1. 一站式药筛
  2. 化合物库
  3. 靶向丝氨酸/苏氨酸的共价片段库
靶向丝氨酸/苏氨酸的共价片段库 - Serine/Threonine Focused Covalent Fragment Library

Cat. No.: HY-L914

含有羟基的侧链氨基酸(如丝氨酸和苏氨酸)在靶向共价酶抑制剂的研究中有着悠久的历史。最著名的共价药物,如阿司匹林,靶向环氧酶的非催化域丝氨酸(人COX1中的Ser529);β-内酰胺抗生素,靶向青霉素结合蛋白的催化域丝氨酸。除此之外,还有许多共价抑制剂是靶向各种蛋白酶或水解酶的催化域丝氨酸或者苏氨酸,这些羟基由于其周围的环境,如催化三联体的引入,比一般的羟基的亲核性更强。近期有许多共价抑制剂的例子使用酰基化化合物、磷酸酯和磷酸盐、硼酸盐、磺酰氟化物来靶向催化丝氨酸和苏氨酸。

我们基于最新的研究收集了上百种不同类型的共价抑制剂。经过谨慎选择,构建了一组含有110多种亲电基团的结构过滤器。通过对结构过滤器选择的亲电性片段进行分析,去除任何具有琐碎或不需要的结构特征的分子。最终获得 3,300 个具有靶向丝氨酸/苏氨酸共价修饰潜力的片段分子,用于基于片段的共价药物发现。

  • 96-well Plate with Peelable Foil Seal
  • 384-well Microplate with Peelable Foil Seal
  • 96-well Storage Tubes with Rack
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  • 产品详情

活性描述 & 特点

Biological Activity

•   A unique collection of 3,300 Fragments that show covalent binding with serine/threonine.

•   Careful selection of warheads: only those with experimentally validated reactivity are chosen, avoiding over-reactive warheads and any alternative reactive functionalities.

•   A useful tool for the fragment-based approach to drug discovery (FBDD).

•   All compounds are available off the shelf.

•   LCMS or NMR validated to ensure high purity and quality.

产品详情

Product Details

Formulation:

This fragment library containing 3,300 fragments with warheads targeting serine and threonine residues.

Layout:

96-well storage tube or 96-well plate: 1st and 12th column are left empty.
384-well plate: the first two columns and the last two columns are left empty.
Compounds with different concentrations or dissolved in different solvents will be put on separate plates. This way of layout may increase the number of plates because there could be three solvents and three concentrations.
If you have other requirements, please let us know.

Container:

96- or 384-well Plate with Peelable Foil Seal; 96-well Format Sample Storage Tube With Screw Cap and Optional 2D Barcode.

Storage:

-80°C

Shipping:

Blue ice or dry ice

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  • 96-well Plate with Peelable Foil Seal
  • 384-well Microplate with Peelable Foil Seal
  • 96-well Storage Tubes with Rack

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    产品名称:
    Serine/Threonine Focused Covalent Fragment Library
    目录号:
    HY-L914
    需求量: