Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTXJ47W)

• DTT Name: Metabotropic glutamate receptor 2 (mGluR2)
• Synonyms: mGLUR2; Group II metabotropic glutamate receptor; Glutamate receptor mGLU2; GPRC1B
• Gene Name: GRM2
• DTT Type: Clinical trial target; [1]
• BioChemical Class: GPCR glutamate
• UniProt ID: GRM2_HUMAN
• TTD ID: T62820
• Sequence:
  MGSLLALLALLLLWGAVAEGPAKKVLTLEGDLVLGGLFPVHQKGGPAEDCGPVNEHRGIQ
  RLEAMLFALDRINRDPHLLPGVRLGAHILDSCSKDTHALEQALDFVRASLSRGADGSRHI
  CPDGSYATHGDAPTAITGVIGGSYSDVSIQVANLLRLFQIPQISYASTSAKLSDKSRYDY
  FARTVPPDFFQAKAMAEILRFFNWTYVSTVASEGDYGETGIEAFELEARARNICVATSEK
  VGRAMSRAAFEGVVRALLQKPSARVAVLFTRSEDARELLAASQRLNASFTWVASDGWGAL
  ESVVAGSEGAAEGAITIELASYPISDFASYFQSLDPWNNSRNPWFREFWEQRFRCSFRQR
  DCAAHSLRAVPFEQESKIMFVVNAVYAMAHALHNMHRALCPNTTRLCDAMRPVNGRRLYK
  DFVLNVKFDAPFRPADTHNEVRFDRFGDGIGRYNIFTYLRAGSGRYRYQKVGYWAEGLTL
  DTSLIPWASPSAGPLPASRCSEPCLQNEVKSVQPGEVCCWLCIPCQPYEYRLDEFTCADC
  GLGYWPNASLTGCFELPQEYIRWGDAWAVGPVTIACLGALATLFVLGVFVRHNATPVVKA
  SGRELCYILLGGVFLCYCMTFIFIAKPSTAVCTLRRLGLGTAFSVCYSALLTKTNRIARI
  FGGAREGAQRPRFISPASQVAICLALISGQLLIVVAWLVVEAPGTGKETAPERREVVTLR
  CNHRDASMLGSLAYNVLLIALCTLYAFKTRKCPENFNEAKFIGFTMYTTCIIWLAFLPIF
  YVTSSDYRVQTTTMCVSVSLSGSVVLGCLFAPKLHIILFQPQKNVVSHRAPTSRFGSAAA
  RASSSLGQGSGSQFVPTVCNGREVVDSTTSSL
• Function: Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. May mediate suppression of neurotransmission or may be involved in synaptogenesis or synaptic stabilization. G-protein coupled receptor for glutamate.
• KEGG Pathway:
  Neuroactive ligand-receptor interaction (hsa04080)
  Glutamatergic synapse (hsa04724)
  Cocaine addiction (hsa05030)
• Reactome Pathway:
  Class C/3 (Metabotropic glutamate/pheromone receptors) (R-HSA-420499)
  G alpha (i) signalling events (R-HSA-418594)

Molecular Interaction Atlas (MIA) of This DTT

10 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
JNJ-64281802	DMNMSVX	Dengue	1D20-1D2Z	Phase 2	[2]
MP-101	DMYCITZ	Alzheimer disease	8A20	Phase 2	[3]
Oleoyl-estrone	DM0RA8F	Alzheimer disease	8A20	Phase 2	[4]
RO-4995819	DMNTC7O	Major depressive disorder	6A70.3	Phase 2	[5]
ADX71149	DMBUOX4	Epilepsy	8A60-8A68	Phase 1	[6]
BCI-632	DMZYCWT	Alzheimer disease	8A20	Phase 1	[7]
BCI-838	DMRXDN3	Major depressive disorder	6A70.3	Phase 1	[8]
JNJ-42491293	DMOL9JR	Psychiatric disorder	6E8Z	Phase 1	[9]
LY-2979165	DM16IX2	Bipolar disorder	6A60	Phase 1	[10]
Pomaglumetad	DMTOLI5	Schizophrenia	6A20	Phase 1	[1]

