Current 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.

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

Name	Number of compounds	Approach	Available on-line
GPCR Agonists	465	Ligand-based	search on-line
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	search on-line
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	-

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