrying an additional phosphoryloxy substituent at position 4. The major hallucinogenic alkaloid isolated from Psilocybe mushrooms (also known as Teonanacatl or "magic mushrooms").psilocybin
rizatriptanrizatriptan
sumatriptanA sulfonamide that consists of N,N-dimethyltryptamine bearing an additional (N-methylsulfamoyl)methyl substituent at position 5. Selective agonist for a vascular 5-HT1 receptor subtype (probably a member of the 5-HT1D family). Used (in the form of its succinate salt) for the acute treatment of migraine with or without aura in adults.sumatriptan
tegaserodtegaserod
tegaserod maleatetegaserod maleate
tetrindoleA racemate composed of equimolar amounts of (R)- and (S)-tetrindole hydrochloride.tetrindole hydrochloride
vilazodoneA 1-benzofuran that is 5-(piperazin-1-yl}-1-benzofuran-2-carboxamide having a (5-cyanoindol-3-yl)butyl group attached at position N-4 on the piperazine ring. Used for the treatment of major depressive disorder.vilazodone
vilazodone hydrochlorideA hydrochloride obtained by reaction of vilazodone with one equivalent of hydrochloric acid. Used for the treatment of major depressive disorder.vilazodone hydrochloride
vortioxetineAn N-arylpiperazine in which the aryl group is specified as 2-[(2,4-dimethylphenyl)sulfanyl]phenyl. Used (as its hydrobromide salt) for treatment of major depressive disorder.vortioxetine
xaliprodenA tetrahydropyridine that is 1,2,3,6-tetrahydropyridine which is substituted on the nitrogen by a 2-(2-naphthyl)ethyl group and at position 4 by a m-trifluoromethylphenyl group.xaliproden
xanomelinexanomeline
zolmitriptanA member of the class of tryptamines that is N,N-dimethyltryptamine in which the hydrogen at position 5 of the indole ring has been replaced by a [(4S)-2-oxo-1,3-oxazolidin-4-yl]methyl group. A serotonin 5-HT1 B and D receptor agonist, it is used for the treatment of migraine.zolmitriptan

Research

Studies (22,967)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19908,611 (37.49)18.7374
1990's4,573 (19.91)18.2507
2000's4,263 (18.56)29.6817
2010's3,950 (17.20)24.3611
2020's1,570 (6.84)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials3,272 (12.10%)5.53%
Reviews3,066 (11.34%)6.00%
Case Studies2,269 (8.39%)4.05%
Observational65 (0.24%)0.25%
Other18,363 (67.92%)84.16%

Protein Targets (303)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
67.9K proteinVaccinia virusPotency14.433224
acetylcholinesteraseHomo sapiens (human)Potency36.9713316
activating transcription factor 6Homo sapiens (human)Potency26.832522
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency16.408718
Alpha-synucleinHomo sapiens (human)Potency35.481311
AR proteinHomo sapiens (human)Potency22.9284718
aryl hydrocarbon receptorHomo sapiens (human)Potency21.399723
arylsulfatase AHomo sapiens (human)Potency6.717813
ATAD5 protein, partialHomo sapiens (human)Potency36.610811
Ataxin-2Homo sapiens (human)Potency14.834425
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency3.380113
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency10.849713
Bloom syndrome protein isoform 1Homo sapiens (human)Potency56.234122
BRCA1Homo sapiens (human)Potency12.589311
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency70.794611
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency22.687412
caspase-3Cricetulus griseus (Chinese hamster)Potency33.491511
caspase-3Homo sapiens (human)Potency22.687412
Caspase-7Cricetulus griseus (Chinese hamster)Potency33.491511
Cellular tumor antigen p53Homo sapiens (human)Potency25.534725
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency22.106024
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency31.382414
Chain A, Beta-lactamaseEscherichia coli K-12Potency44.668411
Chain A, Ferritin light chainEquus caballus (horse)Potency25.118911
Chain A, HADH2 proteinHomo sapiens (human)Potency39.810712
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency51.647514
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency10.704015
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency11.193611
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency30.782815
Chain B, HADH2 proteinHomo sapiens (human)Potency39.810712
chromobox protein homolog 1Homo sapiens (human)Potency70.300829
cytochrome P450 2C19 precursorHomo sapiens (human)Potency12.719015
cytochrome P450 2C9 precursorHomo sapiens (human)Potency24.536715
cytochrome P450 2C9, partialHomo sapiens (human)Potency29.885216
cytochrome P450 2D6Homo sapiens (human)Potency7.9128113
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency21.479219
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency16.7428214
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency25.774219
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency5.392911
D(1A) dopamine receptorHomo sapiens (human)Potency5.142329
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency10.000011
