Page last updated: 2024-09-25

l 158809

Description

L 158809: RN & structure given in first source; angiotensin receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID183134
CHEMBL ID7550
SCHEMBL ID683357
MeSH IDM0193006

Synonyms (27)

Synonym
l-158809
l 158809
L004397
CHEMBL7550 ,
2-ethyl-5,7-dimethyl-3-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]imidazo[4,5-b]pyridine
2-ethyl-5,7-dimethyl-3-[2''-(2h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3h-imidazo[4,5-b]pyridine(l-158809)
2-ethyl-5,7-dimethyl-3-[2''-(1h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3h-imidazo[4,5-b]pyridine (l158809)
2-ethyl-5,7-dimethyl-3-[2''-(1h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3h-imidazo[4,5-b]pyridine
2-ethyl-5,7-dimethyl-3-[2''-(2h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3h-imidazo[4,5-b]pyridine
2-ethyl-5,7-dimethyl-3-[2''-(1h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3h-imidazo[4,5-b]pyridine (l-158809)
bdbm50009718
133240-46-7
2-ethyl-5,7-dimethyl-3-((4-(2-(2h-tetrazol-5-yl)phenyl)phenyl)methyl)imidazo(4,5-b)pyridine
3h-imidazo(4,5-b)pyridine, 2-ethyl-5,7-dimethyl-3-((2'-(2h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-
[3h]l-158,809
[3h]-l158809
gtpl3939
[3h]l158809
2-ethyl-5,7-dimethyl-3-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]imidazo[5,4-b]pyridine
SCHEMBL683357
YFWXFHNZGKNDBC-UHFFFAOYSA-N ,
2-ethyl-5,7-dimethyl-3-[(2'-(1h-tetrazol-5-yl)biphenyl-4-yl)methyl]-3h-imidazo[4,5-b]pyridine
DTXSID00928018
2-ethyl-5,7-dimethyl-3-{[2'-(2h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl}-3h-imidazo[4,5-b]pyridine
3-((2'-(2h-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-ethyl-5,7-dimethyl-3h-imidazo[4,5-b]pyridine
2-ethyl-5,7-dimethyl-3-[2'-(1h-tetrazole-5-yl)biphenyl-4-ylmethyl]-3h-imidazo[4,5-b]pyridine
AKOS040745965

Protein Targets (8)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Type-1A angiotensin II receptor Rattus norvegicus (Norway rat)IC50 (µMol)0.00210.00040.15553.8000AID39505
Type-1A angiotensin II receptor Rattus norvegicus (Norway rat)Ki0.00040.00020.10251.7000AID39022
Type-1B angiotensin II receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00120.00040.13343.8000AID37687; AID39505
Type-1 angiotensin II receptorHomo sapiens (human)IC50 (µMol)0.00150.00020.09323.6000AID607037; AID711558
Type-1 angiotensin II receptorOryctolagus cuniculus (rabbit)IC50 (µMol)0.00030.00010.09130.5000AID37549; AID568899
Type-2 angiotensin II receptorRattus norvegicus (Norway rat)IC50 (µMol)16.00040.00100.39573.3000AID38161; AID38276; AID38284; AID39505; AID39524
Type-2 angiotensin II receptorHomo sapiens (human)IC50 (µMol)0.00020.00010.02890.2000AID568926
Type-2 angiotensin II receptorHomo sapiens (human)Ki0.00040.00020.56507.7790AID39022
5-hydroxytryptamine receptor 1AMus musculus (house mouse)IC50 (µMol)0.00210.00210.35812.0000AID39505
[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)
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)EC50 (µMol)20.00000.00000.992210.0000AID607038
[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)
Type-1 angiotensin II receptorHomo sapiens (human)Affinity0.00050.00050.03150.2300AID243379
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (119)

