Details of the Drug-Related molecule(s) Interaction Atlas

General Information of DTT (ID: TTHS256)

• DTT Name: Metabotropic glutamate receptor 5 (mGluR5) DTT Info
• UniProt ID: GRM5_HUMAN
• Gene Name: GRM5

Molecule-Related Drug & Molecule List

9 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], [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]

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	[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]

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	[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]

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	[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]

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] 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.