Page last updated: 2024-11-10

a 85380

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Description

A 85380: structure given in first source; A-85380 is the S-enantiomer; A-159470 is the R-enantiomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5310969
CHEMBL ID59986
SCHEMBL ID676026
MeSH IDM0272455

Synonyms (17)

Synonym
(s)-3-(azetidin-2-ylmethoxy)pyridine
bdbm50049750
3-((s)-1-azetidin-2-ylmethoxy)-pyridine
a-85380
a 85380
CHEMBL59986 ,
a-159470
3-[[(2s)-azetidin-2-yl]methoxy]pyridine
gtpl5460
a85380
3-[(2s)-azetidin-2-ylmethoxy]pyridine
SCHEMBL676026
161416-98-4
3-(2(s)-azetidinylmethoxy)pyridine
NCGC00387223-01
Q27074089
pyridine, 3-(2-azetidinylmethoxy)-, (s)-

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" The oxazolo[4,5-b]pyridine, (R)-18, and 4-methoxyphenylurea, (R)-47, were identified as potent and selective modulators of the α7 nAChR with favorable in vitro safety profiles and good oral bioavailability in mouse."( Discovery of novel 2-((pyridin-3-yloxy)methyl)piperazines as α7 nicotinic acetylcholine receptor modulators for the treatment of inflammatory disorders.
Clark, RB; Elbaum, D; Kumar, A; Lamppu, D; LaRosa, G; Libertine, L; McDonough, A; Rush, R, 2014
)
0.4
"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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (22)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 2D6Homo sapiens (human)Potency26.83700.00108.379861.1304AID1645840
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Acetylcholine receptor subunit alphaHomo sapiens (human)Ki0.31400.00553.31338.2000AID1179333
Acetylcholine receptor subunit alphaTetronarce californica (Pacific electric ray)Ki0.31400.00279.359634.0000AID219643
Neuronal acetylcholine receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki0.01450.00000.352210.0000AID145682; AID145685; AID146006; AID146162
Acetylcholine receptor subunit gammaHomo sapiens (human)Ki0.31400.00553.31338.2000AID1179333
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)IC50 (µMol)0.00150.00030.30952.3000AID146322
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki0.00130.00000.12345.5000AID145682; AID145685; AID146486; AID146772; AID700118
Acetylcholine receptor subunit betaHomo sapiens (human)Ki0.31400.00553.31338.2000AID1179333
Neuronal acetylcholine receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki0.00010.00000.04230.4500AID145682; AID145685; AID145983
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)IC50 (µMol)0.00150.00030.32092.3000AID146322
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Ki0.00010.00000.10825.5000AID145682; AID145685; AID145983; AID146006; AID146486; AID700118
Neuronal acetylcholine receptor subunit beta-3Rattus norvegicus (Norway rat)Ki0.00020.00000.05250.4500AID145682; AID145685
Neuronal acetylcholine receptor subunit beta-4Rattus norvegicus (Norway rat)Ki0.01590.00000.296310.0000AID145682; AID145685; AID146162; AID146772
Neuronal acetylcholine receptor subunit beta-2Homo sapiens (human)IC50 (µMol)0.00150.00110.539010.0000AID414713
Neuronal acetylcholine receptor subunit beta-2Homo sapiens (human)Ki0.00000.00000.11173.5400AID1143254; AID146300; AID146301
Neuronal acetylcholine receptor subunit alpha-5Rattus norvegicus (Norway rat)Ki0.00020.00000.05250.4500AID145682; AID145685
Neuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)Ki0.14800.00221.742710.0000AID1143255; AID146786; AID146788
Neuronal acetylcholine receptor subunit alpha-6Rattus norvegicus (Norway rat)Ki0.00020.00000.05250.4500AID145682; AID145685
Neuronal acetylcholine receptor subunit alpha-9Rattus norvegicus (Norway rat)Ki0.00020.00000.05250.4500AID145682; AID145685
Neuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)IC50 (µMol)0.00150.00110.491110.0000AID414713
Neuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)Ki0.00000.00000.11573.5400AID1143254; AID146300; AID146301
Neuronal acetylcholine receptor subunit alpha-7Rattus norvegicus (Norway rat)Ki0.00020.00000.73078.0000AID145682; AID145685
Acetylcholine receptor subunit deltaHomo sapiens (human)Ki0.31400.00553.31338.2000AID1179333
Neuronal acetylcholine receptor subunit alpha-10Rattus norvegicus (Norway rat)Ki0.00020.00000.05250.4500AID145682; AID145685
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)EC50 (µMol)0.70000.01402.272410.0000AID1179366; AID146297
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)EC50 (µMol)0.70000.01402.310410.0000AID1179366; AID146297
Neuronal acetylcholine receptor subunit beta-2Homo sapiens (human)EC50 (µMol)0.70160.00001.51729.4000AID1179366; AID146297; AID414714; AID710187
Neuronal acetylcholine receptor subunit beta-4Homo sapiens (human)EC50 (µMol)0.70000.00703.454010.0000AID145356
Neuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)EC50 (µMol)0.70000.00702.25879.4000AID145356; AID225721
Neuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)EC50 (µMol)8.90000.12802.80188.9000AID146778; AID146779; AID710185
Neuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)EC50 (µMol)0.70160.00001.61869.4000AID1179366; AID146297; AID414714; AID710187
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (90)

Processvia Protein(s)Taxonomy
neuromuscular synaptic transmissionAcetylcholine receptor subunit alphaHomo sapiens (human)
neuromuscular junction developmentAcetylcholine receptor subunit alphaHomo sapiens (human)
regulation of membrane potentialAcetylcholine receptor subunit alphaHomo sapiens (human)
skeletal muscle contractionAcetylcholine receptor subunit alphaHomo sapiens (human)
monoatomic cation transportAcetylcholine receptor subunit alphaHomo sapiens (human)
neuronal action potentialAcetylcholine receptor subunit alphaHomo sapiens (human)
monoatomic ion transmembrane transportAcetylcholine receptor subunit alphaHomo sapiens (human)
regulation of membrane potentialAcetylcholine receptor subunit alphaHomo sapiens (human)
muscle cell cellular homeostasisAcetylcholine receptor subunit alphaHomo sapiens (human)
