Target Validation Information
TTD ID	TTDS00267
Target Name	Type-1 angiotensin II receptor
Type of Target	Successful target
Drug Potency against Target	Irbesartan		IC50 = 1.3 nM	[1]
	Eprosartan		IC50 = 1.5 nM	[1]
	Candesartan		IC50 = 12.76 nM	[1]
	Losartan		IC50 = 19 nM	[1]
	Olmesartan		IC50 = 7.7 nM	[1]
	Valsartan		IC50 = 8.9 nM	[1]
	Telmisartan		IC50 = 9.2 nM	[1]
	Irbesartan		Ki = 0.8 nM	[2]
	Losartan		Ki = 2.2 nM	[3]
	Candesartan		Ki = 2100 nM	[4]
	L-159093		IC50 = 0.1 nM	[2]
	SARALASIN		IC50 = 1 nM	[5]
	L-159689		IC50 = 1.7 nM	[2]
	HELENALIN		IC50 = 18639 nM	[6]
	Carboxylic Acid Metabolite (E-3174)		IC50 = 22 nM	[7]
	GNF-PF-3832		IC50 = 2893 nM	[6]
	TAK-536		IC50 = 420 nM	[8]
	CV-11194		IC50 = 550 nM	[8]
	GNF-PF-2812		IC50 = 6975 nM	[6]
	GNF-PF-2307		IC50 = 7431 nM	[6]
	4-(2-Butyl-benzoimidazol-1-ylmethyl)-phenol		IC50 = 8500 nM	[9]
	[Sar1,Bpa3]AngII		Ki = 0.7 nM	[10]
	L-162782		Ki = 0.7 nM	[11]
	[Sar1,Bpa8]AngII		Ki = 0.8 nM	[10]
	ANGIOTENSIN II		Ki = 0.9 nM	[10]
	[Sar1,Tdf8]AngII		Ki = 0.9 nM	[10]
	[Sar1,Tdf3]AngII		Ki = 1.3 nM	[10]
	BMS-248360		Ki = 10 nM	[2]
	[Sar1,Bpa2]AngII		Ki = 18.3 nM	[10]
	[Bpa1]AngII		Ki = 19.4 nM	[10]
	L-162313		Ki = 2 nM	[11]
	[Sar1,Tdf2]AngII		Ki = 24.7 nM	[10]
	[Tdf1]AngII		Ki = 26.4 nM	[10]
Ref 1	Med Chem. 2005 Jul;1(4):405-21.GPCR agonists and antagonists in the clinic. To Reference
Ref 2	J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm. To Reference
Ref 3	Drug Discov Today. 2006 Jun;11(11-12):481-93.I want a new drug: G-protein-coupled receptors in drug development. To Reference
Ref 4	Nat Rev Drug Discov. 2007 Apr;6(4):313-25.Antagonism of the prostaglandin D2 receptors DP1 and CRTH2 as an approach to treat allergic diseases. To Reference
Ref 5	J 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. To Reference
Ref 6	Bioorg 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). To Reference
Ref 7	Bioorg. Med. Chem. Lett. 4(1):177-182 (1994) To Reference
Ref 8	J 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. To Reference
Ref 9	Bioorg. Med. Chem. Lett. 4(1):213-218 (1994) To Reference
Ref 10	J Med Chem. 2010 Mar 11;53(5):2063-75.The amino-terminus of angiotensin II contacts several ectodomains of the angiotensin II receptor AT1. To Reference
Ref 11	Bioorg Med Chem. 2008 Jul 15;16(14):6841-9. Epub 2008 Jul 1.Selective angiotensin II AT2 receptor agonists: Benzamide structure-activity relationships. To Reference

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Dr. Chen Yuzong
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Professor in Department of Pharmacy
National University of Singapore, Singapore

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