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Assay Development and DMPK Testing

Biochemical Assay Development

DMPK Testing

Protein Production

 

Biochemical Assay Development

Domainex is able to support its clients in the development of biochemical assays, as a component of integrated drug discovery projects.

Our skilled assay biologists are able to develop and validate enzyme and ligand-binding assays in a wide-range of spectrophotometric, luminescence and fluorescence based formats.  We can screen and characterise compounds in medium-throughput assays for hit-finding and later during the lead optimization phase of your discovery programme.

We are also able to characterise compounds as they are produced using kinetic solubility, Cytochrome P450 inhibition and microsomal clearance assays and feed this information back into our drug design.

Domainex is also able to clone and express target protein if required to support assay development. As target protein production can be challenging, Domainex also offers its proprietary Combinatorial Domain hunting technology when needed, for the fast and efficient identification of expressible, soluble, ligand binding protein domains. Click here to find out more.

 

DMPK Testing

Domainex is also able to offer seamless support of its clients' DMPK testing requirements via its closely located partner, Pharmidex. Domainex and Pharmidex have built up an excellent working relationship over a number of years and both companies work together to ensure speed and efficiency at all stages of a client's discovery program.

Pharmidex provides an extensive range of ADMET technologies aimed at optimizing potential new medicines for drug development risks using both preclinical and human prediction data. Together with a wealth of knowledge and experience in CNS, CV, respiratory and inflammatory discovery programmes, Pharmidex can aid rapid progression and improvement in the probability of success of potential new medicines.

Pharmidex's offering includes, but is not limited to:

  • In vitro
    • Physico-chemical properties
      • LogD
      • Solubility in PBS or biological fluids
      • Stability in PBS or biological fluids
    • Metabolic stability
      • Metabolic stability in liver microsomes, S9 fraction
      • Metabolic stability in cryopreserved hepatocytes
      • Metabolic stability in other tissues and fluids (as % turnover, half life or intrinsic clearance)
    • Blood distribution and protein binding
      • Plasma protein binding - human & most species
      • Blood partitioning - human & most species
      • Tissue partitioning human & most species
      • Blood to brain partitioning - human & most species (fraction unbound)
    • Cell Permeability and transporter interactions
      • Cell permeation - passive and Pgp mediated (MDR/MDCK)
    • CYP interactions
      • Inhibition in singly-expressed human P450 inhibition
      • Inhibition of Human P450 in microsomes (probe drugs via LC-MS/MS)
      • Time dependent inhibition of human P450s
      • Induction- Human P450 induction in hepatocytes
      • Reaction Phenotyping -Human P450├é isoform specific metabolism reactive metabolism glutathione trapping
      • Metabolite identification in biological samples

Please contact us for more information, or see Pharmidex's website for further information