skeletal muscle tissue growthAcetylcholine receptor subunit alphaHomo sapiens (human)
musculoskeletal movementAcetylcholine receptor subunit alphaHomo sapiens (human)
neuromuscular processAcetylcholine receptor subunit alphaHomo sapiens (human)
excitatory postsynaptic potentialAcetylcholine receptor subunit alphaHomo sapiens (human)
neuron cellular homeostasisAcetylcholine receptor subunit alphaHomo sapiens (human)
membrane depolarizationAcetylcholine receptor subunit alphaHomo sapiens (human)
acetylcholine receptor signaling pathwayAcetylcholine receptor subunit alphaHomo sapiens (human)
response to nicotineAcetylcholine receptor subunit alphaHomo sapiens (human)
synaptic transmission, cholinergicAcetylcholine receptor subunit alphaHomo sapiens (human)
muscle contractionAcetylcholine receptor subunit gammaHomo sapiens (human)
signal transductionAcetylcholine receptor subunit gammaHomo sapiens (human)
synaptic transmission, cholinergicAcetylcholine receptor subunit gammaHomo sapiens (human)
monoatomic ion transmembrane transportAcetylcholine receptor subunit gammaHomo sapiens (human)
excitatory postsynaptic potentialAcetylcholine receptor subunit gammaHomo sapiens (human)
membrane depolarizationAcetylcholine receptor subunit gammaHomo sapiens (human)
chemical synaptic transmissionAcetylcholine receptor subunit gammaHomo sapiens (human)
acetylcholine receptor signaling pathwayAcetylcholine receptor subunit gammaHomo sapiens (human)
postsynaptic membrane organizationAcetylcholine receptor subunit betaHomo sapiens (human)
monoatomic cation transportAcetylcholine receptor subunit betaHomo sapiens (human)
muscle contractionAcetylcholine receptor subunit betaHomo sapiens (human)
signal transductionAcetylcholine receptor subunit betaHomo sapiens (human)
synaptic transmission, cholinergicAcetylcholine receptor subunit betaHomo sapiens (human)
neuromuscular synaptic transmissionAcetylcholine receptor subunit betaHomo sapiens (human)
monoatomic ion transmembrane transportAcetylcholine receptor subunit betaHomo sapiens (human)
behavioral response to nicotineAcetylcholine receptor subunit betaHomo sapiens (human)
regulation of membrane potentialAcetylcholine receptor subunit betaHomo sapiens (human)
nervous system processAcetylcholine receptor subunit betaHomo sapiens (human)
muscle cell developmentAcetylcholine receptor subunit betaHomo sapiens (human)
excitatory postsynaptic potentialAcetylcholine receptor subunit betaHomo sapiens (human)
membrane depolarizationAcetylcholine receptor subunit betaHomo sapiens (human)
chemical synaptic transmissionAcetylcholine receptor subunit betaHomo sapiens (human)
acetylcholine receptor signaling pathwayAcetylcholine receptor subunit betaHomo sapiens (human)
response to hypoxiaNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
monoatomic ion transportNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
calcium ion transportNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
smooth muscle contractionNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
signal transductionNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
synaptic transmission, cholinergicNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
visual perceptionNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
sensory perception of soundNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
learningNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
memoryNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
locomotory behaviorNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
associative learningNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
visual learningNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
regulation of dopamine secretionNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
sensory perception of painNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
vestibulocochlear nerve developmentNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
optic nerve morphogenesisNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
lateral geniculate nucleus developmentNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
central nervous system projection neuron axonogenesisNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
positive regulation of B cell proliferationNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
regulation of synaptic transmission, dopaminergicNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
positive regulation of dopamine secretionNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
monoatomic ion transmembrane transportNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
response to nicotineNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
behavioral response to nicotineNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
social behaviorNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
regulation of dopamine metabolic processNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
B cell activationNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
response to cocaineNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
regulation of circadian sleep/wake cycle, REM sleepNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
response to ethanolNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
negative regulation of action potentialNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
regulation of dendrite morphogenesisNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
nervous system processNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
cognitionNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
membrane depolarizationNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
regulation of synapse assemblyNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
excitatory postsynaptic potentialNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
synaptic transmission involved in micturitionNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