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency64.467912
DNA polymerase kappa isoform 1Homo sapiens (human)Potency56.932213
dopamine D1 receptorHomo sapiens (human)Potency6.832713
endonuclease IVEscherichia coliPotency0.281811
estrogen nuclear receptor alphaHomo sapiens (human)Potency29.8972930
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency29.347736
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency27.5977929
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency24.3274112
EWS/FLI fusion proteinHomo sapiens (human)Potency5.6987410
farnesoid X nuclear receptorHomo sapiens (human)Potency30.389936
flap endonuclease 1Homo sapiens (human)Potency50.118711
Fumarate hydrataseHomo sapiens (human)Potency36.985014
GVesicular stomatitis virusPotency29.885216
GABA theta subunitRattus norvegicus (Norway rat)Potency16.742817
GALC proteinHomo sapiens (human)Potency4.466811
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency16.742817
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency16.742817
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency16.742817
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency16.742817
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency16.742817
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency16.742817
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency16.742817
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency16.742817
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency16.742817
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency16.742817
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency16.742817
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency16.742817
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency16.742817
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency16.742817
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency16.742817
gemininHomo sapiens (human)Potency14.831128
GLI family zinc finger 3Homo sapiens (human)Potency22.7551214
glp-1 receptor, partialHomo sapiens (human)Potency12.698823
GLS proteinHomo sapiens (human)Potency15.490327
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency14.783016
glucokinase regulatory proteinHomo sapiens (human)Potency4.466812
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency37.911314
Guanine nucleotide-binding protein GHomo sapiens (human)Potency7.943311
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency50.118711
heat shock protein beta-1Homo sapiens (human)Potency40.668526
hexokinase-4 isoform 1Homo sapiens (human)Potency4.466812
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency21.2455223
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency22.393814
Histone H2A.xCricetulus griseus (Chinese hamster)Potency76.172225
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency29.885216
huntingtin isoform 2Homo sapiens (human)Potency35.481311
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency25.173826
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency12.589322
IDH1Homo sapiens (human)Potency3.286012
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency29.8852112
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency7.943311
Integrin alpha-IIbHomo sapiens (human)Potency31.622811
Integrin beta-3Homo sapiens (human)Potency31.622811
Interferon betaHomo sapiens (human)Potency22.1487316
lamin isoform A-delta10Homo sapiens (human)Potency12.209712
lethal factor (plasmid)Bacillus anthracis str. A2012Potency13.815412
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency1.778322
M-phase phosphoprotein 8Homo sapiens (human)Potency44.668411
Microtubule-associated protein tauHomo sapiens (human)Potency13.828227
mitogen-activated protein kinase 1Homo sapiens (human)Potency15.890413
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency17.652828
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency1.778311
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency1.778311
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Potency1.778311
neuropeptide S receptor isoform AHomo sapiens (human)Potency12.589311
NFKB1 protein, partialHomo sapiens (human)Potency5.337326
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency0.316211
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency27.045829
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency23.519513
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency34.912124
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency14.339023
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency25.3262311
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency26.751814
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency80.303912
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency30.947926
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency19.914137
