Page last updated: 2024-11-11

way 133537

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 CID9883778
CHEMBL ID2062142
SCHEMBL ID4258934
MeSH IDM0305544

Synonyms (7)

Synonym
way-133537
CHEMBL2062142 ,
(+)-(r)-4-[3,4-dioxo-2-(1,2,2-trimethyl-propylamino)-cyclobut-1-enylamino]-3-ethylbenzonitrile
KDOHDKFUZYPGPN-LLVKDONJSA-N
SCHEMBL4258934
bdbm50475963
4-[[2-[[(2r)-3,3-dimethylbutan-2-yl]amino]-3,4-dioxocyclobuten-1-yl]amino]-3-ethylbenzonitrile
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 9Homo sapiens (human)EC50 (µMol)0.69200.02190.70193.5400AID272328; AID272330; AID272331; AID93974; AID93977; AID93984
ATP-binding cassette sub-family C member 8Homo sapiens (human)EC50 (µMol)0.34320.02191.12578.8000AID93974; AID93977; AID93984
ATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)EC50 (µMol)0.69200.02190.97088.8000AID272328; AID272330; AID272331; AID93974; AID93977; AID93984
ATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)EC50 (µMol)0.34320.02190.54852.7542AID93974; AID93977; AID93984
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (81)

Processvia Protein(s)Taxonomy
defense response to virusATP-binding cassette sub-family C member 9Homo sapiens (human)
action potentialATP-binding cassette sub-family C member 9Homo sapiens (human)
heart morphogenesisATP-binding cassette sub-family C member 9Homo sapiens (human)
response to xenobiotic stimulusATP-binding cassette sub-family C member 9Homo sapiens (human)
response to ATPATP-binding cassette sub-family C member 9Homo sapiens (human)
negative regulation of blood pressureATP-binding cassette sub-family C member 9Homo sapiens (human)
fibroblast proliferationATP-binding cassette sub-family C member 9Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 9Homo sapiens (human)
coronary vasculature developmentATP-binding cassette sub-family C member 9Homo sapiens (human)
cardiac conductionATP-binding cassette sub-family C member 9Homo sapiens (human)
potassium ion transmembrane transportATP-binding cassette sub-family C member 9Homo sapiens (human)
cardiac muscle cell contractionATP-binding cassette sub-family C member 9Homo sapiens (human)
monoatomic cation transmembrane transportATP-binding cassette sub-family C member 9Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 9Homo sapiens (human)
inorganic cation transmembrane transportATP-binding cassette sub-family C member 9Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 9Homo sapiens (human)
potassium ion import across plasma membraneATP-binding cassette sub-family C member 9Homo sapiens (human)
intracellular glucose homeostasisATP-binding cassette sub-family C member 8Homo sapiens (human)
potassium ion transportATP-binding cassette sub-family C member 8Homo sapiens (human)
female pregnancyATP-binding cassette sub-family C member 8Homo sapiens (human)
memoryATP-binding cassette sub-family C member 8Homo sapiens (human)
visual learningATP-binding cassette sub-family C member 8Homo sapiens (human)
response to pHATP-binding cassette sub-family C member 8Homo sapiens (human)
response to xenobiotic stimulusATP-binding cassette sub-family C member 8Homo sapiens (human)
response to zinc ionATP-binding cassette sub-family C member 8Homo sapiens (human)
negative regulation of low-density lipoprotein particle clearanceATP-binding cassette sub-family C member 8Homo sapiens (human)
negative regulation of angiogenesisATP-binding cassette sub-family C member 8Homo sapiens (human)
response to lipopolysaccharideATP-binding cassette sub-family C member 8Homo sapiens (human)
positive regulation of tumor necrosis factor productionATP-binding cassette sub-family C member 8Homo sapiens (human)
response to insulinATP-binding cassette sub-family C member 8Homo sapiens (human)
positive regulation of insulin secretion involved in cellular response to glucose stimulusATP-binding cassette sub-family C member 8Homo sapiens (human)
positive regulation of potassium ion transportATP-binding cassette sub-family C member 8Homo sapiens (human)
negative regulation of insulin secretionATP-binding cassette sub-family C member 8Homo sapiens (human)
neuromuscular processATP-binding cassette sub-family C member 8Homo sapiens (human)
negative regulation of glial cell proliferationATP-binding cassette sub-family C member 8Homo sapiens (human)
glutamate secretion, neurotransmissionATP-binding cassette sub-family C member 8Homo sapiens (human)
negative regulation of neuroblast migrationATP-binding cassette sub-family C member 8Homo sapiens (human)
cellular response to organic substanceATP-binding cassette sub-family C member 8Homo sapiens (human)
potassium ion transmembrane transportATP-binding cassette sub-family C member 8Homo sapiens (human)
inorganic cation transmembrane transportATP-binding cassette sub-family C member 8Homo sapiens (human)
positive regulation of uterine smooth muscle relaxationATP-binding cassette sub-family C member 8Homo sapiens (human)
positive regulation of tight junction disassemblyATP-binding cassette sub-family C member 8Homo sapiens (human)
negative regulation of blood-brain barrier permeabilityATP-binding cassette sub-family C member 8Homo sapiens (human)
potassium ion import across plasma membraneATP-binding cassette sub-family C member 8Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 8Homo sapiens (human)
action potentialATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to hypoxiaATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to ischemiaATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
ventricular cardiac muscle tissue developmentATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