49 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ethinyl-pyrazole derivative 1	DMLOBAQ	N. A.	N. A.	Patented	[11]
Ethinyl-pyrazole derivative 2	DMA3PE7	N. A.	N. A.	Patented	[11]
Ethinyl-pyrazole derivative 3	DM87DOX	N. A.	N. A.	Patented	[11]
Heteroaryl-pyrazole derivative 1	DM9LQCH	N. A.	N. A.	Patented	[11]
Heteroaryl-pyrazole derivative 2	DMIG0TQ	N. A.	N. A.	Patented	[11]
Heteroaryl-pyrazole derivative 3	DMO45G3	N. A.	N. A.	Patented	[11]
N-substituted pyrazole derivative 1	DMHTVGM	N. A.	N. A.	Patented	[11]
N-substituted pyrazole derivative 2	DMQWODI	N. A.	N. A.	Patented	[11]
N-substituted pyrazole derivative 3	DM5TIFH	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-10	DM12QO7	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-15	DMHBWNS	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-16	DMKFX2G	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-20	DMG9FYH	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-22	DM27U1F	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-25	DMIVJMO	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-26	DMTJHAK	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-37	DMTYHCU	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-38	DMSIKM2	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-39	DMG2ES1	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-40	DMW2C19	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-41	DMJ5LGA	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-42	DMTN79G	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-43	DMEGJ73	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-44	DM4K3AU	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-45	DM74WSJ	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-46	DMC6HPV	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-47	DM92F1C	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-49	DM7G51M	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-50	DML48NA	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-51	DM2VZG6	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-52	DMXD8L1	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-53	DMSRYIP	N. A.	N. A.	Patented	[11]
Pyrazole derivative 76	DM6Y27J	N. A.	N. A.	Patented	[11]
Pyrazole derivative 77	DM5E1ZJ	N. A.	N. A.	Patented	[11]
Pyrazole derivative 78	DMMCHOW	N. A.	N. A.	Patented	[11]
Pyrazole derivative 79	DM9JHYL	N. A.	N. A.	Patented	[11]
Quinoline derivative 3	DMDV6EY	N. A.	N. A.	Patented	[11]
Quinoline derivative 4	DMPB4L6	N. A.	N. A.	Patented	[11]
Quinoline derivative 5	DMS1TOX	N. A.	N. A.	Patented	[11]
Quinoline derivative 6	DMVBPGI	N. A.	N. A.	Patented	[11]
Quinoline derivative 7	DM56I8H	N. A.	N. A.	Patented	[11]
Quinoline derivative 8	DMLIW1X	N. A.	N. A.	Patented	[11]
Quinoline derivative 9	DMIC86N	N. A.	N. A.	Patented	[11]
Tetra-hydro-imidazo[1,5-d][1,4]oxazepin-3-yl derivative 1	DM3W5SM	N. A.	N. A.	Patented	[11]
Tetra-hydro-imidazo[1,5-d][1,4]oxazepin-3-yl derivative 2	DMB1T6S	N. A.	N. A.	Patented	[11]
Tetra-hydro-imidazo[1,5-d][1,4]oxazepin-3-yl derivative 3	DM71LVY	N. A.	N. A.	Patented	[11]
Tetra-hydro-imidazo[1,5-d][1,4]oxazepin-3-yl derivative 4	DMLMXT6	N. A.	N. A.	Patented	[11]
Tetra-hydro-imidazo[1,5-d][1,4]oxazepin-3-yl derivative 5	DM7C0R8	N. A.	N. A.	Patented	[11]
Tetra-hydro-imidazo[1,5-d][1,4]oxazepin-3-yl derivative 6	DMCE3J0	N. A.	N. A.	Patented	[11]

6 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LY-544344	DMSC4K1	Anxiety disorder	6B00-6B0Z	Discontinued in Phase 3	[12]
LY-2300559	DMTS1X5	Migraine	8A80	Discontinued in Phase 2	[13]
LY354740	DM08BIZ	Anxiety disorder	6B00-6B0Z	Discontinued in Phase 2	[14]
R-1578	DMAPRGQ	Mood disorder	6A60-6E23	Discontinued in Phase 2	[15]
RG1578	DM3TU7D	Major depressive disorder	6A70.3	Discontinued in Phase 2	[16]
TS-032	DMOHEYU	Schizophrenia	6A20	Discontinued in Phase 1	[17]

