Target family: Metabotropic glutamate receptors (type: gpcr)
Target: mGlu<sub>5</sub> receptor

Ligand: (1S,3R)-ACPD (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.7 pIC50
Reference (Journal): Characterization of [(3)H]Quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections.
Published in: J Neurochem

Ligand: 3,3'-difluorobenzaldazine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5.
Published in: Mol Pharmacol

Ligand: 3,3'-difluorobenzaldazine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain.
Published in: J Pharmacol Exp Ther

Ligand: 3,5-DHPG (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 5.4 pIC50
Reference (Journal): Characterization of [(3)H]Quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections.
Published in: J Neurochem

Ligand: 5-MPEP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Neutral
Ligand approved: no
Median affinity: 6.4 pKi
Reference (Journal): A close structural analog of 2-methyl-6-(phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators.
Published in: Mol Pharmacol

Ligand: 5PAM523 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 5.7 pKi
Reference (Journal): Mechanism based neurotoxicity of mGlu5 positive allosteric modulators--development challenges for a promising novel antipsychotic target.
Published in: Neuropharmacology

Ligand: 5PAM523 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.51 pEC50
Reference (Journal): Mechanism based neurotoxicity of mGlu5 positive allosteric modulators--development challenges for a promising novel antipsychotic target.
Published in: Neuropharmacology

Ligand: 5PAM523 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.7 pEC50
Reference (Journal): Mechanism based neurotoxicity of mGlu5 positive allosteric modulators--development challenges for a promising novel antipsychotic target.
Published in: Neuropharmacology

Ligand: ACDPP (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.9 pIC50
Reference (Journal): Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: ADX-47273 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.5 pIC50
Reference (Journal): <i>In vitro</i> pharmacological characterisation of selective mGluR5 positive allosteric modulators.
Published in: Neuropharmacology

Ligand: ADX-47273 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 5.44 pKi
Reference (Journal): In vitro characterisation of the novel positive allosteric modulators of the mGlu₅ receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat.
Published in: Neuropharmacology

Ligand: ADX-47273 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.8 pEC50
Reference (Journal): In vitro characterisation of the novel positive allosteric modulators of the mGlu₅ receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat.
Published in: Neuropharmacology

Ligand: ADX-47273 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.26 pEC50
Reference (Journal): In vitro characterisation of the novel positive allosteric modulators of the mGlu₅ receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat.
Published in: Neuropharmacology

Ligand: alloswitch-1 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: yes
Median affinity: 8.069999694824219 pIC50
Reference (Journal): An allosteric modulator to control endogenous G protein-coupled receptors with light.
Published in: Nat Chem Biol

Ligand: AZ12216052 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 5.380000114440918 pKB
Reference (Journal): &quot;Selective&quot; Class C G Protein-Coupled Receptor Modulators Are Neutral or Biased mGlu<sub>5</sub> Allosteric Ligands.
Published in: Mol Pharmacol

Ligand: AZD6538 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.55 pKi
Reference (Journal): Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development.
Published in: Bioorg Med Chem Lett

Ligand: AZD6538 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.87 pIC50
Reference (Journal): Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development.
Published in: Bioorg Med Chem Lett

Ligand: AZD9272 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.12 pIC50
Reference (Journal): Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development.
Published in: Bioorg Med Chem Lett

Ligand: AZD9272 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.42 pKi
Reference (Journal): Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development.
Published in: Bioorg Med Chem Lett

Ligand: basimglurant (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 7.440000057220459 pKi
Reference (Journal): Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases.
Published in: J Med Chem

Ligand: BOMA (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.5 pKi
Reference (Journal): Discovery of novel modulators of metabotropic glutamate receptor subtype-5.
Published in: Bioorg Med Chem

Ligand: Br-5MPEPy (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 6.52 pKi
Reference (Journal): A close structural analog of 2-methyl-6-(phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators.
Published in: Mol Pharmacol

Ligand: CDPPB (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.
Published in: J Med Chem

