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. | ||||
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