Page last updated: 2024-11-13

cep 26401

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

Cross-References

ID SourceID
PubMed CID25070031
CHEMBL ID1829335
CHEMBL ID1813052
CHEBI ID177564
SCHEMBL ID118744
MeSH IDM0561268

Synonyms (29)

Synonym
3-[4-[3-[(2r)-2-methylpyrrolidin-1-yl]propoxy]phenyl]-1h-pyridazin-6-one
CHEBI:177564
1005402-19-6
irdabisant
CHEMBL1829335
cep 26401
cep-26401
D10128
irdabisant (usan)
bdbm50350021
chembl1813052
cep26401
unii-wh7isp34ka
wh7isp34ka ,
irdabisant [usan:inn]
irdabisant [who-dd]
irdabisant [usan]
irdabisant [inn]
SCHEMBL118744
XUKROCVZGZNGSI-CQSZACIVSA-N
6-{4-[3-((r)-2-methyl-pyrrolidin-1-yl)-propoxy]-phenyl}-2h-pyridazin-3-one
DTXSID50143375
DB12900
(r)-6-(4-(3-(2-methylpyrrolidin-1-yl)propoxy)phenyl)pyridazin-3(2h)-one
Q27292641
CS-0034318
HY-109968
AT38262
AKOS040752101

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"5 nM) but displayed low oral bioavailability in the rat."( Optimization of 5-pyridazin-3-one phenoxypropylamines as potent, selective histamine H₃ receptor antagonists with potent cognition enhancing activity.
Aimone, LD; Huang, Z; Hudkins, RL; Lyons, J; Mathiasen, J; Raddatz, R; Tao, M, 2012
)
0.38
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
ring assemblyTwo or more cyclic systems (single rings or fused systems) which are directly joined to each other by double or single bonds are named ring assemblies when the number of such direct ring junctions is one less than the number of cyclic systems involved.
pyridazines
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (10)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki3.70000.00000.690210.0000AID611539
Poly [ADP-ribose] polymerase 1Homo sapiens (human)IC50 (µMol)30.00000.00020.81239.8100AID611630
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC50 (µMol)17.50000.00081.541620.0000AID611632
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki10.00000.00031.465610.0000AID611542
Alpha-1A adrenergic receptorHomo sapiens (human)Ki9.80000.00000.272610.0000AID611540
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Ki0.00850.00020.484110.0000AID648454
5-hydroxytryptamine receptor 3AHomo sapiens (human)Ki0.00200.00000.74119.9000AID648455
Sodium-dependent dopamine transporter Homo sapiens (human)IC50 (µMol)9.40000.00071.841946.0000AID611631
Sodium-dependent dopamine transporter Homo sapiens (human)Ki11.00000.00021.11158.0280AID611541
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)13.80000.00091.901410.0000AID611725
Histamine H3 receptorRattus norvegicus (Norway rat)Ki0.00650.00010.29638.5110AID1071994; AID1201927; AID611518; AID611527; AID618582; AID622486; AID630098
Histamine H3 receptorHomo sapiens (human)Ki0.00200.00010.33998.5110AID1071995; AID1201926; AID611517; AID618581; AID622483; AID630097
[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)
Histamine H3 receptorRattus norvegicus (Norway rat)EC50 (µMol)0.00200.00201.55926.2000AID611532
Histamine H3 receptorHomo sapiens (human)EC50 (µMol)0.00110.00000.09473.1623AID611530
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histamine H3 receptorRattus norvegicus (Norway rat)Kb0.00110.00110.00110.0011AID611531
Histamine H3 receptorHomo sapiens (human)Kb0.00040.00020.20972.0000AID611529
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (154)

