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EBCL-0016

GPCR-binding Ligands

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 3005 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

Library image

Action of GPCR mechanism (Created by BioRender.com)

Preplated options

Dry powder/solution (DMSO)Dry powder
Number of compounds3005
Comment
Dry powder/solution (DMSO)DMSO
Number of compounds2943
Comment

Highlights

Molecule highlight
EBC-13129CAS: 2254706-21-1

CVN424, potent GPR6, inhibitor EBC-13129

Molecule highlight
EBC-58081CAS: 1024828-77-0

Difelikefalin, selective KOR agonist, approved in 2021 (analgetic) EBC-58081

Molecule highlight
EBC-13154CAS: 851881-60-2

ADX-47273 is a mGlu 5 receptor allosteric modulator EBC-13154

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Disclaimer

All our products are for research purpose only. Any personal or non-scientific use is strictly prohibited.

Note

All the compounds with solubility below 10 mM are shipped as 2 mM solutions.

Product Features

  • A set of 3005 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.