Page last updated: 2024-12-05

tert-butyl peroxybenzoate

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Cross-References

ID SourceID
PubMed CID10092649
CHEMBL ID522460
SCHEMBL ID5473311
MeSH IDM0168166

Synonyms (28)

Synonym
tbpb ,
bdbm50263887
1-(1''-(2-methylbenzyl)-1,4''-bipiperidin-4-yl)-1h-benzo[d]imidazol-2(3h)-one
1-(1''-2-methylbenzyl)-1,4''-bipiperidin-4-yl)-1h-benzo[d]imidazol-2(3h)-one
CHEMBL522460 ,
634616-95-8
gtpl3258
3-[1-[1-[(2-methylphenyl)methyl]piperidin-4-yl]piperidin-4-yl]-1h-benzimidazol-2-one
SCHEMBL5473311
1-[1-[1-(2-methylbenzyl)piperidin-4-yl]piperidin-4-yl]-1,3-dihydro-2h-benzimidazol-2-one
CWPKTBMRVATCBL-UHFFFAOYSA-N
CS-3517
2-pyrrolo-1,3,2-dioxa-phospholan
2-pyrrol-1-yl-1,3,2-dioxaphospholan
1-(1'-(2-methylbenzyl)-1,4'-bipiperidin-4-yl)-1h-benzo[d]imidazol-2(3h)-one
HY-14562
AKOS026750197
tbpb, >=98% (hplc)
NCGC00390669-01
1-(1a?(2-methylbenzyl)-1,4a?bipiperidin-4-yl)-1h-benzo[d]imidazol-2(3h)-one
FT-0746315
Q27088942
BCP13406
BRD-K86989957-001-01-7
1,3-dihydro-1-[1'-[(2-methylphenyl)methyl][1,4'-bipiperidin]-4-yl]-2h-benzimidazol-2-one
A918055
F85081
MS-26922