acetylcholine receptor signaling pathwayNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
response to acetylcholineNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
chemical synaptic transmissionNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
monoatomic ion transportNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
smooth muscle contractionNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
regulation of smooth muscle contractionNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
signal transductionNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
synaptic transmission, cholinergicNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
locomotory behaviorNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
neuronal action potentialNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
monoatomic ion transmembrane transportNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
behavioral response to nicotineNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
regulation of neurotransmitter secretionNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
positive regulation of transmission of nerve impulseNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
excitatory postsynaptic potentialNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
synaptic transmission involved in micturitionNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
chemical synaptic transmissionNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
acetylcholine receptor signaling pathwayNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
membrane depolarizationNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
monoatomic ion transportNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
regulation of smooth muscle contractionNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
signal transductionNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
activation of transmembrane receptor protein tyrosine kinase activityNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
synaptic transmission, cholinergicNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
nervous system developmentNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
locomotory behaviorNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
regulation of acetylcholine secretion, neurotransmissionNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
monoatomic ion transmembrane transportNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
behavioral response to nicotineNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
regulation of membrane potentialNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
regulation of dendrite morphogenesisNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
excitatory postsynaptic potentialNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
synaptic transmission involved in micturitionNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
acetylcholine receptor signaling pathwayNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
response to acetylcholineNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
response to nicotineNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
membrane depolarizationNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
negative regulation of tumor necrosis factor productionNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
response to hypoxiaNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of protein phosphorylationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
monoatomic ion transportNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
calcium ion transportNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
intracellular calcium ion homeostasisNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
signal transductionNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
synaptic transmission, cholinergicNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
learning or memoryNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
memoryNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
short-term memoryNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of cell population proliferationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
negative regulation of tumor necrosis factor productionNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
monoatomic ion transmembrane transportNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
response to nicotineNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of MAPK cascadeNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of angiogenesisNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
synapse organizationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
cognitionNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
sensory processingNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of protein metabolic processNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
excitatory postsynaptic potentialNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
calcium ion transmembrane transportNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
acetylcholine receptor signaling pathwayNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
dendritic spine organizationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
modulation of excitatory postsynaptic potentialNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
dendrite arborizationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of long-term synaptic potentiationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of amyloid-beta formationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
negative regulation of amyloid-beta formationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
regulation of amyloid precursor protein catabolic processNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
response to amyloid-betaNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
response to acetylcholineNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
