sb-649915 profile

SB-649915: potent 5-HT1A and 5-HT1B autoreceptor antagonist and 5-HT re-uptake inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	10296414
CHEMBL ID	183460
SCHEMBL ID	5364247
MeSH ID	M0500141

Synonym
6-[[1-[2-(2-methylquinolin-5-yl)oxyethyl]piperidin-4-yl]methyl]-4h-1,4-benzoxazin-3-one
sb 649915
gtpl76
L023338
sb-649915
CHEMBL183460 ,
bdbm50412114
SCHEMBL5364247
6-{1-[2-(2-methylquinolin-5-yloxy)ethyl]piperidin-4-ylmethyl}-4h-benzo[1,4]oxazin-3-one
6-(1-(2-(2-methylquinolin-5-yloxy)ethyl)piperidin-4-ylmethyl)-4h-benzo[1,4]oxazin-3-one
PJSUYRBCBFPCQW-UHFFFAOYSA-N ,
6-[(1-{2-[(2-methyl-5-quinolinyl)oxy]ethyl}-4-piperidinyl)methyl]-2h-1,4-benzoxazin-3(4h)-one
hd3uv2mfj8 ,
sb-649915-b
2h-1,4-benzoxazin-3(4h)-one, 6-((1-(2-((2-methyl-5-quinolinyl)oxy)ethyl)-4-piperidinyl)methyl)-
6-((1-(2-((2-methylquinolin-5-yl)oxy)ethyl)piperidin-4-yl)methyl)-2h-1,4-benzoxazin-3(4h)-one
420785-70-2
sb 649915b
unii-hd3uv2mfj8
6-[1-[2-((2-methylquinolin-5-yl)oxy)ethyl]piperidin-4-ylmethyl]-4h-benzo[1,4]oxazin-3-one
DTXSID701028478
6-(1-(2-((2-methylquinolin-5-yl)oxy)ethyl)piperidin-4-ylmethyl)-4h-benzo(1,4)oxazin-3-one
sb649915b
AKOS040749417

Excerpt	Reference	Relevance
" This compound also had good oral bioavailability and brain penetration in the rat."	( 3,4-Dihydro-2H-benzoxazinones are 5-HT(1A) receptor antagonists with potent 5-HT reuptake inhibitory activity. Atkinson, PJ; Bromidge, SM; Duxon, MS; Gaster, LM; Hadley, MS; Hammond, B; Johnson, CN; Middlemiss, DN; North, SE; Price, GW; Rami, HK; Riley, GJ; Scott, CM; Shaw, TE; Starr, KR; Stemp, G; Thewlis, KM; Thomas, DR; Thompson, M; Vong, AK; Watson, JM, 2005)	0.33

Protein Targets (14)

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Beta-2 adrenergic receptor	Homo sapiens (human)	Ki	0.5012	0.0000	0.6635	9.5499	AID254588
Beta-1 adrenergic receptor	Homo sapiens (human)	Ki	2.5119	0.0001	1.3391	9.9840	AID305574
5-hydroxytryptamine receptor 1A	Homo sapiens (human)	Ki	0.0015	0.0001	0.5326	10.0000	AID239973; AID239981; AID254592; AID305565; AID308950; AID308951; AID389417; AID408275; AID408276
D(2) dopamine receptor	Homo sapiens (human)	Ki	1.2589	0.0000	0.6518	10.0000	AID305575
5-hydroxytryptamine receptor 1D	Homo sapiens (human)	Ki	0.0016	0.0001	0.8087	10.0000	AID239979; AID305567; AID308955; AID389419; AID408278
5-hydroxytryptamine receptor 1B	Homo sapiens (human)	Ki	0.0100	0.0001	0.5485	9.2100	AID239978; AID305566; AID308953; AID389418; AID408277
5-hydroxytryptamine receptor 2A	Homo sapiens (human)	Ki	3.1623	0.0000	0.3855	10.0000	AID305569
5-hydroxytryptamine receptor 2C	Homo sapiens (human)	Ki	7.9433	0.0001	0.9549	10.0000	AID305571
Sodium-dependent serotonin transporter	Homo sapiens (human)	Ki	0.0063	0.0000	0.7048	8.1930	AID254586
Sodium-dependent serotonin transporter	Rattus norvegicus (Norway rat)	Ki	0.0035	0.0000	0.7056	10.0000	AID239952; AID305565; AID389417; AID408276
5-hydroxytryptamine receptor 7	Homo sapiens (human)	Ki	0.1995	0.0003	0.3806	10.0000	AID305573
D(3) dopamine receptor	Homo sapiens (human)	Ki	0.6310	0.0000	0.6020	10.0000	AID305576
5-hydroxytryptamine receptor 2B	Homo sapiens (human)	Ki	1.5849	0.0003	0.7693	10.0000	AID305570
5-hydroxytryptamine receptor 6	Homo sapiens (human)	Ki	10.0000	0.0002	0.5229	10.0000	AID305572
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (248)