Ligand: CDPPB (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.7 pEC50
Reference (Journal): Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.
Published in: J Med Chem

Ligand: CDPPB (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models.
Published in: J Pharmacol Exp Ther

Ligand: CGP7930 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 4.78000020980835 pKB
Reference (Journal): &quot;Selective&quot; Class C G Protein-Coupled Receptor Modulators Are Neutral or Biased mGlu<sub>5</sub> Allosteric Ligands.
Published in: Mol Pharmacol

Ligand: CHPG (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 3.4000000953674316 pIC50
Reference (Journal): Characterization of [(3)H]Quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections.
Published in: J Neurochem

Ligand: cinacalcet (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: EMA & FDA (2004)
Primary target: no
Median affinity: 4.349999904632568 pKi
Reference (Journal): &quot;Selective&quot; Class C G Protein-Coupled Receptor Modulators Are Neutral or Biased mGlu<sub>5</sub> Allosteric Ligands.
Published in: Mol Pharmacol

Ligand: compound 10 [PMID: 15482906] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.17 pIC50
Reference (Journal): 2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist.
Published in: Bioorg Med Chem Lett

Ligand: compound 10 [PMID: 15482906] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.92 pKi
Reference (Journal): 2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist.
Published in: Bioorg Med Chem Lett

Ligand: compound 10 [PMID: 15482908] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.72 pKi
Reference (Journal): Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity.
Published in: Bioorg Med Chem Lett

Ligand: compound 10 [PMID: 15482908] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.11 pIC50
Reference (Journal): Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity.
Published in: Bioorg Med Chem Lett

Ligand: compound 11a [PMID: 14697765] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.4 pIC50
Reference (Journal): Discovery of novel modulators of metabotropic glutamate receptor subtype-5.
Published in: Bioorg Med Chem

Ligand: compound 11a [PMID: 14697765] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 6.8 pKi
Reference (Journal): Discovery of novel modulators of metabotropic glutamate receptor subtype-5.
Published in: Bioorg Med Chem

Ligand: compound 13 [PMID: 15686941] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.55 pIC50
Reference (Journal): Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: compound 16a [PMID: 14697765] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.04 pKi
Reference (Journal): Discovery of novel modulators of metabotropic glutamate receptor subtype-5.
Published in: Bioorg Med Chem

Ligand: compound 16a [PMID: 14697765] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.66 pIC50
Reference (Journal): Discovery of novel modulators of metabotropic glutamate receptor subtype-5.
Published in: Bioorg Med Chem

Ligand: compound 16m [PMID: 19931453] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.49 pIC50
Reference (Journal): Piperidyl amides as novel, potent and orally active mGlu5 receptor antagonists with anxiolytic-like activity.
Published in: Bioorg Med Chem Lett

Ligand: compound 16m [PMID: 19931453] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.42 pKi
Reference (Journal): Piperidyl amides as novel, potent and orally active mGlu5 receptor antagonists with anxiolytic-like activity.
Published in: Bioorg Med Chem Lett

Ligand: compound 18 [PMID: 17723296] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 9.14 pIC50
Reference (Journal): Synthesis and SAR of 2-aryl pyrido[2,3-d]pyrimidines as potent mGlu5 receptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: compound 18 [PMID: 21927650] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 6.32 pKi
Reference (Journal): (3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu(5): Discovery of a new tool compound with activity in the OSS mouse model of addiction.
Published in: ACS Chem Neurosci

Ligand: compound 18 [PMID: 21927650] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.21 pIC50
Reference (Journal): (3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu(5): Discovery of a new tool compound with activity in the OSS mouse model of addiction.
Published in: ACS Chem Neurosci

Ligand: compound 20 [PMID: 16439120] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 9 pKi
Reference (Journal): Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: compound 23 [PMID: 17590335] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.66 pKi
Reference (Journal): Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Published in: Bioorg Med Chem Lett

Ligand: compound 23 [PMID: 17590335] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 9.1 pIC50
Reference (Journal): Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Published in: Bioorg Med Chem Lett

