Target Information
Target General Information | Top | |||||
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Target ID |
T74456
(Former ID: TTDS00267)
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Target Name |
Angiotensin II receptor type-1 (AGTR1)
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Synonyms |
Type-1 angiotensin II receptor; Angiotensin II type-1 receptor; Angiotensin II receptor 1; Angiotensin 1 receptor; AT2R1B; AT2R1; AT1BR; AT1AR; AT1; AGTR1B; AGTR1A
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Gene Name |
AGTR1
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 3 Target-related Diseases | + | ||||
1 | Essential hypertension [ICD-11: BA00] | |||||
2 | Hypertension [ICD-11: BA00-BA04] | |||||
3 | Secondary hypertension [ICD-11: BA04] | |||||
Function |
Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Receptor for angiotensin II.
Click to Show/Hide
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BioChemical Class |
GPCR rhodopsin
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UniProt ID | ||||||
Sequence |
MILNSSTEDGIKRIQDDCPKAGRHNYIFVMIPTLYSIIFVVGIFGNSLVVIVIYFYMKLK
TVASVFLLNLALADLCFLLTLPLWAVYTAMEYRWPFGNYLCKIASASVSFNLYASVFLLT CLSIDRYLAIVHPMKSRLRRTMLVAKVTCIIIWLLAGLASLPAIIHRNVFFIENTNITVC AFHYESQNSTLPIGLGLTKNILGFLFPFLIILTSYTLIWKALKKAYEIQKNKPRNDDIFK IIMAIVLFFFFSWIPHQIFTFLDVLIQLGIIRDCRIADIVDTAMPITICIAYFNNCLNPL FYGFLGKKFKRYFLQLLKYIPPKAKSHSNLSTKMSTLSYRPSDNVSSSTKKPAPCFEVE Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
HIT2.0 ID | T23RWU |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 15 Approved Drugs | + | ||||
1 | ANGIOTENSIN II | Drug Info | Approved | Increase blood pressure | [2] | |
2 | Azilsartan | Drug Info | Approved | Hypertension | [3], [4] | |
3 | Candesartan | Drug Info | Approved | Hypertension | [5], [6] | |
4 | Eprosartan | Drug Info | Approved | Hypertension | [6], [7] | |
5 | Forasartan | Drug Info | Approved | Hypertension | [8], [9] | |
6 | Irbesartan | Drug Info | Approved | Hypertension | [10], [11] | |
7 | Losartan | Drug Info | Approved | Hypertension | [11], [12] | |
8 | Micardis telmisartan | Drug Info | Approved | Hypertension | [13] | |
9 | Olmesartan medoxomil | Drug Info | Approved | High blood pressure | [14] | |
10 | Saprisartan | Drug Info | Approved | Hypertension | [15], [16] | |
11 | SARALASIN | Drug Info | Approved | Hypertension | [17], [18] | |
12 | Saralasin Acetate | Drug Info | Approved | Hypertension | [18] | |
13 | Tasosartan | Drug Info | Approved | Hypertension | [6], [19] | |
14 | Telmisartan | Drug Info | Approved | Hypertension | [6], [20] | |
15 | Valsartan | Drug Info | Approved | Hypertension | [6], [21] | |
Clinical Trial Drug(s) | [+] 7 Clinical Trial Drugs | + | ||||
1 | Pratosartan | Drug Info | Phase 3 | Hypertension | [22] | |
2 | S-474474 | Drug Info | Phase 3 | Metabolic syndrome x | [23] | |
3 | sparsentan | Drug Info | Phase 3 | Focal segmental glomerulosclerosis | [24] | |
4 | TAK-491 | Drug Info | Phase 3 | Hypertension | [25] | |
5 | CL-329167 | Drug Info | Phase 2 | Hypertension | [26] | |
6 | TRV027 | Drug Info | Phase 2 | Heart failure | [27] | |
7 | YM-358 | Drug Info | Phase 2 | Hypertension | [28] | |
Discontinued Drug(s) | [+] 13 Discontinued Drugs | + | ||||
1 | KRH-594 | Drug Info | Discontinued in Phase 2 | Hypertension | [29] | |
2 | MILFASARTAN | Drug Info | Discontinued in Phase 2 | Hypertension | [30] | |
3 | RIPISARTAN | Drug Info | Discontinued in Phase 2 | Hypertension | [31] | |
4 | Zolasartan | Drug Info | Discontinued in Phase 2 | Hypotension | [32] | |
5 | TAK-591 | Drug Info | Discontinued in Phase 1 | Hypertension | [33] | |
6 | UR-7198 | Drug Info | Discontinued in Phase 1 | Hypertension | [34] | |
7 | A-81988 | Drug Info | Terminated | Hypertension | [35] | |
8 | CR-3834 | Drug Info | Terminated | Hypertension | [36] | |
9 | L-158809 | Drug Info | Terminated | Hypertension | [37] | |
10 | L-159689 | Drug Info | Terminated | Hypertension | [38] | |
11 | RS-66252 | Drug Info | Terminated | Alzheimer disease | [39] | |
12 | UP-275-22 | Drug Info | Terminated | Hypertension | [40] | |
13 | XR-510 | Drug Info | Terminated | Hypertension | [41] | |
Mode of Action | [+] 5 Modes of Action | + | ||||
Inhibitor | [+] 20 Inhibitor drugs | + | ||||
1 | ANGIOTENSIN II | Drug Info | [42] | |||
2 | SARALASIN | Drug Info | [56] | |||
3 | HELENALIN | Drug Info | [74] | |||
4 | L-159689 | Drug Info | [62] | |||
