Fragment Based Lead Generation for Novel Kinase Inhibitors; Frontloading Binding-Kinetic Properties

Gerhard MULLER; Frank LEEMHUIS; Doris HAFENBRADL

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Fragment Based Lead Generation for Novel Kinase Inhibitors; Frontloading Binding-Kinetic Properties

机译：新型激酶抑制剂的基于片段的线索生成;前载结合动力学特性

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Fragment-Based Lead Discovery has matured into an established and feasible alternative to e.g. high-throughput screening of traditional corporate libraries within the pharmaceutical industry, thus focusing the interest of medicinal chemists onto smaller fragment hits with high ligand efficiency. Fragment hits are most effectively evolved to traditional lead structures if high-resolution structure data become available within the course of the corresponding optimization campaigns.

机译：基于片段的潜在顾客发现已发展成为一种成熟且可行的替代方案，例如制药行业中传统公司库的高通量筛选，因此将药物化学家的兴趣集中在具有高配体效率的较小片段上。如果在相应的优化活动过程中可以获得高分辨率的结构数据，则片段命中将最有效地演变为传统的线索结构。

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《Chimie Nouvelle》 |2009年第102期|共1页
作者
Gerhard MULLER; Frank LEEMHUIS; Doris HAFENBRADL;
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中图分类化学;
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1. Fragment Based Lead Generation for Novel Kinase Inhibitors; Frontloading Binding-Kinetic Properties [J] . Gerhard MULLER, Frank LEEMHUIS, Doris HAFENBRADL Chimie Nouvelle . 2009,第102期

机译：新型激酶抑制剂的基于片段的线索生成;前载结合动力学特性
2. New Lead Generation Strategies for Protein Kinase Inhibitors - Fragment Based Screening Approaches [J] . Adrian Gill Mini-Reviews in Medicinal Chemistry . 2004,第3期

机译：蛋白质激酶抑制剂的新的铅生成策略-基于片段的筛选方法。
3. New lead generation strategies for protein kinase inhibitors - fragment based screening approaches. [J] . Gill A Mini reviews in medicinal chemistry . 2004,第3期

机译：蛋白激酶抑制剂的新线索生成策略-基于片段的筛选方法。
4. Utilization of Flavonoid Compounds as HER2 Tyrosine Kinase Inhibitor in Breast Cancer Using Fragment-Based Drug Design [C] . Vincent Jonathan Fleming, Mutiara Saragih, Usman Sumo Friend Tambunan International Conference on Science and Technology . 2020

机译：使用碎片的药物设计在乳腺癌中用黄酮类化合物作为HER2酪氨酸激酶抑制剂
5. The Use of Fragment-Based Lead Discovery Towards the Design and Development of Metalloenzyme Inhibitors. [D] . Sardo, Jessica L. 2013

机译：使用基于片段的线索发现进行金属酶抑制剂的设计和开发。
6. Fragment-Based Lead Generation of 5-Phenyl-1H-pyrazole-3-carboxamide Derivatives as Leads for Potent Factor Xia Inhibitors [O] . Qunchao Wei, Zhichao Zheng, Shijun Zhang, 2018

机译：5-苯基-1H-吡唑-3-羧酰胺衍生物基于片段的铅生成作为潜在的Xia抑制剂的铅
7. Creating novel activated factor XI inhibitors through fragment based lead generation and structure aided drug design. [O] . Ola Fjellström, Sibel Akkaya, Hans-Georg Beisel, 2015

机译：通过基于片段的铅生成和结构辅助药物设计创建新的活化因子XI抑制剂。

Fragment Based Lead Generation for Novel Kinase Inhibitors; Frontloading Binding-Kinetic Properties

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