Target Validation Information
TTD ID	T74456
Target Name	Angiotensin II receptor type-1 (AGTR1)
Type of Target	Successful
Drug Potency against Target	Candesartan	Drug Info	IC50 = 12.76 nM	[8]
	Eprosartan	Drug Info	IC50 = 1.5 nM	[8]
	Irbesartan	Drug Info	Ki = 0.8 nM	[1]
	Losartan	Drug Info	Ki = 2.2 nM	[7]
	Telmisartan	Drug Info	IC50 = 9.2 nM	[8]
	Valsartan	Drug Info	IC50 = 8.9 nM	[8]
	4-(2-Butyl-benzoimidazol-1-ylmethyl)-phenol	Drug Info	IC50 = 8500 nM
	ANGIOTENSIN II	Drug Info	Ki = 0.9 nM	[4]
	Azilsartan	Drug Info	IC50 = 420 nM	[6]
	CV-11194	Drug Info	IC50 = 550 nM	[6]
	EXP3174	Drug Info	IC50 = 22 nM
	GNF-PF-2307	Drug Info	IC50 = 7431 nM	[5]
	GNF-PF-2812	Drug Info	IC50 = 6975 nM	[5]
	GNF-PF-3832	Drug Info	IC50 = 2893 nM	[5]
	HELENALIN	Drug Info	IC50 = 18639 nM	[5]
	L-159093	Drug Info	IC50 = 0.1 nM	[1]
	L-159689	Drug Info	IC50 = 1.7 nM	[1]
	L-162313	Drug Info	Ki = 2 nM	[3]
	L-162782	Drug Info	Ki = 0.7 nM	[3]
	SARALASIN	Drug Info	IC50 = 1 nM	[2]
	Sparsentan	Drug Info	Ki = 10 nM	[1]
	[Bpa1]AngII	Drug Info	Ki = 19.4 nM	[4]
	[Sar1,Bpa2]AngII	Drug Info	Ki = 18.3 nM	[4]
	[Sar1,Bpa3]AngII	Drug Info	Ki = 0.7 nM	[4]
	[Sar1,Bpa8]AngII	Drug Info	Ki = 0.8 nM	[4]
	[Sar1,Tdf2]AngII	Drug Info	Ki = 24.7 nM	[4]
	[Sar1,Tdf3]AngII	Drug Info	Ki = 1.3 nM	[4]
	[Sar1,Tdf8]AngII	Drug Info	Ki = 0.9 nM	[4]
	[Tdf1]AngII	Drug Info	Ki = 26.4 nM	[4]
References
REF 1	Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.
REF 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.
REF 3	Selective angiotensin II AT2 receptor agonists: Benzamide structure-activity relationships. Bioorg Med Chem. 2008 Jul 15;16(14):6841-9.
REF 4	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 5	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 6	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 7	I want a new drug: G-protein-coupled receptors in drug development. Drug Discov Today. 2006 Jun;11(11-12):481-93.
REF 8	GPCR agonists and antagonists in the clinic. Med Chem. 2005 Jul;1(4):405-21.

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