Target family: Metabotropic glutamate receptors (type: gpcr)
Target: mGlu<sub>1</sub> receptor

Ligand: (1S,3R)-ACPD (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): A pharmacological characterization of the mGluR1 alpha subtype of the metabotropic glutamate receptor expressed in a cloned baby hamster kidney cell line.
Published in: Brain Res

Ligand: (1S,3R)-ACPD (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
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: (1S,3R)-ACPD (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.
Published in: Mol Pharmacol

Ligand: 3,5-DHPG (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.8 pKi
Reference (Journal): [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.
Published in: Mol Pharmacol

Ligand: 3,5-dimethyl PPP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pIC50
Reference (Journal): Synthesis and pharmacological characterisation of 2,4-dicarboxy-pyrroles as selective non-competitive mGluR1 antagonists.
Published in: Bioorg Med Chem

Ligand: 3-MATIDA (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.199999809265137 pIC50
Reference (Journal): The novel and systemically active metabotropic glutamate 1 (mGlu1) receptor antagonist 3-MATIDA reduces post-ischemic neuronal death.
Published in: Neuropharmacology

Ligand: A-794278 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.27 pKi
Reference (Journal): Analgesic activity of metabotropic glutamate receptor 1 antagonists on spontaneous post-operative pain in rats.
Published in: Eur J Pharmacol

Ligand: A-794278 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8 pIC50
Reference (Journal): Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
Published in: J Med Chem

Ligand: A-794282 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
Published in: J Med Chem

Ligand: A-794282 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.33 pIC50
Reference (Journal): Analgesic activity of metabotropic glutamate receptor 1 antagonists on spontaneous post-operative pain in rats.
Published in: Eur J Pharmacol

Ligand: A-841720 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Analgesic activity of metabotropic glutamate receptor 1 antagonists on spontaneous post-operative pain in rats.
Published in: Eur J Pharmacol

Ligand: A-841720 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
Published in: J Med Chem

Ligand: A-841720 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
Published in: Bioorg Med Chem Lett

Ligand: A-850002 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.37 pIC50
Reference (Journal): Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
Published in: J Med Chem

Ligand: A-850002 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.39 pIC50
Reference (Journal): Analgesic activity of metabotropic glutamate receptor 1 antagonists on spontaneous post-operative pain in rats.
Published in: Eur J Pharmacol

Ligand: AIDA (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 4.199999809265137 pA2
Reference (Journal): Pharmacological characterization of 1-aminoindan-1,5-dicarboxylic acid, a potent mGluR1 antagonist.
Published in: J Pharmacol Exp Ther

Ligand: AIDA (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4 pKi
Reference (Journal): [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.
Published in: Mol Pharmacol

Ligand: BAY 367620 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.
Published in: Mol Pharmacol

Ligand: BAY 367620 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): BAY36-7620: a potent non-competitive mGlu1 receptor antagonist with inverse agonist activity.
Published in: Mol Pharmacol

Ligand: BAY 367620 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 9.470000267028809 pKi
Reference (Journal): BAY36-7620: a potent non-competitive mGlu1 receptor antagonist with inverse agonist activity.
Published in: Mol Pharmacol

Ligand: CFMMC (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.3 pIC50
Reference (Journal): Identification of a novel transmembrane domain involved in the negative modulation of mGluR1 using a newly discovered allosteric mGluR1 antagonist, 3-cyclohexyl-5-fluoro-6-methyl-7-(2-morpholin-4-ylethoxy)-4H-chromen-4-one.
Published in: Neuropharmacology

Ligand: CFMTI (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.59 pIC50
Reference (Journal): Unique antipsychotic activities of the selective metabotropic glutamate receptor 1 allosteric antagonist 2-cyclopropyl-5-[1-(2-fluoro-3-pyridinyl)-5-methyl-1H-1,2,3-triazol-4-yl]-2,3-dihydro-1H-isoindol-1-one.
Published in: J Pharmacol Exp Ther

Ligand: compound 10i [PMID: 23084894] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.22 pIC50
Reference (Journal): Synthesis and SAR development of novel mGluR1 antagonists for the treatment of chronic pain.
Published in: Bioorg Med Chem Lett

Ligand: compound 11c [PMID: 17929793] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 9 pKi
Reference (Journal): Discovery of orally efficacious tetracyclic metabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of chronic pain.
Published in: J Med Chem

Ligand: compound 11c [PMID: 17929793] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.31 pIC50
Reference (Journal): Discovery of orally efficacious tetracyclic metabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of chronic pain.
Published in: J Med Chem

