Targeted covalent inhibitors (TCIs), also known as targeted covalent drugs, are rationally designed irreversible inhibitors that bind covalently to their target proteins. Covalent binders are very attractive molecules for drug discovery and HTS as they possess many desirable features, such as:
- increased biochemical efficiency of target disruption
- lower sensitivity toward pharmacokinetic parameters
- increased duration of action that outlasts pharmacokinetics of the compound.
However, several safety concerns must be mitigated in the covalent drug discovery, including the lack of target specificity and the potential immunogenicity of the protein-inhibitor adducts.
Life Chemicals presents a carefully designed proprietary collection of potential covalent modifiers. Structurally diverse screening compounds were selected from the Life Chemicals HTS Compound Collection by the presence of specific bond-forming functional groups (covalent warheads) in their structure. Separate focused sets targeting each of the indicated amino acid residues (Cysteine, Serine, Tyrosine, Lysine, etc.) are offered (Fig. 2).
The full list of available compound sets for covalent screening is shown at the top of the page. Taking into account a growing interest and widespread use of fragment-based drug discovery (FBDD), Life Chemicals also designed an exclusive Covalent Fragment Library and Specific Covalent Inhibitor Fragment Library.
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Download SD files with compound structures directly in our Downloads section
You can cherry-pick compounds or focus on a specific class of covalent-binding molecules. A custom selection of compounds by any parameter can be provided on requests.
Figure 1. Approved covalent inhibitors in history: Timeline. Picture credit: A. Aljoundi et al., 2020 (DOI: 10.1007/s10930-020-09884-2)
Figure 2. Small-molecule screening compound distribution between different subsets of potential covalent modifiers.