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Cysteine focused Covalent Fragments

Library of Cys-specific covalent electrophilic binders

3 200 compounds

Covalent chemical probes become an important tool in drug discovery within last few years. The impressive number of successful applications in protein drugability assessment, especially focusing on Cys residue, brought aspiration to discovery and synthesis of new covalent modifiers.

We used deep knowledge-based approach to design and synthesize our cysteine focused fragment library. Careful choice of covalent warheads based on their reactivity was performed by experienced chemists and reflected a small set of specific structural filters. Electrophilic fragments selected by structural filters were then analyzed to remove any molecules with trivial or unwanted structural features. The resulting set of molecules was refined with slightly expanded Ro3 criteria to yield 3 200 fragments able to form covalent bonds with cysteine residues.

Most popular Library Formats

Catalog ID
Compounds
Amount
Format
Price

Catalog ID

CYS-3200-10-Y-100

Compounds

3 200
10 plates

Amount

10 µL of 100 mM DMSO stock solutions

Plates and formats

384-well microplates, Echo qualified Labcyte, 320 compounds per plate

Catalog ID

CYS-3200-25-Y-20

Compounds

3 200
10 plates

Amount

25 µL of 20 mM DMSO stock solutions

Plates and formats

384-well plates, Greiner Cat. No. 781280, 1, 2 and 23, 24 columns empty, 320 compounds per plate

Catalog ID

CYS-3200-50-X-20

Compounds

3 200
40 plates

Amount

50 µL of 20 mM DMSO stock solutions

Plates and formats

96-well plates, 2D-barcoded Matrix microtubes capped with sepraseals

Hits derived from this library can be easily followed with analogues from stock or either synthesis of new compounds through REAL Database technology.

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Key features

  • Only well-validated covalent warheads, which can form easy to interpret adducts.
  • Contains fragments with described reactivity.
  • Attractive scaffolds, derived from the latest core building blocks.

The following warhead types were used for the library design and synthesis:

  • Acrylamides
  • Chloroacetamides & 2-chloropropionamides
  • Acrylonitriles
  • Disulfides

Examples of the molecules in Cysteine focused Library

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