Ligand: compound 24d [PMID: 23357634] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.64 pIC50
Reference (Journal): Discovery and structure-activity relationship of 1,3-cyclohexyl amide derivatives as novel mGluR5 negative allosteric modulators.
Published in: Bioorg Med Chem Lett

Ligand: compound 24d [PMID: 23357634] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.52 pKi
Reference (Journal): Discovery and structure-activity relationship of 1,3-cyclohexyl amide derivatives as novel mGluR5 negative allosteric modulators.
Published in: Bioorg Med Chem Lett

Ligand: compound 24 [PMID: 23374867] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.72 pIC50
Reference (Journal): Discovery of (1R,2R)-N-(4-(6-isopropylpyridin-2-yl)-3-(2-methyl-2H-indazol-5-yl)isothiazol-5-yl)-2-methylcyclopropanecarboxamide, a potent and orally efficacious mGlu5 receptor negative allosteric modulator.
Published in: Bioorg Med Chem Lett

Ligand: compound 26 [PMID: 16439120] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8 pKi
Reference (Journal): Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: compound 27 [PMID: 20598884] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.35 pIC50
Reference (Journal): 3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats.
Published in: Bioorg Med Chem Lett

Ligand: compound 27 [PMID: 20598884] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 6.69 pKi
Reference (Journal): 3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats.
Published in: Bioorg Med Chem Lett

Ligand: compound 29b [PMID: 20809633] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.77 pKi
Reference (Journal): Design, synthesis, and structure-activity relationships of novel bicyclic azole-amines as negative allosteric modulators of metabotropic glutamate receptor 5.
Published in: J Med Chem

Ligand: compound 29b [PMID: 20809633] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.8 pIC50
Reference (Journal): Design, synthesis, and structure-activity relationships of novel bicyclic azole-amines as negative allosteric modulators of metabotropic glutamate receptor 5.
Published in: J Med Chem

Ligand: compound 30 [PMID: 21757343] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.92 pIC50
Reference (Journal): 6-Aryl-3-pyrrolidinylpyridines as mGlu5 receptor negative allosteric modulators.
Published in: Bioorg Med Chem Lett

Ligand: compound 30 [PMID: 21757343] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.92 pKi
Reference (Journal): 6-Aryl-3-pyrrolidinylpyridines as mGlu5 receptor negative allosteric modulators.
Published in: Bioorg Med Chem Lett

Ligand: compound 30 [PMID: 21757343] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.77 pIC50
Reference (Journal): 6-Aryl-3-pyrrolidinylpyridines as mGlu5 receptor negative allosteric modulators.
Published in: Bioorg Med Chem Lett

Ligand: compound 36 [PMID: 17936624] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.29 pIC50
Reference (Journal): Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: compound 41 [PMID: 23434029] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.89 pEC50
Reference (Journal): Discovery of biological evaluation of pyrazole/imidazole amides as mGlu5 receptor negative allosteric modulators.
Published in: Bioorg Med Chem Lett

Ligand: compound 42 [PMID: 17189691] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.22 pIC50
Reference (Journal): Rational design, synthesis, and structure-activity relationship of benzoxazolones: new potent mglu5 receptor antagonists based on the fenobam structure.
Published in: Bioorg Med Chem Lett

Ligand: compound 42 [PMID: 17189691] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.02 pKi
Reference (Journal): Rational design, synthesis, and structure-activity relationship of benzoxazolones: new potent mglu5 receptor antagonists based on the fenobam structure.
Published in: Bioorg Med Chem Lett

Ligand: compound 47 [PMID: 21295468] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.3 pEC50
Reference (Journal): Discovery of novel positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5).
Published in: Bioorg Med Chem Lett

Ligand: compound 53 [PMID: 23434029] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.4 pIC50
Reference (Journal): Discovery of biological evaluation of pyrazole/imidazole amides as mGlu5 receptor negative allosteric modulators.
Published in: Bioorg Med Chem Lett

Ligand: compound 8 [PMID: 15482908] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.41 pIC50
Reference (Journal): Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity.
Published in: Bioorg Med Chem Lett

