DEL – PPI Inhibitor Direct – Seamless small molecule drug discovery – Get an early lead
Protein-protein interaction inhibitors
Protein-protein interactions (PPIs) are fundamental to cellular signaling and transduction which marks them as attractive therapeutic drug development targets. Once considered “undruggable” by small molecules due to their complexity, PPIs are now established as druggable targets in drug discovery. This paradigm shift provides a unique opportunity to develop novel therapies for a diverse range of conditions.
Our unique DEL – PPI Inhibitor Direct service takes advantage of our unique capability for multiplexing. The two interacting target proteins are screened in a multiplexed format and compared to monoplexed screens whereby PPI inhibitors are identified.
Service in brief
- 1. You provide the purified target proteins (micrograms)
- 2. We conduct a feasibility 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
Feasibility study: 2-4 weeks
Screening: 4-8 weeks
Keys
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Screen requires small quantities of purified target proteins (micrograms)
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Screen is conducted in a multiplexed fashion (unique capability)
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Screen is conducted with many conditions in parallel
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Screen is conducted in a homogeneous assay to avoid matrix binders and target denaturation
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Identifies PPI inhibitors directly
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Identifies hits and hit families
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Instant structure-activity relationship (SAR)
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High success rate (>75%)
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Low false positive rates (100% match between DNA code and compound)
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Applicable across disease areas and target classes
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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 Feasibility 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 target proteins (100 micrograms)
- Vipergen performs Feasibility Study (go-no-go)
- Vipergen performs one or two rounds of screening, each under varying conditions and with different libraries.
- After each screening round, 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 becomes 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 |
|
|
|
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
- Kinases
- Oxidoreductase Proteases
- Hydrolases
- Isomerases
- Transferases
- Lyases
- Phosphatases
- Transcription factors
- Synthases
- E3 biquitin ligases
- Deubiquitinases (DUBs)
- Helicases
- Polymerases
- Nucleotide exchange factors
- Decarboxylases
- Ligases
- Integral membrane proteins
- G protein-coupled receptors (GPCRs)
- Ion channels
- Single-pass membrane proteins
- Nuclear receptors
- Cytosolic receptors
- Extracellular receptors
- Transcription factors
- E3 ligases
- Deubiquitinases (DUBs)
- Antibodies
- Cytokines
- Interleukins
- Growth factors
- Carrier proteins
- Adaptor proteins
- Oncoproteins
- Histone binders
- Methyl transferases
- Acetyltransferase
- Demethylases
- Deacetylases
- Viral proteins (enzymes and coat proteins)
- Bacterial proteins (enzymes and receptors)
- Fungal proteins (enzymes and receptors)
Technical information
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