膜受体配体
Membranes are the boundaries of cells that divide the inside and the outside of the cell. These barriers prevent inner molecules from leaking out of the cell and unwanted molecules from diffusing in. For transport purposes, they contain specific transport systems (membrane receptors) that allow the cell to accept concrete molecules and remove unwanted ones. The small molecules can be cytokines, growth factors, hormones, nutrients, neurotransmitters, and many others. Membrane receptors are differentiated into three various classes: the G-protein coupled receptors, ion channel linked receptors, and enzyme-linked receptors. They represent important molecular targets for medicinal chemistry research.
Membrane Receptor Ligands Library contains 1251 small ligands, some representative molecules are given below: Risperidone, 5-HT2 receptor blocker, D2 receptor antagonist; VU0071063, ATP dependent potassium channel activator; CU-T12-9, TLR1/2 antagonist; LY354740, mGlu2/3 receptor agonist.
Related terms: 5-Hydroxytryptamine receptor, adrenoceptor, adenosine, dopamine, acetylcholine, histamine, metabotropic glutamate, cannabinoid receptor
A:the G-protein coupled receptor; B: ion channel linked receptor; C:enzyme-linked receptor(Created by BioRender.com)
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Highlights
Risperidone, 5-HT2 receptor blocker, D2 receptor antagonist. Target class: G protein-coupled receptors
VU0071063, ATP dependent potassium channel activator. Target class: ion channel linked receptors
CU-T12-9, TLR1/2 antagonist. Target class: enzyme-linked receptors
LY354740, mGlu2/3 receptor agonist. Target class: G protein-coupled receptors
Product Features
A set of 1251 membrane receptors relevant molecules with sub-10 micromolar activity coefficient values for HTS/HCS programs.
The library is composed of ligands that target all major pharmaceutically relevant membrane receptors targets.
Membrane Receptor Ligands Library covers novel promising preclinical lead compounds, clinical candidates and approved drugs.
Calculated structural diversity of the collection: 0.86.
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.