regulation of amyloid fibril formationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of CoA-transferase activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of excitatory postsynaptic potentialNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
regulation of membrane potentialNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
chemical synaptic transmissionNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
action potentialNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
response to hypoxiaNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
DNA repairNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
monoatomic ion transportNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
calcium ion transportNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
response to oxidative stressNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
signal transductionNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
chemical synaptic transmissionNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
synaptic transmission, cholinergicNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
regulation of dopamine secretionNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
sensory perception of painNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
monoatomic ion transmembrane transportNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
response to nicotineNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
behavioral response to nicotineNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
B cell activationNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
regulation of membrane potentialNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
nervous system processNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
cognitionNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
membrane depolarizationNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
excitatory postsynaptic potentialNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
inhibitory postsynaptic potentialNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
acetylcholine receptor signaling pathwayNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
skeletal muscle contractionAcetylcholine receptor subunit deltaHomo sapiens (human)
monoatomic cation transportAcetylcholine receptor subunit deltaHomo sapiens (human)
muscle contractionAcetylcholine receptor subunit deltaHomo sapiens (human)
signal transductionAcetylcholine receptor subunit deltaHomo sapiens (human)
synaptic transmission, cholinergicAcetylcholine receptor subunit deltaHomo sapiens (human)
monoatomic ion transmembrane transportAcetylcholine receptor subunit deltaHomo sapiens (human)
skeletal muscle tissue growthAcetylcholine receptor subunit deltaHomo sapiens (human)
musculoskeletal movementAcetylcholine receptor subunit deltaHomo sapiens (human)
neuromuscular processAcetylcholine receptor subunit deltaHomo sapiens (human)
excitatory postsynaptic potentialAcetylcholine receptor subunit deltaHomo sapiens (human)
acetylcholine receptor signaling pathwayAcetylcholine receptor subunit deltaHomo sapiens (human)
chemical synaptic transmissionAcetylcholine receptor subunit deltaHomo sapiens (human)
membrane depolarizationAcetylcholine receptor subunit deltaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (16)

Processvia Protein(s)Taxonomy
acetylcholine receptor activityAcetylcholine receptor subunit alphaHomo sapiens (human)
acetylcholine-gated monoatomic cation-selective channel activityAcetylcholine receptor subunit alphaHomo sapiens (human)
acetylcholine bindingAcetylcholine receptor subunit alphaHomo sapiens (human)
acetylcholine-gated monoatomic cation-selective channel activityAcetylcholine receptor subunit alphaHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialAcetylcholine receptor subunit alphaHomo sapiens (human)
protein bindingAcetylcholine receptor subunit gammaHomo sapiens (human)
channel activityAcetylcholine receptor subunit gammaHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialAcetylcholine receptor subunit gammaHomo sapiens (human)
acetylcholine receptor activityAcetylcholine receptor subunit gammaHomo sapiens (human)
acetylcholine-gated monoatomic cation-selective channel activityAcetylcholine receptor subunit gammaHomo sapiens (human)
acetylcholine receptor activityAcetylcholine receptor subunit betaHomo sapiens (human)
acetylcholine-gated monoatomic cation-selective channel activityAcetylcholine receptor subunit betaHomo sapiens (human)
protein bindingAcetylcholine receptor subunit betaHomo sapiens (human)
channel activityAcetylcholine receptor subunit betaHomo sapiens (human)
ligand-gated monoatomic ion channel activityAcetylcholine receptor subunit betaHomo sapiens (human)
acetylcholine bindingAcetylcholine receptor subunit betaHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialAcetylcholine receptor subunit betaHomo sapiens (human)
acetylcholine-gated monoatomic cation-selective channel activityAcetylcholine receptor subunit betaHomo sapiens (human)
protein bindingNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
ligand-gated monoatomic ion channel activityNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
acetylcholine receptor activityNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
acetylcholine-gated monoatomic cation-selective channel activityNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
acetylcholine bindingNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
protein-containing complex bindingNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
quaternary ammonium group bindingNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
heterocyclic compound bindingNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
protein bindingNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
ligand-gated monoatomic ion channel activityNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
acetylcholine receptor activityNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