Process	via Protein(s)	Taxonomy
diet induced thermogenesis	Beta-2 adrenergic receptor	Homo sapiens (human)
regulation of sodium ion transport	Beta-2 adrenergic receptor	Homo sapiens (human)
transcription by RNA polymerase II	Beta-2 adrenergic receptor	Homo sapiens (human)
receptor-mediated endocytosis	Beta-2 adrenergic receptor	Homo sapiens (human)
smooth muscle contraction	Beta-2 adrenergic receptor	Homo sapiens (human)
cell surface receptor signaling pathway	Beta-2 adrenergic receptor	Homo sapiens (human)
activation of transmembrane receptor protein tyrosine kinase activity	Beta-2 adrenergic receptor	Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	Beta-2 adrenergic receptor	Homo sapiens (human)
endosome to lysosome transport	Beta-2 adrenergic receptor	Homo sapiens (human)
response to cold	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of protein kinase A signaling	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of bone mineralization	Beta-2 adrenergic receptor	Homo sapiens (human)
heat generation	Beta-2 adrenergic receptor	Homo sapiens (human)
negative regulation of multicellular organism growth	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of MAPK cascade	Beta-2 adrenergic receptor	Homo sapiens (human)
bone resorption	Beta-2 adrenergic receptor	Homo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathway	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Beta-2 adrenergic receptor	Homo sapiens (human)
negative regulation of smooth muscle contraction	Beta-2 adrenergic receptor	Homo sapiens (human)
brown fat cell differentiation	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of mini excitatory postsynaptic potential	Beta-2 adrenergic receptor	Homo sapiens (human)
adrenergic receptor signaling pathway	Beta-2 adrenergic receptor	Homo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathway	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of protein serine/threonine kinase activity	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of cold-induced thermogenesis	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of autophagosome maturation	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of lipophagy	Beta-2 adrenergic receptor	Homo sapiens (human)
cellular response to amyloid-beta	Beta-2 adrenergic receptor	Homo sapiens (human)
response to psychosocial stress	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of cAMP-dependent protein kinase activity	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of AMPA receptor activity	Beta-2 adrenergic receptor	Homo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrine	Beta-1 adrenergic receptor	Homo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrine	Beta-1 adrenergic receptor	Homo sapiens (human)
diet induced thermogenesis	Beta-1 adrenergic receptor	Homo sapiens (human)
response to cold	Beta-1 adrenergic receptor	Homo sapiens (human)
heat generation	Beta-1 adrenergic receptor	Homo sapiens (human)
negative regulation of multicellular organism growth	Beta-1 adrenergic receptor	Homo sapiens (human)
fear response	Beta-1 adrenergic receptor	Homo sapiens (human)
regulation of circadian sleep/wake cycle, sleep	Beta-1 adrenergic receptor	Homo sapiens (human)
brown fat cell differentiation	Beta-1 adrenergic receptor	Homo sapiens (human)
regulation of postsynaptic membrane potential	Beta-1 adrenergic receptor	Homo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathway	Beta-1 adrenergic receptor	Homo sapiens (human)
positive regulation of cold-induced thermogenesis	Beta-1 adrenergic receptor	Homo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure	Beta-1 adrenergic receptor	Homo sapiens (human)
positive regulation of MAPK cascade	Beta-1 adrenergic receptor	Homo sapiens (human)
behavioral fear response	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
G protein-coupled receptor signaling pathway	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
serotonin receptor signaling pathway	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
gamma-aminobutyric acid signaling pathway	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
positive regulation of cell population proliferation	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
regulation of serotonin secretion	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
regulation of vasoconstriction	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
exploration behavior	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
regulation of dopamine metabolic process	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
serotonin metabolic process	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
regulation of hormone secretion	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
regulation of behavior	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
chemical synaptic transmission	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathway	D(2) dopamine receptor	Homo sapiens (human)
temperature homeostasis	D(2) dopamine receptor	Homo sapiens (human)
response to hypoxia	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of protein phosphorylation	D(2) dopamine receptor	Homo sapiens (human)
response to amphetamine	D(2) dopamine receptor	Homo sapiens (human)
nervous system process involved in regulation of systemic arterial blood pressure	D(2) dopamine receptor	Homo sapiens (human)
regulation of heart rate	D(2) dopamine receptor	Homo sapiens (human)
regulation of sodium ion transport	D(2) dopamine receptor	Homo sapiens (human)
G protein-coupled receptor internalization	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of neuroblast proliferation	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of receptor internalization	D(2) dopamine receptor	Homo sapiens (human)
autophagy	D(2) dopamine receptor	Homo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathway	D(2) dopamine receptor	Homo sapiens (human)
neuron-neuron synaptic transmission	D(2) dopamine receptor	Homo sapiens (human)
neuroblast proliferation	D(2) dopamine receptor	Homo sapiens (human)
axonogenesis	D(2) dopamine receptor	Homo sapiens (human)
synapse assembly	D(2) dopamine receptor	Homo sapiens (human)
sensory perception of smell	D(2) dopamine receptor	Homo sapiens (human)
long-term memory	D(2) dopamine receptor	Homo sapiens (human)
grooming behavior	D(2) dopamine receptor	Homo sapiens (human)
locomotory behavior	D(2) dopamine receptor	Homo sapiens (human)
adult walking behavior	D(2) dopamine receptor	Homo sapiens (human)
protein localization	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of cell population proliferation	D(2) dopamine receptor	Homo sapiens (human)
associative learning	D(2) dopamine receptor	Homo sapiens (human)
visual learning	D(2) dopamine receptor	Homo sapiens (human)
response to xenobiotic stimulus	D(2) dopamine receptor	Homo sapiens (human)
response to light stimulus	D(2) dopamine receptor	Homo sapiens (human)
response to toxic substance	D(2) dopamine receptor	Homo sapiens (human)
response to iron ion	D(2) dopamine receptor	Homo sapiens (human)
response to inactivity	D(2) dopamine receptor	Homo sapiens (human)
Wnt signaling pathway	D(2) dopamine receptor	Homo sapiens (human)
striatum development	D(2) dopamine receptor	Homo sapiens (human)
orbitofrontal cortex development	D(2) dopamine receptor	Homo sapiens (human)
cerebral cortex GABAergic interneuron migration	D(2) dopamine receptor	Homo sapiens (human)
adenohypophysis development	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of cell migration	D(2) dopamine receptor	Homo sapiens (human)
peristalsis	D(2) dopamine receptor	Homo sapiens (human)
auditory behavior	D(2) dopamine receptor	Homo sapiens (human)
regulation of synaptic transmission, GABAergic	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of cytokinesis	D(2) dopamine receptor	Homo sapiens (human)
circadian regulation of gene expression	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of dopamine secretion	D(2) dopamine receptor	Homo sapiens (human)
response to histamine	D(2) dopamine receptor	Homo sapiens (human)
response to nicotine	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of urine volume	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of renal sodium excretion	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of multicellular organism growth	D(2) dopamine receptor	Homo sapiens (human)
response to cocaine	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of circadian sleep/wake cycle, sleep	D(2) dopamine receptor	Homo sapiens (human)
dopamine metabolic process	D(2) dopamine receptor	Homo sapiens (human)
drinking behavior	D(2) dopamine receptor	Homo sapiens (human)
regulation of potassium ion transport	D(2) dopamine receptor	Homo sapiens (human)
response to morphine	D(2) dopamine receptor	Homo sapiens (human)
pigmentation	D(2) dopamine receptor	Homo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathway	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of blood pressure	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of innate immune response	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of insulin secretion	D(2) dopamine receptor	Homo sapiens (human)
acid secretion	D(2) dopamine receptor	Homo sapiens (human)
behavioral response to cocaine	D(2) dopamine receptor	Homo sapiens (human)
behavioral response to ethanol	D(2) dopamine receptor	Homo sapiens (human)
regulation of long-term neuronal synaptic plasticity	D(2) dopamine receptor	Homo sapiens (human)
response to axon injury	D(2) dopamine receptor	Homo sapiens (human)
branching morphogenesis of a nerve	D(2) dopamine receptor	Homo sapiens (human)
arachidonic acid secretion	D(2) dopamine receptor	Homo sapiens (human)
epithelial cell proliferation	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of epithelial cell proliferation	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of protein secretion	D(2) dopamine receptor	Homo sapiens (human)
release of sequestered calcium ion into cytosol	D(2) dopamine receptor	Homo sapiens (human)
dopamine uptake involved in synaptic transmission	D(2) dopamine receptor	Homo sapiens (human)
regulation of dopamine uptake involved in synaptic transmission	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmission	D(2) dopamine receptor	Homo sapiens (human)
regulation of synapse structural plasticity	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of synaptic transmission, glutamatergic	D(2) dopamine receptor	Homo sapiens (human)
excitatory postsynaptic potential	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of growth hormone secretion	D(2) dopamine receptor	Homo sapiens (human)
prepulse inhibition	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of dopamine receptor signaling pathway	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	D(2) dopamine receptor	Homo sapiens (human)
regulation of locomotion involved in locomotory behavior	D(2) dopamine receptor	Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmission	D(2) dopamine receptor	Homo sapiens (human)
presynaptic modulation of chemical synaptic transmission	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of cellular response to hypoxia	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of glial cell-derived neurotrophic factor production	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of long-term synaptic potentiation	D(2) dopamine receptor	Homo sapiens (human)
hyaloid vascular plexus regression	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of neuron migration	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of cytosolic calcium ion concentration	D(2) dopamine receptor	Homo sapiens (human)
regulation of dopamine secretion	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of adenylate cyclase activity	D(2) dopamine receptor	Homo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathway	D(2) dopamine receptor	Homo sapiens (human)
negative regulation of voltage-gated calcium channel activity	D(2) dopamine receptor	Homo sapiens (human)
positive regulation of MAPK cascade	D(2) dopamine receptor	Homo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathway	D(2) dopamine receptor	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	5-hydroxytryptamine receptor 1D	Homo sapiens (human)
intestine smooth muscle contraction	5-hydroxytryptamine receptor 1D	Homo sapiens (human)
regulation of locomotion	5-hydroxytryptamine receptor 1D	Homo sapiens (human)
vasoconstriction	5-hydroxytryptamine receptor 1D	Homo sapiens (human)
regulation of behavior	5-hydroxytryptamine receptor 1D	Homo sapiens (human)
chemical synaptic transmission	5-hydroxytryptamine receptor 1D	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	5-hydroxytryptamine receptor 1D	Homo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway	5-hydroxytryptamine receptor 1D	Homo sapiens (human)
G protein-coupled receptor internalization	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
negative regulation of gamma-aminobutyric acid secretion	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
regulation of dopamine secretion	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
negative regulation of serotonin secretion	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
negative regulation of synaptic transmission, GABAergic	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
response to cocaine	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
vasoconstriction	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
drinking behavior	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
response to ethanol	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
bone remodeling	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
regulation of behavior	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
response to mineralocorticoid	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
