Target Information
Target General Infomation | |||||
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Target ID |
T99347
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Former ID |
TTDC00100
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Target Name |
Metabotropic glutamate receptor 5
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Gene Name |
GRM5
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Synonyms |
5b; Glutamate receptor mGLU5; mGluR5; GRM5
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Target Type |
Clinical Trial
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Disease | Autism [ICD9: 299; ICD10: F84.0] | ||||
Alzheimer disease [ICD9: 331; ICD10: G30] | |||||
Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42] | |||||
Central nervous system disease [ICD10: G00-G99] | |||||
Chronic neuropathic pain [ICD9: 338, 356.0, 356.8, 530,780; ICD10: G64, G90.0, K21, R52, G89] | |||||
Fragile X syndrome [ICD9: 332, 759.83; ICD10: F02.3, G20, Q99.2] | |||||
Mood disorder [ICD10: F30-F39] | |||||
Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32] | |||||
Major depressive disorder; GERD; Chronic neuropathic pain [ICD9: 296.2, 296.3, 338, 356.0, 356.8, 530,780; ICD10: F32, F33, G64, G90.0, K21, R52, G89] | |||||
Neuropathic pain; Migraine [ICD9: 338, 346,780; ICD10: G43, R52, G89] | |||||
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89] | |||||
Unspecified [ICD code not available] | |||||
Function |
G-protein coupled receptor for glutamate. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Signaling activates a phosphatidylinositol-calcium second messenger system and generates a calcium-activated chloride current. Plays an important role in the regulation of synaptic plasticity and the modulation of the neural network activity.
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BioChemical Class |
GPCR glutamate
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Target Validation |
T99347
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UniProt ID | |||||
Sequence |
MVLLLILSVLLLKEDVRGSAQSSERRVVAHMPGDIIIGALFSVHHQPTVDKVHERKCGAV
REQYGIQRVEAMLHTLERINSDPTLLPNITLGCEIRDSCWHSAVALEQSIEFIRDSLISS EEEEGLVRCVDGSSSSFRSKKPIVGVIGPGSSSVAIQVQNLLQLFNIPQIAYSATSMDLS DKTLFKYFMRVVPSDAQQARAMVDIVKRYNWTYVSAVHTEGNYGESGMEAFKDMSAKEGI CIAHSYKIYSNAGEQSFDKLLKKLTSHLPKARVVACFCEGMTVRGLLMAMRRLGLAGEFL LLGSDGWADRYDVTDGYQREAVGGITIKLQSPDVKWFDDYYLKLRPETNHRNPWFQEFWQ HRFQCRLEGFPQENSKYNKTCNSSLTLKTHHVQDSKMGFVINAIYSMAYGLHNMQMSLCP GYAGLCDAMKPIDGRKLLESLMKTNFTGVSGDTILFDENGDSPGRYEIMNFKEMGKDYFD YINVGSWDNGELKMDDDEVWSKKSNIIRSVCSEPCEKGQIKVIRKGEVSCCWTCTPCKEN EYVFDEYTCKACQLGSWPTDDLTGCDLIPVQYLRWGDPEPIAAVVFACLGLLATLFVTVV FIIYRDTPVVKSSSRELCYIILAGICLGYLCTFCLIAKPKQIYCYLQRIGIGLSPAMSYS ALVTKTNRIARILAGSKKKICTKKPRFMSACAQLVIAFILICIQLGIIVALFIMEPPDIM HDYPSIREVYLICNTTNLGVVTPLGYNGLLILSCTFYAFKTRNVPANFNEAKYIAFTMYT TCIIWLAFVPIYFGSNYKIITMCFSVSLSATVALGCMFVPKVYIILAKPERNVRSAFTTS TVVRMHVGDGKSSSAASRSSSLVNLWKRRGSSGETLRYKDRRLAQHKSEIECFTPKGSMG NGGRATMSSSNGKSVTWAQNEKSSRGQHLWQRLSIHINKKENPNQTAVIKPFPKSTESRG LGAGAGAGGSAGGVGATGGAGCAGAGPGGPESPDAGPKALYDVAEAEEHFPAPARPRSPS PISTLSHRAGSASRTDDDVPSLHSEPVARSSSSQGSLMEQISSVVTRFTANISELNSMML STAAPSPGVGAPLCSSYLIPKEIQLPTTMTTFAEIQPLPAIEVTGGAQPAAGAQAAGDAA RESPAAGPEAAAAKPDLEELVALTPPSPFRDSVDSGSTTPNSPVSESALCIPSSPKYDTL IIRDYTQSSSSL |
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Drugs and Mode of Action | |||||
Drug(s) | AFQ056 | Drug Info | Phase 2/3 | Fragile X syndrome | [523621], [542576] |
