Target Validation Information
Target ID T52522
Target Name Beta-2 adrenergic receptor
Target Type
Successful
Drug Potency against Target Formoterol Drug Info EC50 = 2.4 nM
CGP-12177A Drug Info Ki = 0.1 nM [526033]
(R,S)-(-)-fenoterol Drug Info Ki = 3690 nM [528842]
Fenoterol Drug Info EC50 = 74.5 nM
GSK961081 Drug Info Ki < 10 nM [552942]
SDZ-201106 Drug Info Ki = 57.3 nM [529732]
GNF-PF-1694 Drug Info Ki = 0.145 nM [529732]
GSK642444 Drug Info Ki = 123 nM [552570]
2-fluoronorepinehprine Drug Info Ki = 15800 nM [530478]
(S,R)-(+)-fenoterol Drug Info Ki = 10300 nM [528842]
(R,R)-(-)-fenoterol Drug Info Ki = 350 nM [528842]
1-(2-isopropylphenoxy)-3-morpholinopropan-2-ol Drug Info Ki = 1.2 nM [530883]
1-(2-allylphenoxy)-3-morpholinopropan-2-ol Drug Info Ki = 7 nM [530883]
DICHLOROISOPROTERENOL Drug Info Ki = 140 nM [533801]
L-755507 Drug Info Ki = 160 nM [526033]
L-796568 Drug Info IC50 = 2300 nM [530748]
References
Ref 526033J Med Chem. 2001 Apr 26;44(9):1456-66.(4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists.
Ref 528842J 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.
Ref 552942Muscarinic antagonist-beta-adrenergic agonist dual pharmacology molecules as bronchodilators: a patent review. Expert Opin Ther Pat. 2009 Jan;19(1):1-12. doi: 10.1517/13543770802630331.
Ref 529732Bioorg 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.
Ref 529732Bioorg 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.
Ref 552570Inhibitors of dipeptidyl peptidase IV--recent advances and structural views. Curr Top Med Chem. 2005;5(16):1623-37.
Ref 530478Bioorg 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.
Ref 528842J 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.
Ref 528842J 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.
Ref 530883Bioorg Med Chem Lett. 2010 Jun 1;20(11):3399-404. Epub 2010 Apr 9.A vHTS approach for the identification of beta-adrenoceptor ligands.
Ref 530883Bioorg Med Chem Lett. 2010 Jun 1;20(11):3399-404. Epub 2010 Apr 9.A vHTS approach for the identification of beta-adrenoceptor ligands.
Ref 533801J 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.
Ref 526033J Med Chem. 2001 Apr 26;44(9):1456-66.(4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists.
Ref 530748Bioorg 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.

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