Target Information
| Target General Information | Top | |||||
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| Target ID |
T62820
(Former ID: TTDR00321)
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| Target Name |
Metabotropic glutamate receptor 2 (mGluR2)
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| Synonyms |
mGLUR2; Group II metabotropic glutamate receptor; Glutamate receptor mGLU2; GPRC1B
Click to Show/Hide
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| Gene Name |
GRM2
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 9 Target-related Diseases | + | ||||
| 1 | Alzheimer disease [ICD-11: 8A20] | |||||
| 2 | Dengue fever [ICD-11: 1D2Z] | |||||
| 3 | Obesity [ICD-11: 5B80-5B81] | |||||
| 4 | Psychotic disorder [ICD-11: 6A20-6A25] | |||||
| 5 | Bipolar disorder [ICD-11: 6A60] | |||||
| 6 | Depression [ICD-11: 6A70-6A7Z] | |||||
| 7 | Epilepsy/seizure [ICD-11: 8A61-8A6Z] | |||||
| 8 | Mental/behavioural/neurodevelopmental disorder [ICD-11: 6E20-6E8Z] | |||||
| 9 | Schizophrenia [ICD-11: 6A20] | |||||
| 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.
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| BioChemical Class |
GPCR glutamate
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| UniProt ID | ||||||
| Sequence |
MGSLLALLALLLLWGAVAEGPAKKVLTLEGDLVLGGLFPVHQKGGPAEDCGPVNEHRGIQ
RLEAMLFALDRINRDPHLLPGVRLGAHILDSCSKDTHALEQALDFVRASLSRGADGSRHI CPDGSYATHGDAPTAITGVIGGSYSDVSIQVANLLRLFQIPQISYASTSAKLSDKSRYDY FARTVPPDFFQAKAMAEILRFFNWTYVSTVASEGDYGETGIEAFELEARARNICVATSEK VGRAMSRAAFEGVVRALLQKPSARVAVLFTRSEDARELLAASQRLNASFTWVASDGWGAL ESVVAGSEGAAEGAITIELASYPISDFASYFQSLDPWNNSRNPWFREFWEQRFRCSFRQR DCAAHSLRAVPFEQESKIMFVVNAVYAMAHALHNMHRALCPNTTRLCDAMRPVNGRRLYK DFVLNVKFDAPFRPADTHNEVRFDRFGDGIGRYNIFTYLRAGSGRYRYQKVGYWAEGLTL DTSLIPWASPSAGPLPASRCSEPCLQNEVKSVQPGEVCCWLCIPCQPYEYRLDEFTCADC GLGYWPNASLTGCFELPQEYIRWGDAWAVGPVTIACLGALATLFVLGVFVRHNATPVVKA SGRELCYILLGGVFLCYCMTFIFIAKPSTAVCTLRRLGLGTAFSVCYSALLTKTNRIARI FGGAREGAQRPRFISPASQVAICLALISGQLLIVVAWLVVEAPGTGKETAPERREVVTLR CNHRDASMLGSLAYNVLLIALCTLYAFKTRKCPENFNEAKFIGFTMYTTCIIWLAFLPIF YVTSSDYRVQTTTMCVSVSLSGSVVLGCLFAPKLHIILFQPQKNVVSHRAPTSRFGSAAA RASSSLGQGSGSQFVPTVCNGREVVDSTTSSL Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Drugs and Modes of Action | Top | |||||
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| Clinical Trial Drug(s) | [+] 8 Clinical Trial Drugs | + | ||||
| 1 | Oleoyl-estrone | Drug Info | Phase 2 | Obesity | [4] | |
| 2 | RO-4995819 | Drug Info | Phase 2 | Major depressive disorder | [5] | |
| 3 | ADX71149 | Drug Info | Phase 1 | Epilepsy | [6] | |
| 4 | BCI-632 | Drug Info | Phase 1 | Major depressive disorder | [7] | |
| 5 | BCI-838 | Drug Info | Phase 1 | Major depressive disorder | [8] | |
| 6 | JNJ-42491293 | Drug Info | Phase 1 | Psychiatric disorder | [9] | |
| 7 | LY-2979165 | Drug Info | Phase 1 | Bipolar disorder | [10] | |
| 8 | Pomaglumetad | Drug Info | Phase 1 | Schizophrenia | [11] | |
| Discontinued Drug(s) | [+] 4 Discontinued Drugs | + | ||||
