Cereblon ligands and functionalized intermediates

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 8 million CRBN-focused compounds, which can be synthesized within only 4 weeks and with 80% success rate.

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Screening Compounds and Libraries

Over 11 000 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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CRBN focused compounds

11 452 compounds

IMiD Library

Library code: IMiD-4900

Version: 15 March 2024

4 900 compounds

at 20 mM in DMSO

Diverse CRBN Library

Library code: CRBN-960

Version: 14 March 2024

960 compounds

at 20 mM in DMSO

sublibrary of IMiD-4900

Covalent CRBN Library

Library code: CCRBN-160

Version: 7 September 2023

160 compounds

 

 

Typical Formats

Catalog No.
Compounds
Amount
Format
Price

Catalog No.

IMiD Library
IMID-4900-10-Y-20

Compounds

4 900
16 plates

Amount

10 µL of 20 mM DMSO solutions

Plates and formats

384-well Echo Qualified plates, 320 compounds per plate, first two and last two columns empty

Price

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Catalog No.

Diverse CRBN Library
CRBN-960-25-Y-20

Compounds

960
3 plates

Amount

25 µL of 20 mM DMSO solutions

Plates and formats

384-well Greiner plates, 320 compounds per plate, first two and last two columns empty

Price

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Catalog No.

Covalent CRBN Library
CCRBN-160-50-X-20

Compounds

160
2 plates

Amount

50 µL of 20 mM DMSO solutions

Plates and formats

96-well Greiner plates, 80 compounds per plate, first and last columns empty

Price

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Catalog No.

CRBN Library
CRBN-960

Compounds

960

Amount

Custom

Plates and formats

Any custom format

Price

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All our screening compounds can be represented by the following subclasses and types of CRBN binders:

  • All Glutarimides in stock – 5 758 compounds
  • Lenalidomide scaffold-based molecules – 2 720 compounds
  • Thalidomide-like derivatives with linkers – 300 compounds
  • REAL Molecular Glues – 4M+ compounds
  • CRBN ligands with linkers – 300 compounds
  • REAL CRBN ligands with covalent warheads

 

We are constantly working on the update and synthesis of new derivatives of known binders and new potential CRBN ligands.

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

Building Blocks

  • CRBN 1st generation Intermediates – 600 compounds
  • CRBN 2nd generation Intermediates – 200 compounds
  • CRBN 3rd generation 5-membered Intermediates – 400 compounds
  • CRBN MADE Building Blocks – over 80 000 intermediates.

Latest Arrivals

Glutarimide ring variation

 

 

Imide motif variation

 

 

Core structure variation

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