Page last updated: 2024-11-08

zeneca zd 6169

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

Description

Zeneca ZD 6169: an ATP-sensitive potassium channel opener; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID177852
CHEMBL ID18861
SCHEMBL ID4261046
MeSH IDM0250228

Synonyms (13)

Synonym
zd-6169
zd 6169
zeneca zd 6169
zd6169
CHEMBL18861
(2s)-n-(4-benzoylphenyl)-3,3,3-trifluoro-2-hydroxy-2-methylpropanamide
147696-46-6
h6uio70f5e ,
unii-h6uio70f5e
bdbm86249
(s)-(-)-n-(4-benzoylphenyl)-3,3,3-trifluoro-2-hydroxy-2-methylpropanamide
SCHEMBL4261046
propanamide, n-(4-benzoylphenyl)-3,3,3-trifluoro-2-hydroxy-2-methyl-, (2s)-

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Bladder activity and selectivity after oral dosing were studied in conscious, normotensive rats and dogs by monitoring cystometric and cardiovascular (CV) parameters."( ZENECA ZD6169: a novel KATP channel opener with in vivo selectivity for urinary bladder.
Do, ML; Empfield, JR; Halterman, TJ; Howe, BB; Ohnmacht, CJ; Pettinger, SJ; Russell, K; Stow, RB; Trainor, DA; Yochim, CL, 1995
)
0.29
" The bell-shaped dose-response relationship for ZD6169 activation of I(K(ATP)) has also been seen in bladder myocytes, albeit at a lower concentration, and it has been proposed to contribute to the reported lack of in vivo cardiovascular side effects."( The effects of ZD6169 on the ATP-dependent K(+) current (I(K)(ATP)) in isolated cat ventricular myocytes.
Jow, B; Numann, R, 1999
)
0.3
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (9)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 9Homo sapiens (human)IC50 (µMol)1.60000.22001.56004.3000AID78294
Bile salt export pumpHomo sapiens (human)IC50 (µMol)21.39000.11007.190310.0000AID1449628
ATP-binding cassette sub-family C member 8Homo sapiens (human)IC50 (µMol)1.60000.00431.07038.2000AID78294
ATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)IC50 (µMol)1.60000.00431.36868.2000AID78294
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrialHomo sapiens (human)IC50 (µMol)9.30000.00051.89099.5000AID162832
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)IC50 (µMol)9.30000.06503.12999.5000AID162832
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrialHomo sapiens (human)IC50 (µMol)9.30000.02603.56669.5000AID162832
ATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)IC50 (µMol)1.60000.47000.88001.6000AID78294
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrialHomo sapiens (human)IC50 (µMol)9.30000.02103.58609.5000AID162832
[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)
ATP-binding cassette sub-family C member 9Homo sapiens (human)EC50 (µMol)1.34330.02190.70193.5400AID159674; AID272328; AID272330; AID272331; AID93974; AID93977; AID93984; AID95329
ATP-binding cassette sub-family C member 8Homo sapiens (human)EC50 (µMol)1.48760.02191.12578.8000AID159674; AID93974; AID93977; AID93984
ATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)EC50 (µMol)1.24260.02190.97088.8000AID159674; AID272328; AID272330; AID272331; AID303727; AID93974; AID93977; AID93984; AID95329
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrialHomo sapiens (human)EC50 (µMol)8.30008.30008.30008.3000AID162830
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)EC50 (µMol)8.30000.08004.19008.3000AID162830
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrialHomo sapiens (human)EC50 (µMol)8.30008.30008.30008.3000AID162830
ATP-sensitive inward rectifier potassium channel 8Homo sapiens (human)EC50 (µMol)1.48760.02190.54852.7542AID159674; AID93974; AID93977; AID93984
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrialHomo sapiens (human)EC50 (µMol)8.30008.30008.30008.3000AID162830
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (128)

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)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo 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)
glucose metabolic process[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrialHomo sapiens (human)
cell population proliferation[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrialHomo sapiens (human)
intrinsic apoptotic signaling pathway in response to oxidative stress[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrialHomo sapiens (human)
regulation of acetyl-CoA biosynthetic process from pyruvate[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrialHomo sapiens (human)
regulation of glucose metabolic process[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrialHomo sapiens (human)
hypoxia-inducible factor-1alpha signaling pathway[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrialHomo sapiens (human)
protein phosphorylation[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrialHomo sapiens (human)
glucose metabolic process[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
regulation of gluconeogenesis[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
regulation of pH[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
insulin receptor signaling pathway[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
regulation of acetyl-CoA biosynthetic process from pyruvate[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
regulation of cellular ketone metabolic process[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
regulation of glucose metabolic process[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
cellular response to nutrient[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
cellular response to reactive oxygen species[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
glucose homeostasis[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
regulation of calcium-mediated signaling[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediator[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
protein phosphorylation[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
regulation of acetyl-CoA biosynthetic process from pyruvate[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrialHomo sapiens (human)
regulation of glucose metabolic process[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrialHomo sapiens (human)
peptidyl-serine phosphorylation[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrialHomo sapiens (human)
peroxisome proliferator activated receptor signaling pathway[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrialHomo sapiens (human)
cellular response to fatty acid[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrialHomo sapiens (human)
hypoxia-inducible factor-1alpha signaling pathway[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrialHomo sapiens (human)
regulation of reactive oxygen species metabolic process[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrialHomo sapiens (human)
protein phosphorylation[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrialHomo 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)
regulation of pH[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrialHomo sapiens (human)
insulin receptor signaling pathway[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrialHomo sapiens (human)
cellular response to starvation[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrialHomo sapiens (human)
regulation of acetyl-CoA biosynthetic process from pyruvate[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrialHomo sapiens (human)
regulation of cellular ketone metabolic process[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrialHomo sapiens (human)
regulation of glucose metabolic process[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrialHomo sapiens (human)
regulation of fatty acid biosynthetic process[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrialHomo sapiens (human)
glucose homeostasis[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrialHomo sapiens (human)
response to starvation[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrialHomo sapiens (human)
regulation of bone resorption[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrialHomo sapiens (human)
regulation of fatty acid oxidation[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrialHomo sapiens (human)
cellular response to fatty acid[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrialHomo sapiens (human)
reactive oxygen species metabolic process[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrialHomo sapiens (human)
negative regulation of anoikis[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrialHomo sapiens (human)
protein phosphorylation[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrialHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (32)

