Target Information

Target General Infomation
Target ID
T74456
Former ID
TTDS00267
Target Name
Type-1 angiotensin II receptor
Gene Name
AGTR1
Synonyms
AT1; AT1AR; Angiotensin 1 receptor; Angiotensin II receptor 1; AGTR1
Target Type
Successful
Disease Alzheimer disease [ICD9: 331; ICD10: G30]
Hypertension [ICD9: 401; ICD10: I10-I16]
Heart failure [ICD9: 428; ICD10: I50]
Hypotension [ICD9: 458, 796.3; ICD10: I95]
High blood pressure [ICD9: 401; ICD10: I10-I16]
Myocardial infarction [ICD9: 410; ICD10: I21, I22]
Metabolic syndrome x [ICD9: 277.7; ICD10: E88.81]
Restenosis [ICD10: I51.89]
Unspecified [ICD code not available]
Function
Receptor for angiotensin II.Mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system.
BioChemical Class
GPCR rhodopsin
Target Validation
T74456
UniProt ID
P30556
Sequence
MILNSSTEDGIKRIQDDCPKAGRHNYIFVMIPTLYSIIFVVGIFGNSLVVIVIYFYMKLK
TVASVFLLNLALADLCFLLTLPLWAVYTAMEYRWPFGNYLCKIASASVSFNLYASVFLLT
CLSIDRYLAIVHPMKSRLRRTMLVAKVTCIIIWLLAGLASLPAIIHRNVFFIENTNITVC
AFHYESQNSTLPIGLGLTKNILGFLFPFLIILTSYTLIWKALKKAYEIQKNKPRNDDIFK
IIMAIVLFFFFSWIPHQIFTFLDVLIQLGIIRDCRIADIVDTAMPITICIAYFNNCLNPL
FYGFLGKKFKRYFLQLLKYIPPKAKSHSNLSTKMSTLSYRPSDNVSSSTKKPAPCFEVE
Drugs and Mode of Action
Drug(s) Azilsartan Drug Info Approved Hypertension [541957], [551719]
Candesartan Drug Info Approved Hypertension [536361], [541178]
Eprosartan Drug Info Approved Hypertension [536361], [541182]
Forasartan Drug Info Approved Hypertension [535697], [541952]
Irbesartan Drug Info Approved Hypertension [536095], [541187]
Losartan Drug Info Approved Hypertension [536095], [541193]
Micardis telmisartan Drug Info Approved Hypertension [551881]
Olmesartan medoxomil Drug Info Approved High blood pressure [537312]
Saprisartan Drug Info Approved Hypertension [534931], [541954]
SARALASIN Drug Info Approved Hypertension [541252], [551871]
Saralasin Acetate Drug Info Approved Hypertension [551871]
Tasosartan Drug Info Approved Hypertension [536361], [541953]
Telmisartan Drug Info Approved Hypertension [536361], [541207]
Valsartan Drug Info Approved Hypertension [536361], [540559]
Pratosartan Drug Info Phase 3 Hypertension [545261]
S-474474 Drug Info Phase 3 Metabolic syndrome x [551683]
TAK-491 Drug Info Phase 3 Hypertension [525243]
CL-329167 Drug Info Phase 2 Hypertension [545836]
sparsentan Drug Info Phase 2 Myocardial infarction [527366]
TRV027 Drug Info Phase 2 Heart failure [524481]
YM-358 Drug Info Phase 2 Hypertension [545253]
KRH-594 Drug Info Discontinued in Phase 2 Hypertension [546398]
MILFASARTAN Drug Info Discontinued in Phase 2 Hypertension [545356]
RIPISARTAN Drug Info Discontinued in Phase 2 Hypertension [545748]
Zolasartan Drug Info Discontinued in Phase 2 Hypotension [544984]
TAK-591 Drug Info Discontinued in Phase 1 Hypertension [548747]
UR-7198 Drug Info Discontinued in Phase 1 Hypertension [546845]
CR-3834 Drug Info Terminated Hypertension [548162]
HELENALIN Drug Info Terminated Discovery agent [544640]
L-159689 Drug Info Terminated Hypertension [545497]
RS-66252 Drug Info Terminated Alzheimer disease [546339]
UP-275-22 Drug Info Terminated Hypertension [545814]
XR-510 Drug Info Terminated Hypertension [545812]
Antagonist (E)-N-(3-iodoprop-2-enyl)-2beta-carbomethoxy-3beta-(4'-methylphenyl)n Drug Info [534913]
4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone Drug Info [534957]
4-[(diphenylmethyl)amino]-2-phenylquinazoline Drug Info [535513]
