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DELs in Cells – Express – a new standard for speedy drug discovery

DELs in Cells – Express service is fast and easy. You simply provide the amino acid sequence of your target protein, and Vipergen handles the rest and ships hit compounds to you in just 30 business days. The process is designed for speed without compromising success rate and false positive rate. The utilized DNA encoded library (DEL) is optimized for fast off-DNA hit resynthesis. This makes the DELs in Cells – Express service an excellent choice for projects seeking rapid progression, even if purified target protein is not readily accessible.

Service in brief

  • 1. You provide the amino acid sequence of the target protein(s)
  • 2. We conduct an expression study and provide a report
  • 3. You say ”go”
  • 4. We conduct the screening, perform the analysis and provide a report, including hit list
    with chemical structure information
  • 5. You order hits
  • 6. We synthesize the hits and ship to you

Timelines

Expression study: 10 business days (for target with MW up to 75 kDa)
Screening: 10 business days
Resynthesis of hits: 10 business days (for up to 25 hits per batch)

Keys

  • Screen is conducted in a living cell
  • More physiologically relevant conditions
  • Lower attrition rate (assumed)
  • Broader target space – no need for purified target protein
  • Higher success rate (>80%)
  • Shorter TAT
  • Identifies hits and hit families
  • Low false positive rates (100% match between DNA code and compound)
  • Applicable across disease areas and target classes (no structural information required)
  • Demonstrated ability to address targets considered difficult, including transcription factors, protein complexes, and PPI targets
  • Straight forward and transparent data analysis

Business Model

  • Simple fee-based plan with no reach-through and royalty payments
  • The compensation plan comprises a total of 4 payments (pay as you go)
    • Pre-Project Expression Study Fee
    • Screening Fee
    • Synthesis Fee – scales numbers of hits
    • Chemical Series Nomination Fee
  • Hit exclusivity
  • The project flow is rapid and straightforward:
    • Client provides the amino acid sequence for the target protein
    • Vipergen performs the Expression Study (go-no-go)
    • Vipergen performs one round of screenings using 4 screening slots with varying constructs.
    • 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 resynthesize and 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 step after each chemical transformation, thus providing 100% correspondence between code and compound (no truncates). DELs applied for the Express service are optimized for fast off-DNA hit resynthesis.

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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