Compounds > ica 27243
Page last updated: 2024-11-12

ica 27243

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Description

N-(6-Chloropyridin-3-yl)-3,4-difluorobenzamide: a KCNQ2/3 channel activator; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9903497
CHEMBL ID402146
SCHEMBL ID367538
MeSH IDM0520079

Synonyms (27)

Synonym
VU0409857-1
ZTZ233
CHEMBL402146 ,
ica-27243
ica 27243
ica27243
n-(6-chloropyridin-3-yl)-3,4-difluorobenzamide
VU0409857-2
bdbm50420049
AKOS016340338
gtpl7667
unii-vu7278d853
vu7278d853 ,
325457-89-4
benzamide, n-(6-chloro-3-pyridinyl)-3,4-difluoro-
GG-0057
SCHEMBL367538
mfcd17166959
A1-06007
HY-122114
CS-0081878
Q27078022
BCP32732
ica 27243; ica27243
W10725
ica-027243
c12h7clf2n2o

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" This compound was active in several rodent models of epilepsy and pain but upon repeated dosing had a number of unacceptable toxicities that prevented further development."( N-Pyridyl and Pyrimidine Benzamides as KCNQ2/Q3 Potassium Channel Openers for the Treatment of Epilepsy.
Amato, G; Antonio, B; Fritch, P; McNaughton-Smith, G; Mersch, T; Rigdon, GC; Roeloffs, R; Suto, MJ; Wickenden, AD, 2011)		0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (7)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Potassium voltage-gated channel subfamily E member 1Homo sapiens (human)IC50 (µMol)41.00000.12004.048010.0000AID669436
Potassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)IC50 (µMol)41.00000.12004.048010.0000AID669436
[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 2Rattus norvegicus (Norway rat)EC50 (µMol)14.40000.230061.1402554.6400AID2548
Potassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)EC50 (µMol)3.61330.04001.52084.3800AID1414246; AID1414248; AID669435
Potassium voltage-gated channel subfamily KQT member 2Homo sapiens (human)EC50 (µMol)0.42000.04001.32274.3800AID1414246; AID669435
Potassium voltage-gated channel subfamily KQT member 4Homo sapiens (human)EC50 (µMol)10.00001.60002.97005.9000AID1414249
Potassium voltage-gated channel subfamily KQT member 5Homo sapiens (human)EC50 (µMol)10.00000.50001.78753.4500AID1414248
[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)
Potassium voltage-gated channel subfamily KQT member 3Homo sapiens (human)Activity0.46000.04000.27330.4600AID1414250
Potassium voltage-gated channel subfamily KQT member 2Homo sapiens (human)Activity0.46000.04000.27330.4600AID1414250
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (85)

Processvia Protein(s)Taxonomy
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)
epithelial cell maturationPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
sensory perception of soundPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
male gonad developmentPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
vestibular nucleus developmentPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
secretory granule organizationPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
cellular response to cAMPPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
cellular response to acidic pHPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
cellular response to light stimulusPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
cardiac muscle cell action potential involved in contractionPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
cardiac muscle cell contractionPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
negative regulation of protein targeting to membranePotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
regulation of delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
negative regulation of delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
gastrin-induced gastric acid secretionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
glucose metabolic processPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
heart developmentPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
sensory perception of soundPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
rhythmic behaviorPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
regulation of heart contractionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
regulation of blood pressurePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
positive regulation of heart ratePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
iodide transportPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
erythrocyte differentiationPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
intracellular chloride ion homeostasisPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
response to insulinPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
social behaviorPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
corticosterone secretionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
inner ear morphogenesisPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
inner ear developmentPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
intestinal absorptionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception of soundPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
auditory receptor cell developmentPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
positive regulation of cardiac muscle contractionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
regulation of gastric acid secretionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
stomach developmentPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
renal absorptionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
renal sodium ion absorptionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cellular response to cAMPPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cellular response to epinephrine stimulusPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
adrenergic receptor signaling pathwayPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cardiac muscle cell contractionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
atrial cardiac muscle cell action potentialPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cochlea developmentPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
membrane repolarization during atrial cardiac muscle cell action potentialPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
non-motile cilium assemblyPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
action potentialPotassium voltage-gated channel subfamily KQT member 1Homo 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)
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 (19)