acetylcholine-gated monoatomic cation-selective channel activityNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
protein bindingNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
ligand-gated monoatomic ion channel activityNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
acetylcholine receptor activityNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
acetylcholine-gated monoatomic cation-selective channel activityNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
acetylcholine bindingNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
amyloid-beta bindingNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
monoatomic ion channel activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
calcium channel activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
protein bindingNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
acetylcholine receptor activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
toxic substance bindingNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
chloride channel regulator activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
acetylcholine-gated monoatomic cation-selective channel activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
acetylcholine bindingNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
protein homodimerization activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
protein bindingNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
ligand-gated monoatomic ion channel activityNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
acetylcholine receptor activityNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
acetylcholine-gated monoatomic cation-selective channel activityNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
acetylcholine bindingNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
acetylcholine-gated monoatomic cation-selective channel activityAcetylcholine receptor subunit deltaHomo sapiens (human)
acetylcholine bindingAcetylcholine receptor subunit deltaHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialAcetylcholine receptor subunit deltaHomo sapiens (human)
acetylcholine-gated monoatomic cation-selective channel activityAcetylcholine receptor subunit deltaHomo sapiens (human)
acetylcholine receptor activityAcetylcholine receptor subunit deltaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
neuromuscular junctionAcetylcholine receptor subunit alphaHomo sapiens (human)
plasma membraneAcetylcholine receptor subunit alphaHomo sapiens (human)
cell surfaceAcetylcholine receptor subunit alphaHomo sapiens (human)
neuromuscular junctionAcetylcholine receptor subunit alphaHomo sapiens (human)
postsynaptic membraneAcetylcholine receptor subunit alphaHomo sapiens (human)
postsynaptic specialization membraneAcetylcholine receptor subunit alphaHomo sapiens (human)
acetylcholine-gated channel complexAcetylcholine receptor subunit alphaHomo sapiens (human)
synapseAcetylcholine receptor subunit alphaHomo sapiens (human)
plasma membraneAcetylcholine receptor subunit alphaHomo sapiens (human)
neuron projectionAcetylcholine receptor subunit alphaHomo sapiens (human)
plasma membraneAcetylcholine receptor subunit gammaHomo sapiens (human)
postsynaptic membraneAcetylcholine receptor subunit gammaHomo sapiens (human)
acetylcholine-gated channel complexAcetylcholine receptor subunit gammaHomo sapiens (human)
plasma membraneAcetylcholine receptor subunit gammaHomo sapiens (human)
synapseAcetylcholine receptor subunit gammaHomo sapiens (human)
neuron projectionAcetylcholine receptor subunit gammaHomo sapiens (human)
neuromuscular junctionAcetylcholine receptor subunit betaHomo sapiens (human)
plasma membraneAcetylcholine receptor subunit betaHomo sapiens (human)
synapseAcetylcholine receptor subunit betaHomo sapiens (human)
postsynaptic specialization membraneAcetylcholine receptor subunit betaHomo sapiens (human)
acetylcholine-gated channel complexAcetylcholine receptor subunit betaHomo sapiens (human)
plasma membraneAcetylcholine receptor subunit betaHomo sapiens (human)
synapseAcetylcholine receptor subunit betaHomo sapiens (human)
neuron projectionAcetylcholine receptor subunit betaHomo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
external side of plasma membraneNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
membraneNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
presynaptic membraneNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
plasma membrane raftNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
cholinergic synapseNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
postsynaptic specialization membraneNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
acetylcholine-gated channel complexNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
neuron projectionNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
synapseNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
membraneNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
specific granule membraneNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
postsynaptic membraneNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
tertiary granule membraneNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
cholinergic synapseNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
acetylcholine-gated channel complexNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
neuron projectionNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
synapseNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
endoplasmic reticulumNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
Golgi apparatusNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
postsynaptic densityNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
membraneNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
nuclear speckNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
dendriteNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