Ligand: compound 8 [PMID: 15482908] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.85 pKi
Reference (Journal): Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity.
Published in: Bioorg Med Chem Lett

Ligand: compound 8 [PMID: 20598884] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.23 pIC50
Reference (Journal): 3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats.
Published in: Bioorg Med Chem Lett

Ligand: compound 8 [PMID: 20598884] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 6.99 pKi
Reference (Journal): 3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats.
Published in: Bioorg Med Chem Lett

Ligand: CPCCOEt (Synthetic organic)
Interaction type: Allosteric modulator
Action: Neutral
Ligand approved: no
Primary target: no
Median affinity: 4.900000095367432 pKB
Reference (Journal): &quot;Selective&quot; Class C G Protein-Coupled Receptor Modulators Are Neutral or Biased mGlu<sub>5</sub> Allosteric Ligands.
Published in: Mol Pharmacol

Ligand: CPPHA (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pIC50
Reference (Journal): A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain.
Published in: J Pharmacol Exp Ther

Ligand: CPPZ (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 5.51 pKi
Reference (Journal): Preclinical profile of a novel metabotropic glutamate receptor 5 positive allosteric modulator.
Published in: Eur J Pharmacol

Ligand: CPPZ (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.3 pEC50
Reference (Journal): Preclinical profile of a novel metabotropic glutamate receptor 5 positive allosteric modulator.
Published in: Eur J Pharmacol

Ligand: CTEP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases.
Published in: J Med Chem

Ligand: CTEP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.9 pKi
Reference (Journal): CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor.
Published in: J Pharmacol Exp Ther

Ligand: CTEP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor.
Published in: J Pharmacol Exp Ther

Ligand: CTEP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor.
Published in: J Pharmacol Exp Ther

Ligand: CTEP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.02 pKi
Reference (Journal): CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor.
Published in: J Pharmacol Exp Ther

Ligand: DCG-IV (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.7 pIC50
Reference (Journal): Characterization of [(3)H]Quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections.
Published in: J Neurochem

Ligand: dipraglurant (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.7 pIC50
Reference (Journal): Discovery of biological evaluation of pyrazole/imidazole amides as mGlu5 receptor negative allosteric modulators.
Published in: Bioorg Med Chem Lett

Ligand: fenobam (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.2 pIC50
Reference (Journal): Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity.
Published in: J Pharmacol Exp Ther

Ligand: GRN-529 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.6 pIC50
Reference (Journal): Negative allosteric modulation of metabotropic glutamate receptor 5 results in broad spectrum activity relevant to treatment resistant depression.
Published in: Neuropharmacology

Ligand: GRN-529 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.27 pKi
Reference (Journal): Negative allosteric modulation of metabotropic glutamate receptor 5 results in broad spectrum activity relevant to treatment resistant depression.
Published in: Neuropharmacology

Ligand: GS39783 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Neutral
Ligand approved: no
Primary target: no
Median affinity: 6.269999980926514 pKB
Reference (Journal): &quot;Selective&quot; Class C G Protein-Coupled Receptor Modulators Are Neutral or Biased mGlu<sub>5</sub> Allosteric Ligands.
Published in: Mol Pharmacol

Ligand: GSK2210875 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.4 pIC50
Reference (Journal): The identification of novel orally active mGluR5 antagonist GSK2210875.
Published in: Bioorg Med Chem Lett

Ligand: ibotenic acid (Natural product)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.7 pIC50
Reference (Journal): Characterization of [(3)H]Quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections.
Published in: J Neurochem

Ligand: (S)-3HPG (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 5 pIC50
Reference (Journal): Characterization of [(3)H]Quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections.
Published in: J Neurochem

Ligand: (S)-4C3HPG (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.6 pIC50
Reference (Journal): Characterization of [(3)H]Quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections.
Published in: J Neurochem

Ligand: L-CCG-I (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.8 pIC50
Reference (Journal): Characterization of [(3)H]Quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections.
Published in: J Neurochem

