1. Screening Libraries
  2. Covalent Screening Library

Covalent Screening Library

Cat. No.: HY-L036
Library Contents: XLSX 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 807 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.

MCE Covalent Screening Library can be supplied as pre-dissolved Solutions or Solid. For pre-dissolved solutions in this library, there are 802 compounds supplied in 10 mM solution and 5 compounds supplied in 2 mM solution.

For pre-dissolved solutions, 10 mM for compounds with the solubility not lower than 10 mM, and 2 mM for compounds with solubility between 2 mM and 10 mM.

  • 96-well Plate with Peelable Foil Seal
  • 96-well Storage Tubes with Rack
Size (Pre-dissolved Solution or Solid) Price Stock
30 μL/well Solution

10 mM and 2 mM
Pre-dissolved Solution

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50 μL/well Solution

10 mM and 2 mM
Pre-dissolved Solution

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100 μL/well Solution

10 mM and 2 mM
Pre-dissolved Solution

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2 × 100 μL/well Solution

10 mM and 2 mM
Pre-dissolved Solution

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Description
& Advantages

•   A unique collection of 807 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.

Product Details
Formulation:
A collection of 807 molecules supplied as pre-dissolved Solutions or Solid
Solution: 802 compounds supplied in 10 mM solution, 5 compounds supplied in 2 mM solution.
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
Documentation

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    Product Name:
    Covalent Screening Library
    Cat. No.:
    HY-L036
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    • 96-well Plate with Peelable Foil Seal
    • 96-well Storage Tubes with Rack