Target Validation Information
Target ID T99347
Target Name Metabotropic glutamate receptor 5
Target Type
Clinical Trial
Drug Potency against Target 2-(3-bromophenyl)pyrido[2,3-d]pyrimidine Drug Info IC50 = 333 nM [528998]
4-(2-Methyl-thiazol-4-ylethynyl)-pyridine Drug Info IC50 = 127 nM [527127]
5-Chloro-2-(2-methylquinolin-7-yl)benzonitrile Drug Info IC50 = 9150 nM [530843]
QUISQUALATE Drug Info IC50 = 25 nM [534590]
3-chloro-N-(6-chloropyridin-2-yl)benzamide Drug Info IC50 = 1530 nM [528186]
7-(3-(methoxymethyl)phenyl)-2-methylquinoline Drug Info IC50 = 5800 nM [528922]
3-fluoro-5-(1,6-naphthyridin-7-yl)benzonitrile Drug Info IC50 = 1590 nM [529101]
3-chloro-5-(2-methylquinolin-7-yl)benzonitrile Drug Info IC50 = 1.4 nM [528922]
2-phenyl-1,8-naphthyridine Drug Info IC50 = 1840 nM [529101]
5-Biphenyl-4-ylethynyl-pyrimidine Drug Info IC50 = 7800 nM [529531]
3-(1,5-naphthyridin-3-yl)benzonitrile Drug Info IC50 = 18600 nM [529101]
2-Methyl-4-o-tolylethynyl-thiazole Drug Info IC50 = 15 nM [527127]
2-(2-Methyl-thiazol-4-ylethynyl)-pyridine Drug Info IC50 = 53 nM [527127]
N-(3-chlorophenyl)-6-methoxyquinazolin-4-amine Drug Info IC50 = 1510 nM [530473]
(3-(2-methylquinolin-7-yl)phenyl)methanol Drug Info IC50 = 8700 nM [528922]
N-(3-chlorophenyl)-3-cyano-5-fluorobenzamide Drug Info Ki = 206 nM [531010]
3-cyano-5-fluoro-N-(3-fluorophenyl)benzamide Drug Info IC50 = 2160 nM [531010]
4-(2-(4-fluorophenyl)ethynyl)-2-methylthiazole Drug Info IC50 = 2966 nM [528003]
3-methoxy-5-(1,5-naphthyridin-3-yl)benzonitrile Drug Info IC50 = 55 nM [529101]
7-(3-methoxyphenyl)-2-methyl-1,6-naphthyridine Drug Info IC50 = 7900 nM [529101]
2-methyl-6-(phenylethynyl)pyridine Drug Info Ki = 4.7 nM [530473]
2-(3-chlorophenyl)-7-methyl-1,8-naphthyridine Drug Info IC50 = 177 nM [529101]
3-ethoxy-5-(2-methylquinolin-7-yl)benzonitrile Drug Info IC50 = 17 nM [528922]
3-fluoro-5-(2-methylquinolin-7-yl)benzonitrile Drug Info Ki = 22 nM [528922]
3-[(2-methyl-4-thiazolyl)ethynyl]benzonitrile Drug Info Ki = 0.25 nM [528003]
3-(2-methylquinolin-7-yl)phenol Drug Info IC50 = 19000 nM [528922]
3-[(5-ethyl-2-methyl-4-thiazolyl)ethynyl]pyridine Drug Info IC50 = 1243 nM [528003]
1-(3-(2-methylquinolin-7-yl)phenyl)ethanone Drug Info IC50 = 4760 nM [528922]
5-(2-methylquinolin-7-yl)isophthalonitrile Drug Info IC50 = 2 nM [528922]
4-(3-methoxyphenylethynyl)-2-methylthiazole Drug Info IC50 = 49 nM [528003]
2-methyl-7-phenylquinoline Drug Info IC50 = 9000 nM [528922]
7-m-tolyl-1,6-naphthyridine Drug Info IC50 = 1270 nM [529101]
7-(2-methoxyphenyl)-2-methylquinoline Drug Info IC50 = 4200 nM [528922]
N-[4-(3-pyridylethynyl)-2-thiazolyl]acetamide Drug Info IC50 = 1920 nM [528003]
2-(4-(3-chlorophenyl)but-1-ynyl)-6-methylpyridine Drug Info IC50 = 5 nM [528307]
2-Methyl-4-p-tolylethynyl-thiazole Drug Info IC50 = 845 nM [527127]
3-methyl-N-(6-methylpyridin-2-yl)benzamide Drug Info IC50 = 1840 nM [528186]
7-(3,5-dimethoxyphenyl)-1,6-naphthyridine Drug Info IC50 = 6070 nM [529101]
3-(2-methylquinolin-7-yl)benzonitrile Drug Info Ki = 72 nM [528922]
2-methyl-6-(3-(p-tolyloxy)prop-1-ynyl)pyridine Drug Info IC50 = 115 nM [528311]
5-(2-Methylquinolin-7-yl)-2-phenylbenzonitrile Drug Info IC50 = 1250 nM [530843]
7-(3-fluoro-5-methylphenyl)-1,6-naphthyridine Drug Info IC50 = 6570 nM [529101]
7-methyl-2-phenylpyrido[2,3-d]pyrimidine Drug Info IC50 = 2700 nM [528998]
3-chloro-N-(6-methylpyridin-2-yl)benzamide Drug Info IC50 = 1870 nM [530140]
4-(3-fluorophenylethynyl)-2-thiazolylamine Drug Info IC50 = 78.6 nM [528003]
2-(3,5-difluorophenyl)-7-methyl-1,8-naphthyridine Drug Info IC50 = 181 nM [529101]
SIB-1757 Drug Info IC50 = 1170 nM [528186]
(E)-3-[2-(2-methyl-4-thiazolyl)vinyl]pyridine Drug Info IC50 = 3090 nM [528003]
4-Biphenyl-4-ylethynyl-2-methyl-thiazole Drug Info IC50 = 22 nM [527127]
4-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide Drug Info Ki = 1560 nM [528212]
