Page last updated: 2024-08-05 15:15:26

angiotensin receptor antagonist

A hormone antagonist that blocks angiotensin receptors.

ChEBI ID: 61016

Members (12)

MemberDefinitionClass
avaproA biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.irbesartan
azilsartanA benzimidazolecarboxylic acid that is benzimidazole-7-carboxylic acid substituted at position 2 by a methoxy group and at position 1 by a 2'-[(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl group. Used (as the prodrug, azilsartan medoxomil) for treatment of hypertension.azilsartan
candesartanA benzimidazolecarboxylic acid that is 1H-benzimidazole-7-carboxylic acid substituted by an ethoxy group at position 2 and a ({2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl) group at position 1. It is a angiotensin receptor antagonist used for the treatment of hypertension.candesartan
eprosartanA member of the class of imidazoles and thiophenes that is an angiotensin II receptor antagonist used for the treatment of high blood pressure.eprosartan
forasartanA member of the class of pyridines that is pyridine which is substituted at positions 2 and 5 by o-(tetrazol-5-yl)phenyl and (3,5-dibutyl-1,2,4-triazol-1-yl)methyl groups, respectively. It is a nonpeptide antagonist of angiotensin II, type 1 (AT1) receptors, used for the treatment of hypertension.forasartan
gr 117289A member of the class of 1-benzofurans that is 3-bromo-1-benzofuran which is substituted by a 2-(1H-tetrazol-5-yl)phenyl group at position 2 and by a (2-butyl-5-carboxy-4-chloro-1H-imidazol-1-yl)methyl group at position 5. It is an angiotensin II receptor type 1 (AT1) antagonist and was in clinical trials for the treatment of hypertension (now discontinued).zolasartan
losartanA biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-positionlosartan
olmesartanolmesartan
pd 123319An imidazopyridine consisting of 4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine having 4-(dimethylamino)-3-methylbenzyl, diphenylacetyl and carboxy and groups at positions 1, 5 and 6 respectivelyPD123319
tak 491A carboxylic ester obtained by formal condensation of the carboxy group of azilsartan with the hydroxy group of 4-(hydroxymethyl)-5-methyl-1,3-dioxol-2-one. A prodrug for azilsartan, it is used for treatment of hypertension.azilsartan medoxomil
telmisartanA member of the class of benzimidazoles used widely in the treatment of hypertension.telmisartan
valsartanA monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2'-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group. It exhibits antihypertensive activity.valsartan

Research

Studies (15,602)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199014 (0.09)18.7374
1990's2,281 (14.62)18.2507
2000's5,901 (37.82)29.6817
2010's5,674 (36.37)24.3611
2020's1,732 (11.10)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials3,719 (20.32%)5.53%
Reviews1,575 (8.61%)6.00%
Case Studies616 (3.37%)4.05%
Observational116 (0.63%)0.25%
Other12,277 (67.08%)84.16%

