Page last updated: 2024-11-06

tasosartan

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Description

tasosartan: angiotensin II antagonist; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID60919
CHEMBL ID432162
CHEBI ID135666
SCHEMBL ID49626
MeSH IDM0228453

Synonyms (61)

Synonym
2,4-dimethyl-8-[2''-(2h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-5,8-dihydro-6h-pyrido[2,3-d]pyrimidin-7-one
2,4-dimethyl-8-[2''-(1h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-5,8-dihydro-6h-pyrido[2,3-d]pyrimidin-7-one
bdbm50040439
ana-756
verdia
tasosartan
way-ana-756
way-126756
tasosartan (usan/inn)
D06010
145733-36-4
DB01349
CHEBI:135666
AKOS000278114
CHEMBL432162 ,
2,4-dimethyl-8-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]-5,6-dihydropyrido[2,3-d]pyrimidin-7-one
L001443
taso-sartan
5,8-dihydro-2,4-dimethyl-8-((2'-(1h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)pyrido(2,3-d)pyrimidin-7(6h)-one
ana756
5,8-dihydro-2,4-dimethyl-8-(p-(o-1h-tetrazol-5-ylphenyl)benzyl)pyrido(2,3-d)pyrimidin-7(6h)-one
ana 756
tasosartan [usan:inn:ban]
48g92v856h ,
pyrido(2,3-d)pyrimidin-7(6h)-one, 5,8-dihydro-2,4-dimethyl-8-((2'-(1h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-
unii-48g92v856h
AKOS016011082
FT-0631174
2,4-dimethyl-8-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]-5,6-dihydropyrido[6,5-d]pyrimidin-7-one
tasosartan [who-dd]
tasosartan [mi]
tasosartan [inn]
tasosartan [mart.]
tasosartan [usan]
gtpl6898
SCHEMBL49626
ADXGNEYLLLSOAR-UHFFFAOYSA-N
2,4-dimethyl-8-[2'-(1h-tetrazol-5-yl)biphenyl-4-ylmethyl]-5,8-dihydro-6h-pyrido[2,3-d]pyrimidin-7-one
ethylglycidylether
AC-35374
DTXSID40163148
2,4-dimethyl-8-({4-[2-(2h-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)-5h,6h,7h,8h-pyrido[2,3-d]pyrimidin-7-one
J-524315
EX-A082
5,8-dihydro-2,4-dimethyl-8-[[2'-(2h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]pyrido[2,3-d]pyrimidin-7(6h)-one
mfcd00865905
NCGC00390218-01
CS-0017594
HY-A0250
8-((2'-(1h-tetrazol-5-yl)biphenyl-4-yl)methyl)-2,4-dimethyl-5,6-dihydropyrido[2,3-d]pyrimidin-7(8h)-one
DS-6574
BCP06091
8-((2'-(1h-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2,4-dimethyl-5,8-dihydropyrido[2,3-d]pyrimidin-7(6h)-one
8-((2'-(1h-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2,4-dimethyl-5,6-dihydropyrido[2,3-d]pyrimidin-7(8h)-one
Q1317131
pyrido[2,3-d]pyrimidin-7(6h)-one, 5,8-dihydro-2,4-dimethyl-8-[[2'-(2h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-
AMY31168
2,4-dimethyl-8-{[2'-(1h-tetrazol-5-yl)biphenyl-4-yl]methyl}-5,8-dihydropyrido[2,3-d]pyrimidin-7(6h)-one
way-ana 756
A846571
5,8-dihydro-2,4-dimethyl-8-[[2'-(2h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-pyrido[2,3-d]pyrimidin-7(6h)-one

Research Excerpts

Overview

Tasosartan is a long-acting angiotensin II (AngII) receptor blocker.

ExcerptReferenceRelevance
"Tasosartan is a long-acting angiotensin II (AngII) receptor blocker. "( Tasosartan, enoltasosartan, and angiotensin II receptor blockade: the confounding role of protein binding.
Brunner, HR; Burnier, M; Maillard, MP; Rossat, J, 2000
)
3.19
"Tasosartan is a newly developed nonpeptide AT1 receptor blocker."( Efficacy and tolerability of tasosartan, a novel angiotensin II receptor blocker: results from a 10-week, double-blind, placebo-controlled, dose-titration study. Tasosartan Investigators Group.
Buckalew, V; Chrysant, SG; Mroczek, WJ; Neutel, JM; Ruff, DA; Weber, M, 1999
)
1.32