2-(2-methylquinolin-7-yl)benzonitrile Drug Info IC50 = 9800 nM [528922]
2-methyl-7-m-tolyl-1,6-naphthyridine Drug Info IC50 = 676 nM [529101]
4-(2-methoxyphenylethynyl)-2-methylthiazole Drug Info IC50 = 36.3 nM [528003]
3-hydroxy-5-(2-methylquinolin-7-yl)benzonitrile Drug Info IC50 = 360 nM [528922]
3-cyano-N-(3-ethynylphenyl)-5-fluorobenzamide Drug Info IC50 = 331 nM [531010]
N-(6-methylpyridin-2-yl)biphenyl-3-carboxamide Drug Info Ki = 7300 nM [530140]
2-bromo-4-(3-fluorophenylethynyl)thiazole Drug Info IC50 = 526 nM [528003]
2-ethynyl-4-(3-fluorophenylethynyl)thiazole Drug Info IC50 = 2920 nM [528003]
3-chloro-N-(4-methylthiazol-2-yl)benzamide Drug Info IC50 = 5490 nM [528186]
5-(2-(3,5-difluorophenyl)ethynyl)pyrimidine Drug Info IC50 = 6400 nM [529531]
N-(3-(3-cyanobenzamido)phenyl)-2-methoxybenzamide Drug Info IC50 = 1800 nM [530486]
7-bromo-N-(3-bromophenyl)isoquinolin-1-amine Drug Info IC50 = 4330 nM [530473]
3-bromo-5-[(2-methyl-4-thiazolyl)ethynyl]pyridine Drug Info IC50 = 60 nM [528003]
3-bromo-5-(2-methylquinolin-7-yl)benzonitrile Drug Info IC50 = 13 nM [528922]
2-methyl-4-(m-tolylethynyl)thiazole Drug Info IC50 = 82.6 nM [528003]
2-methyl-4-(3-thienylethynyl)thiazole Drug Info IC50 = 337 nM [528003]
3-bromo-N-(6-methylpyridin-2-yl)benzamide Drug Info IC50 = 650 nM [528186]
3-cyano-5-fluoro-N-(pyridin-2-yl)benzamide Drug Info IC50 = 3010 nM [531010]
5-(2-(3-chlorophenyl)ethynyl)pyrimidine Drug Info IC50 = 34 nM [529531]
2-phenylethynyl-5,6,7,8-tetrahydro-quinoline Drug Info Ki = 1500 nM [529241]
3-iodo-N-(6-methylpyridin-2-yl)benzamide Drug Info IC50 = 1080 nM [528186]
4-(2-fluorophenylethynyl)-2-methylthiazole Drug Info IC50 = 140 nM [528003]
6-bromo-N-(3-chlorophenyl)quinazolin-4-amine Drug Info Ki = 116 nM [530473]
3-cyano-N-(3-ethylphenyl)-5-fluorobenzamide Drug Info IC50 = 4940 nM [531010]
2-phenylethynyl-5,6,7,8-tetrahydro-quinolin-5-ol Drug Info Ki = 7600 nM [529241]
3-(7-methyl-1,8-naphthyridin-2-yl)benzonitrile Drug Info IC50 = 480 nM [529101]
6-chloro-N-(3-chlorophenyl)quinazolin-4-amine Drug Info IC50 = 130 nM [530473]
N-(3-bromophenyl)-6-chloroquinazolin-4-amine Drug Info Ki = 249 nM [530473]
6-bromo-N-(3-fluorophenyl)quinazolin-4-amine Drug Info IC50 = 1970 nM [530473]
N-(3-chlorophenyl)-6-nitroquinazolin-4-amine Drug Info IC50 = 274 nM [530473]
3-(3-Pyridin-2-yl-pyrazol-1-yl)-benzonitrile Drug Info Ki = 530 nM [527190]
3-(3-Pyridin-2-yl-pyrrol-1-yl)-benzonitrile Drug Info IC50 = 190 nM [527190]
7-(3-methoxyphenyl)-2-methylquinoline Drug Info IC50 = 860 nM [528922]
2-(3-chlorobenzyloxy)-6-chloroisonicotinonitrile Drug Info Ki = 5 nM [527989]
7-(4,6-dimethoxypyrimidin-2-yl)-2-methylquinoline Drug Info Ki = 5430 nM [528793]
3-Phenyl-1-(2-methylthiazol-4-ylethynyl)benzene Drug Info IC50 = 3.05 nM [530140]
3-methoxy-5-(1,6-naphthyridin-7-yl)benzonitrile Drug Info IC50 = 68 nM [529101]
3-[(6-Methylpyridin-2-yl)ethynyl]benzonitrile Drug Info IC50 = 0.415 nM [530140]
2-(3,4-dimethylphenyl)-1,8-naphthyridine Drug Info IC50 = 45 nM [529101]
2-methyl-4-(2-thienylethynyl)thiazole Drug Info IC50 = 475 nM [528003]
3-[(2-methyl-4-thiazolyl)ethynyl]benzamide Drug Info IC50 = 1000 nM [528003]
4-(3-bromophenoxy)-6-chloroquinazoline Drug Info IC50 = 6570 nM [530473]
6-fluoro-N-m-tolylquinazolin-4-amine Drug Info IC50 = 1350 nM [530473]
2-methyl-7-m-tolylquinoline Drug Info IC50 = 3400 nM [528922]
2-methyl-7-(pyridin-3-yl)quinoline Drug Info IC50 = 510 nM [528922]
3-(1-Pyridin-2-yl-1H-pyrazol-4-yl)-benzonitrile Drug Info IC50 = 890 nM [527190]
3-[(2,5-dimethyl-4-thiazolyl)ethynyl]pyridine Drug Info IC50 = 698 nM [528003]
7-(3-fluorophenyl)-2-methylquinoline Drug Info IC50 = 1800 nM [528922]
3-(3,4-dimethylphenyl)-1,5-naphthyridine Drug Info IC50 = 12000 nM [529101]
5-((6-Methylpyridin-2-yl)ethynyl)nicotinonitrile Drug Info IC50 = 13 nM [530843]