Ligand: L-glutamic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.1 pIC50
Reference (Journal): Characterization of [(3)H]Quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections.
Published in: J Neurochem

Ligand: L-glutamic acid (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): New perspectives for the development of selective metabotropic glutamate receptor ligands.
Published in: Eur J Pharmacol

Ligand: LSN2463359 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.42 pKi
Reference (Journal): In vitro characterisation of the novel positive allosteric modulators of the mGlu₅ receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat.
Published in: Neuropharmacology

Ligand: LSN2463359 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.62 pEC50
Reference (Journal): In vitro characterisation of the novel positive allosteric modulators of the mGlu₅ receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat.
Published in: Neuropharmacology

Ligand: LSN2463359 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.48 pEC50
Reference (Journal): In vitro characterisation of the novel positive allosteric modulators of the mGlu₅ receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat.
Published in: Neuropharmacology

Ligand: LSN2814617 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 5.87 pKi
Reference (Journal): In vitro characterisation of the novel positive allosteric modulators of the mGlu₅ receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat.
Published in: Neuropharmacology

Ligand: LSN2814617 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.28 pEC50
Reference (Journal): In vitro characterisation of the novel positive allosteric modulators of the mGlu₅ receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat.
Published in: Neuropharmacology

Ligand: LSN2814617 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.03 pEC50
Reference (Journal): In vitro characterisation of the novel positive allosteric modulators of the mGlu₅ receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat.
Published in: Neuropharmacology

Ligand: LY341495 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.1 pIC50
Reference (Journal): LY341495 is a nanomolar potent and selective antagonist of group II metabotropic glutamate receptors.
Published in: Neuropharmacology

Ligand: M-5MPEP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 6.52 pKi
Reference (Journal): A close structural analog of 2-methyl-6-(phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators.
Published in: Mol Pharmacol

Ligand: (+)-MCPG (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 3.7 pIC50
Reference (Journal): Characterization of [(3)H]Quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections.
Published in: J Neurochem

Ligand: methoxymethyl-MTEP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 7.5 pIC50
Reference (Journal): [3H]Methoxymethyl-3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine binding to metabotropic glutamate receptor subtype 5 in rodent brain: in vitro and in vivo characterization.
Published in: J Pharmacol Exp Ther

Ligand: methoxy-MPEP (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.4399995803833 pIC50
Reference (Journal): [(3)H]-M-MPEP, a potent, subtype-selective radioligand for the metabotropic glutamate receptor subtype 5.
Published in: Bioorg Med Chem Lett

Ligand: MPEP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): [(3)H]-M-MPEP, a potent, subtype-selective radioligand for the metabotropic glutamate receptor subtype 5.
Published in: Bioorg Med Chem Lett

Ligand: MPEP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist.
Published in: Neuropharmacology

Ligand: MTEB (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.7 pIC50
Reference (Journal): Discovery of novel modulators of metabotropic glutamate receptor subtype-5.
Published in: Bioorg Med Chem

Ligand: MTEP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): Reduced stress-induced hyperthermia in mGluR5 knockout mice.
Published in: Eur J Neurosci

Ligand: NCFP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.43 pEC50
Reference (Journal): A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signaling.
Published in: Mol Pharmacol

Ligand: NCFP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.67 pEC50
Reference (Journal): A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signaling.
Published in: Mol Pharmacol

Ligand: NCFP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.01 pEC50
Reference (Journal): A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signaling.
Published in: Mol Pharmacol

Ligand: NPS 2143 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 5.079999923706055 pKB
Reference (Journal): &quot;Selective&quot; Class C G Protein-Coupled Receptor Modulators Are Neutral or Biased mGlu<sub>5</sub> Allosteric Ligands.
Published in: Mol Pharmacol

Ligand: PHCCC (Synthetic organic)
Interaction type: Allosteric modulator
Action: Neutral
Ligand approved: no
Primary target: no
Median affinity: 5.630000114440918 pKB
Reference (Journal): &quot;Selective&quot; Class C G Protein-Coupled Receptor Modulators Are Neutral or Biased mGlu<sub>5</sub> Allosteric Ligands.
Published in: Mol Pharmacol

