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Discovery Plus™ Screening: Transporter Inhibition

Our Transporter Inhibition Screening service gives you quick, low-cost inhibition data for one or more compounds to inform you of your drug candidates’ potential to inhibit clinically relevant drug transporters, allowing efficient prediction of drug-drug interactions (DDIs) in early stages of drug development. 

Discovery Plus™ Transporter Inhibition studies provide a first look at the possible interaction between new drug candidates and the transporters listed in the FDA, PMDA and EMA drug interaction guidance documents. Drug transporters can affect the absorption, distribution, metabolism, and excretion (ADME) properties of drugs and have the potential to be involved in drug-drug interactions. 

Moving quickly through drug discovery and development saves you time and money; get data from a Discovery Plus™ screening study quickly to make risk-based decisions faster and get you through the pipeline more efficiently.

For compounds that will be submitted for regulatory agency approval, please see our definitive Drug Transporter services.

Our Approach to Medium-Throughput Transporter Inhibition Screening

Discovery Plus™ transporter inhibition is a non-GLP service that quickly provides customers with a tabular data summary. Our assay designs allow the flexibility to mix and match the number of compounds, transporters, and concentrations. All experiments are carried out on cell lines expressing the transporter of interest.

  • Incubations performed in 24-well transwell plates (for efflux transporters, e.g. P-gp and BCRP) or 24-well cell culture plates for SLC (uptake) transporters
  • Incubations performed in triplicate
  • Positive control inhibitors included
In vitro drug transporters being used
TransporterTest SystemProbe Substrate (µM)
P-gp (MDR1)Caco-2 cellsDigoxin
OATP1B1HEK293 cells3H-Estradiol-17β-glucuronide
OATP1B3HEK293 cells3H-Estradiol-17β-glucuronide
OCT2HEK293 cells14C-Metformin
OAT1HEK293 cells3H-Estrone-3-sulfate
OAT3HEK293 cells3H-Tetraethylammonium bromide

What’s Next?

When you’re ready to start contracting IND-enabling preclinical ADME & DDI studies, work with a specialty CRO you can trust to give you high-quality data every time

CTA - Products 7 - Subcellular fraction test systems preparation