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DELs in Cells – Snap – Seamless small molecule drug discovery – Get an early lead

DELs in Cells – Snap. Our easy, fast, and affordable DNA-encoded chemical library (DEL) in living cells screening service.

Service in brief

  • 1. You provide the amino acid sequence of the target protein(s)
  • 2. We conduct an expression studyand provide a report
  • 3. You say ”go”
  • 4. We conduct the screening, perform the analysis and provide a report, and chemical structure information for 25 top hits

Timelines

Expression study: 4 weeks
Screening: 4 weeks

Keys

  • Screen is conducted in a living cell
  • Screen is conducted using 2 screening slots (2 constructs or 2 DELs) in parallel
  • Chemical structure information for 25 top hits
  • More physiologically relevant conditions
  • Lower attrition rate (assumed)
  • Broader target space – no need for purified target protein
  • High success rate (>70%)
  • 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)
  • Straightforward and transparent data analysis

Business Model

  • Simple fee-based plan with no reach-through and royalty payments
  • Hit exclusivity
  • The compensation plan comprises a total of 2 payments
    • Expression Study Fee 
    • Screening Fee
  • 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 2 screening slots ( 2 constructs or 2 DELs) 
    • Vipergen delivers a hit list and report, including metrics from screens and chemical structure information for top 25 hits 
    • Vipergen assigns its rights for top 25 hits 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).

Key drivers for library design

  • Chemical diversity
  • Physicochemical properties
  • Fidelity
  • Hit resynthesis (off DNA)
Parameter Lib047 Lib058 Lib081 Lib100
Size (million of compounds) 499 603 381 511
Chemistries
  • Acylation
  • Red. amination
  • SNAr
  • Acylation
  • Red. amination
  • Acylation
  • Red. amination
  • Acylation
  • Red. amination
Compounds w 1 cyclic, tertiary amide 48% 50% 52% 37%
Compounds w 2 cyclic, tertiary amides 34% 33% 57%
Total number of building blocks (#) 1580 1339 1138 1043
Designer building blocks (#) 948 657 617 635
Scaffolds (#) 394 353 295 323
Toxicophores (%) 1.0 1.3 1.1 2.2
Molecular weight (avg) 605 503 525 598
cLogP (avg) 2.7 2.8 2.9 2.6
HBA (avg) 8.6 6.0 6.2 6.9
HBD (avg) 2.8 2.8 2.9 2.5
Rotatable bonds (avg) 10.5 8.3 8.9 9.2
TPSA (avg) 152 135 137 144
Fsp3 (avg) 0.5 0.6 0.6 0.5
Suitability for difficult targets *** ** ** ***

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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Snap – easy, fast, and affordable