5 | 4-(2-Butyl-benzoimidazol-1-ylmethyl)-phenol | Drug Info | [80] | |||
6 | CV-11194 | Drug Info | [86] | |||
7 | GNF-PF-2307 | Drug Info | [74] | |||
8 | GNF-PF-2812 | Drug Info | [74] | |||
9 | GNF-PF-3832 | Drug Info | [74] | |||
10 | L-159093 | Drug Info | [62] | |||
11 | L-162313 | Drug Info | [89] | |||
12 | L-162782 | Drug Info | [89] | |||
13 | [Bpa1]AngII | Drug Info | [42] | |||
14 | [Sar1,Bpa2]AngII | Drug Info | [42] | |||
15 | [Sar1,Bpa3]AngII | Drug Info | [42] | |||
16 | [Sar1,Bpa8]AngII | Drug Info | [42] | |||
17 | [Sar1,Tdf2]AngII | Drug Info | [42] | |||
18 | [Sar1,Tdf3]AngII | Drug Info | [42] | |||
19 | [Sar1,Tdf8]AngII | Drug Info | [42] | |||
20 | [Tdf1]AngII | Drug Info | [42] | |||
Modulator | [+] 7 Modulator drugs | + | ||||
1 | Azilsartan | Drug Info | [43] | |||
2 | Saralasin Acetate | Drug Info | [57] | |||
3 | TAK-491 | Drug Info | [43] | |||
4 | RS-66252 | Drug Info | [76] | |||
5 | UP-275-22 | Drug Info | [77] | |||
6 | XR-510 | Drug Info | [78] | |||
7 | CGP-49870 | Drug Info | [85] | |||
Antagonist | [+] 35 Antagonist drugs | + | ||||
1 | Candesartan | Drug Info | [44], [45], [46] | |||
2 | Eprosartan | Drug Info | [47], [48] | |||
3 | Forasartan | Drug Info | [9], [49] | |||
4 | Irbesartan | Drug Info | [1], [50] | |||
5 | Losartan | Drug Info | [1], [51], [52], [53] | |||
6 | Micardis telmisartan | Drug Info | [54] | |||
7 | Olmesartan medoxomil | Drug Info | [55] | |||
8 | Saprisartan | Drug Info | [16] | |||
9 | Tasosartan | Drug Info | [58] | |||
10 | Telmisartan | Drug Info | [59] | |||
11 | Valsartan | Drug Info | [1], [51], [60] | |||
12 | Pratosartan | Drug Info | [61] | |||
13 | sparsentan | Drug Info | [62] | |||
14 | CL-329167 | Drug Info | [63], [18] | |||
15 | TRV027 | Drug Info | [64] | |||
16 | YM-358 | Drug Info | [65], [18] | |||
17 | KRH-594 | Drug Info | [66] | |||
18 | MILFASARTAN | Drug Info | [67], [18] | |||
19 | RIPISARTAN | Drug Info | [68], [18] | |||
20 | TAK-591 | Drug Info | [70] | |||
21 | UR-7198 | Drug Info | [71] | |||
22 | A-81988 | Drug Info | [72] | |||
23 | CR-3834 | Drug Info | [73] | |||
24 | L-158809 | Drug Info | [75] | |||
25 | (E)-N-(3-iodoprop-2-enyl)-2beta-carbomethoxy-3beta-(4'-methylphenyl)n | Drug Info | [79] | |||
26 | 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone | Drug Info | [81] | |||
27 | 4-[(diphenylmethyl)amino]-2-phenylquinazoline | Drug Info | [82] | |||
28 | 5-butyl-methyl immidazole carboxylate 30 | Drug Info | [83] | |||
29 | 5-oxo-1-2-4-oxadiazol biphenyl | Drug Info | [84] | |||
30 | EXP3174 | Drug Info | [87], [88] | |||
31 | LY301875 | Drug Info | [91] | |||
32 | LY303336 | Drug Info | [91] | |||
33 | N,N`-bis-alkyl butylimmidazole 12b | Drug Info | [92] | |||
34 | [125I]EXP985 | Drug Info | [93] | |||
35 | [3H]GBR12935 | Drug Info | [94] | |||
Blocker | [+] 1 Blocker drugs | + | ||||
1 | S-474474 | Drug Info | [23] | |||
Agonist | [+] 3 Agonist drugs | + | ||||
1 | Zolasartan | Drug Info | [69] | |||
2 | angiotensin III | Drug Info | [77] | |||
3 | L-163,101 | Drug Info | [90] |
Chemical Structure based Activity Landscape of Target | Top |
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Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Co-Targets | Top | |||||
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Co-Targets |
Target Poor or Non Binders | Top | |||||
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Target Poor or Non Binders |
Target Regulators | Top | |||||
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Target-regulating microRNAs |
Target Profiles in Patients | Top | |||||
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Target Expression Profile (TEP) |
Target-Related Models and Studies | Top | |||||
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Target Validation | ||||||
Target QSAR Model |
References | Top | |||||
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REF 1 | Radioligand binding assays: application of [(125)I]angiotensin II receptor binding. Methods Mol Biol. 2009;552:131-41. | |||||
REF 2 | 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85. | |||||
REF 3 | URL: 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 4 | Clinical pipeline report, company report or official report of Takeda. | |||||
REF 5 | URL: 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 6 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
