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.
Typical Formats
Catalog No.
LYS-1600-0-Z-2
Compounds
1 600
2 plates
Amount
≤300 nL of 2 mM or 10 mM DMSO stock solutions
Plates and formats
1536-well echo plates, Labcyte Cat. No. LP-0400,
1280 compounds per plate,
1-4 and 44-48 columns empty
Price
This email address is being protected from spambots. You need JavaScript enabled to view it.
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
Price
This email address is being protected from spambots. You need JavaScript enabled to view it.
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, Greiner Cat. No. 650201,
80 compounds per plate,
1 and 12 columns emty
Price
This email address is being protected from spambots. You need JavaScript enabled to view it.
Catalog No.
LYS-1600
Compounds
1 600
Amount
Custom
Plates and formats
Any custom format
Price
This email address is being protected from spambots. You need JavaScript enabled to view it.
