Target Validation Information
TTD ID T99347
Target Name Metabotropic glutamate receptor 5 (mGluR5)
Type of Target
Clinical trial
Drug Potency against Target ADX10059 Drug Info IC50 = 17.1 nM [33]
Drug Info Ki = 390 nM [18]
(3-(2-methylquinolin-7-yl)phenyl)methanol Drug Info IC50 = 8700 nM [16]
(3-Ethoxy-pyridin-2-yl)-pyridin-2-yl-amine Drug Info IC50 = 138 nM [3]
(E)-1-Adamantan-1-yl-3-quinolin-3-yl-propenone Drug Info Ki = 807 nM [25]
(E)-3-[2-(2-methyl-4-thiazolyl)vinyl]pyridine Drug Info IC50 = 3090 nM [6]
1-(3-(2-methylquinolin-7-yl)phenyl)ethanone Drug Info IC50 = 4760 nM [16]
2-(2-Methyl-thiazol-4-ylethynyl)-pyridine Drug Info IC50 = 53 nM [1]
2-(2-methylquinolin-7-yl)benzonitrile Drug Info IC50 = 9800 nM [16]
2-(3,4-dimethylphenyl)-1,8-naphthyridine Drug Info IC50 = 45 nM [19]
2-(3,5-dichlorophenyl)pyrido[2,3-d]pyrimidine Drug Info IC50 = 228 nM [17]
2-(3,5-difluorophenyl)-7-methyl-1,8-naphthyridine Drug Info IC50 = 181 nM [19]
2-(3,5-dimethoxyphenyl)-1,8-naphthyridine Drug Info IC50 = 67 nM [19]
2-(3-(2-methylquinolin-7-yl)phenyl)acetonitrile Drug Info IC50 = 430 nM [16]
2-(3-(3-methoxyphenoxy)prop-1-ynyl)pyridine Drug Info IC50 = 1540 nM [11]
2-(3-(benzyloxy)phenyl)isoindoline-1,3-dione Drug Info Ki = 2100 nM [5]
2-(3-bromophenyl)-7-methyl-1,8-naphthyridine Drug Info IC50 = 47.9 nM [19]
2-(3-bromophenyl)-7-methylpyrido[2,3-d]pyrimidine Drug Info IC50 = 38 nM [17]
2-(3-bromophenyl)pyrido[2,3-d]pyrimidine Drug Info IC50 = 333 nM [17]
2-(3-chlorobenzyloxy)-6-chloroisonicotinonitrile Drug Info Ki = 5 nM [5]
2-(3-chlorophenyl)-7-methyl-1,8-naphthyridine Drug Info IC50 = 177 nM [19]
2-(4-(3-chlorophenyl)but-1-ynyl)-6-methylpyridine Drug Info IC50 = 5 nM [10]
2-(m-tolylethynyl)pyrimidine Drug Info IC50 = 10.8 nM [24]
2-(phenylethynyl)pyrimidine Drug Info IC50 = 195 nM [24]
2-(pyridin-2-yl)-4-(m-tolylthio)pyrimidine Drug Info IC50 = 2300 nM [7]
2-Benzoxy-5-(2-methylquinolin-7-yl)benzonitrile Drug Info Ki = 1040 nM [29]
2-benzyloxy-7,8-dihydro-6H-quinolin-5-one Drug Info IC50 = 1900 nM [20]
2-bromo-4-(3-fluorophenylethynyl)thiazole Drug Info IC50 = 526 nM [6]
2-chloro-N-(3-(3-chlorobenzamido)phenyl)benzamide Drug Info IC50 = 2620 nM [27]
2-Cyclohex-1-enylethynyl-pyridine Drug Info IC50 = 2.4 nM [4]
2-Cyclohexylethynyl-pyridine Drug Info IC50 = 106 nM [4]
2-Cyclopent-1-enylethynyl-pyridine Drug Info IC50 = 3.1 nM [4]
2-ethoxy-5-(m-tolylethynyl)pyrimidine Drug Info IC50 = 21.1 nM [24]
