Covalent Screening Library

Cat. No. : CS-L036 (1641 compounds)
Library Contents: PDF | SDF

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 1641 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.

Size (Pre-dissolved DMSO or Solid) Stock Price
30 μL/well (10 mM solution) In-stock Get quote
50 μL/well (10 mM solution) In-stock Get quote
100 μL/well (10 mM solution) In-stock Get quote
250 μL/well (10 mM solution) In-stock Get quote
Products are for research use only. Not for human use. We do not sell to patients.

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  • Data Sheet

  • Description & Advantages

  • Composition

  • Contents

Formulation:A collection of 1641 molecules supplied as pre-dissolved Solutions or Solid
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

•   A unique collection of 1641 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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