Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

Target Validation Information
TTD IDTTDS00037
Target NameBeta-2 adrenergic receptor    
Type of TargetSuccessful target    
Drug Potency against TargetFormoterolEC50 = 2.4 nM[1]
FenoterolEC50 = 74.5 nM[1]
Budesonide & formoterol fumarate dihydrateIC50 = 26 nM[2]
GSK642444IC50 = 420 nM[3]
GSK961081Ki < 10 nM[4]
GSK642444Ki = 123 nM[5]
L-796568IC50 = 2300 nM[6]
BRL-37344IC50 = 9.1 nM[7]
CGP-12177AKi = 0.1 nM[8]
GNF-PF-1694Ki = 0.145 nM[9]
ICI-118551Ki = 1 nM[10]
1-(2-isopropylphenoxy)-3-morpholinopropan-2-olKi = 1.2 nM[11]
(S,R)-(+)-fenoterolKi = 10300 nM[12]
DICHLOROISOPROTERENOLKi = 140 nM[13]
2-fluoronorepinehprineKi = 15800 nM[14]
L-755507Ki = 160 nM[8]
(R,R)-(-)-fenoterolKi = 350 nM[12]
(R,S)-(-)-fenoterolKi = 3690 nM[12]
SDZ-201106Ki = 57.3 nM[9]
1-(2-allylphenoxy)-3-morpholinopropan-2-olKi = 7 nM[11]
Ref 1Optimization of the Tango ADRB2-bla U2OS Cell Line To Reference
Ref 2Thorax. 2002 Mar;57(3):237-41.Additive anti-inflammatory effect of formoterol and budesonide on human lung fibroblasts. To Reference
Ref 3Mini Rev Med Chem. 2009 Feb;9(2):215-26.The prolyl-aminodipeptidases and their inhibitors as therapeutic targets for fibrogenic disorders. To Reference
Ref 4Expert Opin Ther Pat. 2009 Jan;19(1):1-12.Muscarinic antagonist-beta-adrenergic agonist dual pharmacology molecules as bronchodilators: a patent review. To Reference
Ref 5Curr Top Med Chem. 2005;5(16):1623-37.Inhibitors of dipeptidyl peptidase IV--recent advances and structural views. To Reference
Ref 6Bioorg Med Chem Lett. 2010 Mar 15;20(6):1895-9. Epub 2010 Feb 4.Heterocyclic acetamide and benzamide derivatives as potent and selective beta3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles. To Reference
Ref 7J Med Chem. 2003 Jan 2;46(1):105-12.Relationship between stereochemistry and the beta3-adrenoceptor agonistic activity of 4'-hydroxynorephedrine derivative as an agent for treatment of frequent urination and urinary incontinence. To Reference
Ref 8J Med Chem. 2001 Apr 26;44(9):1456-66.(4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists. To Reference
Ref 9Bioorg Med Chem Lett. 2008 Oct 15;18(20):5391-5. Epub 2008 Sep 14.Use of the X-ray structure of the beta2-adrenergic receptor for drug discovery. Part 2: Identification of active compounds. To Reference
Ref 10J Med Chem. 2009 Mar 26;52(6):1773-7.Synthesis and pharmacological characterization of beta2-adrenergic agonist enantiomers: zilpaterol. To Reference
Ref 11Bioorg Med Chem Lett. 2010 Jun 1;20(11):3399-404. Epub 2010 Apr 9.A vHTS approach for the identification of beta-adrenoceptor ligands. To Reference
Ref 12J Med Chem. 2007 Jun 14;50(12):2903-15. Epub 2007 May 17.Comparative molecular field analysis of the binding of the stereoisomers of fenoterol and fenoterol derivatives to the beta2 adrenergic receptor. To Reference
Ref 13J Med Chem. 1994 May 13;37(10):1518-25.The [(methyloxy)imino]methyl moiety as a bioisoster of aryl. A novel class of completely aliphatic beta-adrenergic receptor antagonists. To Reference
Ref 14Bioorg Med Chem. 2009 Dec 1;17(23):7987-92. Epub 2009 Oct 13.Structural basis of the selectivity of the beta(2)-adrenergic receptor for fluorinated catecholamines. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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