neuronal cell bodyNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
plasma membrane raftNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
postsynaptic membraneNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
acetylcholine-gated channel complexNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
neuron projectionNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
synapseNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
membraneNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
plasma membrane raftNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
postsynaptic membraneNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
postsynapseNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
acetylcholine-gated channel complexNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
neuron projectionNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
synapseNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit alpha-9Rattus norvegicus (Norway rat)
plasma membraneNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
external side of plasma membraneNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
membraneNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
dendriteNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
neuronal cell bodyNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
postsynaptic membraneNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
acetylcholine-gated channel complexNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
synapseNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
neuron projectionNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
neuromuscular junctionAcetylcholine receptor subunit deltaHomo sapiens (human)
plasma membraneAcetylcholine receptor subunit deltaHomo sapiens (human)
acetylcholine-gated channel complexAcetylcholine receptor subunit deltaHomo sapiens (human)
postsynaptic membraneAcetylcholine receptor subunit deltaHomo sapiens (human)
postsynaptic specialization membraneAcetylcholine receptor subunit deltaHomo sapiens (human)
plasma membraneAcetylcholine receptor subunit deltaHomo sapiens (human)
neuron projectionAcetylcholine receptor subunit deltaHomo sapiens (human)
synapseAcetylcholine receptor subunit deltaHomo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit alpha-10Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (66)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings 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.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID414715Intrinsic activity at human alpha4beta2 nAChR expressed in HEK293 cells assessed as intracellular calcium level by FLIPR assay relative to (-)nicotine2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Complementary three-dimensional quantitative structure-activity relationship modeling of binding affinity and functional potency: a study on alpha4beta2 nicotinic ligands.
AID146786Binding affinity against human Nicotinic acetylcholine receptor alpha-7 was determined1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Synthesis and nicotinic acetylcholine receptor in vivo binding properties of 2-fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine: a new positron emission tomography ligand for nicotinic receptors.
AID146611Binding affinity towards Nicotinic acetylcholine receptor alpha4-beta2 in rat brain using [3H]-cytisine as radioligand1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
Structure-activity studies related to ABT-594, a potent nonopioid analgesic agent: effect of pyridine and azetidine ring substitutions on nicotinic acetylcholine receptor binding affinity and analgesic activity in mice.
AID146788Compound was evaluated for its ability to displace [125I]alpha-bungarotoxin (alpha-BgT) from K28 cells expressing human Nicotinic acetylcholine receptor alpha71998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors.
AID146322In vitro binding affinity for Nicotinic acetylcholine receptor alpha4-beta2 in rat cerebral cortical membrane using [3H]cytisine as radioligand2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
Novel potent ligands for the central nicotinic acetylcholine receptor: synthesis, receptor binding, and 3D-QSAR analysis.
AID710185Agonist activity at human alpha7 nAChR2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent and selective α4β2-nicotinic acetylcholine receptor (nAChR) partial agonists containing an isoxazolylpyridine ether scaffold that demonstrate antidepressant-like activity. Part II.
AID414714Agonist activity at human alpha4beta2 nAChR expressed in HEK293 cells assessed as intracellular calcium level by FLIPR assay2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Complementary three-dimensional quantitative structure-activity relationship modeling of binding affinity and functional potency: a study on alpha4beta2 nicotinic ligands.
AID1143254Agonist activity at alpha4beta2 nAChR (unknown origin)2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Discovery of novel 2-((pyridin-3-yloxy)methyl)piperazines as α7 nicotinic acetylcholine receptor modulators for the treatment of inflammatory disorders.
AID91540Maximal response of compound was determined in an in vitro [86Rb+] release assay using IMR-32 cells1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
Structure-activity studies related to ABT-594, a potent nonopioid analgesic agent: effect of pyridine and azetidine ring substitutions on nicotinic acetylcholine receptor binding affinity and analgesic activity in mice.
AID231913Ratio between the binding affinities towards rat alpha3-beta4 and forebrain nACh Receptor using [3H]EB2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.
AID710188Binding affinity to human alpha7 nAChR in human brain2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent and selective α4β2-nicotinic acetylcholine receptor (nAChR) partial agonists containing an isoxazolylpyridine ether scaffold that demonstrate antidepressant-like activity. Part II.
