General Information of DTT (ID: TTHS256)

DTT Name Metabotropic glutamate receptor 5 (mGluR5) DTT Info
Gene Name GRM5

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Investigative Drug(s)
10 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
ADX-48621 DM6GTMD Parkinson disease 8A00.0 Phase 2/3 [1]
AFQ056 DMMHSLC Fragile X syndrome LD55 Phase 2/3 [2]
ADX10059 DMGVKHQ Anxiety disorder 6B00-6B0Z Phase 2 [3]
RG-7090 DMX8JYN Fragile X syndrome LD55 Phase 2 [4]
STX-107 DMLNKX7 Autism spectrum disorder 6A02 Phase 2 [5]
McN3377 DMTCADJ Fragile X syndrome LD55 Phase 1/2 [6]
BMS-984923 DMFNDUL Alzheimer disease 8A20 Phase 1 [7]
MK-3328 DMW2O5D Alzheimer disease 8A20 Phase 1 [8]
RG7342 DMIW5NG Schizophrenia 6A20 Phase 1 [9]
[3H]fenobam DMBOXA1 Allodynia MB40.1 Phase 1 [10]
------------------------------------------------------------------------------------
⏷ Show the Full List of 10 Clinical Trial Drug(s)
68 Patented Agent(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
2-(substituted ethynyl)quinoline derivative 1 DMOY5EK N. A. N. A. Patented [11]
2-(substituted ethynyl)quinoline derivative 2 DMPCYSW N. A. N. A. Patented [11]
2-(substituted ethynyl)quinoline derivative 3 DMMF8A1 N. A. N. A. Patented [11]
2-(substituted ethynyl)quinoline derivative 4 DMTXZUF N. A. N. A. Patented [11]
6-aryl-imidazopyridine and 6-aryl-triazolopyridine carboxamide analog 1 DMTXGYS N. A. N. A. Patented [11]
6-aryl-imidazopyridine and 6-aryl-triazolopyridine carboxamide analog 2 DMFKTBM N. A. N. A. Patented [11]
6-aryl-imidazopyridine and 6-aryl-triazolopyridine carboxamide analog 3 DMXMTLP N. A. N. A. Patented [11]
Bicarboxylic and tricarboxylic ethynyl derivative 1 DMDK7LQ N. A. N. A. Patented [11]
Bicarboxylic and tricarboxylic ethynyl derivative 2 DMG9O7D N. A. N. A. Patented [11]
Bicarboxylic and tricarboxylic ethynyl derivative 3 DM1KVTZ N. A. N. A. Patented [11]
Bicyclic heteroaryl carboxamide analog 1 DMB5XDM N. A. N. A. Patented [11]
Bicyclic heteroaryl carboxamide analog 2 DMKT7MD N. A. N. A. Patented [11]
Bicyclic heteroaryl carboxamide analog 3 DM3QMA0 N. A. N. A. Patented [11]
Central azetidine derivative 1 DM7INA1 N. A. N. A. Patented [11]
Central azetidine derivative 2 DM2BLJ6 N. A. N. A. Patented [11]
Diazepinone derivative 1 DM9YD0Q Parkinson disease 8A00.0 Patented [11]
Diazepinone derivative 2 DMLQ7PG Parkinson disease 8A00.0 Patented [11]
Diazepinone derivative 3 DMPTZ69 Parkinson disease 8A00.0 Patented [11]
Diazepinone derivative 4 DM389YD Parkinson disease 8A00.0 Patented [11]
Diazepinone derivative 5 DM2U1QH Parkinson disease 8A00.0 Patented [11]
Ethynyl compound 1 DMWXKRZ N. A. N. A. Patented [11]
Ethynyl compound 2 DMJDG37 N. A. N. A. Patented [11]
Ethynyl compound 3 DMD9PZQ N. A. N. A. Patented [11]
Ethynyl compound 4 DMLDMO8 N. A. N. A. Patented [11]
Ethynyl compound 5 DM53ZPE N. A. N. A. Patented [11]
Ethynyl compound 6 DMDOEFC N. A. N. A. Patented [11]
Ethynyl compound 7 DMPUG2M N. A. N. A. Patented [11]
Heterocyclic derivative 1 DMJ5X46 N. A. N. A. Patented [11]
Heterocyclic derivative 2 DM2QCBF N. A. N. A. Patented [11]
Heterocyclic derivative 3 DMCD0MS N. A. N. A. Patented [11]
Imidazopyridine and triazolopyridine compound 1 DMTUS0Y N. A. N. A. Patented [11]
Imidazopyridine and triazolopyridine compound 2 DMYCLAM N. A. N. A. Patented [11]
Imidazopyridine and triazolopyridine compound 3 DMWU8VM N. A. N. A. Patented [11]
Imidazopyridine and triazolopyridine compound 4 DMI1OWK N. A. N. A. Patented [11]
