General Information of the Protein
Protein ID
PT01748
Protein Name
Metabotropic glutamate receptor 2
Gene Name
GRM2
Secondarily
Gene Name
GPRC1B
MGLUR2
Sequence
MGSLLALLALLLLWGAVAEGPAKKVLTLEGDLVLGGLFPVHQKGGPAEDCGPVNEHRGIQRLEAMLFALDRINRDPHLLPGVRLGAHILDSCSKDTHALEQALDFVRASLSRGADGSRHICPDGSYATHGDAPTAITGVIGGSYSDVSIQVANLLRLFQIPQISYASTSAKLSDKSRYDYFARTVPPDFFQAKAMAEILRFFNWTYVSTVASEGDYGETGIEAFELEARARNICVATSEKVGRAMSRAAFEGVVRALLQKPSARVAVLFTRSEDARELLAASQRLNASFTWVASDGWGALESVVAGSEGAAEGAITIELASYPISDFASYFQSLDPWNNSRNPWFREFWEQRFRCSFRQRDCAAHSLRAVPFEQESKIMFVVNAVYAMAHALHNMHRALCPNTTRLCDAMRPVNGRRLYKDFVLNVKFDAPFRPADTHNEVRFDRFGDGIGRYNIFTYLRAGSGRYRYQKVGYWAEGLTLDTSLIPWASPSAGPLPASRCSEPCLQNEVKSVQPGEVCCWLCIPCQPYEYRLDEFTCADCGLGYWPNASLTGCFELPQEYIRWGDAWAVGPVTIACLGALATLFVLGVFVRHNATPVVKASGRELCYILLGGVFLCYCMTFIFIAKPSTAVCTLRRLGLGTAFSVCYSALLTKTNRIARIFGGAREGAQRPRFISPASQVAICLALISGQLLIVVAWLVVEAPGTGKETAPERREVVTLRCNHRDASMLGSLAYNVLLIALCTLYAFKTRKCPENFNEAKFIGFTMYTTCIIWLAFLPIFYVTSSDYRVQTTTMCVSVSLSGSVVLGCLFAPKLHIILFQPQKNVVSHRAPTSRFGSAAARASSSLGQGSGSQFVPTVCNGREVVDSTTSSL
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family C G protein-coupled receptor
>
Small molecule receptor (family C GPCR)
>
Neurotransmitter receptor (family C GPCR)
>
Metabotropic glutamate receptor
Function
G-protein coupled receptor for glutamate. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. May mediate suppression of neurotransmission or may be involved in synaptogenesis or synaptic stabilization.
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Uniprot ID
Primary ID:
Q14416

Secondarily ID:
B0M0K7
Q14CU5
Q52MC6
Q9H3N6
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Ensembl ID
ENSG00000164082
HGNC ID
HGNC:4594
Subcellular Location
Cell membrane
Synapse
Cell projection
Dendrite
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000094 , 1321N1
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0170781
 Compound Info 
9-Dimethylamino-3-(4-ethyl-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one
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C19H18N4OS
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000051 , BHK-21
 Cell Line Info 
Cell Line ID: CL000064 , Chem-1
 Cell Line Info 
Cell Line ID: CL000011 , CHO
 Cell Line Info 
Cell Line ID: CL000389 , CHO-DXB11
 Cell Line Info 
Cell Line ID: CL000026 , CHO-K1
 Cell Line Info 
Cell Line ID: CL000460 , Flp-In-T-REx-293
 Cell Line Info 
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000125 , MCB3901
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0217750
 Compound Info 
2,2,2-Trifluoro-ethanesulfonic acid [3-(1-methyl-butoxy)-phenyl]-pyridin-3-ylmethyl-amide
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C19H23F3N2O3S
  1
1 EC50 = 14 nM
CP0070721
 Compound Info 
3-(cyclopropylmethyl)-7-(4-phenylpiperidin-1-yl)-8-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine
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C22H23F3N4
  2
1 EC50 = 147 nM
2 Ki = 15 nM
CP0693205
 Compound Info 
5-Phenethylamino-2-propylisoquinolin-1(2H)-one
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C20H22N2O
  1
1 EC50 = 158.49 nM
CP0002355
 Compound Info 
(2S)-2-aminopentanedioic acid
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C5H9NO4
  3
1 EC50 = 290 nM
2 EC50 = 4700 nM
3 Ki = 1200 nM
CP0047317
 Compound Info 