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"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 (17)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency23.91850.01237.983543.2770AID1645841
cytochrome P450 2D6Homo sapiens (human)Potency11.98770.00108.379861.1304AID1645840
[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)
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC50 (µMol)3.48370.00001.23267.7930AID724753
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.32000.00000.690210.0000AID511606
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC50 (µMol)0.73770.00001.15467.5858AID724751
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.13000.00000.79519.1201AID511608
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki0.60130.00010.579710.0000AID724747
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)IC50 (µMol)5.48770.00052.891925.1700AID724762
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC50 (µMol)0.49140.00052.747825.1700AID724761
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC50 (µMol)3.97000.00052.780225.1700AID724760
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC50 (µMol)4.89890.00010.99178.0000AID724750
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki0.94000.00000.72926.9183AID511609
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC50 (µMol)1.28910.00053.314249.5000AID724763
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC50 (µMol)3.98110.00001.403910.0000AID724759
D(2) dopamine receptorHomo sapiens (human)IC50 (µMol)3.87500.00000.74728.0000AID344740; AID388098
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC50 (µMol)2.32210.00011.01049.9280AID724752
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.43000.00000.54057.7600AID511607
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.29000.00000.360910.0000AID511765
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.08500.00010.954910.0000AID511734
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.01100.00000.272610.0000AID511763
Alpha-1B adrenergic receptorHomo sapiens (human)Ki0.01900.00000.471310.0000AID511764
[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)
Muscarinic acetylcholine receptor M2Homo sapiens (human)EC50 (µMol)43.33330.00000.737810.0000AID344727; AID388100; AID724757
Muscarinic acetylcholine receptor M4Homo sapiens (human)EC50 (µMol)43.33330.00570.84656.6069AID344731; AID388102; AID724755
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)EC50 (µMol)0.07950.00001.262610.0000AID725035
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)EC50 (µMol)30.00000.00000.764610.0000AID724766
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)EC50 (µMol)30.00000.00000.990510.0000AID724764; AID724765
Muscarinic acetylcholine receptor M5Homo sapiens (human)EC50 (µMol)43.33330.05501.957010.0000AID344733; AID388103; AID724754
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)EC50 (µMol)30.00000.00001.160510.0000AID724767
Muscarinic acetylcholine receptor M1Homo sapiens (human)EC50 (µMol)0.21930.00161.304310.0000AID344725; AID388096; AID511592; AID724759
Muscarinic acetylcholine receptor M3Homo sapiens (human)EC50 (µMol)43.33330.00040.99355.9000AID344729; AID388101; AID724756
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (173)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of heart contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
response to virusMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M2Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M4Homo sapiens (human)
cell surface receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
regulation of locomotionMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M4Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M4Homo sapiens (human)
gastric acid secretionMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
dopamine transportMuscarinic acetylcholine receptor M5Homo sapiens (human)
transmission of nerve impulseMuscarinic acetylcholine receptor M5Homo sapiens (human)
regulation of phosphatidylinositol dephosphorylationMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M5Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M5Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
positive regulation of monoatomic ion transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
neuromuscular synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of locomotionMuscarinic acetylcholine receptor M1Homo sapiens (human)
saliva secretionMuscarinic acetylcholine receptor M1Homo sapiens (human)
cognitionMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of postsynaptic membrane potentialMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of glial cell proliferationMuscarinic acetylcholine receptor M1Homo sapiens (human)
positive regulation of intracellular protein transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
temperature homeostasisD(2) dopamine receptorHomo sapiens (human)
response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein phosphorylationD(2) dopamine receptorHomo sapiens (human)
response to amphetamineD(2) dopamine receptorHomo sapiens (human)
nervous system process involved in regulation of systemic arterial blood pressureD(2) dopamine receptorHomo sapiens (human)
regulation of heart rateD(2) dopamine receptorHomo sapiens (human)
regulation of sodium ion transportD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(2) dopamine receptorHomo sapiens (human)
positive regulation of neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
positive regulation of receptor internalizationD(2) dopamine receptorHomo sapiens (human)
autophagyD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
neuron-neuron synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
axonogenesisD(2) dopamine receptorHomo sapiens (human)
synapse assemblyD(2) dopamine receptorHomo sapiens (human)
sensory perception of smellD(2) dopamine receptorHomo sapiens (human)
long-term memoryD(2) dopamine receptorHomo sapiens (human)
grooming behaviorD(2) dopamine receptorHomo sapiens (human)
locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
adult walking behaviorD(2) dopamine receptorHomo sapiens (human)
protein localizationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell population proliferationD(2) dopamine receptorHomo sapiens (human)
associative learningD(2) dopamine receptorHomo sapiens (human)
visual learningD(2) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(2) dopamine receptorHomo sapiens (human)
response to light stimulusD(2) dopamine receptorHomo sapiens (human)
response to toxic substanceD(2) dopamine receptorHomo sapiens (human)
response to iron ionD(2) dopamine receptorHomo sapiens (human)
response to inactivityD(2) dopamine receptorHomo sapiens (human)
Wnt signaling pathwayD(2) dopamine receptorHomo sapiens (human)
striatum developmentD(2) dopamine receptorHomo sapiens (human)
orbitofrontal cortex developmentD(2) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(2) dopamine receptorHomo sapiens (human)
adenohypophysis developmentD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell migrationD(2) dopamine receptorHomo sapiens (human)
peristalsisD(2) dopamine receptorHomo sapiens (human)
auditory behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of synaptic transmission, GABAergicD(2) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(2) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
response to histamineD(2) dopamine receptorHomo sapiens (human)
response to nicotineD(2) dopamine receptorHomo sapiens (human)
positive regulation of urine volumeD(2) dopamine receptorHomo sapiens (human)
positive regulation of renal sodium excretionD(2) dopamine receptorHomo sapiens (human)
positive regulation of multicellular organism growthD(2) dopamine receptorHomo sapiens (human)
response to cocaineD(2) dopamine receptorHomo sapiens (human)
negative regulation of circadian sleep/wake cycle, sleepD(2) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(2) dopamine receptorHomo sapiens (human)
drinking behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(2) dopamine receptorHomo sapiens (human)
response to morphineD(2) dopamine receptorHomo sapiens (human)
pigmentationD(2) dopamine receptorHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(2) dopamine receptorHomo sapiens (human)
negative regulation of innate immune responseD(2) dopamine receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IID(2) dopamine receptorHomo sapiens (human)
negative regulation of insulin secretionD(2) dopamine receptorHomo sapiens (human)
acid secretionD(2) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(2) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(2) dopamine receptorHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityD(2) dopamine receptorHomo sapiens (human)
response to axon injuryD(2) dopamine receptorHomo sapiens (human)
branching morphogenesis of a nerveD(2) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(2) dopamine receptorHomo sapiens (human)
epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(2) dopamine receptorHomo sapiens (human)
release of sequestered calcium ion into cytosolD(2) dopamine receptorHomo sapiens (human)
dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of synapse structural plasticityD(2) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(2) dopamine receptorHomo sapiens (human)
excitatory postsynaptic potentialD(2) dopamine receptorHomo sapiens (human)
positive regulation of growth hormone secretionD(2) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeD(2) dopamine receptorHomo sapiens (human)
regulation of locomotion involved in locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
negative regulation of cellular response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
positive regulation of glial cell-derived neurotrophic factor productionD(2) dopamine receptorHomo sapiens (human)
positive regulation of long-term synaptic potentiationD(2) dopamine receptorHomo sapiens (human)
hyaloid vascular plexus regressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of neuron migrationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(2) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
calcium-mediated signalingMuscarinic acetylcholine receptor M3Homo sapiens (human)
regulation of monoatomic ion transmembrane transporter activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
synaptic transmission, cholinergicMuscarinic acetylcholine receptor M3Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M3Homo sapiens (human)
positive regulation of insulin secretionMuscarinic acetylcholine receptor M3Homo sapiens (human)
protein modification processMuscarinic acetylcholine receptor M3Homo sapiens (human)
positive regulation of smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
saliva secretionMuscarinic acetylcholine receptor M3Homo sapiens (human)
acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
ion channel modulating, G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
ligand-gated ion channel signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M3Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-1D adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1D adrenergic receptorHomo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 2CHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
locomotory behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
feeding behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2CHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of nervous system process5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of corticotropin-releasing hormone secretion5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of calcium-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2CHomo sapiens (human)
MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
apoptotic processAlpha-1A adrenergic receptorHomo sapiens (human)
smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
activation of phospholipase C activityAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1A adrenergic receptorHomo sapiens (human)
adult heart developmentAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of cell population proliferationAlpha-1A adrenergic receptorHomo sapiens (human)
response to xenobiotic stimulusAlpha-1A adrenergic receptorHomo sapiens (human)
response to hormoneAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of autophagyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of action potentialAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
calcium ion transport into cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
cell growth involved in cardiac muscle cell developmentAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase C signalingAlpha-1A adrenergic receptorHomo sapiens (human)
pilomotor reflexAlpha-1A adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-1B adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of cardiac muscle contractionAlpha-1B adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (21)

