Target Validation Information
Target ID T74456
Target Name Type-1 angiotensin II receptor
Target Type
Successful
Drug Potency against Target Eprosartan Drug Info IC50 = 1.5 nM [552611]
Candesartan Drug Info IC50 = 12.76 nM [552611]
Irbesartan Drug Info Ki = 0.8 nM [527799]
[Sar1,Bpa3]AngII Drug Info Ki = 0.7 nM [530710]
[Sar1,Bpa8]AngII Drug Info Ki = 0.8 nM [530710]
GNF-PF-2307 Drug Info IC50 = 7431 nM [531262]
L-159093 Drug Info IC50 = 0.1 nM [527799]
L-159689 Drug Info IC50 = 1.7 nM [527799]
GNF-PF-3832 Drug Info IC50 = 2893 nM [531262]
GNF-PF-2812 Drug Info IC50 = 6975 nM [531262]
Losartan Drug Info Ki = 2.2 nM [552598]
CV-11194 Drug Info IC50 = 550 nM [534298]
[Sar1,Tdf3]AngII Drug Info Ki = 1.3 nM [530710]
Telmisartan Drug Info IC50 = 9.2 nM [552611]
4-(2-Butyl-benzoimidazol-1-ylmethyl)-phenol Drug Info IC50 = 8500 nM
Valsartan Drug Info IC50 = 8.9 nM [552611]
Azilsartan Drug Info IC50 = 420 nM [534298]
PS433540 Drug Info Ki = 10 nM [527799]
[Bpa1]AngII Drug Info Ki = 19.4 nM [530710]
HELENALIN Drug Info IC50 = 18639 nM [531262]
[Sar1,Tdf2]AngII Drug Info Ki = 24.7 nM [530710]
[Sar1,Bpa2]AngII Drug Info Ki = 18.3 nM [530710]
[Tdf1]AngII Drug Info Ki = 26.4 nM [530710]
[Sar1,Tdf8]AngII Drug Info Ki = 0.9 nM [530710]
ANGIOTENSIN II Drug Info Ki = 0.9 nM [530710]
SARALASIN Drug Info IC50 = 1 nM [529569]
L-162313 Drug Info Ki = 2 nM [529578]
L-162782 Drug Info Ki = 0.7 nM [529578]
Carboxylic Acid Metabolite (E-3174) Drug Info IC50 = 22 nM
References
Ref 552611GPCR agonists and antagonists in the clinic. Med Chem. 2005 Jul;1(4):405-21.
Ref 552611GPCR agonists and antagonists in the clinic. Med Chem. 2005 Jul;1(4):405-21.
Ref 527799J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm.
Ref 530710J Med Chem. 2010 Mar 11;53(5):2063-75.The amino-terminus of angiotensin II contacts several ectodomains of the angiotensin II receptor AT1.
Ref 530710J Med Chem. 2010 Mar 11;53(5):2063-75.The amino-terminus of angiotensin II contacts several ectodomains of the angiotensin II receptor AT1.
Ref 531262Bioorg 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).
Ref 527799J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm.
Ref 527799J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm.
Ref 531262Bioorg 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).
Ref 531262Bioorg 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).
Ref 552598I want a new drug: G-protein-coupled receptors in drug development. Drug Discov Today. 2006 Jun;11(11-12):481-93.
Ref 534298J 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.
Ref 530710J Med Chem. 2010 Mar 11;53(5):2063-75.The amino-terminus of angiotensin II contacts several ectodomains of the angiotensin II receptor AT1.
Ref 552611GPCR agonists and antagonists in the clinic. Med Chem. 2005 Jul;1(4):405-21.
Ref 552611GPCR agonists and antagonists in the clinic. Med Chem. 2005 Jul;1(4):405-21.
Ref 534298J 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.
Ref 527799J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm.
Ref 530710J Med Chem. 2010 Mar 11;53(5):2063-75.The amino-terminus of angiotensin II contacts several ectodomains of the angiotensin II receptor AT1.
Ref 531262Bioorg 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).
Ref 530710J Med Chem. 2010 Mar 11;53(5):2063-75.The amino-terminus of angiotensin II contacts several ectodomains of the angiotensin II receptor AT1.
Ref 530710J Med Chem. 2010 Mar 11;53(5):2063-75.The amino-terminus of angiotensin II contacts several ectodomains of the angiotensin II receptor AT1.
Ref 530710J Med Chem. 2010 Mar 11;53(5):2063-75.The amino-terminus of angiotensin II contacts several ectodomains of the angiotensin II receptor AT1.
Ref 530710J Med Chem. 2010 Mar 11;53(5):2063-75.The amino-terminus of angiotensin II contacts several ectodomains of the angiotensin II receptor AT1.
Ref 530710J Med Chem. 2010 Mar 11;53(5):2063-75.The amino-terminus of angiotensin II contacts several ectodomains of the angiotensin II receptor AT1.
Ref 529569J 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.
Ref 529578Bioorg Med Chem. 2008 Jul 15;16(14):6841-9. Epub 2008 Jul 1.Selective angiotensin II AT2 receptor agonists: Benzamide structure-activity relationships.
Ref 529578Bioorg Med Chem. 2008 Jul 15;16(14):6841-9. Epub 2008 Jul 1.Selective angiotensin II AT2 receptor agonists: Benzamide structure-activity relationships.

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