2. One-stop Drug Screening
  3. Screening Libraries
  4. Lysine Focused Covalent Fragment Library
Lysine Focused Covalent Fragment Library

Cat. No.: HY-L915

Lysine is the second most common target residue used in the design of TCIs and related covalent ligands. Its appeal lies in its abundance in human proteins, which is approximately three times higher than that of cysteine (5.8% vs. 1.9%). This significantly increases the number of proteins suitable for covalent targeting, especially given that many human proteins lack ligandable cysteine residues. Moreover, it has been suggested that functional lysines have a lower probability of being replaced by mutation, as they often play a crucial role in catalysis by acting as bases or nucleophiles. Additionally, lysines are essential for maintaining the structural integrity of proteins and for regulating post-translational modifications (PTMs). Consequently, targeting lysine has garnered significant interest in recent years.

Through careful selection, we constructed a structural filter containing over 110 electrophilic groups. By analyzing the electrophilic fragments selected by the structural filter, we removed any molecules with trivial or undesirable structural features. Ultimately, we obtained 445 fragment molecules which can target lysine residue and can be used for fragment-based covalent drug discovery.

  • 96-well Plate with Peelable Foil Seal
  • 384-well Microplate with Peelable Foil Seal
  • 96-well Storage Tubes with Rack
- +
Contact Us for Customization

Compound Screening Libraries

Download
Related Products
Recommendation

Top Publications Citing Use of MedChemExpress (MCE) Products

View More

Publications Citing Use of MedChemExpress (MCE) Products

  • Biological Activity
  • Product Details

Description & Advantages

•   A unique collection of 445 fragments that show covalent binding with lysine.

•    Careful selection of warheads: only those with experimentally validated reactivity are chosen, avoiding over-reactive warheads and any alternative reactive functionalities.

•   A useful tool for the fragment-based approach to drug discovery (FBDD).

•   All compounds are available off the shelf.

•   LCMS or NMR validated to ensure high purity and quality.

Product Details

Formulation:

This fragment library containing 445 fragments with warheads targeting lysine residue.

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

Related Service
Recommendation
Compound Customization
  •  Specific Compounds
  •  Quantities
  •  Plate Map
  •  Concentration
  •  Form (Solid or Solution)
  •  YES
Contact Us for Customization

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Container *

    Remarks

    Inquiry Information

    Product Name:
    Lysine Focused Covalent Fragment Library
    Cat. No.:
    HY-L915
    Quantity:
    MCE Japan Authorized Agent:

    Request SDF File

    Please enter your email address. We will send your requested SDF file to you as soon as possible.

    • 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

    Request for SDF File

    Please fill out this form to request the SDF file. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Applicant Name *

    Email Address *

    		 

    Organization Name *

    Phone Number

    		     

    Remarks

    Request for SDF File

    We have received your request and will respond to you as soon as possible.