Recommanded Product: 1-(Bromomethyl)-4-ethylbenzene. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 1-(Bromomethyl)-4-ethylbenzene, is researched, Molecular C9H11Br, CAS is 57825-30-6, about Structure-Affinity Relationships and Structure-Kinetics Relationships of Pyrido[2,1-f]purine-2,4-dione Derivatives as Human Adenosine A3 Receptor Antagonists. Author is Xia, Lizi; Burger, Wessel A. C.; van Veldhoven, Jacobus P. D.; Kuiper, Boaz J.; van Duijl, Tirsa T.; Lenselink, Eelke B.; Paasman, Ellen; Heitman, Laura H.; IJzerman, Adriaan P..
We expanded on a series of pyrido[2,1-f]purine-2,4-dione derivatives as human adenosine A3 receptor (hA3R) antagonists to determine their kinetic profiles and affinities. Many compounds showed high affinities and a diverse range of kinetic profiles. We found hA3R antagonists with very short residence time (RT) at the receptor (2.2 min for II 5) and much longer RTs (e.g., 376 min for I or 391 min for 31). Two representative antagonists (I) and (II) were tested in [35S]GTPγS binding assays, and their RTs appeared correlated to their (in)surmountable antagonism. From a kon-koff-KD kinetic map, we divided the antagonists into three subgroups, providing a possible direction for the further development of hA3R antagonists. Addnl., we performed a computational modeling study that sheds light on the crucial receptor interactions, dictating the compounds’ binding kinetics. Knowledge of target binding kinetics appears useful for developing and triaging new hA3R antagonists in the early phase of drug discovery.
Here is a brief introduction to this compound(57825-30-6)Recommanded Product: 1-(Bromomethyl)-4-ethylbenzene, if you want to know about other compounds related to this compound(57825-30-6), you can read my other articles.
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