ADX-48621 | Drug Info | Phase 2 | Mood disorder | [523431], [541593] | |
ADX10059 | Drug Info | Phase 2 | Anxiety disorder | [522540] | |
RG-7090 | Drug Info | Phase 2 | Fragile X syndrome | [524162] | |
STX-107 | Drug Info | Phase 2 | Autism | [523414], [540295] | |
McN3377 | Drug Info | Phase 1/2 | Fragile X syndrome | [522263], [538912] | |
MK-3328 | Drug Info | Phase 1 | Alzheimer disease | [522751] | |
AZD2066 | Drug Info | Discontinued in Phase 2 | Major depressive disorder; GERD; Chronic neuropathic pain | [548676] | |
AZD2516 | Drug Info | Discontinued in Phase 2 | Chronic neuropathic pain | [548860] | |
LY467711 | Drug Info | Terminated | Neuropathic pain; Migraine | [547372] | |
LY525327 | Drug Info | Terminated | Neuropathic pain; Migraine | [547372] | |
Antagonist | (+)-MCPG | Drug Info | [525911] | ||
(S)-4C3HPG | Drug Info | [525911] | |||
(S)-4CPG | Drug Info | [525911] | |||
ACDPP | Drug Info | [527417] | |||
AZD2066 | Drug Info | [550288] | |||
AZD2516 | Drug Info | [550288] | |||
CTEP | Drug Info | [543750] | |||
GSK-2210875 | Drug Info | [543750] | |||
LY467711 | Drug Info | [536166] | |||
LY525327 | Drug Info | [536166] | |||
MGluR5 antagonists (anxiety), Novartis | Drug Info | [543750] | |||
RG-7090 | Drug Info | [544380] | |||
RTI-4229-982 | Drug Info | [543750] | |||
STX-107 | Drug Info | [544372] | |||
Agonist | (1S,3R)-ACPD | Drug Info | [525911] | ||
(S)-(+)-CBPG | Drug Info | [525552] | |||
(S)-3HPG | Drug Info | [525911] | |||
3,5-DHPG | Drug Info | [525911] | |||
CHPG | Drug Info | [525911] | |||
ibotenate | Drug Info | [525911] | |||
L-CCG-I | Drug Info | [525911] | |||
Inhibitor | (3-(2-methylquinolin-7-yl)phenyl)methanol | Drug Info | [528922] | ||
(3-Ethoxy-pyridin-2-yl)-pyridin-2-yl-amine | Drug Info | [527656] | |||
(E)-1-Adamantan-1-yl-3-quinolin-3-yl-propenone | Drug Info | [530245] | |||
(E)-3-[2-(2-methyl-4-thiazolyl)vinyl]pyridine | Drug Info | [528003] | |||
1-(3-(2-methylquinolin-7-yl)phenyl)ethanone | Drug Info | [528922] | |||
2-(2-Methyl-thiazol-4-ylethynyl)-pyridine | Drug Info | [527127] | |||
2-(2-methylquinolin-7-yl)benzonitrile | Drug Info | [528922] | |||
2-(3,4-dimethylphenyl)-1,8-naphthyridine | Drug Info | [529101] | |||
2-(3,5-dichlorophenyl)pyrido[2,3-d]pyrimidine | Drug Info | [528998] | |||
2-(3,5-difluorophenyl)-7-methyl-1,8-naphthyridine | Drug Info | [529101] | |||
2-(3,5-dimethoxyphenyl)-1,8-naphthyridine | Drug Info | [529101] | |||
2-(3-(2-methylquinolin-7-yl)phenyl)acetonitrile | Drug Info | [528922] | |||
2-(3-(3-methoxyphenoxy)prop-1-ynyl)pyridine | Drug Info | [528311] | |||
2-(3-(benzyloxy)phenyl)isoindoline-1,3-dione | Drug Info | [527989] | |||
2-(3-bromophenyl)-7-methyl-1,8-naphthyridine | Drug Info | [529101] | |||
2-(3-bromophenyl)-7-methylpyrido[2,3-d]pyrimidine | Drug Info | [528998] | |||
2-(3-bromophenyl)pyrido[2,3-d]pyrimidine | Drug Info | [528998] | |||
2-(3-chlorobenzyloxy)-6-chloroisonicotinonitrile | Drug Info | [527989] | |||
2-(3-chlorophenyl)-7-methyl-1,8-naphthyridine | Drug Info | [529101] | |||
2-(4-(3-chlorophenyl)but-1-ynyl)-6-methylpyridine | Drug Info | [528307] | |||
2-(m-tolylethynyl)pyrimidine | Drug Info | [530217] | |||
2-(phenylethynyl)pyrimidine | Drug Info | [530217] | |||
2-(pyridin-2-yl)-4-(m-tolylthio)pyrimidine | Drug Info | [528038] | |||
2-Benzoxy-5-(2-methylquinolin-7-yl)benzonitrile | Drug Info | [530843] | |||
2-benzyloxy-7,8-dihydro-6H-quinolin-5-one | Drug Info | [529241] | |||
2-bromo-4-(3-fluorophenylethynyl)thiazole | Drug Info | [528003] | |||
