Original design beyond Ro5 compounds
1 952 compounds for cherry-picking and 500 in Macrocycles Library
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
Macrocycles Library is available for supply in various pre-plated formats, including the following most popular ones:
Catalog No.
MCR-500-0-Z-10
Compounds
500
1 plate
Amount
≤ 300 nL of 10 mM of DMSO solutions
Plates and formats
1536-well Echo LDV microplates, first and last four columns empty, 1280 compounds per plate
Price
Catalog No.
MCR-500-10-Y-10
Compounds
500
2 plate
Amount
≤ 10 µL of 10 mM DMSO solutions
Plates and formats
384-well, Echo Qualified LDV microplates #001-12782 (LP-0200), first and last two columns empty, 320 compounds per plate
Price
Catalog No.
MCR-500-50-Y-10
Compounds
500
2 plate
Amount
50 μL of 10 mM DMSO solutions
Plates and formats
384-well, Greiner Bio-One plates #781280, 1,2 and 23,24 columns empty, 320 compounds per plate
Price
Catalog No.
Library & follow-up package
Plates and formats
MCR-500-10-Y-10 screening library 500 cmpds, hit resupply, synthesis of analogs from REAL Macrocycles
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), C52621 or send your preferred labware. Compounds pooling can be provided upon request.
Download SD files
1 952 compounds for cherry-picking
4.72M compounds
Key features
- Favorable ADME and PK
- CNS-like molecular parameters
- Balanced Complexity
- High novelty
Ring-enlargement application
RCM-application
Macrocycles Design:
- 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