AID710186Agonist activity at ganglionic nAChR2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent and selective α4β2-nicotinic acetylcholine receptor (nAChR) partial agonists containing an isoxazolylpyridine ether scaffold that demonstrate antidepressant-like activity. Part II.
AID94464Compound was evaluated for functional activation to [86Rb+] efflux from human K177 cells expressing recombinant alpha4-beta2 receptors.1998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors.
AID146779Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor alpha71997Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26
Neuronal nicotinic acetylcholine receptors as targets for drug discovery.
AID145983Binding affinity towards rat nicotinic acetylcholine receptor alpha2-beta2 expressed in HEK293 cells using [3H]EB as radioligand2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.
AID242876Maximal response against Nicotinic acetylcholine receptor alpha3-beta42005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.
AID132950Analgesic activity in a mouse hot plate assay1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
Structure-activity studies related to ABT-594, a potent nonopioid analgesic agent: effect of pyridine and azetidine ring substitutions on nicotinic acetylcholine receptor binding affinity and analgesic activity in mice.
AID91525Ability to stimulate Rb+ efflux from human IMR-32 cell preparations containing human alpha3-betaX receptors1996Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
Novel 3-Pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors.
AID710189Binding affinity to muscle type alpha1beta1gammadelta-nAChR2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent and selective α4β2-nicotinic acetylcholine receptor (nAChR) partial agonists containing an isoxazolylpyridine ether scaffold that demonstrate antidepressant-like activity. Part II.
AID1179362Binding affinity to human brain alpha4beta2* nAChR2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors.
AID700124Agonist activity at human alpha4beta2 nACHR expressed in SH-EP1 cells at 10 uM by 86Rb+ efflux assay2012Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
Identification of novel α4β2-nicotinic acetylcholine receptor (nAChR) agonists based on an isoxazole ether scaffold that demonstrate antidepressant-like activity.
AID1179363Binding affinity to human brain alpha3beta4* nAChR2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors.
AID220120Binding affinity for alpha4 beta-2 nAChR using [3H]epibatidine in rat brain1998Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19
2-, 5-, and 6-Halo-3-(2(S)-azetidinylmethoxy)pyridines: synthesis, affinity for nicotinic acetylcholine receptors, and molecular modeling.
AID176047compound was evaluated for functional potencies and efficacies at rat nAChR subtype DA release1997Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26
Neuronal nicotinic acetylcholine receptors as targets for drug discovery.
AID225720Binding affinity towards rat alpha2-beta4 nACh receptor expressed in HEK293 cells using [3H]EB as radioligand2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.
AID145685Binding affinity towards rat forebrain nicotinic acetylcholine receptor using [3H]EB as radioligand2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.
AID242877Maximal response against Nicotinic acetylcholine receptor alpha4-beta22005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.
AID146301Compound was evaluated for its ability to displace [3H]cytisine from K177 cells expressing human Nicotinic acetylcholine receptor alpha4-beta21998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors.
AID132955Compound was evaluated for the analgesic activity by mouse hotplate assay at the doses of 0.62 and 6.2; No significant effect observed at the doses tested1998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors.
AID146772Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta4 expressed in HEK293 cells using [3H]EB as radioligand2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.
AID146300Binding affinity against human Nicotinic acetylcholine receptor alpha4-beta21999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Synthesis and nicotinic acetylcholine receptor in vivo binding properties of 2-fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine: a new positron emission tomography ligand for nicotinic receptors.
AID146486Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK293 cells using [3H]EB as radioligand2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.
AID1179366Agonist activity at human alpha4beta2 nAChR2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors.
AID145682Binding affinity against Nicotinic Acetylcholine Receptor was determined by measuring the displacement of [3H]cytisine from a preparation of whole rat brain.1996Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
Novel 3-Pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors.
AID242872Maximal response against Nicotinic acetylcholine receptor alpha 72005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.
AID225721Functional activation of human sympathetic ganglionic type nAChRs in IMR-32 cells containing alpha-3 subtype1998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors.
AID91534Maximum efficacy relative to 100(uM) (S)-nicotine for cell preparations containing alpha3-betaX IMR32 cells1996Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
Novel 3-Pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors.
AID1179365Binding affinity to rat brain alpha4beta2* nAChR2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors.