2-Chloro-5-(2-methylquinolin-7-yl)nicotinonitrile | Drug Info | [530843] | |||
2-chloro-N-(3-(3-chlorobenzamido)phenyl)benzamide | Drug Info | [530486] | |||
2-Cyclohex-1-enylethynyl-pyridine | Drug Info | [527696] | |||
2-Cyclohexylethynyl-pyridine | Drug Info | [527696] | |||
2-Cyclopent-1-enylethynyl-pyridine | Drug Info | [527696] | |||
2-ethoxy-5-(m-tolylethynyl)pyrimidine | Drug Info | [530217] | |||
2-ethynyl-4-(3-fluorophenylethynyl)thiazole | Drug Info | [528003] | |||
2-m-tolyl-1,8-naphthyridine | Drug Info | [529101] | |||
2-methyl-4-(2-thienylethynyl)thiazole | Drug Info | [528003] | |||
2-methyl-4-(3-thienylethynyl)thiazole | Drug Info | [528003] | |||
2-methyl-4-(m-tolylethynyl)thiazole | Drug Info | [528003] | |||
2-methyl-4-(pyridin-3-ylethynyl)thiazole | Drug Info | [530843] | |||
2-Methyl-4-o-tolylethynyl-thiazole | Drug Info | [527127] | |||
2-Methyl-4-p-tolylethynyl-thiazole | Drug Info | [527127] | |||
2-Methyl-4-phenylethynyl-thiazole | Drug Info | [527127] | |||
2-methyl-6-((3-methoxyphenyl)ethynyl)-pyridine | Drug Info | [528525] | |||
2-methyl-6-(3-(p-tolyloxy)prop-1-ynyl)pyridine | Drug Info | [528311] | |||
2-methyl-6-(3-(phenylthio)prop-1-ynyl)pyridine | Drug Info | [528307] | |||
2-methyl-6-(4-phenylbut-1-ynyl)pyridine | Drug Info | [528307] | |||
2-methyl-6-(4-phenylpent-1-ynyl)pyridine | Drug Info | [528307] | |||
2-methyl-6-(5-phenylpent-1-ynyl)pyridine | Drug Info | [528307] | |||
2-methyl-6-(phenylethynyl)pyridine | Drug Info | [530473] | |||
2-methyl-7-(pyridin-3-yl)quinoline | Drug Info | [528922] | |||
2-methyl-7-m-tolyl-1,6-naphthyridine | Drug Info | [529101] | |||
2-methyl-7-m-tolyl-1,8-naphthyridine | Drug Info | [529101] | |||
2-methyl-7-m-tolylquinoline | Drug Info | [528922] | |||
2-methyl-7-phenyl-1,8-naphthyridine | Drug Info | [529101] | |||
2-methyl-7-phenylquinoline | Drug Info | [528922] | |||
2-phenyl-1,8-naphthyridine | Drug Info | [529101] | |||
2-Phenyl-5-(2-methylthiazol-4ylethynyl)pyridine | Drug Info | [530140] | |||
2-phenylethynyl-5,6,7,8-tetrahydro-quinolin-5-ol | Drug Info | [529241] | |||
2-phenylethynyl-5,6,7,8-tetrahydro-quinoline | Drug Info | [529241] | |||
2-phenylethynyl-7,8-dihydro-6H-quinolin-5-one | Drug Info | [529241] | |||
2-[(2-methyl-4-thiazolyl)ethynyl]pyrazine | Drug Info | [528003] | |||
3-(1,5-naphthyridin-3-yl)benzonitrile | Drug Info | [529101] | |||
3-(1,8-naphthyridin-2-yl)benzonitrile | Drug Info | [529101] | |||
3-(1-Pyridin-2-yl-1H-pyrazol-3-yl)-benzonitrile | Drug Info | [527190] | |||
3-(1-Pyridin-2-yl-1H-pyrazol-4-yl)-benzonitrile | Drug Info | [527190] | |||
3-(1-Pyridin-2-yl-1H-pyrrol-3-yl)-benzonitrile | Drug Info | [527190] | |||
3-(2-methylbenzo[d]thiazol-5-yl)benzonitrile | Drug Info | [528793] | |||
3-(2-methylquinolin-7-yl)benzonitrile | Drug Info | [528922] | |||
3-(2-methylquinolin-7-yl)phenol | Drug Info | [528922] | |||
3-(2-Pyridin-2-yl-2H-tetrazol-5-yl)-benzonitrile | Drug Info | [527190] | |||
3-(3,4-dimethylphenyl)-1,5-naphthyridine | Drug Info | [529101] | |||
3-(3-(3-chlorobenzyloxy)-5-methylphenyl)pyridine | Drug Info | [527989] | |||
3-(3-bromophenylethynyl)-5-methyl[1,2,4]triazine | Drug Info | [528893] | |||
3-(3-methylphenylethynyl)-5-methyl[1,2,4]triazine | Drug Info | [528893] | |||
3-(3-Pyridin-2-yl-pyrazol-1-yl)-benzonitrile | Drug Info | [527190] | |||
3-(3-Pyridin-2-yl-pyrrol-1-yl)-benzonitrile | Drug Info | [527190] | |||
3-(4-Pyridin-2-yl-imidazol-1-yl)-benzonitrile | Drug Info | [527190] | |||