Ligand: compound 11q [PMID: 19433355] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 9.05 pIC50
Reference (Journal): Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain.
Published in: Bioorg Med Chem Lett

Ligand: compound 11q [PMID: 19433355] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.46 pKi
Reference (Journal): Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain.
Published in: Bioorg Med Chem Lett

Ligand: compound 11s [PMID: 19433355] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.68 pIC50
Reference (Journal): Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain.
Published in: Bioorg Med Chem Lett

Ligand: compound 11s [PMID: 19433355] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.33 pKi
Reference (Journal): Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain.
Published in: Bioorg Med Chem Lett

Ligand: compound 12e [PMID: 22266036] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.92 pIC50
Reference (Journal): Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain.
Published in: Bioorg Med Chem Lett

Ligand: compound 12e [PMID: 22266036] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.28 pKi
Reference (Journal): Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain.
Published in: Bioorg Med Chem Lett

Ligand: compound 22 [PMID: 17276684] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 6.78 pIC50
Reference (Journal): From pyrroles to 1-oxo-2,3,4,9-tetrahydro-1H-beta-carbolines: a new class of orally bioavailable mGluR1 antagonists.
Published in: Bioorg Med Chem Lett

Ligand: compound 22 [PMID: 17276684] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.44 pKi
Reference (Journal): From pyrroles to 1-oxo-2,3,4,9-tetrahydro-1H-beta-carbolines: a new class of orally bioavailable mGluR1 antagonists.
Published in: Bioorg Med Chem Lett

Ligand: compound 22 [PMID: 19289283] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.52 pIC50
Reference (Journal): In vitro and in vivo SAR of pyrido[3,4-d]pyramid-4-ylamine based mGluR1 antagonists.
Published in: Bioorg Med Chem Lett

Ligand: compound 23c [PMID: 17929793] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.6 pIC50
Reference (Journal): Discovery of orally efficacious tetracyclic metabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of chronic pain.
Published in: J Med Chem

Ligand: compound 23c [PMID: 17929793] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 9.4 pKi
Reference (Journal): Discovery of orally efficacious tetracyclic metabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of chronic pain.
Published in: J Med Chem

Ligand: compound 23e [PMID: 17929793] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.54 pIC50
Reference (Journal): Discovery of orally efficacious tetracyclic metabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of chronic pain.
Published in: J Med Chem

Ligand: compound 23e [PMID: 17929793] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.82 pKi
Reference (Journal): Discovery of orally efficacious tetracyclic metabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of chronic pain.
Published in: J Med Chem

Ligand: compound 23h [PMID: 17929793] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.66 pIC50
Reference (Journal): Discovery of orally efficacious tetracyclic metabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of chronic pain.
Published in: J Med Chem

Ligand: compound 23h [PMID: 17929793] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.82 pKi
Reference (Journal): Discovery of orally efficacious tetracyclic metabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of chronic pain.
Published in: J Med Chem

Ligand: compound 23i [PMID: 17929793] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.85 pIC50
Reference (Journal): Discovery of orally efficacious tetracyclic metabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of chronic pain.
Published in: J Med Chem

Ligand: compound 24 [PMID: 20346665] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 6.94 pKi
Reference (Journal): A-ring modifications on the triazafluorenone core structure and their mGluR1 antagonist properties.
Published in: Bioorg Med Chem Lett

Ligand: compound 24 [PMID: 20346665] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.68 pIC50
Reference (Journal): A-ring modifications on the triazafluorenone core structure and their mGluR1 antagonist properties.
Published in: Bioorg Med Chem Lett

Ligand: compound 24 [PMID: 20346665] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 6.94 pKi
Reference (Journal): A-ring modifications on the triazafluorenone core structure and their mGluR1 antagonist properties.
Published in: Bioorg Med Chem Lett

Ligand: compound 27 [PMID: 20346665] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.57 pIC50
Reference (Journal): A-ring modifications on the triazafluorenone core structure and their mGluR1 antagonist properties.
Published in: Bioorg Med Chem Lett

Ligand: compound 27 [PMID: 20346665] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.1 pKi
Reference (Journal): A-ring modifications on the triazafluorenone core structure and their mGluR1 antagonist properties.
Published in: Bioorg Med Chem Lett

Ligand: compound 29 [PMID: 17064898] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.03 pKi
Reference (Journal): Structure-activity relationships of novel non-competitive mGluR1 antagonists: a potential treatment for chronic pain.
Published in: Bioorg Med Chem Lett

Ligand: compound 29 [PMID: 17064898] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.05 pIC50
Reference (Journal): Structure-activity relationships of novel non-competitive mGluR1 antagonists: a potential treatment for chronic pain.
Published in: Bioorg Med Chem Lett