Imidazo[1,2-a]pyridine derivative 1 DM5NEQ2 N. A. N. A. Patented [11]
N-alkylamide derivative 1 DMXPBL5 N. A. N. A. Patented [11]
N-alkylamide derivative 2 DM568TX N. A. N. A. Patented [11]
PMID28067079-Compound-95 DMG2PCZ N. A. N. A. Patented [11]
PMID28067079-Compound-97 DMCUX42 N. A. N. A. Patented [11]
PMID28067079-Compound-98 DMLKP1O N. A. N. A. Patented [11]
Pyrazolopyrimidine derivative 1 DMHO3NB N. A. N. A. Patented [11]
Pyrazolopyrimidine derivative 2 DMZEP5X N. A. N. A. Patented [11]
Pyrazolopyrimidine derivative 3 DMI0J7D N. A. N. A. Patented [11]
Pyrazolopyrimidine derivative 4 DM7XSHK N. A. N. A. Patented [11]
Pyrazolopyrimidine derivative 5 DMVUSF3 N. A. N. A. Patented [11]
Pyrazolopyrimidine derivative 6 DMG8V31 N. A. N. A. Patented [11]
Pyridine derivative 12 DM8KBHX N. A. N. A. Patented [11]
Pyridine derivative 13 DMX8RGH N. A. N. A. Patented [11]
Pyridine derivative 14 DM7JCM6 N. A. N. A. Patented [11]
Pyridine derivative 15 DMGBR43 N. A. N. A. Patented [11]
Pyridine derivative 16 DMICZLS N. A. N. A. Patented [11]
Pyridine derivative 17 DMLC5WA N. A. N. A. Patented [11]
Pyrrolidine derivative 1 DMXALJE N. A. N. A. Patented [11]
Pyrrolidine derivative 2 DM5WA29 N. A. N. A. Patented [11]
Pyrrolidine derivative 3 DMHM8WJ N. A. N. A. Patented [11]
Pyrrolidine derivative 4 DMZ2HBL N. A. N. A. Patented [11]
Pyrrolidine derivative 5 DM5NKXO N. A. N. A. Patented [11]
Tetra-hydro-oxazolopyridine derivative 1 DM72MDA N. A. N. A. Patented [11]
Tetra-hydro-oxazolopyridine derivative 2 DMP65Z4 N. A. N. A. Patented [11]
Tetra-hydro-oxazolopyridine derivative 3 DMQYKT2 N. A. N. A. Patented [11]
Tetra-hydro-oxazolopyridine derivative 4 DM21J83 N. A. N. A. Patented [11]
Tetra-hydro-oxazolopyridine derivative 5 DMQGA1I N. A. N. A. Patented [11]
Tetra-hydro-oxazolopyridine derivative 6 DMLW7YO N. A. N. A. Patented [11]
Tetra-hydro-pyrazolopyrazine derivative 1 DM3HVCZ N. A. N. A. Patented [11]
Tetra-hydro-pyrazolopyrazine derivative 2 DMQ027F N. A. N. A. Patented [11]
Tetra-hydro-pyrazolopyrazine derivative 3 DMKGJ1S N. A. N. A. Patented [11]
Tetra-hydro-pyrazolopyrazine derivative 4 DMRMTF6 N. A. N. A. Patented [11]
Tetra-hydro-pyrazolopyrazine derivative 5 DMAM7Y2 N. A. N. A. Patented [11]
------------------------------------------------------------------------------------
⏷ Show the Full List of 68 Patented Agent(s)
4 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
AZD2066 DMHP6OY Chronic neuropathic pain MG30.5 Discontinued in Phase 2 [12]
AZD2516 DM9OPDE Chronic neuropathic pain MG30.5 Discontinued in Phase 2 [12]
LY467711 DM0TV9L Migraine 8A80 Terminated [6]
LY525327 DMPNMAR Migraine 8A80 Terminated [6]
------------------------------------------------------------------------------------
264 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
(+)-MCPG DMG5QJB Discovery agent N.A. Investigative [13]
(1S,3R)-ACPD DM5DOAF Discovery agent N.A. Investigative [13]
(3-(2-methylquinolin-7-yl)phenyl)methanol DMR6JTQ Discovery agent N.A. Investigative [14]
(3-Ethoxy-pyridin-2-yl)-pyridin-2-yl-amine DMG1KIJ Discovery agent N.A. Investigative [15]
(E)-1-Adamantan-1-yl-3-quinolin-3-yl-propenone DMQ9TWD Discovery agent N.A. Investigative [16]
(E)-3-[2-(2-methyl-4-thiazolyl)vinyl]pyridine DMITXKJ Discovery agent N.A. Investigative [17]
(S)-(+)-CBPG DMPDOY8 Discovery agent N.A. Investigative [18]
(S)-3HPG DMQ0FVJ Discovery agent N.A. Investigative [13]
(S)-4C3HPG DMQK4I2 Discovery agent N.A. Investigative [13]
(S)-4CPG DMZ9UIL Discovery agent N.A. Investigative [13]