Processvia Protein(s)Taxonomy
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)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
potassium channel regulator activityPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
telethonin bindingPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
protein-containing complex bindingPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
transmembrane transporter bindingPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
calmodulin bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
phosphatidylinositol-4,5-bisphosphate bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
protein phosphatase 1 bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
outward rectifier potassium channel activityPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
protein kinase A catalytic subunit bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
protein kinase A regulatory subunit bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
transmembrane transporter bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
voltage-gated potassium channel activity involved in atrial cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily KQT member 1Homo 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)
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 (27)

Processvia Protein(s)Taxonomy
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)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
lysosomePotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
apical plasma membranePotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
Z discPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
membrane raftPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
early endosomePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
endoplasmic reticulumPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cytoplasmPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
lysosomePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
early endosomePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
late endosomePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
endoplasmic reticulumPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
basolateral plasma membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
apical plasma membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
transport vesiclePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cytoplasmic vesicle membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
neuron projectionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
neuronal cell bodyPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
membrane raftPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
ciliary basePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
lumenal side of membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
basolateral part of cellPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
monoatomic ion channel complexPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
membranePotassium voltage-gated channel subfamily KQT member 1Homo 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 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 (22)

Assay IDTitleYearJournalArticle
AID669435Agonist activity at KCNQ2/KCNQ3 expressed in CHO cells assessed as increase in KCl-induced 86Rb+ efflux incubated for 10 mins prior to KCl-induction by liquid scintillation counting2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
N-Pyridyl and Pyrimidine Benzamides as KCNQ2/Q3 Potassium Channel Openers for the Treatment of Epilepsy.
AID1414246Activation of human Kv7.2/7.3 by patch clamp method2018Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
Novel K
AID1604622Activation of human Kv7.2 expressed in CHO cells assessed as increase in current amplitude at 10 uM measured at holding potential of 0 mV by whole cell patch clamp electrophysiology assay relative to control
AID313162Analgesic activity in SNL nerve injury in po dosed rat model2007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
Kv7 (KCNQ) channel modulators and neuropathic pain.
AID1414250Activation of human wild type Kv7.2/7.3 expressed in CHO cells assessed as 86Rb efflux at 0.001 to 100 uM after 10 mins by microbeta liquid scintillation counting analysis2018Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
