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An Intuitive Look at the Relationship of K_i and IC_50: A More General Use for the Dixon Plot

机译:直观了解K_i和IC_50的关系:狄克逊图的更一般用法

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The design and synthesis of small-molecule enzyme in-hibitors is of great interest in current research. Finding a potent inhibitor of an enzyme linked to a disease may lead to a multi-billion-dollar pharmaceutical product. To find such in-hibitors, it is often necessary to quantitatively compare the inhibitory ability of a large number of target compounds. A recent review of protease inhibitors gives a perspective on the wide range and sheer number of reversible inhibitors of one class of enzymes (1). Without a standard measurement of inhibition, comparing the inhibitor potencies of these molecules would be impossible.
机译:小分子酶抑制剂的设计与合成在当前研究中引起了极大的兴趣。寻找一种有效的与疾病有关的酶抑制剂可能会导致数十亿美元的医药产品。为了找到这样的抑制剂,通常需要定量比较大量目标化合物的抑制能力。蛋白酶抑制剂的最新综述提供了对一类酶的可逆抑制剂的广泛范围和绝对数量的一种观点(1)。如果没有标准的抑制方法,则无法比较这些分子的抑制剂效能。

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