3-(4-Pyridin-2-yl-pyrazol-1-yl)-benzonitrile | Drug Info | [527190] | |||
3-(5-Pyridin-2-yl-tetrazol-2-yl)-benzonitrile | Drug Info | [527190] | |||
3-(6-fluoroquinazolin-4-ylamino)benzonitrile | Drug Info | [530473] | |||
3-(7-methyl-1,8-naphthyridin-2-yl)benzonitrile | Drug Info | [529101] | |||
3-biphenyl-4-ylethynyl-5-methyl-[1,2,4]triazine | Drug Info | [528893] | |||
3-bromo-5-(2-methylquinolin-7-yl)benzonitrile | Drug Info | [528922] | |||
3-bromo-5-[(2-methyl-4-thiazolyl)ethynyl]pyridine | Drug Info | [528003] | |||
3-bromo-N-(6-methylpyridin-2-yl)benzamide | Drug Info | [528186] | |||
3-chloro-5-(2-methylquinolin-7-yl)benzonitrile | Drug Info | [528922] | |||
3-chloro-N-(3-isobutyramidophenyl)benzamide | Drug Info | [530486] | |||
3-chloro-N-(4-methylthiazol-2-yl)benzamide | Drug Info | [528186] | |||
3-chloro-N-(6-chloropyridin-2-yl)benzamide | Drug Info | [528186] | |||
3-chloro-N-(6-methylpyridin-2-yl)benzamide | Drug Info | [530140] | |||
3-cyano-5-fluoro-N-(3-fluorophenyl)benzamide | Drug Info | [531010] | |||
3-cyano-5-fluoro-N-(pyridin-2-yl)benzamide | Drug Info | [531010] | |||
3-cyano-5-fluoro-N-m-tolylbenzamide | Drug Info | [531010] | |||
3-cyano-5-fluoro-N-phenylbenzamide | Drug Info | [531010] | |||
3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide | Drug Info | [528212] | |||
3-cyano-N-(1,4-diphenyl-1H-pyrazol-5-yl)benzamide | Drug Info | [528212] | |||
3-cyano-N-(3-cyanophenyl)-5-fluorobenzamide | Drug Info | [531010] | |||
3-cyano-N-(3-ethylphenyl)-5-fluorobenzamide | Drug Info | [531010] | |||
3-cyano-N-(3-ethynylphenyl)-5-fluorobenzamide | Drug Info | [531010] | |||
3-cyano-N-(6-ethylpyridin-2-yl)-5-fluorobenzamide | Drug Info | [531010] | |||
3-cyano-N-(6-methylpyridin-2-yl)benzamide | Drug Info | [530140] | |||
3-ethoxy-5-(2-methylquinolin-7-yl)benzonitrile | Drug Info | [528922] | |||
3-fluoro-5-(1,6-naphthyridin-7-yl)benzonitrile | Drug Info | [529101] | |||
3-fluoro-5-(2-methylquinolin-7-yl)benzonitrile | Drug Info | [528922] | |||
3-hydroxy-5-(2-methylquinolin-7-yl)benzonitrile | Drug Info | [528922] | |||
3-iodo-N-(6-methylpyridin-2-yl)benzamide | Drug Info | [528186] | |||
3-isobutoxy-5-(2-methylquinolin-7-yl)benzonitrile | Drug Info | [528922] | |||
3-m-tolyl-1,5-naphthyridine | Drug Info | [529101] | |||
3-methoxy-5-(1,5-naphthyridin-3-yl)benzonitrile | Drug Info | [529101] | |||
3-methoxy-5-(1,6-naphthyridin-7-yl)benzonitrile | Drug Info | [529101] | |||
3-methoxy-5-(2-methylquinolin-7-yl)benzonitrile | Drug Info | [528922] | |||
3-methoxy-N-(4-methylthiazol-2-yl)benzamide | Drug Info | [528186] | |||
3-methoxy-N-(6-methylpyridin-2-yl)benzamide | Drug Info | [528186] | |||
3-methyl-5-(2-methylquinolin-7-yl)benzonitrile | Drug Info | [528922] | |||
3-methyl-N-(6-methylpyridin-2-yl)benzamide | Drug Info | [528186] | |||
3-nitro-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide | Drug Info | [528212] | |||
3-Phenyl-1-(2-methylthiazol-4-ylethynyl)benzene | Drug Info | [530140] | |||
3-[(2,5-dimethyl-4-thiazolyl)ethynyl]pyridine | Drug Info | [528003] | |||
3-[(2-methyl-4-thiazolyl)ethynyl]-5-vinylpyridine | Drug Info | [528003] | |||
3-[(2-methyl-4-thiazolyl)ethynyl]benzamide | Drug Info | [528003] | |||
3-[(2-methyl-4-thiazolyl)ethynyl]benzonitrile | Drug Info | [528003] | |||
3-[(2-methyl-4-thiazolyl)ethynyl]phenol | Drug Info | [528003] | |||
3-[(5-ethyl-2-methyl-4-thiazolyl)ethynyl]pyridine | Drug Info | [528003] | |||
3-[(6-Methylpyridin-2-yl)ethynyl]benzonitrile | Drug Info | [530140] | |||
