Binding kinetics of ZM241385 derivatives at the human adenosine A2A receptor

…, M Hazeu, T Mocking, J Brussee, AP IJzerman…

文献索引：Guo, Dong; Xia, Lizi; Van Veldhoven, Jacobus P. D.; Hazeu, Marc; Mocking, Tamara; Brussee, Johannes; Ijzerman, Adriaan P.; Heitman, Laura H. ChemMedChem, 2014 , vol. 9, # 4 p. 752 - 761

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被引用次数: 17

摘要

Abstract Classical drug design and development rely mostly on affinity-or potency-driven structure–activity relationships (SAR). Thus far, a given compound's binding kinetics have been largely ignored, the importance of which is now being increasingly recognized. In the present study, we performed an extensive structure–kinetics relationship (SKR) study in addition to a traditional SAR analysis at the adenosine A 2A receptor (A 2A R). The ...