2-ethynyl-4-(3-fluorophenylethynyl)thiazole Drug Info IC50 = 2920 nM [6]
2-m-tolyl-1,8-naphthyridine Drug Info IC50 = 225 nM [19]
2-methyl-4-(2-thienylethynyl)thiazole Drug Info IC50 = 475 nM [6]
2-methyl-4-(3-thienylethynyl)thiazole Drug Info IC50 = 337 nM [6]
2-methyl-4-(m-tolylethynyl)thiazole Drug Info IC50 = 82.6 nM [6]
2-Methyl-4-o-tolylethynyl-thiazole Drug Info IC50 = 15 nM [1]
2-Methyl-4-p-tolylethynyl-thiazole Drug Info IC50 = 845 nM [1]
2-Methyl-4-phenylethynyl-thiazole Drug Info IC50 = 4 nM [1]
2-methyl-6-(3-(p-tolyloxy)prop-1-ynyl)pyridine Drug Info IC50 = 115 nM [11]
2-methyl-6-(3-(phenylthio)prop-1-ynyl)pyridine Drug Info IC50 = 589 nM [10]
2-methyl-6-(4-phenylbut-1-ynyl)pyridine Drug Info IC50 = 78 nM [10]
2-methyl-6-(4-phenylpent-1-ynyl)pyridine Drug Info IC50 = 59 nM [10]
2-methyl-6-(5-phenylpent-1-ynyl)pyridine Drug Info IC50 = 258 nM [10]
2-methyl-6-(phenylethynyl)pyridine Drug Info Ki = 4.7 nM [26]
2-methyl-7-(pyridin-3-yl)quinoline Drug Info IC50 = 510 nM [16]
2-methyl-7-m-tolyl-1,6-naphthyridine Drug Info IC50 = 676 nM [19]
2-methyl-7-m-tolyl-1,8-naphthyridine Drug Info IC50 = 277 nM [19]
2-methyl-7-m-tolylquinoline Drug Info IC50 = 3400 nM [16]
2-methyl-7-phenyl-1,8-naphthyridine Drug Info IC50 = 664 nM [19]
2-methyl-7-phenylquinoline Drug Info IC50 = 9000 nM [16]
2-phenyl-1,8-naphthyridine Drug Info IC50 = 1840 nM [19]
2-Phenyl-5-(2-methylthiazol-4ylethynyl)pyridine Drug Info IC50 = 1.21 nM [23]
2-phenylethynyl-5,6,7,8-tetrahydro-quinolin-5-ol Drug Info Ki = 7600 nM [20]
2-phenylethynyl-5,6,7,8-tetrahydro-quinoline Drug Info Ki = 1500 nM [20]
2-phenylethynyl-7,8-dihydro-6H-quinolin-5-one Drug Info Ki = 800 nM [20]
2-[(2-methyl-4-thiazolyl)ethynyl]pyrazine Drug Info IC50 = 1830 nM [6]
3-(1,5-naphthyridin-3-yl)benzonitrile Drug Info IC50 = 18600 nM [19]
3-(1,8-naphthyridin-2-yl)benzonitrile Drug Info IC50 = 115 nM [19]
3-(1-Pyridin-2-yl-1H-pyrazol-3-yl)-benzonitrile Drug Info IC50 = 3600 nM [2]
3-(1-Pyridin-2-yl-1H-pyrazol-4-yl)-benzonitrile Drug Info IC50 = 890 nM [2]
3-(1-Pyridin-2-yl-1H-pyrrol-3-yl)-benzonitrile Drug Info IC50 = 4620 nM [2]
3-(2-methylbenzo[d]thiazol-5-yl)benzonitrile Drug Info Ki = 2100 nM [14]
3-(2-methylquinolin-7-yl)benzonitrile Drug Info Ki = 72 nM [16]
3-(2-methylquinolin-7-yl)phenol Drug Info IC50 = 19000 nM [16]
3-(2-Pyridin-2-yl-2H-tetrazol-5-yl)-benzonitrile Drug Info Ki = 450 nM [2]