Novel K
AID313161Analgesic activity in carrageenan model in po dosed rat model2007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
Kv7 (KCNQ) channel modulators and neuropathic pain.
AID669441Toxicity in po dosed rat assessed as nonhemolytic anemia after 14 days2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
N-Pyridyl and Pyrimidine Benzamides as KCNQ2/Q3 Potassium Channel Openers for the Treatment of Epilepsy.
AID669439Toxicity in rat assessed as nonhemolytic anemia after 28 days administered with repeated doses2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
N-Pyridyl and Pyrimidine Benzamides as KCNQ2/Q3 Potassium Channel Openers for the Treatment of Epilepsy.
AID1414270Anti-seizure activity in CD-1 mouse assessed as increase in seizure threshold at 10 to 60 mg/kg, po by maximal electroshock-threshold test2018Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
Novel K
AID1604633Activation of ICA-insensitive human Kv7.2 F168L mutant expressed in CHO cells assessed as increase in channel current amplitude at 10 uM measured at holding potential of -40 mV by whole cell patch clamp electrophysiology assay
AID669436Antagonist activity at KCNQ1/MINK expressed in CHO cells assessed as inhibition of KCl-induced 86Rb+ efflux incubated for 10 mins prior to KCl-induction by liquid scintillation counting2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
N-Pyridyl and Pyrimidine Benzamides as KCNQ2/Q3 Potassium Channel Openers for the Treatment of Epilepsy.
AID1414249Activation of human Kv7.4 by patch clamp method2018Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
Novel K
AID1414248Activation of human Kv7.3/7.5 by patch clamp method2018Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
Novel K
AID1604632Activation of human Kv7.2 W236L mutant expressed in CHO cells assessed as channel current amplitude at 10 uM measured at holding potential of -40 mV by whole cell patch clamp electrophysiology assay
AID1414271Toxicity in in CD-1 mouse at 10 to 60 mg/kg, po by rotarod test2018Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
Novel K
AID669440Toxicity in cynomolgus monkey assessed as nonhemolytic anemia after 28 days administered with repeated doses2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
N-Pyridyl and Pyrimidine Benzamides as KCNQ2/Q3 Potassium Channel Openers for the Treatment of Epilepsy.
AID1604623Activation of human Kv7.2 expressed in CHO cells assessed as increase in current amplitude at 10 uM measured at holding potential of -40 mV by whole cell patch clamp electrophysiology assay relative to control
AID1414251Activation of human Kv7.2 W236L mutant/Kv7.3 W265L mutant expressed in CHO cells assessed as 86Rb efflux at 0.001 to 100 uM after 10 mins by microbeta liquid scintillation counting analysis2018Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
Novel K
AID669446Antiepileptic activity in po dosed Sprague-Dawley rat assessed as latency in PTZ-induced seizure administered 30 mins prior to PTZ-challenge measured up to 15 minutes2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
N-Pyridyl and Pyrimidine Benzamides as KCNQ2/Q3 Potassium Channel Openers for the Treatment of Epilepsy.
AID313159Analgesic activity in formalin-induced pain hypersensitivity in po dosed rat2007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
Kv7 (KCNQ) channel modulators and neuropathic pain.
AID669445Antiepileptic activity in po dosed Wistar rat assessed as latency in maximum electric shock-induced hind limb extension administered 30 mins prior to electric shock-challenge measured up to 6 secs2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
N-Pyridyl and Pyrimidine Benzamides as KCNQ2/Q3 Potassium Channel Openers for the Treatment of Epilepsy.
AID1346696Human Kv7.2 (Voltage-gated potassium channels)2009Neuroscience letters, Nov-13, Volume: 465, Issue:2
The KCNQ2/3 selective channel opener ICA-27243 binds to a novel voltage-sensor domain site.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (15)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's5 (33.33)29.6817
2010's9 (60.00)24.3611
2020's1 (6.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 19.33