negative regulation of synaptic transmission, glutamatergic	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
cellular response to alkaloid	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
cellular response to xenobiotic stimulus	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
cellular response to temperature stimulus	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
presynaptic modulation of chemical synaptic transmission	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentration	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferation	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
regulation of synaptic vesicle exocytosis	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
chemical synaptic transmission	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
temperature homeostasis	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of cytokine production involved in immune response	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
glycolytic process	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
intracellular calcium ion homeostasis	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
activation of phospholipase C activity	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
memory	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of cell population proliferation	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
response to xenobiotic stimulus	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
regulation of dopamine secretion	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
artery smooth muscle contraction	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
urinary bladder smooth muscle contraction	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of heat generation	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
negative regulation of potassium ion transport	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of neuron apoptotic process	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
protein localization to cytoskeleton	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of fat cell differentiation	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of glycolytic process	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of vasoconstriction	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
symbiont entry into host cell	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
sensitization	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
behavioral response to cocaine	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of inflammatory response	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
release of sequestered calcium ion into cytosol	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
negative regulation of synaptic transmission, glutamatergic	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
presynaptic modulation of chemical synaptic transmission	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of execution phase of apoptosis	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of platelet aggregation	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of DNA biosynthetic process	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
chemical synaptic transmission	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
behavioral fear response	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
intracellular calcium ion homeostasis	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
locomotory behavior	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
feeding behavior	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
cGMP-mediated signaling	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
regulation of nervous system process	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
regulation of appetite	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
regulation of corticotropin-releasing hormone secretion	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
positive regulation of fat cell differentiation	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
positive regulation of calcium-mediated signaling	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
release of sequestered calcium ion into cytosol	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
chemical synaptic transmission	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
monoamine transport	Sodium-dependent serotonin transporter	Homo sapiens (human)
response to hypoxia	Sodium-dependent serotonin transporter	Homo sapiens (human)
neurotransmitter transport	Sodium-dependent serotonin transporter	Homo sapiens (human)
response to nutrient	Sodium-dependent serotonin transporter	Homo sapiens (human)
memory	Sodium-dependent serotonin transporter	Homo sapiens (human)
circadian rhythm	Sodium-dependent serotonin transporter	Homo sapiens (human)
response to xenobiotic stimulus	Sodium-dependent serotonin transporter	Homo sapiens (human)
response to toxic substance	Sodium-dependent serotonin transporter	Homo sapiens (human)
positive regulation of gene expression	Sodium-dependent serotonin transporter	Homo sapiens (human)
positive regulation of serotonin secretion	Sodium-dependent serotonin transporter	Homo sapiens (human)
negative regulation of cerebellar granule cell precursor proliferation	Sodium-dependent serotonin transporter	Homo sapiens (human)
negative regulation of synaptic transmission, dopaminergic	Sodium-dependent serotonin transporter	Homo sapiens (human)
response to estradiol	Sodium-dependent serotonin transporter	Homo sapiens (human)
social behavior	Sodium-dependent serotonin transporter	Homo sapiens (human)
vasoconstriction	Sodium-dependent serotonin transporter	Homo sapiens (human)
sperm ejaculation	Sodium-dependent serotonin transporter	Homo sapiens (human)
negative regulation of neuron differentiation	Sodium-dependent serotonin transporter	Homo sapiens (human)
positive regulation of cell cycle	Sodium-dependent serotonin transporter	Homo sapiens (human)
negative regulation of organ growth	Sodium-dependent serotonin transporter	Homo sapiens (human)
behavioral response to cocaine	Sodium-dependent serotonin transporter	Homo sapiens (human)
enteric nervous system development	Sodium-dependent serotonin transporter	Homo sapiens (human)
brain morphogenesis	Sodium-dependent serotonin transporter	Homo sapiens (human)
serotonin uptake	Sodium-dependent serotonin transporter	Homo sapiens (human)
membrane depolarization	Sodium-dependent serotonin transporter	Homo sapiens (human)
platelet aggregation	Sodium-dependent serotonin transporter	Homo sapiens (human)
cellular response to retinoic acid	Sodium-dependent serotonin transporter	Homo sapiens (human)
cellular response to cGMP	Sodium-dependent serotonin transporter	Homo sapiens (human)
regulation of thalamus size	Sodium-dependent serotonin transporter	Homo sapiens (human)
conditioned place preference	Sodium-dependent serotonin transporter	Homo sapiens (human)
sodium ion transmembrane transport	Sodium-dependent serotonin transporter	Homo sapiens (human)
amino acid transport	Sodium-dependent serotonin transporter	Homo sapiens (human)
smooth muscle contraction	5-hydroxytryptamine receptor 7	Homo sapiens (human)
circadian rhythm	5-hydroxytryptamine receptor 7	Homo sapiens (human)
blood circulation	5-hydroxytryptamine receptor 7	Homo sapiens (human)
vasoconstriction	5-hydroxytryptamine receptor 7	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	5-hydroxytryptamine receptor 7	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	5-hydroxytryptamine receptor 7	Homo sapiens (human)
chemical synaptic transmission	5-hydroxytryptamine receptor 7	Homo sapiens (human)
response to ethanol	D(3) dopamine receptor	Homo sapiens (human)
synaptic transmission, dopaminergic	D(3) dopamine receptor	Homo sapiens (human)
G protein-coupled receptor internalization	D(3) dopamine receptor	Homo sapiens (human)
intracellular calcium ion homeostasis	D(3) dopamine receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	D(3) dopamine receptor	Homo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathway	D(3) dopamine receptor	Homo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathway	D(3) dopamine receptor	Homo sapiens (human)
learning or memory	D(3) dopamine receptor	Homo sapiens (human)
learning	D(3) dopamine receptor	Homo sapiens (human)
locomotory behavior	D(3) dopamine receptor	Homo sapiens (human)
visual learning	D(3) dopamine receptor	Homo sapiens (human)
response to xenobiotic stimulus	D(3) dopamine receptor	Homo sapiens (human)
regulation of dopamine secretion	D(3) dopamine receptor	Homo sapiens (human)
positive regulation of cytokinesis	D(3) dopamine receptor	Homo sapiens (human)
circadian regulation of gene expression	D(3) dopamine receptor	Homo sapiens (human)
response to histamine	D(3) dopamine receptor	Homo sapiens (human)
social behavior	D(3) dopamine receptor	Homo sapiens (human)
response to cocaine	D(3) dopamine receptor	Homo sapiens (human)
dopamine metabolic process	D(3) dopamine receptor	Homo sapiens (human)
response to morphine	D(3) dopamine receptor	Homo sapiens (human)
negative regulation of blood pressure	D(3) dopamine receptor	Homo sapiens (human)
positive regulation of mitotic nuclear division	D(3) dopamine receptor	Homo sapiens (human)
acid secretion	D(3) dopamine receptor	Homo sapiens (human)
behavioral response to cocaine	D(3) dopamine receptor	Homo sapiens (human)
negative regulation of oligodendrocyte differentiation	D(3) dopamine receptor	Homo sapiens (human)
arachidonic acid secretion	D(3) dopamine receptor	Homo sapiens (human)
negative regulation of protein secretion	D(3) dopamine receptor	Homo sapiens (human)
musculoskeletal movement, spinal reflex action	D(3) dopamine receptor	Homo sapiens (human)
regulation of dopamine uptake involved in synaptic transmission	D(3) dopamine receptor	Homo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	D(3) dopamine receptor	Homo sapiens (human)
prepulse inhibition	D(3) dopamine receptor	Homo sapiens (human)
positive regulation of dopamine receptor signaling pathway	D(3) dopamine receptor	Homo sapiens (human)
negative regulation of adenylate cyclase activity	D(3) dopamine receptor	Homo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathway	D(3) dopamine receptor	Homo sapiens (human)
negative regulation of voltage-gated calcium channel activity	D(3) dopamine receptor	Homo sapiens (human)
regulation of potassium ion transport	D(3) dopamine receptor	Homo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathway	D(3) dopamine receptor	Homo sapiens (human)
positive regulation of MAPK cascade	D(3) dopamine receptor	Homo sapiens (human)
negative regulation of cytosolic calcium ion concentration	D(3) dopamine receptor	Homo sapiens (human)
negative regulation of synaptic transmission, glutamatergic	D(3) dopamine receptor	Homo sapiens (human)
neural crest cell migration	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of cytokine production	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of endothelial cell proliferation	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
G protein-coupled receptor internalization	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
heart morphogenesis	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
cardiac muscle hypertrophy	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
intracellular calcium ion homeostasis	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
G protein-coupled receptor signaling pathway	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
activation of phospholipase C activity	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of cell population proliferation	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
response to xenobiotic stimulus	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
neural crest cell differentiation	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
intestine smooth muscle contraction	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
phosphorylation	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
calcium-mediated signaling	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
cGMP-mediated signaling	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
vasoconstriction	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
negative regulation of apoptotic process	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of MAP kinase activity	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
embryonic morphogenesis	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
regulation of behavior	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of nitric-oxide synthase activity	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
release of sequestered calcium ion into cytosol	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of cell division	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
ERK1 and ERK2 cascade	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
protein kinase C signaling	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
cellular response to temperature stimulus	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
chemical synaptic transmission	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
cerebral cortex cell migration	5-hydroxytryptamine receptor 6	Homo sapiens (human)
positive regulation of TOR signaling	5-hydroxytryptamine receptor 6	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	5-hydroxytryptamine receptor 6	Homo sapiens (human)
chemical synaptic transmission	5-hydroxytryptamine receptor 6	Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	5-hydroxytryptamine receptor 6	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	5-hydroxytryptamine receptor 6	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (44)