3-(1,8-naphthyridin-2-yl)benzonitrile Drug Info IC50 = 115 nM [529101]
2-(3-bromophenyl)-7-methyl-1,8-naphthyridine Drug Info IC50 = 47.9 nM [529101]
3-methoxy-5-(2-methylquinolin-7-yl)benzonitrile Drug Info IC50 = 2.4 nM [528922]
3-[(2-methyl-4-thiazolyl)ethynyl]-5-vinylpyridine Drug Info Ki = 0.71 nM [528003]
2-methyl-6-(4-phenylpent-1-ynyl)pyridine Drug Info IC50 = 59 nM [528307]
7-(3-chlorophenyl)-2-methylquinoline Drug Info IC50 = 14000 nM [528922]
4-(3-chlorophenylethynyl)-2-methylthiazole Drug Info IC50 = 129 nM [528003]
3-(2-Pyridin-2-yl-2H-tetrazol-5-yl)-benzonitrile Drug Info Ki = 450 nM [527190]
3-(5-Pyridin-2-yl-tetrazol-2-yl)-benzonitrile Drug Info Ki = 190 nM [527190]
2-Phenyl-5-(2-methylthiazol-4ylethynyl)pyridine Drug Info IC50 = 1.21 nM [530140]
3-isobutoxy-5-(2-methylquinolin-7-yl)benzonitrile Drug Info IC50 = 12000 nM [528922]
3-methyl-5-(2-methylquinolin-7-yl)benzonitrile Drug Info IC50 = 1.6 nM [528922]
2-methyl-7-phenyl-1,8-naphthyridine Drug Info IC50 = 664 nM [529101]
5-(3-chlorophenylethynyl)-5-methyl[1,2,4]triazine Drug Info IC50 = 4.2 nM [528893]
3-(1-Pyridin-2-yl-1H-pyrrol-3-yl)-benzonitrile Drug Info IC50 = 4620 nM [527190]
SIB-1893 Drug Info IC50 = 1080 nM [528186]
5-(2-m-tolylethynyl)pyrimidine Drug Info IC50 = 7 nM [529531]
N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide Drug Info Ki = 4180 nM [528212]
4-nitro-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide Drug Info Ki = 250 nM [528212]
5-(2-methylquinolin-7-yl)nicotinonitrile Drug Info IC50 = 23 nM [528922]
2-Benzoxy-5-(2-methylquinolin-7-yl)benzonitrile Drug Info Ki = 1040 nM [530843]
3-cyano-5-fluoro-N-m-tolylbenzamide Drug Info Ki = 100 nM [531010]
N-(2-phenylimidazo[1,2-a]pyridin-3-yl)benzamide Drug Info Ki = 1990 nM [528212]
3-m-tolyl-1,5-naphthyridine Drug Info IC50 = 15700 nM [529101]
7-methyl-2-m-tolylpyrido[2,3-d]pyrimidine Drug Info IC50 = 53 nM [528998]
3-biphenyl-4-ylethynyl-5-methyl-[1,2,4]triazine Drug Info IC50 = 510 nM [528893]
2-(3-(3-methoxyphenoxy)prop-1-ynyl)pyridine Drug Info IC50 = 1540 nM [528311]
2-[(2-methyl-4-thiazolyl)ethynyl]pyrazine Drug Info IC50 = 1830 nM [528003]
4-(2-(3-fluorophenyl)ethynyl)-2-methylthiazole Drug Info IC50 = 23 nM [528003]
4-(4-chlorophenylthio)-2-(pyridin-2-yl)pyrimidine Drug Info IC50 = 320 nM [528038]
5-[(2-methyl-4-thiazolyl)ethynyl]pyrimidine Drug Info IC50 = 946 nM [528003]
3-nitro-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide Drug Info Ki = 2220 nM [528212]
2-(pyridin-2-yl)-4-(m-tolylthio)pyrimidine Drug Info IC50 = 2300 nM [528038]
4-(3,5-difluorophenylethynyl)-2-methylthiazole Drug Info IC50 = 25.3 nM [528003]
3-[(2-methyl-4-thiazolyl)ethynyl]phenol Drug Info IC50 = 654 nM [528003]
2-Cyclohex-1-enylethynyl-pyridine Drug Info IC50 = 2.4 nM [527696]
3-cyano-N-(1,4-diphenyl-1H-pyrazol-5-yl)benzamide Drug Info Ki = 1200 nM [528212]
2-methyl-7-m-tolyl-1,8-naphthyridine Drug Info IC50 = 277 nM [529101]
2-(3,5-dimethoxyphenyl)-1,8-naphthyridine Drug Info IC50 = 67 nM [529101]
3-(4-Pyridin-2-yl-pyrazol-1-yl)-benzonitrile Drug Info Ki = 250 nM [527190]
4-(3-pyridylethynyl)-2-thiazolylamine Drug Info IC50 = 789 nM [528003]
6-bromo-N-(3-bromophenyl)quinazolin-4-amine Drug Info IC50 = 174 nM [530473]
3-cyano-5-fluoro-N-phenylbenzamide Drug Info IC50 = 5440 nM [531010]
3-cyano-N-(6-ethylpyridin-2-yl)-5-fluorobenzamide Drug Info IC50 = 505 nM [531010]
GLUTAMATE Drug Info Ki = 390 nM [529001]
ADX10059 Drug Info IC50 = 17.1 nM [553028]
2-methyl-6-((3-methoxyphenyl)ethynyl)-pyridine Drug Info Ki = 11 nM [528525]
6-(4-chlorophenylamino)-N,N-diethylnicotinamide Drug Info IC50 = 460 nM [530531]
6-bromo-N-m-tolylquinazolin-4-amine Drug Info IC50 = 246 nM [530473]
2-methyl-4-(pyridin-3-ylethynyl)thiazole Drug Info Ki = 16 nM [530843]
7-(4,6-dimethylpyrimidin-2-yl)-2-methylquinoline Drug Info Ki = 2090 nM [528793]
