2. 一站式药筛
  3. 化合物库
  4. 类药共价化合物库
类药共价化合物库 - Lead-like Covalent Screening Library

Cat. No.: HY-L908

小分子共价抑制剂是一类通过共价键与靶点结合来发挥其生物学功能的抑制剂。与非共价抑制剂相比，共价抑制剂在生物活性方面具有明显优势，共价弹头靶向特定靶蛋白的稀有残基，可以用于开发高选择性抑制剂。

近年来，随着一系列共价抑制剂的成功问世，特别是针对那些传统上被认为难以成药的受体，如 EGFR、BTK、KRAS 的抑制剂，以及共价抑制剂在解决耐药性问题方面表现出显著优势，共价抑制剂已然成为小分子药物研发的热点。但是此类抑制剂一旦出现脱靶，也将带来更强的毒副作用。因此，通过合理的筛选设计和结构修饰发现共价抑制剂药物也逐渐成为一个药物研发的焦点。

MCE 类药共价化合物库含有 1,049 个共价分子，这些分子包含共价反应常用的弹头，如丙烯酰胺、活化末端乙炔、酰基氧甲基酮、硼酸等，可以与半胱氨酸、赖氨酸、丝氨酸和组氨酸等发生共价反应，是筛选共价化合物的有利工具。

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

Biological Activity

•   A unique collection of 1,049 compounds that show covalent binding with target proteins for high throughput screening (HTS) and high content screening (HCS).

•   Careful choice of warheads: only experimentally confirmed reactivity, no over-reactive warheads, no alternative reactive functionalities.

•   Chemical probes that show enhanced selectivity, potency and utility for biological studies.

•   Compatible with “Lipinski’s Rule of Five”, with multiple characteristics such as calculated good solubility (-3.2 < logP < 5), oral bioavailability (RotB <= 10), drug transportability (PSA < 120), MW between 300 to 500, number of Hydrogen Bond Donor (HBD)≤5, number of Hydrogen Bond Acceptor (HBA)≤10.

•   All compounds are available off the shelf.

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

产品详情

Product Details

•   A unique collection of 1,049 compounds that show covalent binding with target proteins for high throughput screening (HTS) and high content screening (HCS).

•   Careful choice of warheads: only experimentally confirmed reactivity, no over-reactive warheads, no alternative reactive functionalities.

•   Chemical probes that show enhanced selectivity, potency and utility for biological studies.

•   Compatible with “Lipinski’s Rule of Five”, with multiple characteristics such as calculated good solubility (-3.2 < logP < 5), oral bioavailability (RotB <= 10), drug transportability (PSA < 120), MW between 300 to 500, number of Hydrogen Bond Donor (HBD)≤5, number of Hydrogen Bond Acceptor (HBA)≤10.

•   All compounds are available off the shelf.

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

产品资料

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  •  化合物数量
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  •  形式（固体或溶液）
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联系专家定制
  • 96-well Plate with Peelable Foil Seal
  • 384-well Microplate with Peelable Foil Seal
  • 96-well Storage Tubes with Rack
  • 96-well Plate with Peelable Foil Seal
  • 384-well Microplate with Peelable Foil Seal
  • 96-well Storage Tubes with Rack

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    Lead-like Covalent Screening Library
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