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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 Number of compounds Approach Details
GPCR Agonists 465 Ligand-based
5 Hydroxytryptamine agonist 54 Ligand-based
Acetylcholine muscarinic agonist 10 Ligand-based
Alpha adrenoreceptor agonist 45 Ligand-based
Cholecystokinin agonist 12 Ligand-based
Dopamine agonist 29 Ligand-based
Dopamine autoreceptor agonist 181 Ligand-based
GABA receptor agonist 117 Ligand-based
Melatonin agonist 17 Ligand-based
GPCR Antagonists 5089 Ligand-based
5 Hydroxytryptamine antagonist 347 Ligand-based
Acetylcholine muscarinic antagonist 81 Ligand-based
Adenosine receptor antagonist 110 Ligand-based
Alpha adrenoreceptor antagonist 1045 Ligand-based
Beta adrenoreceptor antagonist 89 Ligand-based
Dopamine antagonist 61 Ligand-based
Endothelin receptor antagonist 165 Ligand-based
GABA receptor antagonist 1133 Ligand-based
Glucagon receptor antagonist 526 Ligand-based
Glutamate receptor antagonist 15 Ligand-based
Histamine antagonist 590 Ligand-based
Neuropeptide antagonist 106 Ligand-based
Prostaglandin antagonist 665 Ligand-based
Thromboxane antagonist 133 Ligand-based
Vasopressin 1 antagonist 23 Ligand-based
5-Hydroxytryptamine Receptor (5-HT1B) Antagonist 1836 Receptor-based read more
Histamine Receptor Antagonist 1295 Receptor-based read more


Otava's Target-Focused Libraries collection
Name Number
Kinases 67
Proteases 12
GPCRs 24
Ion channels 3
Disease-based libraries 29
Epigenetic targets 6
Protein-Protein Interaction 2
Peptidomimetic 1
Nuclear Receptors 1
General Activities 127
Other 101



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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