3-(3,4-dimethylphenyl)-1,5-naphthyridine Drug Info IC50 = 12000 nM [19]
3-(3-(3-chlorobenzyloxy)-5-methylphenyl)pyridine Drug Info Ki = 58 nM [5]
3-(3-bromophenylethynyl)-5-methyl[1,2,4]triazine Drug Info IC50 = 6 nM [15]
3-(3-methylphenylethynyl)-5-methyl[1,2,4]triazine Drug Info IC50 = 2.3 nM [15]
3-(3-Pyridin-2-yl-pyrazol-1-yl)-benzonitrile Drug Info Ki = 530 nM [2]
3-(3-Pyridin-2-yl-pyrrol-1-yl)-benzonitrile Drug Info IC50 = 190 nM [2]
3-(4-Pyridin-2-yl-imidazol-1-yl)-benzonitrile Drug Info IC50 = 1150 nM [2]
3-(4-Pyridin-2-yl-pyrazol-1-yl)-benzonitrile Drug Info Ki = 250 nM [2]
3-(5-Pyridin-2-yl-tetrazol-2-yl)-benzonitrile Drug Info Ki = 190 nM [2]
3-(6-fluoroquinazolin-4-ylamino)benzonitrile Drug Info IC50 = 1370 nM [26]
3-(7-methyl-1,8-naphthyridin-2-yl)benzonitrile Drug Info IC50 = 480 nM [19]
3-biphenyl-4-ylethynyl-5-methyl-[1,2,4]triazine Drug Info IC50 = 510 nM [15]
3-bromo-5-(2-methylquinolin-7-yl)benzonitrile Drug Info IC50 = 13 nM [16]
3-bromo-5-[(2-methyl-4-thiazolyl)ethynyl]pyridine Drug Info IC50 = 60 nM [6]
3-bromo-N-(6-methylpyridin-2-yl)benzamide Drug Info IC50 = 650 nM [8]
3-chloro-5-(2-methylquinolin-7-yl)benzonitrile Drug Info IC50 = 1.4 nM [16]
3-chloro-N-(3-isobutyramidophenyl)benzamide Drug Info IC50 = 5820 nM [27]
3-chloro-N-(4-methylthiazol-2-yl)benzamide Drug Info IC50 = 5490 nM [8]
3-chloro-N-(6-chloropyridin-2-yl)benzamide Drug Info IC50 = 1530 nM [8]
3-chloro-N-(6-methylpyridin-2-yl)benzamide Drug Info IC50 = 1870 nM [23]
3-cyano-5-fluoro-N-(3-fluorophenyl)benzamide Drug Info IC50 = 2160 nM [30]
3-cyano-5-fluoro-N-(pyridin-2-yl)benzamide Drug Info IC50 = 3010 nM [30]
3-cyano-5-fluoro-N-m-tolylbenzamide Drug Info Ki = 100 nM [30]
3-cyano-5-fluoro-N-phenylbenzamide Drug Info IC50 = 5440 nM [30]
3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide Drug Info Ki = 3760 nM [9]
3-cyano-N-(1,4-diphenyl-1H-pyrazol-5-yl)benzamide Drug Info Ki = 1200 nM [9]
3-cyano-N-(3-cyanophenyl)-5-fluorobenzamide Drug Info IC50 = 489 nM [30]
3-cyano-N-(3-ethylphenyl)-5-fluorobenzamide Drug Info IC50 = 4940 nM [30]
3-cyano-N-(3-ethynylphenyl)-5-fluorobenzamide Drug Info IC50 = 331 nM [30]
3-cyano-N-(6-ethylpyridin-2-yl)-5-fluorobenzamide Drug Info IC50 = 505 nM [30]
3-cyano-N-(6-methylpyridin-2-yl)benzamide Drug Info IC50 = 490 nM [23]
3-ethoxy-5-(2-methylquinolin-7-yl)benzonitrile Drug Info IC50 = 17 nM [16]
3-fluoro-5-(1,6-naphthyridin-7-yl)benzonitrile Drug Info IC50 = 1590 nM [19]