Protein Targets (139)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
acetylcholinesteraseHomo sapiens (human)Potency13.802911
activating transcription factor 6Homo sapiens (human)Potency21.313811
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.810711
AR proteinHomo sapiens (human)Potency15.697566
Cellular tumor antigen p53Homo sapiens (human)Potency23.733123
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency18.169612
Chain A, Beta-lactamaseEscherichia coli K-12Potency44.668411
Chain A, CruzipainTrypanosoma cruziPotency39.810712
Chain A, HADH2 proteinHomo sapiens (human)Potency31.622811
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency1.306012
Chain B, HADH2 proteinHomo sapiens (human)Potency31.622811
cytochrome P450 2C9, partialHomo sapiens (human)Potency8.566114
cytochrome P450 2D6Homo sapiens (human)Potency19.460612
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency17.216826
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency9.821814
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency10.000011
estrogen nuclear receptor alphaHomo sapiens (human)Potency12.3121612
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency8.991666
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency14.792812
EWS/FLI fusion proteinHomo sapiens (human)Potency34.185444
eyes absent homolog 2 isoform aHomo sapiens (human)Potency28.183811
farnesoid X nuclear receptorHomo sapiens (human)Potency29.847011
GVesicular stomatitis virusPotency8.566114
GABA theta subunitRattus norvegicus (Norway rat)Potency17.216813
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency17.216813
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency17.216813
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency17.216813
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency17.216813
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency17.216813
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency17.216813
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency17.216813
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency17.216813
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency17.216813
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency17.216813
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency17.216813
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency17.216813
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency17.216813
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency17.216813
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency17.216813
gemininHomo sapiens (human)Potency13.335911
GLI family zinc finger 3Homo sapiens (human)Potency5.486423
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency20.549034
Guanine nucleotide-binding protein GHomo sapiens (human)Potency3.162311
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency39.810711
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency8.566114
IDH1Homo sapiens (human)Potency8.199511
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency8.566118
Interferon betaHomo sapiens (human)Potency8.566114
lamin isoform A-delta10Homo sapiens (human)Potency0.199512
LuciferasePhotinus pyralis (common eastern firefly)Potency12.975235
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency0.446722
mitogen-activated protein kinase 1Homo sapiens (human)Potency17.900822
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency0.446711
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Potency0.446711
neuropeptide S receptor isoform AHomo sapiens (human)Potency1.258911
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency24.672623
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency23.109311
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency22.718422
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency35.481311
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency32.410412
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency12.558937
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency35.481311
pregnane X nuclear receptorHomo sapiens (human)Potency22.695123
RAR-related orphan receptor gammaMus musculus (house mouse)Potency6.308611
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency10.174635
retinoid X nuclear receptor alphaHomo sapiens (human)Potency24.887223
SMAD family member 2Homo sapiens (human)Potency1.899611
SMAD family member 3Homo sapiens (human)Potency1.899611
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency28.127415
TAR DNA-binding protein 43Homo sapiens (human)Potency0.316211
TDP1 proteinHomo sapiens (human)Potency20.101123
thioredoxin reductaseRattus norvegicus (Norway rat)Potency79.432811
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency30.027224
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency10.000011
USP1 protein, partialHomo sapiens (human)Potency36.253012
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency6.681911
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency28.183811

