way-208466 profile

ID Source	ID
PubMed CID	10337743
CHEMBL ID	571858
SCHEMBL ID	3892710
MeSH ID	M0557860

Synonym
way-208466
CHEMBL571858 ,
n-(2-{3-[(3-fluorophenyl)sulfonyl]-1h-pyrrolo[2,3-b]pyridin-1-yl}ethyl)-n,n-dimethylamine
2-(3-(3-fluorophenylsulfonyl)-1h-pyrrolo[2,3-b]pyridin-1-yl)-n,n-dimethylethanamine
bdbm50300828
way-208,466
633304-27-5
SCHEMBL3892710
2-[3-(3-fluorophenyl)sulfonylpyrrolo[2,3-b]pyridin-1-yl]-n,n-dimethylethanamine
gtpl8429
0AXW9ALG9W ,
1h-pyrrolo(2,3-b)pyridine-1-ethanamine, 3-((3-fluorophenyl)sulfonyl)-n,n-dimethyl-
DTXSID60621755
3-((3-fluorophenyl)sulfonyl)-n,n-dimethyl-1h-pyrrolo(2,3-b)pyridine-1-ethanamine
way-208466 dihydrochloride, >=98% (hplc)
unii-0axw9alg9w
NCGC00370934-02
{2-[3-(3-fluoro-benzenesulfonyl)-pyrrolo[2,3-b]pyridin-1-yl]-ethyl}-dimethyl-amine
3-[(3-fluorophenyl)sulfonyl]-n,n-dimethyl-1h-pyrrolo[2,3-b]pyridine-1-ethanamine
way-208466 2hcl
3-[(-3-fluorophenyl)sulfonyl]-n,n-dimethyl-1h-pyrrolo[2,3-b]pyridine-1-ethanaminedihydrochloride

Excerpt	Reference	Relevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51

Protein Targets (9)

Potency Measurements

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
cytochrome P450 2D6	Homo sapiens (human)	Potency	21.3174	0.0010	8.3798	61.1304	AID1645840
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
D(2) dopamine receptor	Homo sapiens (human)	IC50 (µMol)	5.0000	0.0000	0.7472	8.0000	AID447771
D(4) dopamine receptor	Homo sapiens (human)	IC50 (µMol)	5.0000	0.0001	1.1423	9.3280	AID447773
5-hydroxytryptamine receptor 2A	Homo sapiens (human)	IC50 (µMol)	0.3510	0.0001	0.8801	8.8500	AID447588
5-hydroxytryptamine receptor 2C	Homo sapiens (human)	IC50 (µMol)	0.6440	0.0001	1.0302	9.0000	AID447769
Delta-type opioid receptor	Mus musculus (house mouse)	IC50 (µMol)	5.0000	0.0001	0.7298	10.0000	AID447773
5-hydroxytryptamine receptor 7	Homo sapiens (human)	IC50 (µMol)	4.7640	0.0005	0.4546	4.7640	AID447770
D(3) dopamine receptor	Homo sapiens (human)	IC50 (µMol)	5.0000	0.0001	1.0178	8.7960	AID447772
5-hydroxytryptamine receptor 6	Homo sapiens (human)	Ki	0.0048	0.0002	0.5229	10.0000	AID1249636; AID1916471; AID443718; AID447580
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
5-hydroxytryptamine receptor 6	Homo sapiens (human)	EC50 (µMol)	0.0073	0.0001	0.0096	0.0448	AID1249637; AID443720; AID447581
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (166)