Ligand: compound 2f [PMID: 17532216] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 6.9 pKi
Reference (Journal): Rapid hit to lead evaluation of pyrazolo[3,4-d]pyrimidin-4-one as selective and orally bioavailable mGluR1 antagonists.
Published in: Bioorg Med Chem Lett

Ligand: compound 32 [PMID: 19289283] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.22 pIC50
Reference (Journal): In vitro and in vivo SAR of pyrido[3,4-d]pyramid-4-ylamine based mGluR1 antagonists.
Published in: Bioorg Med Chem Lett

Ligand: compound 3a [PMID: 16099654] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.19 pEC50
Reference (Journal): 9H-Xanthene-9-carboxylic acid [1,2,4]oxadiazol-3-yl- and (2H-tetrazol-5-yl)-amides as potent, orally available mGlu1 receptor enhancers.
Published in: Bioorg Med Chem Lett

Ligand: compound 3 [PMID: 12470711] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.8 pIC50
Reference (Journal): Synthesis and pharmacological characterisation of 2,4-dicarboxy-pyrroles as selective non-competitive mGluR1 antagonists.
Published in: Bioorg Med Chem

Ligand: compound 4b [PMID: 16099654] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.19 pEC50
Reference (Journal): 9H-Xanthene-9-carboxylic acid [1,2,4]oxadiazol-3-yl- and (2H-tetrazol-5-yl)-amides as potent, orally available mGlu1 receptor enhancers.
Published in: Bioorg Med Chem Lett

Ligand: compound 9a [PMID: 22266036] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.2 pIC50
Reference (Journal): Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain.
Published in: Bioorg Med Chem Lett

Ligand: compound 9a [PMID: 22266036] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.44 pKi
Reference (Journal): Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain.
Published in: Bioorg Med Chem Lett

Ligand: compound 9n [PMID: 23084894] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.15 pIC50
Reference (Journal): Synthesis and SAR development of novel mGluR1 antagonists for the treatment of chronic pain.
Published in: Bioorg Med Chem Lett

Ligand: CPCCOEt (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 5.3 pKi
Reference (Journal): [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.
Published in: Mol Pharmacol

Ligand: CPCCOEt (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 5.3 pEC50
Reference (Journal): Supersensitivity of human metabotropic glutamate 1a receptor signaling in L929sA cells.
Published in: Mol Pharmacol

Ligand: CPCCOEt (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): CPCCOEt, a noncompetitive metabotropic glutamate receptor 1 antagonist, inhibits receptor signaling without affecting glutamate binding.
Published in: Mol Pharmacol

Ligand: DCG-IV (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.1 pKi
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: DM-PPP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.8 pIC50
Reference (Journal): Synthesis and pharmacological characterisation of 2,4-dicarboxy-pyrroles as selective non-competitive mGluR1 antagonists.
Published in: Bioorg Med Chem

Ligand: EM-TBPC (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 6.900000095367432 pIC50
Reference (Journal): Mutational analysis and molecular modeling of the allosteric binding site of a novel, selective, noncompetitive antagonist of the metabotropic glutamate 1 receptor.
Published in: J Biol Chem

Ligand: EM-TBPC (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 7.769999980926514 pKi
Reference (Journal): Mutational analysis and molecular modeling of the allosteric binding site of a novel, selective, noncompetitive antagonist of the metabotropic glutamate 1 receptor.
Published in: J Biol Chem

Ligand: FITM (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 8.270000457763672 pKi
Reference (Journal): Synthesis and evaluation of novel radioligands for positron emission tomography imaging of metabotropic glutamate receptor subtype 1 (mGluR1) in rodent brain.
Published in: J Med Chem

Ligand: FPTQ (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.9 pKi
Reference (Journal): Synthesis and evaluation of 6-[1-(2-[(18)F]fluoro-3-pyridyl)-5-methyl-1H-1,2,3-triazol-4-yl]quinoline for positron emission tomography imaging of the metabotropic glutamate receptor type 1 in brain.
Published in: Bioorg Med Chem

Ligand: FTIDC (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.32 pIC50
Reference (Journal): Pharmacological characterization of a new, orally active and potent allosteric metabotropic glutamate receptor 1 antagonist, 4-[1-(2-fluoropyridin-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1(2H)-carboxamide (FTIDC).
Published in: J Pharmacol Exp Ther

Ligand: FTIDC (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.24 pIC50
Reference (Journal): Pharmacological characterization of a new, orally active and potent allosteric metabotropic glutamate receptor 1 antagonist, 4-[1-(2-fluoropyridin-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1(2H)-carboxamide (FTIDC).
Published in: J Pharmacol Exp Ther

