Explora ADMET
- Physico-chemical properties
HTS solubility, shake-flask solubility, stability in buffers, plasma/serum protein binding, etc. - Membrane permeability
Artificial membranes (PAMPA), cell lines e.g. Caco-2, hMDR1-MDCK - Stability in biological matrices
Plasma, serum, liver microsomes or S9 fractions, cryopreserved hepatocytes, lung and intestinal homogenates; several species available - Metabolite identification studies
From in vitro incubation in any biological matrix, plasma and/or other matrices from in vivo treatments - Drug-drug interaction
- CYP450 inhibition studies (human recombinant isoforms, fluorimetric assay, liver microsomes, LC-MS/MS)
- Time-dependent CYP3A4 inhibition
- P-glycoprotein inhibition (hMDR1-MDCK cells, calcein assay)
- CYP450 phenotyping (human recombinant isoforms)
- In vitro toxicity
- Different cell lines available (HepG2, human dermal fibroblasts, human epidermal keratinocytes, HeLa cells)
- hERG binding (HEK293-hERG cells,
3H-astemizole binding)
Our Services: Early ADMET for Developabilty Assessment
Explora ADMET: Reveal and Focus Assays
The Explora ADMET Service is a range of robust, high quality in vitro developability and toxicology assays designed to support all stages of drug discovery from hit validation to preclinical candidate selection. They are available either as a standalone service or as part of our integrated drug discovery service.
The Reveal Assays are a collection of basic, essential in vitro assays for the rapid generation of key developability data to guide the medicinal chemists during the lead optimization process.
The Focus Assays are available to probe developability parameters in more detail.