phosphopantetheinyl transferaseBacillus subtilisPotency40.860415
plasminogen precursorMus musculus (house mouse)Potency1.412511
polyproteinZika virusPotency36.985014
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency15.074414
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency13.481319
PPM1D proteinHomo sapiens (human)Potency17.117816
pregnane X nuclear receptorHomo sapiens (human)Potency24.5877211
progesterone receptorHomo sapiens (human)Potency19.102127
RAR-related orphan receptor gammaMus musculus (house mouse)Potency28.483026
regulator of G-protein signaling 4Homo sapiens (human)Potency17.096013
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency43.616239
retinoid X nuclear receptor alphaHomo sapiens (human)Potency30.193329
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency18.492711
SMAD family member 2Homo sapiens (human)Potency22.987536
SMAD family member 3Homo sapiens (human)Potency22.987536
Smad3Homo sapiens (human)Potency35.481311
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency31.539228
survival motor neuron protein isoform dHomo sapiens (human)Potency28.183812
TAR DNA-binding protein 43Homo sapiens (human)Potency3.162311
TDP1 proteinHomo sapiens (human)Potency22.1982233
thioredoxin reductaseRattus norvegicus (Norway rat)Potency4.228422
ThrombopoietinHomo sapiens (human)Potency9.670426
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency40.2009215
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency18.548222
thyroid stimulating hormone receptorHomo sapiens (human)Potency38.1153615
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency5.745712
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency10.000011
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency1.412511
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency1.412511
USP1 protein, partialHomo sapiens (human)Potency32.961614
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency22.3319211
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency42.641437
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency57.457012
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency37.911314

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
3-hydroxy-3-methylglutaryl-coenzyme A reductase Rattus norvegicus (Norway rat)Ki0.022011
5-hydroxytryptamine receptor 1AHomo sapiens (human)IC500.17521010
5-hydroxytryptamine receptor 1AMus musculus (house mouse)IC500.450011
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC500.3882917
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki0.06296375
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.19622340
5-hydroxytryptamine receptor 1BHomo sapiens (human)IC500.015479
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC502.6522814
5-hydroxytryptamine receptor 1BGorilla gorilla gorilla (western lowland gorilla)Ki0.006411
5-hydroxytryptamine receptor 1BHomo sapiens (human)Ki0.02391522
5-hydroxytryptamine receptor 1BOryctolagus cuniculus (rabbit)Ki0.001211
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki0.23891021
5-hydroxytryptamine receptor 1DHomo sapiens (human)IC500.24701013
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)IC501.687033
5-hydroxytryptamine receptor 1DSus scrofa (pig)IC500.059366
5-hydroxytryptamine receptor 1DHomo sapiens (human)Ki0.05562230
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Ki0.016734
5-hydroxytryptamine receptor 1EHomo sapiens (human)IC505.500011
5-hydroxytryptamine receptor 1EHomo sapiens (human)Ki6.697723
5-hydroxytryptamine receptor 1FHomo sapiens (human)IC501.000011
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)IC501.000011
5-hydroxytryptamine receptor 1FHomo sapiens (human)Ki0.025711
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)Ki0.016734
5-hydroxytryptamine receptor 2ABos taurus (cattle)IC5018.620922
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC503.2088710
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC504.0190910
5-hydroxytryptamine receptor 2ABos taurus (cattle)Ki0.178011
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.16304247
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.92642732
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC500.153325
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC502.061756
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.04211316
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki1.55441518
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC5015.36281316
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC501.921278
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.13882024
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki1.35552530
5-hydroxytryptamine receptor 3ACavia porcellus (domestic guinea pig)IC50630.000011
5-hydroxytryptamine receptor 3AHomo sapiens (human)IC503.483879
5-hydroxytryptamine receptor 3AMus musculus (house mouse)IC5010.000011