| 1 | LY-544344 | Drug Info | Discontinued in Phase 3 | Anxiety disorder | [12] | |
| 2 | LY-2300559 | Drug Info | Discontinued in Phase 2 | Migraine | [16] | |
| 3 | RG1578 | Drug Info | Discontinued in Phase 2 | Major depressive disorder | [13] | |
| 4 | TS-032 | Drug Info | Discontinued in Phase 1 | Schizophrenia | [17] | |
| Mode of Action | [+] 6 Modes of Action | + | ||||
| Agonist | [+] 7 Agonist drugs | + | ||||
| 1 | Oleoyl-estrone | Drug Info | [6], [18] | |||
| 2 | LY-544344 | Drug Info | [26] | |||
| 3 | TS-032 | Drug Info | [29] | |||
| 4 | (1S,3R)-ACPD | Drug Info | [31] | |||
| 5 | (2R,4R)-4-aminopyrrolidine-2,4-dicarboxylate | Drug Info | [32], [33] | |||
| 6 | (S)-4C3HPG | Drug Info | [30] | |||
| 7 | MGS0028 | Drug Info | [42] | |||
| Modulator | [+] 8 Modulator drugs | + | ||||
| 1 | RO-4995819 | Drug Info | [19] | |||
| 2 | ADX71149 | Drug Info | [20] | |||
| 3 | BCI-838 | Drug Info | [22] | |||
| 4 | LY-2979165 | Drug Info | [24] | |||
| 5 | Pomaglumetad | Drug Info | [1] | |||
| 6 | LY-2300559 | Drug Info | [27] | |||
| 7 | RG1578 | Drug Info | [28] | |||
| 8 | DT-2228 | Drug Info | [37] | |||
| Antagonist | [+] 51 Antagonist drugs | + | ||||
| 1 | BCI-632 | Drug Info | [21] | |||
| 2 | Ethinyl-pyrazole derivative 1 | Drug Info | [25] | |||
| 3 | Ethinyl-pyrazole derivative 2 | Drug Info | [25] | |||
| 4 | Ethinyl-pyrazole derivative 3 | Drug Info | [25] | |||
| 5 | Heteroaryl-pyrazole derivative 1 | Drug Info | [25] | |||
| 6 | Heteroaryl-pyrazole derivative 2 | Drug Info | [25] | |||
| 7 | Heteroaryl-pyrazole derivative 3 | Drug Info | [25] | |||
| 8 | N-substituted pyrazole derivative 1 | Drug Info | [25] | |||
| 9 | PMID25435285-Compound-10 | Drug Info | [25] | |||
| 10 | PMID25435285-Compound-15 | Drug Info | [25] | |||
| 11 | PMID25435285-Compound-16 | Drug Info | [25] | |||
| 12 | PMID25435285-Compound-20 | Drug Info | [25] | |||
| 13 | PMID25435285-Compound-22 | Drug Info | [25] | |||
| 14 | PMID25435285-Compound-25 | Drug Info | [25] | |||
| 15 | PMID25435285-Compound-26 | Drug Info | [25] | |||
| 16 | PMID25435285-Compound-37 | Drug Info | [25] | |||
| 17 | PMID25435285-Compound-38 | Drug Info | [25] | |||
| 18 | PMID25435285-Compound-39 | Drug Info | [25] | |||
| 19 | PMID25435285-Compound-40 | Drug Info | [25] | |||
| 20 | PMID25435285-Compound-42 | Drug Info | [25] | |||
| 21 | PMID25435285-Compound-43 | Drug Info | [25] | |||
| 22 | PMID25435285-Compound-44 | Drug Info | [25] | |||
| 23 | PMID25435285-Compound-45 | Drug Info | [25] | |||
| 24 | PMID25435285-Compound-46 | Drug Info | [25] | |||
| 25 | PMID25435285-Compound-47 | Drug Info | [25] | |||
| 26 | PMID25435285-Compound-49 | Drug Info | [25] | |||
| 27 | PMID25435285-Compound-51 | Drug Info | [25] | |||
| 28 | PMID25435285-Compound-52 | Drug Info | [25] | |||
| 29 | PMID25435285-Compound-53 | Drug Info | [25] | |||
| 30 | Pyrazole derivative 76 | Drug Info | [25] | |||
| 31 | Pyrazole derivative 77 | Drug Info | [25] | |||
| 32 | Pyrazole derivative 78 | Drug Info | [25] | |||
