Page last updated: 2024-12-08

bms204352

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Description

BMS204352: a calcium-sensitive opener of maxi-K potassium channels; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID214350
CHEMBL ID266510
SCHEMBL ID4877314
MeSH IDM0385217

Synonyms (37)

Synonym
gtpl2307
maxipost
D04192
bms-204352
2h-indol-2-one, 3-(5-chloro-2-methoxyphenyl)-3-fluoro-1,3-dihydro-6-(trifluoromethyl)-, (3s)-
flindokalner [usan:inn]
(3s)-3-(5-chloro-2-methoxyphenyl)-3-fluoro-6-(trifluoromethyl)-1,3-dihydro-2h-indol-2-one
flindokalner
bms 204352
187523-35-9
bms204352
CHEMBL266510
bms-204352-01
(3s)-3-(5-chloro-2-methoxyphenyl)-3-fluoro-6-(trifluoromethyl)-1h-indol-2-one
unii-j57o328w4w
j57o328w4w ,
(+)-maxipost
2h-indol-2-one,3-(5-chloro-2-methoxyphenyl)-3-fluoro-1,3-dihydro-6-(trifluoromethyl)-, (3s)-
flindokalner [usan]
flindokalner [inn]
bdbm50426567
SCHEMBL4877314
(s)-ii
(s)-3-(5-chloro-2-methoxy-phenyl)-3-fluoro-6-trifluoromethyl-1,3-dihydro-indol-2-one
(s)-3-(5-chloro-2-methoxyphenyl)-3-fluoro-6-(trifluoromethyl)-indolin-2-one
(3s)-3-(5-chloro-2-methoxyphenyl)-3-fluoro-1,3-dihydro-6-(trifluoromethyl)-2h-indol-2-one
(s)-(+)-bms 204352
AKOS024458430
bms 204352, >=98% (hplc)
(s)-3-(5-chloro-2-methoxyphenyl)-3-fluoro-6-(trifluoromethyl)indolin-2-one
DTXSID70870176
CS-0029243
HY-108584
Q27077683
SB19641
MS-25672
E98786

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic analysis was performed using a non-compartmental method."( Pharmacokinetics and dose proportionality of BMS-204352 after intravenous administration to dogs.
Krishna, R; Mantha, S; Shah, VR; Srinivas, N; Vachharajani, NN, 2002
)
0.31
" Pharmacokinetic analysis was performed using a non-compartmental method."( Pharmacokinetics and dose proportionality of BMS-204352 after intraarterial administration to rats.
Krishna, R; Shah, VR; Srinivas, N, 2002
)
0.31
" Recent studies with a 103-compound dataset suggested that scaling from monkey pharmacokinetic data tended to be the most accurate method for predicting human clearance."( Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
Evans, CA; Jolivette, LJ; Nagilla, R; Ward, KW, 2006
)
0.33
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35

Bioavailability

ExcerptReferenceRelevance
" The objective of this study was to determine the pharmacokinetics, mass balance and absolute oral bioavailability of [(14)C]-BMS-204352 in rats and dogs."( Disposition of radiolabeled BMS-204352 in rats and dogs.
Arnold, M; Krishna, R; Pursley, JM; Shah, V; Srinivas, NR; Vachharajani, NN; Yao, M, 2002
)
0.31

