Page last updated: 2024-12-11

cgs 35066

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Description

CGS 35066: an endothelin-converting enzyme-1 inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9863167
CHEMBL ID146936
SCHEMBL ID7697566
MeSH IDM0358514

Synonyms (16)

Synonym
cgs 35066
cgs-35066
(s)-3-(dibenzo[b,d]furan-3-yl)-2-(phosphonomethylamino)propanoic acid
3-dibenzofuran-3-yl-2-(phosphonomethyl-amino)-propionic acid
bdbm50084893
CHEMBL146936 ,
(2s)-3-dibenzofuran-3-yl-2-(phosphonomethylamino)propanoic acid
SCHEMBL7697566
?-[(s)-(phosphonomethyl)amino]-3-dibenzofuranpropanoic acid
261619-50-5
AKOS024457142
J-016288
3-dibenzofuranpropanoic acid, alpha-((phosphonomethyl)amino)-, (alphas)-
(s)-3-dibenzofuran-3-yl-2-[phosphonomethylamino]-propionic acid
(s)-3-(dibenzo[b,d]furan-3-yl)-2-((phosphonomethyl)amino)propanoic acid
alpha-[(s)-(phosphonomethyl)amino]-3-dibenzofuranpropanoic acid

Research Excerpts

Treatment

ExcerptReferenceRelevance
"Treatment with CGS 35066 significantly attenuated basilar arterial narrowing at a dose of 1 mg/kg in both protocols."( Attenuation of SAH-induced cerebral vasospasm by a selective ECE inhibitor.
Chang, CZ; Howng, SL; Jeng, AY; Kwan, AL; Lin, CL; Wu, SC, 2002
)
0.65

Dosage Studied

ExcerptRelevanceReference
"8-fold rightward shift of dose-response curve; P<0."( Role of endothelin-converting enzyme, chymase and neutral endopeptidase in the processing of big ET-1, ET-1(1-21) and ET-1(1-31) in the trachea of allergic mice.
De Campo, BA; Goldie, RG; Henry, PJ; Jeng, AY, 2002
)
0.31
" The dose-response curve for ET-1 was shifted to the left in the diabetics, so that at some lower doses of ET-1 the vasoconstriction was greater than in the controls."( Diabetes-associated changes and role of N epsilon-(carboxymethyl)lysine in big ET-1-induced coronary vasoconstriction.
Kamata, K; Kobayashi, T; Matsumoto, T; Ozawa, Y; Taguchi, K, 2010
)
0.36
[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)
NeprilysinRattus norvegicus (Norway rat)IC50 (µMol)2.30000.00100.17022.3000AID143636
NeprilysinOryctolagus cuniculus (rabbit)IC50 (µMol)2.30000.00040.66118.2000AID147216
NeprilysinHomo sapiens (human)IC50 (µMol)2.30000.00020.54226.7000AID444547
Angiotensin-converting enzyme Homo sapiens (human)IC50 (µMol)1.16100.00010.533610.0000AID444547; AID444548
Endothelin-converting enzyme 1Homo sapiens (human)IC50 (µMol)0.02200.01200.56782.0000AID228593; AID444548; AID67196
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (87)