5-butyl-methyl immidazole carboxylate 30 Drug Info [532000]
5-oxo-1-2-4-oxadiazol biphenyl Drug Info [531841]
Candesartan Drug Info [535067], [537549]
CL-329167 Drug Info [533874], [551871]
CR-3834 Drug Info [529503]
Eprosartan Drug Info [536887]
EXP3174 Drug Info [533998]
Forasartan Drug Info [535264], [535697]
GBR-12935 Drug Info [538041]
Irbesartan Drug Info [537449]
KRH-594 Drug Info [526535]
Losartan Drug Info [534973], [535660], [537449]
LY301875 Drug Info [526029]
LY303336 Drug Info [526029]
Micardis telmisartan Drug Info [527783]
MILFASARTAN Drug Info [532043], [551871]
N,N`-bis-alkyl butylimmidazole 12b Drug Info [532215]
Olmesartan medoxomil Drug Info [537475]
Pratosartan Drug Info [529390]
RIPISARTAN Drug Info [533666], [551871]
Saprisartan Drug Info [534931]
sparsentan Drug Info [527799]
TAK-591 Drug Info [551717]
Tasosartan Drug Info [535061]
Telmisartan Drug Info [537265]
TRV027 Drug Info [532415]
UR-7198 Drug Info [525714]
Valsartan Drug Info [535660], [537449]
YM-358 Drug Info [525713], [551871]
[125I]EXP985 Drug Info [526828]
[3H]A81988 Drug Info [533927]
[3H]candesartan Drug Info [525439]
[3H]eprosartan Drug Info [534043]
[3H]irbesartan Drug Info [526320]
[3H]L158809 Drug Info [526960]
[3H]losartan Drug Info [533967]
[3H]valsartan Drug Info [525979]
Inhibitor 4-(2-Butyl-benzoimidazol-1-ylmethyl)-phenol Drug Info [551262]
ANGIOTENSIN II Drug Info [530710]
Carboxylic Acid Metabolite (E-3174) Drug Info [551260]
CV-11194 Drug Info [534298]
GNF-PF-2307 Drug Info [531262]
GNF-PF-2812 Drug Info [531262]
GNF-PF-3832 Drug Info [531262]
HELENALIN Drug Info [531262]
L-159093 Drug Info [527799]
L-159689 Drug Info [527799]
L-162313 Drug Info [529578]
L-162782 Drug Info [529578]
SARALASIN Drug Info [529569]
[Bpa1]AngII Drug Info [530710]
[Sar1,Bpa2]AngII Drug Info [530710]
[Sar1,Bpa3]AngII Drug Info [530710]
[Sar1,Bpa8]AngII Drug Info [530710]
[Sar1,Tdf2]AngII Drug Info [530710]
[Sar1,Tdf3]AngII Drug Info [530710]
[Sar1,Tdf8]AngII Drug Info [530710]
[Tdf1]AngII Drug Info [530710]
Agonist angiotensin III Drug Info [543777]
L-163,101 Drug Info [534516]
Zolasartan Drug Info [531650]
Modulator Azilsartan Drug Info [531783]
CGP-49870 Drug Info
RS-66252 Drug Info [551841]
Saralasin Acetate Drug Info [556264]
TAK-491 Drug Info [531783]
UP-275-22 Drug Info [543777]
XR-510 Drug Info [534102]
Blocker S-474474 Drug Info [551683]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Calcium signaling pathway
cGMP-PKG signaling pathway
Neuroactive ligand-receptor interaction
Adrenergic signaling in cardiomyocytes
Vascular smooth muscle contraction
Renin-angiotensin system
Renin secretion
Pathways in cancer
NetPath Pathway TGF_beta_Receptor Signaling Pathway
PANTHER Pathway Angiotensin II-stimulated signaling through G proteins and beta-arrestin
Pathway Interaction Database Arf6 trafficking events
Arf6 signaling events
Angiopoietin receptor Tie2-mediated signaling
PathWhiz Pathway Angiotensin Metabolism
Muscle/Heart Contraction
Reactome Peptide ligand-binding receptors
G alpha (q) signalling events
WikiPathways ACE Inhibitor Pathway
GPCRs, Class A Rhodopsin-like
Gastrin-CREB signalling pathway via PKC and MAPK
Peptide GPCRs
Allograft Rejection
GPCR ligand binding
GPCR downstream signaling
References
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Ref 525243ClinicalTrials.gov (NCT02480764) TAK-491 (Azilsartan Medoxomil) Compared to Valsartan in Chinese Participants With Hypertension.