Processvia Protein(s)Taxonomy
regulation of cell growthType-1 angiotensin II receptorHomo sapiens (human)
kidney developmentType-1 angiotensin II receptorHomo sapiens (human)
renin-angiotensin regulation of aldosterone productionType-1 angiotensin II receptorHomo sapiens (human)
maintenance of blood vessel diameter homeostasis by renin-angiotensinType-1 angiotensin II receptorHomo sapiens (human)
regulation of systemic arterial blood pressure by renin-angiotensinType-1 angiotensin II receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayType-1 angiotensin II receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationType-1 angiotensin II receptorHomo sapiens (human)
Rho protein signal transductionType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationType-1 angiotensin II receptorHomo sapiens (human)
regulation of vasoconstrictionType-1 angiotensin II receptorHomo sapiens (human)
calcium-mediated signalingType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of phospholipase A2 activityType-1 angiotensin II receptorHomo sapiens (human)
low-density lipoprotein particle remodelingType-1 angiotensin II receptorHomo sapiens (human)
regulation of renal sodium excretionType-1 angiotensin II receptorHomo sapiens (human)
angiotensin-activated signaling pathwayType-1 angiotensin II receptorHomo sapiens (human)
regulation of cell population proliferationType-1 angiotensin II receptorHomo sapiens (human)
symbiont entry into host cellType-1 angiotensin II receptorHomo sapiens (human)
regulation of inflammatory responseType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of inflammatory responseType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of protein metabolic processType-1 angiotensin II receptorHomo sapiens (human)
cell chemotaxisType-1 angiotensin II receptorHomo sapiens (human)
phospholipase C-activating angiotensin-activated signaling pathwayType-1 angiotensin II receptorHomo sapiens (human)
blood vessel diameter maintenanceType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of blood vessel endothelial cell proliferation involved in sprouting angiogenesisType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of CoA-transferase activityType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of reactive oxygen species metabolic processType-1 angiotensin II receptorHomo sapiens (human)
inflammatory responseType-1 angiotensin II receptorHomo sapiens (human)
negative regulation of gene expressionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of cholesterol effluxPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
long-chain fatty acid transportPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of osteoblast differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of smooth muscle cell proliferationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of receptor signaling pathway via STATPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of low-density lipoprotein receptor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of signaling receptor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of gene expressionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of BMP signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of MAP kinase activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of adiponectin secretionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of miRNA transcriptionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of cardiac muscle hypertrophy in response to stressPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of connective tissue replacement involved in inflammatory response wound healingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
placenta developmentPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
regulation of transcription by RNA polymerase IIPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
lipid metabolic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
signal transductionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
G protein-coupled receptor signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
response to nutrientPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
regulation of blood pressurePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of gene expressionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of gene expressionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
macrophage derived foam cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of macrophage derived foam cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of cholesterol storagePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of lipid storagePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of sequestering of triglyceridePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of angiogenesisPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
monocyte differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
BMP signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
epithelial cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cellular response to insulin stimulusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
response to lipidPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
peroxisome proliferator activated receptor signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
glucose homeostasisPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
regulation of circadian rhythmPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
mRNA transcription by RNA polymerase IIPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
lipoprotein transportPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of blood vessel endothelial cell migrationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
innate immune responsePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cell fate commitmentPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of fat cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of DNA-templated transcriptionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of DNA-templated transcriptionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
retinoic acid receptor signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cell maturationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
rhythmic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
white fat cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of DNA-binding transcription factor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
lipid homeostasisPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of type II interferon-mediated signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of SMAD protein signal transductionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
regulation of cholesterol transporter activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cellular response to low-density lipoprotein particle stimulusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cellular response to hypoxiaPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of mitochondrial fissionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
regulation of cellular response to insulin stimulusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of extracellular matrix assemblyPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of miRNA transcriptionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of miRNA transcriptionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of cellular response to transforming growth factor beta stimulusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of adipose tissue developmentPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of vascular associated smooth muscle cell proliferationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell apoptotic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of vascular endothelial cell proliferationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of fatty acid metabolic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
fatty acid metabolic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of inflammatory responsePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
hormone-mediated signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
blood vessel remodelingType-2 angiotensin II receptorHomo sapiens (human)
regulation of systemic arterial blood pressure by circulatory renin-angiotensinType-2 angiotensin II receptorHomo sapiens (human)
angiotensin-mediated vasodilation involved in regulation of systemic arterial blood pressureType-2 angiotensin II receptorHomo sapiens (human)
brain renin-angiotensin systemType-2 angiotensin II receptorHomo sapiens (human)
cell surface receptor signaling pathwayType-2 angiotensin II receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayType-2 angiotensin II receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway coupled to cGMP nucleotide second messengerType-2 angiotensin II receptorHomo sapiens (human)
brain developmentType-2 angiotensin II receptorHomo sapiens (human)
regulation of blood pressureType-2 angiotensin II receptorHomo sapiens (human)
negative regulation of heart rateType-2 angiotensin II receptorHomo sapiens (human)
negative regulation of cell growthType-2 angiotensin II receptorHomo sapiens (human)
positive regulation of phosphoprotein phosphatase activityType-2 angiotensin II receptorHomo sapiens (human)
regulation of metanephros sizeType-2 angiotensin II receptorHomo sapiens (human)
exploration behaviorType-2 angiotensin II receptorHomo sapiens (human)
nitric oxide-cGMP-mediated signalingType-2 angiotensin II receptorHomo sapiens (human)
angiotensin-activated signaling pathwayType-2 angiotensin II receptorHomo sapiens (human)
vasodilationType-2 angiotensin II receptorHomo sapiens (human)
negative regulation of blood vessel endothelial cell migrationType-2 angiotensin II receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionType-2 angiotensin II receptorHomo sapiens (human)
negative regulation of neurotrophin TRK receptor signaling pathwayType-2 angiotensin II receptorHomo sapiens (human)
neuron apoptotic processType-2 angiotensin II receptorHomo sapiens (human)
positive regulation of metanephric glomerulus developmentType-2 angiotensin II receptorHomo sapiens (human)
positive regulation of branching involved in ureteric bud morphogenesisType-2 angiotensin II receptorHomo sapiens (human)
positive regulation of extrinsic apoptotic signaling pathwayType-2 angiotensin II receptorHomo sapiens (human)
inflammatory responseType-2 angiotensin II receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (33)