Dosage Studied

ExcerptRelevanceReference
" Results indicated that (1) addition of diazepam, phenytoin, propranolol, or warfarin did not alter the free fraction of BMS-204352; (2) BMS-204352 did not displace diazepam, phenytoin, propranolol, or warfarin from their protein binding sites, and (3) comparison of ex vivo plasma samples after BMS-204352 dosing indicated no impact of BMS-204352 and/or its metabolites on the free fraction of diazepam, phenytoin, propranolol, or warfarin."( In vitro protein binding studies with BMS-204352: lack of protein binding displacement interaction in human serum.
Kaczor, D; Krishna, R; Srinivas, NR; Vachharajani, N; Yao, M, 2001
)
0.31
" Following acid hydrolysis in 6 M HCl for 24 h at 110 degrees C from plasma proteins collected from nine rats dosed with [14C]BMS-204352, one major radioactive product was isolated and identified as a lysine-adduct of des-fluoro des-O-methyl BMS-204352 by liquid chromatography/mass spectrometry and NMR analyses as well as by comparison with the synthetic analog, lysine-adduct of des-fluoro BMS-204352 (BMS-349821)."( Protein covalent binding of maxipost through a cytochrome P450-mediated ortho-quinone methide intermediate in rats.
Dai, R; Gedamke, R; Klunk, L; Mitroka, J; Ogan, M; Rinehart, JK; Roongta, V; Zhang, D; Zhu, M, 2003
)
0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (10)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)134.00000.11007.190310.0000AID1443980; AID1473738
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[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)
Potassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)EC50 (µMol)2.40000.04001.52084.3800AID726086
Potassium voltage-gated channel subfamily KQT member 2Homo sapiens (human)EC50 (µMol)2.40000.04001.32274.3800AID726087
Potassium voltage-gated channel subfamily KQT member 4Homo sapiens (human)EC50 (µMol)2.40001.60002.97005.9000AID726088
Calcium-activated potassium channel subunit alpha-1Homo sapiens (human)EC50 (µMol)0.35200.35200.35200.3520AID726264
Potassium voltage-gated channel subfamily KQT member 5Homo sapiens (human)EC50 (µMol)2.40000.50001.78753.4500AID726084
[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)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (85)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
protein targetingPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
protein import into nucleusPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
exocytosisPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
endocytosisPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
chemical synaptic transmissionPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
sensory perception of soundPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
gene expressionPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
response to auditory stimulusPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
response to organic cyclic compoundPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
neuron remodelingPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
neuronal action potentialPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
nerve developmentPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
psychomotor behaviorPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
regulation of synaptic plasticityPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
neuron apoptotic processPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
mitochondrial depolarizationPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
membrane hyperpolarizationPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
cellular response to calcium ionPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
apoptosome assemblyPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
excitatory chemical synaptic transmissionPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
inhibitory chemical synaptic transmissionPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
action potential initiationPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
regulation of action potential firing thresholdPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
substantia propria of cornea developmentPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
chemical synaptic transmissionPotassium voltage-gated channel subfamily KQT member 2Homo sapiens (human)
nervous system developmentPotassium voltage-gated channel subfamily KQT member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily KQT member 2Homo sapiens (human)
action potentialPotassium voltage-gated channel subfamily KQT member 2Homo 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)
lipid metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
androgen metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 2B7Homo sapiens (human)
potassium ion transportPotassium voltage-gated channel subfamily KQT member 4Homo sapiens (human)
sensory perception of soundPotassium voltage-gated channel subfamily KQT member 4Homo sapiens (human)
inner ear morphogenesisPotassium voltage-gated channel subfamily KQT member 4Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily KQT member 4Homo sapiens (human)
response to hypoxiaCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
potassium ion transportCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
response to osmotic stressCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
intracellular potassium ion homeostasisCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
response to carbon monoxideCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
regulation of membrane potentialCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
positive regulation of apoptotic processCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
negative regulation of cell volumeCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
response to calcium ionCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
micturitionCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
smooth muscle contraction involved in micturitionCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
potassium ion transmembrane transportCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
vasodilationCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily KQT member 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (34)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
calmodulin bindingPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily KQT member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily KQT member 2Homo sapiens (human)
calmodulin bindingPotassium voltage-gated channel subfamily KQT member 2Homo sapiens (human)
ankyrin bindingPotassium voltage-gated channel subfamily KQT member 2Homo 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)
retinoic acid bindingUDP-glucuronosyltransferase 2B7Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 2B7Homo sapiens (human)
potassium channel activityPotassium voltage-gated channel subfamily KQT member 4Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily KQT member 4Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily KQT member 4Homo sapiens (human)
actin bindingCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
voltage-gated potassium channel activityCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
protein bindingCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
calcium-activated potassium channel activityCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
metal ion bindingCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
large conductance calcium-activated potassium channel activityCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily KQT member 5Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily KQT member 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (26)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
mitochondrionPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
node of RanvierPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
axon initial segmentPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
synapsePotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily KQT member 2Homo sapiens (human)
node of RanvierPotassium voltage-gated channel subfamily KQT member 2Homo sapiens (human)
axon initial segmentPotassium voltage-gated channel subfamily KQT member 2Homo sapiens (human)
synapsePotassium voltage-gated channel subfamily KQT member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily KQT member 2Homo sapiens (human)
membranePotassium voltage-gated channel subfamily KQT member 2Homo 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)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 2B7Homo sapiens (human)
membraneUDP-glucuronosyltransferase 2B7Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily KQT member 4Homo sapiens (human)
basal plasma membranePotassium voltage-gated channel subfamily KQT member 4Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily KQT member 4Homo sapiens (human)
plasma membraneCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
caveolaCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
membraneCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
apical plasma membraneCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
voltage-gated potassium channel complexCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
postsynaptic membraneCalcium-activated potassium channel subunit alpha-1Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily KQT member 5Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily KQT member 5Homo sapiens (human)
clathrin coatPotassium voltage-gated channel subfamily KQT member 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (44)

