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Transporters or membrane transport proteins assist in the movement of ions, small molecules, lipids, and macromolecules across biological membranes. Membrane transporters can be classified as ABC transporters (primary active transporters), P-type ATPases (transport enzymes that use the energy of hydrolysis to move ions across membranes), and the solute carrier family of transporters (SLCs, which act by secondary active transport and facilitative diffusion). Some diseases involve defects in the work of membrane transporters making them an important group of drug targets. For instance, ABC transporters play an essential role in the study of multi-drug resistance in cancer cells because of their ability to remove chemotherapeutic agents from the cell faster than they can cross the membrane. Inhibitors of the SLC family of transporters can be efficient in the treatment of many disorders, particularly depression (SERT), epilepsy (GABA transporter), and Parkinson's disease (DAT).
Transporter Ligands Library is composed of 799 small molecules.
Related terms: SERT, ABCG2, ABCB1, NET, ferroportin, DAT, organic anion transporter, organic cation transporter, ATP-binding cassette, CFTR/MRP, glucose transporter
Action of kinase transporter proteins(Created by BioRender.com)
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Highlights
Paroxetine is a serotinin reuptake inhibitor
VU046327 is a solute carrier family 12 member 5 inhibitor
ML-352 is a choline transporter 1 inhibitor
AR-C155858 is a MCT1 and MCT2 inhibitor
Product Features
A set of 799 ion transporter molecules with sub-10 micromolar activity coefficient values for HTS/HCS programs.
The library is composed of ligands that target all major pharmaceutically relevant ion channel targets.
The Transporter Ligands Library covers novel promising preclinical lead compounds, clinical candidates and approved drugs.
Calculated structural diversity of the collection: 0.88.
Comprehensive documentation with structures, trivial names, synonyms, activity coefficients values, types of action on target and references to original literature.
NMR and LCMS validated purity.
All the compounds are available in stock for hit follow-up.
The library is continuously updated.
Product Details
Format: 10 - 100 µL of 10 mM DMSO stock solutions; dry powders (1 mg);
Container: 384-well microplates;
Storage: - 18 °C;
Shipping: Dry ice.
Utility
High throughput screening (HTS);
High content screening (HCS);
Cherry picking.