Processvia Protein(s)Taxonomy
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
arrestin family protein bindingMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M4Homo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(2) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(2) dopamine receptorHomo sapiens (human)
protein bindingD(2) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(2) dopamine receptorHomo sapiens (human)
dopamine bindingD(2) dopamine receptorHomo sapiens (human)
ionotropic glutamate receptor bindingD(2) dopamine receptorHomo sapiens (human)
identical protein bindingD(2) dopamine receptorHomo sapiens (human)
heterocyclic compound bindingD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(2) dopamine receptorHomo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
signaling receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
acetylcholine bindingMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
identical protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1D adrenergic receptorHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1B adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1B adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (41)

Processvia Protein(s)Taxonomy
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
clathrin-coated endocytic vesicle membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
asymmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
symmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
neuronal cell bodyMuscarinic acetylcholine receptor M2Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M2Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M4Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M4Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M5Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M5Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M1Homo sapiens (human)
Schaffer collateral - CA1 synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic density membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M1Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
Golgi membraneD(2) dopamine receptorHomo sapiens (human)
acrosomal vesicleD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
ciliumD(2) dopamine receptorHomo sapiens (human)
lateral plasma membraneD(2) dopamine receptorHomo sapiens (human)
endocytic vesicleD(2) dopamine receptorHomo sapiens (human)
axonD(2) dopamine receptorHomo sapiens (human)
dendriteD(2) dopamine receptorHomo sapiens (human)
synaptic vesicle membraneD(2) dopamine receptorHomo sapiens (human)
sperm flagellumD(2) dopamine receptorHomo sapiens (human)
dendritic spineD(2) dopamine receptorHomo sapiens (human)
perikaryonD(2) dopamine receptorHomo sapiens (human)
axon terminusD(2) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(2) dopamine receptorHomo sapiens (human)
ciliary membraneD(2) dopamine receptorHomo sapiens (human)
non-motile ciliumD(2) dopamine receptorHomo sapiens (human)
dopaminergic synapseD(2) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(2) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(2) dopamine receptorHomo sapiens (human)
presynaptic membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
endoplasmic reticulum membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
basal plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
basolateral plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M3Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M3Homo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2CHomo sapiens (human)
nucleusAlpha-1A adrenergic receptorHomo sapiens (human)
nucleoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
caveolaAlpha-1A adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
nucleusAlpha-1B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
caveolaAlpha-1B adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (55)

