PROTAC Services

Viva provides global customers with a full range of PROTAC drug discovery services using the world's leading Structure-Based Drug Discovery technology. These services cover biology and chemistry, including protein preparation and crystal structure studies, high-throughput screening of PROTAC molecules, kinetic studies, drug metabolism, medicinal chemistry, Bioassay, CADD, and other services.

  • 50+
    E3 ligases
  • ~80
    Delivery target protein-PROTAC-E3 ligase ternary complex structures
Drug Metabolism Studies of PROTAC Molecules

PROTACs are bifunctional compounds, an emerging modality, with molecular weights and physicochemical properties that fall outside the classic ‘rule-of-five’ spaces of small-molecule property. In the drug discovery of PROTACs, consequently, there are complex challenges including DMPK, compared with traditional small molecules. Our DMPK group provides flexible, customized services in support of overcoming the challenges in developing oral PROTEC drugs.

 

Common problems and solutions for DMPK evaluation of PROTAC molecules:

DMPK Issue Recommendation
Solubility Insoluable Simulated fluid replace PBS buffer
Permeability Poor recovery Addition of BSA,FBS
Transporter Substrate, or inhibitor Specific transporter, hMDR1 Knockin MDCKll Cells Or, hBCRP Knockin MDCKll Cells
Bioanalysis Unstable Deactivate enzyme in plasma or blood immediately
Bioanalysis Non specific binding Detergent
Bioanalysis Fragment inLs-MS ion source Optimized MS condition
Metabolism Diverse metabolism Comprehensive metabolism system: microsome, hepatocyte, S9,cytosol;AO,UGT activity;  CYP phenotyping
PPB Unstable Enzyme inhibitor
In vivo PK Low bioavailability No fasting
For more information about

Drug Metabolism Studies of PROTAC Molecules”, please contact our team.

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