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)
DNA damage responsePoly [ADP-ribose] polymerase 1Homo sapiens (human)
mitochondrion organizationPoly [ADP-ribose] polymerase 1Homo sapiens (human)
mitochondrial DNA metabolic processPoly [ADP-ribose] polymerase 1Homo sapiens (human)
regulation of protein localizationPoly [ADP-ribose] polymerase 1Homo sapiens (human)
cellular response to oxidative stressPoly [ADP-ribose] polymerase 1Homo sapiens (human)
protein modification processPoly [ADP-ribose] polymerase 1Homo sapiens (human)
mitochondrial DNA repairPoly [ADP-ribose] polymerase 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIPoly [ADP-ribose] polymerase 1Homo sapiens (human)
telomere maintenancePoly [ADP-ribose] polymerase 1Homo sapiens (human)
DNA repairPoly [ADP-ribose] polymerase 1Homo sapiens (human)
double-strand break repairPoly [ADP-ribose] polymerase 1Homo sapiens (human)
transcription by RNA polymerase IIPoly [ADP-ribose] polymerase 1Homo sapiens (human)
apoptotic processPoly [ADP-ribose] polymerase 1Homo sapiens (human)
DNA damage responsePoly [ADP-ribose] polymerase 1Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayPoly [ADP-ribose] polymerase 1Homo sapiens (human)
response to gamma radiationPoly [ADP-ribose] polymerase 1Homo sapiens (human)
positive regulation of cardiac muscle hypertrophyPoly [ADP-ribose] polymerase 1Homo sapiens (human)
carbohydrate biosynthetic processPoly [ADP-ribose] polymerase 1Homo sapiens (human)
protein autoprocessingPoly [ADP-ribose] polymerase 1Homo sapiens (human)
signal transduction involved in regulation of gene expressionPoly [ADP-ribose] polymerase 1Homo sapiens (human)
macrophage differentiationPoly [ADP-ribose] polymerase 1Homo sapiens (human)
DNA ADP-ribosylationPoly [ADP-ribose] polymerase 1Homo sapiens (human)
positive regulation of DNA-templated transcription, elongationPoly [ADP-ribose] polymerase 1Homo sapiens (human)
cellular response to insulin stimulusPoly [ADP-ribose] polymerase 1Homo sapiens (human)
positive regulation of intracellular estrogen receptor signaling pathwayPoly [ADP-ribose] polymerase 1Homo sapiens (human)
negative regulation of transcription elongation by RNA polymerase IIPoly [ADP-ribose] polymerase 1Homo sapiens (human)
cellular response to UVPoly [ADP-ribose] polymerase 1Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionPoly [ADP-ribose] polymerase 1Homo sapiens (human)
innate immune responsePoly [ADP-ribose] polymerase 1Homo sapiens (human)
regulation of circadian sleep/wake cycle, non-REM sleepPoly [ADP-ribose] polymerase 1Homo sapiens (human)
negative regulation of innate immune responsePoly [ADP-ribose] polymerase 1Homo sapiens (human)
negative regulation of DNA-templated transcriptionPoly [ADP-ribose] polymerase 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIPoly [ADP-ribose] polymerase 1Homo sapiens (human)
decidualizationPoly [ADP-ribose] polymerase 1Homo sapiens (human)
regulation of catalytic activityPoly [ADP-ribose] polymerase 1Homo sapiens (human)
positive regulation of mitochondrial depolarizationPoly [ADP-ribose] polymerase 1Homo sapiens (human)
positive regulation of SMAD protein signal transductionPoly [ADP-ribose] polymerase 1Homo sapiens (human)
positive regulation of necroptotic processPoly [ADP-ribose] polymerase 1Homo sapiens (human)
protein poly-ADP-ribosylationPoly [ADP-ribose] polymerase 1Homo sapiens (human)
protein auto-ADP-ribosylationPoly [ADP-ribose] polymerase 1Homo sapiens (human)
protein localization to chromatinPoly [ADP-ribose] polymerase 1Homo sapiens (human)
cellular response to zinc ionPoly [ADP-ribose] polymerase 1Homo sapiens (human)
replication fork reversalPoly [ADP-ribose] polymerase 1Homo sapiens (human)
negative regulation of cGAS/STING signaling pathwayPoly [ADP-ribose] polymerase 1Homo sapiens (human)
positive regulation of protein localization to nucleusPoly [ADP-ribose] polymerase 1Homo sapiens (human)
regulation of oxidative stress-induced neuron intrinsic apoptotic signaling pathwayPoly [ADP-ribose] polymerase 1Homo sapiens (human)