Assay IDTitleYearJournalArticle
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID624640Drug glucuronidation reaction catalyzed by human recombinant UGT2B72005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID82191Tested for the effect on whole cell maxi-K current in HEK 293 cells at 10 nM2002Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7
The synthesis and characterization of BMS-204352 (MaxiPost) and related 3-fluorooxindoles as openers of maxi-K potassium channels.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID726088Positive modulatory activity at voltage-gated K channel 7.4 (unknown origin)2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Ion channels as therapeutic targets: a drug discovery perspective.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540225Volume of distribution at steady state in dog after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID540222Clearance in rat after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID11300Evaluated for Volume of distribution after iv administration of 5 mg/kg to male Sprague-Dawley rats2002Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7
The synthesis and characterization of BMS-204352 (MaxiPost) and related 3-fluorooxindoles as openers of maxi-K potassium channels.
AID82194Tested for the effect on whole cell maxi-K current in HEK 293 cells at 1000 nM2002Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7
The synthesis and characterization of BMS-204352 (MaxiPost) and related 3-fluorooxindoles as openers of maxi-K potassium channels.
AID540229Volume of distribution at steady state in human after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID12284Evaluated for half-life after iv administration of 5 mg/kg to male Sprague-Dawley rats in plasma2002Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7
The synthesis and characterization of BMS-204352 (MaxiPost) and related 3-fluorooxindoles as openers of maxi-K potassium channels.
AID12369Evaluated for AUC after iv administration of 5 mg/kg to male Sprague-Dawley rats in plasma2002Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7
The synthesis and characterization of BMS-204352 (MaxiPost) and related 3-fluorooxindoles as openers of maxi-K potassium channels.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID12367Evaluated for AUC after iv administration of 1 mg/kg to male Sprague-Dawley rats in plasma2002Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7
The synthesis and characterization of BMS-204352 (MaxiPost) and related 3-fluorooxindoles as openers of maxi-K potassium channels.
AID12283Evaluated for half-life after iv administration of 5 mg/kg to male Sprague-Dawley rats in brain2002Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7
The synthesis and characterization of BMS-204352 (MaxiPost) and related 3-fluorooxindoles as openers of maxi-K potassium channels.
AID540227Volume of distribution at steady state in monkey after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID12366Evaluated for AUC after iv administration of 1 mg/kg to male Sprague-Dawley rats in brain; not determined2002Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7
The synthesis and characterization of BMS-204352 (MaxiPost) and related 3-fluorooxindoles as openers of maxi-K potassium channels.
AID540228Clearance in human after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID540226Clearance in monkey after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID726087Positive modulatory activity at voltage-gated K channel 7.2 (unknown origin)2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Ion channels as therapeutic targets: a drug discovery perspective.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID726086Positive modulatory activity at voltage-gated K channel 7.3 (unknown origin)2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Ion channels as therapeutic targets: a drug discovery perspective.
