Page last updated: 2024-11-12

a-317567

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

Description

A-317567: acid sensing ion channel blocker; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID10200844
CHEMBL ID185515
SCHEMBL ID5775814
MeSH IDM0493557

Synonyms (17)

Synonym
6-(2-(1-isopropyl-2-methyl-1,2,3,4-tetrahydroisoquinolin-7-yl)cyclopropyl)-2-naphthimidamide
bdbm50157090
6-[2-(1-isopropyl-2-methyl-1,2,3,4-tetrahydro-isoquinolin-7-yl)-cyclopropyl]-naphthalene-2-carboxamidine
a-317567
CHEMBL185515 ,
a317567
6-{2-[2-methyl-1-(propan-2-yl)-1,2,3,4-tetrahydroisoquinolin-7-yl]cyclopropyl}naphthalene-2-carboximidamide
a 317567
gtpl4116
SCHEMBL5775814
371217-32-2
HY-122135
6-[2-(2-methyl-1-propan-2-yl-3,4-dihydro-1h-isoquinolin-7-yl)cyclopropyl]naphthalene-2-carboximidamide
Q27074064
CS-0081980
2-naphthalenecarboximidamide, 6-[2-[1,2,3,4-tetrahydro-2-methyl-1-(1-methylethyl)-7-isoquinolinyl]cyclopropyl]-
AKOS040741015

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" These compounds possess excellent binding activities and selectivities with significantly improved pharmacokinetic profiles versus previously described amide-linked inhibitors."( Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
Bouska, J; Bruncko, M; Dalton, CR; Dellaria, JF; Geyer, A; Giranda, VL; Gong, J; Kaminski, MA; Klinghofer, V; Mantei, R; McClellan, WJ; Nienaber, VL; Rockway, TW; Sauer, DR; Stewart, K; Weitzberg, M; Wendt, MD; Zhao, X, 2005
)
0.33
[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)
Acid-sensing ion channel 3Rattus norvegicus (Norway rat)IC50 (µMol)9.50009.50009.50009.5000AID726071
PlasminogenHomo sapiens (human)Ki1.30200.01701.15604.4000AID238378
Urokinase-type plasminogen activatorHomo sapiens (human)Ki0.04860.01702.62687.0000AID238828; AID419413
Tissue-type plasminogen activatorHomo sapiens (human)Ki6.23000.01703.71968.6000AID238775
TrypsinSus scrofa (pig)Ki0.09000.09000.09000.0900AID238379
Kallikrein-1Homo sapiens (human)Ki0.57600.06100.41570.6100AID238464
Acid-sensing ion channel 1Rattus norvegicus (Norway rat)IC50 (µMol)2.00002.00002.00002.0000AID1495490
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (42)

