Maybridge Fragment Libraries

View pdf flier here.

Fragment–based screening is gaining wider acceptance, in both the academic and commercial arenas, as a highly effective method of expediting the drug discovery process.  The Maybridge Fragment Range has been developed to meet the needs of researchers by harnessing the quality and structural diversity you have come to expect from Maybridge products.  The range of fragment focussed products includes:

• The Maybridge Fragment Collection: Over 30,000 Maybridge compounds assembled to provide convenient access to the extensive Maybridge portfolio when building your own bespoke Fragment screening libraries or searching for Hit analogues.  The Collection has been filtered in terms of purity, molecular weight (≤350Da) and removal of inappropriate functionality to allow you complete freedom to design a library to your own specific needs.
• The Maybridge Bromo-Fragment Collection: A collection of over 1500 bromine containing Maybridge fragments constructed as an aid to X-ray based fragment screening and to provide a set of Fragments suited to rapid hit evolution.
• The Maybridge Fluoro-Fragment Collection: A set of over 5300 fluorine containing fragments which are a convenient source for 19F NMR based applications.
• The Maybridge Pre-Fragment Collection:  An invaluable source of reactive “Pre-Fragments” which can be used to either synthesise your own bespoke fragments or to evolve your hits.  We currently have available sets of:
  • Sulfonyl chlorides
  • Isocyanates
  • Acid chlorides and pentafluorophenylesters

The Maybridge Fragment range also offers two market leading preselected libraries which have been carefully designed to facilitate the rapid acquisition of high quality fragments:

The Maybridge Ro3 1500 Diversity Fragment Library:  As the field of Fragment–Based Drug Discovery continues to mature there is an increasing need to gain access to fragments of the highest quality.  Built on a pedigree of almost 50 years of heterocycle research, the Maybridge Fragment Range has grown with the technology over the past 6 years as structure based techniques become more central to the drug discovery process and many successful fragment screening programmes have Maybridge Fragments at their heart.

The latest addition to the Maybridge Fragment Range, is the Maybridge Ro3 Diversity Fragment Library.  The library has been engineered to build on the key customer driven features of original Maybridge Ro3 Library, such as Ro3 compliance pharmacophoric enrichment and quality assurance.   The Maybridge Ro3 Diversity Library offers both an improved structural diversity profile and experimental solubility data for each of the 1500 members.

Key Features

• Rule of Three (Ro3) compliance
• Computationally engineered diversity
• Assured solubility in both DMSO (200mM) and PBS buffer (1mM)
• Assured quality to ≥95%, including NMR spectra for each of the 1500 compounds
• Chemically “clean” – removal of reactive group whilst retaining “handles” for conjugation and hit evolution.
• Pharmacophore rich but not too complex

The result is a unique tool for efficiently probing structural space within your target protein. Click here to download the Ro3 Fragment flyer.

• The Maybridge Ro3 500 Fragment Library: A set of 500 fragments extracted from the Maybridge Ro3 Fragment Library which incorporates all of the benefits of its larger parent library.  The Maybridge Ro3 500 Fragment Library has been developed to meet the needs of the customer who wants the convenience of a preselected high value fragment product but is looking for a small scale, cost effective entry point into fragment based drug discovery.

Maybridge Fragments are available custom weighed to your requirements in milligram (≥5mg) or micromolar quantities (≥ 25μmol) and have been selected to ensure that they are readily available for re-supply. Full analytical data is supplied with all orders for the Ro3 1500 or Ro3 500 libraries.

Fragment Hopping with Maybridge Fragments
One of the key advantages of working with Maybridge Fragments is that Fragment Hopping is facilitated across the entire Maybridge portfolio.  Maybridge Building Blocks and Fragments have been developed through a highly structured product innovation strategy allowing the introduction of logical sets of related compounds which benefit from minimal substitution, a key aspect for effective pharmacophore investigation.

Registered users can download SD or ISIS db files from the download section for the product ranges listed above.