37 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(+)-MCPG	DMG5QJB	Discovery agent	N.A.	Investigative	[18]
(1S,3R)-ACPD	DM5DOAF	Discovery agent	N.A.	Investigative	[19]
(2R,4R)-4-aminopyrrolidine-2,4-dicarboxylate	DMYW40T	Discovery agent	N.A.	Investigative	[20]
(S)-4C3HPG	DMQK4I2	Discovery agent	N.A.	Investigative	[18]
3-MPPTS	DMCDLG4	Discovery agent	N.A.	Investigative	[21]
4-APPES	DM1UXHE	Discovery agent	N.A.	Investigative	[21]
4-MPPTS	DM4E6HW	Discovery agent	N.A.	Investigative	[22]
alpha-methylserine-O-phosphate	DMCIH1X	Discovery agent	N.A.	Investigative	[18]
biphenylindanone A	DM2MYKC	Discovery agent	N.A.	Investigative	[23]
CBiPES	DMALVY7	Discovery agent	N.A.	Investigative	[21]
cyPPTS	DME9LPO	Discovery agent	N.A.	Investigative	[21]
DCG IV	DM9HG1Y	Discovery agent	N.A.	Investigative	[24]
DT-2228	DMCKQF7	Major depressive disorder	6A70.3	Investigative	[25]
eGlu	DMKW0Q3	Discovery agent	N.A.	Investigative	[14]
GSK1331268	DMIWY7Q	Discovery agent	N.A.	Investigative	[26]
JNJ-42153605	DMLOQ92	Discovery agent	N.A.	Investigative	[27]
L-CCG-I	DMPZ8XH	Discovery agent	N.A.	Investigative	[19]
LY-379268	DMME40U	Discovery agent	N.A.	Investigative	[28]
LY-389795	DM6Y2XG	Discovery agent	N.A.	Investigative	[28]
MGS0028	DMIMKFZ	Discovery agent	N.A.	Investigative	[29]
MNI-135	DMBJFH9	Discovery agent	N.A.	Investigative	[30]
MNI-136	DM5C9VI	Discovery agent	N.A.	Investigative	[30]
MNI-137	DMKRI1J	Discovery agent	N.A.	Investigative	[30]
PCCG-4	DMD9KYN	Discovery agent	N.A.	Investigative	[31]
PMID20409708C34	DMA2Y74	Discovery agent	N.A.	Investigative	[32]
PMID21155570C14	DM7I341	Discovery agent	N.A.	Investigative	[33]
PMID22364337C48	DMRLG7Z	Discovery agent	N.A.	Investigative	[34]
PTBE	DMY02IR	Discovery agent	N.A.	Investigative	[35]
Ro4491533	DMJLSX0	Discovery agent	N.A.	Investigative	[36]
RO4988546	DM6SQ9A	Discovery agent	N.A.	Investigative	[37]
RO5488608	DMHXGCO	Discovery agent	N.A.	Investigative	[37]
Ro64-5229	DMXOTHC	Discovery agent	N.A.	Investigative	[38]
THIIC	DM3KU46	Discovery agent	N.A.	Investigative	[39]
[3H]2,2,2-TEMPS	DMQO8AF	Discovery agent	N.A.	Investigative	[37]
[3H]JNJ-40068782	DMSE56B	Discovery agent	N.A.	Investigative	[40]
[3H]LY341495	DMGX0Y8	Discovery agent	N.A.	Investigative	[19]
[3H]quisqualate	DMDQBTX	Discovery agent	N.A.	Investigative	[41]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Schizophrenia	6A20	Pre-frontal cortex	1.09E-01	-0.11	-0.2
Schizophrenia	6A20	Superior temporal cortex	3.19E-01	-0.06	-0.34
Bipolar disorder	6A20	Pre-frontal cortex	1.04E-01	-0.13	-0.51
Major depressive disorder	6A20	Pre-frontal cortex	6.83E-01	-0.06	-0.25

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