Process	via Protein(s)	Taxonomy
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)
positive regulation of MAP kinase activity	D(4) dopamine receptor	Homo sapiens (human)
behavioral fear response	D(4) dopamine receptor	Homo sapiens (human)
synaptic transmission, dopaminergic	D(4) dopamine receptor	Homo sapiens (human)
response to amphetamine	D(4) dopamine receptor	Homo sapiens (human)
intracellular calcium ion homeostasis	D(4) dopamine receptor	Homo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathway	D(4) dopamine receptor	Homo sapiens (human)
dopamine receptor signaling pathway	D(4) dopamine receptor	Homo sapiens (human)
adult locomotory behavior	D(4) dopamine receptor	Homo sapiens (human)
positive regulation of sodium:proton antiporter activity	D(4) dopamine receptor	Homo sapiens (human)
positive regulation of kinase activity	D(4) dopamine receptor	Homo sapiens (human)
response to histamine	D(4) dopamine receptor	Homo sapiens (human)
social behavior	D(4) dopamine receptor	Homo sapiens (human)
regulation of dopamine metabolic process	D(4) dopamine receptor	Homo sapiens (human)
dopamine metabolic process	D(4) dopamine receptor	Homo sapiens (human)
fear response	D(4) dopamine receptor	Homo sapiens (human)
regulation of circadian rhythm	D(4) dopamine receptor	Homo sapiens (human)
positive regulation of MAP kinase activity	D(4) dopamine receptor	Homo sapiens (human)
behavioral response to cocaine	D(4) dopamine receptor	Homo sapiens (human)
behavioral response to ethanol	D(4) dopamine receptor	Homo sapiens (human)
rhythmic process	D(4) dopamine receptor	Homo sapiens (human)
arachidonic acid secretion	D(4) dopamine receptor	Homo sapiens (human)
negative regulation of protein secretion	D(4) dopamine receptor	Homo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmission	D(4) dopamine receptor	Homo sapiens (human)
inhibitory postsynaptic potential	D(4) dopamine receptor	Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor internalization	D(4) dopamine receptor	Homo sapiens (human)
negative regulation of voltage-gated calcium channel activity	D(4) dopamine receptor	Homo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway	D(4) dopamine receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	D(4) dopamine receptor	Homo sapiens (human)
chemical synaptic transmission	D(4) dopamine receptor	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)
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)
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 (24)

Process	via Protein(s)	Taxonomy
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)
dopamine neurotransmitter receptor activity, coupled via Gi/Go	D(4) dopamine receptor	Homo sapiens (human)
dopamine neurotransmitter receptor activity	D(4) dopamine receptor	Homo sapiens (human)
protein binding	D(4) dopamine receptor	Homo sapiens (human)
potassium channel regulator activity	D(4) dopamine receptor	Homo sapiens (human)
SH3 domain binding	D(4) dopamine receptor	Homo sapiens (human)
dopamine binding	D(4) dopamine receptor	Homo sapiens (human)
identical protein binding	D(4) dopamine receptor	Homo sapiens (human)
metal ion binding	D(4) dopamine receptor	Homo sapiens (human)
epinephrine binding	D(4) dopamine receptor	Homo sapiens (human)
norepinephrine binding	D(4) dopamine receptor	Homo sapiens (human)
G protein-coupled serotonin receptor activity	D(4) dopamine receptor	Homo sapiens (human)
neurotransmitter receptor activity	D(4) dopamine receptor	Homo sapiens (human)
serotonin binding	D(4) dopamine receptor	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)
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)
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 (33)

Process	via Protein(s)	Taxonomy
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)
centrosome	D(4) dopamine receptor	Homo sapiens (human)
plasma membrane	D(4) dopamine receptor	Homo sapiens (human)
membrane	D(4) dopamine receptor	Homo sapiens (human)
postsynapse	D(4) dopamine receptor	Homo sapiens (human)
glutamatergic synapse	D(4) dopamine receptor	Homo sapiens (human)
plasma membrane	D(4) dopamine receptor	Homo sapiens (human)
dendrite	D(4) dopamine receptor	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	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)
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 (47)

