1. Screening Libraries
  2. Covalent Screening Library Plus

Covalent Screening Library Plus

Cat. No.: HY-L036P
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 3500 small molecules including identified covalent inhibitors and other 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 inhibitor Library plus, with more powerful screening capability, further complement Covalent inhibitor Library (HY-L036) by adding some fragment compounds with covalent warheads.

MCE Covalent Screening Library Plus can be supplied as pre-dissolved Solutions or Solid. For pre-dissolved solutions in this library, there are 3467 compounds supplied in 10 mM solution and 6 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
Size (Pre-dissolved Solution or Solid) Price Stock
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 3500 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.

•   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 3500 molecules supplied as pre-dissolved Solutions or Solid
Solution: 3467 compounds supplied in 10 mM solution, 6 compounds supplied in 2 mM solution.
Container:
96- or 384-well Plate with Peelable Foil Seal
Storage:
-80°C
Shipping:
Blue ice
Documentation

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    Covalent Screening Library Plus
    Cat. No.:
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    • 96-well Plate with Peelable Foil Seal
    • 384-well Microplate with Peelable Foil Seal