GPCR Targeted Libraries
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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.




OTAVAchemicals offers 46 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 agonist general library 465 Ligand-based -
GPCR antagonist general library 5089 Ligand-based -
5-hydroxytryptamine agonist general library 199 Ligand-based -
5-hydroxytryptamine 1A agonist library - Ligand-based -
5-hydroxytryptamine 2 agonist library - Ligand-based -
5-hydroxytryptamine 3 agonist library - Ligand-based -
5-hydroxytryptamine antagonist general library 290 Ligand-based -
5-hydroxytryptamine 1A antagonist library 600 Ligand-based -
5-hydroxytryptamine receptor 1B antagonist library 560 Receptor-based read more
5-hydroxytryptamine 2C antagonist library - Ligand-based -
5-hydroxytryptamine 2D antagonist library - Ligand-based -
5-hydroxytryptamine 6 antagonist library 42 Ligand-based -
Acetylcholine muscarinic agonist library 10 Ligand-based -
Alpha adrenoreceptor agonist library 45 Ligand-based -
Cholecystokinin agonist library 12 Ligand-based -
Dopamine agonist library 29 Ligand-based -
Dopamine autoreceptor agonist library 181 Ligand-based -
GABA receptor agonist library 117 Ligand-based -
Melatonin agonist library 17 Ligand-based -
Acetylcholine muscarinic antagonist library 81 Ligand-based -
Acetylcholine M2 receptor antagonist library - Ligand-based -
Acetylcholine M3 receptor antagonist library - Ligand-based -
Adenosine receptor antagonist library 110 Ligand-based -
Alpha adrenoreceptor antagonist library 1045 Ligand-based -
Alpha 1 adrenoreceptor antagonist library - Ligand-based -
Alpha 1a adrenoreceptor antagonist library - Ligand-based -
Alpha adrenoreceptor agonist general library - Ligand-based -
Alpha 1 adrenoreceptor agonist library - Ligand-based -
Alpha 2 adrenoreceptor agonist library - Ligand-based -
Beta adrenoreceptor antagonist library 89 Ligand-based -
Dopamine antagonist general library 61 Ligand-based -
Dopamine D3 antagonist library - Ligand-based -
Dopamine D4 antagonist library - Ligand-based -
Dopamine D3 agonist library - Ligand-based -
Endothelin receptor antagonist general library 165 Ligand-based -
Endothelin A receptor antagonist library - Ligand-based -
Endothelin B receptor antagonist library - Ligand-based -
GABA receptor antagonist library 1133 Ligand-based -
GABAB agonist library 274 Ligand-based read more
GABAB antagonist library 346 Ligand-based read more
Glucagon receptor antagonist library 526 Ligand-based -
Glutamate receptor antagonist library 27 Ligand-based -
Histamine receptor antagonist library 590 Ligand-based -
Neuropeptide antagonist library 106 Ligand-based -
Prostaglandin antagonist library 665 Ligand-based -
Thromboxane antagonist library 133 Ligand-based -
Vasopressin 1 antagonist library 23 Ligand-based -
Histamine receptor targeted library 1295 Receptor-based read more
Sphingosine-1-phosphate receptor 1 (S1PR1) agonist library 667 Ligand-based read more
Sphingosine-1-phosphate receptor 1 (S1PR1) antagonist library 1215 Ligand-based read more


OTAVAchemicals Targeted Libraries Collection
Name Number
Kinases 69
Proteases 17
GPCRs 51
Ion channels 5
Disease-based libraries 74
Epigenetic targets 8
Protein-Protein Interaction 2
Peptidomimetic 2
Nuclear Receptors 12
Glycomimetic 1
RNA binding 1
SH2 binding 1
General Activities 128
Other 93



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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