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Developed to expand the structural diversity of Molecular Glues

880 compounds

The Phenyl Dihydrouracil (PD) scaffold introduces a fundamentally new concept in the field of CRBN binders. Departing from the paradigm of the glutarimide ring, this scaffold offers significant advantages. In particular, the dihydrouracil fragment demonstrates much higher chemical stability, including resistance to hydrolysis, which has been critical for various Molecular Glues.

The absence of a chiral center solves another major issue for Molecular Glues containing amino glutarimide fragments — the problem of racemization. Moreover, Phenyl Dihydrouracil (PD) scaffold-based Molecular Glues and PROTACs show improved protein degradation efficacy and cellular potency.

Representative examples of building blocks for library design

Examples of the molecules in the library

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Phenyl Dihydrouracil (PD) Library

Library code: PD-880

880 compounds

Typical Formats

Catalog No.
Compounds
Amount
Format
Price

Catalog No.

PD-880-0-Z-20

Compounds

880
1 plate

Amount

≤ 300 nL of 20 mM of DMSO solutions

Plates and formats

1536-well Echo LDV microplates, first and last four columns empty, 1280 compounds per plate

Price

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Catalog No.

PD-880-10-Y-20

Compounds

880
3 plates

Amount

10 µL of 20 mM DMSO solutions

Plates and formats

384-well Echo plates, Labcyte #LP-0200, 320 compounds per plate, first two and last two columns empty

Price

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Catalog No.

PD-880-50-X-20

Compounds

880
11 plates

Amount

50 µL of 20 mM DMSO solutions

Plates and formats

96-well plates, 80 compounds per plate, first and last columns empty; Greiner #781270

Price

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*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.

Selected publication

  1. Phenyl Dihydrouracil: An Alternative Cereblon Binder for PROTAC Design.
    ACS Med. Chem. Lett. 2023, 14, 2, 141–145. DOI: 10.1021/acsmedchemlett.2c00436

Support

We offer comprehensive support in developing your hit compounds. Naturally such programs are realised most efficiently when biological actives originate from our screening collection. However, even if the hit compounds are from the collections of other vendors lead identification and optimization projects can proceed most productively in our hands. Sometimes for this we only need to synthesize first examples of the given chemical series and validate synthesis route.

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