Target Validation Information
TTD ID	T52522
Target Name	Adrenergic receptor beta-2 (ADRB2)
Type of Target	Successful
Drug Potency against Target	Fenoterol	Drug Info	EC50 = 74.5 nM
	Formoterol	Drug Info	EC50 = 2.4 nM
	GSK642444	Drug Info	Ki = 123 nM	[8]
	GSK961081	Drug Info	Ki < 10 nM	[9]
	(R,R)-(-)-fenoterol	Drug Info	Ki = 350 nM	[2]
	(R,S)-(-)-fenoterol	Drug Info	Ki = 3690 nM	[2]
	(S,R)-(+)-fenoterol	Drug Info	Ki = 10300 nM	[2]
	1-(2-allylphenoxy)-3-morpholinopropan-2-ol	Drug Info	Ki = 7 nM	[6]
	1-(2-isopropylphenoxy)-3-morpholinopropan-2-ol	Drug Info	Ki = 1.2 nM	[6]
	2-fluoronorepinehprine	Drug Info	Ki = 15800 nM	[4]
	Dichloroisoproterenol	Drug Info	Ki = 140 nM	[7]
	DPI-201-106	Drug Info	Ki = 57.3 nM	[3]
	GNF-PF-1694	Drug Info	Ki = 0.145 nM	[3]
	L-755507	Drug Info	Ki = 160 nM	[1]
	L-796568	Drug Info	IC50 = 2300 nM	[5]
	[3H]CGP12177	Drug Info	Ki = 0.1 nM	[1]
References
REF 1	(4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists. J Med Chem. 2001 Apr 26;44(9):1456-66.
REF 2	Comparative molecular field analysis of the binding of the stereoisomers of fenoterol and fenoterol derivatives to the beta2 adrenergic receptor. J Med Chem. 2007 Jun 14;50(12):2903-15.
REF 3	Use of the X-ray structure of the beta2-adrenergic receptor for drug discovery. Part 2: Identification of active compounds. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5391-5.
REF 4	Structural basis of the selectivity of the beta(2)-adrenergic receptor for fluorinated catecholamines. Bioorg Med Chem. 2009 Dec 1;17(23):7987-92.
REF 5	Heterocyclic acetamide and benzamide derivatives as potent and selective beta3-adrenergic receptor agonists with improved rodent pharmacokinetic pr... Bioorg Med Chem Lett. 2010 Mar 15;20(6):1895-9.
REF 6	A vHTS approach for the identification of beta-adrenoceptor ligands. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3399-404.
REF 7	The [(methyloxy)imino]methyl moiety as a bioisoster of aryl. A novel class of completely aliphatic beta-adrenergic receptor antagonists. J Med Chem. 1994 May 13;37(10):1518-25.
REF 8	Inhibitors of dipeptidyl peptidase IV--recent advances and structural views. Curr Top Med Chem. 2005;5(16):1623-37.
REF 9	Muscarinic antagonist-beta-adrenergic agonist dual pharmacology molecules as bronchodilators: a patent review. Expert Opin Ther Pat. 2009 Jan;19(1):1-12.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.