Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMKS1DV)

• Drug Name: SARALASIN Drug Info
• Synonyms: Saralasin; 34273-10-4; UNII-H2AFV2HE66; (Sar1,Val5,Ala8)-Angiotensin II; CHEMBL938; H2AFV2HE66; Saralasinum [INN-Latin]; Saralasin [INN:BAN]; Saralasine [INN-French]; Saralasina [INN-Spanish]; Saralasinum; Saralasine; Saralasina; (1-(N-Methylglycin) 5-L-valin, 8-L-alanin)angiotensin II; Angiotensin II, 1-(N-methylglycine)-5-L-valine-8-L-alanine-; NCGC00166135-01; N-(1-(N-(N-(N-(N-(N2-(N-methylglycly)-L-arginyl)-L-valyl)-L-tyrosyl)-L-valyl)-L-histidyl)-L-prolyl)-L-alanine; SCHEMBL23; AC1O44IX; DSSTox_RID_81710

Indication

Disease Entry	ICD 11	Status	REF
Hypertension	BA00-BA04	Approved	[1]

• Cross-matching ID:
  PubChem CID: 6324663
  ChEBI ID: CHEBI:135894
  CAS Number: CAS 34273-10-4
  TTD Drug ID: DMKS1DV

Molecule-Related Drug Atlas

Drug(s) Targeting Angiotensin II receptor type-2 (AGTR2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ANGIOTENSIN II	DMLWQ27	Increase blood pressure	BA04	Approved	[4]
EMA-401	DMYOUB6	Peripheral neuropathy	8C0Z	Phase 2	[5]
MP-157	DM5VXWO	Hypertension	BA00-BA04	Phase 1	[6]
PMID25416646-Compound-Figure5-E	DMYO7VH	N. A.	N. A.	Patented	[7]
Phenylpyridine derivative 3	DMDT5JI	N. A.	N. A.	Patented	[7]
1-(biphenyl-4-yl-methyl)-1H-imidazole derivative 1	DMGYZQ2	N. A.	N. A.	Patented	[7]
Fonsartan	DM15LAP	Hypertension	BA00-BA04	Discontinued in Phase 2	[8]
L-158282	DMKSEIY	N. A.	N. A.	Discontinued in Phase 2	[9]
TAK-591	DM25DB4	Hypertension	BA00-BA04	Discontinued in Phase 1	[10]
L-159689	DM9JE7Y	Hypertension	BA00-BA04	Terminated	[11]

Drug(s) Targeting Angiotensin II receptor type-1 (AGTR1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Losartan	DM72JXH	Diabetic kidney disease	GB61.Z	Approved	[12]
Olmesartan medoxomil	DMWBHRY	High blood pressure	BA00	Approved	[13]
Irbesartan	DMTP1DC	Diabetic kidney disease	GB61.Z	Approved	[12]
Valsartan	DMREUQ6	Chronic heart failure	BD1Z	Approved	[12]
Candesartan	DMRK8OT	Chronic heart failure	BD1Z	Approved	[14]
Telmisartan	DMS3GX2	Hypertension	BA00-BA04	Approved	[15]
ANGIOTENSIN II	DMLWQ27	Increase blood pressure	BA04	Approved	[16]
Tasosartan	DMM13DI	Hypertension	BA00-BA04	Approved	[17]
Eprosartan	DM07K2I	Hypertension	BA00-BA04	Approved	[18]
Sparsentan	DMMP51W	IgA nephropathy	MF8Y	Approved	[19]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Angiotensin II receptor type-1 (AGTR1)	TT8DBY3	AGTR1_HUMAN	Inhibitor	[2]
Angiotensin II receptor type-2 (AGTR2)	TTQVOEI	AGTR2_HUMAN	Inhibitor	[3]

References

• [1] 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).
• [2] 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.
• [3] cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain... J Med Chem. 2008 Nov 27;51(22):7094-8.
• [4] The preparation of (perfluoroalkyl)imidazoles as nonpeptide angiotensin II receptor antagonists, Bioorg. Med. Chem. Lett. 3(5):895-898 (1993).
• [5] Clinical pipeline report, company report or official report of Spinifex.
• [6] As drug target reemerges, the question is to block or stimulate it. Nature Medicine. Spoonful of Medicine. 05 Feb 2014. Cassandra Willyard
• [7] PPAR ligands and their therapeutic applications: a patent review (2008 - 2014).Expert Opin Ther Pat. 2015 Feb;25(2):175-91.
• [8] Role of the angiotensin II AT2-subtype receptors in the blood pressure-lowering effect of losartan in salt-restricted rats. J Hypertens. 1998 Dec;16(12 Pt 2):2039-43.
• [9] Subtituted phenylthiophene benzoylsulfonamides with potent binding affinity to angiotensin II AT1 and AT2 receptors, Bioorg. Med. Chem. Lett. 4(1):189-194 (1994).
• [10] Clinical pipeline report, company report or official report of Takeda (2009).
• [11] The design, binding affinity prediction and synthesis of macrocyclic angiotensin II AT1 and AT2 receptor antagonists, Bioorg. Med. Chem. Lett. 6(8):923-928 (1996).
• [12] Radioligand binding assays: application of [(125)I]angiotensin II receptor binding. Methods Mol Biol. 2009;552:131-41.
• [13] 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.
• [14] Candesartan: widening indications for this angiotensin II receptor blocker Expert Opin Pharmacother. 2009 Aug;10(12):1995-2007.
• [15] Deletion of angiotensin II type I receptor reduces hepatic steatosis. J Hepatol. 2009 Jun;50(6):1226-35.
• [16] 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.
• [17] Tasosartan, enoltasosartan, and angiotensin II receptor blockade: the confounding role of protein binding. J Pharmacol Exp Ther. 2000 Nov;295(2):649-54.
• [18] Clinical profile of eprosartan: a different angiotensin II receptor blocker. Cardiovasc Hematol Agents Med Chem. 2008 Oct;6(4):253-7.
• [19] Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.