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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 24
Ion channels 5
Disease-based libraries 29
Epigenetic targets 6
Protein-Protein Interaction 2
Peptidomimetic 1
Nuclear Receptors 1
General Activities 127
Other 102



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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