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Discovery of inhibitors, binders and modulators – even for hard-to-drug targets – Seamless small molecule drug discovery – Get an early lead

DELs in Cells service with emphasis on high success rate, short turn-around-time, high quality data and low false positive rate.

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

Timelines

Expression study: 4 weeks
Screening: 4 weeks

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
  • High success rate (>80%)
  • Short TAT
  • Identifies hits and hit families
  • Instant structure-activity relationship (SAR)
  • Instant selectivity and specificity of hits by multiplexed screen against target and anti-targets (unique capability)
  • Instant MOA of hits by screening in the presence of a known ligand or resynthesized hit
  • Large scale project with cost reduction by multiplexing (unique capability)
  • 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
  • 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 3 payments
    • Pre-Project Expression Study Fee – scales with work
    • Screening Fee – scales with screening slots
    • Chemical Series Nomination 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 with varying constructs and different libraries. 
    • 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 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).

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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