Target family: Metabotropic glutamate receptors (type: gpcr)
Target: mGlu<sub>2</sub> receptor

Ligand: (1S,3R)-ACPD (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of [(3)H]-LY354740 binding to rat mGlu2 and mGlu3 receptors expressed in CHO cells using semliki forest virus vectors.
Published in: Neuropharmacology

Ligand: (1S,3R)-ACPD (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of [3H]-(2S,2'R,3'R)-2-(2',3'-dicarboxy-cyclopropyl)glycine ([3H]-DCG IV) binding to metabotropic mGlu2 receptor-transfected cell membranes.
Published in: Br J Pharmacol

Ligand: (1S,3R)-ACPD (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.2 pKi
Reference (Journal): [3H]-LY341495 as a novel antagonist radioligand for group II metabotropic glutamate (mGlu) receptors: characterization of binding to membranes of mGlu receptor subtype expressing cells.
Published in: Neuropharmacology

Ligand: 2,2,2-TEMPS (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.85 pEC50
Reference (Journal): SAR study of a subtype selective allosteric potentiator of metabotropic glutamate 2 receptor, N-(4-phenoxyphenyl)-N-(3-pyridinylmethyl)ethanesulfonamide.
Published in: Bioorg Med Chem Lett

Ligand: (2R,3R)-APDC (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5 pKi
Reference (Journal): [3H]-LY341495 as a novel antagonist radioligand for group II metabotropic glutamate (mGlu) receptors: characterization of binding to membranes of mGlu receptor subtype expressing cells.
Published in: Neuropharmacology

Ligand: 3-MPPTS (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.6 pIC50
Reference (Journal): Metabotropic glutamate 2 receptor potentiators: receptor modulation, frequency-dependent synaptic activity, and efficacy in preclinical anxiety and psychosis model(s).
Published in: Psychopharmacology (Berl.)

Ligand: 3-MPPTS (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.6 pIC50
Reference (Journal): Discovery of allosteric potentiators for the metabotropic glutamate 2 receptor: synthesis and subtype selectivity of N-(4-(2-methoxyphenoxy)phenyl)-N-(2,2,2- trifluoroethylsulfonyl)pyrid-3-ylmethylamine.
Published in: J Med Chem

Ligand: 3-MPPTS (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.6 pIC50
Reference (Journal): Pharmacological characterization and identification of amino acids involved in the positive modulation of metabotropic glutamate receptor subtype 2.
Published in: Mol Pharmacol

Ligand: 4-APPES (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 5.65 pEC50
Reference (Journal): Metabotropic glutamate 2 receptor potentiators: receptor modulation, frequency-dependent synaptic activity, and efficacy in preclinical anxiety and psychosis model(s).
Published in: Psychopharmacology (Berl.)

Ligand: 4-MPPTS (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 5.8 pIC50
Reference (Journal): Discovery of allosteric potentiators for the metabotropic glutamate 2 receptor: synthesis and subtype selectivity of N-(4-(2-methoxyphenoxy)phenyl)-N-(2,2,2- trifluoroethylsulfonyl)pyrid-3-ylmethylamine.
Published in: J Med Chem

Ligand: 4-MPPTS (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 5.8 pIC50
Reference (Journal): Metabotropic glutamate 2 receptor potentiators: receptor modulation, frequency-dependent synaptic activity, and efficacy in preclinical anxiety and psychosis model(s).
Published in: Psychopharmacology (Berl.)

Ligand: 4-MPPTS (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 5.8 pIC50
Reference (Journal): SAR study of a subtype selective allosteric potentiator of metabotropic glutamate 2 receptor, N-(4-phenoxyphenyl)-N-(3-pyridinylmethyl)ethanesulfonamide.
Published in: Bioorg Med Chem Lett

Ligand: 4-MPPTS (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 5.8 pIC50
Reference (Journal): Pharmacological characterization and identification of amino acids involved in the positive modulation of metabotropic glutamate receptor subtype 2.
Published in: Mol Pharmacol

Ligand: α-methylserine-O-phosphate (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.3 pKi
Reference (Journal): Characterization of [3H]-(2S,2'R,3'R)-2-(2',3'-dicarboxy-cyclopropyl)glycine ([3H]-DCG IV) binding to metabotropic mGlu2 receptor-transfected cell membranes.
Published in: Br J Pharmacol

Ligand: AZD8529 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: yes
Median affinity: 6.710000038146973 pEC50
Reference (Webpage): AZD8529-Open Innovation.

Ligand: biphenylindanone A (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7 pEC50
Reference (Journal): Biphenyl-indanones: allosteric potentiators of the metabotropic glutamate subtype 2 receptor.
Published in: Bioorg Med Chem Lett

Ligand: CBiPES (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7 pEC50
Reference (Journal): Metabotropic glutamate 2 receptor potentiators: receptor modulation, frequency-dependent synaptic activity, and efficacy in preclinical anxiety and psychosis model(s).
Published in: Psychopharmacology (Berl.)

Ligand: compound 14a [PMID: 18812259] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.6 pEC50
Reference (Journal): 3-(Imidazolyl methyl)-3-aza-bicyclo[3.1.0]hexan-6-yl)methyl ethers: a novel series of mGluR2 positive allosteric modulators.
Published in: Bioorg Med Chem Lett

Ligand: compound 14c [PMID: 18812259] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.5 pEC50
Reference (Journal): 3-(Imidazolyl methyl)-3-aza-bicyclo[3.1.0]hexan-6-yl)methyl ethers: a novel series of mGluR2 positive allosteric modulators.
Published in: Bioorg Med Chem Lett

Ligand: compound 14 [PMID: 21155570] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.77 pEC50
Reference (Journal): Design and synthesis of an orally active metabotropic glutamate receptor subtype-2 (mGluR2) positive allosteric modulator (PAM) that decreases cocaine self-administration in rats.
Published in: J Med Chem

Ligand: compound 19 [PMID: 18812259] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.2 pEC50
Reference (Journal): 3-(Imidazolyl methyl)-3-aza-bicyclo[3.1.0]hexan-6-yl)methyl ethers: a novel series of mGluR2 positive allosteric modulators.
Published in: Bioorg Med Chem Lett

Ligand: compound 2 [PMID: 21105727] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 6 pKi
Reference (Journal): Chemical switch of a metabotropic glutamate receptor 2 silent allosteric modulator into dual metabotropic glutamate receptor 2/3 negative/positive allosteric modulators.
Published in: J Med Chem

Ligand: compound 2 [PMID: 21105727] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 6.1 pIC50
Reference (Journal): Chemical switch of a metabotropic glutamate receptor 2 silent allosteric modulator into dual metabotropic glutamate receptor 2/3 negative/positive allosteric modulators.
Published in: J Med Chem

Ligand: compound 34 [PMID: 20409708] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.08 pEC50
Reference (Journal): 3-Aryl-5-phenoxymethyl-1,3-oxazolidin-2-ones as positive allosteric modulators of mGluR2 for the treatment of schizophrenia: Hit-to-lead efforts.
Published in: Bioorg Med Chem Lett

Ligand: compound 3 [PMID: 21105727] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 6.22 pKi
Reference (Journal): Chemical switch of a metabotropic glutamate receptor 2 silent allosteric modulator into dual metabotropic glutamate receptor 2/3 negative/positive allosteric modulators.
Published in: J Med Chem

Ligand: compound 3 [PMID: 21105727] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 5.82 pIC50
Reference (Journal): Chemical switch of a metabotropic glutamate receptor 2 silent allosteric modulator into dual metabotropic glutamate receptor 2/3 negative/positive allosteric modulators.
Published in: J Med Chem

