Designed for easy and efficient exploration of novel protein targets
800 compounds
Fully functionalized probes are designed to speed up and simplify the early stages of drug development. The introduction of the diazirine photo-crosslinking moiety along with the presence of a functional acetylene group allows the screening of compounds directly in cells. Initially described in the Cell paper by Ben Cravatt this approach has been adopted by other research groups to a number of successful projects, including reported by GSK researchers ‘direct-to-biology’ high-throughput chemistry screening platform.
Enamine currently has over 6 000 fully functionalized compounds in stock and more than 1 million molecules in REAL Database.
The most diverse compounds have been selected and sorted into a small library, which has been pre-plated for the most convenient and fast delivery to our clients.
Typical Formats
Catalog No.
FFP-800-10-Y-20
Compounds
800
3 plates
Amount
10 µL of 20 mM DMSO solutions
Plates and formats
384 well, Greiner Bio-One microplates 781280, first and last two columns empty, 320 compounds per plate
Price
Catalog No.
FFP-800-50-Y-10
Compounds
800
3 plates
Amount
50 µL of 10 mM DMSO solutions
Plates and formats
384 well, Greiner Bio-One microplates 781280, first and last two columns empty, 320 compounds per plate
Price
Catalog No.
FFP-800-100-Y-10
Compounds
800
10 plates
Amount
100 µL of 10 mM DMSO stock solutions
Plates and formats
96 well, Greiner Bio-One microplates 651201, first and last columns empty, 80 compounds per plate
Price
*We will be happy to provide our library in any other most convenient for your project format. Please select among the following our standard microplates: Greiner Bio-One 781270, 784201, 781280, 651201 or Echo Qualified 001-12782 (LP-0200), 001-14555 (PP-0200), 001-6969 (LP-0400) or send your preferred labware. Compounds pooling can be provided upon request.
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Key features
- Discovery of novel tractable protein targets
- Identification of the binding site of the POI
- Screening directly in cells
- Easy hit confirmation via LC-MS
- Next-generation libraries can be rapidly synthesized through parallel chemistry
This fully functionalized library has been designed based on the fragments with experimentally confirmed solubility in aqueous PBS at 1 mM concentration. The most commonly used alkyl diazirine photoaffinity tag was used for the library. Minimalistic diazirine photocrosslinker rapidly generate carbene upon UV-irradiation (typically 340-360 nm; 302 nm also can used). Generated carbene intermediate rapidly reacts with adjacent amino acid residues or is quenched by water. Interesting fact is that photocrosslinking captures wider range of residues comparative to electrophilic libraries. This leads to greater number of ligandable pockets that can be explored. An alkyne tag enable use of the library in ‘FFF’ workflows in cells. The library contains some reference compounds reported in the literature. In addition, we try to cover as much structural diversity as possible to have different chemotypes and pharmacophores within a limited number of compounds.
Examples of structures in the library
Molecular properties
