General Information of Drug Therapeutic Target (DTT) (ID: TTHS256)

DTT Name Metabotropic glutamate receptor 5 (mGluR5)
Synonyms MGLUR5; GPRC1E
Gene Name GRM5
DTT Type
Clinical trial target
[1]
Related Disease
Fragile X chromosome [ICD-11: LD55]
Parkinsonism [ICD-11: 8A00]
BioChemical Class
GPCR glutamate
UniProt ID
GRM5_HUMAN
TTD ID
T99347
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MVLLLILSVLLLKEDVRGSAQSSERRVVAHMPGDIIIGALFSVHHQPTVDKVHERKCGAV
REQYGIQRVEAMLHTLERINSDPTLLPNITLGCEIRDSCWHSAVALEQSIEFIRDSLISS
EEEEGLVRCVDGSSSSFRSKKPIVGVIGPGSSSVAIQVQNLLQLFNIPQIAYSATSMDLS
DKTLFKYFMRVVPSDAQQARAMVDIVKRYNWTYVSAVHTEGNYGESGMEAFKDMSAKEGI
CIAHSYKIYSNAGEQSFDKLLKKLTSHLPKARVVACFCEGMTVRGLLMAMRRLGLAGEFL
LLGSDGWADRYDVTDGYQREAVGGITIKLQSPDVKWFDDYYLKLRPETNHRNPWFQEFWQ
HRFQCRLEGFPQENSKYNKTCNSSLTLKTHHVQDSKMGFVINAIYSMAYGLHNMQMSLCP
GYAGLCDAMKPIDGRKLLESLMKTNFTGVSGDTILFDENGDSPGRYEIMNFKEMGKDYFD
YINVGSWDNGELKMDDDEVWSKKSNIIRSVCSEPCEKGQIKVIRKGEVSCCWTCTPCKEN
EYVFDEYTCKACQLGSWPTDDLTGCDLIPVQYLRWGDPEPIAAVVFACLGLLATLFVTVV
FIIYRDTPVVKSSSRELCYIILAGICLGYLCTFCLIAKPKQIYCYLQRIGIGLSPAMSYS
ALVTKTNRIARILAGSKKKICTKKPRFMSACAQLVIAFILICIQLGIIVALFIMEPPDIM
HDYPSIREVYLICNTTNLGVVTPLGYNGLLILSCTFYAFKTRNVPANFNEAKYIAFTMYT
TCIIWLAFVPIYFGSNYKIITMCFSVSLSATVALGCMFVPKVYIILAKPERNVRSAFTTS
TVVRMHVGDGKSSSAASRSSSLVNLWKRRGSSGETLRYKDRRLAQHKSEIECFTPKGSMG
NGGRATMSSSNGKSVTWAQNEKSSRGQHLWQRLSIHINKKENPNQTAVIKPFPKSTESRG
LGAGAGAGGSAGGVGATGGAGCAGAGPGGPESPDAGPKALYDVAEAEEHFPAPARPRSPS
PISTLSHRAGSASRTDDDVPSLHSEPVARSSSSQGSLMEQISSVVTRFTANISELNSMML
STAAPSPGVGAPLCSSYLIPKEIQLPTTMTTFAEIQPLPAIEVTGGAQPAAGAQAAGDAA
RESPAAGPEAAAAKPDLEELVALTPPSPFRDSVDSGSTTPNSPVSESALCIPSSPKYDTL
IIRDYTQSSSSL
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.
KEGG Pathway
Calcium signaling pathway (hsa04020 )
Neuroactive ligand-receptor interaction (hsa04080 )
Gap junction (hsa04540 )
Long-term potentiation (hsa04720 )
Retrograde endocannabinoid signaling (hsa04723 )
Glutamatergic synapse (hsa04724 )
Huntington's disease (hsa05016 )
Reactome Pathway
Class C/3 (Metabotropic glutamate/pheromone receptors) (R-HSA-420499 )
G alpha (q) signalling events (R-HSA-416476 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
9 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
ADX-48621 DM6GTMD Parkinson disease 8A00.0 Phase 2/3 [2]
Afq056 DMMHSLC Fragile X syndrome LD55 Phase 2/3 [1]
ADX10059 DMGVKHQ Anxiety disorder 6B00-6B0Z Phase 2 [3], [4]
RG-7090 DMX8JYN Fragile X syndrome LD55 Phase 2 [5]
STX-107 DMLNKX7 Autism spectrum disorder 6A02 Phase 2 [6], [7]
McN3377 DMTCADJ Fragile X syndrome LD55 Phase 1/2 [8]
MK-3328 DMW2O5D Alzheimer disease 8A20 Phase 1 [9]
RG7342 DMIW5NG Schizophrenia 6A20 Phase 1 [10]
[3H]fenobam DMBOXA1 Allodynia MB40.1 Phase 1 [11]
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⏷ Show the Full List of 9 Clinical Trial Drug(s)
68 Patented Agent(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
2-(substituted ethynyl)quinoline derivative 1 DMOY5EK N. A. N. A. Patented [12]
2-(substituted ethynyl)quinoline derivative 2 DMPCYSW N. A. N. A. Patented [12]
2-(substituted ethynyl)quinoline derivative 3 DMMF8A1 N. A. N. A. Patented [12]
2-(substituted ethynyl)quinoline derivative 4 DMTXZUF N. A. N. A. Patented [12]
6-aryl-imidazopyridine and 6-aryl-triazolopyridine carboxamide analog 1 DMTXGYS N. A. N. A. Patented [12]
6-aryl-imidazopyridine and 6-aryl-triazolopyridine carboxamide analog 2 DMFKTBM N. A. N. A. Patented [12]
6-aryl-imidazopyridine and 6-aryl-triazolopyridine carboxamide analog 3 DMXMTLP N. A. N. A. Patented [12]
Bicarboxylic and tricarboxylic ethynyl derivative 1 DMDK7LQ N. A. N. A. Patented [12]
Bicarboxylic and tricarboxylic ethynyl derivative 2 DMG9O7D N. A. N. A. Patented [12]
Bicarboxylic and tricarboxylic ethynyl derivative 3 DM1KVTZ N. A. N. A. Patented [12]
Bicyclic heteroaryl carboxamide analog 1 DMB5XDM N. A. N. A. Patented [12]
Bicyclic heteroaryl carboxamide analog 2 DMKT7MD N. A. N. A. Patented [12]
Bicyclic heteroaryl carboxamide analog 3 DM3QMA0 N. A. N. A. Patented [12]
Central azetidine derivative 1 DM7INA1 N. A. N. A. Patented [12]
Central azetidine derivative 2 DM2BLJ6 N. A. N. A. Patented [12]
Diazepinone derivative 1 DM9YD0Q Parkinson disease 8A00.0 Patented [12]
Diazepinone derivative 2 DMLQ7PG Parkinson disease 8A00.0 Patented [12]
Diazepinone derivative 3 DMPTZ69 Parkinson disease 8A00.0 Patented [12]
Diazepinone derivative 4 DM389YD Parkinson disease 8A00.0 Patented [12]
Diazepinone derivative 5 DM2U1QH Parkinson disease 8A00.0 Patented [12]
Ethynyl compound 1 DMWXKRZ N. A. N. A. Patented [12]