4-(2-(3-fluorophenyl)ethynyl)-2-methylthiazole | Drug Info | [528003] | |||
4-(2-(4-fluorophenyl)ethynyl)-2-methylthiazole | Drug Info | [528003] | |||
4-(2-fluorophenylethynyl)-2-methylthiazole | Drug Info | [528003] | |||
4-(2-methoxyphenylethynyl)-2-methylthiazole | Drug Info | [528003] | |||
4-(2-Methyl-thiazol-4-ylethynyl)-pyridine | Drug Info | [527127] | |||
4-(3,5-difluorophenylethynyl)-2-methylthiazole | Drug Info | [528003] | |||
4-(3-bromophenoxy)-6-chloroquinazoline | Drug Info | [530473] | |||
4-(3-bromophenylthio)-2-(pyridin-2-yl)pyrimidine | Drug Info | [528038] | |||
4-(3-chlorophenylethynyl)-2-methylthiazole | Drug Info | [528003] | |||
4-(3-chlorophenylthio)-2-(pyridin-2-yl)pyrimidine | Drug Info | [528038] | |||
4-(3-fluorophenylethynyl)-2-thiazolylamine | Drug Info | [528003] | |||
4-(3-methoxyphenylethynyl)-2-methylthiazole | Drug Info | [528003] | |||
4-(3-pyridylethynyl)-2-thiazolylamine | Drug Info | [528003] | |||
4-(4-chlorophenylthio)-2-(pyridin-2-yl)pyrimidine | Drug Info | [528038] | |||
4-Biphenyl-2-ylethynyl-2-methyl-thiazole | Drug Info | [527127] | |||
4-Biphenyl-4-ylethynyl-2-methyl-thiazole | Drug Info | [527127] | |||
4-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide | Drug Info | [528212] | |||
4-nitro-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide | Drug Info | [528212] | |||
5-((6-Methylpyridin-2-yl)ethynyl)nicotinonitrile | Drug Info | [530843] | |||
5-(2-(2,5-dimethylphenyl)ethynyl)pyrimidine | Drug Info | [529531] | |||
5-(2-(3,5-difluorophenyl)ethynyl)pyrimidine | Drug Info | [529531] | |||
5-(2-(3-chlorophenyl)ethynyl)pyrimidine | Drug Info | [529531] | |||
5-(2-(4-fluoro-3-methylphenyl)ethynyl)pyrimidine | Drug Info | [529531] | |||
5-(2-m-tolylethynyl)pyrimidine | Drug Info | [529531] | |||
5-(2-Methylquinolin-7-yl)-2-phenylbenzonitrile | Drug Info | [530843] | |||
5-(2-Methylquinolin-7-yl)-2-phenylnicotinonitrile | Drug Info | [530843] | |||
5-(2-methylquinolin-7-yl)isophthalonitrile | Drug Info | [528922] | |||
5-(2-methylquinolin-7-yl)nicotinonitrile | Drug Info | [528922] | |||
5-(3-chlorophenylethynyl)-5-methyl[1,2,4]triazine | Drug Info | [528893] | |||
5-(phenylethynyl)pyrimidine | Drug Info | [529531] | |||
5-Biphenyl-4-ylethynyl-pyrimidine | Drug Info | [529531] | |||
5-Chloro-2-(2-methylquinolin-7-yl)benzonitrile | Drug Info | [530843] | |||
5-methyl-3-phenylethynyl[1,2,4]triazine | Drug Info | [528893] | |||
5-[(2-methyl-4-thiazolyl)ethynyl]pyrimidine | Drug Info | [528003] | |||
6-(4-chlorophenylamino)-N,N-diethylnicotinamide | Drug Info | [530531] | |||
6-bromo-N-(3-bromophenyl)quinazolin-4-amine | Drug Info | [530473] | |||
6-bromo-N-(3-chlorophenyl)quinazolin-4-amine | Drug Info | [530473] | |||
6-bromo-N-(3-fluorophenyl)quinazolin-4-amine | Drug Info | [530473] | |||
6-bromo-N-m-tolylquinazolin-4-amine | Drug Info | [530473] | |||
6-chloro-N-(3-chlorophenyl)quinazolin-4-amine | Drug Info | [530473] | |||
6-fluoro-N-m-tolylquinazolin-4-amine | Drug Info | [530473] | |||
6-phenylethynyl-nicotinic acid methyl ester | Drug Info | [529241] | |||
7-(2-methoxyphenyl)-2-methylquinoline | Drug Info | [528922] | |||
7-(3,5-dimethoxyphenyl)-1,6-naphthyridine | Drug Info | [529101] | |||
7-(3-(methoxymethyl)phenyl)-2-methylquinoline | Drug Info | [528922] | |||
7-(3-chlorophenyl)-2-methylquinoline | Drug Info | [528922] | |||
7-(3-fluoro-5-methylphenyl)-1,6-naphthyridine | Drug Info | [529101] | |||
7-(3-fluorophenyl)-2-methylquinoline | Drug Info | [528922] | |||