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)IC502.594644
5-hydroxytryptamine receptor 3AHomo sapiens (human)Ki2.0867813
5-hydroxytryptamine receptor 3AMus musculus (house mouse)Ki1.430011
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Ki0.580368
5-hydroxytryptamine receptor 3BHomo sapiens (human)IC503.049357
5-hydroxytryptamine receptor 3BMus musculus (house mouse)IC5010.000011
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)IC502.594644
5-hydroxytryptamine receptor 3BHomo sapiens (human)Ki0.487327
5-hydroxytryptamine receptor 3BMus musculus (house mouse)Ki1.430011
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)Ki0.580368
5-hydroxytryptamine receptor 3CHomo sapiens (human)IC503.049357
5-hydroxytryptamine receptor 3CHomo sapiens (human)Ki0.487327
5-hydroxytryptamine receptor 3DHomo sapiens (human)IC503.049357
5-hydroxytryptamine receptor 3DHomo sapiens (human)Ki0.487327
5-hydroxytryptamine receptor 3EHomo sapiens (human)IC503.049357
5-hydroxytryptamine receptor 3EHomo sapiens (human)Ki0.487327
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC500.055313
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki2.521524
5-hydroxytryptamine receptor 4Homo sapiens (human)Ki0.045677
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)IC500.252011
5-hydroxytryptamine receptor 5AHomo sapiens (human)IC500.501211
5-hydroxytryptamine receptor 5AHomo sapiens (human)Ki1.265868
5-hydroxytryptamine receptor 5AMus musculus (house mouse)Ki9.133323
5-hydroxytryptamine receptor 6Homo sapiens (human)IC500.005713
5-hydroxytryptamine receptor 6Rattus norvegicus (Norway rat)IC503.000011
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.33161519
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki0.31632125
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)IC503.000011
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki0.090845
AcetylcholinesteraseMus musculus (house mouse)IC5021.300011
AcetylcholinesteraseRattus norvegicus (Norway rat)IC5021.300022
Adenylate cyclase Arthrospira platensisIC5070.000011
Adenylate cyclase type 5Rattus norvegicus (Norway rat)IC500.046811
Advanced glycosylation end product-specific receptorHomo sapiens (human)IC50200.000011
Alpha-1A adrenergic receptorHomo sapiens (human)IC504.641467
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC506.311149
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.030633
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.171168
Alpha-1B adrenergic receptorHomo sapiens (human)IC501.980011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC506.311149
Alpha-1B adrenergic receptorHomo sapiens (human)Ki0.210023
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.192457
Alpha-1D adrenergic receptorHomo sapiens (human)IC500.635225
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC506.311149
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.128825
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.192457
Alpha-2A adrenergic receptorBos taurus (cattle)IC500.022322
Alpha-2A adrenergic receptorHomo sapiens (human)IC501.500924
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC507.750024
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.000413
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki5.011911
Alpha-2B adrenergic receptorHomo sapiens (human)IC501.502124
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC507.750024
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.001313
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki5.011911
Alpha-2C adrenergic receptorHomo sapiens (human)IC501.506624
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC507.750024
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.010524
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki5.011911
Angiotensin-converting enzyme Homo sapiens (human)IC500.024011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000015
ATP-dependent translocase ABCB1Homo sapiens (human)IC500.780011
ATP-dependent translocase ABCB1Homo sapiens (human)Ki308.272524
ATP-dependent translocase ABCB1Mus musculus (house mouse)Ki551.700024
bcl-2-related protein A1Mus musculus (house mouse)IC5020.000011
Beta-1 adrenergic receptorHomo sapiens (human)IC502.233723
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)IC501.000011
Beta-1 adrenergic receptorHomo sapiens (human)Ki0.951723
Beta-2 adrenergic receptorCanis lupus familiaris (dog)IC5018.000011
Beta-2 adrenergic receptorHomo sapiens (human)IC501.401012
Beta-2 adrenergic receptorRattus norvegicus (Norway rat)IC501.000011
Beta-2 adrenergic receptorHomo sapiens (human)Ki0.889023
Beta-3 adrenergic receptorRattus norvegicus (Norway rat)IC501.000011
Bile salt export pumpHomo sapiens (human)IC50118.1230510
Bile salt export pumpRattus norvegicus (Norway rat)IC50369.800011
C-C chemokine receptor type 6Homo sapiens (human)IC5023.400011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000015