Process	via Protein(s)	Taxonomy
amyloid-beta binding	Beta-2 adrenergic receptor	Homo sapiens (human)
beta2-adrenergic receptor activity	Beta-2 adrenergic receptor	Homo sapiens (human)
protein binding	Beta-2 adrenergic receptor	Homo sapiens (human)
adenylate cyclase binding	Beta-2 adrenergic receptor	Homo sapiens (human)
potassium channel regulator activity	Beta-2 adrenergic receptor	Homo sapiens (human)
identical protein binding	Beta-2 adrenergic receptor	Homo sapiens (human)
protein homodimerization activity	Beta-2 adrenergic receptor	Homo sapiens (human)
protein-containing complex binding	Beta-2 adrenergic receptor	Homo sapiens (human)
norepinephrine binding	Beta-2 adrenergic receptor	Homo sapiens (human)
beta-adrenergic receptor activity	Beta-1 adrenergic receptor	Homo sapiens (human)
beta1-adrenergic receptor activity	Beta-1 adrenergic receptor	Homo sapiens (human)
protein binding	Beta-1 adrenergic receptor	Homo sapiens (human)
PDZ domain binding	Beta-1 adrenergic receptor	Homo sapiens (human)
alpha-2A adrenergic receptor binding	Beta-1 adrenergic receptor	Homo sapiens (human)
protein heterodimerization activity	Beta-1 adrenergic receptor	Homo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic membrane potential	Beta-1 adrenergic receptor	Homo sapiens (human)
G protein-coupled serotonin receptor activity	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
protein binding	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
receptor-receptor interaction	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
neurotransmitter receptor activity	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
serotonin binding	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/Go	D(2) dopamine receptor	Homo sapiens (human)
G-protein alpha-subunit binding	D(2) dopamine receptor	Homo sapiens (human)
protein binding	D(2) dopamine receptor	Homo sapiens (human)
heterotrimeric G-protein binding	D(2) dopamine receptor	Homo sapiens (human)
dopamine binding	D(2) dopamine receptor	Homo sapiens (human)
ionotropic glutamate receptor binding	D(2) dopamine receptor	Homo sapiens (human)
identical protein binding	D(2) dopamine receptor	Homo sapiens (human)
heterocyclic compound binding	D(2) dopamine receptor	Homo sapiens (human)
G protein-coupled receptor activity	D(2) dopamine receptor	Homo sapiens (human)
G protein-coupled serotonin receptor activity	5-hydroxytryptamine receptor 1D	Homo sapiens (human)
neurotransmitter receptor activity	5-hydroxytryptamine receptor 1D	Homo sapiens (human)
G protein-coupled serotonin receptor activity	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
protein binding	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
serotonin binding	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
voltage-gated calcium channel activity involved in regulation of presynaptic cytosolic calcium levels	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
neurotransmitter receptor activity	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
Gq/11-coupled serotonin receptor activity	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
virus receptor activity	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
G protein-coupled serotonin receptor activity	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
protein binding	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
protein tyrosine kinase activator activity	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
identical protein binding	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
protein-containing complex binding	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
serotonin binding	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
neurotransmitter receptor activity	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
Gq/11-coupled serotonin receptor activity	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
G protein-coupled serotonin receptor activity	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
protein binding	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
identical protein binding	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
serotonin binding	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
neurotransmitter receptor activity	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
integrin binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
monoatomic cation channel activity	Sodium-dependent serotonin transporter	Homo sapiens (human)
neurotransmitter transmembrane transporter activity	Sodium-dependent serotonin transporter	Homo sapiens (human)
serotonin:sodium:chloride symporter activity	Sodium-dependent serotonin transporter	Homo sapiens (human)
protein binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
monoamine transmembrane transporter activity	Sodium-dependent serotonin transporter	Homo sapiens (human)
antiporter activity	Sodium-dependent serotonin transporter	Homo sapiens (human)
syntaxin-1 binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
cocaine binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
sodium ion binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
identical protein binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
nitric-oxide synthase binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
actin filament binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
serotonin binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
protein binding	5-hydroxytryptamine receptor 7	Homo sapiens (human)
G protein-coupled serotonin receptor activity	5-hydroxytryptamine receptor 7	Homo sapiens (human)
neurotransmitter receptor activity	5-hydroxytryptamine receptor 7	Homo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/Go	D(3) dopamine receptor	Homo sapiens (human)
protein binding	D(3) dopamine receptor	Homo sapiens (human)
G protein-coupled receptor activity	D(3) dopamine receptor	Homo sapiens (human)
Gq/11-coupled serotonin receptor activity	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
G-protein alpha-subunit binding	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
G protein-coupled serotonin receptor activity	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
GTPase activator activity	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
protein binding	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
serotonin binding	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
neurotransmitter receptor activity	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
histamine receptor activity	5-hydroxytryptamine receptor 6	Homo sapiens (human)
protein binding	5-hydroxytryptamine receptor 6	Homo sapiens (human)
neurotransmitter receptor activity	5-hydroxytryptamine receptor 6	Homo sapiens (human)
G protein-coupled serotonin receptor activity	5-hydroxytryptamine receptor 6	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (51)

