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Lysine focused Covalent Fragments

A unique set of 1 600 Lys specific binders

1 600 compounds

Until recently, covalent inhibitors targeting lysine side chain attracted less attention as compared to those modifying cysteine or serine residues. Meanwhile, lysine residue is found both at the surface and in active sites of many enzymes (e. g.some kinases, viral polymerases and integrases, aldolases, DOPA decarboxylase, P-glycoprotein), as well as in the “hot spots” of protein-protein interactions. To address the increased interest to the lysine covalent modifiers, we have designed our Lysine focused covalent fragment library.

The following “warheads” were used for substructure searches of the compounds to be included into the library:

Common electrophiles

  • Vinyl sulfones and sulfonamides
  • Acrylamides
  • β-(Dimethylamino)crotylamides and -enones
  • Propargylamides
  • Sulfonyl fluorides
  • Arenesulfonates
  • Haloacetamides
  • Cyanamides
  • Azine-derived nitriles
  • Aziridines
  • N-nitriles
  • Activated 2-Halogen nitrogen heterocycles
  • Aldehydes

Specific electrophiles

  • Succinimides
  • Salicylic aldehydes
  • o-Carbonylboronic derivatives
  • Maleimides

Further selection process included filtering by molecular parameters according to the extended Ro3 indicated for General covalent fragment library, removal of trivial chemotypes and visual inspection to avoid over reactive entities.

Most popular library formats

Catalog No.
Compounds
Amount
Format*
Price

Catalog No.

LYS-1600-0-Z-2

Compounds

1 600
2 plates

Amount

≤300 nL of 2 mM or 10 mM DMSO stock solutions

Format

1536-well echo plates, Labcyte Cat. No. LP-0400, 1280 compounds per plate, 1-4 and 44-48 columns empty

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Catalog No.

LYS-1600-10-Y-10

Compounds

1 600
5 plates

Amount

10 µL of 10 mM DMSO stock solutions

Format

384-well plates Greiner Cat. No. 781280, 320 compounds per plate, 1, 2 and 23, 24 columns empty

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Catalog No.

LYS-1600-50-X-10

Compounds

1 600
20 plates

Amount

50 µL of 10 mM DMSO stock solutions

Format

96-well plates, Grainer Cat. No. 650201, 80 compounds per plate, 1 and 12 columns emty

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*Please request for any other options through our contact form. We will be happy to deliver our library in any convenient for your project formats.

Examples of the molecules

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