首页> 外国专利> A method for finding of ligands which bind to a drug target, by means of nmr - displacement experiments.

A method for finding of ligands which bind to a drug target, by means of nmr - displacement experiments.

机译:一种通过核磁共振-置换实验发现与药物靶标结合的配体的方法。

摘要

The present invention relates to a method for identifying and screening of active substances which bind to a drug target, which, on the basis of the process of the heteronuclear nmr - spectroscopy is based. It is more particularly based on the principle of the competitive displacement, whereby the displacement of isotope-labeled relatively weakly be bound by the sought scout - ligands, ligands a higher affinity is observed. In a further embodiment, the method according to the invention for admetox - optimization of known active agents. In this case it is important, from known active compounds or derivatives thereof to identify those representatives which, as far as possible, poorly to bind a test enzyme.
机译:本发明涉及一种鉴定和筛选与药物靶标结合的活性物质的方法,该方法基于异核核磁共振光谱法。更具体地,基于竞争性置换的原理,由此同位素标记的置换相对较弱地被寻找的侦察配体所约束,观察到配体具有更高的亲和力。在另一个实施方案中,根据本发明的用于阿达莫斯的方法-已知活性剂的优化。在这种情况下,重要的是从已知的活性化合物或其衍生物中识别出那些可能与测试酶结合不良的代表。

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