7-(3-methoxyphenyl)-2-methyl-1,6-naphthyridine | Drug Info | [529101] | |||
7-(3-methoxyphenyl)-2-methylquinoline | Drug Info | [528922] | |||
7-(4,6-dimethoxypyrimidin-2-yl)-2-methylquinoline | Drug Info | [528793] | |||
7-(4,6-dimethylpyrimidin-2-yl)-2-methylquinoline | Drug Info | [528793] | |||
7-(4-methoxyphenyl)-2-methylquinoline | Drug Info | [528922] | |||
7-(4-methoxypyrimidin-2-yl)-2-methylquinoline | Drug Info | [528793] | |||
7-bromo-N-(3-bromophenyl)isoquinolin-1-amine | Drug Info | [530473] | |||
7-m-tolyl-1,6-naphthyridine | Drug Info | [529101] | |||
7-methyl-2-m-tolylpyrido[2,3-d]pyrimidine | Drug Info | [528998] | |||
7-methyl-2-phenylpyrido[2,3-d]pyrimidine | Drug Info | [528998] | |||
GLUTAMATE | Drug Info | [529001] | |||
N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide | Drug Info | [528212] | |||
N-(1,4-diphenyl-1H-pyrazol-5-yl)benzamide | Drug Info | [528212] | |||
N-(2-phenylimidazo[1,2-a]pyridin-3-yl)benzamide | Drug Info | [528212] | |||
N-(3-(3-cyanobenzamido)phenyl)-2-methoxybenzamide | Drug Info | [530486] | |||
N-(3-acetamidophenyl)-3-chlorobenzamide | Drug Info | [530486] | |||
N-(3-bromophenyl)-6-chloroquinazolin-4-amine | Drug Info | [530473] | |||
N-(3-bromophenyl)-6-fluoroquinazolin-4-amine | Drug Info | [530473] | |||
N-(3-chlorophenyl)-3-cyano-5-fluorobenzamide | Drug Info | [531010] | |||
N-(3-chlorophenyl)-6-fluoroquinazolin-4-amine | Drug Info | [530473] | |||
N-(3-chlorophenyl)-6-methoxyquinazolin-4-amine | Drug Info | [530473] | |||
N-(3-chlorophenyl)-6-nitroquinazolin-4-amine | Drug Info | [530473] | |||
N-(6-methylpyridin-2-yl)-5-phenylpicolinamide | Drug Info | [528711] | |||
N-(6-methylpyridin-2-yl)-6-phenylnicotinamide | Drug Info | [530140] | |||
N-(6-methylpyridin-2-yl)biphenyl-3-carboxamide | Drug Info | [530140] | |||
N-cyclopentyl-6-(2-phenylethynyl)nicotinamide | Drug Info | [530138] | |||
N-[4-(3-pyridylethynyl)-2-thiazolyl]acetamide | Drug Info | [528003] | |||
QUISQUALATE | Drug Info | [534590] | |||
SIB-1757 | Drug Info | [528186] | |||
SIB-1893 | Drug Info | [528186] | |||
Modulator (allosteric modulator) | 3,3'-difluorobenzaldazine | Drug Info | [526693] | ||
5-MPEP | Drug Info | [527733] | |||
5PAM523 | Drug Info | [532177] | |||
alloswitch-1 | Drug Info | [532936] | |||
BOMA | Drug Info | [526911] | |||
Br-5MPEPy | Drug Info | [527733] | |||
CDPPB | Drug Info | [527282] | |||
compound 10 | Drug Info | [527250] | |||
compound 10 | Drug Info | [527251] | |||
compound 11a | Drug Info | [526911] | |||
compound 13 | Drug Info | [527417] | |||
compound 16a | Drug Info | [526911] | |||
compound 16m | Drug Info | [530531] | |||
compound 18 | Drug Info | [528998] | |||
compound 18 | Drug Info | [531628] | |||
compound 20 | Drug Info | [527989] | |||
compound 23 | Drug Info | [528922] | |||
compound 24 | Drug Info | [532212] | |||
compound 24d | Drug Info | [532205] | |||
compound 26 | Drug Info | [527989] | |||
compound 27 | Drug Info | [531010] | |||
compound 29b | Drug Info | [531142] | |||
compound 30 | Drug Info | [531559] | |||
compound 36 | Drug Info | [529101] | |||
compound 41 | Drug Info | [532244] | |||
compound 42 | Drug Info | [528596] | |||
compound 47 | Drug Info | [531355] | |||
compound 53 | Drug Info | [532244] | |||
compound 8 | Drug Info | [527251] | |||
compound 8 | Drug Info | [531010] | |||
CPPHA | Drug Info | [526946] | |||
CPPZ | Drug Info | [531370] | |||
LSN2463359 | Drug Info | [531998] | |||
LSN2814617 | Drug Info | [531998] | |||
M-5MPEP | Drug Info | [527733] | |||