1-(3-(2-methylquinolin-7-yl)phenyl)ethanone DMD25N9 Discovery agent N.A. Investigative [14]
2-(2-Methyl-thiazol-4-ylethynyl)-pyridine DMIHTL0 Discovery agent N.A. Investigative [19]
2-(2-methylquinolin-7-yl)benzonitrile DMENUIH Discovery agent N.A. Investigative [14]
2-(3,4-dimethylphenyl)-1,8-naphthyridine DMDGRWM Discovery agent N.A. Investigative [20]
2-(3,5-dichlorophenyl)pyrido[2,3-d]pyrimidine DM8KM1Q Discovery agent N.A. Investigative [21]
2-(3,5-difluorophenyl)-7-methyl-1,8-naphthyridine DMGJPYO Discovery agent N.A. Investigative [20]
2-(3,5-dimethoxyphenyl)-1,8-naphthyridine DMKND0T Discovery agent N.A. Investigative [20]
2-(3-(2-methylquinolin-7-yl)phenyl)acetonitrile DMLJH92 Discovery agent N.A. Investigative [14]
2-(3-(3-methoxyphenoxy)prop-1-ynyl)pyridine DM1VSOK Discovery agent N.A. Investigative [22]
2-(3-(benzyloxy)phenyl)isoindoline-1,3-dione DM0R5U6 Discovery agent N.A. Investigative [23]
2-(3-bromophenyl)-7-methyl-1,8-naphthyridine DMYSM9L Discovery agent N.A. Investigative [20]
2-(3-bromophenyl)-7-methylpyrido[2,3-d]pyrimidine DMANS5X Discovery agent N.A. Investigative [21]
2-(3-bromophenyl)pyrido[2,3-d]pyrimidine DMVA4XC Discovery agent N.A. Investigative [21]
2-(3-chlorobenzyloxy)-6-chloroisonicotinonitrile DM1VDC3 Discovery agent N.A. Investigative [23]
2-(3-chlorophenyl)-7-methyl-1,8-naphthyridine DM7BC50 Discovery agent N.A. Investigative [20]
2-(4-(3-chlorophenyl)but-1-ynyl)-6-methylpyridine DM27CQJ Discovery agent N.A. Investigative [24]
2-(m-tolylethynyl)pyrimidine DM15BA7 Discovery agent N.A. Investigative [25]
2-(phenylethynyl)pyrimidine DMRIFCW Discovery agent N.A. Investigative [25]
2-(pyridin-2-yl)-4-(m-tolylthio)pyrimidine DM3EBYD Discovery agent N.A. Investigative [26]
2-Benzoxy-5-(2-methylquinolin-7-yl)benzonitrile DMQX9PD Discovery agent N.A. Investigative [27]
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 [17]
2-Chloro-5-(2-methylquinolin-7-yl)nicotinonitrile DM5KR4B Discovery agent N.A. Investigative [27]
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 [25]
2-ethynyl-4-(3-fluorophenylethynyl)thiazole DME6VKS Discovery agent N.A. Investigative [17]
2-m-tolyl-1,8-naphthyridine DMBWDXH Discovery agent N.A. Investigative [20]
2-methyl-4-(2-thienylethynyl)thiazole DMAFPE7 Discovery agent N.A. Investigative [17]
2-methyl-4-(3-thienylethynyl)thiazole DMK4A0J Discovery agent N.A. Investigative [17]
2-methyl-4-(m-tolylethynyl)thiazole DM4P3CW Discovery agent N.A. Investigative [17]
2-Methyl-4-o-tolylethynyl-thiazole DMKFBVS Discovery agent N.A. Investigative [19]
2-Methyl-4-p-tolylethynyl-thiazole DMWRCFY Discovery agent N.A. Investigative [19]
2-Methyl-4-phenylethynyl-thiazole DMRC60A Discovery agent N.A. Investigative [19]
2-methyl-6-(3-(p-tolyloxy)prop-1-ynyl)pyridine DMGPDYE Discovery agent N.A. Investigative [22]
2-methyl-6-(3-(phenylthio)prop-1-ynyl)pyridine DM536IA Discovery agent N.A. Investigative [24]
2-methyl-6-(4-phenylbut-1-ynyl)pyridine DM1YK7M Discovery agent N.A. Investigative [24]
2-methyl-6-(4-phenylpent-1-ynyl)pyridine DM0UNM1 Discovery agent N.A. Investigative [24]
2-methyl-6-(5-phenylpent-1-ynyl)pyridine DMDVO7Z Discovery agent N.A. Investigative [24]
2-methyl-6-(phenylethynyl)pyridine DMVQK4Y Discovery agent N.A. Investigative [31]
2-methyl-7-(pyridin-3-yl)quinoline DM9FZ0B Discovery agent N.A. Investigative [14]
2-methyl-7-m-tolyl-1,6-naphthyridine DMMFKOH Discovery agent N.A. Investigative [20]
2-methyl-7-m-tolyl-1,8-naphthyridine DMZFK4R Discovery agent N.A. Investigative [20]
