Target Information
Target General Information | Top | |||||
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Target ID |
T85574
(Former ID: TTDI01751)
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Target Name |
Angiotensin II receptor (AGTR)
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Gene Name |
NO-GeName
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Target Type |
Clinical trial target
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[1] | ||||
Disease | [+] 1 Target-related Diseases | + | ||||
1 | Hypertension [ICD-11: BA00-BA04] | |||||
Function |
Receptor for angiotensin II. Mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system.
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UniProt ID |
Drugs and Modes of Action | Top | |||||
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Clinical Trial Drug(s) | [+] 2 Clinical Trial Drugs | + | ||||
1 | CYT-006-AngQb | Drug Info | Phase 2 | Hypertension | [2] | |
2 | DA-727 | Drug Info | Phase 1 | Hypertension | [3] | |
Discontinued Drug(s) | [+] 24 Discontinued Drugs | + | ||||
1 | BIBR-363 | Drug Info | Discontinued in Phase 2 | Hypertension | [4] | |
2 | E-4177 | Drug Info | Discontinued in Phase 2 | Hypertension | [5] | |
3 | Elisartan potassium | Drug Info | Discontinued in Phase 2 | Hypertension | [6] | |
4 | ETRX-101 | Drug Info | Discontinued in Phase 2 | Anemia | [7] | |
5 | FK-739 | Drug Info | Discontinued in Phase 2 | Hypertension | [8] | |
6 | ICI-D-8731 | Drug Info | Discontinued in Phase 2 | Hypertension | [9] | |
7 | CGP-48369 | Drug Info | Discontinued in Phase 1 | Hypertension | [10] | |
8 | DuP-532 | Drug Info | Discontinued in Phase 1 | Hypertension | [11] | |
9 | ICI-D-6888 | Drug Info | Discontinued in Phase 1 | Hypertension | [12] | |
10 | A-81282 | Drug Info | Terminated | Hypertension | [15] | |
11 | A-81988 | Drug Info | Terminated | Hypertension | [16] | |
12 | BIBS-222 | Drug Info | Terminated | Hypertension | [17] | |
13 | BIBS-39 | Drug Info | Terminated | Hypertension | [18] | |
14 | BMS-180560 | Drug Info | Terminated | Hypertension | [19] | |
15 | DMP-811 | Drug Info | Terminated | Hypertension | [20] | |
16 | EXP-6803 | Drug Info | Terminated | Hypertension | [21] | |
17 | FR-149581 | Drug Info | Terminated | Hypertension | [22] | |
18 | KW-3433 | Drug Info | Terminated | Hypertension | [23] | |
19 | L-163017 | Drug Info | Terminated | Hypertension | [24] | |
20 | ME-3221 | Drug Info | Terminated | Hypertension | [25] | |
21 | SC-51316 | Drug Info | Terminated | Hypertension | [26] | |
22 | SL-910102 | Drug Info | Terminated | Hypertension | [27] | |
23 | WAY-126227 | Drug Info | Terminated | Hypertension | [28] | |
24 | ZD-7155 | Drug Info | Terminated | Hypertension | [29], [30] | |
Mode of Action | [+] 2 Modes of Action | + | ||||
Modulator | [+] 24 Modulator drugs | + | ||||
1 | DA-727 | Drug Info | [31] | |||
2 | BIBR-363 | Drug Info | [32] | |||
3 | E-4177 | Drug Info | [33] | |||
4 | Elisartan potassium | Drug Info | [34] | |||
5 | ETRX-101 | Drug Info | [35] | |||
6 | FK-739 | Drug Info | [36] | |||
7 | ICI-D-8731 | Drug Info | [37] | |||
8 | CGP-48369 | Drug Info | [38] | |||
9 | DuP-532 | Drug Info | [39] | |||
10 | ICI-D-6888 | Drug Info | [40] | |||
11 | A-81282 | Drug Info | [41] | |||
12 | A-81988 | Drug Info | [42] | |||
13 | BIBS-222 | Drug Info | [43] | |||
14 | BIBS-39 | Drug Info | [43] | |||
15 | BMS-180560 | Drug Info | [44] | |||
16 | DMP-811 | Drug Info | [45] | |||
17 | EXP-6803 | Drug Info | [46] | |||
18 | KW-3433 | Drug Info | [48] | |||
19 | L-163017 | Drug Info | [49] | |||
20 | ME-3221 | Drug Info | [50] | |||
21 | SC-51316 | Drug Info | [51] | |||
22 | SL-910102 | Drug Info | [52] | |||
23 | WAY-126227 | Drug Info | [53] | |||
24 | ZD-7155 | Drug Info | [54] | |||
Antagonist | [+] 1 Antagonist drugs | + | ||||
1 | FR-149581 | Drug Info | [47] |
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 |
Target Poor or Non Binders | Top | |||||
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Target Poor or Non Binders |
Target Affiliated Biological Pathways | Top | |||||
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KEGG Pathway | [+] 8 KEGG Pathways | + | ||||
1 | Calcium signaling pathway | |||||
2 | cGMP-PKG signaling pathway | |||||
3 | Neuroactive ligand-receptor interaction | |||||
4 | Adrenergic signaling in cardiomyocytes | |||||
5 | Vascular smooth muscle contraction | |||||
6 | Renin-angiotensin system | |||||
7 | Renin secretion | |||||
8 | Pathways in cancer |
References | Top | |||||
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REF 1 | CYT-006-AngQb, a vaccine against angiotensin II for the potential treatment of hypertension. Curr Opin Investig Drugs. 2009 Mar;10(3):269-75. | |||||
REF 2 | ClinicalTrials.gov (NCT00710372) Safety, Tolerability and Efficacy of a Vaccine Against Essential Hypertension. U.S. National Institutes of Health. | |||||
REF 3 | Clinical pipeline report, company report or official report of Daiichi Sankyo. | |||||
REF 4 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006457) | |||||
REF 5 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002106) | |||||
REF 6 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002994) | |||||
REF 7 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013086) | |||||
REF 8 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002869) | |||||
REF 9 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002063) | |||||
REF 10 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005020) | |||||