Assay IDTitleYearJournalArticle
AID388102Agonist activity at muscarinic M4 receptor2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties.
AID344727Agonist activity at muscarinic M2 receptor2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen.
AID724747Displacement of [3H]NMS from rat muscarinic M1 receptor expressed in CHO cells after 3 hrs2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
AID724759Partial agonist activity at human muscarinic M1 receptor expressed in CHO cells calcium response2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
AID724764Partial agonist activity at rat muscarinic M5 receptor expressed in CHO cells calcium response2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
AID724753Antagonist activity at human muscarinic M2 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
AID724757Partial agonist activity at human muscarinic M2 receptor expressed in CHO cells calcium response2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
AID724760Antagonist activity at rat muscarinic M5 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
AID724761Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
AID724755Partial agonist activity at human muscarinic M4 receptor expressed in CHO cells calcium response2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
AID388097Agonist activity at muscarinic M1 receptor relative to carbachol2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties.
AID344740Antagonist activity at dopamine D2 receptor2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen.
AID724758Partial agonist activity at human muscarinic M1 receptor expressed in CHO cells calcium response relative to acetylcholine2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
AID724762Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
AID344726Agonist activity at muscarinic M1 receptor relative to carbachol2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen.
AID511609Displacement of [3H]-4-DAMP from human muscarinic M5 receptor expressed in BHK-21 cells2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
AID724752Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
AID388101Agonist activity at muscarinic M3 receptor2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties.
AID511765Binding affinity to human adrenergic Alpha-1D receptor by radioligand displacement assay2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
AID388096Agonist activity at muscarinic M1 receptor2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties.
AID511608Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
AID511593Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay relative to acetylcholine2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
AID511596Agonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux at 10 uM by FLIPR assay relative to acetylcholine2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
AID511602Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux at 10 uM by FLIPR assay relative to acetylcholine2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
AID724765Partial agonist activity at rat muscarinic M4 receptor expressed in CHO cells calcium response2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
AID511763Binding affinity to human adrenergic alpha1A receptor by radioligand displacement assay2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
AID511605Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux at 10 uM by FLIPR assay relative to acetylcholine2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
AID511592Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
AID344729Agonist activity at muscarinic M3 receptor2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen.
AID724766Partial agonist activity at rat muscarinic M3 receptor expressed in CHO cells calcium response2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
AID388100Agonist activity at muscarinic M2 receptor2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties.
AID724768Partial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium response relative to acetylcholine2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
AID388103Agonist activity at muscarinic M5 receptor2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties.
AID511594Agonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
AID724756Partial agonist activity at human muscarinic M3 receptor expressed in CHO cells calcium response2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
AID724754Partial agonist activity at human muscarinic M5 receptor expressed in CHO cells calcium response2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
AID724751Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
AID344733Agonist activity at muscarinic M5 receptor2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen.
AID724763Antagonist activity at rat muscarinic M2 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
AID725035Partial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium response2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
AID388098Inhibition of dopamine D2 receptor2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties.
AID344725Agonist activity at muscarinic M1 receptor2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen.
AID724750Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
AID511607Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
AID511764Binding affinity to human adrenergic Alpha-1B receptor by radioligand displacement assay2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
AID511734Binding affinity to human 5HT2C receptor agonist site by radioligand displacement assay2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
AID511606Displacement of [3H]-AFDX-384 from human muscarinic M2 receptor expressed in CHO-K1 cells2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
AID724767Partial agonist activity at rat muscarinic M2 receptor expressed in CHO cells calcium response2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
AID344731Agonist activity at muscarinic M4 receptor2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen.
AID511599Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux at 10 uM by FLIPR assay relative to acetylcholine2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
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.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (28.57)29.6817
2010's3 (42.86)24.3611
2020's2 (28.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]