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CRBN binders and their functionalized analogs

Cereblon (CRBN) is one of the most explored E3 ligases extensively used to construct PROTACs, search for new Molecular Glues, and develop functionalized tool compounds. The most extensive research has been done in this area. CRBN ligands are also known to have a good ADME profile, allowing for the development of orally bioavailable PROTACs.

We have been working with Thalidomide-like and Glutarimide chemistry for years and gained versatile experience in this chemistry field. Our experienced chemists are continuously working on the design and synthesis of new attractive Building Blocks, while our parallel chemistry group extensively elaborates approaches in the modification of the most interesting intermediates. This knowledge allowed us to enumerate a REAL Array of over 18 million CRBN-focused compounds, which can be synthesized within only 4 weeks and with 80% success rate.

Screening Compounds and Libraries

Over 15 000 CRBN focused compounds are available from stock including Glutarimides, IMiD Library Uracil-like, and Avadomide derivatives. All products are constantly updated with newly synthesized compounds. Covalent modifiers are represented by diverse and the most reliable warheads focusing on Cys, Lys, and Ser residues.

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Plated

IMiD Library

Library code: IMiD-4900

4 900 compounds

at 20 mM in DMSO

Covalent CRBN Library

Library code: CCRBN-160

160 compounds

at 20 mM in DMSO

CRBN Molecular Glues Library

Library code: CRBN-MG-4560

4 560 compounds

Stock

REAL

Product catalog

Product name
Size
Description
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IMiD Library

IMiD-4900

Size

4 900
compounds

Descriptions

Designed and specially synthesized for the discovery of Immunomodulatory Imide Drugs

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CRBN Molecular Glues Library

CRBN-MG-4560

Size

4 560
compounds

Description

Designed to capture the widest possible range of novel chemotypes of CRBN binders, providing a foundation for the discovery of next-generation Molecular Glues

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PAG Library

PAG-640

Size

640
compounds

Description

Built upon novel Phenyl Amino Glutarimide (PAG) analogs, these compounds combine structural innovation with potent activity — offering a fresh perspective in Molecular Glue design

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PD Library

PD-880

Size

880
compounds

Description

Chemical stability, cellular potency, and permeability are just a few of the advantages that make Phenyl Dihydrouracil (PD)-based CRBN ligands promising candidates for optimal Molecular Glue discovery

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PG Library

PG-800

Size

800
compounds

Description

Phenyl Glutarimide (PG)-based library was purposefully developed to expand the structural diversity space of Molecular Glues

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Len Library

Len-640

Size

640
compounds

Description

Lenalidomide- and Pomalidomide-scaffold based — a time-tested backbone, reimagined for modern Molecular Glue design

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AAG Library

AAG-1600

Size

1 600
compounds

Description

Acylated Amino Glutarimide (AAG) featuring 5- and 6-membered heterocyclic systems: a promising platform for the discovery of next-generation Molecular Glues

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Avadomide library

AVD-560

Size

560
compounds

Descriptions

A special selection of new Avadomide analogs

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Diverse CRBN Library

CRBN-960

Size

960
compounds

Descriptions

Designed to cover all structural diversity of CRBN binders, a key component of the E3 ubiquitin ligase complex

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CRBN Covalent Library

CCRBN-160

Size

160
compounds

Descriptions

A small selection of diverse covalent binders capable of interacting with CRBN

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Representative examples of compounds in pre-plated CRBN Diversity Library

Examples of compounds in pre-plated CRBN Covalent Library

Examples of in-stock CRBN binders with linkers

Latest Arrivals

Glutarimide ring variation

Imide motif variation

Core structure variation

 

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