Ethynyl compound 2 DMJDG37 N. A. N. A. Patented [12]
Ethynyl compound 3 DMD9PZQ N. A. N. A. Patented [12]
Ethynyl compound 4 DMLDMO8 N. A. N. A. Patented [12]
Ethynyl compound 5 DM53ZPE N. A. N. A. Patented [12]
Ethynyl compound 6 DMDOEFC N. A. N. A. Patented [12]
Ethynyl compound 7 DMPUG2M N. A. N. A. Patented [12]
Heterocyclic derivative 1 DMJ5X46 N. A. N. A. Patented [12]
Heterocyclic derivative 2 DM2QCBF N. A. N. A. Patented [12]
Heterocyclic derivative 3 DMCD0MS N. A. N. A. Patented [12]
Imidazopyridine and triazolopyridine compound 1 DMTUS0Y N. A. N. A. Patented [12]
Imidazopyridine and triazolopyridine compound 2 DMYCLAM N. A. N. A. Patented [12]
Imidazopyridine and triazolopyridine compound 3 DMWU8VM N. A. N. A. Patented [12]
Imidazopyridine and triazolopyridine compound 4 DMI1OWK N. A. N. A. Patented [12]
Imidazo[1,2-a]pyridine derivative 1 DM5NEQ2 N. A. N. A. Patented [12]
N-alkylamide derivative 1 DMXPBL5 N. A. N. A. Patented [12]
N-alkylamide derivative 2 DM568TX N. A. N. A. Patented [12]
PMID28067079-Compound-95 DMG2PCZ N. A. N. A. Patented [12]
PMID28067079-Compound-97 DMCUX42 N. A. N. A. Patented [12]
PMID28067079-Compound-98 DMLKP1O N. A. N. A. Patented [12]
Pyrazolopyrimidine derivative 1 DMHO3NB N. A. N. A. Patented [12]
Pyrazolopyrimidine derivative 2 DMZEP5X N. A. N. A. Patented [12]
Pyrazolopyrimidine derivative 3 DMI0J7D N. A. N. A. Patented [12]
Pyrazolopyrimidine derivative 4 DM7XSHK N. A. N. A. Patented [12]
Pyrazolopyrimidine derivative 5 DMVUSF3 N. A. N. A. Patented [12]
Pyrazolopyrimidine derivative 6 DMG8V31 N. A. N. A. Patented [12]
Pyridine derivative 12 DM8KBHX N. A. N. A. Patented [12]
Pyridine derivative 13 DMX8RGH N. A. N. A. Patented [12]
Pyridine derivative 14 DM7JCM6 N. A. N. A. Patented [12]
Pyridine derivative 15 DMGBR43 N. A. N. A. Patented [12]
Pyridine derivative 16 DMICZLS N. A. N. A. Patented [12]
Pyridine derivative 17 DMLC5WA N. A. N. A. Patented [12]
Pyrrolidine derivative 1 DMXALJE N. A. N. A. Patented [12]
Pyrrolidine derivative 2 DM5WA29 N. A. N. A. Patented [12]
Pyrrolidine derivative 3 DMHM8WJ N. A. N. A. Patented [12]
Pyrrolidine derivative 4 DMZ2HBL N. A. N. A. Patented [12]
Pyrrolidine derivative 5 DM5NKXO N. A. N. A. Patented [12]
Tetra-hydro-oxazolopyridine derivative 1 DM72MDA N. A. N. A. Patented [12]
Tetra-hydro-oxazolopyridine derivative 2 DMP65Z4 N. A. N. A. Patented [12]
Tetra-hydro-oxazolopyridine derivative 3 DMQYKT2 N. A. N. A. Patented [12]
Tetra-hydro-oxazolopyridine derivative 4 DM21J83 N. A. N. A. Patented [12]
Tetra-hydro-oxazolopyridine derivative 5 DMQGA1I N. A. N. A. Patented [12]
Tetra-hydro-oxazolopyridine derivative 6 DMLW7YO N. A. N. A. Patented [12]
Tetra-hydro-pyrazolopyrazine derivative 1 DM3HVCZ N. A. N. A. Patented [12]
Tetra-hydro-pyrazolopyrazine derivative 2 DMQ027F N. A. N. A. Patented [12]
Tetra-hydro-pyrazolopyrazine derivative 3 DMKGJ1S N. A. N. A. Patented [12]
Tetra-hydro-pyrazolopyrazine derivative 4 DMRMTF6 N. A. N. A. Patented [12]
Tetra-hydro-pyrazolopyrazine derivative 5 DMAM7Y2 N. A. N. A. Patented [12]
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⏷ Show the Full List of 68 Patented Agent(s)
4 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
AZD2066 DMHP6OY Chronic neuropathic pain MG30.5 Discontinued in Phase 2 [13]
AZD2516 DM9OPDE Chronic neuropathic pain MG30.5 Discontinued in Phase 2 [13]
LY467711 DM0TV9L Migraine 8A80 Terminated [8]
LY525327 DMPNMAR Migraine 8A80 Terminated [8]
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264 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
(+)-MCPG DMG5QJB Discovery agent N.A. Investigative [14]
(1S,3R)-ACPD DM5DOAF Discovery agent N.A. Investigative [14]
(3-(2-methylquinolin-7-yl)phenyl)methanol DMR6JTQ Discovery agent N.A. Investigative [15]
(3-Ethoxy-pyridin-2-yl)-pyridin-2-yl-amine DMG1KIJ Discovery agent N.A. Investigative [16]
(E)-1-Adamantan-1-yl-3-quinolin-3-yl-propenone DMQ9TWD Discovery agent N.A. Investigative [17]
(E)-3-[2-(2-methyl-4-thiazolyl)vinyl]pyridine DMITXKJ Discovery agent N.A. Investigative [18]
(S)-(+)-CBPG DMPDOY8 Discovery agent N.A. Investigative [19]
(S)-3HPG DMQ0FVJ Discovery agent N.A. Investigative [14]
(S)-4C3HPG DMQK4I2 Discovery agent N.A. Investigative [14]
(S)-4CPG DMZ9UIL Discovery agent N.A. Investigative [14]
1-(3-(2-methylquinolin-7-yl)phenyl)ethanone DMD25N9 Discovery agent N.A. Investigative [15]
2-(2-Methyl-thiazol-4-ylethynyl)-pyridine DMIHTL0 Discovery agent N.A. Investigative [20]
2-(2-methylquinolin-7-yl)benzonitrile DMENUIH Discovery agent N.A. Investigative [15]