Ligand: PTeB (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.2 pIC50
Reference (Journal): Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity.
Published in: J Med Chem

Ligand: quisqualate (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.5 pIC50
Reference (Journal): Characterization of [(3)H]Quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections.
Published in: J Neurochem

Ligand: (S)-4CPG (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.6 pIC50
Reference (Journal): Characterization of [(3)H]Quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections.
Published in: J Neurochem

Ligand: (S)-(+)-CBPG (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 4.300000190734863 pEC50
Reference (Journal): Biochemical and electrophysiological studies on (S)-(+)-2-(3'-carboxybicyclo(1.1.1)pentyl)-glycine (CBPG), a novel mGlu5 receptor agonist endowed with mGlu1 receptor antagonist activity.
Published in: Neuropharmacology

Ligand: SIB-1757 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): [(3)H]-M-MPEP, a potent, subtype-selective radioligand for the metabotropic glutamate receptor subtype 5.
Published in: Bioorg Med Chem Lett

Ligand: SIB-1757 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): SIB-1757 and SIB-1893: selective, noncompetitive antagonists of metabotropic glutamate receptor type 5.
Published in: J Pharmacol Exp Ther

Ligand: SIB-1893 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): [(3)H]-M-MPEP, a potent, subtype-selective radioligand for the metabotropic glutamate receptor subtype 5.
Published in: Bioorg Med Chem Lett

Ligand: SIB-1893 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): SIB-1757 and SIB-1893: selective, noncompetitive antagonists of metabotropic glutamate receptor type 5.
Published in: J Pharmacol Exp Ther

Ligand: SP203 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 10.44 pIC50
Reference (Journal): Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography.
Published in: J Med Chem

Ligand: [11C]JNJ-16567083 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.630000114440918 pKi
Reference (Journal): A positron emission tomography radioligand for the in vivo labeling of metabotropic glutamate 1 receptor: (3-ethyl-2-[11C]methyl-6-quinolinyl)(cis- 4-methoxycyclohexyl)methanone.
Published in: J Med Chem

Ligand: [14C]MTEP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.7 pIC50
Reference (Journal): [3H]Methoxymethyl-3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine binding to metabotropic glutamate receptor subtype 5 in rodent brain: in vitro and in vivo characterization.
Published in: J Pharmacol Exp Ther

Ligand: [3H]CTEP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.82 pKd
Reference (Journal): CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor.
Published in: J Pharmacol Exp Ther

Ligand: [3H]CTEP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.74 pKd
Reference (Journal): CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor.
Published in: J Pharmacol Exp Ther

Ligand: [3H]CTEP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.77 pKd
Reference (Journal): CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor.
Published in: J Pharmacol Exp Ther

Ligand: [3H]fenobam (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.5 pKd
Reference (Journal): Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity.
Published in: J Pharmacol Exp Ther

Ligand: [3H]fenobam (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.3 pKd
Reference (Journal): Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity.
Published in: J Pharmacol Exp Ther

Ligand: [3H]methoxymethyl-MTEP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.7 pKd
Reference (Journal): [3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor.
Published in: Bioorg Med Chem Lett

Ligand: [3H]methoxy-PEPy (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.47 pKd
Reference (Journal): [3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor.
Published in: Bioorg Med Chem Lett

Ligand: [3H]M-MPEP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.4 pIC50
Reference (Journal): [(3)H]-M-MPEP, a potent, subtype-selective radioligand for the metabotropic glutamate receptor subtype 5.
Published in: Bioorg Med Chem Lett

Ligand: [3H]M-MPEP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.3 pIC50
Reference (Journal): A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5.
Published in: Mol Pharmacol

Ligand: VU0092273 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.89 pEC50
Reference (Journal): Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function.
Published in: Mol Pharmacol

