VENENUM Biodesign‘s drug discovery team is composed of biologists and chemists with years of experience identifying validated small molecule drug targets across therapeutic areas. Once validated, we develop state-of-the-art assays and models for HTS or Rational design, respectively. Using our screening technology, we have a track record of success in finding multiple novel chemotypes to advance compounds into animal studies. We have established a suite of in vitro assays to determine drug-like properties including microsomal stability, protein binding, solubility, CYP450 interactions, cytotoxicity, cell permeability, and specificity. We use state-of-the-art in vivo models to test our compounds PK and efficacy in predictive models of disease to develop PK/PD relationships.
Compounds and Data Management
ECLiPS compound libraries are arrayed into microplates for UHTS using state-of-the-art technology. VENENUM Biodesign’s compound management laboratory is equipped with a variety of plate-to-plate reformatting liquid handlers, allowing the transfer of test compounds from 96-well or 384-well source plates to higher-density microplates. In addition, we use our ATS-100 (Biosero) for acoustic transfer of compound solutions in the 1-1000 nL range. Compound and biological data are maintained in our secure and confidential database.
In the UHTS stage, we develop biological assays that are suitable for compound screening in 1536-well format. This includes both cell-based and biochemical assays designed to measure ligand binding, enzymatic activity, and cell function. Ideal UHTS format assay technologies include, but are not limited to, fluorescence, fluorescence resonance energy transfer (FRET), time-resolved fluorescence (TRF), homogeneous time-resolved fluorescence, absorbance, luminescence, and AlphaScreen®. Screening assays can be configured with either kinetic or endpoint detection.
VENENUM Biodesign optimizes screening assays for high reproducibility and sensitivity. We establish CVs, z-factors, and work with reference compounds to ensure assay quality. Because of the large size of the screening deck (~6 million small molecules), assays are adapted to 1536-well format in <10 microliter assay volume.
Hit-to-Lead and Lead Optimization
Pending joint assessment of the chemical and biological properties of the screening hits, our biology and chemistry teams progress promising compound series through hit-to-lead and lead-to-development candidate studies.