Ligand: compound 48 [PMID: 22364337] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.44 pEC50
Reference (Journal): Discovery of 1,4-disubstituted 3-cyano-2-pyridones: a new class of positive allosteric modulators of the metabotropic glutamate 2 receptor.
Published in: J Med Chem

Ligand: compound 4 [PMID: 21105727] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 6 pIC50
Reference (Journal): Chemical switch of a metabotropic glutamate receptor 2 silent allosteric modulator into dual metabotropic glutamate receptor 2/3 negative/positive allosteric modulators.
Published in: J Med Chem

Ligand: compound 4 [PMID: 21105727] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 6.1 pKi
Reference (Journal): Chemical switch of a metabotropic glutamate receptor 2 silent allosteric modulator into dual metabotropic glutamate receptor 2/3 negative/positive allosteric modulators.
Published in: J Med Chem

Ligand: cyPPTS (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.6 pEC50
Reference (Journal): Metabotropic glutamate 2 receptor potentiators: receptor modulation, frequency-dependent synaptic activity, and efficacy in preclinical anxiety and psychosis model(s).
Published in: Psychopharmacology (Berl.)

Ligand: DCG-IV (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.5 pKi
Reference (Journal): [3H]-LY341495 as a novel antagonist radioligand for group II metabotropic glutamate (mGlu) receptors: characterization of binding to membranes of mGlu receptor subtype expressing cells.
Published in: Neuropharmacology

Ligand: DCG-IV (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7 pKi
Reference (Journal): Characterization of [3H]-(2S,2'R,3'R)-2-(2',3'-dicarboxy-cyclopropyl)glycine ([3H]-DCG IV) binding to metabotropic mGlu2 receptor-transfected cell membranes.
Published in: Br J Pharmacol

Ligand: DCG-IV (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7 pKi
Reference (Journal): Characterization of [(3)H]-LY354740 binding to rat mGlu2 and mGlu3 receptors expressed in CHO cells using semliki forest virus vectors.
Published in: Neuropharmacology

Ligand: eGlu (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of [(3)H]-LY354740 binding to rat mGlu2 and mGlu3 receptors expressed in CHO cells using semliki forest virus vectors.
Published in: Neuropharmacology

Ligand: eGlu (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of [3H]-(2S,2'R,3'R)-2-(2',3'-dicarboxy-cyclopropyl)glycine ([3H]-DCG IV) binding to metabotropic mGlu2 receptor-transfected cell membranes.
Published in: Br J Pharmacol

Ligand: eglumegad (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of [3H]-(2S,2'R,3'R)-2-(2',3'-dicarboxy-cyclopropyl)glycine ([3H]-DCG IV) binding to metabotropic mGlu2 receptor-transfected cell membranes.
Published in: Br J Pharmacol

Ligand: eglumegad (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.9 pKi
Reference (Journal): [3H]-LY341495 as a novel antagonist radioligand for group II metabotropic glutamate (mGlu) receptors: characterization of binding to membranes of mGlu receptor subtype expressing cells.
Published in: Neuropharmacology

Ligand: eglumegad (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of [(3)H]-LY354740 binding to rat mGlu2 and mGlu3 receptors expressed in CHO cells using semliki forest virus vectors.
Published in: Neuropharmacology

Ligand: GSK1331258 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.1 pEC50
Reference (Journal): The identification of structurally novel, selective, orally bioavailable positive modulators of mGluR2.
Published in: Bioorg Med Chem Lett

Ligand: GSK1331268 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.9 pEC50
Reference (Journal): The identification of structurally novel, selective, orally bioavailable positive modulators of mGluR2.
Published in: Bioorg Med Chem Lett

Ligand: (S)-4C3HPG (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.8 pKi
Reference (Journal): Characterization of [3H]-(2S,2'R,3'R)-2-(2',3'-dicarboxy-cyclopropyl)glycine ([3H]-DCG IV) binding to metabotropic mGlu2 receptor-transfected cell membranes.
Published in: Br J Pharmacol

