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GPCR Targeted Libraries

GPCR focused librariesCurrent advances in functional screening methodologies, medicinal chemistry, and structure-based drug design have generated large increases in the number and diversity of GPCR drug targets. Furthermore, basic research advances have opened the way for still further exploitation of this target class. G protein-coupled receptors (GPCRs) are popular drug targets, accounting for about one-third of approved drugs and many hundreds of drugs currently in development.




Otava offers 25 GPCR Targeted Libraries designed with Ligand-based approach. These libraries are proposed for screening in GPCR-associated research and drug development projects.

  • the libraries contain drug-like compounds only
  • all the compounds are in stock
  • cherry picking is available


You can sort data by any column and use "Filter" option to search library's name:

Name Approach Details
GPCR Agonists Ligand-based -
5 Hydroxytryptamine agonist Ligand-based -
Acetylcholine muscarinic agonist Ligand-based -
Alpha adrenoreceptor agonist Ligand-based -
Cholecystokinin agonist Ligand-based -
Dopamine agonist Ligand-based -
Dopamine autoreceptor agonist Ligand-based -
GABA receptor agonist Ligand-based -
Melatonin agonist Ligand-based -
GPCR Antagonists Ligand-based -
5 Hydroxytryptamine antagonist Ligand-based -
Acetylcholine muscarinic antagonist Ligand-based -
Adenosine receptor antagonist Ligand-based -
Alpha adrenoreceptor antagonist Ligand-based -
Beta adrenoreceptor antagonist Ligand-based -
Dopamine antagonist Ligand-based -
Endothelin receptor antagonist Ligand-based -
GABA receptor antagonist Ligand-based -
Glucagon receptor antagonist Ligand-based -
Glutamate receptor antagonist Ligand-based -
Histamine antagonist Ligand-based -
Neuropeptide antagonist Ligand-based -
Prostaglandin antagonist Ligand-based -
Thromboxane antagonist Ligand-based -
Vasopressin 1 antagonist Ligand-based -
5-Hydroxytryptamine Receptor (5-HT1B) Antagonist Receptor-based read more
Histamine Receptor Antagonist Receptor-based read more


Otava's Target-Focused Libraries collection
Name Number
Kinases 67
Proteases 12
GPCRs 25
Ion channels 6
Disease-based libraries 29
Epigenetic targets 7
Protein-Protein Interaction 2
Peptidomimetic 1
Nuclear Receptors 2
Glycomimetic 1
RNA binding 1
General Activities 128
Other 104



The libraries (SDF, XLS, PDF format) are available on request. Feel free to contact us or use on-line form below to send an inquiry if you are interested to obtain these libraries or if you need more information.





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