Ligand: ibotenic acid (Natural product)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): A pharmacological characterization of the mGluR1 alpha subtype of the metabotropic glutamate receptor expressed in a cloned baby hamster kidney cell line.
Published in: Brain Res

Ligand: ibotenic acid (Natural product)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
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: cis-10 [PMID: 15771457] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.03 pIC50
Reference (Journal): Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists.
Published in: J Med Chem

Ligand: (S)-3HPG (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 4.9 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:  pKi
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:  pKi
Reference (Journal): [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.
Published in: Mol Pharmacol

Ligand: JNJ16259685 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 8.899999618530273 pIC50
Reference (Journal): JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist.
Published in: Neuropharmacology

Ligand: JNJ-16567083 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 8.850000381469727 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: L-CCG-I (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.6 pKi
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:  pKi
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:  pKi
Reference (Journal): [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.
Published in: Mol Pharmacol

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: LY341495 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): LY341495 is a nanomolar potent and selective antagonist of group II metabotropic glutamate receptors.
Published in: Neuropharmacology

Ligand: LY367385 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.1 pIC50
Reference (Journal): (+)-2-Methyl-4-carboxyphenylglycine (LY367385) selectively antagonises metabotropic glutamate mGluR1 receptors.
Published in: Bioorg Med Chem Lett

Ligand: LY367385 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.900000095367432 pKi
Reference (Journal): [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.
Published in: Mol Pharmacol

Ligand: LY456066 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.55 pIC50
Reference (Journal): Identification of a novel transmembrane domain involved in the negative modulation of mGluR1 using a newly discovered allosteric mGluR1 antagonist, 3-cyclohexyl-5-fluoro-6-methyl-7-(2-morpholin-4-ylethoxy)-4H-chromen-4-one.
Published in: Neuropharmacology

Ligand: LY456066 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 6.84 pKi
Reference (Journal): Identification of a novel transmembrane domain involved in the negative modulation of mGluR1 using a newly discovered allosteric mGluR1 antagonist, 3-cyclohexyl-5-fluoro-6-methyl-7-(2-morpholin-4-ylethoxy)-4H-chromen-4-one.
Published in: Neuropharmacology

Ligand: LY456236 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 6.900000095367432 pIC50
Reference (Journal): A novel class of succinimide-derived negative allosteric modulators of metabotropic glutamate receptor subtype 1 provides insight into a disconnect in activity between the rat and human receptors.
Published in: ACS Chem Neurosci

Ligand: (+)-MCPG (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 3.8 pKi
Reference (Journal): [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.
Published in: Mol Pharmacol

Ligand: MK-5435 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.37 pIC50
Reference (Journal): Synthesis, characterization, and monkey PET studies of [¹⁸F]MK-1312, a PET tracer for quantification of mGluR1 receptor occupancy by MK-5435.
Published in: Synapse

Ligand: NPS2390 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.9 pKi
Reference (Journal): [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.
Published in: Mol Pharmacol

Ligand: PHCCC (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: quisqualate (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
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: quisqualate (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.
Published in: Mol Pharmacol

Ligand: R214127 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.98 pIC50
Reference (Journal): [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.
Published in: Mol Pharmacol

Ligand: R214127 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.9 pKi
Reference (Journal): [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.
Published in: Mol Pharmacol

Ligand: Ro01-6128 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action, and binding site.
Published in: Proc Natl Acad Sci USA

Ligand: Ro0711401 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.25 pEC50
Reference (Journal): Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides as potent, orally available mGlu1 receptor enhancers.
Published in: Bioorg Med Chem Lett

Ligand: Ro67-4853 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 5.099999904632568 pKi
Reference (Journal): Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action, and binding site.
Published in: Proc Natl Acad Sci USA

Ligand: Ro67-7476 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action, and binding site.
Published in: Proc Natl Acad Sci USA

Ligand: (S)-4CPG (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.4 pKi
Reference (Journal): [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.
Published in: Mol Pharmacol

Ligand: (S)-(+)-CBPG (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 4.199999809265137 pIC50
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: (S)-TBPG (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 4.199999809265137 pIC50
Reference (Journal): Synthesis and biological evaluation of 2-(3'-(1H-tetrazol-5-yl) bicyclo[1.1.1]pent-1-yl)glycine (S-TBPG), a novel mGlu1 receptor antagonist.
Published in: Bioorg Med Chem