Process	via Protein(s)	Taxonomy
nucleus	Beta-2 adrenergic receptor	Homo sapiens (human)
lysosome	Beta-2 adrenergic receptor	Homo sapiens (human)
endosome	Beta-2 adrenergic receptor	Homo sapiens (human)
early endosome	Beta-2 adrenergic receptor	Homo sapiens (human)
Golgi apparatus	Beta-2 adrenergic receptor	Homo sapiens (human)
plasma membrane	Beta-2 adrenergic receptor	Homo sapiens (human)
endosome membrane	Beta-2 adrenergic receptor	Homo sapiens (human)
membrane	Beta-2 adrenergic receptor	Homo sapiens (human)
apical plasma membrane	Beta-2 adrenergic receptor	Homo sapiens (human)
clathrin-coated endocytic vesicle membrane	Beta-2 adrenergic receptor	Homo sapiens (human)
neuronal dense core vesicle	Beta-2 adrenergic receptor	Homo sapiens (human)
receptor complex	Beta-2 adrenergic receptor	Homo sapiens (human)
plasma membrane	Beta-2 adrenergic receptor	Homo sapiens (human)
early endosome	Beta-1 adrenergic receptor	Homo sapiens (human)
plasma membrane	Beta-1 adrenergic receptor	Homo sapiens (human)
Schaffer collateral - CA1 synapse	Beta-1 adrenergic receptor	Homo sapiens (human)
neuronal dense core vesicle	Beta-1 adrenergic receptor	Homo sapiens (human)
plasma membrane	Beta-1 adrenergic receptor	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
synapse	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
dendrite	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
Golgi membrane	D(2) dopamine receptor	Homo sapiens (human)
acrosomal vesicle	D(2) dopamine receptor	Homo sapiens (human)
plasma membrane	D(2) dopamine receptor	Homo sapiens (human)
cilium	D(2) dopamine receptor	Homo sapiens (human)
lateral plasma membrane	D(2) dopamine receptor	Homo sapiens (human)
endocytic vesicle	D(2) dopamine receptor	Homo sapiens (human)
axon	D(2) dopamine receptor	Homo sapiens (human)
dendrite	D(2) dopamine receptor	Homo sapiens (human)
synaptic vesicle membrane	D(2) dopamine receptor	Homo sapiens (human)
sperm flagellum	D(2) dopamine receptor	Homo sapiens (human)
dendritic spine	D(2) dopamine receptor	Homo sapiens (human)
perikaryon	D(2) dopamine receptor	Homo sapiens (human)
axon terminus	D(2) dopamine receptor	Homo sapiens (human)
postsynaptic membrane	D(2) dopamine receptor	Homo sapiens (human)
ciliary membrane	D(2) dopamine receptor	Homo sapiens (human)
non-motile cilium	D(2) dopamine receptor	Homo sapiens (human)
dopaminergic synapse	D(2) dopamine receptor	Homo sapiens (human)
GABA-ergic synapse	D(2) dopamine receptor	Homo sapiens (human)
G protein-coupled receptor complex	D(2) dopamine receptor	Homo sapiens (human)
glutamatergic synapse	D(2) dopamine receptor	Homo sapiens (human)
presynaptic membrane	D(2) dopamine receptor	Homo sapiens (human)
plasma membrane	D(2) dopamine receptor	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 1D	Homo sapiens (human)
synapse	5-hydroxytryptamine receptor 1D	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 1D	Homo sapiens (human)
dendrite	5-hydroxytryptamine receptor 1D	Homo sapiens (human)
endoplasmic reticulum	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
presynaptic membrane	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
calyx of Held	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
serotonergic synapse	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
G protein-coupled serotonin receptor complex	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
dendrite	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 1B	Homo sapiens (human)
neurofilament	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
caveola	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
axon	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
cytoplasmic vesicle	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
presynaptic membrane	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
neuronal cell body	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
dendritic shaft	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
postsynaptic membrane	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
cell body fiber	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
glutamatergic synapse	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
G protein-coupled serotonin receptor complex	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
dendrite	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
synapse	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
G protein-coupled serotonin receptor complex	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
dendrite	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
plasma membrane	Sodium-dependent serotonin transporter	Homo sapiens (human)
focal adhesion	Sodium-dependent serotonin transporter	Homo sapiens (human)
endosome membrane	Sodium-dependent serotonin transporter	Homo sapiens (human)
endomembrane system	Sodium-dependent serotonin transporter	Homo sapiens (human)
presynaptic membrane	Sodium-dependent serotonin transporter	Homo sapiens (human)
membrane raft	Sodium-dependent serotonin transporter	Homo sapiens (human)
synapse	Sodium-dependent serotonin transporter	Homo sapiens (human)
postsynaptic membrane	Sodium-dependent serotonin transporter	Homo sapiens (human)
serotonergic synapse	Sodium-dependent serotonin transporter	Homo sapiens (human)
synapse	Sodium-dependent serotonin transporter	Homo sapiens (human)
plasma membrane	Sodium-dependent serotonin transporter	Homo sapiens (human)
neuron projection	Sodium-dependent serotonin transporter	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 7	Homo sapiens (human)
trans-Golgi network membrane	5-hydroxytryptamine receptor 7	Homo sapiens (human)
synapse	5-hydroxytryptamine receptor 7	Homo sapiens (human)
dendrite	5-hydroxytryptamine receptor 7	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 7	Homo sapiens (human)
plasma membrane	D(3) dopamine receptor	Homo sapiens (human)
synapse	D(3) dopamine receptor	Homo sapiens (human)
plasma membrane	D(3) dopamine receptor	Homo sapiens (human)
nucleoplasm	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
cytoplasm	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
synapse	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
G protein-coupled serotonin receptor complex	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
dendrite	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 6	Homo sapiens (human)
cilium	5-hydroxytryptamine receptor 6	Homo sapiens (human)
synapse	5-hydroxytryptamine receptor 6	Homo sapiens (human)
dendrite	5-hydroxytryptamine receptor 6	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 6	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (59)