Ref 527366Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics. J Med Chem. 2005 Jan 13;48(1):171-9.
Ref 534931Pharmacological properties of angiotensin II receptor antagonists. Can J Cardiol. 1999 Nov;15 Suppl F:26F-8F.
Ref 535697Non-peptide angiotensin II receptor antagonists: chemical feature based pharmacophore identification. J Med Chem. 2003 Feb 27;46(5):716-26.
Ref 536095New antiarrhythmic agents for atrial fibrillation and atrial flutter. Expert Opin Emerg Drugs. 2005 May;10(2):311-22.
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 537312Effect of angiotensin receptor blockade on endothelial function: focus on olmesartan medoxomil. Vasc Health Risk Manag. 2009;5(1):301-14. Epub 2009 Apr 8.
Ref 540559(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3937).
Ref 541178(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 587).
Ref 541182(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 588).
Ref 541187(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 589).
Ref 541193(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 590).
Ref 541207(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 592).
Ref 541252(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 598).
Ref 541952(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6896).
Ref 541953(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6898).
Ref 541954(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6899).
Ref 541957(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6901).
Ref 544640Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000398)
Ref 544984Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001788)
Ref 545253Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002583)
Ref 545261Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002623)
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Ref 545812Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004861)
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Ref 546398Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007913)
Ref 546845Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010597)
Ref 548162Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022642)
Ref 548747Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028308)
Ref 551683Clinical pipeline report, company report or official report of Shionogi (2011).
Ref 551719Clinical pipeline report, company report or official report of Takeda.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 551881Clinical pipeline report, company report or official report of Boehringer-Ingelheim Pharmaceuticals.
Ref 525439Binding of the antagonist [3H]candesartan to angiotensin II AT1 receptor-transfected [correction of tranfected] Chinese hamster ovary cells. Eur J Pharmacol. 1999 Feb 19;367(2-3):413-22.
Ref 525713Effects of YM358, an angiotensin II type 1 (AT1) receptor antagonist, and enalapril on blood pressure and vasoconstriction in two renal hypertension models. Biol Pharm Bull. 2000 Feb;23(2):174-81.
Ref 525714Pharmacologic profile of UR-7247, an orally active angiotensin II AT1 receptor antagonist, in healthy volunteers. p6. J Cardiovasc Pharmacol. 2000 Mar;35(3):383-9.
Ref 525979Interaction between the partially insurmountable antagonist valsartan and human recombinant angiotensin II type 1 receptors. Fundam Clin Pharmacol. 2000 Nov-Dec;14(6):577-85.
Ref 526029Inhibition of angiotensin II-induced inositol phosphate production by triacid nonpeptide antagonists in CHO cells expressing human AT1 receptors. Pharm Res. 2000 Dec;17(12):1482-8.
Ref 526320Binding characteristics of [(3)H]-irbesartan to human recombinant angiotensin type 1 receptors. J Renin Angiotensin Aldosterone Syst. 2000 Jun;1(2):159-65.
Ref 526535Binding of KRH-594, an antagonist of the angiotensin II type 1 receptor, to cloned human and rat angiotensin II receptors. Fundam Clin Pharmacol. 2002 Aug;16(4):317-23.