2-methyl-7-m-tolylquinoline DMC02TI Discovery agent N.A. Investigative [14]
2-methyl-7-phenyl-1,8-naphthyridine DM8RV5X Discovery agent N.A. Investigative [20]
2-methyl-7-phenylquinoline DMT7MVD Discovery agent N.A. Investigative [14]
2-phenyl-1,8-naphthyridine DM3WOHI Discovery agent N.A. Investigative [20]
2-Phenyl-5-(2-methylthiazol-4ylethynyl)pyridine DM7A3GO Discovery agent N.A. Investigative [32]
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 [17]
3,3'-difluorobenzaldazine DMGMJWL Discovery agent N.A. Investigative [33]
3,5-DHPG DMFEQ6S Discovery agent N.A. Investigative [13]
3-(1,5-naphthyridin-3-yl)benzonitrile DM24BG6 Discovery agent N.A. Investigative [20]
3-(1,8-naphthyridin-2-yl)benzonitrile DMSP4N5 Discovery agent N.A. Investigative [20]
3-(1-Pyridin-2-yl-1H-pyrazol-3-yl)-benzonitrile DMTD7VE Discovery agent N.A. Investigative [34]
3-(1-Pyridin-2-yl-1H-pyrazol-4-yl)-benzonitrile DMWI37C Discovery agent N.A. Investigative [34]
3-(1-Pyridin-2-yl-1H-pyrrol-3-yl)-benzonitrile DMJ9LRE Discovery agent N.A. Investigative [34]
3-(2-methylbenzo[d]thiazol-5-yl)benzonitrile DMY782R Discovery agent N.A. Investigative [35]
3-(2-methylquinolin-7-yl)benzonitrile DMUPB9H Discovery agent N.A. Investigative [14]
3-(2-methylquinolin-7-yl)phenol DM41HMZ Discovery agent N.A. Investigative [14]
3-(2-Pyridin-2-yl-2H-tetrazol-5-yl)-benzonitrile DMPWEL8 Discovery agent N.A. Investigative [34]
3-(3,4-dimethylphenyl)-1,5-naphthyridine DMULX9O Discovery agent N.A. Investigative [20]
3-(3-(3-chlorobenzyloxy)-5-methylphenyl)pyridine DMKAEUD Discovery agent N.A. Investigative [23]
3-(3-bromophenylethynyl)-5-methyl[1,2,4]triazine DMFPTXO Discovery agent N.A. Investigative [36]
3-(3-methylphenylethynyl)-5-methyl[1,2,4]triazine DMXAD0R Discovery agent N.A. Investigative [36]
3-(3-Pyridin-2-yl-pyrazol-1-yl)-benzonitrile DMU52WA Discovery agent N.A. Investigative [34]
3-(3-Pyridin-2-yl-pyrrol-1-yl)-benzonitrile DMZLT24 Discovery agent N.A. Investigative [34]
3-(4-Pyridin-2-yl-imidazol-1-yl)-benzonitrile DMDYVA7 Discovery agent N.A. Investigative [34]
3-(4-Pyridin-2-yl-pyrazol-1-yl)-benzonitrile DMTD16H Discovery agent N.A. Investigative [34]
3-(5-Pyridin-2-yl-tetrazol-2-yl)-benzonitrile DMM1CKZ Discovery agent N.A. Investigative [34]
3-(6-fluoroquinazolin-4-ylamino)benzonitrile DMHJ0SV Discovery agent N.A. Investigative [37]
3-(7-methyl-1,8-naphthyridin-2-yl)benzonitrile DMZ53N4 Discovery agent N.A. Investigative [20]
3-biphenyl-4-ylethynyl-5-methyl-[1,2,4]triazine DMMC2Q9 Discovery agent N.A. Investigative [36]
3-bromo-5-(2-methylquinolin-7-yl)benzonitrile DMPQOS2 Discovery agent N.A. Investigative [14]
3-bromo-5-[(2-methyl-4-thiazolyl)ethynyl]pyridine DMOXY78 Discovery agent N.A. Investigative [17]
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 [14]
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 [32]
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]
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 [32]
3-ethoxy-5-(2-methylquinolin-7-yl)benzonitrile DMSK6EM Discovery agent N.A. Investigative [14]
3-fluoro-5-(1,6-naphthyridin-7-yl)benzonitrile DMH9VLF Discovery agent N.A. Investigative [20]
3-fluoro-5-(2-methylquinolin-7-yl)benzonitrile DM2V45Z Discovery agent N.A. Investigative [14]
3-hydroxy-5-(2-methylquinolin-7-yl)benzonitrile DMZS4P7 Discovery agent N.A. Investigative [14]
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 [14]
3-m-tolyl-1,5-naphthyridine DMMFA4N Discovery agent N.A. Investigative [20]