Assay ID	Title	Year	Journal	Article
AID305578	Oral bioavailability in rat at 3 mg/kg, po	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.
AID308967	Half life in rat at 1 mg/kg, iv	2007	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18	Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.
AID389417	Displacement of [3H]5HT from human cloned 5HT1A receptor expressed in CHO cells	2008	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20	Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity.
AID308955	Displacement of [3H]5-HT from human recombinant 5HT1D receptor expressed in CHO cells	2007	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18	Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.
AID239952	Mean negative logarithim of binding affinity was measured for the rat serotonin transporter; n>/=3	2005	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3	3,4-Dihydro-2H-benzoxazinones are 5-HT(1A) receptor antagonists with potent 5-HT reuptake inhibitory activity.
AID389421	Intrinsic activity at human cloned 5HT1A receptor expressed in CHO cells	2008	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20	Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity.
AID389420	Inhibition of [3H]5HT reuptake at SERT in rat cortical synaptosomes	2008	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20	Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity.
AID308968	Oral bioavailability in rat at 3 mg/kg	2007	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18	Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.
AID238015	Mean intrinsic activity was measured for the human 5-hydroxytryptamine 1A receptor; n=3	2005	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3	3,4-Dihydro-2H-benzoxazinones are 5-HT(1A) receptor antagonists with potent 5-HT reuptake inhibitory activity.
AID239978	Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells	2005	Journal of medicinal chemistry, May-19, Volume: 48, Issue:10	Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.
AID254592	Negative logarithm causing 50% receptor occupancy against 5-hydroxytryptamine 1A receptor	2005	Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21	Designed multiple ligands. An emerging drug discovery paradigm.
AID244207	Selectivity for human 5-hydroxytryptamine 1D receptor over 5-hydroxytryptamine 1B receptor	2005	Journal of medicinal chemistry, May-19, Volume: 48, Issue:10	Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.
AID308950	Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHO cells	2007	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18	Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.
AID305569	Displacement of [3H]ketanserin from human cloned 5HT2A receptor expressed in HEK293 cells	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.
AID408279	Inhibition of [3H]5HT uptake at SERT in rat cortical synaptosomes	2008	Journal of medicinal chemistry, May-22, Volume: 51, Issue:10	Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.
AID308966	Volume of distribution at steady state in rat at 1 mg/kg, iv	2007	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18	Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.
AID308969	Ratio of drug level in brain to blood in rat at 3 mg/kg, po	2007	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18	Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.
AID305575	Displacement of [125I]iodosulpiride from human cloned D2 receptor expressed in CHO cells	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.
AID254586	Negative logarithm causing 50% receptor occupancy against serotonin transporter	2005	Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21	Designed multiple ligands. An emerging drug discovery paradigm.
AID308956	Intrinsic activity at human recombinant 5HT1D receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay relative to 5-hydroxytryptamine	2007	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18	Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.
AID308957	Inhibition of [3H]5-HT uptake at SERT in rat cortical synaptosomes	2007	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18	Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.
AID239968	Inhibition of [3H]5-HT binding to serotonin transporter in rat cortical synaptosomes	2005	Journal of medicinal chemistry, May-19, Volume: 48, Issue:10	Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.
AID408277	Displacement of [3H]5HT from human recombinant 5HT1B receptor	2008	Journal of medicinal chemistry, May-22, Volume: 51, Issue:10	Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.
AID305565	Displacement of [3H]WAY-100635 from human cloned 5HT1A receptor expressed in CHO cells	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.
AID305568	Inhibition of [3H]5-HT uptake at SERT in rat cortical synaptosomes	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.
AID305566	Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.
AID389418	Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells	2008	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20	Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity.
AID305571	Displacement of [3H]mesulergine from human cloned 5HT2C receptor expressed in HEK293 cells	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.
AID308964	Metabolic stability assessed as intrinsic clearance in human liver microsomes	2007	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18	Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.
AID389422	Intrinsic activity at human cloned 5HT1B receptor expressed in CHO cells	2008	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20	Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity.
AID408280	Intrinsic activity at human recombinant 5HT1A receptor expressed in HEK293 cells by [35S]GTPgammaS binding relative to 5 hydroxytryptamine	2008	Journal of medicinal chemistry, May-22, Volume: 51, Issue:10	Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.
AID389419	Displacement of [3H]5HT from human cloned 5HT1D receptor expressed in CHO cells	2008	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20	Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity.
AID305577	Blood clearance in rat at 3 mg/kg, po	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.
AID305574	Binding affinity at adrenergic beta 1 receptor	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.
AID408276	Displacement of [3H]WAY100635 from human recombinant 5HT1A receptor	2008	Journal of medicinal chemistry, May-22, Volume: 51, Issue:10	Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.
AID308953	Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells	2007	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18	Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.
AID308963	Metabolic stability assessed as intrinsic clearance in rat liver microsomes	2007	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18	Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.
AID239979	Displacement of [3H]5-HT from human 5-hydroxytryptamine 1D receptor expressed in CHO cells	2005	Journal of medicinal chemistry, May-19, Volume: 48, Issue:10	Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.
AID305579	Ratio of drug level in brain to blood in human	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.
AID308954	Intrinsic activity at human recombinant 5HT1B receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay relative to 5-hydroxytryptamine	2007	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18	Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.
AID305572	Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.
AID308952	Intrinsic activity at human recombinant 5HT1A receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay relative to 5-hydroxytryptamine	2007	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18	Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.
AID389423	Intrinsic activity at human cloned 5HT1D receptor expressed in CHO cells	2008	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20	Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity.
AID305567	Displacement of [3H]5-HT from human cloned 5HT1D receptor expressed in CHO cells	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.
AID305573	Displacement of [3H]5CT from human cloned 5HT7a receptor expressed in HEK293 cells	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.
AID308951	Displacement of [3H]WAY 100635 from human recombinant 5HT1A receptor expressed in CHO cells	2007	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18	Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.
AID408275	Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor	2008	Journal of medicinal chemistry, May-22, Volume: 51, Issue:10	Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.
AID408278	Displacement of [3H]5HT from human recombinant 5HT1D receptor	2008	Journal of medicinal chemistry, May-22, Volume: 51, Issue:10	Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.
AID239973	Mean negative logarithim of binding affinity was measured for the human 5-hydroxytryptamine 1A receptor; n>/=3	2005	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3	3,4-Dihydro-2H-benzoxazinones are 5-HT(1A) receptor antagonists with potent 5-HT reuptake inhibitory activity.
AID305576	Displacement of [125I]iodosulpiride from human cloned D3 receptor expressed in CHO cells	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.
AID308965	Clearance in rat blood at 1 mg/kg, iv	2007	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18	Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.
AID305570	Displacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cells	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.
AID254588	Negative logarithm causing 50% receptor occupancy against beta-2 adrenergic receptor	2005	Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21	Designed multiple ligands. An emerging drug discovery paradigm.
AID239981	Displacement of [3H]WAY-100635 from human 5-hydroxytryptamine 1A receptor expressed in CHO cells	2005	Journal of medicinal chemistry, May-19, Volume: 48, Issue:10	Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.
AID624231	Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1D	2005	Journal of medicinal chemistry, May-19, Volume: 48, Issue:10	Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.
AID1346264	Human 5-HT1B receptor (5-Hydroxytryptamine receptors)	2005	Journal of medicinal chemistry, May-19, Volume: 48, Issue:10	Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.
AID624215	Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1A	2005	Journal of medicinal chemistry, May-19, Volume: 48, Issue:10	Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.
AID1345615	Human 5-HT1A receptor (5-Hydroxytryptamine receptors)	2005	Journal of medicinal chemistry, May-19, Volume: 48, Issue:10	Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.
AID1346528	Human 5-HT1D receptor (5-Hydroxytryptamine receptors)	2005	Journal of medicinal chemistry, May-19, Volume: 48, Issue:10	Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	11 (100.00)	29.6817
2010's	0 (0.00)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	2 (18.18%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	9 (81.82%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
8-hydroxy-2-(di-n-propylamino)tetralin 8-Hydroxy-2-(di-n-propylamino)tetralin: A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.. 8-OH-DPAT : A tetralin substituted at positions 1 and 7 by hydroxy and dipropylamino groups respectively	2.04	1	phenols; tertiary amino compound; tetralins	serotonergic antagonist
