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Metabotropic glutamate receptor 5 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
2-Methyl-6-(phenylethynyl)pyridineIC5022.0 [1]
2-Methyl-4-(pyridin-3-ylethynyl)thiazoleIC505.0 [1], 47.3 [2], 462.0 [3]
2-Methyl-4-(pyridin-3-ylethynyl)thiazoleKi32.7 [1]
FenobamIC5036.3 [1], 43.0 [2], 330.0 [3]
FenobamKi6.76 [1], 31.62 [2], 162.2 [3]
Unii-5900NS9zhiIC5013.0 [1], 133.0 [2]
Unii-5900NS9zhiKi4.9 [1], 10.8 [2], 12.1 [3]
Glutamic acidKi390.0 [1], 1160.0 [2], 4677.35 [3], 11400.0 [4]
(E)-3-(2-(6-Methylpyridin-2-yl)ethynyl)cyclohex-2-enone O-methyl oximeIC502.3 [1], 2.4 [2]
(E)-3-(2-(6-Methylpyridin-2-yl)ethynyl)cyclohex-2-enone O-methyl oximeKi1.7 [1], 3.5 [2]
2-Methyl-6-(2-phenylethenyl)pyridineIC50290.0 [1], 1100.0 [2], 3000.0 [3]
2-Methyl-6-(2-phenylethenyl)pyridineKi290.0 [1]
MavoglurantIC5010.0 [1], 71.6 [2]
MavoglurantKi5.6 [1], 10.0 [2]
3-Fluoro-N-(4-methyl-1,3-thiazol-2-yl)-5-pyrimidin-5-yloxybenzamideIC5023.0 [1], 26.0 [2], 49.0 [3]
3-Fluoro-N-(4-methyl-1,3-thiazol-2-yl)-5-pyrimidin-5-yloxybenzamideKi6.8 [1]
2-Methyl-4-[2-(6-pyridin-3-ylpyridin-3-yl)ethynyl]-1,3-thiazoleIC502.0 [1], 6.1 [2]
2-Methyl-4-[2-(6-pyridin-3-ylpyridin-3-yl)ethynyl]-1,3-thiazoleKi4.7 [1], 5.65 [2]
9-(Dimethylamino)-3-(4-methoxyphenyl)-4-pyrido[1,2]thieno[3,4-d]pyrimidinoneIC503000.0 [1], 10000.0 [2]
CID 6324634IC50300000.0 [1]
CID 6324634Ki300000.0 [1]
3-(3,4-Dimethyl-benzenesulfonyl)-4-(morpholin-4-yl)-quinolineKi52.0 [1]
(5-Chloro-6-((6-methylpyridin-3-yl)amino)pyridin-3-yl)-((2R)-2-ethylpiperidin-1-yl)methanoneIC5032.0 [1], 36.0 [2]
(5-Chloro-6-((6-methylpyridin-3-yl)amino)pyridin-3-yl)-((2R)-2-ethylpiperidin-1-yl)methanoneKi38.0 [1]
N-(1-Methyl-4-oxo-4,5-dihydro-1H-imidazol-2-yl)-N'-phenylureaIC501360.0 [1], 3300.0 [2], 4900.0 [3]
(1E)-1-(1-Methyl-4-oxoimidazolidin-2-ylidene)-3-(3-methylpyridin-2-yl)ureaIC50320.0 [1], 681.0 [2], 1900.0 [3]
2-Methyl-6-[2-[3-(tritritiomethoxymethyl)phenyl]ethynyl]pyridineIC503.6 [1], 7.0 [2], 10.0 [3]
N-[5-[8-[4-[[2-Methoxy-4-[[4-(2-methoxyphenyl)piperazin-1-yl]methyl]phenoxy]methyl]triazol-1-yl]octyl-methylamino]pentyl]-2-[5-[2-(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridin-3-yl]oxyacetamideIC50110.0 [1]
N-[5-[8-[4-[[2-Methoxy-4-[[4-(2-methoxyphenyl)piperazin-1-yl]methyl]phenoxy]methyl]triazol-1-yl]octyl-methylamino]pentyl]-2-[5-[2-(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridin-3-yl]oxyacetamideKi1000.0 [1], 1300.0 [2]
N-[4-[2-[(5-Hydroxy-1,2,3,4-tetrahydronaphthalen-2-yl)-propylamino]ethyl]phenyl]-3-[1-[8-[methyl-[5-[[2-[5-[2-(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridin-3-yl]oxyacetyl]amino]pentyl]amino]octyl]triazol-4-yl]propanamideIC50170.0 [1]