3-(1-Pyridin-2-yl-1H-pyrazol-3-yl)-benzonitrile Drug Info IC50 = 3600 nM [527190]
2-m-tolyl-1,8-naphthyridine Drug Info IC50 = 225 nM [529101]
3-methoxy-N-(6-methylpyridin-2-yl)benzamide Drug Info IC50 = 9760 nM [528186]
7-(4-methoxyphenyl)-2-methylquinoline Drug Info IC50 = 16000 nM [528922]
3-(3-(3-chlorobenzyloxy)-5-methylphenyl)pyridine Drug Info Ki = 58 nM [527989]
2-Cyclopent-1-enylethynyl-pyridine Drug Info IC50 = 3.1 nM [527696]
2-Cyclohexylethynyl-pyridine Drug Info IC50 = 106 nM [527696]
2-(3,5-dichlorophenyl)pyrido[2,3-d]pyrimidine Drug Info IC50 = 228 nM [528998]
2-(3-bromophenyl)-7-methylpyrido[2,3-d]pyrimidine Drug Info IC50 = 38 nM [528998]
2-(3-(2-methylquinolin-7-yl)phenyl)acetonitrile Drug Info IC50 = 430 nM [528922]
6-phenylethynyl-nicotinic acid methyl ester Drug Info Ki = 1400 nM [529241]
4-(3-chlorophenylthio)-2-(pyridin-2-yl)pyrimidine Drug Info IC50 = 620 nM [528038]
3-cyano-N-(3-cyanophenyl)-5-fluorobenzamide Drug Info IC50 = 489 nM [531010]
5-(phenylethynyl)pyrimidine Drug Info IC50 = 480 nM [529531]
(E)-1-Adamantan-1-yl-3-quinolin-3-yl-propenone Drug Info Ki = 807 nM [530245]
N-cyclopentyl-6-(2-phenylethynyl)nicotinamide Drug Info Ki = 1800 nM [530138]
5-(2-(4-fluoro-3-methylphenyl)ethynyl)pyrimidine Drug Info IC50 = 350 nM [529531]
N-(3-bromophenyl)-6-fluoroquinazolin-4-amine Drug Info Ki = 736 nM [530473]
N-(3-chlorophenyl)-6-fluoroquinazolin-4-amine Drug Info IC50 = 311 nM [530473]
2-phenylethynyl-7,8-dihydro-6H-quinolin-5-one Drug Info Ki = 800 nM [529241]
2-benzyloxy-7,8-dihydro-6H-quinolin-5-one Drug Info IC50 = 1900 nM [529241]
3-(4-Pyridin-2-yl-imidazol-1-yl)-benzonitrile Drug Info IC50 = 1150 nM [527190]
5-(2-Methylquinolin-7-yl)-2-phenylnicotinonitrile Drug Info IC50 = 81 nM [530843]
3-methoxy-N-(4-methylthiazol-2-yl)benzamide Drug Info IC50 = 9100 nM [528186]
N-(6-methylpyridin-2-yl)-6-phenylnicotinamide Drug Info Ki = 356 nM [530140]
2-(m-tolylethynyl)pyrimidine Drug Info IC50 = 10.8 nM [530217]
3-cyano-N-(6-methylpyridin-2-yl)benzamide Drug Info IC50 = 490 nM [530140]
5-(2-(2,5-dimethylphenyl)ethynyl)pyrimidine Drug Info IC50 = 11200 nM [529531]
4-Biphenyl-2-ylethynyl-2-methyl-thiazole Drug Info IC50 = 423 nM [527127]
N-(1,4-diphenyl-1H-pyrazol-5-yl)benzamide Drug Info Ki = 1170 nM [528212]
3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide Drug Info Ki = 3760 nM [528212]
2-(3-(benzyloxy)phenyl)isoindoline-1,3-dione Drug Info Ki = 2100 nM [527989]
N-(6-methylpyridin-2-yl)-5-phenylpicolinamide Drug Info Ki = 2800 nM [528711]
2-chloro-N-(3-(3-chlorobenzamido)phenyl)benzamide Drug Info IC50 = 2620 nM [530486]
3-chloro-N-(3-isobutyramidophenyl)benzamide Drug Info IC50 = 5820 nM [530486]
N-(3-acetamidophenyl)-3-chlorobenzamide Drug Info IC50 = 7970 nM [530486]
3-(3-bromophenylethynyl)-5-methyl[1,2,4]triazine Drug Info IC50 = 6 nM [528893]
5-methyl-3-phenylethynyl[1,2,4]triazine Drug Info IC50 = 140 nM [528893]
3-(3-methylphenylethynyl)-5-methyl[1,2,4]triazine Drug Info IC50 = 2.3 nM [528893]
2-Methyl-4-phenylethynyl-thiazole Drug Info IC50 = 4 nM [527127]
2-methyl-6-(5-phenylpent-1-ynyl)pyridine Drug Info IC50 = 258 nM [528307]
2-methyl-6-(4-phenylbut-1-ynyl)pyridine Drug Info IC50 = 78 nM [528307]
2-methyl-6-(3-(phenylthio)prop-1-ynyl)pyridine Drug Info IC50 = 589 nM [528307]
4-(3-bromophenylthio)-2-(pyridin-2-yl)pyrimidine Drug Info IC50 = 2860 nM [528038]
(3-Ethoxy-pyridin-2-yl)-pyridin-2-yl-amine Drug Info IC50 = 138 nM [527656]
3-(2-methylbenzo[d]thiazol-5-yl)benzonitrile Drug Info Ki = 2100 nM [528793]
7-(4-methoxypyrimidin-2-yl)-2-methylquinoline Drug Info Ki = 1550 nM [528793]
2-(phenylethynyl)pyrimidine Drug Info IC50 = 195 nM [530217]
3-(6-fluoroquinazolin-4-ylamino)benzonitrile Drug Info IC50 = 1370 nM [530473]
2-ethoxy-5-(m-tolylethynyl)pyrimidine Drug Info IC50 = 21.1 nM [530217]