1-(1-naphthyl)piperazine 1-(1-naphthyl)piperazine: serotonin agonist; structure given in first source	3.12	1	N-arylpiperazine
celecoxib [no description available]	3.12	1	organofluorine compound; pyrazoles; sulfonamide; toluenes	cyclooxygenase 2 inhibitor; geroprotector; non-narcotic analgesic; non-steroidal anti-inflammatory drug
cetirizine Cetirizine: A potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects.. cetirizine : A member of the class of piperazines that is piperazine in which the hydrogens attached to nitrogen are replaced by a (4-chlorophenyl)(phenyl)methyl and a 2-(carboxymethoxy)ethyl group respectively.	3.12	1	ether; monocarboxylic acid; monochlorobenzenes; piperazines	anti-allergic agent; environmental contaminant; H1-receptor antagonist; xenobiotic
cyproheptadine Cyproheptadine: A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc.. cyproheptadine : The product resulting from the formal oxidative coupling of position 5 of 5H-dibenzo[a,d]cycloheptene with position 4 of 1-methylpiperidine resulting in the formation of a double bond between the two fragments. It is a sedating antihistamine with antimuscarinic and calcium-channel blocking actions. It is used (particularly as the hydrochloride sesquihydrate) for the relief of allergic conditions including rhinitis, conjunctivitis due to inhalant allergens and foods, urticaria and angioedema, and in pruritic skin disorders. Unlike other antihistamines, it is also a seratonin receptor antagonist, making it useful in conditions such as vascular headache and anorexia.	3.12	1	piperidines; tertiary amine	anti-allergic agent; antipruritic drug; gastrointestinal drug; H1-receptor antagonist; serotonergic antagonist
fentanyl Fentanyl: A potent narcotic analgesic, abuse of which leads to habituation or addiction. It is primarily a mu-opioid agonist. Fentanyl is also used as an adjunct to general anesthetics, and as an anesthetic for induction and maintenance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1078). fentanyl : A monocarboxylic acid amide resulting from the formal condensation of the aryl amino group of N-phenyl-1-(2-phenylethyl)piperidin-4-amine with propanoic acid.	3.12	1	anilide; monocarboxylic acid amide; piperidines	adjuvant; anaesthesia adjuvant; anaesthetic; intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic
fluoxetine Fluoxetine: The first highly specific serotonin uptake inhibitor. It is used as an antidepressant and often has a more acceptable side-effects profile than traditional antidepressants.. fluoxetine : A racemate comprising equimolar amounts of (R)- and (S)-fluoxetine. A selective serotonin reuptake inhibitor (SSRI), it is used (generally as the hydrochloride salt) for the treatment of depression (and the depressive phase of bipolar disorder), bullimia nervosa, and obsessive-compulsive disorder.. N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine : An aromatic ether consisting of 4-trifluoromethylphenol in which the hydrogen of the phenolic hydroxy group is replaced by a 3-(methylamino)-1-phenylpropyl group.	3.12	1	(trifluoromethyl)benzenes; aromatic ether; secondary amino compound
avapro Irbesartan: A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease.. irbesartan : A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.	3.12	1	azaspiro compound; biphenylyltetrazole	angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic
loratadine Loratadine: A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.. loratadine : A benzocycloheptapyridine that is 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine substituted by a chloro group at position 8 and a 1-(ethoxycarbonyl)piperidin-4-ylidene group at position 11. It is a H1-receptor antagonist commonly employed in the treatment of allergic disorders.	3.12	1	benzocycloheptapyridine; ethyl ester; N-acylpiperidine; organochlorine compound; tertiary carboxamide	anti-allergic agent; cholinergic antagonist; geroprotector; H1-receptor antagonist
pindolol Pindolol: A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638). pindolol : A member of the class of indols which is the 2-hydroxy-3-(isopropylamino)propyl ether derivative of 1H-indol-4-ol.	3.12	1	indoles; secondary amine	antiglaucoma drug; antihypertensive agent; beta-adrenergic antagonist; serotonergic antagonist; vasodilator agent
roxatidine acetate roxatidine acetate: structure given in first source	3.12	1	piperidines
imatinib [no description available]	3.12	1	aromatic amine; benzamides; N-methylpiperazine; pyridines; pyrimidines	antineoplastic agent; apoptosis inducer; tyrosine kinase inhibitor
n-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-n-(2-pyridinyl)cyclohexanecarboxamide [no description available]	2.04	1	piperazines
paroxetine Paroxetine: A serotonin uptake inhibitor that is effective in the treatment of depression.. paroxetine : A benzodioxole that consists of piperidine bearing 1,3-benzodioxol-5-yloxy)methyl and 4-fluorophenyl substituents at positions 3 and 4 respectively; the (3S,4R)-diastereomer. Highly potent and selective 5-HT uptake inhibitor that binds with high affinity to the serotonin transporter (Ki = 0.05 nM). Ki values are 1.1, 350 and 1100 nM for inhibition of [3H]-5-HT, [3H]-l-NA and [3H]-DA uptake respectively. Displays minimal affinity for alpha1-, alpha2- or beta-adrenoceptors, 5-HT2A, 5-HT1A, D2 or H1 receptors at concentrations below 1000 nM, however displays weak affinity for muscarinic ACh receptors (Ki = 42 nM). Antidepressant and anxiolytic in vivo.	2.03	1	aromatic ether; benzodioxoles; organofluorine compound; piperidines	antidepressant; anxiolytic drug; hepatotoxic agent; P450 inhibitor; serotonin uptake inhibitor
captopril Captopril: A potent and specific inhibitor of PEPTIDYL-DIPEPTIDASE A. It blocks the conversion of ANGIOTENSIN I to ANGIOTENSIN II, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the RENIN-ANGIOTENSIN SYSTEM and inhibits pressure responses to exogenous angiotensin.. captopril : A L-proline derivative in which L-proline is substituted on nitrogen with a (2S)-2-methyl-3-sulfanylpropanoyl group. It is used as an anti-hypertensive ACE inhibitor drug.	3.12	1	alkanethiol; L-proline derivative; N-acylpyrrolidine; pyrrolidinemonocarboxylic acid	antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
sulotroban sulotroban: thromboxane receptor antagonist	3.12	1
sch 37370 N-acetyldesloratadine: dual antagonist of platelet-activating factor and histamine	3.12	1
duloxetine [no description available]	3.12	1	duloxetine
ziprasidone ziprasidone: a benzisothiazoylpiperazine derivative; has combined dopamine and serotonin receptor antagonist activity; structurally related to tiospirone. ziprasidone : A piperazine compound having 1,2-benzothiazol-3-yl- and 2-(6-chloro-1,3-dihydro-2-oxindol-5-yl)ethyl substituents attached to the nitrogen atoms.	3.12	1	1,2-benzisothiazole; indolones; organochlorine compound; piperazines	antipsychotic agent; dopaminergic antagonist; histamine antagonist; muscarinic antagonist; psychotropic drug; serotonergic antagonist
prifelone prifelone: structure given in first source	3.12	1	aromatic ketone
gr 127935 GR 127935: a 5-HT 1D receptor antagonist. GR 127935 : A member of the class of benzamides obtained by formal condensation of the carboxy group of 2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-carboxylic acid and the anilino group of 4-methoxy-3-(4-methylpiperazin-1-yl)aniline. Potent and selective 5-HT1B/1D receptor antagonist (pKi values are 8.5 for both guinea pig 5-HT1D and rat 5-HT1B receptors). Displays > 100-fold selectivity over 5HT1A, 5-HT2A, 5-HT2C receptors and other receptor types. Centrally active following oral administration.	2.43	2	1,2,4-oxadiazole; benzamides; N-alkylpiperazine; N-arylpiperazine
sq 28603 SQ 28603: a selective neutral endopeptidase inhibitor	3.12	1
rupatadine rupatadine: structure given in first source; RN given refers to trihydrochloride	3.12	1	benzocycloheptapyridine
ml-3000 [no description available]	3.12	1
mk 767 5-((2,4-dioxo-5-thiazolidinyl)methyl)-2-methoxy-N-((4-(trifluoromethyl)phenyl)methyl)benzamide: an antihyperlipidemic agent that also functions as an insulin sensitizer, PPARalpha agonist, and PPARgamma agonist; structure in first source	3.12	1
bms 207940 N-((2'-(((4,5-dimethyl-3-isoxazolyl)amino)sulfonyl)-4-(2-oxazolyl)(1,1'-biphenyl)-2-yl)methyl)-N,3,3-trimethylbutanamide: an ET(A) receptor antagonist; structure in first source	3.12	1
e 3040 E 3040: a dual inhibitor of 5-lipoxygenase and thromboxane A2 synthetase; structure given in first source	3.12	1	benzothiazoles; organic hydroxy compound; pyridines; secondary amino compound	anti-inflammatory drug; EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor; uricosuric drug
tropisetron Tropisetron: An indole derivative and 5-HT3 RECEPTOR antagonist that is used for the prevention of nausea and vomiting.. tropisetron : An indolyl carboxylate ester obtained by formal condensation of the carboxy group of indole-3-carboxylic acid with the hydroxy group of tropine.	3.12	1	indolyl carboxylic acid
sb-224289 SB 224289 : A member of the class of benzamides obtained by formal condensation of the carboxy group of 2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-carboxylic acid with the secondary amino group of 1'-methyl-6,7-dihydro-5H-spiro[furo[2,3-f]indole-3,4'-piperidine]. Selective 5-HT1B receptor antagonist (pKi = 8.2). Displays >60-fold selectivity over 5-HT1D, 5-HT1A, 5-HT1E, 5-HT1F, 5-HT2A and 5-HT2C receptors in radioligand binding and functional assays. Centrally active following oral administration in vivo.	2.04	1	1,2,4-oxadiazole; azaspiro compound; benzamides; organic heterotetracyclic compound	serotonergic antagonist
l 365260 L 365260: a CCK-B antagonist; structure given in first source; potent & selective CCK-B & gastrin receptor ligand; L 365260 and L 365346 are (R)- and (S)-stereoisomers, respectively	3.12	1	benzodiazepine
bosutinib 4-((2,4-dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methyl-1-piperazinyl)propoxy)-3-quinolinecarbonitrile: a Src kinase inhibitor; structure in first source	3.12	1	aminoquinoline; aromatic ether; dichlorobenzene; N-methylpiperazine; nitrile; tertiary amino compound	antineoplastic agent; tyrosine kinase inhibitor
6-(4-(2-(((4-chlorophenyl)sulfonyl)amino)ethyl)phenyl)-6-(3-pyridyl)hex-5-enoic acid 6-(4-(2-(((4-chlorophenyl)sulfonyl)amino)ethyl)phenyl)-6-(3-pyridyl)hex-5-enoic acid: combined thromboxane A2 receptor & thromboxane synthesis inhibitor; structure given in first source; RN given refers to (E)-isomer	3.12	1
5-chloro-2,3-dihydro-6-(4-methylpiperazin-1-yl)-1-(4-(pyridin-4-yl)naphth-1-ylaminocarbonyl)-1h-indole [no description available]	2.02	1
bms 248360 [no description available]	3.12	1
milnacipran [no description available]	3.12	1	acetamides
piperidines Piperidines: A family of hexahydropyridines.	4.05	4
guanosine 5'-o-(3-thiotriphosphate) Guanosine 5'-O-(3-Thiotriphosphate): Guanosine 5'-(trihydrogen diphosphate), monoanhydride with phosphorothioic acid. A stable GTP analog which enjoys a variety of physiological actions such as stimulation of guanine nucleotide-binding proteins, phosphoinositide hydrolysis, cyclic AMP accumulation, and activation of specific proto-oncogenes.	2.03	1	nucleoside triphosphate analogue
clozapine Clozapine: A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.. clozapine : A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia.	3.12	1	benzodiazepine; N-arylpiperazine; N-methylpiperazine; organochlorine compound	adrenergic antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; GABA antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; xenobiotic

