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Macrocycles

Original design beyong Ro5 compounds

179 compounds in stock

Macrocyclic motifs are commonly found in natural products and their grown usage in drug discovery helps to tackle “difficult” targets with extended binding sites. The size and complexity of macrocyclic compounds make possible to ensure numerous and spatially distributed binding interactions, thereby increasing both binding affinity and selectivity. Macrocylic structure often provides necessary balance between degree of structural preorganisation (that may reduce the entropy cost of receptor binding as compared to linear analogues) and sufficient flexibility (comparing to common rigid (poly)cyclic cores) that can facilitate interactions with diverse dynamic protein targets. In addition, is spite of their size macrocyclic compounds show favorable ADME- and PK-properties.

Key features

  • Favorable ADME and PK
  • CNS-like molecular parameters
  • Balanced Complexity
  • No more than one amide bond in the macrocycle scaffolds
  • High novelty

Ring-enlargement application

RCM-application

Our products and advantages:

  • Libraries of drug-like compounds with middle-size-macrocyclic cores
  • Only MedChem friendly compounds, all industry affiliated filters including PAINS were applied
  • Well-elaborated methods of macrocyclization (RCM, click, ring-enlargment, macrolacton/lactamization etc.)
  • Valuable scaffolds, over 20 diverse key middle-size macrocyclic intermediates in stock
  • Decoration with diverse Enamine’s off-the-shelf capping agents
  • Rapid synthesis of macrocyclic library in 4 weeks only through well-validated parallel chemistry
  • Rapidly expanding REAL MacroSpace

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