725 compounds in stock and over 920K in REAL
240 compounds pre-plated Covalent Screening N-nitriles Library
Cyanamides, also known as N-nitriles, have recently emerged as promising electrophilic warheads in covalent drug discovery, offering a balance between reactivity and selectivity. Their moderate electrophilicity makes them attractive alternatives to more reactive groups like acrylamides or vinyl sulfones. Cyanamides have also been explored for their ability to engage in reversible binding, forming isothioureas, which can be beneficial in certain applications.
Cyanamide-based inhibitors have been applied in targeting kinases, such as BTK, and even viral proteases. Recent studies have demonstrated that cyanamides can be engineered to attain high selectivity. For instance, N-cyanopiperazines were shown to covalently and selectively inhibit the deubiquitinating enzyme UCHL1, avoiding off-target effects on closely related enzymes like PARK7.
Cyanamide reversible binding to Cys-residues
We offer over 700 cyanamide compounds as dry powders and have designed a pre-plated library of 240 compounds. Covalent Screening N-nitriles Library is available in a pre-plated format at 10 mM concentration in DMSO. It can be purchased either as a standalone set or as a sublibrary of Covalent Screening Library.
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725 compounds for cherry-picking
920K compounds
Plated libraries in stock:
Examples of Cyanamides
Synthetic approaches
Two complementary synthetic strategies have enabled the development of a diverse range of cyanamide compounds. On the one hand, alkylation or acylation of building blocks with pre-installed cyanamide warhead has enabled the generation of many diverse compounds. On the other hand, direct cyanation of Enamine`s vast amine collection using a novel and convenient reagent (CBX) has provided access to structurally diverse cyanamides. Validation of various synthetic approaches, combined with access to our extensive building block stock allowed us to create 920,000-compound REAL Cyanamides array. Compounds from this array can be synthesis within 3-4 weeks, with 80% success rate.