methoxymethyl-MTEP | Drug Info | [526461] | |||
MPEP | Drug Info | [525618] | |||
MTEB | Drug Info | [526911] | |||
NCFP | Drug Info | [532201] | |||
PTeB | Drug Info | [527190] | |||
SP203 | Drug Info | [528895] | |||
VU-1545 | Drug Info | [528212] | |||
VU-29 | Drug Info | [528679] | |||
VU0092273 | Drug Info | [531671] | |||
VU0240382 | Drug Info | [531671] | |||
VU0285683 | Drug Info | [531194] | |||
VU0357121 | Drug Info | [531240] | |||
VU0360172 | Drug Info | [531194] | |||
VU0361747 | Drug Info | [531671] | |||
VU0364289 | Drug Info | [532189] | |||
VU0366058 | Drug Info | [531769] | |||
VU0404251 | Drug Info | [532044] | |||
VU0424465 | Drug Info | [532112] | |||
VU0463841 | Drug Info | [532357] | |||
[14C]MTEP | Drug Info | [526461] | |||
[3H]CTEP | Drug Info | [531601] | |||
[3H]fenobam | Drug Info | [527659] | |||
[3H]M-MPEP | Drug Info | [526258] | |||
[3H]methoxy-PEPy | Drug Info | [526531] | |||
[3H]methoxymethyl-MTEP | Drug Info | [526531] | |||
Modulator | ADX-48621 | Drug Info | [550205] | ||
ADX-63365 | Drug Info | [543750] | |||
ADX10059 | Drug Info | [536890], [537360] | |||
AFQ056 | Drug Info | [532401] | |||
GRN-529 | Drug Info | [543750] | |||
LY-3390334 | Drug Info | ||||
McN3377 | Drug Info | [536166] | |||
MK-3328 | Drug Info | [543750] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Calcium signaling pathway | ||||
Neuroactive ligand-receptor interaction | |||||
Gap junction | |||||
Long-term potentiation | |||||
Retrograde endocannabinoid signaling | |||||
Glutamatergic synapse | |||||
Huntington' | |||||
s disease | |||||
PANTHER Pathway | Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway | ||||
Metabotropic glutamate receptor group III pathway | |||||
Metabotropic glutamate receptor group I pathway | |||||
Endogenous cannabinoid signaling | |||||
Reactome | G alpha (q) signalling events | ||||
Class C/3 (Metabotropic glutamate/pheromone receptors) | |||||
WikiPathways | Hypothetical Network for Drug Addiction | ||||
GPCRs, Class C Metabotropic glutamate, pheromone | |||||
Gastrin-CREB signalling pathway via PKC and MAPK | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
References | |||||
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Ref 528596 | Rational design, synthesis, and structure-activity relationship of benzoxazolones: new potent mglu5 receptor antagonists based on the fenobam structure. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1302-6.Epub 2006 Dec 15. | ||||
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Ref 528711 | Bioorg 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. | ||||
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Ref 528895 | Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography. J Med Chem. 2007 Jul 12;50(14):3256-66. Epub 2007 Jun 16. | ||||
Ref 528922 | Bioorg 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 528998 | Bioorg 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 531142 | Design, synthesis, and structure-activity relationships of novel bicyclic azole-amines as negative allosteric modulators of metabotropic glutamate receptor 5. J Med Chem. 2010 Oct 14;53(19):7107-18. | ||||
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Ref 531240 | Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology. ACS Chem Neurosci. 2010 Oct 20;1(10):702-716. Epub 2010 Aug 19. | ||||
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Ref 531601 | CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. J Pharmacol Exp Ther. 2011 Nov;339(2):474-86. | ||||