Processvia Protein(s)Taxonomy
angiotensin type I receptor activityType-1 angiotensin II receptorHomo sapiens (human)
angiotensin type II receptor activityType-1 angiotensin II receptorHomo sapiens (human)
protein bindingType-1 angiotensin II receptorHomo sapiens (human)
bradykinin receptor bindingType-1 angiotensin II receptorHomo sapiens (human)
protein heterodimerization activityType-1 angiotensin II receptorHomo sapiens (human)
transcription cis-regulatory region bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
transcription coregulator bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
nucleic acid bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
chromatin bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
double-stranded DNA bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA-binding transcription factor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
nuclear receptor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
prostaglandin receptor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
protein bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
zinc ion bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
enzyme bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
peptide bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
identical protein bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
sequence-specific DNA bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
nuclear retinoid X receptor bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
arachidonic acid bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA binding domain bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
LBD domain bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
alpha-actinin bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
R-SMAD bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
E-box bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
STAT family protein bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA-binding transcription factor bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
angiotensin type II receptor activityType-2 angiotensin II receptorHomo sapiens (human)
protein bindingType-2 angiotensin II receptorHomo sapiens (human)
receptor antagonist activityType-2 angiotensin II receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
plasma membraneType-1 angiotensin II receptorHomo sapiens (human)
membraneType-1 angiotensin II receptorHomo sapiens (human)
plasma membraneType-1 angiotensin II receptorHomo sapiens (human)
nucleusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
nucleusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
nucleoplasmPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cytosolPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
intracellular membrane-bounded organellePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
RNA polymerase II transcription regulator complexPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
chromatinPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
receptor complexPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
plasma membraneType-2 angiotensin II receptorHomo sapiens (human)
plasma membraneType-2 angiotensin II receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (68)