2-(3,4-dimethylphenyl)-1,8-naphthyridine DMDGRWM Discovery agent N.A. Investigative [21]
2-(3,5-dichlorophenyl)pyrido[2,3-d]pyrimidine DM8KM1Q Discovery agent N.A. Investigative [22]
2-(3,5-difluorophenyl)-7-methyl-1,8-naphthyridine DMGJPYO Discovery agent N.A. Investigative [21]
2-(3,5-dimethoxyphenyl)-1,8-naphthyridine DMKND0T Discovery agent N.A. Investigative [21]
2-(3-(2-methylquinolin-7-yl)phenyl)acetonitrile DMLJH92 Discovery agent N.A. Investigative [15]
2-(3-(3-methoxyphenoxy)prop-1-ynyl)pyridine DM1VSOK Discovery agent N.A. Investigative [23]
2-(3-(benzyloxy)phenyl)isoindoline-1,3-dione DM0R5U6 Discovery agent N.A. Investigative [24]
2-(3-bromophenyl)-7-methyl-1,8-naphthyridine DMYSM9L Discovery agent N.A. Investigative [21]
2-(3-bromophenyl)-7-methylpyrido[2,3-d]pyrimidine DMANS5X Discovery agent N.A. Investigative [22]
2-(3-bromophenyl)pyrido[2,3-d]pyrimidine DMVA4XC Discovery agent N.A. Investigative [22]
2-(3-chlorobenzyloxy)-6-chloroisonicotinonitrile DM1VDC3 Discovery agent N.A. Investigative [24]
2-(3-chlorophenyl)-7-methyl-1,8-naphthyridine DM7BC50 Discovery agent N.A. Investigative [21]
2-(4-(3-chlorophenyl)but-1-ynyl)-6-methylpyridine DM27CQJ Discovery agent N.A. Investigative [25]
2-(m-tolylethynyl)pyrimidine DM15BA7 Discovery agent N.A. Investigative [26]
2-(phenylethynyl)pyrimidine DMRIFCW Discovery agent N.A. Investigative [26]
2-(pyridin-2-yl)-4-(m-tolylthio)pyrimidine DM3EBYD Discovery agent N.A. Investigative [27]
2-Benzoxy-5-(2-methylquinolin-7-yl)benzonitrile DMQX9PD Discovery agent N.A. Investigative [7]
2-benzyloxy-7,8-dihydro-6H-quinolin-5-one DMCLAXG Discovery agent N.A. Investigative [28]
2-bromo-4-(3-fluorophenylethynyl)thiazole DMCM01R Discovery agent N.A. Investigative [18]
2-Chloro-5-(2-methylquinolin-7-yl)nicotinonitrile DM5KR4B Discovery agent N.A. Investigative [7]
2-chloro-N-(3-(3-chlorobenzamido)phenyl)benzamide DM2W71L Discovery agent N.A. Investigative [29]
2-Cyclohex-1-enylethynyl-pyridine DM2U1N5 Discovery agent N.A. Investigative [30]
2-Cyclohexylethynyl-pyridine DM2JZ84 Discovery agent N.A. Investigative [30]
2-Cyclopent-1-enylethynyl-pyridine DMVP6CW Discovery agent N.A. Investigative [30]
2-ethoxy-5-(m-tolylethynyl)pyrimidine DMGRA3T Discovery agent N.A. Investigative [26]
2-ethynyl-4-(3-fluorophenylethynyl)thiazole DME6VKS Discovery agent N.A. Investigative [18]
2-m-tolyl-1,8-naphthyridine DMBWDXH Discovery agent N.A. Investigative [21]
2-methyl-4-(2-thienylethynyl)thiazole DMAFPE7 Discovery agent N.A. Investigative [18]
2-methyl-4-(3-thienylethynyl)thiazole DMK4A0J Discovery agent N.A. Investigative [18]
2-methyl-4-(m-tolylethynyl)thiazole DM4P3CW Discovery agent N.A. Investigative [18]
2-Methyl-4-o-tolylethynyl-thiazole DMKFBVS Discovery agent N.A. Investigative [20]
2-Methyl-4-p-tolylethynyl-thiazole DMWRCFY Discovery agent N.A. Investigative [20]
2-Methyl-4-phenylethynyl-thiazole DMRC60A Discovery agent N.A. Investigative [20]
2-methyl-6-(3-(p-tolyloxy)prop-1-ynyl)pyridine DMGPDYE Discovery agent N.A. Investigative [23]
2-methyl-6-(3-(phenylthio)prop-1-ynyl)pyridine DM536IA Discovery agent N.A. Investigative [25]
2-methyl-6-(4-phenylbut-1-ynyl)pyridine DM1YK7M Discovery agent N.A. Investigative [25]
2-methyl-6-(4-phenylpent-1-ynyl)pyridine DM0UNM1 Discovery agent N.A. Investigative [25]
2-methyl-6-(5-phenylpent-1-ynyl)pyridine DMDVO7Z Discovery agent N.A. Investigative [25]
2-methyl-6-(phenylethynyl)pyridine DMVQK4Y Discovery agent N.A. Investigative [31], [32]
2-methyl-7-(pyridin-3-yl)quinoline DM9FZ0B Discovery agent N.A. Investigative [15]
2-methyl-7-m-tolyl-1,6-naphthyridine DMMFKOH Discovery agent N.A. Investigative [21]
2-methyl-7-m-tolyl-1,8-naphthyridine DMZFK4R Discovery agent N.A. Investigative [21]
2-methyl-7-m-tolylquinoline DMC02TI Discovery agent N.A. Investigative [15]
2-methyl-7-phenyl-1,8-naphthyridine DM8RV5X Discovery agent N.A. Investigative [21]
2-methyl-7-phenylquinoline DMT7MVD Discovery agent N.A. Investigative [15]
2-phenyl-1,8-naphthyridine DM3WOHI Discovery agent N.A. Investigative [21]
2-Phenyl-5-(2-methylthiazol-4ylethynyl)pyridine DM7A3GO Discovery agent N.A. Investigative [33]
2-phenylethynyl-5,6,7,8-tetrahydro-quinolin-5-ol DMNYOH5 Discovery agent N.A. Investigative [28]
2-phenylethynyl-5,6,7,8-tetrahydro-quinoline DM4LCRS Discovery agent N.A. Investigative [28]
2-phenylethynyl-7,8-dihydro-6H-quinolin-5-one DMFRQJ3 Discovery agent N.A. Investigative [28]
2-[(2-methyl-4-thiazolyl)ethynyl]pyrazine DM75WN4 Discovery agent N.A. Investigative [18]
3,3'-difluorobenzaldazine DMGMJWL Discovery agent N.A. Investigative [34]