Ref 531628 | (3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu(5): Discovery of a new tool compound with activity in the OSS mouse model of addiction. ACS Chem Neurosci. 2011 Aug 17;2(8):471-482. | ||||
Ref 531671 | Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function. Mol Pharmacol.2012 Feb;81(2):120-33. | ||||
Ref 531769 | Discovery of 2-(2-benzoxazoyl amino)-4-aryl-5-cyanopyrimidine as negative allosteric modulators (NAMs) of metabotropic glutamate receptor?? (mGlu??: from an artificial neural network virtual screen to an in vivo tool compound. ChemMedChem. 2012 Mar 5;7(3):406-14. | ||||
Ref 531998 | In vitro characterisation of the novel positive allosteric modulators of the mGlu??receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat. Neuropharmacology. 2013 Jan;64:224-39. | ||||
Ref 532044 | Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover. Bioorg Med Chem Lett. 2012 Oct 15;22(20):6481-5. | ||||
Ref 532112 | Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity. Biol Psychiatry. 2013 Mar 15;73(6):501-9. | ||||
Ref 532177 | Mechanism based neurotoxicity of mGlu5 positive allosteric modulators--development challenges for a promising novel antipsychotic target. Neuropharmacology. 2014 Jul;82:161-73. | ||||
Ref 532189 | Discovery of N-Aryl Piperazines as Selective mGlu(5) Potentiators with Efficacy in a Rodent Model Predictive of Anti-Psychotic Activity. ACS Med Chem Lett. 2010 Nov 11;1(8):433-438. Epub 2010 Aug 13. | ||||
Ref 532201 | A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signaling. Mol Pharmacol. 2013 Apr;83(4):835-47. | ||||
Ref 532205 | Discovery and structure-activity relationship of 1,3-cyclohexyl amide derivatives as novel mGluR5 negative allosteric modulators. Bioorg Med Chem Lett. 2013 Mar 1;23(5):1398-406. | ||||
Ref 532212 | Discovery of (1R,2R)-N-(4-(6-isopropylpyridin-2-yl)-3-(2-methyl-2H-indazol-5-yl)isothiazol-5-yl)-2-methylcyclopropanecarboxamide, a potent and orally efficacious mGlu5 receptor negative allosteric modulator. Bioorg Med Chem Lett. 2013 Mar 1;23(5):1249-52. | ||||
Ref 532244 | Discovery of biological evaluation of pyrazole/imidazole amides as mGlu5 receptor negative allosteric modulators. Bioorg Med Chem Lett. 2013 Apr 1;23(7):2134-9. | ||||
Ref 532357 | Substituted 1-Phenyl-3-(pyridin-2-yl)urea negative allosteric modulators of mGlu5: discovery of a new tool compound VU0463841 with activity in rat models of cocaine addiction. ACS Chem Neurosci. 2013Aug 21;4(8):1217-28. | ||||
Ref 532401 | Metabolism and disposition of the metabotropic glutamate receptor 5 antagonist (mGluR5) mavoglurant (AFQ056) in healthy subjects. Drug Metab Dispos. 2013 Sep;41(9):1626-41. | ||||
Ref 532936 | An allosteric modulator to control endogenous G protein-coupled receptors with light. Nat Chem Biol. 2014 Oct;10(10):813-5. | ||||
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Ref 536890 | Novel treatments of GERD: focus on the lower esophageal sphincter. Eur Rev Med Pharmacol Sci. 2008 Aug;12 Suppl 1:103-10. | ||||
Ref 537360 | A 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. | ||||
Ref 543750 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 293). | ||||
Ref 544372 | Social Communication is an Emerging Target for Pharmacotherapy in Autism Spectrum Disorder - A Review of the Literature on Potential Agents. J Can Acad Child Adolesc Psychiatry. 2014 February; 23(1):20-30. |
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