Ref 526828[125I]EXP985: a highly potent and specific nonpeptide radioligand antagonist for the AT1 angiotensin receptor. Biochem Biophys Res Commun. 1992 Nov 16;188(3):1030-9.
Ref 526960Characterization of the binding of [3H]L-158,809: a new potent and selective nonpeptide angiotensin II receptor (AT1) antagonist radioligand. Mol Pharmacol. 1992 Dec;42(6):1077-82.
Ref 527783The angiotensin II receptor antagonist telmisartan reduces urinary albumin excretion in patients with isolated systolic hypertension: results of a randomized, double-blind, placebo-controlled trial. J Hypertens. 2005 Nov;23(11):2055-61.
Ref 527799J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm.
Ref 529390Clinical efficacy of a new angiotensin II type 1 receptor blocker, pratosartan, in hypertensive patients. Hypertens Res. 2008 Feb;31(2):281-7.
Ref 529503Pharmacokinetic study of a new angiotensin-AT1 antagonist by HPLC. J Pharm Biomed Anal. 2008 Sep 29;48(2):422-7.
Ref 529569J Med Chem. 2008 Jul 24;51(14):4150-69. Epub 2008 Jun 28.Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.
Ref 529578Bioorg Med Chem. 2008 Jul 15;16(14):6841-9. Epub 2008 Jul 1.Selective angiotensin II AT2 receptor agonists: Benzamide structure-activity relationships.
Ref 530710J Med Chem. 2010 Mar 11;53(5):2063-75.The amino-terminus of angiotensin II contacts several ectodomains of the angiotensin II receptor AT1.
Ref 531262Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2).
Ref 531650Azilsartan: a newly approved angiotensin II receptor blocker. Cardiol Rev. 2011 Nov-Dec;19(6):300-4.
Ref 5317832011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
Ref 531841Synthesis and biological evaluation of novel potent angiotensin II receptor antagonists with anti-hypertension effect. Bioorg Med Chem. 2012 Apr 15;20(8):2747-61.
Ref 532000The discovery of new potent non-peptide Angiotensin II AT1 receptor blockers: a concise synthesis, molecular docking studies and biological evaluation of N-substituted 5-butylimidazole derivatives. Eur J Med Chem. 2012 Sep;55:358-74.
Ref 532043Dual action molecules: bioassays of combined novel antioxidants and angiotensin II receptor antagonists. Eur J Pharmacol. 2012 Nov 15;695(1-3):96-103.
Ref 532215Rational design, efficient syntheses and biological evaluation of N,N'-symmetrically bis-substituted butylimidazole analogs as a new class of potent Angiotensin II receptor blockers. Eur J Med Chem. 2013 Apr;62:352-70.
Ref 532415First clinical experience with TRV027: pharmacokinetics and pharmacodynamics in healthy volunteers. J Clin Pharmacol. 2013 Sep;53(9):892-9.
Ref 533666In vitro pharmacological characterization of UP 269-6, a novel nonpeptide angiotensin II receptor antagonist. Fundam Clin Pharmacol. 1995;9(2):119-28.
Ref 533874Distribution and function of cardiac angiotensin AT1- and AT2-receptor subtypes in hypertrophied rat hearts. Am J Physiol. 1994 Aug;267(2 Pt 2):H844-52.
Ref 533927[3H]A-81988, a potent, selective, competitive antagonist radioligand for angiotensin AT1 receptors. Eur J Pharmacol. 1994 Mar 15;267(1):49-54.
Ref 533967Characterization of [3H]losartan receptors in isolated rat glomeruli. Eur J Pharmacol. 1993 Oct 15;247(2):193-8.
Ref 533998Angiotensin II receptors and angiotensin II receptor antagonists. Pharmacol Rev. 1993 Jun;45(2):205-51.
Ref 534043Characterization of [3H]SK&F 108566 as a radioligand for angiotensin type-1 receptor. J Recept Res. 1993;13(5):849-61.
Ref 534102Pharmacology of XR510, a potent orally active nonpeptide angiotensin II AT1 receptor antagonist with high affinity for the AT2 receptor subtype. J Cardiovasc Pharmacol. 1995 Sep;26(3):354-62.
