Enantiomeric pairs of covalent electrophilic fragments
960 compounds
Covalent chemical probes have become a valuable tool in drug discovery within the last few years. New technologies and development of fast mass spectrometric screening and imaging open a new horizon for proteome-wide screening and proteomics discoveries. The impressive number of successful applications brought aspiration to the discovery and synthesis of new covalent probes. Previously developed by Cravatt research group mapping of the ligandable proteome using fully functionalized enantiomeric probe pairs makes this field especially attractive for further investigations.
To support further research of the stereoselective interaction of proteins with chiral covalent small-molecules we designed and specially synthesized two sets of fragments with the most robust covalent warheads – acrylamides and chloroacetamides.
Typical Formats
Catalog No.
EPL-960-10-Y-100
Compounds
9603 plates
Amount
10 µL of 100 mM DMSO solutions
Plates and formats
384-well echo qualified LDV microplates, 1,2 and 23, 24 columns empty, 320 compounds per plate
Price
Catalog No.
EPL-960-25-Y-20
Compounds
9603 plates
Amount
25 µL of 20 mM DMSO solutions
Plates and formats
384-well microplates, Greiner bio-one, 1, 2 and 23, 24 columns empty, 320 compounds per plate
Price
Catalog No.
EPL-960-50-X-20
Compounds
96012 plates
Amount
50 µL of 20 mM DMSO solutions
Plates and formats
96-well plates, 2D-barcoded microtubes with first and last columns empty, 80 compounds per plate
Price
Catalog No.
EPL-960
Compounds
960
Amount
Custom
Plates and formats
Any custom format
Price
Download SD file
Library code: EPL-960
Version: 3 March 2024
960 compounds
at 100 mM in DMSO
640 compounds
at 100 mM in DMSO
320 compounds
at 100 mM in DMSO
More than 6000 chiral building blocks with enantiomeric excess (ee) purity of 90%+ were analyzed and triaged for further synthesis of covalent binder pairs. The resulting set of over 2000 of the most diverse novel covalent modifiers has been synthesized. The enantiomeric purity of the corresponding enantiomeric pairs was analyzed by chiral chromatography. Compounds that passed rigorous QC and selection based on the diversity and Ro3 criteria were assembled into the Covalent Enantiomeric Pairs Library.
Key features
- Stereoselective interaction of target with enantiomeric covalent binder provides evidence of ligand-protein interaction
- Information about “correct” stereochemistry of hit on early stage
- Most common and well-validated warheads
Enatiomeric Pairs Fragment Library is plated at 100 mM concentration and is available for fast supply in different formats. The Library consists of two sublibraries, which can be acquired separately.