Carboxypeptidase MHomo sapiens (human)IC500.020011
Caspase-3Homo sapiens (human)IC50100.000011
Catechol O-methyltransferaseRattus norvegicus (Norway rat)Ki0.002511
Cholecystokinin receptor type AHomo sapiens (human)Ki0.302011
Cytochrome P450 2C9 Homo sapiens (human)IC5050.000011
Cytochrome P450 2D6Homo sapiens (human)IC500.016011
Cytochrome P450 2J2Homo sapiens (human)IC5050.000011
Cytochrome P450 3A4Homo sapiens (human)IC507.574834
Cytochrome P450 3A4Homo sapiens (human)Ki0.574012
DBos taurus (cattle)IC50270.000012
DRattus norvegicus (Norway rat)IC500.120012
DMus musculus (house mouse)Ki0.590022
DRattus norvegicus (Norway rat)Ki0.990244
D(1A) dopamine receptorHomo sapiens (human)IC501.432013
D(1A) dopamine receptorHomo sapiens (human)Ki0.5305711
D(1B) dopamine receptorRattus norvegicus (Norway rat)IC500.120012
D(1B) dopamine receptorHomo sapiens (human)Ki1.180033
D(2) dopamine receptorBos taurus (cattle)IC504.000023
D(2) dopamine receptorHomo sapiens (human)IC500.046559
D(2) dopamine receptorRattus norvegicus (Norway rat)IC500.271367
D(2) dopamine receptorHomo sapiens (human)Ki0.24814954
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.334899
D(3) dopamine receptorHomo sapiens (human)IC500.013514
D(3) dopamine receptorRattus norvegicus (Norway rat)IC500.103723
D(3) dopamine receptorHomo sapiens (human)Ki0.00572327
D(4) dopamine receptorRattus norvegicus (Norway rat)IC501.213323
D(4) dopamine receptorHomo sapiens (human)Ki0.14981213
D(4) dopamine receptorRattus norvegicus (Norway rat)Ki0.510011
Fatty-acid amide hydrolase 1Rattus norvegicus (Norway rat)Ki0.026911
GABA theta subunitRattus norvegicus (Norway rat)Ki0.003212
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki0.003212
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki0.003212
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki0.003212
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki0.003212
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Ki0.003212
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Ki0.003212
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Ki0.003212
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Ki0.003212
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Ki0.003212
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Ki0.003212
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Ki0.003212
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Ki0.003212
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Ki0.003212
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Ki0.003212
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Ki0.003212
Gastrin/cholecystokinin type B receptorHomo sapiens (human)Ki0.302011
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Ki0.009011
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Ki0.009011
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Ki0.009011
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Ki0.009011
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Ki0.009011
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Ki0.009011
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Ki0.009011
Histamine H1 receptorHomo sapiens (human)IC500.355044
Histamine H1 receptorCavia porcellus (domestic guinea pig)Ki0.048911
Histamine H1 receptorHomo sapiens (human)Ki0.286566
Histamine H2 receptorHomo sapiens (human)IC501.040011
Histamine H2 receptorHomo sapiens (human)Ki1.022011
Histamine H3 receptorHomo sapiens (human)Ki1.385522
Histamine H4 receptorHomo sapiens (human)Ki6.918311
LacZ protein (plasmid)Escherichia coliIC5066.600011
Lysosomal alpha-glucosidaseBos taurus (cattle)IC500.030011
Mu-type opioid receptorCavia porcellus (domestic guinea pig)IC500.000311
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC5035.300014
Multidrug and toxin extrusion protein 2Homo sapiens (human)IC50186.200013
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000015
Muscarinic acetylcholine receptorCavia porcellus (domestic guinea pig)Ki0.158511
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC501.396766
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki0.68291010
Muscarinic acetylcholine receptor M1Mus musculus (house mouse)Ki0.158511
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC500.164422
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.54561313
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC50100.000011
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.044944
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC500.025122
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.040744
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki0.708288
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC502.919489
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki0.879333
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2Ki107.360011
