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Macrocyclic Compound Libraries


Medicinal chemists have long considered compounds with medium- and large-sized rings to be a distinct class of molecules, not only because of their interesting biological properties but also due to the specificfeatures of their synthesis. ASINEX has extensively researched the development of the most effective synthetic methods leading to macrocyclic entities and their corresponding pharmacological properties with a particular focus on solubility and cellular permeability. Currently, Asinex is the leading source of macrocyclic screening compounds of unparalleled diversity which covers both peptide-like and non-peptidicchemotypes. Our macrocyclic library is comprised of 200+ scaffolds and this number is growing, making our library the largest commercial screening collection of scaffold-based macrocycles. Macrocycles tend to be larger than traditional screening molecules which make them perfect discovery tools for targets with shallow or extended binding sites. Their unique character based on restricted flexibility and ability to form intra-molecular hydrogen bonds facilitates a balance between aqueous solubility and cellular permeability. More than 4000 of our macrocycles have been tested for aqueous solubility and PAMPA permeability.This valuable dataset was used to build up an ML-based computational model to predict the permeability of novel macrocycles based on their 2D and 3D descriptors. Please visit our online catalog for available macrocyclic compounds or contact our customer support team for any additional information about our macrocycle-directed platforms.

Product Name: Format/Size Descriptions Download
Macrocycles 10091 compounds
For cherry-picking
Update: 2021-04
ASINEX has elaborated a library of diverse macrocycles using an effective tool box of synthetic methods. The resulting scaffolds are novel and have allowed us to generate tremendously diverse, medchem-relevant, macrocyclic frameworks. Many of our macrocycles have been tested for aqueous and DMSO solubility with cut-offs applied at 10 mM in DMSO and 50 µM in PBS (pH 7.4) followed by PAMPA permeability assay.
Macrocycles for RNA 1065 compounds
For cherry-picking
Update: 2020-10
Macrocyclic Glycomimetics 1412 compounds
For cherry-picking
Update: 2020-07
Macrocyclic glycomimetics are an extremely interesting class of glycomimetics as they occupy space between small and macro molecules. Macrocyclic glycomimetics are mostly represented by naturally occurring molecules derived from marine microorganisms and bacterial or fungal metabolites.
CNS Macrocycles 1122 compounds
For cherry-picking
Update: 2020-07
SL#008, 016, 036, 039,100
Macrocyclic Glycomimetics
80 compounds x 5
Pre-Plated Set
Release: 2016-2018
Macrocyclic glycomimetics are an extremely interesting class of glycomimetics as they occupy space between small and macro molecules. Macrocyclic glycomimetics are mostly represented by naturally occurring molecules derived from marine microorganisms and bacterial or fungal metabolites.
SL#009
Cell Permeable Macrocycles
80 compounds
Pre-Plated Set
Release: 2016
This library has been tested in PAMPA assays and show permeability Pe greater than 4-16*10-6 cm/s. Generally, such compounds have excellent cellular permeability.
SL#032
Macrocyclic BH3 mimetics
80 compounds
Pre-Plated Set
Release: 2016
Extensive in vitro screening of the Asinex Macrocyclic collection has revealed a series of molecules showing a μM range of activity against anti-apototic proteins Bcl-2 and Mcl-1. In silico modeling studies suggest that some active macrocycles can adopt a-helix-mimetic conformations that effectively mimic the BH3-epitope of pro-apoptotic peptides (e.g. Bak, Bax).
SL#034
Macrocyclic β-turn mimetics
80 compounds
Pre-Plated Set
Release: 2016
Asinex has created a library of partially peptidic macrocyclic beta-turn mimetics that are able to reproduce the orientation of key amino-acid side chains forming a b-turn-like motif.
SL#035
Oncology
Phenotypic Screening-3
80 compounds
Pre-Plated Set
Release: 2016
ASINEX, has evaluated the susceptibility of several cancer cell lines (i.e. RKO, HCT116, Molt-4, Rs4-11, U937, A549, H1568, H23, PANC1, A2780) to an array of peptidic and non-peptidic macrocycles and identified a series of compounds that kill cancer cells at µM concentrations.
Contact
Global

Ludmila Sadovenko

lsadovenko@asinex.com
North America

Mark Parisi

mparisi@asinex.com

Toll Free: +1 877 ASINEX1

Tel: +1 336 721 1617

Fax: +1 336 721 1618

N.Chestnut St., Ste.104

Winston-Salem, NC 27101

USA

Europe

Galina Afanasyeva

gafanasyeva@asinex.com

Tel: +31 (0) 203416183

Klaprozenweg 75C, 1033NN

Amsterdam, The Netherlands

Japan

Shingo Ota

sota@asinex.com

Tel: 080-3401-9097

30-2 Higashihazu, Nishio,

Aichi Japan

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