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DEL Express – fast and easy – a new standard for speedy drug discovery

Our fast and easy DNA-encoded chemical library (DEL) screening service for biotinylated target proteins. You simply provide the biotinylated protein, and Vipergen handles the rest and ships hit compounds to you in just 20 business days. The utilized DNA encoded library (DEL) is optimized for fast off-DNA hit resynthesis The process is designed for speed without compromising success rate and false positive rate. This makes the DELs Express service an excellent choice for projects seeking rapid progression.

Service in brief

  • 1. You provide the biotinylated purified target protein (micrograms)
  • 2. We conduct the screening, perform the analysis and provide a report, including hit list with chemical structure information
  • 3. You order hits
  • 4. We synthesize the hits and ship to you

Timelines

Screening: 10 business days
Hit resynthesis: 10 business days (for up to 25 hits)

Keys

  • Screen requires small quantities of purified biotinylated target protein (micrograms)
  • Screen is conducted with 12 screening slots with varying conditions in parallel
  • Screen is conducted in a homogeneous assay to avoid matrix binders and target denaturation
  • Identifies hits and hit families
  • Instant structure-activity relationship (SAR)
  • High success rate (>75%)
  • Low false positive rates (100% match between DNA code and compound)
  • Applicable across disease areas and target classes (no structural information required)
  • Straightforward and transparent data analysis

Business Model

  • Simple fee-based plan with no reach-through and royalty payments
  • The compensation plan comprises a total of 3 payments
    • Screening Fee – scales with screening slots
    • Synthesis Fee – scales numbers of hits
    • Chemical Series Nomination Fee
  • Hit exclusivity
  • The project flow is rapid and straightforward:
    • Client provides the biotinylated target protein (100 micrograms)
    • Vipergen performs the screening using 12 screening slots in parallel under varying conditions
    • Vipergen delivers a hit list and report, including metrics from screens and chemical structure information 
    • Hits are reserved for client for 1 year
    • Client may request Vipergen to resynthesize hits
    • Vipergen synthesize and ship hits
    • Client may test hits in relevant assays and use data for 1 year 
    • Client may nominate Chemical Series for 1 year
    • Vipergen assigns its rights to Nominated Chemical Series and these become exclusive for client

DELs

Vipergen’s high fidelity DELs are synthesized using robust chemistry and with a purification steps after each chemical transformation, thus providing 100% correspondence between code and compound (no truncates).

Key drivers for library design

  • Chemical diversity
  • Physicochemical properties
  • Fidelity
  • Hit resynthesis (off DNA)
Parameter Lib046 Lib056 Lib081
Size (million of compounds) 445 522 381
Chemistries
  • Acylation
  • Red. amination
  • SNAr
  • Acylation
  • Red. amination
  • Acylation
  • Red. amination
Compounds w 1 cyclic, tertiary amide 49% 47% 52%
Compounds w 2 cyclic, tertiary amides 42% 33%
Total number of building blocks (#) 1507 1327 1138
Designer building blocks (#) 979 755 617
Scaffolds (#) 368 343 295
Toxicophores (%) 1.1 0.4 1.1
Molecular weight (avg) 612 529 525
cLogP (avg) 2.8 0.75 0.9
HBA (avg) 8.7 6.3 6.2
HBD (avg) 2.8 2.8 2.9
Rotatable bonds (avg) 10.7 8.8 8.9
TPSA (avg) 153 139 137
Fsp3 (avg) 0.5 0.6 0.6

Target classes

Our streamlined DNA-encoded chemical library (DEL) screening service for purified proteins has successfully delivered hits and leads against numerous target classes. Including:
Enzymes
  • Kinases
  • Oxidoreductase Proteases
  • Hydrolases
  • Isomerases
  • Transferases
  • Lyases
  • Phosphatases
  • Transcription factors
  • Synthases
  • E3 biquitin ligases
  • Deubiquitinases (DUBs)
  • Helicases
  • Polymerases
  • Nucleotide exchange factors
  • Decarboxylases
  • Ligases
Membrane proteins
  • Integral membrane proteins
  • G protein-coupled receptors (GPCRs)
  • Ion channels
  • Single-pass membrane proteins
Receptors
  • Nuclear receptors
  • Cytosolic receptors
  • Extracellular receptors
Protein-protein interaction targets
  • Transcription factors
  • E3 ligases
  • Deubiquitinases (DUBs)
  • Antibodies
  • Cytokines
  • Interleukins
  • Growth factors
  • Carrier proteins
  • Adaptor proteins
  • Oncoproteins
Epigenetic targets
  • Histone binders
  • Methyl transferases
  • Acetyltransferase
  • Demethylases
  • Deacetylases
Pathogenic targets
  • Viral proteins (enzymes and coat proteins)
  • Bacterial proteins (enzymes and receptors)
  • Fungal proteins (enzymes and receptors)

Technical information

Do you have an inquiry?

Contact us today and explore partnership opportunities.

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