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- 2025年07月06日
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Covalent Screening Library
MCE 国际站：Covalent Screening Library
Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery.MCE covalent inhibitor library contains 1643 small molecules including identified covalent inhibitors and other bioactive molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, Sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc.
Description & Advantages:
• A unique collection of 1643 compounds that show irreversible covalent binding with target proteins for high throughput screening (HTS) and high content screening (HCS).
• Chemical probes that show enhanced selectivity, potency and utility for biological studies.
• A useful tool for drug discovery with irreversible inhibition.
• Bioactivity and safety confirmed by preclinical research and clinical trials. Some have been approved by FDA.
• Structurally diverse, medicinally active, and cell permeable.
• Detailed compound information with structure, IC50, and brief introduction.
• Validated NMR and HPLC to ensure high purity and quality.
• All compounds are in stock and continuously updated.
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文献和实验?streptavidin conjugates are synthesized by covalent coupling of thiol?modified DNA oligonucleotides and streptavidin (STV). The resulting conjugates have binding capacities for four equivalents of biotin and a complementary nucleic acid sequence. The conjugates
Selecting, Acquiring, and Using Small Molecule Libraries for High‐Throughput Screening
in the choice of library composition. This overview attempts to offer advice to all organizations engaged in small molecule screening based upon current best practices and theoretical considerations in library selection and acquisition. Curr. Protoc. Chem. Biol
悬浮点阵(MASA)[3]。二、液相芯片的制备和检测1、彩色微球的制作和探针分子的固定：液相芯片的核心技术是把微小的乳胶颗粒亦称微球(beadormicrosphere)分别染成不同的荧光色，然后再把针对不同检测物的寡核苷酸或蛋白质探针以共价方式吸附到不同颜色的微球上。乳胶颗粒是由聚苯乙烯制成的大小均一的圆形微球(直径约5.6um)，在其制作过程中按照严格的精确比例掺入了两种不同的红色分类荧光染料，每种染料各有10种区分，因而根据其搭配比例不同可以把球型基质分为100种，使得每个微球都获得了其特定
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