Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

Target Validation Information
TTD IDTTDS00267
Target NameType-1 angiotensin II receptor    
Type of TargetSuccessful target    
Drug Potency against TargetIrbesartanIC50 = 1.3 nM[1]
EprosartanIC50 = 1.5 nM[1]
CandesartanIC50 = 12.76 nM[1]
LosartanIC50 = 19 nM[1]
OlmesartanIC50 = 7.7 nM[1]
ValsartanIC50 = 8.9 nM[1]
TelmisartanIC50 = 9.2 nM[1]
IrbesartanKi = 0.8 nM[2]
LosartanKi = 2.2 nM[3]
CandesartanKi = 2100 nM[4]
L-159093IC50 = 0.1 nM[2]
SARALASINIC50 = 1 nM[5]
L-159689IC50 = 1.7 nM[2]
HELENALINIC50 = 18639 nM[6]
Carboxylic Acid Metabolite (E-3174)IC50 = 22 nM[7]
GNF-PF-3832IC50 = 2893 nM[6]
TAK-536IC50 = 420 nM[8]
CV-11194IC50 = 550 nM[8]
GNF-PF-2812IC50 = 6975 nM[6]
GNF-PF-2307IC50 = 7431 nM[6]
4-(2-Butyl-benzoimidazol-1-ylmethyl)-phenolIC50 = 8500 nM[9]
[Sar1,Bpa3]AngIIKi = 0.7 nM[10]
L-162782Ki = 0.7 nM[11]
[Sar1,Bpa8]AngIIKi = 0.8 nM[10]
ANGIOTENSIN IIKi = 0.9 nM[10]
[Sar1,Tdf8]AngIIKi = 0.9 nM[10]
[Sar1,Tdf3]AngIIKi = 1.3 nM[10]
BMS-248360Ki = 10 nM[2]
[Sar1,Bpa2]AngIIKi = 18.3 nM[10]
[Bpa1]AngIIKi = 19.4 nM[10]
L-162313Ki = 2 nM[11]
[Sar1,Tdf2]AngIIKi = 24.7 nM[10]
[Tdf1]AngIIKi = 26.4 nM[10]
Ref 1Med Chem. 2005 Jul;1(4):405-21.GPCR agonists and antagonists in the clinic. To Reference
Ref 2J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm. To Reference
Ref 3Drug Discov Today. 2006 Jun;11(11-12):481-93.I want a new drug: G-protein-coupled receptors in drug development. To Reference
Ref 4Nat 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 5J 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 6Bioorg 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 7Bioorg. Med. Chem. Lett. 4(1):177-182 (1994) To Reference
Ref 8J 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 9Bioorg. Med. Chem. Lett. 4(1):213-218 (1994) To Reference
Ref 10J 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 11Bioorg 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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Professor in Department of Pharmacy
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