12500 compounds in stock and over 13.4 million in REAL
1360 compounds pre-plated Covalent Fragments Chloroacetamides Library
1200 compounds pre-plated Covalent Screening Chloroacetamides Library
320 compounds pre-plated Covalent Enantiomeric Pairs Fragments Chloroacetamides Library
Chloroacetamides are a well-known class of electrophilic warheads widely used in the design of covalent inhibitors, particularly for their ability to selectively bind to cysteine residues. Although chloroacetamides are often considered overly reactive, their main advantage over commonly used warheads such as acrylamides and vinyl sulfones, lies in their ability to form irreversible covalent bonds with target residues, enabling unambiguous detection of covalent binding events.
Several compounds with сhloroacetamide warheads are under active investigation and demonstrate encouraging therapeutic potential: RHA-059, UPR1376, and DK2403 (highly potent and selective covalent MAP2K7 inhibitor, targeting Cys218 in the kinase active site).
Enamine has almost 13k compounds in stock (90%+ pure by LCMS and/or NMR analysis), which can be delivered as dry powders or in any customized plated formats. Alternatively, you can acquire new compounds from our pool of more than 13.4 million REAL Сhloroacetamides. Synthesis takes only 3-4 weeks yielding over 80% of the selected compounds.
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15 865 compounds for cherry-picking
Plated libraries in stock:
Examples of the chloroacetamides from stock
Chlorofluoroacetamides and 2-Chloropropionamides
3200 compounds in stock and over 12.4 million in REAL
320 compounds pre-plated Covalent Fragments Chlorofluoroacetamides Library
320 compounds pre-plated Covalent Fragments Chloropropionamides Library
560 compounds pre-plated Covalent Screening Chloropropionamides Library
Beyond chloroacetamides, chlorofluoroacetamides and chloropropionamides introduce unique reactivity profiles and molecular features, enhancing the versatility in warhead selection.
Сhlorofluoroacetamides exhibit reversible binding behavior, which provides an advantage in certain cases. For example, YH-6 is an aza-peptide inhibitor of SARS-CoV-2 3CLpro wich bonding Cys145.
2-Chloropropionamides are a less reactive class of electrophilic warheads compared to chloroacetamides, offering improved selectivity and tunability for covalent modification of target proteins. For example, S-CW3554 is selectively targets protein disulfide isomerase (PDIA1), demonstrating cytotoxicity in multiple myeloma cells.
Examples of the chlorofluoroacetamides and chloropropionamides from stock
Enamine has 1.5k chlorofluoroacetamides and 1.7k chloropropionamides in stock (90%+ pure by LCMS and/or NMR analysis), which can be delivered as dry powders or in any customized plated formats.