3,5-DHPG DMFEQ6S Discovery agent N.A. Investigative [14]
3-(1,5-naphthyridin-3-yl)benzonitrile DM24BG6 Discovery agent N.A. Investigative [21]
3-(1,8-naphthyridin-2-yl)benzonitrile DMSP4N5 Discovery agent N.A. Investigative [21]
3-(1-Pyridin-2-yl-1H-pyrazol-3-yl)-benzonitrile DMTD7VE Discovery agent N.A. Investigative [35]
3-(1-Pyridin-2-yl-1H-pyrazol-4-yl)-benzonitrile DMWI37C Discovery agent N.A. Investigative [35]
3-(1-Pyridin-2-yl-1H-pyrrol-3-yl)-benzonitrile DMJ9LRE Discovery agent N.A. Investigative [35]
3-(2-methylbenzo[d]thiazol-5-yl)benzonitrile DMY782R Discovery agent N.A. Investigative [36]
3-(2-methylquinolin-7-yl)benzonitrile DMUPB9H Discovery agent N.A. Investigative [15]
3-(2-methylquinolin-7-yl)phenol DM41HMZ Discovery agent N.A. Investigative [15]
3-(2-Pyridin-2-yl-2H-tetrazol-5-yl)-benzonitrile DMPWEL8 Discovery agent N.A. Investigative [35]
3-(3,4-dimethylphenyl)-1,5-naphthyridine DMULX9O Discovery agent N.A. Investigative [21]
3-(3-(3-chlorobenzyloxy)-5-methylphenyl)pyridine DMKAEUD Discovery agent N.A. Investigative [24]
3-(3-bromophenylethynyl)-5-methyl[1,2,4]triazine DMFPTXO Discovery agent N.A. Investigative [37]
3-(3-methylphenylethynyl)-5-methyl[1,2,4]triazine DMXAD0R Discovery agent N.A. Investigative [37]
3-(3-Pyridin-2-yl-pyrazol-1-yl)-benzonitrile DMU52WA Discovery agent N.A. Investigative [35]
3-(3-Pyridin-2-yl-pyrrol-1-yl)-benzonitrile DMZLT24 Discovery agent N.A. Investigative [35]
3-(4-Pyridin-2-yl-imidazol-1-yl)-benzonitrile DMDYVA7 Discovery agent N.A. Investigative [35]
3-(4-Pyridin-2-yl-pyrazol-1-yl)-benzonitrile DMTD16H Discovery agent N.A. Investigative [35]
3-(5-Pyridin-2-yl-tetrazol-2-yl)-benzonitrile DMM1CKZ Discovery agent N.A. Investigative [35]
3-(6-fluoroquinazolin-4-ylamino)benzonitrile DMHJ0SV Discovery agent N.A. Investigative [32]
3-(7-methyl-1,8-naphthyridin-2-yl)benzonitrile DMZ53N4 Discovery agent N.A. Investigative [21]
3-biphenyl-4-ylethynyl-5-methyl-[1,2,4]triazine DMMC2Q9 Discovery agent N.A. Investigative [37]
3-bromo-5-(2-methylquinolin-7-yl)benzonitrile DMPQOS2 Discovery agent N.A. Investigative [15]
3-bromo-5-[(2-methyl-4-thiazolyl)ethynyl]pyridine DMOXY78 Discovery agent N.A. Investigative [18]
3-bromo-N-(6-methylpyridin-2-yl)benzamide DM62Y1S Discovery agent N.A. Investigative [38]
3-chloro-5-(2-methylquinolin-7-yl)benzonitrile DMBMH96 Discovery agent N.A. Investigative [15]
3-chloro-N-(3-isobutyramidophenyl)benzamide DMV8TNO Discovery agent N.A. Investigative [29]
3-chloro-N-(4-methylthiazol-2-yl)benzamide DM4EL6M Discovery agent N.A. Investigative [38]
3-chloro-N-(6-chloropyridin-2-yl)benzamide DMLC2I6 Discovery agent N.A. Investigative [38]
3-chloro-N-(6-methylpyridin-2-yl)benzamide DMLJGF1 Discovery agent N.A. Investigative [33]
3-cyano-5-fluoro-N-(3-fluorophenyl)benzamide DMF1PIW Discovery agent N.A. Investigative [39]
3-cyano-5-fluoro-N-(pyridin-2-yl)benzamide DMBA4XN Discovery agent N.A. Investigative [39]
3-cyano-5-fluoro-N-m-tolylbenzamide DMF097H Discovery agent N.A. Investigative [39]
3-cyano-5-fluoro-N-phenylbenzamide DMIZ8RC Discovery agent N.A. Investigative [39]
3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide DMH7FC9 Discovery agent N.A. Investigative [40], [41]
3-cyano-N-(1,4-diphenyl-1H-pyrazol-5-yl)benzamide DM3EIWC Discovery agent N.A. Investigative [41]
3-cyano-N-(3-cyanophenyl)-5-fluorobenzamide DMRD8VM Discovery agent N.A. Investigative [39]
3-cyano-N-(3-ethylphenyl)-5-fluorobenzamide DMFUT57 Discovery agent N.A. Investigative [39]
3-cyano-N-(3-ethynylphenyl)-5-fluorobenzamide DM9FEMV Discovery agent N.A. Investigative [39]
3-cyano-N-(6-ethylpyridin-2-yl)-5-fluorobenzamide DMUB9XW Discovery agent N.A. Investigative [39]
3-cyano-N-(6-methylpyridin-2-yl)benzamide DMTDEYL Discovery agent N.A. Investigative [33]
3-ethoxy-5-(2-methylquinolin-7-yl)benzonitrile DMSK6EM Discovery agent N.A. Investigative [15]
3-fluoro-5-(1,6-naphthyridin-7-yl)benzonitrile DMH9VLF Discovery agent N.A. Investigative [21]
3-fluoro-5-(2-methylquinolin-7-yl)benzonitrile DM2V45Z Discovery agent N.A. Investigative [15]
3-hydroxy-5-(2-methylquinolin-7-yl)benzonitrile DMZS4P7 Discovery agent N.A. Investigative [15]
3-iodo-N-(6-methylpyridin-2-yl)benzamide DMDSJ0O Discovery agent N.A. Investigative [38]
3-isobutoxy-5-(2-methylquinolin-7-yl)benzonitrile DMWP0LZ Discovery agent N.A. Investigative [15]
3-m-tolyl-1,5-naphthyridine DMMFA4N Discovery agent N.A. Investigative [21]
3-methoxy-5-(1,5-naphthyridin-3-yl)benzonitrile DMHYRES Discovery agent N.A. Investigative [21]