Processvia Protein(s)Taxonomy
proteolysisPlasminogenHomo sapiens (human)
blood coagulationPlasminogenHomo sapiens (human)
negative regulation of cell population proliferationPlasminogenHomo sapiens (human)
negative regulation of cell-substrate adhesionPlasminogenHomo sapiens (human)
extracellular matrix disassemblyPlasminogenHomo sapiens (human)
tissue regenerationPlasminogenHomo sapiens (human)
fibrinolysisPlasminogenHomo sapiens (human)
positive regulation of blood vessel endothelial cell migrationPlasminogenHomo sapiens (human)
myoblast differentiationPlasminogenHomo sapiens (human)
muscle cell cellular homeostasisPlasminogenHomo sapiens (human)
tissue remodelingPlasminogenHomo sapiens (human)
biological process involved in interaction with symbiontPlasminogenHomo sapiens (human)
negative regulation of fibrinolysisPlasminogenHomo sapiens (human)
positive regulation of fibrinolysisPlasminogenHomo sapiens (human)
trophoblast giant cell differentiationPlasminogenHomo sapiens (human)
labyrinthine layer blood vessel developmentPlasminogenHomo sapiens (human)
mononuclear cell migrationPlasminogenHomo sapiens (human)
trans-synaptic signaling by BDNF, modulating synaptic transmissionPlasminogenHomo sapiens (human)
negative regulation of cell-cell adhesion mediated by cadherinPlasminogenHomo sapiens (human)
positive regulation of cell migrationUrokinase-type plasminogen activatorHomo sapiens (human)
response to hypoxiaUrokinase-type plasminogen activatorHomo sapiens (human)
proteolysisUrokinase-type plasminogen activatorHomo sapiens (human)
chemotaxisUrokinase-type plasminogen activatorHomo sapiens (human)
signal transductionUrokinase-type plasminogen activatorHomo sapiens (human)
blood coagulationUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of signaling receptor activityUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of plasminogen activationUrokinase-type plasminogen activatorHomo sapiens (human)
negative regulation of plasminogen activationUrokinase-type plasminogen activatorHomo sapiens (human)
smooth muscle cell migrationUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of smooth muscle cell migrationUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of cell adhesionUrokinase-type plasminogen activatorHomo sapiens (human)
plasminogen activationUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of cell adhesion mediated by integrinUrokinase-type plasminogen activatorHomo sapiens (human)
urokinase plasminogen activator signaling pathwayUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of cell population proliferationUrokinase-type plasminogen activatorHomo sapiens (human)
fibrinolysisUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of fibrinolysisUrokinase-type plasminogen activatorHomo sapiens (human)
negative regulation of fibrinolysisUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of wound healingUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of smooth muscle cell-matrix adhesionUrokinase-type plasminogen activatorHomo sapiens (human)
response to hypoxiaTissue-type plasminogen activatorHomo sapiens (human)
proteolysisTissue-type plasminogen activatorHomo sapiens (human)
blood coagulationTissue-type plasminogen activatorHomo sapiens (human)
negative regulation of plasminogen activationTissue-type plasminogen activatorHomo sapiens (human)
plasminogen activationTissue-type plasminogen activatorHomo sapiens (human)
protein modification processTissue-type plasminogen activatorHomo sapiens (human)
fibrinolysisTissue-type plasminogen activatorHomo sapiens (human)
negative regulation of proteolysisTissue-type plasminogen activatorHomo sapiens (human)
negative regulation of fibrinolysisTissue-type plasminogen activatorHomo sapiens (human)
prevention of polyspermyTissue-type plasminogen activatorHomo sapiens (human)
trans-synaptic signaling by BDNF, modulating synaptic transmissionTissue-type plasminogen activatorHomo sapiens (human)
platelet-derived growth factor receptor signaling pathwayTissue-type plasminogen activatorHomo sapiens (human)
smooth muscle cell migrationTissue-type plasminogen activatorHomo sapiens (human)
zymogen activationKallikrein-1Homo sapiens (human)
regulation of systemic arterial blood pressureKallikrein-1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Processvia Protein(s)Taxonomy
protease bindingPlasminogenHomo sapiens (human)
endopeptidase activityPlasminogenHomo sapiens (human)
serine-type endopeptidase activityPlasminogenHomo sapiens (human)
signaling receptor bindingPlasminogenHomo sapiens (human)
protein bindingPlasminogenHomo sapiens (human)
serine-type peptidase activityPlasminogenHomo sapiens (human)
enzyme bindingPlasminogenHomo sapiens (human)
kinase bindingPlasminogenHomo sapiens (human)
protein domain specific bindingPlasminogenHomo sapiens (human)
apolipoprotein bindingPlasminogenHomo sapiens (human)
protein-folding chaperone bindingPlasminogenHomo sapiens (human)
protein antigen bindingPlasminogenHomo sapiens (human)
serine-type endopeptidase activityUrokinase-type plasminogen activatorHomo sapiens (human)
protein bindingUrokinase-type plasminogen activatorHomo sapiens (human)
serine-type endopeptidase activityTissue-type plasminogen activatorHomo sapiens (human)
signaling receptor bindingTissue-type plasminogen activatorHomo sapiens (human)
protein bindingTissue-type plasminogen activatorHomo sapiens (human)
phosphoprotein bindingTissue-type plasminogen activatorHomo sapiens (human)
serine-type endopeptidase activityKallikrein-1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (21)