glucose metabolic processATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
apoptotic processATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
determination of adult lifespanATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to xenobiotic stimulusATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to estradiolATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to ATPATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to testosteroneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
regulation of membrane potentialATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
negative regulation of insulin secretionATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
regulation of insulin secretionATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
nervous system processATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
CAMKK-AMPK signaling cascadeATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
cellular response to nicotineATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
cellular response to glucose stimulusATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
cellular response to tumor necrosis factorATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
potassium ion transmembrane transportATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
inorganic cation transmembrane transportATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
regulation of presynaptic membrane potentialATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
positive regulation of protein localization to plasma membraneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to resveratrolATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
potassium ion import across plasma membraneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
regulation of monoatomic ion transmembrane transportATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to hypoxiaATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
microglial cell activationATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
kidney developmentATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
regulation of heart rateATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
adaptive immune responseATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
response to ischemiaATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
heart morphogenesisATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
ventricular cardiac muscle tissue developmentATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
potassium ion transportATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
apoptotic processATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
regulation of blood pressureATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
determination of adult lifespanATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
protein secretionATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
response to xenobiotic stimulusATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
gene expressionATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
fatty acid transportATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
transmission of nerve impulseATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
establishment of cell polarityATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
response to lipopolysaccharideATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
response to insulinATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
response to ATPATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
response to cytokineATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
response to endoplasmic reticulum stressATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
p38MAPK cascadeATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
vasodilationATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
response to exogenous dsRNAATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
NLRP3 inflammasome complex assemblyATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
fat cell differentiationATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
fibroblast proliferationATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
neuromuscular processATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
synaptic assembly at neuromuscular junctionATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
defense response to virusATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
atrioventricular node cell differentiationATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
coronary vasculature developmentATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
glutamate secretion, neurotransmissionATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
CAMKK-AMPK signaling cascadeATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
calcium ion transmembrane transportATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
potassium ion transmembrane transportATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
inorganic cation transmembrane transportATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
regulation of presynaptic membrane potentialATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
reactive gliosisATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
transport across blood-brain barrierATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
response to resveratrolATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
potassium ion import across plasma membraneATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
regulation of monoatomic ion transmembrane transportATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (23)