3-methoxy-5-(1,6-naphthyridin-7-yl)benzonitrile DMKHJ8G Discovery agent N.A. Investigative [21]
3-methoxy-5-(2-methylquinolin-7-yl)benzonitrile DMRMZLV Discovery agent N.A. Investigative [15]
3-methoxy-N-(4-methylthiazol-2-yl)benzamide DM4WJX3 Discovery agent N.A. Investigative [38]
3-methoxy-N-(6-methylpyridin-2-yl)benzamide DMSFJNE Discovery agent N.A. Investigative [38]
3-methyl-5-(2-methylquinolin-7-yl)benzonitrile DMM3RNV Discovery agent N.A. Investigative [15]
3-methyl-N-(6-methylpyridin-2-yl)benzamide DMRNMKG Discovery agent N.A. Investigative [38]
3-nitro-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide DMIZJ9G Discovery agent N.A. Investigative [41]
3-Phenyl-1-(2-methylthiazol-4-ylethynyl)benzene DMGPOZE Discovery agent N.A. Investigative [33]
3-[(2,5-dimethyl-4-thiazolyl)ethynyl]pyridine DMBAHRJ Discovery agent N.A. Investigative [18]
3-[(2-methyl-4-thiazolyl)ethynyl]-5-vinylpyridine DMZ78WB Discovery agent N.A. Investigative [18]
3-[(2-methyl-4-thiazolyl)ethynyl]benzamide DMMLDOZ Discovery agent N.A. Investigative [18]
3-[(2-methyl-4-thiazolyl)ethynyl]benzonitrile DMQUDR1 Discovery agent N.A. Investigative [42], [18]
3-[(2-methyl-4-thiazolyl)ethynyl]phenol DMF0QM2 Discovery agent N.A. Investigative [18]
3-[(5-ethyl-2-methyl-4-thiazolyl)ethynyl]pyridine DM9OI2R Discovery agent N.A. Investigative [18]
3-[(6-Methylpyridin-2-yl)ethynyl]benzonitrile DMH5329 Discovery agent N.A. Investigative [33]
4-(2-(3-fluorophenyl)ethynyl)-2-methylthiazole DMRDWUT Discovery agent N.A. Investigative [18]
4-(2-(4-fluorophenyl)ethynyl)-2-methylthiazole DMOX40J Discovery agent N.A. Investigative [18]
4-(2-fluorophenylethynyl)-2-methylthiazole DMCWZF6 Discovery agent N.A. Investigative [18]
4-(2-methoxyphenylethynyl)-2-methylthiazole DMFVYHI Discovery agent N.A. Investigative [18]
4-(2-Methyl-thiazol-4-ylethynyl)-pyridine DMEAV9Q Discovery agent N.A. Investigative [20]
4-(3,5-difluorophenylethynyl)-2-methylthiazole DM48Z5Y Discovery agent N.A. Investigative [18]
4-(3-bromophenoxy)-6-chloroquinazoline DM3LGOT Discovery agent N.A. Investigative [32]
4-(3-bromophenylthio)-2-(pyridin-2-yl)pyrimidine DMQBHF2 Discovery agent N.A. Investigative [27]
4-(3-chlorophenylethynyl)-2-methylthiazole DMDTFKL Discovery agent N.A. Investigative [18]
4-(3-chlorophenylthio)-2-(pyridin-2-yl)pyrimidine DMJH2OE Discovery agent N.A. Investigative [27]
4-(3-fluorophenylethynyl)-2-thiazolylamine DM6RV9L Discovery agent N.A. Investigative [18]
4-(3-methoxyphenylethynyl)-2-methylthiazole DMGCPKU Discovery agent N.A. Investigative [18]
4-(3-pyridylethynyl)-2-thiazolylamine DMRXKMP Discovery agent N.A. Investigative [18]
4-(4-chlorophenylthio)-2-(pyridin-2-yl)pyrimidine DM9YRHW Discovery agent N.A. Investigative [27]
4-Biphenyl-2-ylethynyl-2-methyl-thiazole DM3B2TG Discovery agent N.A. Investigative [20]
4-Biphenyl-4-ylethynyl-2-methyl-thiazole DMCQYKO Discovery agent N.A. Investigative [20]
4-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide DMJ610E Discovery agent N.A. Investigative [41]
5-((6-Methylpyridin-2-yl)ethynyl)nicotinonitrile DMBSFLW Discovery agent N.A. Investigative [7]
5-(2-(2,5-dimethylphenyl)ethynyl)pyrimidine DMCFKGW Discovery agent N.A. Investigative [43]
5-(2-(3,5-difluorophenyl)ethynyl)pyrimidine DM3XMKJ Discovery agent N.A. Investigative [43]
5-(2-(3-chlorophenyl)ethynyl)pyrimidine DM37KG6 Discovery agent N.A. Investigative [43]
5-(2-(4-fluoro-3-methylphenyl)ethynyl)pyrimidine DMRS1Q5 Discovery agent N.A. Investigative [43]
5-(2-m-tolylethynyl)pyrimidine DMO5WG8 Discovery agent N.A. Investigative [43]
5-(2-Methylquinolin-7-yl)-2-phenylbenzonitrile DMIQJM4 Discovery agent N.A. Investigative [7]
5-(2-Methylquinolin-7-yl)-2-phenylnicotinonitrile DMO74HX Discovery agent N.A. Investigative [7]
5-(2-methylquinolin-7-yl)isophthalonitrile DMMX69H Discovery agent N.A. Investigative [15]
5-(2-methylquinolin-7-yl)nicotinonitrile DM8LN2X Discovery agent N.A. Investigative [15]
5-(3-chlorophenylethynyl)-5-methyl[1,2,4]triazine DMABSOC Discovery agent N.A. Investigative [37]
5-(phenylethynyl)pyrimidine DMP4RO3 Discovery agent N.A. Investigative [43]
5-Biphenyl-4-ylethynyl-pyrimidine DMMG9PV Discovery agent N.A. Investigative [43]
5-Chloro-2-(2-methylquinolin-7-yl)benzonitrile DMH4SLZ Discovery agent N.A. Investigative [7]
5-methyl-3-phenylethynyl[1,2,4]triazine DMF0IJ2 Discovery agent N.A. Investigative [37]
5-MPEP DMSRGTI Discovery agent N.A. Investigative [44]
5-[(2-methyl-4-thiazolyl)ethynyl]pyrimidine DMM9GCA Discovery agent N.A. Investigative [18]
5PAM523 DMPLB3S Discovery agent N.A. Investigative [45]