3-fluoro-5-(2-methylquinolin-7-yl)benzonitrile Drug Info Ki = 22 nM [16]
3-hydroxy-5-(2-methylquinolin-7-yl)benzonitrile Drug Info IC50 = 360 nM [16]
3-iodo-N-(6-methylpyridin-2-yl)benzamide Drug Info IC50 = 1080 nM [8]
3-isobutoxy-5-(2-methylquinolin-7-yl)benzonitrile Drug Info IC50 = 12000 nM [16]
3-m-tolyl-1,5-naphthyridine Drug Info IC50 = 15700 nM [19]
3-methoxy-5-(1,5-naphthyridin-3-yl)benzonitrile Drug Info IC50 = 55 nM [19]
3-methoxy-5-(1,6-naphthyridin-7-yl)benzonitrile Drug Info IC50 = 68 nM [19]
3-methoxy-5-(2-methylquinolin-7-yl)benzonitrile Drug Info IC50 = 2.4 nM [16]
3-methoxy-N-(4-methylthiazol-2-yl)benzamide Drug Info IC50 = 9100 nM [8]
3-methoxy-N-(6-methylpyridin-2-yl)benzamide Drug Info IC50 = 9760 nM [8]
3-methyl-5-(2-methylquinolin-7-yl)benzonitrile Drug Info IC50 = 1.6 nM [16]
3-methyl-N-(6-methylpyridin-2-yl)benzamide Drug Info IC50 = 1840 nM [8]
3-nitro-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide Drug Info Ki = 2220 nM [9]
3-Phenyl-1-(2-methylthiazol-4-ylethynyl)benzene Drug Info IC50 = 3.05 nM [23]
3-[(2,5-dimethyl-4-thiazolyl)ethynyl]pyridine Drug Info IC50 = 698 nM [6]
3-[(2-methyl-4-thiazolyl)ethynyl]-5-vinylpyridine Drug Info Ki = 0.71 nM [6]
3-[(2-methyl-4-thiazolyl)ethynyl]benzamide Drug Info IC50 = 1000 nM [6]
3-[(2-methyl-4-thiazolyl)ethynyl]benzonitrile Drug Info Ki = 0.25 nM [6]
3-[(2-methyl-4-thiazolyl)ethynyl]phenol Drug Info IC50 = 654 nM [6]
3-[(5-ethyl-2-methyl-4-thiazolyl)ethynyl]pyridine Drug Info IC50 = 1243 nM [6]
3-[(6-Methylpyridin-2-yl)ethynyl]benzonitrile Drug Info IC50 = 0.415 nM [23]
4-(2-(3-fluorophenyl)ethynyl)-2-methylthiazole Drug Info IC50 = 23 nM [6]
4-(2-(4-fluorophenyl)ethynyl)-2-methylthiazole Drug Info IC50 = 2966 nM [6]
4-(2-fluorophenylethynyl)-2-methylthiazole Drug Info IC50 = 140 nM [6]
4-(2-methoxyphenylethynyl)-2-methylthiazole Drug Info IC50 = 36.3 nM [6]
4-(2-Methyl-thiazol-4-ylethynyl)-pyridine Drug Info IC50 = 127 nM [1]
4-(3,5-difluorophenylethynyl)-2-methylthiazole Drug Info IC50 = 25.3 nM [6]
4-(3-bromophenoxy)-6-chloroquinazoline Drug Info IC50 = 6570 nM [26]
4-(3-bromophenylthio)-2-(pyridin-2-yl)pyrimidine Drug Info IC50 = 2860 nM [7]
4-(3-chlorophenylethynyl)-2-methylthiazole Drug Info IC50 = 129 nM [6]
4-(3-chlorophenylthio)-2-(pyridin-2-yl)pyrimidine Drug Info IC50 = 620 nM [7]
4-(3-fluorophenylethynyl)-2-thiazolylamine Drug Info IC50 = 78.6 nM [6]
4-(3-methoxyphenylethynyl)-2-methylthiazole Drug Info IC50 = 49 nM [6]