Processvia Protein(s)Taxonomy
monoatomic cation channel activityATP-binding cassette sub-family C member 9Homo sapiens (human)
potassium channel activityATP-binding cassette sub-family C member 9Homo sapiens (human)
ATP-activated inward rectifier potassium channel activityATP-binding cassette sub-family C member 9Homo sapiens (human)
transmembrane transporter activityATP-binding cassette sub-family C member 9Homo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 9Homo sapiens (human)
sulfonylurea receptor activityATP-binding cassette sub-family C member 9Homo sapiens (human)
potassium channel regulator activityATP-binding cassette sub-family C member 9Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 9Homo sapiens (human)
ATPase-coupled monoatomic cation transmembrane transporter activityATP-binding cassette sub-family C member 9Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 9Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 9Homo sapiens (human)
transmembrane transporter bindingATP-binding cassette sub-family C member 9Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 9Homo sapiens (human)
ATP-activated inward rectifier potassium channel activityATP-binding cassette sub-family C member 8Homo sapiens (human)
potassium channel activityATP-binding cassette sub-family C member 8Homo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 8Homo sapiens (human)
sulfonylurea receptor activityATP-binding cassette sub-family C member 8Homo sapiens (human)
ATP-activated inward rectifier potassium channel activityATP-binding cassette sub-family C member 8Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 8Homo sapiens (human)
ATPase-coupled monoatomic cation transmembrane transporter activityATP-binding cassette sub-family C member 8Homo sapiens (human)
ADP bindingATP-binding cassette sub-family C member 8Homo sapiens (human)
transmembrane transporter bindingATP-binding cassette sub-family C member 8Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 8Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 8Homo sapiens (human)
voltage-gated potassium channel activityATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
protein bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
ATP bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
ATP-activated inward rectifier potassium channel activityATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
ATPase-coupled monoatomic cation transmembrane transporter activityATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
ankyrin bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
potassium ion bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
heat shock protein bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
transmembrane transporter bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
voltage-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
inward rectifier potassium channel activityATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
protein bindingATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
ATP bindingATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
ATP-activated inward rectifier potassium channel activityATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
sulfonylurea receptor bindingATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
ATPase-coupled monoatomic cation transmembrane transporter activityATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
voltage-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (20)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 9Homo sapiens (human)
sarcomereATP-binding cassette sub-family C member 9Homo sapiens (human)
inward rectifying potassium channelATP-binding cassette sub-family C member 9Homo sapiens (human)
potassium ion-transporting ATPase complexATP-binding cassette sub-family C member 9Homo sapiens (human)
membraneATP-binding cassette sub-family C member 9Homo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 8Homo sapiens (human)
inward rectifying potassium channelATP-binding cassette sub-family C member 8Homo sapiens (human)
synaptic vesicle membraneATP-binding cassette sub-family C member 8Homo sapiens (human)
sarcolemmaATP-binding cassette sub-family C member 8Homo sapiens (human)
potassium ion-transporting ATPase complexATP-binding cassette sub-family C member 8Homo sapiens (human)
membraneATP-binding cassette sub-family C member 8Homo sapiens (human)
acrosomal vesicleATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
nuclear envelopeATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
endosomeATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
plasma membraneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
inward rectifying potassium channelATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
intercalated discATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
T-tubuleATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
axolemmaATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
presynaptic membraneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
neuronal cell bodyATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
cell body fiberATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
glutamatergic synapseATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
plasma membraneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
plasma membraneATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
myofibrilATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
sarcolemmaATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
presynaptic active zone membraneATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
glutamatergic synapseATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
voltage-gated potassium channel complexATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
inward rectifying potassium channelATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
potassium ion-transporting ATPase complexATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
plasma membraneATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (24)