Processvia Protein(s)Taxonomy
kidney developmentNeprilysinHomo sapiens (human)
placenta developmentNeprilysinHomo sapiens (human)
proteolysisNeprilysinHomo sapiens (human)
peptide metabolic processNeprilysinHomo sapiens (human)
learning or memoryNeprilysinHomo sapiens (human)
substance P catabolic processNeprilysinHomo sapiens (human)
bradykinin catabolic processNeprilysinHomo sapiens (human)
sensory perception of painNeprilysinHomo sapiens (human)
protein catabolic processNeprilysinHomo sapiens (human)
lung developmentNeprilysinHomo sapiens (human)
hormone catabolic processNeprilysinHomo sapiens (human)
response to estrogenNeprilysinHomo sapiens (human)
creatinine metabolic processNeprilysinHomo sapiens (human)
amyloid-beta metabolic processNeprilysinHomo sapiens (human)
positive regulation of neurogenesisNeprilysinHomo sapiens (human)
neuropeptide processingNeprilysinHomo sapiens (human)
cellular response to cytokine stimulusNeprilysinHomo sapiens (human)
cellular response to UV-ANeprilysinHomo sapiens (human)
cellular response to UV-BNeprilysinHomo sapiens (human)
replicative senescenceNeprilysinHomo sapiens (human)
amyloid-beta clearanceNeprilysinHomo sapiens (human)
amyloid-beta clearance by cellular catabolic processNeprilysinHomo sapiens (human)
positive regulation of long-term synaptic potentiationNeprilysinHomo sapiens (human)
protein processingNeprilysinHomo sapiens (human)
response to hypoxiaAngiotensin-converting enzyme Homo sapiens (human)
kidney developmentAngiotensin-converting enzyme Homo sapiens (human)
blood vessel remodelingAngiotensin-converting enzyme Homo sapiens (human)
angiotensin maturationAngiotensin-converting enzyme Homo sapiens (human)
regulation of renal output by angiotensinAngiotensin-converting enzyme Homo sapiens (human)
neutrophil mediated immunityAngiotensin-converting enzyme Homo sapiens (human)
antigen processing and presentation of peptide antigen via MHC class IAngiotensin-converting enzyme Homo sapiens (human)
regulation of systemic arterial blood pressure by renin-angiotensinAngiotensin-converting enzyme Homo sapiens (human)
proteolysisAngiotensin-converting enzyme Homo sapiens (human)
spermatogenesisAngiotensin-converting enzyme Homo sapiens (human)
female pregnancyAngiotensin-converting enzyme Homo sapiens (human)
regulation of blood pressureAngiotensin-converting enzyme Homo sapiens (human)
male gonad developmentAngiotensin-converting enzyme Homo sapiens (human)
response to xenobiotic stimulusAngiotensin-converting enzyme Homo sapiens (human)
embryo development ending in birth or egg hatchingAngiotensin-converting enzyme Homo sapiens (human)
post-transcriptional regulation of gene expressionAngiotensin-converting enzyme Homo sapiens (human)
negative regulation of gene expressionAngiotensin-converting enzyme Homo sapiens (human)
substance P catabolic processAngiotensin-converting enzyme Homo sapiens (human)
bradykinin catabolic processAngiotensin-converting enzyme Homo sapiens (human)
regulation of smooth muscle cell migrationAngiotensin-converting enzyme Homo sapiens (human)
regulation of vasoconstrictionAngiotensin-converting enzyme Homo sapiens (human)
animal organ regenerationAngiotensin-converting enzyme Homo sapiens (human)
response to nutrient levelsAngiotensin-converting enzyme Homo sapiens (human)
response to lipopolysaccharideAngiotensin-converting enzyme Homo sapiens (human)
mononuclear cell proliferationAngiotensin-converting enzyme Homo sapiens (human)
response to laminar fluid shear stressAngiotensin-converting enzyme Homo sapiens (human)
angiotensin-activated signaling pathwayAngiotensin-converting enzyme Homo sapiens (human)
vasoconstrictionAngiotensin-converting enzyme Homo sapiens (human)
hormone metabolic processAngiotensin-converting enzyme Homo sapiens (human)
hormone catabolic processAngiotensin-converting enzyme Homo sapiens (human)
eating behaviorAngiotensin-converting enzyme Homo sapiens (human)
positive regulation of apoptotic processAngiotensin-converting enzyme Homo sapiens (human)
peptide catabolic processAngiotensin-converting enzyme Homo sapiens (human)
positive regulation of vasoconstrictionAngiotensin-converting enzyme Homo sapiens (human)
negative regulation of glucose importAngiotensin-converting enzyme Homo sapiens (human)
regulation of synaptic plasticityAngiotensin-converting enzyme Homo sapiens (human)
lung alveolus developmentAngiotensin-converting enzyme Homo sapiens (human)
amyloid-beta metabolic processAngiotensin-converting enzyme Homo sapiens (human)
arachidonic acid secretionAngiotensin-converting enzyme Homo sapiens (human)
positive regulation of neurogenesisAngiotensin-converting enzyme Homo sapiens (human)
heart contractionAngiotensin-converting enzyme Homo sapiens (human)
regulation of angiotensin metabolic processAngiotensin-converting enzyme Homo sapiens (human)
hematopoietic stem cell differentiationAngiotensin-converting enzyme Homo sapiens (human)
angiogenesis involved in coronary vascular morphogenesisAngiotensin-converting enzyme Homo sapiens (human)
cellular response to glucose stimulusAngiotensin-converting enzyme Homo sapiens (human)
response to dexamethasoneAngiotensin-converting enzyme Homo sapiens (human)
cell proliferation in bone marrowAngiotensin-converting enzyme Homo sapiens (human)
regulation of heart rate by cardiac conductionAngiotensin-converting enzyme Homo sapiens (human)
negative regulation of calcium ion importAngiotensin-converting enzyme Homo sapiens (human)
response to thyroid hormoneAngiotensin-converting enzyme Homo sapiens (human)
blood vessel diameter maintenanceAngiotensin-converting enzyme Homo sapiens (human)
regulation of hematopoietic stem cell proliferationAngiotensin-converting enzyme Homo sapiens (human)
negative regulation of gap junction assemblyAngiotensin-converting enzyme Homo sapiens (human)
cellular response to aldosteroneAngiotensin-converting enzyme Homo sapiens (human)
positive regulation of peptidyl-cysteine S-nitrosylationAngiotensin-converting enzyme Homo sapiens (human)
positive regulation of systemic arterial blood pressureAngiotensin-converting enzyme Homo sapiens (human)
positive regulation of receptor recyclingEndothelin-converting enzyme 1Homo sapiens (human)
regulation of systemic arterial blood pressure by endothelinEndothelin-converting enzyme 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayEndothelin-converting enzyme 1Homo sapiens (human)
heart developmentEndothelin-converting enzyme 1Homo sapiens (human)
substance P catabolic processEndothelin-converting enzyme 1Homo sapiens (human)
bradykinin catabolic processEndothelin-converting enzyme 1Homo sapiens (human)
calcitonin catabolic processEndothelin-converting enzyme 1Homo sapiens (human)
protein processingEndothelin-converting enzyme 1Homo sapiens (human)
peptide hormone processingEndothelin-converting enzyme 1Homo sapiens (human)
regulation of vasoconstrictionEndothelin-converting enzyme 1Homo sapiens (human)
endothelin maturationEndothelin-converting enzyme 1Homo sapiens (human)
embryonic heart tube developmentEndothelin-converting enzyme 1Homo sapiens (human)
hormone catabolic processEndothelin-converting enzyme 1Homo sapiens (human)
embryonic digit morphogenesisEndothelin-converting enzyme 1Homo sapiens (human)
ear developmentEndothelin-converting enzyme 1Homo sapiens (human)
pharyngeal system developmentEndothelin-converting enzyme 1Homo sapiens (human)
axonogenesis involved in innervationEndothelin-converting enzyme 1Homo sapiens (human)
sympathetic neuron axon guidanceEndothelin-converting enzyme 1Homo sapiens (human)
semaphorin-plexin signaling pathway involved in axon guidanceEndothelin-converting enzyme 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (23)