Action against Disease Model ADX10059 In preclinical models, antagonism of metabotropic glutamate receptor 5 (mGluR5) by such as agents as ADX10059 (a potent, selective, negative allosteric modulator of mGluR5) reduces transient lower oesophageal sphincter relaxations (TLOSRs) and increases LOS pressure. [537360] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations The control AMPA/NMDA EPSC ratio is reduced in mGlu5-deficient mice compared to wild-types. Moreover, cocaine-induced enhancement of this EPSC ratio is also absent in mutant mice, which suggests that mGlu5 receptors are required for single-dose cocaine-induced plasticity onto VTA cells. While the temporal profile of hyperactivity to acute cocaine is altered in mGlu5-deficient mice; these mice still develop and express sensitized psychomotor responses to cocaine. These data suggest that the mGlu5 receptor is required for cocaine-induced plasticity in VTA dopaminergic cells. In contrast, the mGlu5 receptor may not be essential for psychostimulant behavioural sensitization; although it probably impacts other aspects drug addiction, such as motivation to self-administer [528998]
References
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Ref 529531Bioorg Med Chem Lett. 2008 Jul 15;18(14):4098-101. Epub 2008 May 29.Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold.
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Ref 527127Bioorg Med Chem Lett. 2004 Aug 2;14(15):3993-6.5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist withanxiolytic activity.
Ref 530473Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. Epub 2009 Oct 9.Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.
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Ref 531010Bioorg Med Chem Lett. 2010 Aug 1;20(15):4390-4. Epub 2010 Jun 15.3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds withCNS exposure in rats.
Ref 531010Bioorg Med Chem Lett. 2010 Aug 1;20(15):4390-4. Epub 2010 Jun 15.3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds withCNS exposure in rats.
Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 529101Bioorg Med Chem Lett. 2007 Dec 1;17(23):6525-8. Epub 2007 Sep 29.Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
Ref 529101Bioorg Med Chem Lett. 2007 Dec 1;17(23):6525-8. Epub 2007 Sep 29.Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
Ref 530473Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. Epub 2009 Oct 9.Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.
Ref 529101Bioorg Med Chem Lett. 2007 Dec 1;17(23):6525-8. Epub 2007 Sep 29.Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
Ref 528922Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. Epub 2007 Jun 10.Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 528922Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. Epub 2007 Jun 10.Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 528922Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. Epub 2007 Jun 10.Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 528922Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. Epub 2007 Jun 10.Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 528922Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. Epub 2007 Jun 10.Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 528922Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. Epub 2007 Jun 10.Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 529101Bioorg Med Chem Lett. 2007 Dec 1;17(23):6525-8. Epub 2007 Sep 29.Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
Ref 528922Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. Epub 2007 Jun 10.Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 528307Bioorg Med Chem Lett. 2006 Sep 15;16(18):4788-91. Epub 2006 Jul 11.Structure-activity relationships for the linker in a series of pyridinyl-alkynes that are antagonists of the metabotropic glutamatereceptor 5 (mGluR5).