Assay IDTitleYearJournalArticle
AID17957Apparent bioavailability after oral dose of 3.87 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID243379Binding affinity for AT1 receptor2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Pharmacophore, drug metabolism, and pharmacokinetics models on non-peptide AT1, AT2, and AT1/AT2 angiotensin II receptor antagonists.
AID568899Binding affinity to angiotensin AT1 receptor in rabbit aortic rings2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID192970The compound was evaluated for the percentage of inhibition of A II pressor response in rat for intravenous administration1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
A highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1-selective angiotensin II receptor antagonist.
AID197549Percentage peak pressor response in rat after intravenous administration at a dose of 0.03 mg/kg of the compound.1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
Potent, orally active imidazo[4,5-b]pyridine-based angiotensin II receptor antagonists.
AID38276In vitro antagonist activity against angiotensin II receptor type 2 in rat midbrain using [125I]-Sar,Ile AII.1993Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26
Non-peptide angiotensin II receptor antagonists. 1. Design, synthesis, and biological activity of N-substituted indoles and dihydroindoles.
AID22406Volume of distribution of the terminal phase (= CLp+ plasma elimination rate constant) after intravenous dose of 3.87 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID167369Compound was tested for its antagonistic activity against angiotensin II-induced contractions in rabbit aorta1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID39505Binding affinity against AT1 receptor of rat adrenal cortical membranes1994Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
Non-peptide angiotensin II receptor antagonists: synthesis and biological activity of a series of novel 4,5-dihydro-4-oxo-3H-imidazo[4,5-c]pyridine derivatives.
AID37514Displacement of [1251][Sar1,IIe8]AII from rabbit aorta Angiotensin II receptor, type 11993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
(Dipropylphenoxy)phenylacetic acids: a new generation of nonpeptide angiotensin II receptor antagonists.
AID234499Ratio of the of A II pressor responses in rat, p.o./i.v.1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
A highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1-selective angiotensin II receptor antagonist.
AID38161In vitro antagonist activity against angiotensin II type 2 (AT2) receptor in rat midbrain using [125I]- Sar, Ile AII.1993Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26
Non-peptide angiotensin II receptor antagonists. 2. Design, synthesis, and biological activity of N-substituted (phenylamino)phenylacetic acids and acyl sulfonamides.
AID24000Half-life period after oral dose of 3.87 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID231153Ratio of the of A II pressor responses in dog, p.o./i.v.; ND= Not determined1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
A highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1-selective angiotensin II receptor antagonist.
AID22398Volume of distribution of central compartment (= dose+ plasma concentration at time zero) after intravenous dose of 3.87 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID167537Compound was tested for its antagonistic activity against angiotensin II-induced contractions in rabbit aorta1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID37687Binding affinity for rat angiotensin II receptor, type 12004Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
Design, synthesis, structural studies, biological evaluation, and computational simulations of novel potent AT(1) angiotensin II receptor antagonists based on the 4-phenylquinoline structure.
AID37542Potency to antagonize the ability of angiotensin II to contract rabbit aorta1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID39047Inhibition of Angiotensin II induced contractions in rabbit aortic rings1994Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
Non-peptide angiotensin II receptor antagonists: synthesis and biological activity of a series of novel 4,5-dihydro-4-oxo-3H-imidazo[4,5-c]pyridine derivatives.
AID174386% decrease in blood pressure after 4 hours in male rats at a dose of 0.1 mg/kg by using Renal artery hypertensive model1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID39503In vitro binding affinity for angiotensin II AT1 receptor in rabbit aorta1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
A highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1-selective angiotensin II receptor antagonist.
AID197552Percentage peak pressor response in rat after peroral administration at a dose of 0.03 mg/kg of the compound.1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
Potent, orally active imidazo[4,5-b]pyridine-based angiotensin II receptor antagonists.
AID56499The compound was evaluated for the percentage of inhibition of A II pressor response in dogs for intravenous administration1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
A highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1-selective angiotensin II receptor antagonist.
AID39360The compound was tested for inhibition of angiotensin II receptor induced pressor response in rat after intravenous administration.1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
Potent, orally active imidazo[4,5-b]pyridine-based angiotensin II receptor antagonists.
AID37519Inhibitory activity was evaluated against Angiotensin II receptor, type 1 in rabbit aorta1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID56383The compound was evaluated for the percentage of inhibition of A II pressor response in dog for peroral administration; ND= Not determined1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
A highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1-selective angiotensin II receptor antagonist.
AID15900Plasma clearance after intravenous dose of 3.87 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID607038Partial agonist activity at human PPARgamma-LBD/Gal4 DNA binding domain by transactivation assay2011Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12
Discovery of a series of imidazo[4,5-b]pyridines with dual activity at angiotensin II type 1 receptor and peroxisome proliferator-activated receptor-γ.
AID23995Half-life period of compound after intravenous dose of 3.87 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID38284Displacement of [1251][Sar1,IIe8]AII from rat midbrain angiotensin II (AT2) receptor1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
(Dipropylphenoxy)phenylacetic acids: a new generation of nonpeptide angiotensin II receptor antagonists.
AID174388% decrease in blood pressure after 4 hours in male rats at a dose of 0.3 mg/kg by using Renal artery hypertensive model1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID174797The duration of action for the % peak inhibition of angiotensin II pressor response for dose of 0.1 mg/kg perol administration in conscious rats.1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
A highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1-selective angiotensin II receptor antagonist.
AID18416Oral bioavailability was evaluated in rat by oral administration1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID22341Tmax value after oral dose of 3.87 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID231155Ratio of the of A II pressor responses in rhesus monkey, p.o./i.v.1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
A highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1-selective angiotensin II receptor antagonist.