Ligand: JNJ-40068782 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Pharmacological characterization of JNJ-40068782, a new potent, selective, and systemically active positive allosteric modulator of the mGlu2 receptor and its radioligand [3H]JNJ-40068782.
Published in: J Pharmacol Exp Ther

Ligand: JNJ-40068782 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.28 pEC50
Reference (Journal): Pharmacological characterization of JNJ-40068782, a new potent, selective, and systemically active positive allosteric modulator of the mGlu2 receptor and its radioligand [3H]JNJ-40068782.
Published in: J Pharmacol Exp Ther

Ligand: JNJ-40411813 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: yes
Median affinity: 6.829999923706055 pEC50
Reference (Journal): Pharmacological and pharmacokinetic properties of JNJ-40411813, a positive allosteric modulator of the mGlu2 receptor.
Published in: Pharmacol Res Perspect

Ligand: JNJ-42153605 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.77 pEC50
Reference (Journal): Discovery of 3-cyclopropylmethyl-7-(4-phenylpiperidin-1-yl)-8-trifluoromethyl[1,2,4]triazolo[4,3-a]pyridine (JNJ-42153605): a positive allosteric modulator of the metabotropic glutamate 2 receptor.
Published in: J Med Chem

Ligand: JNJ-42153605 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.82 pKi
Reference (Journal): Discovery of 3-cyclopropylmethyl-7-(4-phenylpiperidin-1-yl)-8-trifluoromethyl[1,2,4]triazolo[4,3-a]pyridine (JNJ-42153605): a positive allosteric modulator of the metabotropic glutamate 2 receptor.
Published in: J Med Chem

Ligand: JNJ-46281222 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: yes
Median affinity: 8.770000457763672 pKd
Reference (Journal): Molecular mechanism of positive allosteric modulation of the metabotropic glutamate receptor 2 by JNJ-46281222.
Published in: Br J Pharmacol

Ligand: JNJ-46281222 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: yes
Median affinity: 8.329999923706055 pKi
Reference (Journal): Molecular mechanism of positive allosteric modulation of the metabotropic glutamate receptor 2 by JNJ-46281222.
Published in: Br J Pharmacol

Ligand: L-CCG-I (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of [(3)H]-LY354740 binding to rat mGlu2 and mGlu3 receptors expressed in CHO cells using semliki forest virus vectors.
Published in: Neuropharmacology

Ligand: L-CCG-I (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.3 pKi
Reference (Journal): [3H]-LY341495 as a novel antagonist radioligand for group II metabotropic glutamate (mGlu) receptors: characterization of binding to membranes of mGlu receptor subtype expressing cells.
Published in: Neuropharmacology

Ligand: L-CCG-I (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of [3H]-(2S,2'R,3'R)-2-(2',3'-dicarboxy-cyclopropyl)glycine ([3H]-DCG IV) binding to metabotropic mGlu2 receptor-transfected cell membranes.
Published in: Br J Pharmacol

Ligand: L-glutamic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.9 pKi
Reference (Journal): [3H]-LY341495 as a novel antagonist radioligand for group II metabotropic glutamate (mGlu) receptors: characterization of binding to membranes of mGlu receptor subtype expressing cells.
Published in: Neuropharmacology

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: L-glutamic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Complex interactions between mGluRs, intracellular Ca2+ stores and ion channels in neurons.
Published in: Trends Neurosci

Ligand: L-glutamic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): L-cysteine sulfinic acid as an endogenous agonist of a novel metabotropic receptor coupled to stimulation of phospholipase D activity.
Published in: Mol Pharmacol

Ligand: LY341495 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of [3H]-(2S,2'R,3'R)-2-(2',3'-dicarboxy-cyclopropyl)glycine ([3H]-DCG IV) binding to metabotropic mGlu2 receptor-transfected cell membranes.
Published in: Br J Pharmacol