N-[4-[2-[(5-Hydroxy-1,2,3,4-tetrahydronaphthalen-2-yl)-propylamino]ethyl]phenyl]-3-[1-[8-[methyl-[5-[[2-[5-[2-(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridin-3-yl]oxyacetyl]amino]pentyl]amino]octyl]triazol-4-yl]propanamideKi1100.0 [1], 2300.0 [2]
N-[5-[8-Azidooctyl(methyl)amino]pentyl]-2-[5-[2-(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridin-3-yl]oxyacetamideIC502600.0 [1]
N-[5-[8-Azidooctyl(methyl)amino]pentyl]-2-[5-[2-(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridin-3-yl]oxyacetamideKi5700.0 [1], 5800.0 [2]
4-[(S)-Amino(carboxy)methyl]-3-methylbenzoic acidIC50100000.0 [1], 300000.0 [2]
2-[(1s,2s)-2-Carboxycyclopropyl]-3-(9h-Xanthen-9-Yl)-D-AlanineIC508200.0 [1]
2-[(1s,2s)-2-Carboxycyclopropyl]-3-(9h-Xanthen-9-Yl)-D-AlanineKi8200.0 [1]
(2S)-2-Amino-4-phosphonobutanoic acidKi1000000.0 [1]
6-Methyl-2-(phenylazo)-3-pyridinolIC50370.0 [1]
6-Methyl-2-(phenylazo)-3-pyridinolKi370.0 [1]
CtepIC5010.0 [1]
CtepKi20.0 [1]
BasimglurantIC507.0 [1]
BasimglurantKi36.0 [1]
3-[(S)-Amino(carboxy)methyl]bicyclo[1.1.1]pentane-1-carboxylic acidIC50300000.0 [1]
3-[(S)-Amino(carboxy)methyl]bicyclo[1.1.1]pentane-1-carboxylic acidKi103000.0 [1]
FtidcIC506200.0 [1], 10000.0 [2]
(S)-4-CarboxyphenylglycineIC50155000.0 [1]
(S)-4-CarboxyphenylglycineKi2000000.0 [1]
3-Fluoro-5-[5-(pyridin-2-yl)-2H-tetrazol-2-yl]benzonitrileIC503.9 [1], 4.0 [2]
13-(Dimethylamino)-5-(4-ethylphenyl)-8-thia-3,5,10-triazatricyclo[7.4.0.02,7]trideca-1(13),2(7),3,9,11-pentaen-6-oneIC50442.0 [1]
3-(5-Pyridin-2-yl-tetrazol-2-yl)-benzonitrileIC5070.0 [1], 73.0 [2]
2-(2-Methyl-thiazol-4-ylethynyl)-pyridineIC5053.0 [1]
6,6-Dimethyl-2-phenylethynyl-7,8-dihydro-6H-quinolin-5-oneIC5020.0 [1], 23.2 [2]
3-Chloro-5-[6-(5-Fluoropyridin-2-Yl)pyrimidin-4-Yl]benzonitrileIC500.63 [1]
3-Chloro-5-[6-(5-Fluoropyridin-2-Yl)pyrimidin-4-Yl]benzonitrileKi0.5 [1]
3-(3-(Pyridin-2-yl)-1,2,4-oxadiazol-5-yl)benzonitrileIC5043.0 [1], 100.0 [2]
2-Amino-4-(2,2-diphenyl-ethyl)-pentanedioic acidIC50300000.0 [1]
2-Amino-4-(2,2-diphenyl-ethyl)-pentanedioic acidKi300000.0 [1]
3-[(2-Methyl-4-thiazolyl)ethynyl]benzonitrileIC500.94 [1]
3-[(2-Methyl-4-thiazolyl)ethynyl]benzonitrileKi0.37 [1]
[(1R)-1-(6-Methyl-[1,3]thiazolo[3,2-b][1,2,4]triazol-5-yl)ethyl] N-phenylcarbamateIC5039.81 [1], 31622.78 [2]
3-Cyano-N-(6-methylpyridin-2-yl)benzamideIC505330.0 [1]
1-Adamantyl-[4-(1,3-thiazol-2-yl)piperazin-1-yl]methanoneIC50540.0 [1]
1-Adamantyl-[4-(1,3-thiazol-2-yl)piperazin-1-yl]methanoneKi440.0 [1]
(1R,2R)-N-(3-(4-Methoxyphenyl)-4-methyl-5-isothiazolyl)-2-methylcyclopropanecarboxamideIC50158.0 [1]
6-(5-(3-Cyano-5-fluorophenyl)-1,2,4-oxadiazol-3-yl)nicotinonitrileKi17.9 [1], 28.0 [2]
4-[1-(4-Fluoro-phenyl)-2-methyl-1H-imidazol-4-ylethynyl]-2-methyl-pyridineIC5028.0 [1]
4-[1-(4-Fluoro-phenyl)-2-methyl-1H-imidazol-4-ylethynyl]-2-methyl-pyridineKi22.0 [1]
2-Methyl-4-phenylethynyl-thiazoleIC504.0 [1], 6.0 [2]
