Page last updated: 2024-11-13

gsk299423

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

Description

GSK299423: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID46835136
CHEMBL ID1235773
MeSH IDM0550511

Synonyms (18)

Synonym
gsk299423
CHEMBL1235773 ,
6-methoxy-4-(2-{4-[([1,3]oxathiolo[5,4-c]pyridin-6-ylmethyl)amino]piperidin-1-yl}ethyl)quinoline-3-carbonitrile
rxv ,
bdbm50359538
gsk-299423
unii-2q0g81h7fk
2q0g81h7fk ,
1352149-24-6
3-quinolinecarbonitrile, 6-methoxy-4-(2-(4-(((1,3)oxathiolo(5,4-c)pyridin-6-ylmethyl)amino)-1-piperidinyl)ethyl)-
6-methoxy-4-[2-[4-[([1,3]oxathiolo[5,4-c]pyridin-6-ylmethyl)amino]-1-piperidinyl]ethyl]-3-quinolinecarbonitrile
DTXSID50159279
BCP17725
Q5514569
4-(2-(4-(([1,3]oxathiolo[5,4-c]pyridin-6-ylmethyl)amino)piperidin-1-yl)ethyl)-6-methoxyquinoline-3-carbonitrile
6-methoxy-4-[2-[4-([1,3]oxathiolo[5,4-c]pyridin-6-ylmethylamino)piperidin-1-yl]ethyl]quinoline-3-carbonitrile
3-quinolinecarbonitrile, 6-methoxy-4-[2-[4-[([1,3]oxathiolo[5,4-c]pyridin-6-ylmethyl)amino]-1-piperidinyl]ethyl]-
AKOS040751965
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (5)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
DNA gyrase subunit BStaphylococcus aureusIC50 (µMol)0.01400.00401.50207.7000AID1576770
DNA gyrase subunit AEscherichia coli K-12IC50 (µMol)0.10000.02390.56295.2300AID1576769
DNA gyrase subunit BEscherichia coli K-12IC50 (µMol)0.10000.00500.43985.2300AID1576769
DNA gyrase subunit AStaphylococcus aureusIC50 (µMol)0.01400.00401.98397.7000AID1576770
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)1.25000.00091.901410.0000AID635826; AID635827
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (29)

Processvia Protein(s)Taxonomy
DNA topological changeDNA gyrase subunit AEscherichia coli K-12
DNA-templated transcriptionDNA gyrase subunit AEscherichia coli K-12
response to xenobiotic stimulusDNA gyrase subunit AEscherichia coli K-12
DNA-templated DNA replicationDNA gyrase subunit AEscherichia coli K-12
DNA topological changeDNA gyrase subunit AEscherichia coli K-12
response to antibioticDNA gyrase subunit AEscherichia coli K-12
chromosome organizationDNA gyrase subunit AEscherichia coli K-12
negative regulation of DNA-templated DNA replicationDNA gyrase subunit AEscherichia coli K-12
DNA topological changeDNA gyrase subunit BEscherichia coli K-12
DNA-templated transcriptionDNA gyrase subunit BEscherichia coli K-12
response to xenobiotic stimulusDNA gyrase subunit BEscherichia coli K-12
DNA-templated DNA replicationDNA gyrase subunit BEscherichia coli K-12
DNA topological changeDNA gyrase subunit BEscherichia coli K-12
response to antibioticDNA gyrase subunit BEscherichia coli K-12
chromosome organizationDNA gyrase subunit BEscherichia coli K-12
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (19)

Processvia Protein(s)Taxonomy
DNA bindingDNA gyrase subunit AEscherichia coli K-12
DNA topoisomerase activityDNA gyrase subunit AEscherichia coli K-12
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) activityDNA gyrase subunit AEscherichia coli K-12
protein bindingDNA gyrase subunit AEscherichia coli K-12
ATP bindingDNA gyrase subunit AEscherichia coli K-12
ATP-dependent activity, acting on DNADNA gyrase subunit AEscherichia coli K-12
DNA negative supercoiling activityDNA gyrase subunit AEscherichia coli K-12
identical protein bindingDNA gyrase subunit AEscherichia coli K-12
DNA bindingDNA gyrase subunit BEscherichia coli K-12
DNA topoisomerase activityDNA gyrase subunit BEscherichia coli K-12
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) activityDNA gyrase subunit BEscherichia coli K-12
protein bindingDNA gyrase subunit BEscherichia coli K-12
ATP bindingDNA gyrase subunit BEscherichia coli K-12
ATP-dependent activity, acting on DNADNA gyrase subunit BEscherichia coli K-12
DNA negative supercoiling activityDNA gyrase subunit BEscherichia coli K-12
metal ion bindingDNA gyrase subunit BEscherichia coli K-12
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Processvia Protein(s)Taxonomy
chromosomeDNA gyrase subunit AEscherichia coli K-12
cytoplasmDNA gyrase subunit AEscherichia coli K-12
cytosolDNA gyrase subunit AEscherichia coli K-12
membraneDNA gyrase subunit AEscherichia coli K-12
cytoplasmDNA gyrase subunit AEscherichia coli K-12
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) complexDNA gyrase subunit AEscherichia coli K-12
chromosomeDNA gyrase subunit BEscherichia coli K-12
cytoplasmDNA gyrase subunit BEscherichia coli K-12
cytosolDNA gyrase subunit BEscherichia coli K-12
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) complexDNA gyrase subunit BEscherichia coli K-12
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (10)

Assay IDTitleYearJournalArticle
AID1576770Inhibition of Staphylococcus aureus DNA gyrase2019Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
Virtual Screening Approach and Investigation of Structure-Activity Relationships To Discover Novel Bacterial Topoisomerase Inhibitors Targeting Gram-Positive and Gram-Negative Pathogens.
AID635823Antibacterial activity against Haemophilus influenzae H128 after 18 to 24 hrs by broth microdilution method2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases.
AID635821Inhibition of Haemophilus influenzae DNA gyrase-dependent DNA replication by scintillation proximity assay2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases.
AID635826Inhibition of human ERG expressed in HEK293 cells by patch-clamp electrophysiology2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases.
AID1576774Antibacterial activity against Escherichia coli2019Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
Virtual Screening Approach and Investigation of Structure-Activity Relationships To Discover Novel Bacterial Topoisomerase Inhibitors Targeting Gram-Positive and Gram-Negative Pathogens.
AID635827Displacement of [3H]dofetilide from human ERG by liquid scintillation counting2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases.
AID1576769Inhibition of Escherichia coli DNA gyrase2019Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
Virtual Screening Approach and Investigation of Structure-Activity Relationships To Discover Novel Bacterial Topoisomerase Inhibitors Targeting Gram-Positive and Gram-Negative Pathogens.
AID635824Antibacterial activity against Staphylococcus aureus WCUH 29 after 18 to 24 hrs by broth microdilution method2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases.
AID635825Antibacterial activity against Streptococcus pneumoniae 1629 after 18 to 24 hrs by broth microdilution method2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases.
AID635828Distribution coefficient, log D of the compound at pH 7.42011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's4 (80.00)24.3611
2020's1 (20.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 13.20

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 Index13.20 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.99 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (13.20)

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%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]