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)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo 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)
protein kinase activity[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrialHomo sapiens (human)
pyruvate dehydrogenase (acetyl-transferring) kinase activity[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrialHomo sapiens (human)
protein binding[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrialHomo sapiens (human)
ATP binding[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrialHomo sapiens (human)
protein kinase activity[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
pyruvate dehydrogenase (acetyl-transferring) kinase activity[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
protein binding[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
ATP binding[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
protein homodimerization activity[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
protein kinase activity[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrialHomo sapiens (human)
protein serine/threonine kinase activity[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrialHomo sapiens (human)
pyruvate dehydrogenase (acetyl-transferring) kinase activity[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrialHomo sapiens (human)
protein binding[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrialHomo sapiens (human)
ATP binding[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrialHomo 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)
protein kinase activity[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrialHomo sapiens (human)
pyruvate dehydrogenase (acetyl-transferring) kinase activity[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrialHomo sapiens (human)
protein binding[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrialHomo sapiens (human)
ATP binding[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrialHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (35)

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)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo 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)
mitochondrial matrix[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrialHomo sapiens (human)
mitochondrion[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrialHomo sapiens (human)
nucleoplasm[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
mitochondrion[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
mitochondrial matrix[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
cytosol[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
pyruvate dehydrogenase complex[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
mitochondrion[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)
nucleolus[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrialHomo sapiens (human)
mitochondrion[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrialHomo sapiens (human)
mitochondrial matrix[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrialHomo sapiens (human)
mitochondrion[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrialHomo 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)
mitochondrial matrix[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrialHomo sapiens (human)
mitochondrion[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrialHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (34)

Assay IDTitleYearJournalArticle
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.
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.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID162961In vivo inhibition of pyruvate dehydrogenase kinase, reduced lactate level in normal 24 hr r fasted rats at 300 umol/kg oral dose; Not active1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
(R)-3,3,3-Trifluoro-2-hydroxy-2-methylpropionamides are orally active inhibitors of pyruvate dehydrogenase kinase.
AID159674In vitro functional potassium channel opening activity in tissue strips from Landrace pig bladders(LPD)2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Design and synthesis of novel cyanoguanidine ATP-sensitive potassium channel openers for the treatment of overactive bladder.
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.
AID303736Half life in dog at 10 nmol/kg, iv2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Structure-activity studies of novel cyanoguanidine ATP-sensitive potassium channel openers for the treatment of overactive bladder.
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.
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)
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.
AID303744Oral bioavailability in dog at 10 nmol/kg, po2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Structure-activity studies of novel cyanoguanidine ATP-sensitive potassium channel openers for the treatment of overactive bladder.
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.
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.
AID303740Tmax in dog at 10 nmol/kg, po2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Structure-activity studies of novel cyanoguanidine ATP-sensitive potassium channel openers for the treatment of overactive bladder.
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.
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.
AID162830In vivo inhibion of pyruvate dehydrogenase kinase, increased oxidation of lactate1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
(R)-3,3,3-Trifluoro-2-hydroxy-2-methylpropionamides are orally active inhibitors of pyruvate dehydrogenase kinase.
AID303727Channel opening activity at human bladder Kir6.2 channel containing SUR2B expressed in L cells by FLIPR assay2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Structure-activity studies of novel cyanoguanidine ATP-sensitive potassium channel openers for the treatment of overactive bladder.
AID303738Plasma clearance in dog at 10 nmol/kg, iv2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Structure-activity studies of novel cyanoguanidine ATP-sensitive potassium channel openers for the treatment of overactive bladder.
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.
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.
AID95329In vitro ATP-sensitive potassium channel (KATP) activity in cells expressing human KATP channels Kir6.2 and sulfonylurea receptor 2B2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Design and synthesis of novel cyanoguanidine ATP-sensitive potassium channel openers for the treatment of overactive bladder.
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)
AID303742Half life in dog at 10 nmol/kg, po2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Structure-activity studies of novel cyanoguanidine ATP-sensitive potassium channel openers for the treatment of overactive bladder.
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.
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)
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.
AID162832In vitro inhibitory activity against Pyruvate dehydrogenase kinase by primary enzymatic assay1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
(R)-3,3,3-Trifluoro-2-hydroxy-2-methylpropionamides are orally active inhibitors of pyruvate dehydrogenase kinase.
AID78294IC50 evaluated by measuring contraction and relaxation of guinea pig bladder strips with KCl and glibenclamide respectively1996Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23
N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropanamides: KATP potassium channel openers. Modifications on the western region.
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.
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.
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.
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)
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (41)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's14 (34.15)18.2507
2000's24 (58.54)29.6817
2010's3 (7.32)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: 10.55

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 Index10.55 (24.57)
Research Supply Index3.76 (2.92)
Research Growth Index4.31 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.55)

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%
Other42 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]