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
10 kDa chaperonin Escherichia coliIC50175.000022
10 kDa heat shock protein, mitochondrialHomo sapiens (human)IC50100.000011
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC500.019011
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.000611
60 kDa chaperoninEscherichia coli K-12IC50250.000011
60 kDa chaperonin Escherichia coliIC50175.000022
60 kDa heat shock protein, mitochondrialHomo sapiens (human)IC50100.000011
Adenosine receptor A2aRattus norvegicus (Norway rat)IC500.003211
Adenosine receptor A3Homo sapiens (human)IC501.219911
Adenosine receptor A3Homo sapiens (human)Ki0.689511
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC503.065211
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki3.039811
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC501.219911
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.689511
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC501.219911
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.689511
Alpha-2B adrenergic receptorHomo sapiens (human)IC503.843011
Alpha-2B adrenergic receptorHomo sapiens (human)Ki1.754411
Angiotensin-converting enzyme Homo sapiens (human)IC500.019011
Angiotensin-converting enzyme Homo sapiens (human)Ki6.000011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC5055.187514
Atrial natriuretic peptide receptor 3Homo sapiens (human)IC500.001811
Beta-3 adrenergic receptorHomo sapiens (human)IC504.300011
Beta-3 adrenergic receptorHomo sapiens (human)Ki3.200011
Bile salt export pumpHomo sapiens (human)IC5040.7400613
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC5025.950022
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)IC5026.000011
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC5026.000011
cAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)IC5026.000011
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC5026.000011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50107.966713
cGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)IC5013.000011
cGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)IC5013.000011
Cytochrome P450 2C9 Homo sapiens (human)IC5014.075524
Cytochrome P450 2J2Homo sapiens (human)IC5012.875034
Cytochrome P450 2J2Homo sapiens (human)Ki0.145022
Cytochrome P450 3A4Homo sapiens (human)IC509.000011
Endothelin-1 receptorHomo sapiens (human)Ki6.666733
Epidermal growth factor receptorHomo sapiens (human)IC503.276911
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC50255.966713
Multidrug resistance-associated protein 4Homo sapiens (human)IC5096.300014
NeprilysinHomo sapiens (human)IC5010.000011
Peroxisome proliferator-activated receptor alphaHomo sapiens (human)IC5010.000011
Peroxisome proliferator-activated receptor deltaHomo sapiens (human)IC5010.000011
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)IC5012.200011
Platelet glycoprotein VIHomo sapiens (human)IC504.000022
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50194.984011
Receptor tyrosine-protein kinase erbB-2Homo sapiens (human)IC505.947211
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC503.065211
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki3.039811
Sodium/bile acid cotransporterHomo sapiens (human)IC5030.000011
Sodium/bile acid cotransporterHomo sapiens (human)Ki11.900011
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)IC501.075212
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)Ki0.595012
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)IC501.203512
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)Ki0.925012
Squalene synthaseRattus norvegicus (Norway rat)Ki6.668323
Thiosulfate sulfurtransferaseHomo sapiens (human)IC50100.000011
Thromboxane A2 receptor Homo sapiens (human)IC5020.000011
Thromboxane-A synthase Homo sapiens (human)IC503.059411
Type-1 angiotensin II receptorCavia porcellus (domestic guinea pig)IC500.018011
Type-1 angiotensin II receptorHomo sapiens (human)IC500.03072229
Type-1 angiotensin II receptorOryctolagus cuniculus (rabbit)IC500.025022
Type-1 angiotensin II receptorHomo sapiens (human)Ki0.34081214
Type-1 angiotensin II receptorOryctolagus cuniculus (rabbit)Ki3.133523
Type-1A angiotensin II receptor Rattus norvegicus (Norway rat)IC500.04671821
Type-1A angiotensin II receptor Rattus norvegicus (Norway rat)Ki0.013258
Type-1B angiotensin II receptorRattus norvegicus (Norway rat)IC501.32372328
Type-1B angiotensin II receptorRattus norvegicus (Norway rat)Ki0.0192710
Type-2 angiotensin II receptorHomo sapiens (human)IC505.717567
Type-2 angiotensin II receptorRattus norvegicus (Norway rat)IC5018.71661112
Type-2 angiotensin II receptorHomo sapiens (human)Ki46.666733
Type-2 angiotensin II receptorRattus norvegicus (Norway rat)Ki0.031611

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Amine oxidase [flavin-containing] A Rattus norvegicus (Norway rat)EC5010.000011
Cystic fibrosis transmembrane conductance regulatorHomo sapiens (human)Kd189.300011
Glycine receptor subunit alpha-1Homo sapiens (human)EC503.200011
Leukotriene B4 receptor 2Homo sapiens (human)EC5010.470013
Peroxisome proliferator-activated receptor alphaHomo sapiens (human)EC5010.000011
Peroxisome proliferator-activated receptor alphaMus musculus (house mouse)EC5010.000011
Peroxisome proliferator-activated receptor deltaHomo sapiens (human)EC5010.000011
Peroxisome proliferator-activated receptor deltaMus musculus (house mouse)EC5010.000011
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)EC503.12771313
Peroxisome proliferator-activated receptor gammaMus musculus (house mouse)EC504.060011
Platelet glycoprotein VIHomo sapiens (human)Kd185.000024
Type-1 angiotensin II receptorHomo sapiens (human)EC5010.000022
Type-1 angiotensin II receptorCavia porcellus (domestic guinea pig)Kd0.012611
Type-1 angiotensin II receptorHomo sapiens (human)Kd0.004812
Type-1 angiotensin II receptorOryctolagus cuniculus (rabbit)Kd0.042656
Type-1A angiotensin II receptor Rattus norvegicus (Norway rat)EC5010.000011
Type-1A angiotensin II receptor Rattus norvegicus (Norway rat)Kd0.006612

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
ATP-dependent translocase ABCB1Homo sapiens (human)Km245.066733
Platelet glycoprotein VIHomo sapiens (human)MEC500.000011
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)Km42.600011
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)Km71.800011
Thromboxane A2 receptor Homo sapiens (human)MEC14.000014
Type-1 angiotensin II receptorHomo sapiens (human)Affinity0.003316
Type-1 angiotensin II receptorHomo sapiens (human)Kb0.006033