3-methoxy-5-(1,5-naphthyridin-3-yl)benzonitrile DMHYRES Discovery agent N.A. Investigative [20]
3-methoxy-5-(1,6-naphthyridin-7-yl)benzonitrile DMKHJ8G Discovery agent N.A. Investigative [20]
3-methoxy-5-(2-methylquinolin-7-yl)benzonitrile DMRMZLV Discovery agent N.A. Investigative [14]
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 [14]
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 [32]
3-[(2,5-dimethyl-4-thiazolyl)ethynyl]pyridine DMBAHRJ Discovery agent N.A. Investigative [17]
3-[(2-methyl-4-thiazolyl)ethynyl]-5-vinylpyridine DMZ78WB Discovery agent N.A. Investigative [17]
3-[(2-methyl-4-thiazolyl)ethynyl]benzamide DMMLDOZ Discovery agent N.A. Investigative [17]
3-[(2-methyl-4-thiazolyl)ethynyl]benzonitrile DMQUDR1 Discovery agent N.A. Investigative [42]
3-[(2-methyl-4-thiazolyl)ethynyl]phenol DMF0QM2 Discovery agent N.A. Investigative [17]
3-[(5-ethyl-2-methyl-4-thiazolyl)ethynyl]pyridine DM9OI2R Discovery agent N.A. Investigative [17]
3-[(6-Methylpyridin-2-yl)ethynyl]benzonitrile DMH5329 Discovery agent N.A. Investigative [32]
4-(2-(3-fluorophenyl)ethynyl)-2-methylthiazole DMRDWUT Discovery agent N.A. Investigative [17]
4-(2-(4-fluorophenyl)ethynyl)-2-methylthiazole DMOX40J Discovery agent N.A. Investigative [17]
4-(2-fluorophenylethynyl)-2-methylthiazole DMCWZF6 Discovery agent N.A. Investigative [17]
4-(2-methoxyphenylethynyl)-2-methylthiazole DMFVYHI Discovery agent N.A. Investigative [17]
4-(2-Methyl-thiazol-4-ylethynyl)-pyridine DMEAV9Q Discovery agent N.A. Investigative [19]
4-(3,5-difluorophenylethynyl)-2-methylthiazole DM48Z5Y Discovery agent N.A. Investigative [17]
4-(3-bromophenoxy)-6-chloroquinazoline DM3LGOT Discovery agent N.A. Investigative [37]
4-(3-bromophenylthio)-2-(pyridin-2-yl)pyrimidine DMQBHF2 Discovery agent N.A. Investigative [26]
4-(3-chlorophenylethynyl)-2-methylthiazole DMDTFKL Discovery agent N.A. Investigative [17]
4-(3-chlorophenylthio)-2-(pyridin-2-yl)pyrimidine DMJH2OE Discovery agent N.A. Investigative [26]
4-(3-fluorophenylethynyl)-2-thiazolylamine DM6RV9L Discovery agent N.A. Investigative [17]
4-(3-methoxyphenylethynyl)-2-methylthiazole DMGCPKU Discovery agent N.A. Investigative [17]
4-(3-pyridylethynyl)-2-thiazolylamine DMRXKMP Discovery agent N.A. Investigative [17]
4-(4-chlorophenylthio)-2-(pyridin-2-yl)pyrimidine DM9YRHW Discovery agent N.A. Investigative [26]
4-Biphenyl-2-ylethynyl-2-methyl-thiazole DM3B2TG Discovery agent N.A. Investigative [19]
4-Biphenyl-4-ylethynyl-2-methyl-thiazole DMCQYKO Discovery agent N.A. Investigative [19]
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 [27]
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 [27]
5-(2-Methylquinolin-7-yl)-2-phenylnicotinonitrile DMO74HX Discovery agent N.A. Investigative [27]
5-(2-methylquinolin-7-yl)isophthalonitrile DMMX69H Discovery agent N.A. Investigative [14]
5-(2-methylquinolin-7-yl)nicotinonitrile DM8LN2X Discovery agent N.A. Investigative [14]
5-(3-chlorophenylethynyl)-5-methyl[1,2,4]triazine DMABSOC Discovery agent N.A. Investigative [36]
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 [27]
5-methyl-3-phenylethynyl[1,2,4]triazine DMF0IJ2 Discovery agent N.A. Investigative [36]
5-MPEP DMSRGTI Discovery agent N.A. Investigative [44]
5-[(2-methyl-4-thiazolyl)ethynyl]pyrimidine DMM9GCA Discovery agent N.A. Investigative [17]
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 [37]
6-bromo-N-(3-chlorophenyl)quinazolin-4-amine DM0A3DB Discovery agent N.A. Investigative [37]