Processvia Protein(s)Taxonomy
extracellular regionPlasminogenHomo sapiens (human)
extracellular spacePlasminogenHomo sapiens (human)
plasma membranePlasminogenHomo sapiens (human)
external side of plasma membranePlasminogenHomo sapiens (human)
cell surfacePlasminogenHomo sapiens (human)
platelet alpha granule lumenPlasminogenHomo sapiens (human)
collagen-containing extracellular matrixPlasminogenHomo sapiens (human)
extracellular exosomePlasminogenHomo sapiens (human)
blood microparticlePlasminogenHomo sapiens (human)
Schaffer collateral - CA1 synapsePlasminogenHomo sapiens (human)
glutamatergic synapsePlasminogenHomo sapiens (human)
extracellular spacePlasminogenHomo sapiens (human)
extracellular regionUrokinase-type plasminogen activatorHomo sapiens (human)
extracellular spaceUrokinase-type plasminogen activatorHomo sapiens (human)
plasma membraneUrokinase-type plasminogen activatorHomo sapiens (human)
focal adhesionUrokinase-type plasminogen activatorHomo sapiens (human)
external side of plasma membraneUrokinase-type plasminogen activatorHomo sapiens (human)
cell surfaceUrokinase-type plasminogen activatorHomo sapiens (human)
specific granule membraneUrokinase-type plasminogen activatorHomo sapiens (human)
extracellular exosomeUrokinase-type plasminogen activatorHomo sapiens (human)
tertiary granule membraneUrokinase-type plasminogen activatorHomo sapiens (human)
serine protease inhibitor complexUrokinase-type plasminogen activatorHomo sapiens (human)
protein complex involved in cell-matrix adhesionUrokinase-type plasminogen activatorHomo sapiens (human)
serine-type endopeptidase complexUrokinase-type plasminogen activatorHomo sapiens (human)
extracellular spaceUrokinase-type plasminogen activatorHomo sapiens (human)
collagen-containing extracellular matrixTissue-type plasminogen activatorHomo sapiens (human)
extracellular regionTissue-type plasminogen activatorHomo sapiens (human)
cytoplasmTissue-type plasminogen activatorHomo sapiens (human)
cell surfaceTissue-type plasminogen activatorHomo sapiens (human)
secretory granuleTissue-type plasminogen activatorHomo sapiens (human)
apical part of cellTissue-type plasminogen activatorHomo sapiens (human)
extracellular exosomeTissue-type plasminogen activatorHomo sapiens (human)
serine protease inhibitor complexTissue-type plasminogen activatorHomo sapiens (human)
Schaffer collateral - CA1 synapseTissue-type plasminogen activatorHomo sapiens (human)
glutamatergic synapseTissue-type plasminogen activatorHomo sapiens (human)
extracellular spaceTissue-type plasminogen activatorHomo sapiens (human)
nucleusKallikrein-1Homo sapiens (human)
extracellular exosomeKallikrein-1Homo sapiens (human)
secretory granuleKallikrein-1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (15)

Assay IDTitleYearJournalArticle
AID238464Binding affinity value against kallikrein2005Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
AID238379Binding affinity value against trypsin2005Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
AID237274Terminal half life value in sprague dawley rat was determined at a dosage of 3 mg/kg2005Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
AID238775Binding affinity value against Tissue plasminogen activator2005Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
AID419413Inhibition of urokinase2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Large-scale application of high-throughput molecular mechanics with Poisson-Boltzmann surface area for routine physics-based scoring of protein-ligand complexes.
AID236447Area under the curve time curve value in sprague dawley rat was determined at a dosage of 3 mg/kg2005Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
AID1495490Inhibition of ASIC1a in rat dorsal root ganglion neurons assessed as reduction in peak current preincubated for 120 secs followed by acid medium stimulation at pH 5.5 for 3 secs by automated patch clamp electrophysiology assay2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Novel amidrazone derivatives: Design, synthesis and activity evaluation.
AID238828Binding affinity value against urokinase plasminogen activator2005Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
AID236071Bioavailability in rat (Sprague-Dawley) (dose 10 mg/kg)2005Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
AID236159Clearance value in sprague dawley rat was determined at a dosage of 3 mg/kg2005Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
AID726071Inhibition of ASIC3 in rat DRG neurons2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Ion channels as therapeutic targets: a drug discovery perspective.
AID236307Volume distribution value in sprague dawley rat was determined at a dosage of 3 mg/kg2005Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
AID238378Binding affinity value against plasmin2005Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
AID238407Binding affinity value against thrombin2005Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
AID1346898Rat ASIC1 (Acid-sensing (proton-gated) ion channels (ASICs))2005Pain, Sep, Volume: 117, Issue:1-2
Electrophysiological and in vivo characterization of A-317567, a novel blocker of acid sensing ion channels.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's7 (58.33)29.6817
2010's5 (41.67)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.76

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 Index11.76 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index4.32 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.76)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (8.33%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (91.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]