Page last updated: 2024-12-07

mk 996

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Description

MK 996: an AT1-selective angiotensin II receptor antagonist; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID133031
CHEMBL ID293511
SCHEMBL ID1826878
MeSH IDM0239879

Synonyms (21)

Synonym
bdbm50038189
4''-(2-ethyl-5,7-dimethyl-imidazo[4,5-b]pyridin-3-ylmethyl)-biphenyl-2-sulfonic acid benzoylamide
157263-00-8
l-159282
l-159,282
3-((2'-(benzoylaminosulfonyl)biphenyl-4-yl)methyl)-2-ethyl-5,7-dimethyl-3h-imidazo(4,5-b)pyridine
benzamide, n-((4'-((2-ethyl-5,7-dimethyl-3h-imidazo(4,5-b)pyridin-3-yl)methyl)(1,1'-biphenyl)-2-yl)sulfonyl)-
l 159282
mk 996
CHEMBL293511 ,
mk-996
l-158282
L009110
n-[2-[4-[(2-ethyl-5,7-dimethylimidazo[4,5-b]pyridin-3-yl)methyl]phenyl]phenyl]sulfonylbenzamide
SCHEMBL1826878
DTXSID80166239
HY-19191
CS-6780
n-((4'-((2-ethyl-5,7-dimethyl-3h-imidazo[4,5-b]pyridin-3-yl)methyl)-[1,1'-biphenyl]-2-yl)sulfonyl)benzamide
benzamide, n-[[4'-[(2-ethyl-5,7-dimethyl-3h-imidazo[4,5-b]pyridin-3-yl)methyl][1,1'-biphenyl]-2-yl]sulfonyl]-
AKOS040741925
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Type-1 angiotensin II receptorHomo sapiens (human)IC50 (µMol)0.00020.00020.09323.6000AID711558
Type-1 angiotensin II receptorOryctolagus cuniculus (rabbit)IC50 (µMol)0.00020.00010.09130.5000AID568899
Type-2 angiotensin II receptorRattus norvegicus (Norway rat)IC50 (µMol)2.90000.00100.39573.3000AID39524
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (28)

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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (2)

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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (44)

Assay IDTitleYearJournalArticle
AID199398Oral effective dose required for inhibition of Ang II pressor response in conscious rhesus monkey1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
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.
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.
AID192969The compound was evaluated for the percentage of inhibition of A II pressor response in dogs 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.
AID192965The compound was evaluated for the % peak inhibition of angiotensin II pressor response for dose of 1.0 mg/kg peroral 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.
AID192957The compound was evaluated for the % peak inhibition of A II pressor response for dose of 1.0 mg/kg peroral administration in conscious dogs.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.
AID192973The 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.
AID568928Antihypertensive activity in po dosed conscious dog assessed as angiotensin 2-induced response2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID174793The duration of action for the % peak inhibition of A II pressor response for dose of 0.3 mg/kg peroral administration in conscious dogs.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.
AID192962The compound was evaluated for the % peak inhibition of angiotensin II pressor response for dose of 0.3 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.
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.
AID231154Ratio 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.
AID192974The compound was evaluated for the percentage of inhibition of A II pressor response in rhesus monkeys 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.
AID167381Inhibition of angiotensin II-induced contractions in rabbit aorta in vitro.1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID192842The compound was evaluated for the % peak inhibition of A II pressor response for dose of 0.1 mg/kg intravenous administration in conscious dogs.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.
AID174791The duration of action for the % peak inhibition of A II pressor response for dose of 0.03 mg/kg intravenous administration in rhesus monkeys.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.
AID568927Antihypertensive activity in po dosed conscious rat assessed as angiotensin 2-induced response2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID192972The compound was evaluated for the percentage of inhibition of A II pressor response in rats 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.
AID174928The duration of action for the % peak inhibition of angiotensin II pressor response for dose of 1.0 mg/kg peroral 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.
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.
AID8648The compound was evaluated for the % peak inhibition of A II pressor response for dose of 0.3 mg/kg peroral administration in rhesus monkeys.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.
AID192844The compound was evaluated for the % peak inhibition of A II pressor response for dose of 0.1 mg/kg peroral administration in rhesus monkeys.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.
AID174798The duration of action for the % peak inhibition of angiotensin II pressor response for dose of 0.3 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.
AID192960The compound was evaluated for the % peak inhibition of angiotensin II pressor response for dose of 0.1 mg/kg peroral 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.
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.
AID174795The duration of action for the % peak inhibition of A II pressor response for dose of 1.0 mg/kg peroral administration in rhesus monkeys.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.
AID8646The duration of action for the % peak inhibition of A II pressor response for dose of 1.0 mg/kg peroral administration in rhesus monkeys.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.
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.
AID192968The 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.
AID174792The duration of action for the % peak inhibition of A II pressor response for dose of 0.1 mg/kg intravenous administration in rhesus monkeys.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.
AID192845The compound was evaluated for the % peak inhibition of A II pressor response for dose of 0.3 mg/kg peroral administration in conscious dogs.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.
AID192843The compound was evaluated for the % peak inhibition of A II pressor response for dose of 0.1 mg/kg intravenous administration in rhesus monkeys.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.
AID60019Oral effective dose required for inhibition of Ang II pressor response in conscious dog1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
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.
AID568783Antagonist activity at angiotensin AT1 receptor in rabbit aorta2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID174794The duration of action for the % peak inhibition of A II pressor response for dose of 1.0 mg/kg peroral administration in conscious dogs.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.
AID231152Ratio of the of A II pressor responses in dog, 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.
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.
AID192841The compound was evaluated for the % peak inhibition of A II pressor response for dose of 0.03 mg/kg intravenous administration in rhesus monkeys.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.
AID8649The compound was evaluated for the percentage of inhibition of A II pressor response in rats 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.
AID8645The duration of action for the % peak inhibition of A II pressor response for dose of 0.1 mg/kg intravenous administration in conscious dogs.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.
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.
AID8647The duration of action for the % peak inhibition of angiotensin II pressor response for dose of 0.1 mg/kg peroral 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.
AID568929Antihypertensive activity in po dosed conscious rhesus monkey assessed as angiotensin 2-induced response2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's5 (62.50)18.2507
2000's1 (12.50)29.6817
2010's2 (25.00)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: 19.68

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

MetricThis Compound (vs All)
Research Demand Index19.68 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.25 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (19.68)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (37.50%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (62.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]