6-(4-chlorophenylamino)-N,N-diethylnicotinamide DMOZFU5 Discovery agent N.A. Investigative [46]
6-bromo-N-(3-bromophenyl)quinazolin-4-amine DMP9O7G Discovery agent N.A. Investigative [32]
6-bromo-N-(3-chlorophenyl)quinazolin-4-amine DM0A3DB Discovery agent N.A. Investigative [32]
6-bromo-N-(3-fluorophenyl)quinazolin-4-amine DM2IP5F Discovery agent N.A. Investigative [32]
6-bromo-N-m-tolylquinazolin-4-amine DM2MJ9F Discovery agent N.A. Investigative [32]
6-chloro-N-(3-chlorophenyl)quinazolin-4-amine DMPIFLA Discovery agent N.A. Investigative [32]
6-fluoro-N-m-tolylquinazolin-4-amine DMVADTP Discovery agent N.A. Investigative [32]
6-phenylethynyl-nicotinic acid methyl ester DMIKRP6 Discovery agent N.A. Investigative [28]
7-(2-methoxyphenyl)-2-methylquinoline DMO8DYW Discovery agent N.A. Investigative [15]
7-(3,5-dimethoxyphenyl)-1,6-naphthyridine DM2RFOB Discovery agent N.A. Investigative [21]
7-(3-(methoxymethyl)phenyl)-2-methylquinoline DMYNLOI Discovery agent N.A. Investigative [15]
7-(3-chlorophenyl)-2-methylquinoline DM0Q56N Discovery agent N.A. Investigative [15]
7-(3-fluoro-5-methylphenyl)-1,6-naphthyridine DME2VD7 Discovery agent N.A. Investigative [21]
7-(3-fluorophenyl)-2-methylquinoline DMDXOBH Discovery agent N.A. Investigative [15]
7-(3-methoxyphenyl)-2-methyl-1,6-naphthyridine DMEC9YK Discovery agent N.A. Investigative [21]
7-(3-methoxyphenyl)-2-methylquinoline DMW6LCH Discovery agent N.A. Investigative [15]
7-(4,6-dimethoxypyrimidin-2-yl)-2-methylquinoline DMHXMY5 Discovery agent N.A. Investigative [36]
7-(4,6-dimethylpyrimidin-2-yl)-2-methylquinoline DMQFBTW Discovery agent N.A. Investigative [36]
7-(4-methoxyphenyl)-2-methylquinoline DMBT1KS Discovery agent N.A. Investigative [15]
7-(4-methoxypyrimidin-2-yl)-2-methylquinoline DMSRKF0 Discovery agent N.A. Investigative [36]
7-bromo-N-(3-bromophenyl)isoquinolin-1-amine DML8PH7 Discovery agent N.A. Investigative [32]
7-m-tolyl-1,6-naphthyridine DMBDFP2 Discovery agent N.A. Investigative [21]
7-methyl-2-m-tolylpyrido[2,3-d]pyrimidine DMCV891 Discovery agent N.A. Investigative [22]
7-methyl-2-phenylpyrido[2,3-d]pyrimidine DMJ4G27 Discovery agent N.A. Investigative [22]
ACDPP DMPMH7Z Discovery agent N.A. Investigative [47]
ADX-63365 DMA74PO Central nervous system disease 8A04-8D87 Investigative [9]
alloswitch-1 DM05AYE Discovery agent N.A. Investigative [48]
BOMA DMAW40Y Discovery agent N.A. Investigative [42]
Br-5MPEPy DMBTC23 Discovery agent N.A. Investigative [44]
CHPG DMZ956E Discovery agent N.A. Investigative [14]
CPPHA DMDG2Y9 Discovery agent N.A. Investigative [49]
CPPZ DM9OWG5 Discovery agent N.A. Investigative [50]
CTEP DMYRVZ8 Fragile X syndrome LD55 Investigative [9], [51]
GRN-529 DMJ47DM Major depressive disorder 6A70.3 Investigative [9]
GSK-2210875 DM0DKQN Anxiety disorder 6B00-6B0Z Investigative [9]
ibotenate DM8RZE0 Discovery agent N.A. Investigative [14]
L-CCG-I DMPZ8XH Discovery agent N.A. Investigative [14]
LSN2463359 DMWVTS3 Discovery agent N.A. Investigative [52]
LSN2814617 DMV9NP6 Discovery agent N.A. Investigative [52]
LY-3390334 DMUXFZQ Discovery agent N.A. Investigative [53]
M-5MPEP DMFS7QK Discovery agent N.A. Investigative [44]
N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide DMDW8VX Discovery agent N.A. Investigative [41]
N-(1,4-diphenyl-1H-pyrazol-5-yl)benzamide DMEDJ7X Discovery agent N.A. Investigative [41]
N-(2-phenylimidazo[1,2-a]pyridin-3-yl)benzamide DMUILX8 Discovery agent N.A. Investigative [41]
N-(3-(3-cyanobenzamido)phenyl)-2-methoxybenzamide DMXL70A Discovery agent N.A. Investigative [29]
N-(3-acetamidophenyl)-3-chlorobenzamide DMH3R21 Discovery agent N.A. Investigative [29]
N-(3-bromophenyl)-6-chloroquinazolin-4-amine DMEWQCN Discovery agent N.A. Investigative [32]
N-(3-bromophenyl)-6-fluoroquinazolin-4-amine DMRIK7P Discovery agent N.A. Investigative [32]
N-(3-chlorophenyl)-3-cyano-5-fluorobenzamide DM3RQHG Discovery agent N.A. Investigative [39]
N-(3-chlorophenyl)-6-fluoroquinazolin-4-amine DM3AGJH Discovery agent N.A. Investigative [32]
N-(3-chlorophenyl)-6-methoxyquinazolin-4-amine DMQEPV0 Discovery agent N.A. Investigative [32]
N-(3-chlorophenyl)-6-nitroquinazolin-4-amine DMIKP5Y Discovery agent N.A. Investigative [32]
N-(6-methylpyridin-2-yl)-5-phenylpicolinamide DMQRE5D Discovery agent N.A. Investigative [54]
N-(6-methylpyridin-2-yl)-6-phenylnicotinamide DMQZMRG Discovery agent N.A. Investigative [33]
N-(6-methylpyridin-2-yl)biphenyl-3-carboxamide DMBNJ2L Discovery agent N.A. Investigative [33]
N-cyclopentyl-6-(2-phenylethynyl)nicotinamide DMDPKCM Discovery agent N.A. Investigative [55]