Ref 534298J Med Chem. 1996 Dec 20;39(26):5228-35.Synthesis and angiotensin II receptor antagonistic activities of benzimidazole derivatives bearing acidic heterocycles as novel tetrazole bioisosteres.
Ref 534516Structural model of antagonist and agonist binding to the angiotensin II, AT1 subtype, G protein coupled receptor. Chem Biol. 1994 Dec;1(4):211-21.
Ref 534913Pharmacological characterization of (E)-N-(3-iodoprop-2-enyl)-2beta-carbomethoxy-3beta-(4'-methylphenyl)n ortropane as a selective and potent inhibitor of the neuronal dopamine transporter. J Pharmacol Exp Ther. 1999 Nov;291(2):648-54.
Ref 534931Pharmacological properties of angiotensin II receptor antagonists. Can J Cardiol. 1999 Nov;15 Suppl F:26F-8F.
Ref 534957Discovery of a novel dopamine transporter inhibitor, 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone, as a potential cocaine antagonist through 3D-database pharmacophore searching. Molecular modeling, structure-activity relationships, and behavioral pharmacological studies. J Med Chem. 2000 Feb 10;43(3):351-60.
Ref 534973Effect of episodic hypoxia on sympathetic activity and blood pressure. Respir Physiol. 2000 Feb;119(2-3):189-97.
Ref 535061Tasosartan, enoltasosartan, and angiotensin II receptor blockade: the confounding role of protein binding. J Pharmacol Exp Ther. 2000 Nov;295(2):649-54.
Ref 535067Angiotensin II type 1 receptor blockade: a novel therapeutic concept. Blood Press Suppl. 2000;1:9-13.
Ref 535264Possible involvement of calcium-calmodulin pathways in the positive chronotropic response to angiotensin II on the canine cardiac sympathetic ganglia. Jpn J Pharmacol. 2001 Aug;86(4):381-9.
Ref 535513Identification of a novel partial inhibitor of dopamine transporter among 4-substituted 2-phenylquinazolines. Bioorg Med Chem Lett. 2002 Aug 19;12(16):2225-8.
Ref 535660Knockouts model the 100 best-selling drugs--will they model the next 100? Nat Rev Drug Discov. 2003 Jan;2(1):38-51.
Ref 535697Non-peptide angiotensin II receptor antagonists: chemical feature based pharmacophore identification. J Med Chem. 2003 Feb 27;46(5):716-26.
Ref 536887Clinical profile of eprosartan: a different angiotensin II receptor blocker. Cardiovasc Hematol Agents Med Chem. 2008 Oct;6(4):253-7.
Ref 537265Deletion of angiotensin II type I receptor reduces hepatic steatosis. J Hepatol. 2009 Jun;50(6):1226-35. Epub 2009 Mar 11.
Ref 537449Radioligand binding assays: application of [(125)I]angiotensin II receptor binding. Methods Mol Biol. 2009;552:131-41.
Ref 537475Mechanism of diastolic stiffening of the failing myocardium and its prevention by angiotensin receptor and calcium channel blockers. J Cardiovasc Pharmacol. 2009 Jul;54(1):47-56.
Ref 537549Candesartan: widening indications for this angiotensin II receptor blocker? Expert Opin Pharmacother. 2009 Aug;10(12):1995-2007.
Ref 538041Specific binding of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenyl propyl) piperazine (GBR-12935), an inhibitor of the dopamine transporter, to human CYP2D6. Biochem Pharmacol. 1997 Jun 15;53(12):1937-9.
Ref 543777(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 34).
Ref 551260Angiotensin II receptor antagonists: imidazoles and pyrroles bearing hydroxymethyl and carboxy substituents, Bioorg. Med. Chem. Lett. 4(1):177-182 (1994).
Ref 551262Discovery and development of aryl-fused imidazole-based angiotensin II antagonists, Bioorg. Med. Chem. Lett. 4(1):213-218 (1994).
Ref 551683Clinical pipeline report, company report or official report of Shionogi (2011).
Ref 551717Clinical pipeline report, company report or official report of Takeda (2009).
Ref 551841Virtual Screening in Drug Discovery, Juan Alvarez Brian Shoichet. Page(218).
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

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