Processvia Protein(s)Taxonomy
phosphatidylserine bindingNeprilysinHomo sapiens (human)
endopeptidase activityNeprilysinHomo sapiens (human)
metalloendopeptidase activityNeprilysinHomo sapiens (human)
protein bindingNeprilysinHomo sapiens (human)
exopeptidase activityNeprilysinHomo sapiens (human)
zinc ion bindingNeprilysinHomo sapiens (human)
peptide bindingNeprilysinHomo sapiens (human)
protein homodimerization activityNeprilysinHomo sapiens (human)
oligopeptidase activityNeprilysinHomo sapiens (human)
cardiolipin bindingNeprilysinHomo sapiens (human)
endopeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
carboxypeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
metalloendopeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
calmodulin bindingAngiotensin-converting enzyme Homo sapiens (human)
peptidase activityAngiotensin-converting enzyme Homo sapiens (human)
metallopeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
exopeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
tripeptidyl-peptidase activityAngiotensin-converting enzyme Homo sapiens (human)
peptidyl-dipeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
zinc ion bindingAngiotensin-converting enzyme Homo sapiens (human)
chloride ion bindingAngiotensin-converting enzyme Homo sapiens (human)
mitogen-activated protein kinase kinase bindingAngiotensin-converting enzyme Homo sapiens (human)
bradykinin receptor bindingAngiotensin-converting enzyme Homo sapiens (human)
mitogen-activated protein kinase bindingAngiotensin-converting enzyme Homo sapiens (human)
metallodipeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
heterocyclic compound bindingAngiotensin-converting enzyme Homo sapiens (human)
endopeptidase activityEndothelin-converting enzyme 1Homo sapiens (human)
metalloendopeptidase activityEndothelin-converting enzyme 1Homo sapiens (human)
protein bindingEndothelin-converting enzyme 1Homo sapiens (human)
zinc ion bindingEndothelin-converting enzyme 1Homo sapiens (human)
peptide hormone bindingEndothelin-converting enzyme 1Homo sapiens (human)
protein homodimerization activityEndothelin-converting enzyme 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (32)