6-bromo-N-(3-fluorophenyl)quinazolin-4-amine DM2IP5F Discovery agent N.A. Investigative [37]
6-bromo-N-m-tolylquinazolin-4-amine DM2MJ9F Discovery agent N.A. Investigative [37]
6-chloro-N-(3-chlorophenyl)quinazolin-4-amine DMPIFLA Discovery agent N.A. Investigative [37]
6-fluoro-N-m-tolylquinazolin-4-amine DMVADTP Discovery agent N.A. Investigative [37]
6-phenylethynyl-nicotinic acid methyl ester DMIKRP6 Discovery agent N.A. Investigative [28]
7-(2-methoxyphenyl)-2-methylquinoline DMO8DYW Discovery agent N.A. Investigative [14]
7-(3,5-dimethoxyphenyl)-1,6-naphthyridine DM2RFOB Discovery agent N.A. Investigative [20]
7-(3-(methoxymethyl)phenyl)-2-methylquinoline DMYNLOI Discovery agent N.A. Investigative [14]
7-(3-chlorophenyl)-2-methylquinoline DM0Q56N Discovery agent N.A. Investigative [14]
7-(3-fluoro-5-methylphenyl)-1,6-naphthyridine DME2VD7 Discovery agent N.A. Investigative [20]
7-(3-fluorophenyl)-2-methylquinoline DMDXOBH Discovery agent N.A. Investigative [14]
7-(3-methoxyphenyl)-2-methyl-1,6-naphthyridine DMEC9YK Discovery agent N.A. Investigative [20]
7-(3-methoxyphenyl)-2-methylquinoline DMW6LCH Discovery agent N.A. Investigative [14]
7-(4,6-dimethoxypyrimidin-2-yl)-2-methylquinoline DMHXMY5 Discovery agent N.A. Investigative [35]
7-(4,6-dimethylpyrimidin-2-yl)-2-methylquinoline DMQFBTW Discovery agent N.A. Investigative [35]
7-(4-methoxyphenyl)-2-methylquinoline DMBT1KS Discovery agent N.A. Investigative [14]
7-(4-methoxypyrimidin-2-yl)-2-methylquinoline DMSRKF0 Discovery agent N.A. Investigative [35]
7-bromo-N-(3-bromophenyl)isoquinolin-1-amine DML8PH7 Discovery agent N.A. Investigative [37]
7-m-tolyl-1,6-naphthyridine DMBDFP2 Discovery agent N.A. Investigative [20]
7-methyl-2-m-tolylpyrido[2,3-d]pyrimidine DMCV891 Discovery agent N.A. Investigative [21]
7-methyl-2-phenylpyrido[2,3-d]pyrimidine DMJ4G27 Discovery agent N.A. Investigative [21]
ACDPP DMPMH7Z Discovery agent N.A. Investigative [47]
ADX-63365 DMA74PO Central nervous system disease 8A04-8D87 Investigative [8]
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 [13]
CPPHA DMDG2Y9 Discovery agent N.A. Investigative [49]
CPPZ DM9OWG5 Discovery agent N.A. Investigative [50]
CTEP DMYRVZ8 Fragile X syndrome LD55 Investigative [8]
GRN-529 DMJ47DM Major depressive disorder 6A70.3 Investigative [8]
GSK-2210875 DM0DKQN Anxiety disorder 6B00-6B0Z Investigative [8]
ibotenate DM8RZE0 Discovery agent N.A. Investigative [13]
L-CCG-I DMPZ8XH Discovery agent N.A. Investigative [13]
LSN2463359 DMWVTS3 Discovery agent N.A. Investigative [51]
LSN2814617 DMV9NP6 Discovery agent N.A. Investigative [51]
LY-3390334 DMUXFZQ Discovery agent N.A. Investigative [52]
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 [37]
N-(3-bromophenyl)-6-fluoroquinazolin-4-amine DMRIK7P Discovery agent N.A. Investigative [37]
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 [37]
N-(3-chlorophenyl)-6-methoxyquinazolin-4-amine DMQEPV0 Discovery agent N.A. Investigative [37]
N-(3-chlorophenyl)-6-nitroquinazolin-4-amine DMIKP5Y Discovery agent N.A. Investigative [37]
N-(6-methylpyridin-2-yl)-5-phenylpicolinamide DMQRE5D Discovery agent N.A. Investigative [53]
N-(6-methylpyridin-2-yl)-6-phenylnicotinamide DMQZMRG Discovery agent N.A. Investigative [32]
N-(6-methylpyridin-2-yl)biphenyl-3-carboxamide DMBNJ2L Discovery agent N.A. Investigative [32]
N-cyclopentyl-6-(2-phenylethynyl)nicotinamide DMDPKCM Discovery agent N.A. Investigative [54]
N-[4-(3-pyridylethynyl)-2-thiazolyl]acetamide DMC62K1 Discovery agent N.A. Investigative [17]
