An antagonist at the metabotropic glutamate receptor.
| Member | Definition | Class |
|---|
| 2-amino-3-phosphonopropionic acid | A non-proteinogenc alpha-amino acid that is alanine in which one of the hydrogens of the terminal methyl group has been replaced by a dihydroxy(oxido)-lambda(5)-phosphanyl group. | 2-amino-3-phosphonopropanoic acid |
| 2-methyl-6-(phenylethynyl)pyridine hydrochloride | A hydrochloride salt obtained by reaction of 2-methyl-6-(phenylethynyl)pyridine with one equivalent of hydrochloric acid. Potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and a positive allosteric modulator at mGlu4 receptors. Centrally active following systemic administration in vivo. Reverses mechanical hyperalgesia in the inflamed rat hind paw. | 2-methyl-6-(phenylethynyl)pyridine hydrochloride |
| 6-methyl-2-(phenylethynyl)pyridine | A methylpyridine that coinsists of 2-methylp[yridine bearing an additional phenylethynyl group at position 6. Potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and a positive allosteric modulator at mGlu4 receptors. Centrally active following systemic administration in vivo. Reverses mechanical hyperalgesia in the inflamed rat hind paw. | 2-methyl-6-(phenylethynyl)pyridine |
| alpha-methyl-4-carboxyphenylglycine | A non-proteinogenic alpha-amino acid that is alanine in which the alpha-hydrogen is replaced by a 4-carboxyphenyl group (the S-enantiomer). It is a non-selective group I/group II metabotropic glutamate receptor (mGluR) antagonist. | (S)-alpha-methyl-4-carboxyphenylglycine |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| 15-lipoxygenase, partial | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| 2,3-bisphosphoglycerate-independent phosphoglycerate mutase | Leishmania major strain Friedlin | Potency | 23.9341 | 1 | 1 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 34.2121 | 1 | 2 |
| arylsulfatase A | Homo sapiens (human) | Potency | 37.9330 | 1 | 1 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 8.9521 | 4 | 4 |
| Ataxin-2 | Homo sapiens (human) | Potency | 2.5119 | 1 | 1 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 15.1014 | 1 | 1 |
| atrial natriuretic peptide receptor 1 precursor | Homo sapiens (human) | Potency | 37.9330 | 1 | 1 |
| atrial natriuretic peptide receptor 2 precursor | Homo sapiens (human) | Potency | 18.4927 | 1 | 1 |
| beta-2 adrenergic receptor | Homo sapiens (human) | Potency | 18.3564 | 1 | 1 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 0.2812 | 2 | 4 |
| BRCA1 | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| cellular tumor antigen p53 isoform a | Homo sapiens (human) | Potency | 14.2191 | 2 | 4 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 7.0795 | 1 | 1 |
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 39.8107 | 1 | 1 |
| Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 89.1251 | 1 | 1 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 15.8489 | 1 | 1 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 62.0506 | 2 | 2 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 24.2910 | 1 | 3 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 14.9763 | 1 | 2 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 23.8770 | 1 | 4 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 7.4038 | 2 | 6 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 46.0110 | 1 | 2 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 9.1011 | 4 | 4 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 31.6395 | 1 | 5 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 20.4314 | 4 | 4 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 8.4368 | 1 | 1 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 7.4038 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 7.4038 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 7.4038 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 7.4038 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 7.4038 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 7.4038 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 7.4038 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 7.4038 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 7.4038 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 7.4038 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 7.4038 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 7.4038 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 7.4038 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 7.4038 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 7.4038 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 7.4038 | 1 | 3 |
| geminin | Homo sapiens (human) | Potency | 5.8048 | 1 | 1 |
| GLS protein | Homo sapiens (human) | Potency | 5.6234 | 1 | 1 |
| heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa) | Homo sapiens (human) | Potency | 32.8851 | 1 | 1 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 14.9763 | 1 | 6 |
| Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 2.8184 | 1 | 1 |
| Integrin alpha-IIb | Homo sapiens (human) | Potency | 14.2191 | 1 | 2 |
| Integrin beta-3 | Homo sapiens (human) | Potency | 14.2191 | 1 | 2 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 0.0042 | 1 | 2 |
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 14.5734 | 2 | 3 |
| luciferase | Photuris pensylvanica (Pennsylania firefly) | Potency | 11.9048 | 1 | 2 |
| M-phase phosphoprotein 8 | Homo sapiens (human) | Potency | 56.2341 | 1 | 1 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 13.9480 | 2 | 2 |
| NPC intracellular cholesterol transporter 1 precursor | Homo sapiens (human) | Potency | 4.4836 | 1 | 2 |
| Nrf2 | Homo sapiens (human) | Potency | 25.9290 | 1 | 1 |
| nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 20.5962 | 1 | 1 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 24.8033 | 2 | 2 |
| Ornithine decarboxylase | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1 | 1 |
| parathyroid hormone/parathyroid hormone-related peptide receptor precursor | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| Parkin | Homo sapiens (human) | Potency | 2.9093 | 1 | 1 |
| peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Potency | 19.0115 | 1 | 1 |
| peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 42.6995 | 1 | 2 |
| phosphoglycerate kinase | Trypanosoma brucei brucei TREU927 | Potency | 37.9330 | 1 | 1 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 45.2396 | 1 | 3 |
| plasminogen precursor | Mus musculus (house mouse) | Potency | 10.0000 | 1 | 1 |
| pyruvate kinase | Leishmania mexicana mexicana | Potency | 15.8489 | 2 | 2 |
| pyruvate kinase PKM isoform b | Homo sapiens (human) | Potency | 25.1189 | 2 | 2 |
| ras-related protein Rab-9A | Homo sapiens (human) | Potency | 4.4965 | 1 | 2 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 0.4744 | 1 | 1 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 15.1861 | 1 | 2 |
| TDP1 protein | Homo sapiens (human) | Potency | 17.1611 | 2 | 2 |
| thioredoxin glutathione reductase | Schistosoma mansoni | Potency | 50.1187 | 1 | 1 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 1 |
| Thrombopoietin | Homo sapiens (human) | Potency | 1.0000 | 2 | 2 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 3.9811 | 2 | 2 |
| urokinase plasminogen activator surface receptor precursor | Mus musculus (house mouse) | Potency | 10.0000 | 1 | 1 |
| urokinase-type plasminogen activator precursor | Mus musculus (house mouse) | Potency | 10.0000 | 1 | 1 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 1.7783 | 1 | 1 |