1-(2,2-dimethylpropyl)-5-[5-(2-hydroxypropan-2-yl)-2-methylphenyl]-3-methylimidazo[4,5-b]pyridin-2-one
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C22H29N3O2
  1
1 EC50 = 600 nM
CP0049004
 Compound Info 
(1S,3R)-1-aminocyclopentane-1,3-dicarboxylic acid;hydrate
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C7H11NO4
  2
1 EC50 = 2000 nM
2 EC50 = 12100 nM
CP0069484
 Compound Info 
(+/-)-trans-ACPD
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C7H11NO4
  1
1 EC50 = 13000 nM
CP0076675
 Compound Info 
(1S,2S,5R,6S)-2-Amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C8H11NO4
  3
1 IC50 = 7 nM
2 Ki = 13 nM
3 Ki = 84.7 nM
CP0445963
 Compound Info 
(1S,2S,4R,5R,6R)-2-amino-4-hydroxybicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C8H11NO5
  1
1 IC50 = 8.6 nM
CP0068843
 Compound Info 
US9278960, 2-7
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C21H16FN3O3
  2
1 IC50 = 9 nM
2 IC50 = 20 nM
CP0322665
 Compound Info 
US9278960, 3-45
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C24H20F4N4O2
  1
1 IC50 = 16 nM
CP0367697
 Compound Info 
US9278960, 2-21
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C22H18FN3O3
  1
1 IC50 = 21 nM
CP0432878
 Compound Info 
(1S,2S,4S,5R,6R)-2-amino-4-hydroxybicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C8H11NO5
  1
1 IC50 = 22.6 nM
CP0134841
 Compound Info 
US9278960, 3-16
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C22H18F4N6O2
  1
1 IC50 = 36 nM
CP0489699
 Compound Info 
US9278960, 2-37
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C22H20FN3O2
  1
1 IC50 = 58 nM
CP0576400
 Compound Info 
US9278960, 4-25
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C21H18F3N3O
  1
1 IC50 = 61 nM
CP0419157
 Compound Info 
US9278960, 4-1
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C21H20FN3O2
  1
1 IC50 = 68 nM
CP0238235
 Compound Info 
US9278960, 8-29
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C24H21FN4O2
  1
1 IC50 = 146 nM
CP0367698
 Compound Info 
US9278960, 1-24
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C16H11FN2O
  1
1 IC50 = 149 nM
CP0202837
 Compound Info 
4-(3-(2,6-dimethylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C24H20F3N3O
  1
1 IC50 = 296 nM
CP0211752
 Compound Info 
(1R,2R,3R,5R,6R)-2-Amino-3-(3,4-dichloro-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C15H14Cl2FNO5
  1
1 Ki = 2.2 nM
CP0046845
 Compound Info 
3-(cyclopropylmethyl)-7-[[4-(2,4-difluorophenyl)piperazin-1-yl]methyl]-8-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine
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C22H22F5N5
  1
1 Ki = 150 nM
CP0054727
 Compound Info 
1-butyl-3-chloro-4-(4-phenylpiperidin-1-yl)pyridin-2-one
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C20H25ClN2O
  1
1 Ki = 180 nM
Clinical Information about the Protein
Target 1 ( Metabotropic glutamate receptor 2 (mGluR2) )
Target Type Clinical trial Target
Disease 3 Target-related Diseases  3
1 Major depressive disorder [ICD-11: 6A70.3]
2 Anxiety disorder [ICD-11: 6B00-6B0Z]
3 Epilepsy [ICD-11: 8A60-8A68]
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 BCI-632
 Drug Info 
Phase 1
Major depressive disorder
2 ADX71149
 Drug Info 
Phase 1
Epilepsy
Discontinued Drug(s) 2 Discontinued Drugs  2
1 LY-544344
 Drug Info 
Discontinued in Phase 3
Anxiety disorder
2 LY354740
 Drug Info 
Discontinued in Phase 2
Anxiety disorder