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.
MCR-436-10-Y-10
Compounds
436
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-436-50-X-10
Compounds
436
6 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-436
Compounds
436
Amount
Custom
Format
Any custom format
Download SD files
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