Target Information

Target General Information

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Target ID

T85574 (Former ID: TTDI01751)

Target Name

Angiotensin II receptor (AGTR)

Gene Name

NO-GeName

Target Type

Clinical trial target

[1]

Disease

[+] 1 Target-related Diseases

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

NOUNIPROTAC

Drugs and Modes of Action

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Clinical Trial Drug(s)

[+] 2 Clinical Trial Drugs

CYT-006-AngQb

Drug Info

Phase 2

Hypertension

[2]

DA-727

Drug Info

Phase 1

Hypertension

[3]

Discontinued Drug(s)

[+] 26 Discontinued Drugs

BIBR-363

Drug Info

Discontinued in Phase 2

Hypertension

[4]

E-4177

Drug Info

Discontinued in Phase 2

Hypertension

[5]

Elisartan potassium

Drug Info

Discontinued in Phase 2

Hypertension

[6]

ETRX-101

Drug Info

Discontinued in Phase 2

Anemia

[7]

FK-739

Drug Info

Discontinued in Phase 2

Hypertension

[8]

ICI-D-8731

Drug Info

Discontinued in Phase 2

Hypertension

[9]

CGP-48369

Drug Info

Discontinued in Phase 1

Hypertension

[10]

DuP-532

Drug Info

Discontinued in Phase 1

Hypertension

[11]

ICI-D-6888

Drug Info

Discontinued in Phase 1

Hypertension

[12]

A-81282

Drug Info

Terminated

Hypertension

[13]

A-81988

Drug Info

Terminated

Hypertension

[14]

BIBS-222

Drug Info

Terminated

Hypertension

[15]

BIBS-39

Drug Info

Terminated

Hypertension

[16]

BMS-180560

Drug Info

Terminated

Hypertension

[17]

CI-996

Drug Info

Terminated

Hypertension

[18]

DMP-811

Drug Info

Terminated

Hypertension

[19]

EXP-6803

Drug Info

Terminated

Hypertension

[20]

FR-149581

Drug Info

Terminated

Hypertension

[21]

KW-3433

Drug Info

Terminated

Hypertension

[22]

L-163017

Drug Info

Terminated

Hypertension

[23]

ME-3221

Drug Info

Terminated

Hypertension

[24]

RWJ-46458

Drug Info

Terminated

Hypertension

[25]

SC-51316

Drug Info

Terminated

Hypertension

[26]

SL-910102

Drug Info

Terminated

Hypertension

[27]

WAY-126227

Drug Info

Terminated

Hypertension

[28]

ZD-7155

Drug Info

Terminated

Hypertension

[29], [30]

Mode of Action

[+] 2 Modes of Action

Modulator

[+] 27 Modulator drugs

DA-727

Drug Info

[31]

BIBR-363

Drug Info

[32]

E-4177

Drug Info

[33]

Elisartan potassium

Drug Info

[34]

ETRX-101

Drug Info

[35]

FK-739

Drug Info

[36]

ICI-D-8731

Drug Info

[37]

CGP-48369

Drug Info

[38]

DuP-532

Drug Info

[39]

ICI-D-6888

Drug Info

[40]

A-81282

Drug Info

[41]

A-81988

Drug Info

[42]

BIBS-222

Drug Info

[43]

BIBS-39

Drug Info

[43]

BMS-180560

Drug Info

[44]

CI-996

Drug Info

[45]

DMP-811

Drug Info

[46]

EXP-6803

Drug Info

[47]

KW-3433

Drug Info

[49]

L-163017

Drug Info

[50]

ME-3221

Drug Info

[51]

RWJ-46458

Drug Info

[52]

SC-51316

Drug Info

[53]

SL-910102

Drug Info

[54]

WAY-126227

Drug Info

[52]

ZD-7155

Drug Info

[55]

A-82186

Drug Info

[56]

Antagonist

[+] 1 Antagonist drugs

FR-149581

Drug Info

[48]

Chemical Structure based Activity Landscape of Target

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Drug Property Profile of Target

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(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"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

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Target Poor or Non Binders

Target Poor or Non Binders Info

Target Affiliated Biological Pathways

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KEGG Pathway

[+] 8 KEGG Pathways

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

References

Top

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 800002508)

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 800002509)

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 800003145)

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 800002512)

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 800002622)

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 800003447)

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 800002624)

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 800000418)

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 800007779)

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 800004961)

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 800004951)

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 800002995)

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 800002575)

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

Pharmacologic characterization of CI-996, a new angiotensin receptor antagonist. J Pharmacol Exp Ther. 1995 Mar;272(3):963-9.

REF 46

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 47

Nonpeptide angiotensin II receptor antagonists. IV. EXP6155 and EXP6803. Hypertension. 1989 May;13(5):489-97.

REF 48

US patent application no. 2003,0087,306, Methods for identifying novel multimeric agents that modulate receptors.

REF 49

Effects of various antihypertensive drugs on the function of osteoblast. Biol Pharm Bull. 2001 Jun;24(6):628-33.

REF 50

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 51

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 52

WO patent application no. 1996,0402,58, Spironolactone and angiotensin ii antagonist combination therapy for treatment of congestive heart failure.

REF 53

In vitro pharmacology of a nonpeptidic angiotensin II receptor antagonist, SC-51316. J Pharmacol Exp Ther. 1992 Jun;261(3):1037-43.

REF 54

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 55

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.

REF 56

WO patent application no. 2011,0583,31, Pemirolast for the treatment of systemic low grade inflammation.

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