positive regulation of single strand break repairPoly [ADP-ribose] polymerase 1Homo sapiens (human)
response to aldosteronePoly [ADP-ribose] polymerase 1Homo sapiens (human)
negative regulation of adipose tissue developmentPoly [ADP-ribose] polymerase 1Homo sapiens (human)
negative regulation of telomere maintenance via telomere lengtheningPoly [ADP-ribose] polymerase 1Homo sapiens (human)
cellular response to amyloid-betaPoly [ADP-ribose] polymerase 1Homo sapiens (human)
positive regulation of myofibroblast differentiationPoly [ADP-ribose] polymerase 1Homo sapiens (human)
regulation of base-excision repairPoly [ADP-ribose] polymerase 1Homo sapiens (human)
positive regulation of double-strand break repair via homologous recombinationPoly [ADP-ribose] polymerase 1Homo sapiens (human)
cellular response to nerve growth factor stimulusPoly [ADP-ribose] polymerase 1Homo sapiens (human)
ATP generation from poly-ADP-D-ribosePoly [ADP-ribose] polymerase 1Homo sapiens (human)
negative regulation of ATP biosynthetic processPoly [ADP-ribose] polymerase 1Homo sapiens (human)
monoamine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent noradrenaline transporter Homo sapiens (human)
chemical synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent noradrenaline transporter Homo sapiens (human)
response to painSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent noradrenaline transporter Homo sapiens (human)
neuron cellular homeostasisSodium-dependent noradrenaline transporter Homo sapiens (human)
amino acid transportSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent noradrenaline transporter Homo 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)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3AHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
monoamine transportSodium-dependent dopamine transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent dopamine transporter Homo sapiens (human)
lactationSodium-dependent dopamine transporter Homo sapiens (human)
sensory perception of smellSodium-dependent dopamine transporter Homo sapiens (human)
locomotory behaviorSodium-dependent dopamine transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent dopamine transporter Homo sapiens (human)
response to iron ionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine transportSodium-dependent dopamine transporter Homo sapiens (human)
adenohypophysis developmentSodium-dependent dopamine transporter Homo sapiens (human)
response to nicotineSodium-dependent dopamine transporter Homo sapiens (human)
positive regulation of multicellular organism growthSodium-dependent dopamine transporter Homo sapiens (human)
regulation of dopamine metabolic processSodium-dependent dopamine transporter Homo sapiens (human)
response to cocaineSodium-dependent dopamine transporter Homo sapiens (human)
dopamine biosynthetic processSodium-dependent dopamine transporter Homo sapiens (human)
dopamine catabolic processSodium-dependent dopamine transporter Homo sapiens (human)
response to ethanolSodium-dependent dopamine transporter Homo sapiens (human)
cognitionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent dopamine transporter Homo sapiens (human)
response to cAMPSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent dopamine transporter Homo sapiens (human)
prepulse inhibitionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine uptakeSodium-dependent dopamine transporter Homo sapiens (human)
hyaloid vascular plexus regressionSodium-dependent dopamine transporter Homo sapiens (human)
amino acid transportSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine transportSodium-dependent dopamine transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent dopamine transporter Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
neurotransmitter secretionHistamine H3 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H3 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H3 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H3 receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (65)