AID176261Intravenous effective dose required for inhibition of Ang II pressor response in conscious rat1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID711558Antagonist activity at angiotensin 1 receptor2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synopsis of some recent tactical application of bioisosteres in drug design.
AID568926Binding affinity to angiotensin AT2 receptor2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID192958The compound was evaluated for the % peak inhibition of angiotensin II pressor response for dose of 0.1 mg/kg intravenous administration in conscious rats.1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
A highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1-selective angiotensin II receptor antagonist.
AID607039Partial agonist activity at human PPARgamma-LBD/Gal4 DNA binding domain by transactivation assay relative to darglitazone2011Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12
Discovery of a series of imidazo[4,5-b]pyridines with dual activity at angiotensin II type 1 receptor and peroxisome proliferator-activated receptor-γ.
AID607037Displacement of [125I]Tyr4-Sar1,Ile8-Angiotensin II from human Angiotensin 1 receptor after 60 mins by scintillation counting2011Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12
Discovery of a series of imidazo[4,5-b]pyridines with dual activity at angiotensin II type 1 receptor and peroxisome proliferator-activated receptor-γ.
AID197554Percentage peak pressor response in rat after peroral administration at a dose of 0.3 mg/kg of the compound.1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
Potent, orally active imidazo[4,5-b]pyridine-based angiotensin II receptor antagonists.
AID174247% decrease in blood pressure after 4 hours at a dose of 1 mg/kg in male rats by using Furosemide-treated spontaneous hypertensive model1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID39807In vitro antagonist activity against angiotensin II receptor type 1 in rabbit aorta using [125I]-Sar, Ile AII.1993Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26
Non-peptide angiotensin II receptor antagonists. 1. Design, synthesis, and biological activity of N-substituted indoles and dihydroindoles.
AID174250% decrease in blood pressure after 4 hours at a dose of 3 mg/kg in male rats by using Renal artery hypertensive model1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID174254% decrease in blood pressure after 4 hours in male rats at a dose of 0.03 mg/kg by using Renal artery hypertensive model1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID39808In vitro antagonist activity against angiotensin II receptor type 1 in rabbit aorta using [125I]-Sar, Ile AII.1993Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26
Non-peptide angiotensin II receptor antagonists. 2. Design, synthesis, and biological activity of N-substituted (phenylamino)phenylacetic acids and acyl sulfonamides.
AID330796Displacement of [125I]Sar1,Ile8-Ang2 from AT1 receptor in Wistar rat hepatic membrane2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Design, synthesis, and biological evaluation of AT1 angiotensin II receptor antagonists based on the pyrazolo[3,4-b]pyridine and related heteroaromatic bicyclic systems.
AID176434Oral effective dose required for inhibition of Ang II pressor response in conscious rat1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID18419Oral bioavailability was evaluated in rhesus monkey1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID125514The compound was evaluated for the percentage of inhibition of A II pressor response in rhesus monkey for peroral administration.1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
A highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1-selective angiotensin II receptor antagonist.
AID195024pA2 value was evaluated against angiotensin II-induced aldosterone release in rat adrenal cortical cells1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID197550Percentage peak pressor response in rat after intravenous administration at a dose of 0.1 mg/kg of the compound.1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
Potent, orally active imidazo[4,5-b]pyridine-based angiotensin II receptor antagonists.
AID18415Oral bioavailability in rat1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID192959The compound was evaluated for the % peak inhibition of angiotensin II pressor response for dose of 0.1 mg/kg perol administration in conscious rats.1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
A highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1-selective angiotensin II receptor antagonist.
AID125515The compound was evaluated for the percentage of inhibition of A II pressor response in rhesus monkeys for intravenous administration1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
A highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1-selective angiotensin II receptor antagonist.
AID10481Area under curve after oral dose of 3.87 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID174240% decrease in blood pressure after 24 hours at a dose of 1 mg/kg in male rats by using Furosemide-treated spontaneous hypertensive model1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID39195Binding affinity towards Angiotensin receptor from rabbit aorta1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
Potent, orally active imidazo[4,5-b]pyridine-based angiotensin II receptor antagonists.
AID174796The duration of action for the % peak inhibition of angiotensin II pressor response for dose of 0.1 mg/kg intravenous administration in conscious rats.1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
A highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1-selective angiotensin II receptor antagonist.
AID192971The compound was evaluated for the percentage of inhibition of A II pressor response in rat for peroral administration.1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
A highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1-selective angiotensin II receptor antagonist.
AID37549Inhibition of Angiotensin II receptor, type 11993Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15
Excursions in drug discovery.
AID197553Percentage peak pressor response in rat after peroral administration at a dose of 0.1 mg/kg of the compound.1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
Potent, orally active imidazo[4,5-b]pyridine-based angiotensin II receptor antagonists.
AID39809Displacement of [125I]-Sar1-Ile8-A II at the rabbit aorta angiotensin II receptor, type 11993Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
Nonpeptide angiotensin II antagonists derived from 4H-1,2,4-triazoles and 3H-imidazo[1,2-b][1,2,4]triazoles.
AID197551Percentage peak pressor response in rat after intravenous administration at a dose of 0.3 mg/kg of the compound.1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
Potent, orally active imidazo[4,5-b]pyridine-based angiotensin II receptor antagonists.
AID39022Binding affinity against angiotensin II receptor from rat liver1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID39524In vitro binding affinity for angiotensin II AT2 receptor in rat midbrain1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
A highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1-selective angiotensin II receptor antagonist.
AID15485Cmax value after oral dose of 3.87 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (132)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's70 (53.03)18.2507
2000's52 (39.39)29.6817
2010's10 (7.58)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews4 (2.92%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other133 (97.08%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research Highlights