Processvia Protein(s)Taxonomy
cytoplasmNeprilysinHomo sapiens (human)
early endosomeNeprilysinHomo sapiens (human)
trans-Golgi networkNeprilysinHomo sapiens (human)
plasma membraneNeprilysinHomo sapiens (human)
brush borderNeprilysinHomo sapiens (human)
focal adhesionNeprilysinHomo sapiens (human)
synaptic vesicleNeprilysinHomo sapiens (human)
cell surfaceNeprilysinHomo sapiens (human)
membraneNeprilysinHomo sapiens (human)
axonNeprilysinHomo sapiens (human)
dendriteNeprilysinHomo sapiens (human)
secretory granule membraneNeprilysinHomo sapiens (human)
cytoplasmic vesicleNeprilysinHomo sapiens (human)
neuronal cell bodyNeprilysinHomo sapiens (human)
neuron projection terminusNeprilysinHomo sapiens (human)
membrane raftNeprilysinHomo sapiens (human)
synapseNeprilysinHomo sapiens (human)
extracellular exosomeNeprilysinHomo sapiens (human)
presynapseNeprilysinHomo sapiens (human)
plasma membraneNeprilysinHomo sapiens (human)
extracellular spaceAngiotensin-converting enzyme Homo sapiens (human)
extracellular regionAngiotensin-converting enzyme Homo sapiens (human)
extracellular spaceAngiotensin-converting enzyme Homo sapiens (human)
lysosomeAngiotensin-converting enzyme Homo sapiens (human)
endosomeAngiotensin-converting enzyme Homo sapiens (human)
plasma membraneAngiotensin-converting enzyme Homo sapiens (human)
external side of plasma membraneAngiotensin-converting enzyme Homo sapiens (human)
basal plasma membraneAngiotensin-converting enzyme Homo sapiens (human)
brush border membraneAngiotensin-converting enzyme Homo sapiens (human)
extracellular exosomeAngiotensin-converting enzyme Homo sapiens (human)
sperm midpieceAngiotensin-converting enzyme Homo sapiens (human)
plasma membraneAngiotensin-converting enzyme Homo sapiens (human)
lysosomal membraneEndothelin-converting enzyme 1Homo sapiens (human)
endosomeEndothelin-converting enzyme 1Homo sapiens (human)
plasma membraneEndothelin-converting enzyme 1Homo sapiens (human)
external side of plasma membraneEndothelin-converting enzyme 1Homo sapiens (human)
endosome membraneEndothelin-converting enzyme 1Homo sapiens (human)
membraneEndothelin-converting enzyme 1Homo sapiens (human)
vesicleEndothelin-converting enzyme 1Homo sapiens (human)
Weibel-Palade bodyEndothelin-converting enzyme 1Homo sapiens (human)
perinuclear region of cytoplasmEndothelin-converting enzyme 1Homo sapiens (human)
extracellular exosomeEndothelin-converting enzyme 1Homo sapiens (human)
plasma membraneEndothelin-converting enzyme 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (8)

Assay IDTitleYearJournalArticle
AID235174Selectivity ratio of IC50 NEP/IC50 ECE2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Potent and selective non-peptidic inhibitors of endothelin-converting enzyme-1 with sustained duration of action.
AID228593In Vitro inhibition of recombinant human endothelin converting enzyme-12000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Potent and selective non-peptidic inhibitors of endothelin-converting enzyme-1 with sustained duration of action.
AID67338Inhibition of Endothelin-converting enzyme 1 activity at a concentration of 1 uM2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Potent and selective non-peptidic inhibitors of endothelin-converting enzyme-1 with sustained duration of action.
AID143636In vitro inhibition of rat neutral endopeptidase2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Potent and selective non-peptidic inhibitors of endothelin-converting enzyme-1 with sustained duration of action.
AID67196Inhibition of Endothelin-converting enzyme 1 (ECE)2002Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7
Toward an optimal joint recognition of the S1' subsites of endothelin converting enzyme-1 (ECE-1), angiotensin converting enzyme (ACE), and neutral endopeptidase (NEP).
AID444547Inhibition of human somatic NEP2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Phosphinic tripeptides as dual angiotensin-converting enzyme C-domain and endothelin-converting enzyme-1 inhibitors.
AID147216Inhibition of neutral endopeptidase (NEP)2002Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7
Toward an optimal joint recognition of the S1' subsites of endothelin converting enzyme-1 (ECE-1), angiotensin converting enzyme (ACE), and neutral endopeptidase (NEP).
AID444548Inhibition of human somatic ECE12010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Phosphinic tripeptides as dual angiotensin-converting enzyme C-domain and endothelin-converting enzyme-1 inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (18)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's14 (77.78)29.6817
2010's4 (22.22)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: 11.70

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 Index11.70 (24.57)
Research Supply Index2.94 (2.92)
Research Growth Index4.64 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.70)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (5.56%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other17 (94.44%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]