GPCR 结合配体
G-protein coupled receptors (GPCRs) are the largest family of cell surface receptors. They are responsible for transmitting information initiated by various signals (such as photons, hormones, neurotransmitters, etc) into the cell. As GPCRs regulate a vast variety of signaling pathways in organisms, they are connected to many metabolic, neurological, inflammatory, cardiovascular and immunological disorders. Due to this fact, GPCRs are very important pharmaceutical targets with a highly promising future.
GPCR-binding Ligands Library contains 1366 small ligands, including molecules with inhibitory action against GPCR targets, agonists, and allosteric modulators.
Related terms: 5-hydroxytryptamine receptor, adrenoceptor, dopamine, adenosine, acetylcholine, muscarinic, histamine, metabotropic glutamate receptor, cannabinoid receptor, class A orphans
Action of GPCR mechanism (Created by BioRender.com)
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Highlights
CVN424, potent GPR6, inhibitor
Difelikefalin, selective KOR agonist, approved in 2021 (analgetic)
ADX-47273 is a mGlu5 receptor allosteric modulator
Product Features
A set of 1366 GPCR-binding molecules with sub-10 micromolar activity coefficient values for HTS/HCS programs.
The library is composed of ligands that target all major pharmaceutically relevant GPCR targets.
GPCR Binding 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 coefficient 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.