4-(3-pyridylethynyl)-2-thiazolylamine Drug Info IC50 = 789 nM [6]
4-(4-chlorophenylthio)-2-(pyridin-2-yl)pyrimidine Drug Info IC50 = 320 nM [7]
4-Biphenyl-2-ylethynyl-2-methyl-thiazole Drug Info IC50 = 423 nM [1]
4-Biphenyl-4-ylethynyl-2-methyl-thiazole Drug Info IC50 = 22 nM [1]
4-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide Drug Info Ki = 1560 nM [9]
5-((6-Methylpyridin-2-yl)ethynyl)nicotinonitrile Drug Info IC50 = 13 nM [29]
5-(2-(2,5-dimethylphenyl)ethynyl)pyrimidine Drug Info IC50 = 11200 nM [21]
5-(2-(3,5-difluorophenyl)ethynyl)pyrimidine Drug Info IC50 = 6400 nM [21]
5-(2-(3-chlorophenyl)ethynyl)pyrimidine Drug Info IC50 = 34 nM [21]
5-(2-(4-fluoro-3-methylphenyl)ethynyl)pyrimidine Drug Info IC50 = 350 nM [21]
5-(2-m-tolylethynyl)pyrimidine Drug Info IC50 = 7 nM [21]
5-(2-Methylquinolin-7-yl)-2-phenylbenzonitrile Drug Info IC50 = 1250 nM [29]
5-(2-Methylquinolin-7-yl)-2-phenylnicotinonitrile Drug Info IC50 = 81 nM [29]
5-(2-methylquinolin-7-yl)isophthalonitrile Drug Info IC50 = 2 nM [16]
5-(2-methylquinolin-7-yl)nicotinonitrile Drug Info IC50 = 23 nM [16]
5-(3-chlorophenylethynyl)-5-methyl[1,2,4]triazine Drug Info IC50 = 4.2 nM [15]
5-(phenylethynyl)pyrimidine Drug Info IC50 = 480 nM [21]
5-Biphenyl-4-ylethynyl-pyrimidine Drug Info IC50 = 7800 nM [21]
5-Chloro-2-(2-methylquinolin-7-yl)benzonitrile Drug Info IC50 = 9150 nM [29]
5-methyl-3-phenylethynyl[1,2,4]triazine Drug Info IC50 = 140 nM [15]
5-[(2-methyl-4-thiazolyl)ethynyl]pyrimidine Drug Info IC50 = 946 nM [6]
6-(4-chlorophenylamino)-N,N-diethylnicotinamide Drug Info IC50 = 460 nM [28]
6-bromo-N-(3-bromophenyl)quinazolin-4-amine Drug Info IC50 = 174 nM [26]
6-bromo-N-(3-chlorophenyl)quinazolin-4-amine Drug Info Ki = 116 nM [26]
6-bromo-N-(3-fluorophenyl)quinazolin-4-amine Drug Info IC50 = 1970 nM [26]
6-bromo-N-m-tolylquinazolin-4-amine Drug Info IC50 = 246 nM [26]
6-chloro-N-(3-chlorophenyl)quinazolin-4-amine Drug Info IC50 = 130 nM [26]
6-fluoro-N-m-tolylquinazolin-4-amine Drug Info IC50 = 1350 nM [26]
6-phenylethynyl-nicotinic acid methyl ester Drug Info Ki = 1400 nM [20]
7-(2-methoxyphenyl)-2-methylquinoline Drug Info IC50 = 4200 nM [16]
7-(3,5-dimethoxyphenyl)-1,6-naphthyridine Drug Info IC50 = 6070 nM [19]
7-(3-(methoxymethyl)phenyl)-2-methylquinoline Drug Info IC50 = 5800 nM [16]
7-(3-chlorophenyl)-2-methylquinoline Drug Info IC50 = 14000 nM [16]
