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Home Compound Library Sets Lysine-targeted Covalent Modifiers

Lysine-targeted Covalent Modifiers


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As described on the main page, Covalent Modifiers can offer Drug Discovery scientists the ability to increase the potency and/or selectivity of small molecule inhibitors, by attachment of reactive functional groups designed to covalently bind to specific sites in a target. These interactions are often irreversible and much stronger, leading to higher affinity. [1]
This description is dedicated to our Lysine Targeted Covalent Modifiers Library, a compound collection made specifically for potential covalent binding to the Lysine residues of protein targets.
Even though the most attention is paid to exploring Cysteine Targeted Covalent Modifiers, nucleophilic Lysine can be also targeted efficiently. The pKa of the Lysine amino group on the protein surface is around 10.4, at physiological pH, most of these groups are protonated and unavailable as nucleophiles. This brings a huge advantage to the design of Lysine targeted covalent inhibitors – the residues are protected from non-specific binding. [2]

Chemspace Lysine Targeted Covalent Modifiers Library contains 62K compounds with a covalent warhead, potent for Lysine Binding.
The compound collection is 100% modifiable and can be customized to your needs.
Reach us at info@chem-space.com if you have any questions.

Sources:
  1. Lonsdale, R., & Ward, R. A. (2018). Structure-based design of targeted covalent inhibitors. Chemical Society Reviews, 47(11), 3816–3830. doi: 10.1039/c7cs00220c
  2. Pettinger, J., Jones, K., & Cheeseman, M. D. (2017). Lysine-Targeting Covalent Inhibitors. Angewandte Chemie International Edition, 56(48), 15200–15209. doi: 10.1002/anie.201707630