Macrocycles

Original design beyond Ro5 compounds

1 952 compounds

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.

Typical Formats

Catalog No.
Compounds
Amount
Format

Catalog No.

MCR-491-10-Y-10

Compounds

491
2 plates

Amount

10 µL of 10 mM DMSO solutions

Format

384-well plates, Echo Labcyte LP0200, 320 compounds per plate, first & last two columns empty

Catalog No.

MCR-491-50-X-10

Compounds

491
7 plates

Amount

50 µL of 10 mM DMSO solutions

Format

96-well plates, Greiner # 650201, 80 compounds per plate, first & last columns empty

Catalog No.

MCR-491

Compounds

491

Amount

Custom

Format

Any custom format

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Macrocycles

Library code: MCR-491

Version: 28 June 2021

491 compounds

Macrocycles in stock

1 952 compounds for cherry-picking

Key features

  • Favorable ADME and PK
  • CNS-like molecular parameters
  • Balanced Complexity
  • 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-enlargement, 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

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