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G-protein coupled receptors (GPCRs) are the largest family of cell surface receptors. They are responsible for transmitting information initiated by various signals (such as photons, hormones, neurotransmitters, etc) into the cell. As GPCRs regulate a vast variety of signaling pathways in organisms, they are connected to many metabolic, neurological, inflammatory, cardiovascular and immunological disorders. Due to this fact, GPCRs are very important pharmaceutical targets with a highly promising future.
GPCR-binding Ligands Library contains 1337 small ligands, including molecules with inhibitory action against GPCR targets, agonists, and allosteric modulators.
Related terms: 5-hydroxytryptamine receptor, adrenoceptor, dopamine, adenosine, acetylcholine, muscarinic, histamine, metabotropic glutamate receptor, cannabinoid receptor, class A orphans
Action of GPCR mechanism (Created by BioRender.com)
CVN424, potent GPR6, inhibitor EBC-13129
Difelikefalin, selective KOR agonist, approved in 2021 (analgetic) EBC-58081
ADX-47273 is a mGlu 5 receptor allosteric modulator EBC-13154
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NoteAll the compounds with solubility below 10 mM are shipped as 2 mM solutions.
5-Hydroxytryptamine receptors
287
287
Number of compounds
287
Adrenoceptors
217
217
Number of compounds
217
Dopamine receptors
215
215
Number of compounds
215
Adenosine receptors
146
146
Number of compounds
146
Acetylcholine receptors (muscarinic)
98
98
Number of compounds
98
Histamine receptors
86
86
Number of compounds
86
Metabotropic glutamate receptors
73
73
Number of compounds
73
Cannabinoid receptors
38
38
Number of compounds
38
Class A Orphans
26
26
Number of compounds
26
Chemokine receptors
23
23
Number of compounds
23
Melatonin receptors
22
22
Number of compounds
22
Free fatty acid receptors
22
22
Number of compounds
22
Opioid receptors
21
21
Number of compounds
21
Trace amine receptor
20
20
Number of compounds
20
Prostanoid receptors
17
17
Number of compounds
17
Taste 1 receptors
13
13
Number of compounds
13
Angiotensin receptors
12
12
Number of compounds
12
Somatostatin receptors
9
9
Number of compounds
9
Lysophospholipid (S1P) receptors
8
8
Number of compounds
8
Endothelin receptors
8
8
Number of compounds
8
GABAB receptors
6
6
Number of compounds
6
Glycoprotein hormone receptors
5
5
Number of compounds
5
Neuropeptide FF/neuropeptide AF receptors
5
5
Number of compounds
5
Bile acid receptor
5
5
Number of compounds
5
Tachykinin receptors
5
5
Number of compounds
5
Class C Orphans
3
3
Number of compounds
3
Melanocortin receptors
3
3
Number of compounds
3
Cholecystokinin receptors
3
3
Number of compounds
3
Class Frizzled GPCRs
3
3
Number of compounds
3
Formylpeptide receptors
3
3
Number of compounds
3
Neuropeptide Y receptors
3
3
Number of compounds
3
Taste 2 receptors
3
3
Number of compounds
3
Vasopressin and oxytocin receptors
3
3
Number of compounds
3
P2Y receptors
2
2
Number of compounds
2
Neurotensin receptors
2
2
Number of compounds
2
Proteinase-activated receptors
2
2
Number of compounds
2
Calcium-sensing receptor
2
2
Number of compounds
2
Leukotriene receptors
2
2
Number of compounds
2
Lysophospholipid (LPA) receptors
2
2
Number of compounds
2
Platelet-activating factor receptor
2
2
Number of compounds
2
VIP and PACAP receptors
2
2
Number of compounds
2
Urotensin receptor
1
1
Number of compounds
1
Apelin receptor
1
1
Number of compounds
1
Corticotropin-releasing factor receptors
1
1
Number of compounds
1
Kisspeptin receptor
1
1
Number of compounds
1
Melanin-concentrating hormone receptors
1
1
Number of compounds
1
Motilin receptor
1
1
Number of compounds
1
Opsin receptors
1
1
Number of compounds
1
EBCL-0016