Ref 527127Bioorg Med Chem Lett. 2004 Aug 2;14(15):3993-6.5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist withanxiolytic activity.
Ref 528186Bioorg Med Chem Lett. 2006 Jul 1;16(13):3371-5. Epub 2006 May 5.Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 529101Bioorg Med Chem Lett. 2007 Dec 1;17(23):6525-8. Epub 2007 Sep 29.Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
Ref 528922Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. Epub 2007 Jun 10.Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 528311Bioorg Med Chem Lett. 2006 Sep 15;16(18):4792-5. Epub 2006 Jul 12.A new series of pyridinyl-alkynes as antagonists of the metabotropic glutamate receptor 5 (mGluR5).
Ref 530843Bioorg Med Chem. 2010 May 1;18(9):3026-35. Epub 2010 Mar 27.Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5.
Ref 529101Bioorg Med Chem Lett. 2007 Dec 1;17(23):6525-8. Epub 2007 Sep 29.Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
Ref 528998Bioorg Med Chem Lett. 2007 Oct 1;17(19):5396-9. Epub 2007 Aug 6.Synthesis and SAR of 2-aryl pyrido[2,3-d]pyrimidines as potent mGlu5 receptor antagonists.
Ref 530140J Med Chem. 2009 Jun 11;52(11):3563-75.Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists.
Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 529101Bioorg Med Chem Lett. 2007 Dec 1;17(23):6525-8. Epub 2007 Sep 29.Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
Ref 528186Bioorg Med Chem Lett. 2006 Jul 1;16(13):3371-5. Epub 2006 May 5.Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 527127Bioorg Med Chem Lett. 2004 Aug 2;14(15):3993-6.5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist withanxiolytic activity.
Ref 528212J Med Chem. 2006 Jun 1;49(11):3332-44.Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes.
Ref 528922Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. Epub 2007 Jun 10.Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 529101Bioorg Med Chem Lett. 2007 Dec 1;17(23):6525-8. Epub 2007 Sep 29.Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 528922Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. Epub 2007 Jun 10.Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 531010Bioorg Med Chem Lett. 2010 Aug 1;20(15):4390-4. Epub 2010 Jun 15.3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds withCNS exposure in rats.
Ref 530140J Med Chem. 2009 Jun 11;52(11):3563-75.Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists.
Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 528186Bioorg Med Chem Lett. 2006 Jul 1;16(13):3371-5. Epub 2006 May 5.Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 529531Bioorg Med Chem Lett. 2008 Jul 15;18(14):4098-101. Epub 2008 May 29.Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold.
Ref 530486Bioorg Med Chem Lett. 2009 Dec 1;19(23):6502-6. Epub 2009 Oct 28.Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS.
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Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 528922Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. Epub 2007 Jun 10.Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 528186Bioorg Med Chem Lett. 2006 Jul 1;16(13):3371-5. Epub 2006 May 5.Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 531010Bioorg Med Chem Lett. 2010 Aug 1;20(15):4390-4. Epub 2010 Jun 15.3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds withCNS exposure in rats.
Ref 529531Bioorg Med Chem Lett. 2008 Jul 15;18(14):4098-101. Epub 2008 May 29.Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold.
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Ref 528186Bioorg Med Chem Lett. 2006 Jul 1;16(13):3371-5. Epub 2006 May 5.Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 530473Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. Epub 2009 Oct 9.Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.
Ref 531010Bioorg Med Chem Lett. 2010 Aug 1;20(15):4390-4. Epub 2010 Jun 15.3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds withCNS exposure in rats.
Ref 529241J Med Chem. 2008 Feb 14;51(3):634-47. Epub 2008 Jan 4.Positive and negative modulation of group I metabotropic glutamate receptors.
Ref 529101Bioorg Med Chem Lett. 2007 Dec 1;17(23):6525-8. Epub 2007 Sep 29.Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
Ref 530473Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. Epub 2009 Oct 9.Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.
Ref 530473Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. Epub 2009 Oct 9.Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.
Ref 530473Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. Epub 2009 Oct 9.Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.
Ref 530473Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. Epub 2009 Oct 9.Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.
Ref 527190J Med Chem. 2004 Sep 9;47(19):4645-8.Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity.
Ref 527190J Med Chem. 2004 Sep 9;47(19):4645-8.Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity.
Ref 528922Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. Epub 2007 Jun 10.Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 527989Bioorg Med Chem Lett. 2006 Apr 1;16(7):1892-7. Epub 2006 Jan 24.Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists.
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Ref 530140J Med Chem. 2009 Jun 11;52(11):3563-75.Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists.
Ref 529101Bioorg Med Chem Lett. 2007 Dec 1;17(23):6525-8. Epub 2007 Sep 29.Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
Ref 530140J Med Chem. 2009 Jun 11;52(11):3563-75.Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists.
Ref 529101Bioorg Med Chem Lett. 2007 Dec 1;17(23):6525-8. Epub 2007 Sep 29.Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 530473Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. Epub 2009 Oct 9.Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.
Ref 530473Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. Epub 2009 Oct 9.Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.
Ref 528922Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. Epub 2007 Jun 10.Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 528922Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. Epub 2007 Jun 10.Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 527190J Med Chem. 2004 Sep 9;47(19):4645-8.Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity.
Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 528922Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. Epub 2007 Jun 10.Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 529101Bioorg Med Chem Lett. 2007 Dec 1;17(23):6525-8. Epub 2007 Sep 29.Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
Ref 530843Bioorg Med Chem. 2010 May 1;18(9):3026-35. Epub 2010 Mar 27.Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5.