N-[4-(3-pyridylethynyl)-2-thiazolyl]acetamide DMC62K1 Discovery agent N.A. Investigative [18]
NCFP DM0JCN2 Discovery agent N.A. Investigative [56]
PMID14697765C11a DMFWCAJ Discovery agent N.A. Investigative [42]
PMID14697765C16a DMFT1DO Discovery agent N.A. Investigative [42]
PMID15482906C10 DM7T8BE Discovery agent N.A. Investigative [57]
PMID15482908C8 DMCPIQ4 Discovery agent N.A. Investigative [58]
PMID15686941C13 DMPB7Z6 Discovery agent N.A. Investigative [47]
PMID16439120C20 DMI8HAV Discovery agent N.A. Investigative [24]
PMID16439120C26 DMVM2XD Discovery agent N.A. Investigative [24]
PMID17189691C42 DMG9ZYP Discovery agent N.A. Investigative [59]
PMID17723296C18 DMBP3O7 Discovery agent N.A. Investigative [22]
PMID17936624C36 DMEHC2I Discovery agent N.A. Investigative [21]
PMID19931453C16m DM3DCR9 Discovery agent N.A. Investigative [46]
PMID20598884C8 DMS21ZP Discovery agent N.A. Investigative [39]
PMID20809633C29b DM0W6C9 Discovery agent N.A. Investigative [60]
PMID21295468C47 DM0DNSV Discovery agent N.A. Investigative [61]
PMID21757343C30 DM3ELPS Discovery agent N.A. Investigative [62]
PMID21927650C18 DMLGKD3 Discovery agent N.A. Investigative [63]
PMID23357634C24d DM4NAC9 Discovery agent N.A. Investigative [64]
PMID23374867C24 DMRC14X Discovery agent N.A. Investigative [65]
PMID23434029C41 DMG0XC7 Discovery agent N.A. Investigative [66]
PMID23434029C53 DMG0B4N Discovery agent N.A. Investigative [66]
PTeB DM1NM5F Discovery agent N.A. Investigative [35]
RTI-4229-982 DMG6TOA Neurological disorder 6B60 Investigative [9]
SIB-1757 DMFOGE2 Discovery agent N.A. Investigative [38]
SIB-1893 DMAVBKP Discovery agent N.A. Investigative [38]
SP203 DM6VQZ7 Discovery agent N.A. Investigative [67]
VU-1545 DMCRF48 Discovery agent N.A. Investigative [41]
VU0092273 DMT76JS Discovery agent N.A. Investigative [68]
VU0240382 DMH720P Discovery agent N.A. Investigative [68]
VU0285683 DM7VCDF Discovery agent N.A. Investigative [69]
VU0357121 DMETUHS Discovery agent N.A. Investigative [70]
VU0360172 DM3NXMB Discovery agent N.A. Investigative [69]
VU0361747 DM3ZUH2 Discovery agent N.A. Investigative [68]
VU0364289 DM8TR1Y Discovery agent N.A. Investigative [71]
VU0366058 DMA6CLO Discovery agent N.A. Investigative [72]
VU0404251 DMZRE6X Discovery agent N.A. Investigative [73]
VU0424465 DMZDIVL Discovery agent N.A. Investigative [74]
VU0463841 DMDW9MS Discovery agent N.A. Investigative [75]
[14C]MTEP DMG17IU Discovery agent N.A. Investigative [76]
[3H]methoxy-PEPy DMZ2R1O Discovery agent N.A. Investigative [77]
[3H]methoxymethyl-MTEP DMONI13 Discovery agent N.A. Investigative [76], [77]
[3H]quisqualate DMDQBTX Discovery agent N.A. Investigative [78]
[3H]resolvin E1 DMAMK3P N. A. N. A. Investigative [15]
------------------------------------------------------------------------------------
⏷ Show the Full List of 264 Investigative Drug(s)

Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTT
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Alzheimer's disease 8A00.0 Entorhinal cortex 9.81E-07 -0.26 -0.54
Major depressive disorder 6A20 Pre-frontal cortex 8.60E-01 1.36E-02 0.06
------------------------------------------------------------------------------------

References

1 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.
2 Pipeline of Addex Pharma. Addex Pharma. 2009.
3 A proof-of-concept study evaluating the effect of ADX10059, a metabotropic glutamate receptor-5 negative allosteric modulator, on acid exposure and... Gut. 2009 Sep;58(9):1192-9.
4 Novel treatments of GERD: focus on the lower esophageal sphincter. Eur Rev Med Pharmacol Sci. 2008 Aug;12 Suppl 1:103-10.
5 The challenges of clinical trials in fragile X syndrome. Psychopharmacology (Berl) 2014; 231(6): 1237-1250.
6 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.
7 Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic gluta... Bioorg Med Chem. 2010 May 1;18(9):3026-35.
8 Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17.
9 URL: 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).
10 Clinical pipeline report, company report or official report of Roche.
11 Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agon... J Pharmacol Exp Ther. 2005 Nov;315(2):711-21.
12 mGlu5 negative allosteric modulators: a patent review (2013 - 2016).Expert Opin Ther Pat. 2017 Jun;27(6):691-706.
13 Clinical pipeline report, company report or official report of AstraZeneca (2009).
14 Characterization of [(3)H]Quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections. J Neurochem. 2000 Dec;75(6):2590-601.