NCFP DM0JCN2 Discovery agent N.A. Investigative [55]
PMID14697765C11a DMFWCAJ Discovery agent N.A. Investigative [42]
PMID14697765C16a DMFT1DO Discovery agent N.A. Investigative [42]
PMID15482906C10 DM7T8BE Discovery agent N.A. Investigative [56]
PMID15482908C8 DMCPIQ4 Discovery agent N.A. Investigative [57]
PMID15686941C13 DMPB7Z6 Discovery agent N.A. Investigative [47]
PMID16439120C20 DMI8HAV Discovery agent N.A. Investigative [23]
PMID16439120C26 DMVM2XD Discovery agent N.A. Investigative [23]
PMID17189691C42 DMG9ZYP Discovery agent N.A. Investigative [58]
PMID17723296C18 DMBP3O7 Discovery agent N.A. Investigative [21]
PMID17936624C36 DMEHC2I Discovery agent N.A. Investigative [20]
PMID19931453C16m DM3DCR9 Discovery agent N.A. Investigative [46]
PMID20598884C8 DMS21ZP Discovery agent N.A. Investigative [39]
PMID20809633C29b DM0W6C9 Discovery agent N.A. Investigative [59]
PMID21295468C47 DM0DNSV Discovery agent N.A. Investigative [60]
PMID21757343C30 DM3ELPS Discovery agent N.A. Investigative [61]
PMID21927650C18 DMLGKD3 Discovery agent N.A. Investigative [62]
PMID23357634C24d DM4NAC9 Discovery agent N.A. Investigative [63]
PMID23374867C24 DMRC14X Discovery agent N.A. Investigative [64]
PMID23434029C41 DMG0XC7 Discovery agent N.A. Investigative [65]
PMID23434029C53 DMG0B4N Discovery agent N.A. Investigative [65]
PTeB DM1NM5F Discovery agent N.A. Investigative [34]
RTI-4229-982 DMG6TOA Neurological disorder 6B60 Investigative [8]
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 [66]
VU-1545 DMCRF48 Discovery agent N.A. Investigative [41]
VU0092273 DMT76JS Discovery agent N.A. Investigative [67]
VU0240382 DMH720P Discovery agent N.A. Investigative [67]
VU0285683 DM7VCDF Discovery agent N.A. Investigative [68]
VU0357121 DMETUHS Discovery agent N.A. Investigative [69]
VU0360172 DM3NXMB Discovery agent N.A. Investigative [68]
VU0361747 DM3ZUH2 Discovery agent N.A. Investigative [67]
VU0364289 DM8TR1Y Discovery agent N.A. Investigative [70]
VU0366058 DMA6CLO Discovery agent N.A. Investigative [71]
VU0404251 DMZRE6X Discovery agent N.A. Investigative [72]
VU0424465 DMZDIVL Discovery agent N.A. Investigative [73]
VU0463841 DMDW9MS Discovery agent N.A. Investigative [74]
[14C]MTEP DMG17IU Discovery agent N.A. Investigative [75]
[3H]methoxy-PEPy DMZ2R1O Discovery agent N.A. Investigative [76]
[3H]methoxymethyl-MTEP DMONI13 Discovery agent N.A. Investigative [75]
[3H]quisqualate DMDQBTX Discovery agent N.A. Investigative [77]
[3H]resolvin E1 DMAMK3P N. A. N. A. Investigative [14]
------------------------------------------------------------------------------------
⏷ Show the Full List of 264 Investigative Drug(s)
Molecule Interaction Atlas

References

1 Pipeline of Addex Pharma. Addex Pharma. 2009.
2 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.
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 The challenges of clinical trials in fragile X syndrome. Psychopharmacology (Berl) 2014; 231(6): 1237-1250.
5 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.
6 Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17.
7 Silent Allosteric Modulation of mGluR5 Maintains Glutamate Signaling while Rescuing Alzheimer's Mouse Phenotypes. Cell Rep. 2017 Jul 5;20(1):76-88.
8 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).
9 Clinical pipeline report, company report or official report of Roche.
10 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.
11 mGlu5 negative allosteric modulators: a patent review (2013 - 2016).Expert Opin Ther Pat. 2017 Jun;27(6):691-706.