AID540223Volume of distribution at steady state in rat after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID231753Ratio of brain AUC versus plasma AUC2002Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7
The synthesis and characterization of BMS-204352 (MaxiPost) and related 3-fluorooxindoles as openers of maxi-K potassium channels.
AID82193Tested for the effect on whole cell maxi-K current in HEK 293 cells at 100 nM2002Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7
The synthesis and characterization of BMS-204352 (MaxiPost) and related 3-fluorooxindoles as openers of maxi-K potassium channels.
AID726264Positive modulation of Kca 1.1 (unknown origin)2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Ion channels as therapeutic targets: a drug discovery perspective.
AID88607In vitro reduction of glutamate release in hippocampal slices2001Journal 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.
AID726084Positive modulatory activity at voltage-gated K channel 7.5 (unknown origin)2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Ion channels as therapeutic targets: a drug discovery perspective.
AID12368Evaluated for AUC after iv administration of 5 mg/kg to male Sprague-Dawley rats in brain2002Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7
The synthesis and characterization of BMS-204352 (MaxiPost) and related 3-fluorooxindoles as openers of maxi-K potassium channels.
AID12282Evaluated for half-life after iv administration of 1 mg/kg to male Sprague-Dawley rats in plasma2002Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7
The synthesis and characterization of BMS-204352 (MaxiPost) and related 3-fluorooxindoles as openers of maxi-K potassium channels.
AID11180Evaluated for plasma clearance after iv administration of 5 mg/kg to male Sprague-Dawley rats2002Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7
The synthesis and characterization of BMS-204352 (MaxiPost) and related 3-fluorooxindoles as openers of maxi-K potassium channels.
AID161267Evaluation of maxi-K opening in Xenopus laevis oocytes injected with Hslo1 channels as percent of control current; insoluble at 1 uM2002Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7
The synthesis and characterization of BMS-204352 (MaxiPost) and related 3-fluorooxindoles as openers of maxi-K potassium channels.
AID540224Clearance in dog after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID12281Evaluated for half-life after iv administration of 1 mg/kg to male Sprague-Dawley rats in brain; not determined2002Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7
The synthesis and characterization of BMS-204352 (MaxiPost) and related 3-fluorooxindoles as openers of maxi-K potassium channels.
AID1346696Human Kv7.2 (Voltage-gated potassium channels)2001Neuropharmacology, Jun, Volume: 40, Issue:7
KCNQ4 channel activation by BMS-204352 and retigabine.
AID1346699Human Kv7.4 (Voltage-gated potassium channels)2001American journal of physiology. Cell physiology, Apr, Volume: 280, Issue:4
KCNQ4 channels expressed in mammalian cells: functional characteristics and pharmacology.
AID1346446Human KCa1.1 (Calcium- and sodium-activated potassium channels)2001Nature medicine, Apr, Volume: 7, Issue:4
Targeting acute ischemic stroke with a calcium-sensitive opener of maxi-K potassium channels.
AID1346689Human Kv7.5 (Voltage-gated potassium channels)2002European journal of pharmacology, Feb-22, Volume: 437, Issue:3
Activation of KCNQ5 channels stably expressed in HEK293 cells by BMS-204352.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (49)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's36 (73.47)29.6817
2010's11 (22.45)24.3611
2020's2 (4.08)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.42

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 Index10.42 (24.57)
Research Supply Index3.93 (2.92)
Research Growth Index4.35 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.42)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (2.04%)5.53%
Reviews6 (12.24%)6.00%
Case Studies1 (2.04%)4.05%
Observational0 (0.00%)0.25%
Other41 (83.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]