REF 7 | URL: 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 8 | URL: 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 9 | Non-peptide angiotensin II receptor antagonists: chemical feature based pharmacophore identification. J Med Chem. 2003 Feb 27;46(5):716-26. | |||||
REF 10 | URL: 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 11 | New antiarrhythmic agents for atrial fibrillation and atrial flutter. Expert Opin Emerg Drugs. 2005 May;10(2):311-22. | |||||
REF 12 | URL: 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 13 | Clinical pipeline report, company report or official report of Boehringer-Ingelheim Pharmaceuticals. | |||||
REF 14 | Effect of angiotensin receptor blockade on endothelial function: focus on olmesartan medoxomil. Vasc Health Risk Manag. 2009;5(1):301-14. | |||||
REF 15 | URL: 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 16 | Pharmacological properties of angiotensin II receptor antagonists. Can J Cardiol. 1999 Nov;15 Suppl F:26F-8F. | |||||
REF 17 | URL: 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 18 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 19 | URL: 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 20 | URL: 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 21 | URL: 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 22 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002623) | |||||
REF 23 | Clinical pipeline report, company report or official report of Shionogi (2011). | |||||
REF 24 | ClinicalTrials.gov (NCT03493685) Study of Sparsentan in Patients With Primary Focal Segmental Glomerulosclerosis (FSGS) (DUPLEX). U.S. National Institutes of Health. | |||||
REF 25 | ClinicalTrials.gov (NCT02480764) TAK-491 (Azilsartan Medoxomil) Compared to Valsartan in Chinese Participants With Hypertension. | |||||
REF 26 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004990) | |||||
REF 27 | ClinicalTrials.gov (NCT01966601) A Study to Explore the Efficacy of TRV027 in Patients Hospitalized for Acute Decompensated Heart Failure. U.S. National Institutes of Health. | |||||
REF 28 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002583) | |||||
REF 29 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007913) | |||||
REF 30 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002993) | |||||
REF 31 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004530) | |||||
REF 32 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001788) | |||||
REF 33 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028308) | |||||
REF 34 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010597) | |||||
REF 35 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002509) | |||||
REF 36 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022642) | |||||
REF 37 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001562) | |||||
REF 38 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003495) | |||||
REF 39 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007561) | |||||
REF 40 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004864) | |||||
REF 41 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004861) | |||||
REF 42 | The amino-terminus of angiotensin II contacts several ectodomains of the angiotensin II receptor AT1. J Med Chem. 2010 Mar 11;53(5):2063-75. | |||||
REF 43 | 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4. | |||||
REF 44 | Candesartan: widening indications for this angiotensin II receptor blocker Expert Opin Pharmacother. 2009 Aug;10(12):1995-2007. | |||||
REF 45 | Angiotensin II type 1 receptor blockade: a novel therapeutic concept. Blood Press Suppl. 2000;1:9-13. | |||||
REF 46 | Binding 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 47 | Clinical profile of eprosartan: a different angiotensin II receptor blocker. Cardiovasc Hematol Agents Med Chem. 2008 Oct;6(4):253-7. | |||||
REF 48 | Characterization of [3H]SK&F 108566 as a radioligand for angiotensin type-1 receptor. J Recept Res. 1993;13(5):849-61. | |||||
REF 49 | Possible 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 50 | Binding characteristics of [(3)H]-irbesartan to human recombinant angiotensin type 1 receptors. J Renin Angiotensin Aldosterone Syst. 2000 Jun;1(2):159-65. | |||||
REF 51 | Knockouts model the 100 best-selling drugs--will they model the next 100 Nat Rev Drug Discov. 2003 Jan;2(1):38-51. | |||||
REF 52 | Effect of episodic hypoxia on sympathetic activity and blood pressure. Respir Physiol. 2000 Feb;119(2-3):189-97. | |||||