Toxicity

ExcerptReferenceRelevance
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36
"Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites."( Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
Jones, LH; Nadanaciva, S; Rana, P; Will, Y, 2016
)
0.43

Pharmacokinetics

ExcerptReferenceRelevance
" Finally, some relevant pharmacokinetics and metabolic properties of the database of 53 compounds are calculated using the VolSurf and MetaSite software to allow the simultaneous characterization of pharmacodynamic and pharmacokinetics properties of the chemical space of angiotensin II receptor antagonists."( Pharmacophore, drug metabolism, and pharmacokinetics models on non-peptide AT1, AT2, and AT1/AT2 angiotensin II receptor antagonists.
Berellini, G; Cruciani, G; Mannhold, R, 2005
)
0.33

Bioavailability

ExcerptReferenceRelevance
" Further study of 4a in Goldblatt (2K-1C) rats showed the compound to have oral bioavailability and to be an efficacious and potent compound in a high renin form of hypertension."( Pyrido[2,3-d]pyrimidine angiotensin II antagonists.
Antane, M; Antane, S; Bender, R; Collini, MD; Ellingboe, JW; Hartupee, D; McCallum, J; Nguyen, TT; Park, CH; White, V, 1994
)
0.29
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" A dose-response relationship (P < ."( A randomized, double-blind, placebo-controlled, parallel-group, multicenter trial of four doses of tasosartan in patients with essential hypertension. Tasosartan Investigator's Group.
de Champlain, J; Gradman, AH; Lacourcière, Y; Larochelle, P; Pool, JL; Smith, WB; Svetkey, L, 1998
)
0.52
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
biphenylsBenzenoid aromatic compounds containing two phenyl or substituted-phenyl groups which are joined together by a single bond.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency23.91850.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency9.52210.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency9.52210.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency9.52210.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency9.52210.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency9.52210.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 1AHomo sapiens (human)IC50 (µMol)0.03200.00010.666410.0000AID39655
Type-1A angiotensin II receptor Rattus norvegicus (Norway rat)IC50 (µMol)0.00320.00040.15553.8000AID37821; AID38298
Type-1B angiotensin II receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00320.00040.13343.8000AID37821; AID38298
Type-1 angiotensin II receptorHomo sapiens (human)IC50 (µMol)0.03500.00020.09323.6000AID39046; AID39655
[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)Affinity0.00120.00050.03150.2300AID243379
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (86)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
gamma-aminobutyric acid signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of serotonin secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of vasoconstriction5-hydroxytryptamine receptor 1AHomo sapiens (human)
exploration behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of dopamine metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of hormone secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1AHomo sapiens (human)
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)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (26)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
receptor-receptor interaction5-hydroxytryptamine receptor 1AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
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)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (24)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membraneType-1 angiotensin II receptorHomo sapiens (human)
membraneType-1 angiotensin II receptorHomo sapiens (human)
plasma membraneType-1 angiotensin II receptorHomo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (67)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID39652Inhibition against Angiotensin II receptor, type 12003Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
Angiotensin II AT1 receptor antagonists. Clinical implications of active metabolites.
AID625276FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID568916Antagonist activity at angiotensin AT1 receptor in rat liver membranes2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID186836Compound was evaluated for maximum decrease in mean arterial pressure after an intravenous dose of 0.1 mg/kg in rats1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Metabolites of the angiotensin II antagonist tasosartan: the importance of a second acidic group.
AID29138Acid dissociation value was evaluated2003Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
Angiotensin II AT1 receptor antagonists. Clinical implications of active metabolites.
AID26259Partition coefficient (logD) (octanol/0.01 N K2HPO4)1994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Pyrido[2,3-d]pyrimidine angiotensin II antagonists.
AID247113Maximal effect produced by the drug in human2005Journal 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.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1636436Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 5.8 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID186711Compound was evaluated for maximum decrease in mean arterial pressure after an intragastric dose of 10.0 mg/kg in rats1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Metabolites of the angiotensin II antagonist tasosartan: the importance of a second acidic group.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID186708Compound was evaluated for maximum decrease in mean arterial pressure after an intragastric dose of 0.1 mg/kg in rats1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Metabolites of the angiotensin II antagonist tasosartan: the importance of a second acidic group.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID186712Compound was evaluated for maximum decrease in mean arterial pressure after an intragastric dose of 3.0 mg/kg in rats1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Metabolites of the angiotensin II antagonist tasosartan: the importance of a second acidic group.