REF 11 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001160) | |||||
REF 12 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002319) | |||||
REF 13 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002575) | |||||
REF 14 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003447) | |||||
REF 15 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002508) | |||||
REF 16 | 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 17 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003145) | |||||
REF 18 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002512) | |||||
REF 19 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002622) | |||||
REF 20 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002624) | |||||
REF 21 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000418) | |||||
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 800007779) | |||||
REF 23 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004961) | |||||
REF 24 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004951) | |||||
REF 25 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002995) | |||||
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 800001569) | |||||
REF 27 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003244) | |||||
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 800004966) | |||||
REF 29 | 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: 8324). | |||||
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 800002281) | |||||
REF 31 | WO patent application no. 2009,0880,06, Combined pharmaceutical agent. | |||||
REF 32 | Evaluation of the angiotensin challenge methodology for assessing the pharmacodynamic profile of antihypertensive drugs acting on the renin-angiotensin system. Br J Clin Pharmacol. 1999 October; 48(4): 594-604. | |||||
REF 33 | Prevention of renal damage by angiotensin II blockade, accompanied by increased renal hepatocyte growth factor in experimental hypertensive rats. Hypertension. 1999 Aug;34(2):279-84. | |||||
REF 34 | Safety and tolerability of losartan potassium, an angiotensin II receptor antagonist, compared with hydrochlorothiazide, atenolol, felodipine ER, and angiotensin-converting enzyme inhibitors for the treatment of systemic hypertension. Am J Cardiol. 1995 Apr 15;75(12):793-5. | |||||
REF 35 | WO patent application no. 2010,0332,07, Polymer conjugates of therapeutic peptides. | |||||
REF 36 | The pharmacological characterization of FK 739, a new angiotensin II-receptor antagonist. Jpn J Pharmacol. 1993 Nov;63(3):335-43. | |||||
REF 37 | Vasomotor responses in cyclosporin A-treated rats after chronic angiotensin blockade. Hypertension. 1994 Jun;23(6 Pt 2):832-7. | |||||
REF 38 | Antihypertensive therapy augments endothelium-dependent relaxations in coronary arteries of spontaneously hypertensive rats. Circulation. 1994 May;89(5):2212-8. | |||||
REF 39 | DuP 532, an angiotensin II receptor antagonist: first administration and comparison with losartan. Clin Pharmacol Ther. 1997 Jan;61(1):59-69. | |||||
REF 40 | WO patent application no. 1995,0216,09, Treatment of normotensive glaucoma with angiotensin ii antagonists. | |||||
REF 41 | Pharmacological characterization of Abbott-81282, a novel, non-peptide angiotensin-II antagonist selective for type-1 receptors. Life Sci. 1993;53(11):929-37. | |||||
REF 42 | [3H]A-81988, a potent, selective, competitive antagonist radioligand for angiotensin AT1 receptors. Eur J Pharmacol. 1994 Mar 15;267(1):49-54. | |||||
REF 43 | Characterization of BIBS 39 and BIBS 222: two new nonpeptide angiotensin II receptor antagonists. Eur J Pharmacol. 1992 Jul 21;218(1):35-41. | |||||
REF 44 | BMS-180560, an insurmountable inhibitor of angiotensin II-stimulated responses: comparison with losartan and EXP3174. Br J Pharmacol. 1994 Sep;113(1):179-89. | |||||
REF 45 | Disposition of DMP 811 (L-708,404), a potent angiotensin II receptor antagonist, in the rat, monkey, and chimpanzee. Drug Metab Dispos. 1995 Oct;23(10):1104-9. | |||||
REF 46 | Nonpeptide angiotensin II receptor antagonists. IV. EXP6155 and EXP6803. Hypertension. 1989 May;13(5):489-97. | |||||
REF 47 | US patent application no. 2003,0087,306, Methods for identifying novel multimeric agents that modulate receptors. | |||||
REF 48 | Effects of various antihypertensive drugs on the function of osteoblast. Biol Pharm Bull. 2001 Jun;24(6):628-33. | |||||
REF 49 | In vivo pharmacology of an angiotensin AT1 receptor antagonist with balanced affinity for AT2 receptors. Eur J Pharmacol. 1995 Dec 29;294(2-3):439-50. | |||||
REF 50 | Protective effects of ME3221 on hypertensive complications and lifespan in salt-loaded stroke-prone spontaneously hypertensive rats. Clin Exp Pharmacol Physiol. 1996 Mar;23(3):229-35. | |||||
REF 51 | In vitro pharmacology of a nonpeptidic angiotensin II receptor antagonist, SC-51316. J Pharmacol Exp Ther. 1992 Jun;261(3):1037-43. | |||||
REF 52 | A radioreceptor assay for the analysis of AT1-receptor antagonists. Correlation with complementary LC data reveals a potential contribution of active metabolites. J Pharm Biomed Anal. 1998 May;17(1):111-24. | |||||
REF 53 | WO patent application no. 1996,0402,58, Spironolactone and angiotensin ii antagonist combination therapy for treatment of congestive heart failure. | |||||
REF 54 | Comparative cardiovascular effects of the angiotensin II type 1 receptor antagonists ZD 7155 and losartan in the rat. J Pharm Pharmacol. 1996 Aug;48(8):829-33. |
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