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusKi107.360011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC500.316535
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.952023
Sodium-dependent dopamine transporterMacaca fascicularis (crab-eating macaque)Ki0.340011
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)Ki0.025012
Sodium-dependent dopamine transporter Homo sapiens (human)IC500.295011
Sodium-dependent dopamine transporter Homo sapiens (human)Ki0.340011
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC500.158111
Sodium-dependent serotonin transporterHomo sapiens (human)IC500.000433
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)IC500.005456
Sodium-dependent serotonin transporterHomo sapiens (human)Ki0.405099
Solute carrier family 22 member 2Homo sapiens (human)IC50100.300013
Thromboxane-A synthase Homo sapiens (human)IC503.064011
Transient receptor potential cation channel subfamily M member 8Homo sapiens (human)IC5012.000022
Tyrosine-protein kinase FynHomo sapiens (human)IC503.160011
Tyrosine-protein kinase LckHomo sapiens (human)IC506.499011
ubiquitin-conjugating enzyme E2 NHomo sapiens (human)IC5010.350022
Uracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)IC5030.000011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1AHomo sapiens (human)EC500.12661616
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)EC501.300011
5-hydroxytryptamine receptor 1AHomo sapiens (human)Kd0.127514
5-hydroxytryptamine receptor 1BHomo sapiens (human)EC506.028535
5-hydroxytryptamine receptor 1DHomo sapiens (human)EC500.0095710
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)EC500.097011
5-hydroxytryptamine receptor 1FHomo sapiens (human)EC500.035011
5-hydroxytryptamine receptor 2AHomo sapiens (human)EC500.28572325
5-hydroxytryptamine receptor 2AMus musculus (house mouse)EC502.804223
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)EC500.512345
5-hydroxytryptamine receptor 2BHomo sapiens (human)EC500.30211011
5-hydroxytryptamine receptor 2CHomo sapiens (human)EC500.07891213
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)EC500.001811
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)EC500.009422
5-hydroxytryptamine receptor 4Homo sapiens (human)EC500.004855
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)EC500.080011
Alpha-1A adrenergic receptorHomo sapiens (human)Kd0.028211
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Kd0.208911
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)EC500.080011
Alpha-1B adrenergic receptorHomo sapiens (human)Kd0.028211
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Kd0.208911
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)EC500.080011
Alpha-1D adrenergic receptorHomo sapiens (human)Kd0.028211
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Kd0.208911
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)EC500.378012
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Kd0.023423
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)EC500.378012
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Kd0.023423
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)EC500.378012
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Kd0.023423
Caspase-3Homo sapiens (human)EC5050.000022
D(2) dopamine receptorHomo sapiens (human)EC500.79382429
D(2) dopamine receptorRattus norvegicus (Norway rat)Kd0.000845
D(3) dopamine receptorHomo sapiens (human)EC500.019824
D(4) dopamine receptorHomo sapiens (human)EC500.088511
mu-type opioid receptor isoform MOR-1Homo sapiens (human)EC5092.469011
Muscarinic acetylcholine receptor M1Homo sapiens (human)EC501.70051616
Muscarinic acetylcholine receptor M1Mus musculus (house mouse)EC505.700011
Muscarinic acetylcholine receptor M2Homo sapiens (human)EC500.259522
Muscarinic acetylcholine receptor M3Homo sapiens (human)EC5013,270,233,341.746333
Muscarinic acetylcholine receptor M3Mus musculus (house mouse)EC5011.000011
Muscarinic acetylcholine receptor M4Homo sapiens (human)EC500.967377
Muscarinic acetylcholine receptor M5Homo sapiens (human)EC503.234377
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)EC500.108011
TransporterRattus norvegicus (Norway rat)EC500.000511
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)EC500.012011
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)EC500.012011
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)EC500.012011
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)EC500.012011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1DHomo sapiens (human)ED500.192512
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Efficacy0.051511
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)K0.50.006011
DNA repair protein RAD52 homolog isoform aHomo sapiens (human)AC5016.720011
PAX8Homo sapiens (human)AC5012.410011
Solute carrier family 22 member 1 Homo sapiens (human)Km55.000011