12 Clinical pipeline report, company report or official report of AstraZeneca (2009).
13 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.
14 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.
15 Dipyridyl amines: potent metabotropic glutamate subtype 5 receptor antagonists. Bioorg Med Chem Lett. 2005 Oct 1;15(19):4350-3.
16 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.
17 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.
18 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.
19 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.
20 Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists. Bioorg Med Chem Lett. 2007 Dec 1;17(23):6525-8.
21 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.
22 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.
23 Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1892-7.
24 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.
25 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.
26 Structure-activity relationship of thiopyrimidines as mGluR5 antagonists. Bioorg Med Chem Lett. 2006 May 1;16(9):2467-9.
27 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.
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 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.
33 A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5. Mol Pharmacol. 2003 Sep;64(3):731-40.
34 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
35 Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists. Bioorg Med Chem Lett. 2007 Jun 1;17(11):2987-91.
36 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.
37 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.
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 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.
52 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.
53 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.
54 Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator. Bioorg Med Chem Lett. 2009 Jun 15;19(12):3275-8.
55 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.
56 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.
57 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.
58 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.
59 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.
60 Discovery of novel positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5). Bioorg Med Chem Lett. 2011 Mar 1;21(5):1402-6.
61 6-Aryl-3-pyrrolidinylpyridines as mGlu5 receptor negative allosteric modulators. Bioorg Med Chem Lett. 2011 Aug 15;21(16):4891-9.
62 (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.
63 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.
64 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.
65 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.
66 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.
67 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.
68 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.
69 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.
70 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.
71 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.
72 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.
73 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.
74 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.
75 [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.
76 [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.
77 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.