15 Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8.
16 Dipyridyl amines: potent metabotropic glutamate subtype 5 receptor antagonists. Bioorg Med Chem Lett. 2005 Oct 1;15(19):4350-3.
17 Synergism of virtual screening and medicinal chemistry: identification and optimization of allosteric antagonists of metabotropic glutamate recepto... Bioorg Med Chem. 2009 Aug 1;17(15):5708-15.
18 Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic g... J Med Chem. 2006 Feb 9;49(3):1080-100.
19 Biochemical and electrophysiological studies on (S)-(+)-2-(3'-carboxybicyclo(1.1.1)pentyl)-glycine (CBPG), a novel mGlu5 receptor agonist endowed with mGlu1 receptor antagonist activity. Neuropharmacology. 1999 Jul;38(7):917-26.
20 5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist... Bioorg Med Chem Lett. 2004 Aug 2;14(15):3993-6.
21 Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists. Bioorg Med Chem Lett. 2007 Dec 1;17(23):6525-8.
22 Synthesis and SAR of 2-aryl pyrido[2,3-d]pyrimidines as potent mGlu5 receptor antagonists. Bioorg Med Chem Lett. 2007 Oct 1;17(19):5396-9.
23 A new series of pyridinyl-alkynes as antagonists of the metabotropic glutamate receptor 5 (mGluR5). Bioorg Med Chem Lett. 2006 Sep 15;16(18):4792-5.
24 Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1892-7.
25 Structure-activity relationships for the linker in a series of pyridinyl-alkynes that are antagonists of the metabotropic glutamate receptor 5 (mGl... Bioorg Med Chem Lett. 2006 Sep 15;16(18):4788-91.
26 Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a... J Med Chem. 2009 Jul 23;52(14):4103-6.
27 Structure-activity relationship of thiopyrimidines as mGluR5 antagonists. Bioorg Med Chem Lett. 2006 May 1;16(9):2467-9.
28 Positive and negative modulation of group I metabotropic glutamate receptors. J Med Chem. 2008 Feb 14;51(3):634-47.
29 Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6502-6.
30 Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists. Bioorg Med Chem Lett. 2005 Oct 15;15(20):4589-93.
31 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist. Neuropharmacology. 1999 Oct;38(10):1493-503.
32 Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6.
33 Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-met... J Med Chem. 2009 Jun 11;52(11):3563-75.
34 A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5. Mol Pharmacol. 2003 Sep;64(3):731-40.
35 Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity. J Med Chem. 2004 Sep 9;47(19):4645-8. Letter
36 Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists. Bioorg Med Chem Lett. 2007 Jun 1;17(11):2987-91.
37 Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine. J Med Chem. 2007 Jul 12;50(14):3388-91.
38 Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3371-5.
39 3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure ... Bioorg Med Chem Lett. 2010 Aug 1;20(15):4390-4.
40 Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo. JMed Chem. 2004 Nov 18;47(24):5825-8.
41 Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat... J Med Chem. 2006 Jun 1;49(11):3332-44.
42 Discovery of novel modulators of metabotropic glutamate receptor subtype-5. Bioorg Med Chem. 2004 Jan 2;12(1):17-21.
43 Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5... Bioorg Med Chem Lett. 2008 Jul 15;18(14):4098-101.
44 A close structural analog of 2-methyl-6-(phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtyp... Mol Pharmacol. 2005 Dec;68(6):1793-802.
45 Mechanism based neurotoxicity of mGlu5 positive allosteric modulators--development challenges for a promising novel antipsychotic target. Neuropharmacology. 2014 Jul;82:161-73.
46 Piperidyl amides as novel, potent and orally active mGlu5 receptor antagonists with anxiolytic-like activity. Bioorg Med Chem Lett. 2010 Jan 1;20(1):184-8.
47 Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists. Bioorg Med Chem Lett. 2005 Feb 15;15(4):1197-200.
48 An allosteric modulator to control endogenous G protein-coupled receptors with light. Nat Chem Biol. 2014 Oct;10(10):813-5.
49 A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain. J Pharmacol Exp Ther. 2004 May;309(2):568-77.
50 Preclinical profile of a novel metabotropic glutamate receptor 5 positive allosteric modulator. Eur J Pharmacol. 2011 Jun 1;659(2-3):146-54.
51 CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. J Pharmacol Exp Ther. 2011 Nov;339(2):474-86.
52 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.
53 Inhibition of group I metabotropic glutamate receptor responses in vivo in rats by a new generation of carboxyphenylglycine-like amino acid antagon... Neurosci Lett. 2002 Sep 20;330(2):127-30.
54 Design and synthesis of novel heterobiaryl amides as metabotropic glutamate receptor subtype 5 antagonists. Bioorg Med Chem Lett. 2007 Apr 1;17(7):2074-9.
55 Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator. Bioorg Med Chem Lett. 2009 Jun 15;19(12):3275-8.
56 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.
57 2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist. Bioorg Med Chem Lett. 2004 Nov 15;14(22):5473-6.
58 Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity. Bioorg Med Chem Lett. 2004Nov 15;14(22):5481-4.
59 Rational design, synthesis, and structure-activity relationship of benzoxazolones: new potent mglu5 receptor antagonists based on the fenobam struc... Bioorg Med Chem Lett. 2007 Mar 1;17(5):1302-6.
60 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.
61 Discovery of novel positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5). Bioorg Med Chem Lett. 2011 Mar 1;21(5):1402-6.
62 6-Aryl-3-pyrrolidinylpyridines as mGlu5 receptor negative allosteric modulators. Bioorg Med Chem Lett. 2011 Aug 15;21(16):4891-9.
63 (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.
64 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.
65 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.
66 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.
67 Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging mo... J Med Chem. 2007 Jul 12;50(14):3256-66.
68 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.
69 Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity. Mol Pharmacol. 2010 Dec;78(6):1105-23.
70 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.
71 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.
72 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.
73 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.
74 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.
75 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.
76 [3H]Methoxymethyl-3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine binding to metabotropic glutamate receptor subtype 5 in rodent brain: in vitro and in vivo characterization. J Pharmacol Exp Ther. 2002 Dec;303(3):1044-51.
77 [3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor. Bioorg Med Chem Lett. 2003 Feb 10;13(3):351-4.
78 Excitatory amino acid receptor ligands: resolution, absolute stereochemistry, and enantiopharmacology of 2-amino-3-(4-butyl-3-hydroxyisoxazol-5-yl)... J Med Chem. 1998 Mar 12;41(6):930-9.