Ligand: LY341495 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): [3H]-LY341495 as a novel antagonist radioligand for group II metabotropic glutamate (mGlu) receptors: characterization of binding to membranes of mGlu receptor subtype expressing cells.
Published in: Neuropharmacology

Ligand: LY341495 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of [(3)H]-LY354740 binding to rat mGlu2 and mGlu3 receptors expressed in CHO cells using semliki forest virus vectors.
Published in: Neuropharmacology

Ligand: LY379268 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.9 pKi
Reference (Journal): Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists for group II metabotropic glutamate receptors.
Published in: J Med Chem

Ligand: LY395756 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.78000020980835 pKi
Reference (Journal): LY395756, an mGluR2 agonist and mGluR3 antagonist, enhances NMDA receptor expression and function in the normal adult rat prefrontal cortex, but fails to improve working memory and reverse MK801-induced working memory impairment.
Published in: Exp Neurol

Ligand: (+)-MCPG (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.6 pKi
Reference (Journal): Characterization of [3H]-(2S,2'R,3'R)-2-(2',3'-dicarboxy-cyclopropyl)glycine ([3H]-DCG IV) binding to metabotropic mGlu2 receptor-transfected cell membranes.
Published in: Br J Pharmacol

Ligand: (+)-MCPG (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 3.8 pKi
Reference (Journal): [3H]-LY341495 as a novel antagonist radioligand for group II metabotropic glutamate (mGlu) receptors: characterization of binding to membranes of mGlu receptor subtype expressing cells.
Published in: Neuropharmacology

Ligand: MGS0028 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.2 pKi
Reference (Journal): Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
Published in: J Med Chem

Ligand: MGS0039 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): MGS0039: a potent and selective group II metabotropic glutamate receptor antagonist with antidepressant-like activity.
Published in: Neuropharmacology

Ligand: MGS0039 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Synthesis, in vitro pharmacology, structure-activity relationships, and pharmacokinetics of 3-alkoxy-2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent and selective group II metabotropic glutamate receptor antagonists.
Published in: J Med Chem

Ligand: MNI-135 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): A novel family of potent negative allosteric modulators of group II metabotropic glutamate receptors.
Published in: J Pharmacol Exp Ther

Ligand: MNI-135 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): A novel family of potent negative allosteric modulators of group II metabotropic glutamate receptors.
Published in: J Pharmacol Exp Ther

Ligand: MNI-136 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): A novel family of potent negative allosteric modulators of group II metabotropic glutamate receptors.
Published in: J Pharmacol Exp Ther

Ligand: MNI-136 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): A novel family of potent negative allosteric modulators of group II metabotropic glutamate receptors.
Published in: J Pharmacol Exp Ther

Ligand: MNI-137 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): A novel family of potent negative allosteric modulators of group II metabotropic glutamate receptors.
Published in: J Pharmacol Exp Ther

Ligand: MNI-137 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): A novel family of potent negative allosteric modulators of group II metabotropic glutamate receptors.
Published in: J Pharmacol Exp Ther

Ligand: PCCG-4 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.099999904632568 pIC50
Reference (Journal): Synthesis and pharmacological characterization of all sixteen stereoisomers of 2-(2'-carboxy-3'-phenylcyclopropyl)glycine. Focus on (2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-phenylcyclopropyl)glycine, a novel and selective group II metabotropic glutamate receptors antagonist.
Published in: J Med Chem

Ligand: PTBE (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.5 pIC50
Reference (Journal): Phenyl-tetrazolyl acetophenones: discovery of positive allosteric potentiatiors for the metabotropic glutamate 2 receptor.
Published in: J Med Chem

Ligand: Ro4491533 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.27 pKi
Reference (Journal): Characterization of an mGluR2/3 negative allosteric modulator in rodent models of depression.
Published in: J Neurogenet

Ligand: Ro4491533 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Characterization of an mGluR2/3 negative allosteric modulator in rodent models of depression.
Published in: J Neurogenet