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)
DNA bindingPoly [ADP-ribose] polymerase 1Homo sapiens (human)
chromatin bindingPoly [ADP-ribose] polymerase 1Homo sapiens (human)
damaged DNA bindingPoly [ADP-ribose] polymerase 1Homo sapiens (human)
RNA bindingPoly [ADP-ribose] polymerase 1Homo sapiens (human)
NAD+ ADP-ribosyltransferase activityPoly [ADP-ribose] polymerase 1Homo sapiens (human)
protein bindingPoly [ADP-ribose] polymerase 1Homo sapiens (human)
zinc ion bindingPoly [ADP-ribose] polymerase 1Homo sapiens (human)
nucleotidyltransferase activityPoly [ADP-ribose] polymerase 1Homo sapiens (human)
enzyme bindingPoly [ADP-ribose] polymerase 1Homo sapiens (human)
protein kinase bindingPoly [ADP-ribose] polymerase 1Homo sapiens (human)
nuclear estrogen receptor bindingPoly [ADP-ribose] polymerase 1Homo sapiens (human)
nucleosome bindingPoly [ADP-ribose] polymerase 1Homo sapiens (human)
ubiquitin protein ligase bindingPoly [ADP-ribose] polymerase 1Homo sapiens (human)
identical protein bindingPoly [ADP-ribose] polymerase 1Homo sapiens (human)
protein homodimerization activityPoly [ADP-ribose] polymerase 1Homo sapiens (human)
histone deacetylase bindingPoly [ADP-ribose] polymerase 1Homo sapiens (human)
NAD bindingPoly [ADP-ribose] polymerase 1Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingPoly [ADP-ribose] polymerase 1Homo sapiens (human)
R-SMAD bindingPoly [ADP-ribose] polymerase 1Homo sapiens (human)
NAD DNA ADP-ribosyltransferase activityPoly [ADP-ribose] polymerase 1Homo sapiens (human)
transcription regulator activator activityPoly [ADP-ribose] polymerase 1Homo sapiens (human)
NAD+-protein-serine ADP-ribosyltransferase activityPoly [ADP-ribose] polymerase 1Homo sapiens (human)
NAD+- protein-aspartate ADP-ribosyltransferase activityPoly [ADP-ribose] polymerase 1Homo sapiens (human)
NAD+-protein-glutamate ADP-ribosyltransferase activityPoly [ADP-ribose] polymerase 1Homo sapiens (human)
NAD+-protein-tyrosine ADP-ribosyltransferase activityPoly [ADP-ribose] polymerase 1Homo sapiens (human)
NAD+-protein-histidine ADP-ribosyltransferase activityPoly [ADP-ribose] polymerase 1Homo sapiens (human)
NAD+-histone H2BS6 serine ADP-ribosyltransferase activityPoly [ADP-ribose] polymerase 1Homo sapiens (human)
NAD+-histone H3S10 serine ADP-ribosyltransferase activityPoly [ADP-ribose] polymerase 1Homo sapiens (human)
NAD+-histone H2BE35 glutamate ADP-ribosyltransferase activityPoly [ADP-ribose] polymerase 1Homo sapiens (human)
NAD+-protein ADP-ribosyltransferase activityPoly [ADP-ribose] polymerase 1Homo sapiens (human)
actin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
protein bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
alpha-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
metal ion bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
beta-tubulin bindingSodium-dependent noradrenaline transporter Homo 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 binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3AHomo sapiens (human)
protease bindingSodium-dependent dopamine transporter Homo sapiens (human)
signaling receptor bindingSodium-dependent dopamine transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent dopamine transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent dopamine transporter Homo sapiens (human)
protein bindingSodium-dependent dopamine transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent dopamine transporter Homo sapiens (human)
dopamine bindingSodium-dependent dopamine transporter Homo sapiens (human)
amine bindingSodium-dependent dopamine transporter Homo sapiens (human)
protein-containing complex bindingSodium-dependent dopamine transporter Homo sapiens (human)
metal ion bindingSodium-dependent dopamine transporter Homo sapiens (human)
protein phosphatase 2A bindingSodium-dependent dopamine transporter Homo sapiens (human)
heterocyclic compound bindingSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent dopamine transporter Homo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
histamine receptor activityHistamine H3 receptorHomo sapiens (human)
G protein-coupled acetylcholine receptor activityHistamine H3 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (46)

