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> Products > ION CHANNEL LIBRARIES

ION CHANNEL LIBRARIES

 

Potassium Channel KcsA-Fab complex in Sodium Chloride / Crystal Structure Of Human Potassium Channel Kv Beta-subunit / X-ray structure of a voltage-dependent potassium channel in complex with an Fab

 

Ion channels are pore-forming proteins present in the membrane of all living cells. They control the flow of charged atoms into and out of the cells. In humans, they are involved in important physiological functions like nervous and muscular cell excitability, hormonal secretion, cell multiplication and apoptosis. Thus, they are also involved in many diseases.

The pore of the channel is surrounded by several identical subunits (usually four) with up to six transmembrane helices each, and external conditions (the gating) make the subunits move to open or close the passage. This superfamily of potential targets has been classified in two main ways: according to the gating (voltage gated, extracellular ligand gated, intracellular ligand gated, other gatings) and according to the type of ion (Cl-, Na+, K+, H+, unspecific).

Interest in ion channels peaked in 1990 with eight NCEs approved on the US market, mainly for hypertension and epilepsy. Since then, progresses in structure crystallisation and determination allowed to better understand the processes involved and to identify the active sites where small molecules could interact.

IMIDAZOLE ACETAMIDE LIBRARY
IMIDAZOLE ACETAMIDE LIBRARY

• highly diverse exploration of imidazole-N-acetamides
• condensed imidazole derivatives with reasonable molecular weight
• privileged structures for ion channels, peptidomimetic central cores, enzyme inhibitors, peptide GPCRs and nuclear receptor modulation
• drug-like structures of special interest for CNS, anxiolytic, analgesic, immunoregulatory leads with oral activity

IMIDAZOLE LIBRARY
IMIDAZOLE LIBRARY

• highly diverse exploration of imidazoles, with emphasis on diaryl and triaryl compounds
• condensed imidazole derivatives with reasonable molecular weight
• large array of potential targets: ion channels (GABA subtypes), enzymes, amine and peptide GPCRs
• library based on a new connecting chemistry

QUINOLINE CARBOXAMIDE LIBRARY
QUINOLINE CARBOXAMIDE LIBRARY

• first-line and diverse library exploring the quinoline carboxamides
• wide pharmacological spectrum: peptide and amine GPCRs, protein-protein interactions, ion channels and enzyme inhibitors
• many different therapeutic fields including cancer, analgesia and CNS, immunology, cardiovascular, gastrointestinal and pulmonary
• oral activities reported for similar structures

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