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index19.33 (24.57)
Research Supply Index2.89 (2.92)
Research Growth Index4.59 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (19.33)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (5.88%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other16 (94.12%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
carbamates
[no description available]		3.4570amino-acid anion
formaldehyde
paraform: polymerized formaldehyde; RN given refers to parent cpd; used in root canal therapy		2.110aldehyde;
one-carbon compound		allergen;
carcinogenic agent;
disinfectant;
EC 3.5.1.4 (amidase) inhibitor;
environmental contaminant;
Escherichia coli metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
chlordiazepoxide
Chlordiazepoxide: An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal.. chlordiazepoxide : A benzodiazepine that is 3H-1,4-benzodiazepine 4-oxide substituted by a chloro group at position 7, a phenyl group at position 5 and a methylamino group at position 2.		2.4620benzodiazepine
amphetamine
Amphetamine: A powerful central nervous system stimulant and sympathomimetic. Amphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulation of release of monamines, and inhibiting monoamine oxidase. Amphetamine is also a drug of abuse and a psychotomimetic. The l- and the d,l-forms are included here. The l-form has less central nervous system activity but stronger cardiovascular effects. The d-form is DEXTROAMPHETAMINE.. 1-phenylpropan-2-amine : A primary amine that is isopropylamine in which a hydrogen attached to one of the methyl groups has been replaced by a phenyl group.. amphetamine : A racemate comprising equimolar amounts of (R)-amphetamine (also known as levamphetamine or levoamphetamine) and (S)-amphetamine (also known as dexamfetamine or dextroamphetamine.		2.0510primary amine
lamotrigine
[no description available]		2.05101,2,4-triazines;
dichlorobenzene;
primary arylamine		anticonvulsant;
antidepressant;
antimanic drug;
calcium channel blocker;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
excitatory amino acid antagonist;
geroprotector;
non-narcotic analgesic;
xenobiotic
potassium chloride
Potassium Chloride: A white crystal or crystalline powder used in BUFFERS; FERTILIZERS; and EXPLOSIVES. It can be used to replenish ELECTROLYTES and restore WATER-ELECTROLYTE BALANCE in treating HYPOKALEMIA.. potassium chloride : A metal chloride salt with a K(+) counterion.		2.0610inorganic chloride;
inorganic potassium salt;
potassium salt		fertilizer
dextroamphetamine
Dextroamphetamine: The d-form of AMPHETAMINE. It is a central nervous system stimulant and a sympathomimetic. It has also been used in the treatment of narcolepsy and of attention deficit disorders and hyperactivity in children. Dextroamphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulating release of monamines, and inhibiting monoamine oxidase. It is also a drug of abuse and a psychotomimetic.. (S)-amphetamine : A 1-phenylpropan-2-amine that has S configuration.		2.07101-phenylpropan-2-amineadrenergic agent;
adrenergic uptake inhibitor;
dopamine uptake inhibitor;
dopaminergic agent;
neurotoxin;
sympathomimetic agent
serine
Serine: A non-essential amino acid occurring in natural form as the L-isomer. It is synthesized from GLYCINE or THREONINE. It is involved in the biosynthesis of PURINES; PYRIMIDINES; and other amino acids.. serine : An alpha-amino acid that is alanine substituted at position 3 by a hydroxy group.		2.0710L-alpha-amino acid;
proteinogenic amino acid;
serine family amino acid;
serine zwitterion;
serine		algal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
levodopa
Levodopa: The naturally occurring form of DIHYDROXYPHENYLALANINE and the immediate precursor of DOPAMINE. Unlike dopamine itself, it can be taken orally and crosses the blood-brain barrier. It is rapidly taken up by dopaminergic neurons and converted to DOPAMINE. It is used for the treatment of PARKINSONIAN DISORDERS and is usually given with agents that inhibit its conversion to dopamine outside of the central nervous system.. L-dopa : An optically active form of dopa having L-configuration. Used to treat the stiffness, tremors, spasms, and poor muscle control of Parkinson's disease		2.0810amino acid zwitterion;
dopa;
L-tyrosine derivative;
non-proteinogenic L-alpha-amino acid		allelochemical;
antidyskinesia agent;
antiparkinson drug;
dopaminergic agent;
hapten;
human metabolite;
mouse metabolite;
neurotoxin;
plant growth retardant;
plant metabolite;
prodrug
tryptophan
Tryptophan: An essential amino acid that is necessary for normal growth in infants and for NITROGEN balance in adults. It is a precursor of INDOLE ALKALOIDS in plants. It is a precursor of SEROTONIN (hence its use as an antidepressant and sleep aid). It can be a precursor to NIACIN, albeit inefficiently, in mammals.. tryptophan : An alpha-amino acid that is alanine bearing an indol-3-yl substituent at position 3.		2.0510erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid zwitterion;
L-alpha-amino acid;
proteinogenic amino acid;
tryptophan zwitterion;