AID37840Inhibitory activity against Angiotensin II receptor, type 1 in rat liver membrane1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID39046Compound was tested in vitro for inhibitory activity against human Angiotensin II receptor in cultured preadipocytes2002Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15
Novel human metabolites of the angiotensin-II antagonist tasosartan and their pharmacological effects.
AID237981Percentage modification of drug adsorbed after administration to human2005Journal 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.
AID625293Drug Induced Liver Injury Prediction System (DILIps) validation dataset; compound DILI positive/negative as observed in LTKB-BD2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID186710Compound was evaluated for maximum decrease in mean arterial pressure after an intragastric dose of 1.0 mg/kg in rats1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Metabolites of the angiotensin II antagonist tasosartan: the importance of a second acidic group.
AID37821Compound was evaluated for the in vitro inhibition of specific binding of [125I]-A II to Angiotensin II receptor, type 1 from rat adrenal membranes.1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Metabolites of the angiotensin II antagonist tasosartan: the importance of a second acidic group.
AID186709Compound was evaluated for maximum decrease in mean arterial pressure after an intragastric dose of 0.3 mg/kg in rats1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Metabolites of the angiotensin II antagonist tasosartan: the importance of a second acidic group.
AID186837Compound was evaluated for maximum decrease in mean arterial pressure after an intravenous dose of 1.0 mg/kg in rats1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Metabolites of the angiotensin II antagonist tasosartan: the importance of a second acidic group.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID237841Oral bioavailability2005Journal 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.
AID239885pKa value against human Angiotensin II receptor type 12005Journal 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.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID186839Compound was evaluated for maximum decrease in mean arterial pressure after an intravenous dose of 3.0 mg/kg in rats1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Metabolites of the angiotensin II antagonist tasosartan: the importance of a second acidic group.
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.
AID39791Relative binding affinity of compound to Angiotensin II receptor, type 1 was determined2003Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
Angiotensin II AT1 receptor antagonists. Clinical implications of active metabolites.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID38298In vitro inhibition of specific binding of [125 I] A II to rat liver membrane.1994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Pyrido[2,3-d]pyrimidine angiotensin II antagonists.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID15688Partition coefficient (logP)1994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Pyrido[2,3-d]pyrimidine angiotensin II antagonists.
AID1636356Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID625295Drug Induced Liver Injury Prediction System (DILIps) validation dataset; compound DILI positive/negative as observed in Pfizer data2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID237099Time required for elimination of 50% of the compound2005Journal 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.
AID186713Compound was evaluated for maximum decrease in mean arterial pressure after an intragastric dose of 30.0 mg/kg in rats1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Metabolites of the angiotensin II antagonist tasosartan: the importance of a second acidic group.
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID1636396Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 22.2 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of N2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID27037Half life of compound was determined2003Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
Angiotensin II AT1 receptor antagonists. Clinical implications of active metabolites.
AID39655Compound was tested for inhibition against Angiotensin II receptor, type 12003Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
Angiotensin II AT1 receptor antagonists. Clinical implications of active metabolites.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID10690Area under curve was measured by using concentration Vs time1994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Pyrido[2,3-d]pyrimidine angiotensin II antagonists.
AID181272Oral effective dose required for lowering blood pressure in renal hypertensive rats (RHR)1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID568941Antihypertensive activity in po dosed conscious goldblatt hypertensive rat model assessed as reduction of angiotensin 2-induced mean arterial blood pressure2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
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.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID184364Maximum percent change in A II supported mean arterial pressure 60 minutes following 3 mg/kg i.d. administration.1994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Pyrido[2,3-d]pyrimidine angiotensin II antagonists.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1346995Human AT1 receptor (Angiotensin receptors)2000The Journal of pharmacology and experimental therapeutics, Nov, Volume: 295, Issue:2
Tasosartan, enoltasosartan, and angiotensin II receptor blockade: the confounding role of protein binding.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (24)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's7 (29.17)18.2507
2000's6 (25.00)29.6817
2010's9 (37.50)24.3611
2020's2 (8.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 22.70

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index22.70 (24.57)
Research Supply Index3.47 (2.92)
Research Growth Index4.52 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (22.70)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials6 (24.00%)5.53%
Reviews4 (16.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other15 (60.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]