2. 一站式药筛
  3. 化合物库
  4. 类药多样性化合物库系列
  5. 按潜在通路靶点分类
  6. 靶向GPCR蛋白类药多样库
靶向GPCR蛋白类药多样库 - GPCR Targeted Diversity Library

Cat. No.: HY-L928

G蛋白偶联受体（GPCR）是人类最大的膜蛋白家族，也是药物发现领域最重要的靶点之一，约35%的已上市药物直接作用于GPCR，因此GPCR蛋白是药物研发中一类非常重要的靶点。

GPCR蛋白的正构位点是GPCR与内源性配体（如神经递质、激素）直接结合的位置，该位点在信号传导中起核心作用，结合在该位点的小分子通常需要含有可质子化的氨基，能够与该结合口袋的酸性残基形成盐桥或氢键等作用。与之对应的变构位点不直接启动信号传导，而是通过改变正构位点的结构或稳定构象来调节GPCR受体的信号强度，结合在变构位点的小分子通常含有多个芳香环来占据疏水口袋以达到功能。

MCE收集整理了3000多个已报道的靶向GPCR蛋白的活性小分子，涉及A类，B类和C类GPCR蛋白，对活性小分子进行AI表征，提取2D结构和3D构象特征，再对类药多样库进行基于相似性的筛选，寻找与已报道活性分子在2D和3D上高度相似的分子，筛选阈值大于0.7。进一步对脂水分布系数（cLogP）进行筛选，以获得亲脂性较高的分子，以利于小分子和GPCR蛋白的结合，该类药多样库可广泛应用于靶向GPCR蛋白的发现。

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

活性描述 & 特点

Biological Activity

•    A unique collection of 7,000 compounds can be used for efficient discovery of compounds targeting GPCR proteins.

•    It is obtained by AI screening based on 2D/3D similarity and can be used for efficient discovery of novel molecule targeting GPCR protein.

•    All compounds are available off the shelf.

•    All compounds are validated by LC-MS or NMR to ensure high purity and quality.

产品详情

Product Details

Formulation:

A compound library can be used for efficient discovery of novel molecule targeting GPCR protein.

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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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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