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
Transporter | Test System | Probe Substrate (µM) |
---|---|---|
P-gp (MDR1) | Caco-2 cells | Digoxin |
BCRP | MDCKII-BCRP cells | Prazosin |
OATP1B1 | HEK293 cells | 3H-Estradiol-17β-glucuronide |
OATP1B3 | HEK293 cells | 3H-Estradiol-17β-glucuronide |
OCT2 | HEK293 cells | 14C-Metformin |
OAT1 | HEK293 cells | 3H-Estrone-3-sulfate |
OAT3 | HEK293 cells | 3H-Tetraethylammonium bromide |