REF 53 | Characterization of [3H]losartan receptors in isolated rat glomeruli. Eur J Pharmacol. 1993 Oct 15;247(2):193-8. | |||||
REF 54 | The 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 55 | Mechanism 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 56 | Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. J Med Chem. 2008 Jul 24;51(14):4150-69. | |||||
REF 57 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
REF 58 | Tasosartan, enoltasosartan, and angiotensin II receptor blockade: the confounding role of protein binding. J Pharmacol Exp Ther. 2000 Nov;295(2):649-54. | |||||
REF 59 | Deletion of angiotensin II type I receptor reduces hepatic steatosis. J Hepatol. 2009 Jun;50(6):1226-35. | |||||
REF 60 | Interaction 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 61 | Clinical efficacy of a new angiotensin II type 1 receptor blocker, pratosartan, in hypertensive patients. Hypertens Res. 2008 Feb;31(2):281-7. | |||||
REF 62 | Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43. | |||||
REF 63 | Distribution 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 64 | First clinical experience with TRV027: pharmacokinetics and pharmacodynamics in healthy volunteers. J Clin Pharmacol. 2013 Sep;53(9):892-9. | |||||
REF 65 | Effects 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 66 | Binding 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 67 | Dual action molecules: bioassays of combined novel antioxidants and angiotensin II receptor antagonists. Eur J Pharmacol. 2012 Nov 15;695(1-3):96-103. | |||||
REF 68 | In vitro pharmacological characterization of UP 269-6, a novel nonpeptide angiotensin II receptor antagonist. Fundam Clin Pharmacol. 1995;9(2):119-28. | |||||
REF 69 | Azilsartan: a newly approved angiotensin II receptor blocker. Cardiol Rev. 2011 Nov-Dec;19(6):300-4. | |||||
REF 70 | Clinical pipeline report, company report or official report of Takeda (2009). | |||||
REF 71 | Pharmacologic 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 72 | [3H]A-81988, a potent, selective, competitive antagonist radioligand for angiotensin AT1 receptors. Eur J Pharmacol. 1994 Mar 15;267(1):49-54. | |||||
REF 73 | Pharmacokinetic study of a new angiotensin-AT1 antagonist by HPLC. J Pharm Biomed Anal. 2008 Sep 29;48(2):422-7. | |||||
REF 74 | In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. | |||||
REF 75 | Characterization 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 76 | Virtual Screening in Drug Discovery, Juan Alvarez Brian Shoichet. Page(218). | |||||
REF 77 | URL: 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 78 | Pharmacology 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 79 | Pharmacological 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 80 | Discovery and development of aryl-fused imidazole-based angiotensin II antagonists, Bioorg. Med. Chem. Lett. 4(1):213-218 (1994). | |||||
REF 81 | Discovery 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 82 | Identification 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 83 | The 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 84 | Synthesis 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 85 | Pharmaceutical compositions comprising NEP-inhibitors, inhibitors of the endogenous endothelin producing system and AT1 receptor antagonists | |||||
REF 86 | Synthesis and angiotensin II receptor antagonistic activities of benzimidazole derivatives bearing acidic heterocycles as novel tetrazole bioisoste... J Med Chem. 1996 Dec 20;39(26):5228-35. | |||||
REF 87 | Angiotensin II receptors and angiotensin II receptor antagonists. Pharmacol Rev. 1993 Jun;45(2):205-51. | |||||
REF 88 | Angiotensin II receptor antagonists: imidazoles and pyrroles bearing hydroxymethyl and carboxy substituents, Bioorg. Med. Chem. Lett. 4(1):177-182 (1994). | |||||
REF 89 | Selective angiotensin II AT2 receptor agonists: Benzamide structure-activity relationships. Bioorg Med Chem. 2008 Jul 15;16(14):6841-9. | |||||
REF 90 | Structural 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 91 | Inhibition 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 92 | Rational 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 93 | [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 94 | Specific 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. |
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