E3 Ligand-Linkers Conjugate Kits
Ready-to-use sets to support your discoveries
We at Enamine are constantly working on synthesizing new molecules and elaborating new synthetic approaches to facilitate access to the most demanded chemistry and intermediates for the Drug Discovery Community. We carefully designed and synthesized a series of E3 binders with attached linkers of different lengths and natures to support Degrader Research and Development. Our primary focus has been the derivatization of Cereblon (CRBN) binders since they are most frequently used in constructing PROTAC molecules.
The Kits represented here include commonly used CRBN ligands functionalized at C4 and C5 positions to avoid interference with binding affinity. The attached ligands are of variable lengths from 2 to up to 18 heavy atoms in the chain or as a part of a more rigid construction.
Apart from the standard PEG and Carba-linkers, we offer intermediates with rigid/cyclic linkers that have been successfully utilized in the design of bifunctional molecules. Linkers terminal functional groups can be easily modified through the most straightforward reactions – amide coupling or click-chemistry.
Product catalog
Product name
CRBN Amine Kit-1
Amine-1-96
Description
Thalidomide-based ligands derivatized with most comprehensive and diverse linkers of variable length from 2 to 18 heavy atoms in a chain with terminal amine functional group
Product name
CRBN Amine Kit-2
Amine-2-35
Description
Uracyl-based Cereblon ligands with linear PEG- and Carba-linkers with terminal amine group able for modification
Product name
CRBN Azide Kit-1
Azide-1-28
Description
Thalidomide-based ligands with linear PEG- and Carba-linkers with terminal azide function for Click chemistry
Key features
- Easy access, ready for delivery in plates as 50 mM and 20 mM solutions in DMSO
- Variable in length from 2 up to 18 heavy atoms
- Well-balanced composition including PEG-, Carba- and Rigid-linkers
- Variation of linker conjugation point