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Ref 529101Bioorg Med Chem Lett. 2007 Dec 1;17(23):6525-8. Epub 2007 Sep 29.Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
Ref 528922Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. Epub 2007 Jun 10.Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 528307Bioorg Med Chem Lett. 2006 Sep 15;16(18):4788-91. Epub 2006 Jul 11.Structure-activity relationships for the linker in a series of pyridinyl-alkynes that are antagonists of the metabotropic glutamatereceptor 5 (mGluR5).
Ref 528922Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. Epub 2007 Jun 10.Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 527190J Med Chem. 2004 Sep 9;47(19):4645-8.Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity.
Ref 527190J Med Chem. 2004 Sep 9;47(19):4645-8.Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity.
Ref 530140J Med Chem. 2009 Jun 11;52(11):3563-75.Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists.
Ref 528922Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. Epub 2007 Jun 10.Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 528922Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. Epub 2007 Jun 10.Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 529101Bioorg Med Chem Lett. 2007 Dec 1;17(23):6525-8. Epub 2007 Sep 29.Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
Ref 528893J Med Chem. 2007 Jul 12;50(14):3388-91. Epub 2007 Jun 15.Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine.
Ref 527190J Med Chem. 2004 Sep 9;47(19):4645-8.Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity.
Ref 528186Bioorg Med Chem Lett. 2006 Jul 1;16(13):3371-5. Epub 2006 May 5.Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 529531Bioorg Med Chem Lett. 2008 Jul 15;18(14):4098-101. Epub 2008 May 29.Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold.
Ref 528212J Med Chem. 2006 Jun 1;49(11):3332-44.Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes.
Ref 528212J Med Chem. 2006 Jun 1;49(11):3332-44.Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes.
Ref 528922Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. Epub 2007 Jun 10.Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 530843Bioorg Med Chem. 2010 May 1;18(9):3026-35. Epub 2010 Mar 27.Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5.
Ref 531010Bioorg Med Chem Lett. 2010 Aug 1;20(15):4390-4. Epub 2010 Jun 15.3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds withCNS exposure in rats.
Ref 528212J Med Chem. 2006 Jun 1;49(11):3332-44.Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes.
Ref 529101Bioorg Med Chem Lett. 2007 Dec 1;17(23):6525-8. Epub 2007 Sep 29.Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
Ref 528998Bioorg Med Chem Lett. 2007 Oct 1;17(19):5396-9. Epub 2007 Aug 6.Synthesis and SAR of 2-aryl pyrido[2,3-d]pyrimidines as potent mGlu5 receptor antagonists.
Ref 528893J Med Chem. 2007 Jul 12;50(14):3388-91. Epub 2007 Jun 15.Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine.
Ref 528311Bioorg Med Chem Lett. 2006 Sep 15;16(18):4792-5. Epub 2006 Jul 12.A new series of pyridinyl-alkynes as antagonists of the metabotropic glutamate receptor 5 (mGluR5).
Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
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Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 528212J Med Chem. 2006 Jun 1;49(11):3332-44.Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes.
Ref 528038Bioorg Med Chem Lett. 2006 May 1;16(9):2467-9. Epub 2006 Feb 14.Structure-activity relationship of thiopyrimidines as mGluR5 antagonists.
Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 527696Bioorg Med Chem Lett. 2005 Oct 15;15(20):4589-93.Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.
Ref 528212J Med Chem. 2006 Jun 1;49(11):3332-44.Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes.
Ref 529101Bioorg Med Chem Lett. 2007 Dec 1;17(23):6525-8. Epub 2007 Sep 29.Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
Ref 529101Bioorg Med Chem Lett. 2007 Dec 1;17(23):6525-8. Epub 2007 Sep 29.Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
Ref 527190J Med Chem. 2004 Sep 9;47(19):4645-8.Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity.
Ref 528003J Med Chem. 2006 Feb 9;49(3):1080-100.Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Ref 530473Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. Epub 2009 Oct 9.Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.
Ref 531010Bioorg Med Chem Lett. 2010 Aug 1;20(15):4390-4. Epub 2010 Jun 15.3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds withCNS exposure in rats.
Ref 531010Bioorg Med Chem Lett. 2010 Aug 1;20(15):4390-4. Epub 2010 Jun 15.3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds withCNS exposure in rats.
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Ref 537360A Proof Of Concept Study Evaluating The Effect Of ADX10059, A Metabotropic Glutamate Receptor-5 Negative Allosteric Modulator, On Acid Exposure And Symptoms In Gastro-Esophageal Reflux Disease. Gut. 2009 May 20.
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Ref 527190J Med Chem. 2004 Sep 9;47(19):4645-8.Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity.
Ref 529101Bioorg Med Chem Lett. 2007 Dec 1;17(23):6525-8. Epub 2007 Sep 29.Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
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Ref 527696Bioorg Med Chem Lett. 2005 Oct 15;15(20):4589-93.Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.
Ref 527696Bioorg Med Chem Lett. 2005 Oct 15;15(20):4589-93.Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.
Ref 528998Bioorg Med Chem Lett. 2007 Oct 1;17(19):5396-9. Epub 2007 Aug 6.Synthesis and SAR of 2-aryl pyrido[2,3-d]pyrimidines as potent mGlu5 receptor antagonists.
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Ref 528922Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. Epub 2007 Jun 10.Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 529241J Med Chem. 2008 Feb 14;51(3):634-47. Epub 2008 Jan 4.Positive and negative modulation of group I metabotropic glutamate receptors.
