Target family: Metabotropic glutamate receptors (type: gpcr)
Target: mGlu<sub>8</sub> receptor

Ligand: (1S,3R)-ACPD (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.4 pEC50
Reference (Journal): Group III human metabotropic glutamate receptors 4, 7 and 8: molecular cloning, functional expression, and comparison of pharmacological properties in RGT cells.
Published in: Brain Res Mol Brain Res

Ligand: (1S,3R)-ACPD (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.3 pEC50
Reference (Journal): Cloning and expression of rat metabotropic glutamate receptor 8 reveals a distinct pharmacological profile.
Published in: Mol Pharmacol

Ligand: ACPT-I (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 5.1 pEC50
Reference (Journal): Pharmacological characterization of the rat metabotropic glutamate receptor type 8a revealed strong similarities and slight differences with the type 4a receptor.
Published in: Eur J Pharmacol

Ligand: α-methylserine-O-phosphate (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.3 pIC50
Reference (Journal): The metabotropic glutamate receptors: structure, activation mechanism and pharmacology.
Published in: Curr Drug Targets CNS Neurol Disord

Ligand: AZ12216052 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6 pEC50
Reference (Journal): Acute pharmacological modulation of mGluR8 reduces measures of anxiety.
Published in: Behav Brain Res

Ligand: AZ12216052 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 5.429999828338623 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: CPPG (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.3 pKi
Reference (Journal): Constraints on proper folding of the amino terminal domains of group III metabotropic glutamate receptors.
Published in: Brain Res Mol Brain Res

Ligand: D-AP4 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.5 pEC50
Reference (Journal): Group III human metabotropic glutamate receptors 4, 7 and 8: molecular cloning, functional expression, and comparison of pharmacological properties in RGT cells.
Published in: Brain Res Mol Brain Res

Ligand: DCG-IV (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.5 pIC50
Reference (Journal): Cloning and functional expression of alternative spliced variants of the human metabotropic glutamate receptor 8.
Published in: Brain Res Mol Brain Res

Ligand: eglumegad (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.1 pEC50
Reference (Journal): Cloning and functional expression of alternative spliced variants of the human metabotropic glutamate receptor 8.
Published in: Brain Res Mol Brain Res

Ligand: (R,S)-4-PPG (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.7 pEC50
Reference (Journal): (S)-3,4-DCPG, a potent and selective mGlu8a receptor agonist, activates metabotropic glutamate receptors on primary afferent terminals in the neonatal rat spinal cord.
Published in: Neuropharmacology

Ligand: (R,S)-4-PPG (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.7 pEC50
Reference (Journal): (R,S)-4-phosphonophenylglycine, a potent and selective group III metabotropic glutamate receptor agonist is anticonvulsive and neuroprotective<i>in vivo</i>.
Published in: J Pharmacol Exp Ther

Ligand: (R,S)-4-PPG (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.7 pEC50
Reference (Journal): (+)-4-phosphonophenylglycine (PPG) a new group III selective metabotropic glutamate receptor agonist.
Published in: Bioorg Med Chem Lett

Ligand: (S)-3,4-DCPG (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.5 pEC50
Reference (Journal): (S)-3,4-DCPG, a potent and selective mGlu8a receptor agonist, activates metabotropic glutamate receptors on primary afferent terminals in the neonatal rat spinal cord.
Published in: Neuropharmacology

Ligand: L-AP4 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Cloning and functional expression of alternative spliced variants of the human metabotropic glutamate receptor 8.
Published in: Brain Res Mol Brain Res

Ligand: L-AP4 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.2 pEC50
Reference (Journal): Cloning and expression of rat metabotropic glutamate receptor 8 reveals a distinct pharmacological profile.
Published in: Mol Pharmacol

Ligand: L-CCG-I (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.2 pEC50
Reference (Journal): Cloning and expression of rat metabotropic glutamate receptor 8 reveals a distinct pharmacological profile.
Published in: Mol Pharmacol

Ligand: L-CCG-I (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Cloning and functional expression of alternative spliced variants of the human metabotropic glutamate receptor 8.
Published in: Brain Res Mol Brain Res

Ligand: L-glutamic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Cloning and functional expression of alternative spliced variants of the human metabotropic glutamate receptor 8.
Published in: Brain Res Mol Brain Res

Ligand: L-glutamic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Group III human metabotropic glutamate receptors 4, 7 and 8: molecular cloning, functional expression, and comparison of pharmacological properties in RGT cells.
Published in: Brain Res Mol Brain Res

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-serine-O-phosphate (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Cloning and functional expression of alternative spliced variants of the human metabotropic glutamate receptor 8.
Published in: Brain Res Mol Brain Res

Ligand: L-serine-O-phosphate (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Group III human metabotropic glutamate receptors 4, 7 and 8: molecular cloning, functional expression, and comparison of pharmacological properties in RGT cells.
Published in: Brain Res Mol Brain Res

Ligand: LY341495 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.8 pIC50
Reference (Journal): LY341495 is a nanomolar potent and selective antagonist of group II metabotropic glutamate receptors.
Published in: Neuropharmacology

Ligand: MAP4 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Cloning and expression of rat metabotropic glutamate receptor 8 reveals a distinct pharmacological profile.
Published in: Mol Pharmacol

Ligand: MAP4 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Constraints on proper folding of the amino terminal domains of group III metabotropic glutamate receptors.
Published in: Brain Res Mol Brain Res

Ligand: MPPG (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.33 pIC50
Reference (Journal): Group III human metabotropic glutamate receptors 4, 7 and 8: molecular cloning, functional expression, and comparison of pharmacological properties in RGT cells.
Published in: Brain Res Mol Brain Res

Ligand: [3H]AP4 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Cloning and functional expression of alternative spliced variants of the human metabotropic glutamate receptor 8.
Published in: Brain Res Mol Brain Res

Ligand: VU0155094 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 5 pKB
Reference (Journal): Identification of positive allosteric modulators VU0155094 (ML397) and VU0422288 (ML396) reveals new insights into the biology of metabotropic glutamate receptor 7.
Published in: ACS Chem Neurosci

Ligand: VU0422288 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pKB
Reference (Journal): Identification of positive allosteric modulators VU0155094 (ML397) and VU0422288 (ML396) reveals new insights into the biology of metabotropic glutamate receptor 7.
Published in: ACS Chem Neurosci