Assay ID	Title	Year	Journal	Article
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID447581	Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID447587	Displacement of [3H]5-HT from human cloned 5HT1F receptor expressed in CHO cells at 1 uM	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID447771	Displacement of [3H]spiperone from human cloned dopamine D2 receptor expressed in CHO-K1 cells	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID1249637	Agonist activity at human 5-HT6 receptor expressed in HeLa cells after 10 mins by scintillation proximity assay	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Therapeutic Potential of 5-HT6 Receptor Agonists.
AID447777	Selectivity ratio of IC50 for human cloned 5HT1F receptor to human cloned 5HT6 receptor	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID447582	Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA relative to serotonin	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID1249644	Selectivity ratio of Ki for recombinant human 5-HT2C receptor to Ki for human 5-HT6 receptor	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Therapeutic Potential of 5-HT6 Receptor Agonists.
AID447769	Displacement of [3H]5-HT from human cloned 5HT2C receptor expressed in CHO cells	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID447785	Inhibition of schedule-induced polydipsia in po dosed Sprague-Dawley rat assessed as reduction of adjunctive drinking behavior	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID447773	Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO-K1 cells	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID1916471	Displacement of [3H] LSD from 5-HT6R in human HeLa cells assessed as inhibition constant incubated for 120 mins in presence of methiothepin by scintillation counting method	2021	Bioorganic & medicinal chemistry letters, 10-01, Volume: 49	Chemical update on the potential for serotonin 5-HT
AID447778	Selectivity ratio of IC50 for human cloned 5HT2A receptor to human cloned 5HT6 receptor	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID447776	Selectivity ratio of IC50 for human cloned 5HT1D receptor to human cloned 5HT6 receptor	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID1249645	Selectivity ratio of Ki for recombinant human 5-HT7 receptor to Ki for human 5-HT6 receptor	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Therapeutic Potential of 5-HT6 Receptor Agonists.
AID447580	Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID447586	Displacement of [3H]5-HT from human cloned 5HT1D receptor expressed in CHO cells at 1 uM	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID443722	Agonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassay relative to serotonin	2009	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24	1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-pyrrolopyridines are 5-HT(6) receptor ligands.
AID447772	Displacement of [3H]spiperone from human cloned dopamine D3 receptor expressed in CHO-K1 cells	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID1249648	Selectivity ratio of Ki for dopamine D4 receptor (unknown origin) to Ki for human 5-HT6 receptor	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Therapeutic Potential of 5-HT6 Receptor Agonists.
AID447784	Increase in extracellular glutamate level in Sprague-Dawley rat frontal cortex at 30 mg/kg, sc	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID1249642	Selectivity ratio of Ki for recombinant human 5-HT2A receptor to Ki for human 5-HT6 receptor	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Therapeutic Potential of 5-HT6 Receptor Agonists.
AID1249647	Selectivity ratio of Ki for dopamine D3 receptor (unknown origin) to Ki for human 5-HT6 receptor	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Therapeutic Potential of 5-HT6 Receptor Agonists.
AID447781	Selectivity ratio of IC50 for human cloned dopamine D2 receptor to human cloned 5HT6 receptor	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID447774	Increase in extracellular GABA level in Sprague-Dawley rat frontal cortex at 30 mg/kg, sc	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID443718	Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells	2009	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24	1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-pyrrolopyridines are 5-HT(6) receptor ligands.
AID1249640	Selectivity ratio of Ki for recombinant human 5-HT1D receptor to Ki for human 5-HT6 receptor	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Therapeutic Potential of 5-HT6 Receptor Agonists.
AID1249641	Selectivity ratio of Ki for recombinant human 5-HT1F receptor to Ki for human 5-HT6 receptor	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Therapeutic Potential of 5-HT6 Receptor Agonists.
AID447779	Selectivity ratio of IC50 for human cloned 5HT2C receptor to human cloned 5HT6 receptor	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID1249639	Selectivity ratio of Ki for recombinant human 5-HT1B receptor to Ki for human 5-HT6 receptor	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Therapeutic Potential of 5-HT6 Receptor Agonists.
AID443720	Agonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassay	2009	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24	1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-pyrrolopyridines are 5-HT(6) receptor ligands.