Ref 528038Bioorg Med Chem Lett. 2006 May 1;16(9):2467-9. Epub 2006 Feb 14.Structure-activity relationship of thiopyrimidines as mGluR5 antagonists.
Ref 531010Bioorg Med Chem Lett. 2010 Aug 1;20(15):4390-4. Epub 2010 Jun 15.3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds withCNS exposure in rats.
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Ref 530245Bioorg Med Chem. 2009 Aug 1;17(15):5708-15. Epub 2009 Jun 23.Synergism of virtual screening and medicinal chemistry: identification and optimization of allosteric antagonists of metabotropic glutamate receptor 1.
Ref 530138Bioorg Med Chem Lett. 2009 Jun 15;19(12):3275-8. Epub 2009 Apr 24.Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator.
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Ref 530473Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. Epub 2009 Oct 9.Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.
Ref 530473Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. Epub 2009 Oct 9.Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.
Ref 529241J Med Chem. 2008 Feb 14;51(3):634-47. Epub 2008 Jan 4.Positive and negative modulation of group I metabotropic glutamate receptors.
Ref 529241J Med Chem. 2008 Feb 14;51(3):634-47. Epub 2008 Jan 4.Positive and negative modulation of group I metabotropic glutamate receptors.
Ref 527190J Med Chem. 2004 Sep 9;47(19):4645-8.Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity.
Ref 530843Bioorg Med Chem. 2010 May 1;18(9):3026-35. Epub 2010 Mar 27.Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5.
Ref 528186Bioorg Med Chem Lett. 2006 Jul 1;16(13):3371-5. Epub 2006 May 5.Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists.
Ref 530140J Med Chem. 2009 Jun 11;52(11):3563-75.Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists.
Ref 530217J Med Chem. 2009 Jul 23;52(14):4103-6.Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines.
Ref 530140J Med Chem. 2009 Jun 11;52(11):3563-75.Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists.
Ref 529531Bioorg Med Chem Lett. 2008 Jul 15;18(14):4098-101. Epub 2008 May 29.Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold.
Ref 527127Bioorg Med Chem Lett. 2004 Aug 2;14(15):3993-6.5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist withanxiolytic activity.
Ref 528212J Med Chem. 2006 Jun 1;49(11):3332-44.Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes.
Ref 528212J Med Chem. 2006 Jun 1;49(11):3332-44.Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes.
Ref 527989Bioorg Med Chem Lett. 2006 Apr 1;16(7):1892-7. Epub 2006 Jan 24.Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists.
Ref 528711Bioorg Med Chem Lett. 2007 Apr 1;17(7):2074-9. Epub 2007 Jan 4.Design and synthesis of novel heterobiaryl amides as metabotropic glutamate receptor subtype 5 antagonists.
Ref 530486Bioorg Med Chem Lett. 2009 Dec 1;19(23):6502-6. Epub 2009 Oct 28.Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS.
Ref 530486Bioorg Med Chem Lett. 2009 Dec 1;19(23):6502-6. Epub 2009 Oct 28.Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS.
Ref 530486Bioorg Med Chem Lett. 2009 Dec 1;19(23):6502-6. Epub 2009 Oct 28.Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS.
Ref 528893J Med Chem. 2007 Jul 12;50(14):3388-91. Epub 2007 Jun 15.Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine.
Ref 528893J Med Chem. 2007 Jul 12;50(14):3388-91. Epub 2007 Jun 15.Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine.
Ref 528893J Med Chem. 2007 Jul 12;50(14):3388-91. Epub 2007 Jun 15.Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine.
Ref 527127Bioorg Med Chem Lett. 2004 Aug 2;14(15):3993-6.5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist withanxiolytic activity.
Ref 528307Bioorg Med Chem Lett. 2006 Sep 15;16(18):4788-91. Epub 2006 Jul 11.Structure-activity relationships for the linker in a series of pyridinyl-alkynes that are antagonists of the metabotropic glutamatereceptor 5 (mGluR5).
Ref 528307Bioorg Med Chem Lett. 2006 Sep 15;16(18):4788-91. Epub 2006 Jul 11.Structure-activity relationships for the linker in a series of pyridinyl-alkynes that are antagonists of the metabotropic glutamatereceptor 5 (mGluR5).
Ref 528307Bioorg Med Chem Lett. 2006 Sep 15;16(18):4788-91. Epub 2006 Jul 11.Structure-activity relationships for the linker in a series of pyridinyl-alkynes that are antagonists of the metabotropic glutamatereceptor 5 (mGluR5).
Ref 528038Bioorg Med Chem Lett. 2006 May 1;16(9):2467-9. Epub 2006 Feb 14.Structure-activity relationship of thiopyrimidines as mGluR5 antagonists.
Ref 527656Bioorg Med Chem Lett. 2005 Oct 1;15(19):4350-3.Dipyridyl amines: potent metabotropic glutamate subtype 5 receptor antagonists.
Ref 528793Bioorg Med Chem Lett. 2007 Jun 1;17(11):2987-91. Epub 2007 Mar 24.Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists.
Ref 528793Bioorg Med Chem Lett. 2007 Jun 1;17(11):2987-91. Epub 2007 Mar 24.Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists.
Ref 530217J Med Chem. 2009 Jul 23;52(14):4103-6.Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines.
Ref 530473Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. Epub 2009 Oct 9.Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.
Ref 530217J Med Chem. 2009 Jul 23;52(14):4103-6.Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines.

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