Condition	Relationship Strength	Studies
Diseases, Metabolic [description not available]	2.94	1
Metabolic Diseases Generic term for diseases caused by an abnormal metabolic process. It can be congenital due to inherited enzyme abnormality (METABOLISM, INBORN ERRORS) or acquired due to disease of an endocrine organ or failure of a metabolically important organ such as the liver. (Stedman, 26th ed)	2.94	1
Affective Disorders [description not available]	2.03	1
Absence Seizure [description not available]	2.03	1
Seizures Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or seizure disorder.	2.03	1
Mood Disorders Those disorders that have a disturbance in mood as their predominant feature.	2.03	1
Anxiety Neuroses [description not available]	2.03	1
Anxiety Disorders Persistent and disabling ANXIETY.	2.03	1

sb-649915

Description

Cross-References

Synonyms (24)

Research Excerpts

Bioavailability

Protein Targets (14)

Inhibition Measurements

Biological Processes (248)

Molecular Functions (44)

Ceullar Components (51)

Bioassays (59)

Research

Studies (11)

Market Indicators

Research Demand Index: 11.87

Study Types

sb-649915

Description

Cross-References

Synonyms (24)

Research Excerpts

Bioavailability

Protein Targets (14)

Inhibition Measurements

Biological Processes (248)

Molecular Functions (44)

Ceullar Components (51)

Bioassays (59)

Research

Studies (11)

Market Indicators

Research Demand Index: 11.87

Study Types

Related Drugs (38)

Related Conditions (8)