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SLC (Uptake) Drug Transporter Assay Design

To determine if compounds are substrates of uptake transporters, their accumulation in transporter-expressing cells and control cells are compared. To determine if compounds are inhibitors of uptake (SLC) transporters, the ability of the compound to prevent the uptake of probe substrates is measured. These assays are conducted using attachable host cells (HEK293 or S2 cells) transfected with vectors containing human transporter cDNA.

Experimental model for uptake of substrate into transporter-expressing cells

Comparison of the uptake activity in the transporter-expressing cells and control cells is used to investigate whether the candidate is a substrate of an SLC transporter or not.

The inhibitory effect of the drug candidate is evaluated by measuring the uptake of the probe substrate in the presence of multiple test compound concentrations. These data can then be used to calculate an IC50 value (concentration causing 50% inhibition of transporter-mediated transport).

Drug Transport-Related Resources

For more information to guide your decision making on timing and individual transporters to assess, access our Drug Transporters Decision Treea poster comparing of regulatory expectations between FDA, EMA, and PMDA or our collection of transporter-related scientific content. Additional features of our drug transport study design and a chart of known clinically relevant transporter DDIs can be found on our Drug Transport Services page.

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There’s a lot to choose from

We’re proud to offer you the widest selection of options available when it comes to your transporter studies

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Which transporters could your compound interact with?

When considering follow-up actions to testing compounds as substrates and inhibitors of drug transporters, use our decision tree to make smart choices

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