AID447782	Selectivity ratio of IC50 for human cloned dopamine D3 receptor to human cloned 5HT6 receptor	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID1249646	Selectivity ratio of Ki for dopamine D2 receptor (unknown origin) to Ki for human 5-HT6 receptor	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Therapeutic Potential of 5-HT6 Receptor Agonists.
AID447780	Selectivity ratio of IC50 for human cloned 5HT7 receptor to human cloned 5HT6 receptor	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID447775	Selectivity ratio of IC50 for human cloned 5HT1B receptor to human cloned 5HT6 receptor	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID447783	Selectivity ratio of IC50 for human cloned dopamine D4 receptor to human cloned 5HT6 receptor	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID1249643	Selectivity ratio of Ki for recombinant human 5-HT2B receptor to Ki for human 5-HT6 receptor	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Therapeutic Potential of 5-HT6 Receptor Agonists.
AID447588	Displacement of [125I]DOI from human cloned 5HT2A receptor expressed in CHO cells	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID1249638	Selectivity ratio of Ki for recombinant human 5-HT1A receptor to Ki for human 5-HT6 receptor	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Therapeutic Potential of 5-HT6 Receptor Agonists.
AID447770	Displacement of [3H]LSD from human cloned 5HT7 receptor expressed in CHO cells	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID447585	Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells at 1 uM	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
AID1249636	Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells by scintillation counter	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Therapeutic Potential of 5-HT6 Receptor Agonists.
AID1345170	Human 5-HT6 receptor (5-Hydroxytryptamine receptors)	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
[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	2 (28.57)	29.6817
2010's	2 (28.57)	24.3611
2020's	3 (42.86)	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 (28.57%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	5 (71.43%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
dan 2163 [no description available]	3.41	1	aromatic amide; aromatic amine; benzamides; pyrrolidines; sulfone	environmental contaminant; second generation antipsychotic; xenobiotic
sulpiride Sulpiride: A dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid. (From Merck Index, 11th ed). sulpiride : A member of the class of benzamides obtained from formal condensation between the carboxy group of 2-methoxy-5-sulfamoylbenzoic acid and the primary amino group of (1-ethylpyrrolidin-2-yl)methylamine.	3.41	1	benzamides; N-alkylpyrrolidine; sulfonamide	antidepressant; antiemetic; antipsychotic agent; dopaminergic antagonist
latrepirdine latrepirdine: structure	3.41	1	methylpyridines; pyridoindole	geroprotector
2-ethyl-5-methoxy-n,n-dimethyltryptamine 2-ethyl-5-methoxy-N,N-dimethyltryptamine: a 5-HT(6) receptor agonist; structure in first source	3.21	1
5-methoxy-2-phenyl-n,n-dimethyltryptamine [no description available]	3.21	1
ms-245 N,N-dimethyl-2-(1-(benzenesulfonyl)-5-methoxy-1H-indol-3-yl)ethylamine: a 5-HT(6) receptor ligand; structure in first source	3.21	1
st 1936 2-(5-chloro-2-methyl-1H-indol-3-yl)-N,N-dimethylethanamine: a 5-HT6 receptor agonist	3.21	1
vortioxetine Vortioxetine: A piperazine derivative that acts as a serotonin reuptake inhibitor, as a 5-HT3 receptor antagonist, and 5-HT1A receptor agonist. It is used for the treatment of anxiety and depression.. vortioxetine : An 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.	3.41	1	aryl sulfide; N-arylpiperazine	antidepressant; anxiolytic drug; serotonergic agonist; serotonergic antagonist
way 181187 [no description available]	4.19	2
e-6801 [no description available]	3.41	1
sb 742457 3-benzenesulfonyl-8-piperazin-1-ylquinoline: a 5-HT6 receptor antagonist	3.41	1
4-(4-chlorophenyl)sulfonyl-5-(3,4-dihydro-1H-isoquinolin-2-yl)-2-ethylsulfonylthiazole [no description available]	3.41	1	isoquinolines
sam-531 SAM-531: a 5-HT6 receptor antagonist; structure in first source	3.41	1
lu ae58054 [no description available]	3.41	1

Condition	Relationship Strength	Studies
Congenital Zika Syndrome [description not available]	2.25	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.25	1
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	2.25	1
Acute Confusional Senile Dementia [description not available]	3.23	1
Alzheimer Disease A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57)	3.23	1

way-208466

Cross-References

Synonyms (21)

Research Excerpts

Bioavailability

Protein Targets (9)

Potency Measurements

Inhibition Measurements

Activation Measurements

Biological Processes (166)

Molecular Functions (24)

Ceullar Components (33)

Bioassays (47)

Research

Studies (7)

Market Indicators

Research Demand Index: 12.72

Study Types

way-208466

Cross-References

Synonyms (21)

Research Excerpts

Bioavailability

Protein Targets (9)

Potency Measurements

Inhibition Measurements

Activation Measurements

Biological Processes (166)

Molecular Functions (24)

Ceullar Components (33)

Bioassays (47)

Research

Studies (7)

Market Indicators

Research Demand Index: 12.72

Study Types

Related Drugs (14)

Related Conditions (5)