Ligand: VU0092273 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.46 pEC50
Reference (Journal): Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function.
Published in: Mol Pharmacol

Ligand: VU0240382 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.41 pEC50
Reference (Journal): Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function.
Published in: Mol Pharmacol

Ligand: VU0285683 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity.
Published in: Mol Pharmacol

Ligand: VU0285683 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.61 pIC50
Reference (Journal): Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity.
Published in: Mol Pharmacol

Ligand: VU0357121 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.48 pEC50
Reference (Journal): Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology.
Published in: ACS Chem Neurosci

Ligand: VU0360172 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.8 pEC50
Reference (Journal): Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity.
Published in: Mol Pharmacol

Ligand: VU0360172 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  pKB
Reference (Journal): Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity.
Published in: Mol Pharmacol

Ligand: VU0360172 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  pKB
Reference (Journal): Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships.
Published in: Mol Pharmacol

Ligand: VU0360172 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.71 pKi
Reference (Journal): Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity.
Published in: Mol Pharmacol

Ligand: VU0361747 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.9 pEC50
Reference (Journal): Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function.
Published in: Mol Pharmacol

Ligand: VU0364289 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 5.8 pEC50
Reference (Journal): Discovery of N-Aryl Piperazines as Selective mGlu(5) Potentiators with Efficacy in a Rodent Model Predictive of Anti-Psychotic Activity.
Published in: ACS Med Chem Lett

Ligand: VU0366058 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.04 pIC50
Reference (Journal): Discovery of 2-(2-benzoxazoyl amino)-4-aryl-5-cyanopyrimidine as negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGlu₅): from an artificial neural network virtual screen to an in vivo tool compound.
Published in: ChemMedChem

Ligand: VU0366058 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.08 pKi
Reference (Journal): Discovery of 2-(2-benzoxazoyl amino)-4-aryl-5-cyanopyrimidine as negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGlu₅): from an artificial neural network virtual screen to an in vivo tool compound.
Published in: ChemMedChem

Ligand: VU0404251 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 8.14 pEC50
Reference (Journal): Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover.
Published in: Bioorg Med Chem Lett

Ligand: VU0404251 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.15 pEC50
Reference (Journal): Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover.
Published in: Bioorg Med Chem Lett

Ligand: VU0409551 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pKB
Reference (Journal): Biased mGlu5-Positive Allosteric Modulators Provide In Vivo Efficacy without Potentiating mGlu5 Modulation of NMDAR Currents.
Published in: Neuron

Ligand: VU0424465 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.77 pEC50
Reference (Journal): Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity.
Published in: Biol Psychiatry

Ligand: VU0424465 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 8.82 pEC50
Reference (Journal): Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity.
Published in: Biol Psychiatry

Ligand: VU0463841 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.9 pIC50
Reference (Journal): Substituted 1-Phenyl-3-(pyridin-2-yl)urea negative allosteric modulators of mGlu5: discovery of a new tool compound VU0463841 with activity in rat models of cocaine addiction.
Published in: ACS Chem Neurosci

Ligand: VU0463841 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.89 pEC50
Reference (Journal): Substituted 1-Phenyl-3-(pyridin-2-yl)urea negative allosteric modulators of mGlu5: discovery of a new tool compound VU0463841 with activity in rat models of cocaine addiction.
Published in: ACS Chem Neurosci

Ligand: VU0483605 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 6.480000019073486 pKB
Reference (Journal): &quot;Selective&quot; Class C G Protein-Coupled Receptor Modulators Are Neutral or Biased mGlu<sub>5</sub> Allosteric Ligands.
Published in: Mol Pharmacol

Ligand: VU-1545 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 8 pEC50
Reference (Journal): Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes.
Published in: J Med Chem

Ligand: VU-1545 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.81 pKi
Reference (Journal): Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes.
Published in: J Med Chem

Ligand: VU-29 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.61 pKi
Reference (Journal): Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses.
Published in: Mol Pharmacol

Ligand: VU-29 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 8.05 pEC50
Reference (Journal): Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses.
Published in: Mol Pharmacol