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)
nucleusPoly [ADP-ribose] polymerase 1Homo sapiens (human)
cytosolPoly [ADP-ribose] polymerase 1Homo sapiens (human)
site of double-strand breakPoly [ADP-ribose] polymerase 1Homo sapiens (human)
nuclear replication forkPoly [ADP-ribose] polymerase 1Homo sapiens (human)
site of DNA damagePoly [ADP-ribose] polymerase 1Homo sapiens (human)
chromosome, telomeric regionPoly [ADP-ribose] polymerase 1Homo sapiens (human)
nucleusPoly [ADP-ribose] polymerase 1Homo sapiens (human)
nuclear envelopePoly [ADP-ribose] polymerase 1Homo sapiens (human)
nucleoplasmPoly [ADP-ribose] polymerase 1Homo sapiens (human)
nucleolusPoly [ADP-ribose] polymerase 1Homo sapiens (human)
mitochondrionPoly [ADP-ribose] polymerase 1Homo sapiens (human)
membranePoly [ADP-ribose] polymerase 1Homo sapiens (human)
nuclear bodyPoly [ADP-ribose] polymerase 1Homo sapiens (human)
site of double-strand breakPoly [ADP-ribose] polymerase 1Homo sapiens (human)
site of DNA damagePoly [ADP-ribose] polymerase 1Homo sapiens (human)
chromatinPoly [ADP-ribose] polymerase 1Homo sapiens (human)
transcription regulator complexPoly [ADP-ribose] polymerase 1Homo sapiens (human)
protein-containing complexPoly [ADP-ribose] polymerase 1Homo sapiens (human)
protein-DNA complexPoly [ADP-ribose] polymerase 1Homo sapiens (human)
nucleolusPoly [ADP-ribose] polymerase 1Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
cell surfaceSodium-dependent noradrenaline transporter Homo sapiens (human)
membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
presynaptic membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
axonSodium-dependent noradrenaline transporter Homo 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)
plasma membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
cleavage furrow5-hydroxytryptamine receptor 3AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3AHomo sapiens (human)
cytoplasmSodium-dependent dopamine transporter Homo sapiens (human)
plasma membraneSodium-dependent dopamine transporter Homo sapiens (human)
cell surfaceSodium-dependent dopamine transporter Homo sapiens (human)
membraneSodium-dependent dopamine transporter Homo sapiens (human)
axonSodium-dependent dopamine transporter Homo sapiens (human)
neuron projectionSodium-dependent dopamine transporter Homo sapiens (human)
neuronal cell bodySodium-dependent dopamine transporter Homo sapiens (human)
axon terminusSodium-dependent dopamine transporter Homo sapiens (human)
membrane raftSodium-dependent dopamine transporter Homo sapiens (human)
postsynaptic membraneSodium-dependent dopamine transporter Homo sapiens (human)
dopaminergic synapseSodium-dependent dopamine transporter Homo sapiens (human)
flotillin complexSodium-dependent dopamine transporter Homo sapiens (human)
axonSodium-dependent dopamine transporter Homo sapiens (human)
presynaptic membraneSodium-dependent dopamine transporter Homo sapiens (human)
plasma membraneSodium-dependent dopamine transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent dopamine transporter Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membraneHistamine H3 receptorHomo sapiens (human)
presynapseHistamine H3 receptorHomo sapiens (human)
plasma membraneHistamine H3 receptorHomo sapiens (human)
synapseHistamine H3 receptorHomo sapiens (human)
dendriteHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (58)

