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Cysteine focused Covalent Fragments

Library of Cys-specific electrophilic fragments

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 bond with cysteine residue.

Cysteine focused fragments can be rapidly delivered in a range of convenient pre-plated formats. The library are also available for plate cherry-picking and can be supplied in customized formats.

Most popular Library Formats

Option
Catalog ID
Compounds
Plates
Amount
Format

Option

1

Catalog ID

CYS-3200-Y-10

Compounds

3 200

Plates

10

Amount

10 µL of 100 mM DMSO stock solutions

Plates and formats

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

Option

2

Catalog ID

CYS-3200-X-25

Compounds

3 200

Plates

40

Amount

25 µL of 20 mM DMSO stock solutions

Plates and formats

96-well plates, Greiner No. 6501xx, 80 cmpds per plate

Option

3

Catalog ID

CYS-3200-X-50

Compounds

3 200

Plates

40

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.

Selected covalent warheads

  • Acrylamides
  • Chloroacetamides
  • Vinyl sulfones
  • Thiols
  • Alkyl chlorides

Examples of the molecules

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