tryptophan		antidepressant;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
deoxyglucose
Deoxyglucose: 2-Deoxy-D-arabino-hexose. An antimetabolite of glucose with antiviral activity.. deoxyglucose : A deoxyhexose comprising glucose having at least one hydroxy group replaced by hydrogen.		2.0710
ezogabine
ezogabine: structure in first source. ezogabine : A substituted aniline that is benzene-1,2,4-triamine bearing ethoxycarbonyl and 4-fluorobenzyl substituents at positions N-1 and N-4 respectively. An anticonvulsant used to treat seizures associated with epilepsy in adults.		4.7790carbamate ester;
organofluorine compound;
secondary amino compound;
substituted aniline		anticonvulsant;
potassium channel modulator
bms204352
BMS204352: a calcium-sensitive opener of maxi-K potassium channels; structure in first source		2.7530
xe 991, anthracenone
10,10-bis(4-pyridinylmethyl)-9(10H)-anthracenone: neurotransmitter release enhancer and potassium channel blocker; structure given in first source		2.7730anthracenes
N-(2,4,6-trimethylphenyl)-3-bicyclo[2.2.1]heptanecarboxamide
[no description available]		2.1710monoterpenoid
n-(6-chloropyridin-3-yl)-4-fluorobenzamide
N-(6-chloropyridin-3-yl)-4-fluorobenzamide: structure in first source		2.0610
ConditionIndicatedRelationship StrengthStudiesTrials
Ache
[description not available]		03.3820
Peripheral Nerve Diseases
[description not available]		02.9510
Pain
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.		03.3820
Peripheral Nervous System Diseases
Diseases of the peripheral nerves external to the brain and spinal cord, which includes diseases of the nerve roots, ganglia, plexi, autonomic nerves, sensory nerves, and motor nerves.		02.9510
Aura
[description not available]		02.1710
Absence Seizure
[description not available]		02.4920
Epilepsy
A disorder characterized by recurrent episodes of paroxysmal brain dysfunction due to a sudden, disorderly, and excessive neuronal discharge. Epilepsy classification systems are generally based upon: (1) clinical features of the seizure episodes (e.g., motor seizure), (2) etiology (e.g., post-traumatic), (3) anatomic site of seizure origin (e.g., frontal lobe seizure), (4) tendency to spread to other structures in the brain, and (5) temporal patterns (e.g., nocturnal epilepsy). (From Adams et al., Principles of Neurology, 6th ed, p313)		02.1710
Muscle Contraction
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.		02.1710
Seizures
Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or seizure disorder.		02.4920
Autosomal Dominant Juvenile Parkinson Disease
[description not available]		02.0810
Dyskinesia, Medication-Induced
[description not available]		02.0810
Dyskinesia, Drug-Induced
Abnormal movements, including HYPERKINESIS; HYPOKINESIA; TREMOR; and DYSTONIA, associated with the use of certain medications or drugs. Muscles of the face, trunk, neck, and extremities are most commonly affected. Tardive dyskinesia refers to abnormal hyperkinetic movements of the muscles of the face, tongue, and neck associated with the use of neuroleptic agents (see ANTIPSYCHOTIC AGENTS). (Adams et al., Principles of Neurology, 6th ed, p1199)		02.0810
Parkinsonian Disorders
A group of disorders which feature impaired motor control characterized by bradykinesia, MUSCLE RIGIDITY; TREMOR; and postural instability. Parkinsonian diseases are generally divided into primary parkinsonism (see PARKINSON DISEASE), secondary parkinsonism (see PARKINSON DISEASE, SECONDARY) and inherited forms. These conditions are associated with dysfunction of dopaminergic or closely related motor integration neuronal pathways in the BASAL GANGLIA.		02.0810
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.7530
Allodynia
[description not available]		02.110
Innate Inflammatory Response
[description not available]		02.110
Developmental Coordination Disorder
[description not available]		02.110
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		02.110
Affective Psychosis, Bipolar
[description not available]		02.4620
Hyperactivity, Motor
[description not available]		02.0510
Bipolar Disorder
A major affective disorder marked by severe mood swings (manic or major depressive episodes) and a tendency to remission and recurrence.		02.4620
Hypothermia, Accidental
[description not available]		02.0610
Hypothermia
Lower than normal body temperature, especially in warm-blooded animals.		02.0610
Neuroblastoma
A common neoplasm of early childhood arising from neural crest cells in the sympathetic nervous system, and characterized by diverse clinical behavior, ranging from spontaneous remission to rapid metastatic progression and death. This tumor is the most common intraabdominal malignancy of childhood, but it may also arise from thorax, neck, or rarely occur in the central nervous system. Histologic features include uniform round cells with hyperchromatic nuclei arranged in nests and separated by fibrovascular septa. Neuroblastomas may be associated with the opsoclonus-myoclonus syndrome. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2099-2101; Curr Opin Oncol 1998 Jan;10(1):43-51)		02.0410
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		02.0410