7-(3-fluoro-5-methylphenyl)-1,6-naphthyridine Drug Info IC50 = 6570 nM [19]
7-(3-fluorophenyl)-2-methylquinoline Drug Info IC50 = 1800 nM [16]
7-(3-methoxyphenyl)-2-methyl-1,6-naphthyridine Drug Info IC50 = 7900 nM [19]
7-(3-methoxyphenyl)-2-methylquinoline Drug Info IC50 = 860 nM [16]
7-(4,6-dimethoxypyrimidin-2-yl)-2-methylquinoline Drug Info Ki = 5430 nM [14]
7-(4,6-dimethylpyrimidin-2-yl)-2-methylquinoline Drug Info Ki = 2090 nM [14]
7-(4-methoxyphenyl)-2-methylquinoline Drug Info IC50 = 16000 nM [16]
7-(4-methoxypyrimidin-2-yl)-2-methylquinoline Drug Info Ki = 1550 nM [14]
7-bromo-N-(3-bromophenyl)isoquinolin-1-amine Drug Info IC50 = 4330 nM [26]
7-m-tolyl-1,6-naphthyridine Drug Info IC50 = 1270 nM [19]
7-methyl-2-m-tolylpyrido[2,3-d]pyrimidine Drug Info IC50 = 53 nM [17]
7-methyl-2-phenylpyrido[2,3-d]pyrimidine Drug Info IC50 = 2700 nM [17]
N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide Drug Info Ki = 4180 nM [9]
N-(1,4-diphenyl-1H-pyrazol-5-yl)benzamide Drug Info Ki = 1170 nM [9]
N-(2-phenylimidazo[1,2-a]pyridin-3-yl)benzamide Drug Info Ki = 1990 nM [9]
N-(3-(3-cyanobenzamido)phenyl)-2-methoxybenzamide Drug Info IC50 = 1800 nM [27]
N-(3-acetamidophenyl)-3-chlorobenzamide Drug Info IC50 = 7970 nM [27]
N-(3-bromophenyl)-6-chloroquinazolin-4-amine Drug Info Ki = 249 nM [26]
N-(3-bromophenyl)-6-fluoroquinazolin-4-amine Drug Info Ki = 736 nM [26]
N-(3-chlorophenyl)-3-cyano-5-fluorobenzamide Drug Info Ki = 206 nM [30]
N-(3-chlorophenyl)-6-fluoroquinazolin-4-amine Drug Info IC50 = 311 nM [26]
N-(3-chlorophenyl)-6-methoxyquinazolin-4-amine Drug Info IC50 = 1510 nM [26]
N-(3-chlorophenyl)-6-nitroquinazolin-4-amine Drug Info IC50 = 274 nM [26]
N-(6-methylpyridin-2-yl)-5-phenylpicolinamide Drug Info Ki = 2800 nM [13]
N-(6-methylpyridin-2-yl)-6-phenylnicotinamide Drug Info Ki = 356 nM [23]
N-(6-methylpyridin-2-yl)biphenyl-3-carboxamide Drug Info Ki = 7300 nM [23]
N-cyclopentyl-6-(2-phenylethynyl)nicotinamide Drug Info Ki = 1800 nM [22]
N-[4-(3-pyridylethynyl)-2-thiazolyl]acetamide Drug Info IC50 = 1920 nM [6]
SIB-1757 Drug Info IC50 = 1170 nM [8]
SIB-1893 Drug Info IC50 = 1080 nM [8]
STX-107 Drug Info Ki = 16 nM [29]
VU-29 Drug Info Ki = 250 nM [9]
[3H]M-MPEP Drug Info Ki = 11 nM [12]
[3H]quisqualate Drug Info IC50 = 25 nM [31]
Action against Disease Model ADX10059 Drug Info 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. [32]
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