Designed for easy and rapid follow-up synthesis
860 compounds
Fragment screening is an efficient way of establishing initial points for drug discovery. However, seemingly simple small molecules don’t necessarily mean that their chemistry is not complex. Quite the contrary, fragment hits may be challenging to follow up. Synthesis routes can be long and rigid not allowing making small specific changes while growing, linking or merging the hit.
It was shown by Cox et al., in Chem. Sci. 2016 that the compounds synthesised from a robust and general synthetic reaction can be prioritized for building fragment library. Identification of so-called “poised” bonds in a fragment means that a library of analogues can be rapidly elaborated using standard parallel chemistry. First poised library was developed at Diamond Light Source, UK (Diamond) and Structural Genomic Consortium, UK (SGC) in the frame of one of the iNEXT Joint Research Activities. Enamine collaborated with the joint research alliance in design of a next generation of DSI-poised Library. DSI stands for Diamond, SGC and iNEXT. On January 10 2018 Diamond and SGC announced that Enamine would become a key supplier of poised fragment and analogue libraries to the XChem Facility in Oxford, UK.
Typical Formats
Catalog No.
DSI-860-10-Y-100
Compounds
8603 plates
Amount
10 µL of 100 mM DMSO solutions
Plates and formats
384-well plates Greiner Cat. No 781280, first two and last two columns empty, 320 compounds per plate
Price
Catalog No.
DSI-860-25-Y-100
Compounds
8603 plates
Amount
25 µL of 100 mM solutions in DMSO
Plates and formats
384-well plates, 1,2 & 23,24 columns empty, 320 compounds per plate
Price
Catalog No.
DSI-860-3-Z-500
Compounds
8601 plate
Amount
3 µL of 500 mM solutions in DMSO-D6
Plates and formats
1536-well microplates, Cat. No LP-0400, 1-4 and 44-48 columns empty, 1280 compounds per plate
Price
Catalog No.
DSI-860-100-X-10
Compounds
86011 plates
Amount
100 µL of 10 mM DMSO solutions
Plates and formats
96-well plates, Greiner Cat. No 650201, round (U) bottom, 1 & 12 columns empty, 80 compounds per plate
Price
Catalog No.
DSI-860
Compounds
860
Amount
Custom
Plates and formats
Any custom format
Price
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Library design
The original library developed by Diamond and SGC has been enhanced with a careful selection of fragments synthesized at Enamine via parallel chemistry from its building blocks, which are widely commercially available. Every researcher will be available to quickly synthesize analogues of the poised fragments because such building blocks are not complex and are exemplified with many analogues on the market. The reactions are frequently used in parallel chemistry: amide coupling, reductive amination, Suzuki-Miyaura coupling, aromatic nucleophilic substitution, synthesis of sulfonamides, ureas, etc.
Examples of the molecules
Molecular properties