Assay IDTitleYearJournalArticle
AID611805Inhibition of RAMH-induced dipsogenia in Long Evans rat administered as po 15 mins prior to RAMH challenge2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID648457Oral bioavailability in Sprague-Dawley rat at 10 mg/kg2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Optimization of 5-pyridazin-3-one phenoxypropylamines as potent, selective histamine H₃ receptor antagonists with potent cognition enhancing activity.
AID611542Inhibition of norepinephrine transporter 2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611540Inhibition of adrenergic alpha 1A receptor2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611527Antagonist activity at histamine H3 receptor in rat cortical membrane2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID630097Displacement of [3H]NAMH from human H3R expressed in CHO cells2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Synthesis and evaluation of pyridazinone-phenethylamine derivatives as selective and orally bioavailable histamine H3 receptor antagonists with robust wake-promoting activity.
AID611539Inhibition of muscarinic M2 receptor2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611531Antagonist activity against rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611633Aqueous solubility of the compound at pH 22011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611535Selectivity for human histamine H3 receptor over human H4 receptor2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611631Inhibition of recombinant human dopamine transporter2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611528Dissociation constant, pKa of the compound2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611536Inhibition of human histamine H1 receptor at 10 uM2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611806Toxicity in rat central nervous system assessed as changes in behavioral response at 10 to 300 mg/kg, po measured from 15 mins through 6 hrs by Irwin test2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611529Antagonist activity against human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611803Toxicity in monkey assessed as changes in respiratory function after 28 days2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID648452Clearance in Sprague-Dawley rat at 1 mg/kg, iv and 5 mg/kg, po2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Optimization of 5-pyridazin-3-one phenoxypropylamines as potent, selective histamine H₃ receptor antagonists with potent cognition enhancing activity.
AID1071994Displacement of [3H]NAMH from rat histamine H3 receptor transfected in CHO cells2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
Discovery of (1R,6S)-5-[4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one (R,S-4a): histamine H(3) receptor inverse agonist demonstrating potent cognitive enhancing and wake promoting activity.
AID611802Toxicity in monkey assessed as changes in cardiovascular function after 28 days2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611727Mutagenic activity in human peripheral blood lymphocytes by micronucleus test in absence metabolic activation2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611634Aqueous solubility of the compound at pH 7.42011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611804Inhibition of RAMH-induced dipsogenia in ip dosed Long Evans rat administered 15 mins prior to RAMH challenge2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611728Mutagenic activity in Salmonella Typhimurium by Ames test2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID1201926Binding affinity to human histamine H3 receptor2015European journal of medicinal chemistry, May-05, Volume: 953,4-Diaza-bicyclo[4.1.0]hept-4-en-2-one phenoxypropylamine analogs of irdabisant (CEP-26401) as potent histamine-3 receptor inverse agonists with robust wake-promoting activity.
AID611800Toxicity in rat up to 28 days2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611808Drug level in rat brain at 100 mg/kg, po administered after 1 hr post dosing2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611532Inverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611807Toxicity in rat central nervous system assessed as side effects up to 100 mg/kg, po measured from 15 mins through 6 hrs by Irwin test2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID648458Ratio of drug level in brain to plasma in Sprague-Dawley rat at 10 mg/kg, ip after 1 hr2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Optimization of 5-pyridazin-3-one phenoxypropylamines as potent, selective histamine H₃ receptor antagonists with potent cognition enhancing activity.
AID611537Inhibition of human histamine H2 receptor at 10 uM2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611534Selectivity for human histamine H3 receptor over human H2 receptor2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611517Displacement of [3H]NAMH from human histamine H3 receptor expressed in CHO cells2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611543Inhibition of PDE32011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID1071995Displacement of [3H]NAMH from human histamine H3 receptor transfected in CHO cells2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
Discovery of (1R,6S)-5-[4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one (R,S-4a): histamine H(3) receptor inverse agonist demonstrating potent cognitive enhancing and wake promoting activity.
AID611809Therapeutic index in rat dispogenia model2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611729Mutagenic activity in Salmonella Typhimurium by Ames test in presence of rat liver S9 fraction2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID1201927Binding affinity to rat histamine H3 receptor2015European journal of medicinal chemistry, May-05, Volume: 953,4-Diaza-bicyclo[4.1.0]hept-4-en-2-one phenoxypropylamine analogs of irdabisant (CEP-26401) as potent histamine-3 receptor inverse agonists with robust wake-promoting activity.
AID618581Displacement of [3H]NAMH from human cloned histamine 3 receptor expressed in CHO cells2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Identification of pyridazin-3-one derivatives as potent, selective histamine H₃ receptor inverse agonists with robust wake activity.
AID630098Displacement of [3H]NAMH from rat H3R expressed in CHO cells2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Synthesis and evaluation of pyridazinone-phenethylamine derivatives as selective and orally bioavailable histamine H3 receptor antagonists with robust wake-promoting activity.
AID648455Displacement of [3H]NAMH from human cloned 5HT3 receptor expressed in CHO cells2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Optimization of 5-pyridazin-3-one phenoxypropylamines as potent, selective histamine H₃ receptor antagonists with potent cognition enhancing activity.
AID611630Inhibition of human PARP12011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID622483Displacement of [3H]-NAMH from human histamine H3 receptor expressed in CHO cells2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Synthesis and structure-activity relationships of 4,5-fused pyridazinones as histamine H₃ receptor antagonists.
AID611538Inhibition of human histamine H4 receptor at 10 uM2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611801Toxicity in monkey up to 28 days2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611519Distribution coefficient log D of the compound at pH 7.42011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611632Inhibition of recombinant human norepinephrine transporter2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611635Apparent permeability across human Caco2 cell membrane2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611541Inhibition of dopamine transporter2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611533Selectivity for human histamine H3 receptor over human H1 receptor2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID648453Half life in Sprague-Dawley rat at 1 mg/kg, iv and 5 mg/kg, po2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Optimization of 5-pyridazin-3-one phenoxypropylamines as potent, selective histamine H₃ receptor antagonists with potent cognition enhancing activity.
AID648454Displacement of [3H]NAMH from rat cloned 5HT3 receptor expressed in CHO cells2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Optimization of 5-pyridazin-3-one phenoxypropylamines as potent, selective histamine H₃ receptor antagonists with potent cognition enhancing activity.
AID622486Displacement of [3H]-NAMH from rat histamine H3 receptor expressed in CHO cells2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Synthesis and structure-activity relationships of 4,5-fused pyridazinones as histamine H₃ receptor antagonists.
AID611636Permeability across human Caco2 cells expressing P-gp assessed as directional transport2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID618582Displacement of [3H]NAMH from rat cloned histamine 3 receptor expressed in CHO cells2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Identification of pyridazin-3-one derivatives as potent, selective histamine H₃ receptor inverse agonists with robust wake activity.
AID611530Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611518Displacement of [3H]NAMH from rat histamine H3 receptor expressed in CHO cells2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611725Inhibition of recombinant human ERG channel expressed in human HEK 293 cells by patch clamp assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
AID611726Mutagenic activity in human peripheral blood lymphocytes by micronucleus test in presence metabolic activation2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
[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's0 (0.00)29.6817
2010's7 (100.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 20.06

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 Index20.06 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (20.06)

All Compounds (24.57)

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]