Safety/Toxicity (1)

ArticleYear
Role of humoral mediators in, and influence of a liposomal formulation on, acute amphotericin B nephrotoxicity.
Pharmacology & toxicology, Volume: 88, Issue: 4
2001
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Long-term Use (1)

ArticleYear
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Pharmacokinetics (1)

ArticleYear
Pharmacophore, drug metabolism, and pharmacokinetics models on non-peptide AT1, AT2, and AT1/AT2 angiotensin II receptor antagonists.
Journal of medicinal chemistry, Jun-30, Volume: 48, Issue: 13
2005
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioavailability (6)

ArticleYear
Discovery of a series of imidazo[4,5-b]pyridines with dual activity at angiotensin II type 1 receptor and peroxisome proliferator-activated receptor-γ.
Journal of medicinal chemistry, Jun-23, Volume: 54, Issue: 12
2011
Design, synthesis, and biological evaluation of AT1 angiotensin II receptor antagonists based on the pyrazolo[3,4-b]pyridine and related heteroaromatic bicyclic systems.
Journal of medicinal chemistry, Apr-10, Volume: 51, Issue: 7
2008
Diphenylpropionic acids as new AT1 selective angiotensin II antagonists.
Journal of medicinal chemistry, May-24, Volume: 39, Issue: 11
1996
Nonpeptide angiotensin II antagonists derived from 4H-1,2,4-triazoles and 3H-imidazo[1,2-b][1,2,4]triazoles.
Journal of medicinal chemistry, Mar-05, Volume: 36, Issue: 5
1993
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
Journal of medicinal chemistry, Sep-03, Volume: 36, Issue: 18
1993
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Dosage (9)

ArticleYear
Antisense oligodeoxynucleotides directed against a novel angiotensinogen mRNA-stabilizing protein reduce blood pressure in spontaneously hypertensive rats.
American journal of physiology. Regulatory, integrative and comparative physiology, Volume: 287, Issue: 3
2004
Possible interactions between angiotensin II and insulin: effects on glucose and lipid metabolism in vivo and in vitro.
The Journal of endocrinology, Volume: 167, Issue: 3
2000
Functional role of angiotensin II type 1 and 2 receptors in regulation of uterine blood flow in nonpregnant sheep.
American journal of physiology. Heart and circulatory physiology, Volume: 278, Issue: 2
2000
Combined effects of angiotensin converting enzyme inhibition and angiotensin II receptor antagonism in conscious pigs with congestive heart failure.
Cardiovascular research, Volume: 39, Issue: 2
1998
Inhibitory effects of a subdepressor dose of L-158,809, an angiotensin II type 1 receptor antagonist, on cardiac hypertrophy and nephropathy via the activated human renin-angiotensin system in double transgenic mice with hypertension.
Japanese circulation journal, Volume: 62, Issue: 8
1998
Improved activity of a new angiotensin receptor antagonist by an injectable spray-dried polymer microsphere preparation.
Pharmaceutical research, Volume: 14, Issue: 7
1997
Dual agonistic and antagonistic property of nonpeptide angiotensin AT1 ligands: susceptibility to receptor mutations.
Molecular pharmacology, Volume: 51, Issue: 2
1997
Blood pressure-independent effect of angiotensin inhibition on vascular lesions of chronic renal failure.
Kidney international, Volume: 42, Issue: 1
1992
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]