We combine our best-in-class products, advanced instrumentation, and extensive expertise to perform assays that provide reliable insights for your drug discovery program. Our collection of cell-based assays can uncover modulators of a variety of disease-relevant targets including ion channels, transporters, and GPCRs. We also offer fluorescence-based cardiotoxicity screening for relevant ion channel targets (e.g. hERG inhibition assays) and cytotoxicity assays. [Contact us] today to learn more about what we can do for you.
Ion channels are essential membrane-bound proteins that control the movement of ions, such as sodium, potassium, calcium, and chloride, across cell membranes and are responsible for the regulation of numerous fundamental physiological processes. In pharmacology, ion channels serve as targets for a wide range of medical conditions, including cardiovascular disorders, neurological conditions, and pain management. Moreover, mutations that affect ion channel activity can lead to channelopathies like long QT syndrome, epilepsy, or cystic fibrosis. ION’s goal is to help address these disorders by enabling the discovery of new modulators that restore proper ion channel function. Approximately 15% of approved drugs on the market today modulate ion channels, establishing this large family of proteins (>500) as major drug targets.
Using fluorescence-based ion channel assays, we can measure the activity of a multitude of ligand-gated and voltage-gated ion channels that are important targets for cardiotoxicity screening and many other pathologies. ION’s ion channel assay catalog includes:
Invented for potassium channels, but applicable to so much more. While predominantly used as a surrogate ion for potassium channel research, thallium can also be used to discover new modulators of sodium channels, non-selective cation channels, monovalent cation transporters, and Gi/o GPCRs.
Calcium ions regulate numerous cellular processes and act as secondary messengers in a number of signaling pathways (i.e. GPCRs). The flow of calcium into and out of the cell is controlled by calcium channels, and changes in intracellular calcium concentrations can be detected using fluorescent calcium indicators such as Fluo-4 and Fura-2. We have a large collection of indicators and kits to run calcium mobilization assays.
G protein-coupled receptors (GPCRs) are responsible for transmitting signals from the extracellular environment to the inside of cells, and they represent one of the most important and successful drug target families in pharmacology. GPCRs are involved in a wide range of functions, including neurotransmission, hormone regulation, immune responses, cardiovascular control, and sensory perception. By targeting GPCRs, pharmaceutical interventions can effectively treat conditions such as hypertension, asthma, depression, allergies, and more. Approximately 30% of clinically available drugs modulate GPCRs.
There are four alpha subunits of G-proteins, Gαs, Gαq, Gαi, and Gα12, that are identified based on downstream effectors. ION’s calcium assay kits can be used to discover agonists of Gq GPCRs and other GPCRs coupled to the promiscuous Gα16 G protein. Thallium flux assays can be used to measure activation of Gi/o GPCRs such as metabotropic glutamate receptors, serotonin receptors, and more.
Ion transporters are essential players in neurotransmission and help cells maintain their resting membrane potential. Efflux transporters, like P-glycoprotein, pump drugs out of cells and lead to multidrug resistance. The study and manipulation of transporters hold significant potential for advancing drug development, understanding disease mechanisms, and improving patient outcomes. ION has a collection of assays to assess MDR transporter activity, sodium-dependent SLC transporter activity, and the activity of a variety of other ion transporters.
After identifying a new drug candidate, cytotoxicity assays provide important data for early safety screening, help prioritize hits-to-leads conversion, and guide lead optimization studies.