AID145688Binding affinity towards nicotinic acetylcholine receptor using [3H]nicotine as radioligand in rat brain homogenates2002Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15
A comparison of the binding of three series of nicotinic ligands.
AID146006Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta2 expressed in HEK293 cells using [3H]EB as radioligand2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.
AID94463Maximum efficacy relative to 100(uM) (S)-nicotine for cell preparations containing alpha4-beta2 K177 cells1996Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
Novel 3-Pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors.
AID1179364Binding affinity to human brain alpha7* nAChR2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors.
AID700118Displacement of [3H]epibatidine from rat alpha4beta2 nACHR2012Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
Identification of novel α4β2-nicotinic acetylcholine receptor (nAChR) agonists based on an isoxazole ether scaffold that demonstrate antidepressant-like activity.
AID231915Ratio between the binding affinities towards rat alpha4-beta4 and alpha4-beta2 nACh receptor using [3H]EB as radioligand2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.
AID414713Displacement of [3H]cytisine from human alpha4beta2 nAChR expressed in HEK293 cells2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Complementary three-dimensional quantitative structure-activity relationship modeling of binding affinity and functional potency: a study on alpha4beta2 nicotinic ligands.
AID1179333Antagonist activity at human alpha1beta1gammadelta nAChR2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors.
AID146162Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta4 expressed in HEK293 cells using [3H]EB as radioligand2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.
AID146778Compound was evaluated for functional activation from channel currents at human Nicotinic acetylcholine receptor alpha-7 expressed in oocytes.1998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors.
AID1143255Agonist activity at alpha7 nAChR (unknown origin)2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Discovery of novel 2-((pyridin-3-yloxy)methyl)piperazines as α7 nicotinic acetylcholine receptor modulators for the treatment of inflammatory disorders.
AID231912Ratio between the binding affinities towards rat alpha3-beta4 and alpha3-beta2 nACh receptor using [3H]EB as radioligand2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.
AID1179367Agonist activity at human alpha3beta4* nAChR2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors.
AID145686Compound was evaluated for its ability to displace [3H]-cytisine binding from high-affinity Nicotinic acetylcholine receptor in rat brain (principally the alpha4-beta2 nAChR subtype)1998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors.
AID231911Ratio between the binding affinities towards rat alpha2-beta4 and alpha2-beta2 nACh receptor using [3H]-EB as radioligand2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.
AID219643Compound was evaluated for its ability to displace [125 I]alpha-bungarotoxin (alpha-BgT) from torpedo alpha1-beta1-gamma1 electroplax1998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors.
AID146297Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor alpha4-beta21997Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26
Neuronal nicotinic acetylcholine receptors as targets for drug discovery.
AID710187Agonist activity at human alpha4beta2 nAChR2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent and selective α4β2-nicotinic acetylcholine receptor (nAChR) partial agonists containing an isoxazolylpyridine ether scaffold that demonstrate antidepressant-like activity. Part II.
AID710191Binding affinity to alpha4beta2 nAChR in rat brain2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent and selective α4β2-nicotinic acetylcholine receptor (nAChR) partial agonists containing an isoxazolylpyridine ether scaffold that demonstrate antidepressant-like activity. Part II.
AID710190Binding affinity to alpha4beta2 nAChR in human brain2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent and selective α4β2-nicotinic acetylcholine receptor (nAChR) partial agonists containing an isoxazolylpyridine ether scaffold that demonstrate antidepressant-like activity. Part II.
AID94460Ability to stimulate Rb+ efflux from human K177 cell preparations containing human alpha4-beta2 receptors1996Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
Novel 3-Pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors.
AID225722Intrinsic activity against human sympathetic ganglionic type nAChRs in IMR-32 cells containing alpha-3 subtype1998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors.
AID145356Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor subtype IMR-32 (ganglionic)1997Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26
Neuronal nicotinic acetylcholine receptors as targets for drug discovery.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (101)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's16 (15.84)18.2507
2000's63 (62.38)29.6817
2010's19 (18.81)24.3611
2020's3 (2.97)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 15.09

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index15.09 (24.57)
Research Supply Index4.63 (2.92)
Research Growth Index4.55 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (15.09)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (0.99%)5.53%
Reviews6 (5.94%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other94 (93.07%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]