Transporter Drug Discovery

Custom cell-based tools and advanced technologies for transporter research

Advance your transporter drug discovery with Sygnature Discovery’s Transporter Discovery Platform, featuring custom cell-based tools and advanced technologies, to deliver robust data and accelerate your research.

Human Solute Carrier (SLC) transporters are essential proteins that regulate molecule and ion movement across cell membranes, supporting processes such as nutrient uptake, waste removal, and cell signalling. Their role in cellular balance makes them promising therapeutic targets, with dysfunction linked to cancers, CNS disorders, and metabolic diseases. Sygnature Discovery’s advanced assays, including binding, fluorescence-based screening, and solid-supported membrane electrophysiology (SSME), are designed to identify small molecule modulators and accelerate transporter-targeted drug discovery.

Custom assay development to accelerate your research

Sygnature Discovery’s target development group designs specialized assays precisely tailored to fit your unique discovery research needs. Our extensive assay capabilities enable fluorescence-based screening assays and state-of-the-art transporter electrophysiology to support identification of novel starting points for lead optimization. Working closely with your team, we customize assays to address project-specific challenges, delivering robust, reliable data that supports and enhances each stage of your drug discovery journey.

Access to the transporter assays you need

Amino Acid Transporters
SLC1A1 EAAT3
SLC1A2 EAAT2
SLC1A3 EAAT1

 

Sodium-Dependent Glucose Transporters
SLC5A1 SGLT1
SLC5A2 SGLT2
SLC5A4 SGLT3
SLC5A9 SGLT4
SLC5A10 SGLT5
SLC5A7 CHT
SLC5A11 SGLT6

 

Sodium-Calcium Exchangers
SLC8A1 NCX1

 

Peptide Transporters
SLC15A1 PepT1
SLC15A2 PepT2
SLC15A3 PHT2

 

Nucleoside Transporters
SLC28A1 CNT1

 

Metal Ion Transporters
SLC39A2 ZIP2

 

Heteromeric Amino Acid Transporters
SLC7A3 CAT3
SLC7A5 LAT1

 

Neurotransmitter Transporters
SLC6A2 NET-1
SLC6A3 DAT-1
SLC6A4 SERT
SLC6A1 GAT1
SLC6A11 GAT3
SLC6A9 GLYT1
SLC6A5 GLYT2
SLC6A19 B0AT1

 

Cation-Coupled Chloride Transporters
SLC12A1b NKCC2b
SLC12A2 NKCC1
SLC12A4 KCC1
SLC12A5a KCC2a
SLC12A5b KCC2b

 

Organic Cation and Anion Transporters
SLC22A2 OCT2

 

Proton-Coupled Amino Acid Transporters
SLC36A1 PAT1
SLC36A2 PAT2

 

Transporter Screening Services

icon representing cell line generation in drug discovery

Cell Line generation

membrane purification icon used in solute carrier (SLC) transporter research services

membrane purification

screening assays icon for high-throughput screening assay services

screening assays

customized cascade icon for tailored assay workflows

customized cascades

Leading Technologies for Rapid, Reliable Results

icon representing radiolabelled uptake assays for SLC transporter analysis, featuring a magnifying glass over a bar chart to symbolise sensitive measurement and quantification of substrate transport.

Radiolabeled uptake assays

Radiolabeled uptake assays offer a highly sensitive and reliable way to measure SLC transporter activity providing direct insight into transporter function. Our team applies proven protocols to support hit identification, compound profiling and functional characterization across a wide range of transporter targets.

Bar chart showing [14C]AMG uptake in SGLT2-expressing and control cells with and without inhibitor treatment, demonstrating significant transporter-specific uptake and inhibition.

Figure 1: Uptake of [14C]AMG in SGLT2-transfected HEK cells and control HEK cells in the presence and absence of the inhibitor phloridzin.

Icon representing fluorescence-based screening assays for SLC transporter drug discovery, featuring a stylized lightbulb to symbolise detection of fluorescent signals in high-throughput screening formats.

Fluorescence-Based Screening

Fluorescence-based screening assays offer fast, economical solutions to help identify novel modulators of SLC transporters. At Sygnature Discovery, our experienced team leverages high-throughput, 384- and 1536-well fluorescence-based screening platforms, state-of-the-art compound dispensing technologies and advanced analysis software, setting the standard for excellence by delivering rapid and precise hit identification solutions for your SLC transport discovery needs.

Inhibition curves showing the % activity of SERT and DAT transporters in a fluorescence-based assay following clomipramine treatment, demonstrating differential potency across targets.

Figure 2:  Clomipramine-mediated inhibition of SERT (SLC6A4) and DAT (SLC6A3) activity measured using a fluorescence-based assay. Data show concentration-dependent reduction in transporter activity, with SERT displaying a greater sensitivity to clomipramine inhibition. 

Icon representing electrophysiology studies for SLC transporter functional assays, featuring a waveform signal to symbolise high-sensitivity measurement of transporter activity in real time.

Electrophysiology Studies

Our solid-supported membrane electrophysiology technology provides precise, reliable assessment of transporter activity. The SURFE2R N1 and  SURFE2R 96SE systems enable flexible, high-sensitivity screening and characterization of compounds targeting electrogenic transporters.

The SURFE2R N1 is ideal for detailed mechanistic investigations and low-throughput hit validation, offering robust and precise signal detection with excellent temporal resolution. Complementing this, the SURFE2R 96SE supports higher-throughput workflows, enabling real-time screening and functional profiling across multiple conditions simultaneously.

Together, these systems deliver robust functional recordings within native membrane environments, offering unparalleled versatility and scalability for your transporter research.

SSM electrophysiology current traces showing EAAT3 transporter currents evoked by increasing concentration of L-glutamate, illustrating a clear dose-dependent response.

Figure 3: EAAT3-mediated transporter currents recorded using solid-supported membrane (SSM)-based electrophysiology following increasing concentration of L-glutamate. Traces demonstrate a dose-dependent increase in inward current amplitude, consistent with electrogenic substrate transport by EAAT3. 

icon of a hand selective a gear, symbolising control and precision in two-electrode voltage-clamp transporter assays.

Two-electrode voltage-clamp

Two-Electrode Voltage-Clamp (TEVC) enables sensitive, reproducible measurements of electrogenic transporter activity in Xenous laevis oocytes. The large size and low background activity of these cells make them ideal for challenging targets. TEVC provides an efficient and reliable way to assess responses to compounds and measure transporter function, supporting target validation, hit identification and lead profiling. 

Two-electrode voltage-clamp (TEVC) recordings from Xenopus laevis oocytes expressing SGLT1. Traces show current activation in response to increasing concentrations of Glucose, demonstrating a clear dose-dependent effect consistent with electrogenic substrate transport.

Figure 4: Example transmembrane current traces (nA) of an SGLT1 injected Xenopus oocyte and a water injected oocyte (negative control) using TEVC. Increasing glucose concentration induced a dose-dependent activation of nA in SGLT1-expressing ooctyes. No change was observed in water-injected oocytes. 

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Case Studies from SB Drug Discovery

Transporter Case Studies

Explore our transporter drug discovery case studies. Click on a title to view the full case study.

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