Ligand: Ro4491533 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of an mGluR2/3 negative allosteric modulator in rodent models of depression.
Published in: J Neurogenet

Ligand: Ro4491533 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.85 pIC50
Reference (Journal): Synthesis and characterization of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: Part 4. In vivo active potent and selective non-competitive metabotropic glutamate receptor 2/3 antagonists.
Published in: Bioorg Med Chem Lett

Ligand: Ro4491533 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Synthesis and characterization of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: Part 4. In vivo active potent and selective non-competitive metabotropic glutamate receptor 2/3 antagonists.
Published in: Bioorg Med Chem Lett

Ligand: RO4988546 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.64 pKi
Reference (Journal): Structural determinants of allosteric antagonism at metabotropic glutamate receptor 2: mechanistic studies with new potent negative allosteric modulators.
Published in: Br J Pharmacol

Ligand: RO4988546 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.26 pIC50
Reference (Journal): Structural determinants of allosteric antagonism at metabotropic glutamate receptor 2: mechanistic studies with new potent negative allosteric modulators.
Published in: Br J Pharmacol

Ligand: RO5488608 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Structural determinants of allosteric antagonism at metabotropic glutamate receptor 2: mechanistic studies with new potent negative allosteric modulators.
Published in: Br J Pharmacol

Ligand: Ro64-5229 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7 pIC50
Reference (Journal): Synthesis of heterocyclic enol ethers and their use as group 2 metabotropic glutamate receptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: [3H]2,2,2-TEMPS (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 8.38 pKd
Reference (Journal): Structural determinants of allosteric antagonism at metabotropic glutamate receptor 2: mechanistic studies with new potent negative allosteric modulators.
Published in: Br J Pharmacol

Ligand: [3H]eglumegad (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.7 pKd
Reference (Journal): Characterization of [(3)H]-LY354740 binding to rat mGlu2 and mGlu3 receptors expressed in CHO cells using semliki forest virus vectors.
Published in: Neuropharmacology

Ligand: [3H]JNJ-40068782 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.92 pKd
Reference (Journal): Pharmacological characterization of JNJ-40068782, a new potent, selective, and systemically active positive allosteric modulator of the mGlu2 receptor and its radioligand [3H]JNJ-40068782.
Published in: J Pharmacol Exp Ther

Ligand: [3H]JNJ-40068782 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 8 pKd
Reference (Journal): Pharmacological characterization of JNJ-40068782, a new potent, selective, and systemically active positive allosteric modulator of the mGlu2 receptor and its radioligand [3H]JNJ-40068782.
Published in: J Pharmacol Exp Ther

Ligand: [3H]LY341495 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.8 pKd
Reference (Journal): [3H]-LY341495 as a novel antagonist radioligand for group II metabotropic glutamate (mGlu) receptors: characterization of binding to membranes of mGlu receptor subtype expressing cells.
Published in: Neuropharmacology

Ligand: THIIC (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.65 pEC50
Reference (Journal): N-(4-((2-(trifluoromethyl)-3-hydroxy-4-(isobutyryl)phenoxy)methyl)benzyl)-1-methyl-1H-imidazole-4-carboxamide (THIIC), a novel metabotropic glutamate 2 potentiator with potential anxiolytic/antidepressant properties: in vivo profiling suggests a link between behavioral and central nervous system neurochemical changes.
Published in: J Pharmacol Exp Ther

Ligand: THIIC (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.89 pEC50
Reference (Journal): N-(4-((2-(trifluoromethyl)-3-hydroxy-4-(isobutyryl)phenoxy)methyl)benzyl)-1-methyl-1H-imidazole-4-carboxamide (THIIC), a novel metabotropic glutamate 2 potentiator with potential anxiolytic/antidepressant properties: in vivo profiling suggests a link between behavioral and central nervous system neurochemical changes.
Published in: J Pharmacol Exp Ther