4-(2-Methyl-thiazol-4-ylethynyl)-pyridineIC50122.0 [1], 127.0 [2]
3-Hydroxy-6-methyl-N-(6-methylpyridin-2-yl)pyridine-2-carboxamideIC507.0 [1]
2-Methyl-4-(m-tolylethynyl)thiazoleIC502.0 [1], 82.6 [2]
1-Benzyl-APDCIC50300000.0 [1]
1-Benzyl-APDCKi600000.0 [1]
4-Fluoro-N-methyl-N-(4-(6-(methylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl)benzamideIC507900.0 [1]
4-Fluoro-N-methyl-N-(4-(6-(methylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl)benzamideKi7900.0 [1]
4-(4-Chloro-phenyl)-3-(4-methyl-benzenesulfonyl)-quinolineKi17.0 [1]
N-Cyclopentyl-6-(2-phenylethynyl)nicotinamideKi1800.0 [1], 3300.0 [2]
3-Phenyl-1-(2-methylthiazol-4-ylethynyl)benzeneIC5041.0 [1]
3-Phenyl-1-(2-methylthiazol-4-ylethynyl)benzeneKi10.76 [1]
2-Phenyl-5-(2-methylthiazol-4ylethynyl)pyridineIC500.5 [1]
2-Phenyl-5-(2-methylthiazol-4ylethynyl)pyridineKi5.49 [1]
1-(3-Chlorophenyl)-3-(1-methyl-5-oxo-4H-imidazol-2-yl)ureaIC5058.0 [1], 10000.0 [2]
[(2R)-2-[6-(3-Chlorophenyl)-4-methylpyridin-3-yl]pyrrolidin-1-yl]-(1,3-thiazol-2-yl)methanoneIC5017.0 [1]
[(2R)-2-[6-(3-Chlorophenyl)-4-methylpyridin-3-yl]pyrrolidin-1-yl]-(1,3-thiazol-2-yl)methanoneKi12.0 [1]
(4R,5R)-5-(3-Fluorophenyl)-4-(5-(phenylethynyl)pyridin-3-yl)oxazolidin-2-oneKi1.5 [1], 1.6 [2]
3-Chloro-4-Fluoro-5-[6-(1h-Pyrazol-1-Yl)pyrimidin-4-Yl]benzonitrileIC502.51 [1]
3-Chloro-4-Fluoro-5-[6-(1h-Pyrazol-1-Yl)pyrimidin-4-Yl]benzonitrileKi0.5 [1]
4-[2-Methyl-4-[2-(2-methylpyridin-4-yl)ethynyl]imidazol-1-yl]benzonitrileIC5070.0 [1]
4-[2-Methyl-4-[2-(2-methylpyridin-4-yl)ethynyl]imidazol-1-yl]benzonitrileKi83.0 [1]
3-[2-Methyl-4-[2-(2-methylpyridin-4-yl)ethynyl]imidazol-1-yl]benzonitrileIC5028.0 [1]
3-[2-Methyl-4-[2-(2-methylpyridin-4-yl)ethynyl]imidazol-1-yl]benzonitrileKi90.0 [1]
2-Methyl-6-(2-(pyridin-3-yl)ethynyl)pyridineIC5010.0 [1], 66.0 [2]
4-[2-[1-(3-Fluorophenyl)-2-methylimidazol-4-yl]ethynyl]-2-methylpyridineIC5012.0 [1]
4-[2-[1-(3-Fluorophenyl)-2-methylimidazol-4-yl]ethynyl]-2-methylpyridineKi17.0 [1]
1-[4-(3-Nitro-2-pyridinyl)piperazino]-3-phenyl-2-propyne-1-oneIC500.9 [1]
1-[4-(3-Nitro-2-pyridinyl)piperazino]-3-phenyl-2-propyne-1-oneKi0.5 [1]
4-[2-[1-(2,4-Difluorophenyl)-2-methylimidazol-4-yl]ethynyl]-2-methylpyridineIC5097.0 [1]
4-[2-[1-(2,4-Difluorophenyl)-2-methylimidazol-4-yl]ethynyl]-2-methylpyridineKi32.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Metabotropic glutamate receptor 5 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.9 May2024https://www.aatbio.com/data-sets/metabotropic-glutamate-receptor-5-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 9). Quest Database™ Metabotropic glutamate receptor 5 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/metabotropic-glutamate-receptor-5-inhibitors-ic50-ki.
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