Assay IDTitleYearJournalArticle
AID272346Activity against pig bladder KATP channel opening assessed as ability to relax field-stimulated pig detrusor relative to P10752006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Effects of substitution on 9-(3-bromo-4-fluorophenyl)-5,9-dihydro-3H,4H-2,6-dioxa-4- azacyclopenta[b]naphthalene-1,8-dione, a dihydropyridine ATP-sensitive potassium channel opener.
AID272331Activity against pig bladder KATP channel opening assessed as ability to relax spontaneous bladder contraction2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Effects of substitution on 9-(3-bromo-4-fluorophenyl)-5,9-dihydro-3H,4H-2,6-dioxa-4- azacyclopenta[b]naphthalene-1,8-dione, a dihydropyridine ATP-sensitive potassium channel opener.
AID1915504Inhibition of KCL-induced contraction in rat urinary bladder2021European journal of medicinal chemistry, Jan-01, Volume: 209Squaric acid analogues in medicinal chemistry.
AID179773In vitro inhibitory concentration that relaxed KCL induced contraction in rat detrusor strip by 50%2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Design and SAR of novel potassium channel openers targeted for urge urinary incontinence. 2. Selective and potent benzylamino cyclobutenediones.
AID272330Activity against pig bladder KATP channel opening assessed as ability to relax field-stimulated pig detrusor2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Effects of substitution on 9-(3-bromo-4-fluorophenyl)-5,9-dihydro-3H,4H-2,6-dioxa-4- azacyclopenta[b]naphthalene-1,8-dione, a dihydropyridine ATP-sensitive potassium channel opener.
AID233874Selectivity expressed as the ratio of pEC50 (SLPD) and pEC50 (FSLPD)2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity relationships of a novel series of 2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide K(ATP) channel openers: discovery of (-)-(9S)-9-(3-bromo-4-fluorophenyl)-2,3,5,6,7,9- hexahydrothieno[3,2-b]quinolin-8(4H)
AID93977Evaluated for K-ATP activity in terms of stable twitch response through field-stimulated landrace pig detrusor assay2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity relationships of a novel series of 2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide K(ATP) channel openers: discovery of (-)-(9S)-9-(3-bromo-4-fluorophenyl)-2,3,5,6,7,9- hexahydrothieno[3,2-b]quinolin-8(4H)
AID93984Evaluated for K-ATP activity as in vitro bladder relaxation in spontaneous Landrace pig detrusor strips (SLPD)2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity relationships of a novel series of 2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide K(ATP) channel openers: discovery of (-)-(9S)-9-(3-bromo-4-fluorophenyl)-2,3,5,6,7,9- hexahydrothieno[3,2-b]quinolin-8(4H)
AID179774In vitro inhibitory concentration that relaxes KCL induced contraction in rat detrusor strips by 50%2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Design and SAR of novel potassium channel openers targeted for urge urinary incontinence. 1. N-Cyanoguanidine bioisosteres possessing in vivo bladder selectivity.
AID178736Effective dose in vivo for reduction in the frequency of spontaneous bladder contractions in the rat oral administration2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Design and SAR of novel potassium channel openers targeted for urge urinary incontinence. 1. N-Cyanoguanidine bioisosteres possessing in vivo bladder selectivity.
AID173812Effective dose in vivo for reduction in MAP in normotensive rat model after oral administration2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Design and SAR of novel potassium channel openers targeted for urge urinary incontinence. 1. N-Cyanoguanidine bioisosteres possessing in vivo bladder selectivity.
AID179771In vitro inhibitory concentration for 50% relaxant effect was measured on rat bladder strips2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Recent developments in the biology and medicinal chemistry of potassium channel modulators: update from a decade of progress.
AID233282Selectivity ratio for the reduction of mean arterial pressure to that of unstable concentration in anesthetized obstructed male rat2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Structure-activity relationship of a novel class of naphthyl amide KATP channel openers.
AID711541Oral bioavailability in rat2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synopsis of some recent tactical application of bioisosteres in drug design.
AID177812Compound was evaluated in vivo for the effective dose that cause a 50% reduction in frequency of spontaneous bladder contraction in the rat hypertrophied model after oral administration2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Design and SAR of novel potassium channel openers targeted for urge urinary incontinence. 2. Selective and potent benzylamino cyclobutenediones.
AID173807Compound was evaluated in vivo for the effective dose that cause a 20% drop in MAP normotensive rat after oral administration2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Design and SAR of novel potassium channel openers targeted for urge urinary incontinence. 2. Selective and potent benzylamino cyclobutenediones.
AID272347Activity against pig bladder KATP channel opening assessed as ability to relax spontaneous bladder contraction relative to P10752006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Effects of substitution on 9-(3-bromo-4-fluorophenyl)-5,9-dihydro-3H,4H-2,6-dioxa-4- azacyclopenta[b]naphthalene-1,8-dione, a dihydropyridine ATP-sensitive potassium channel opener.
AID232708Selectivity ratio of MAP ED20/bladder ED502000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Design and SAR of novel potassium channel openers targeted for urge urinary incontinence. 1. N-Cyanoguanidine bioisosteres possessing in vivo bladder selectivity.
AID93974Evaluated for K-ATP activity in terms of change in membrane potential through guinea pig bladder assay2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity relationships of a novel series of 2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide K(ATP) channel openers: discovery of (-)-(9S)-9-(3-bromo-4-fluorophenyl)-2,3,5,6,7,9- hexahydrothieno[3,2-b]quinolin-8(4H)
AID173597In vivo concentration required for the reduction of mean arterial pressure in anesthetized obstructed male rat, administered intravenously at a dose of 50 nM/Kg2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Structure-activity relationship of a novel class of naphthyl amide KATP channel openers.
AID232709Selectivity ratio of MAP ED20/bladder ED502000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Design and SAR of novel potassium channel openers targeted for urge urinary incontinence. 2. Selective and potent benzylamino cyclobutenediones.
AID177220In vivo concentration required for the inhibition of unstable contraction in anesthetized obstructed male rat, administered intravenously at a dose of 30 nM/Kg2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Structure-activity relationship of a novel class of naphthyl amide KATP channel openers.
AID272329Ability to open human urinary bladder Kir6.2 containing SUR2B in Ltk cells by FLIPR assay relative to P10752006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Effects of substitution on 9-(3-bromo-4-fluorophenyl)-5,9-dihydro-3H,4H-2,6-dioxa-4- azacyclopenta[b]naphthalene-1,8-dione, a dihydropyridine ATP-sensitive potassium channel opener.
AID272328Ability to open human urinary bladder Kir6.2 channel containing SUR2B in Ltk cells by FLIPR assay2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Effects of substitution on 9-(3-bromo-4-fluorophenyl)-5,9-dihydro-3H,4H-2,6-dioxa-4- azacyclopenta[b]naphthalene-1,8-dione, a dihydropyridine ATP-sensitive potassium channel opener.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's6 (75.00)29.6817
2010's1 (12.50)24.3611
2020's1 (12.50)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.59

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.59 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.78 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.59)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (25.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (75.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]