Ligand: [11C]JNJ-16567083 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 9.0600004196167 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: [11C]MMTP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.02 pIC50
Reference (Journal): Synthesis, in vitro and in vivo evaluation of [11C]MMTP: a potential PET ligand for mGluR1 receptors.
Published in: Bioorg Med Chem Lett

Ligand: [11C]MMTP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 9.22 pKi
Reference (Journal): Synthesis, in vitro and in vivo evaluation of [11C]MMTP: a potential PET ligand for mGluR1 receptors.
Published in: Bioorg Med Chem Lett

Ligand: [18F]FITM (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.29 pIC50
Reference (Journal): Radiosynthesis and preliminary evaluation of 4-[18F]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as a new positron emission tomography ligand for metabotropic glutamate receptor subtype 1.
Published in: Bioorg Med Chem Lett

Ligand: [18F]FITM (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 9.06 pKi
Reference (Journal): Radiosynthesis and preliminary evaluation of 4-[18F]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as a new positron emission tomography ligand for metabotropic glutamate receptor subtype 1.
Published in: Bioorg Med Chem Lett

Ligand: [18F]FPIT (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.27 pIC50
Reference (Journal): Characterization of 1-(2-[18F] fluoro-3-pyridyl)-4-(2-isopropyl-1-oxo- isoindoline-5-yl)-5-methyl-1H-1,2,3-triazole, a PET ligand for imaging the metabotropic glutamate receptor type 1 in rat and monkey brains.
Published in: J Neurochem

Ligand: [18F]MK-1312 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.44 pIC50
Reference (Journal): Synthesis, characterization, and monkey PET studies of [¹⁸F]MK-1312, a PET tracer for quantification of mGluR1 receptor occupancy by MK-5435.
Published in: Synapse

Ligand: [3H]EM-TBPC (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 8.2 pKd
Reference (Journal): Mutational analysis and molecular modeling of the allosteric binding site of a novel, selective, noncompetitive antagonist of the metabotropic glutamate 1 receptor.
Published in: J Biol Chem

Ligand: [3H]quisqualate (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Mutational analysis and molecular modeling of the allosteric binding site of a novel, selective, noncompetitive antagonist of the metabotropic glutamate 1 receptor.
Published in: J Biol Chem

Ligand: [3H]quisqualate (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.
Published in: Mol Pharmacol

Ligand: [3H]R214127 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 9 pKd
Reference (Journal): [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.
Published in: Mol Pharmacol

Ligand: [3H]YM298198 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.49 pKd
Reference (Journal): Radioligand binding properties and pharmacological characterization of 6-amino-N-cyclohexyl-N,3-dimethylthiazolo[3,2-a]benzimidazole-2-carboxamide (YM-298198), a high-affinity, selective, and noncompetitive antagonist of metabotropic glutamate receptor type 1.
Published in: J Pharmacol Exp Ther

Ligand: VU0469650 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7 pIC50
Reference (Journal): N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats.
Published in: Bioorg Med Chem Lett

Ligand: VU0483605 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 6.409999847412109 pEC50
Reference (Journal): Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenics.
Published in: ACS Chem Biol

Ligand: VU0483605 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 6.019999980926514 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-71 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 5.62 pEC50
Reference (Journal): 9H-Xanthene-9-carboxylic acid [1,2,4]oxadiazol-3-yl- and (2H-tetrazol-5-yl)-amides as potent, orally available mGlu1 receptor enhancers.
Published in: Bioorg Med Chem Lett

Ligand: YM-202074 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.7 pKi
Reference (Journal): Neuroprotective effects of the selective type 1 metabotropic glutamate receptor antagonist YM-202074 in rat stroke models.
Published in: Brain Res

Ligand: YM-202074 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.07 pIC50
Reference (Journal): Neuroprotective effects of the selective type 1 metabotropic glutamate receptor antagonist YM-202074 in rat stroke models.
Published in: Brain Res

Ligand: YM298198 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pIC50
Reference (Journal): Radioligand binding properties and pharmacological characterization of 6-amino-N-cyclohexyl-N,3-dimethylthiazolo[3,2-a]benzimidazole-2-carboxamide (YM-298198), a high-affinity, selective, and noncompetitive antagonist of metabotropic glutamate receptor type 1.
Published in: J Pharmacol Exp Ther

Ligand: YM298198 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 6.92 pIC50
Reference (Journal): Identification of a novel transmembrane domain involved in the negative modulation of mGluR1 using a newly discovered allosteric mGluR1 antagonist, 3-cyclohexyl-5-fluoro-6-methyl-7-(2-morpholin-4-ylethoxy)-4H-chromen-4-one.
Published in: Neuropharmacology