| 33 | Pyrazole derivative 79 | Drug Info | [25] | |||
| 34 | Quinoline derivative 3 | Drug Info | [25] | |||
| 35 | Quinoline derivative 4 | Drug Info | [25] | |||
| 36 | Quinoline derivative 5 | Drug Info | [25] | |||
| 37 | Quinoline derivative 6 | Drug Info | [25] | |||
| 38 | Quinoline derivative 7 | Drug Info | [25] | |||
| 39 | Quinoline derivative 8 | Drug Info | [25] | |||
| 40 | Quinoline derivative 9 | Drug Info | [25] | |||
| 41 | Tetra-hydro-imidazo[1,5-d][1,4]oxazepin-3-yl derivative 1 | Drug Info | [25] | |||
| 42 | Tetra-hydro-imidazo[1,5-d][1,4]oxazepin-3-yl derivative 2 | Drug Info | [25] | |||
| 43 | Tetra-hydro-imidazo[1,5-d][1,4]oxazepin-3-yl derivative 3 | Drug Info | [25] | |||
| 44 | Tetra-hydro-imidazo[1,5-d][1,4]oxazepin-3-yl derivative 4 | Drug Info | [25] | |||
| 45 | Tetra-hydro-imidazo[1,5-d][1,4]oxazepin-3-yl derivative 5 | Drug Info | [25] | |||
| 46 | Tetra-hydro-imidazo[1,5-d][1,4]oxazepin-3-yl derivative 6 | Drug Info | [25] | |||
| 47 | (+)-MCPG | Drug Info | [30] | |||
| 48 | alpha-methylserine-O-phosphate | Drug Info | [30] | |||
| 49 | eGlu | Drug Info | [38] | |||
| 50 | PCCG-4 | Drug Info | [44] | |||
| 51 | [3H]LY341495 | Drug Info | [31], [32] | |||
| Binder | [+] 1 Binder drugs | + | ||||
| 1 | JNJ-42491293 | Drug Info | [23] | |||
| Modulator (allosteric modulator) | [+] 22 Modulator (allosteric modulator) drugs | + | ||||
| 1 | 3-MPPTS | Drug Info | [34] | |||
| 2 | 4-APPES | Drug Info | [34] | |||
| 3 | 4-MPPTS | Drug Info | [35] | |||
| 4 | biphenylindanone A | Drug Info | [36] | |||
| 5 | CBiPES | Drug Info | [34] | |||
| 6 | cyPPTS | Drug Info | [34] | |||
| 7 | GSK1331268 | Drug Info | [39] | |||
| 8 | JNJ-42153605 | Drug Info | [40] | |||
| 9 | MNI-135 | Drug Info | [43] | |||
| 10 | MNI-136 | Drug Info | [43] | |||
| 11 | MNI-137 | Drug Info | [43] | |||
| 12 | PMID20409708C34 | Drug Info | [45] | |||
| 13 | PMID21155570C14 | Drug Info | [46] | |||
| 14 | PMID22364337C48 | Drug Info | [47] | |||
| 15 | PTBE | Drug Info | [48] | |||
| 16 | Ro4491533 | Drug Info | [49] | |||
| 17 | RO4988546 | Drug Info | [50] | |||
| 18 | RO5488608 | Drug Info | [50] | |||
| 19 | Ro64-5229 | Drug Info | [51] | |||
| 20 | THIIC | Drug Info | [52] | |||
| 21 | [3H]2,2,2-TEMPS | Drug Info | [35], [50] | |||
| 22 | [3H]JNJ-40068782 | Drug Info | [53] | |||
| Inhibitor | [+] 3 Inhibitor drugs | + | ||||
| 1 | LY-379268 | Drug Info | [41] | |||
| 2 | LY-389795 | Drug Info | [41] | |||
| 3 | [3H]quisqualate | Drug Info | [54] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: ADX71149 | Ligand Info | |||||
| Structure Description | Cryo-EM structure of Gi-bound metabotropic glutamate receptor mGlu2 | PDB:7E9G | ||||
| Method | Electron microscopy | Resolution | 3.50 Å | Mutation | Yes | [55] |
| PDB Sequence |
KKVLTLEGDL
32 VLGGLFPVHQ42 KGGPAEDCGP52 VNEHRGIQRL62 EAMLFALDRI72 NRDPHLLPGV 82 RLGAHILDSC92 SKDTHALEQA102 LDFVRASLIT137 GVIGGSYSDV147 SIQVANLLRL 157 FQIPQISYAS167 TSAKLSDKSR177 YDYFARTVPP187 DFFQAKAMAE197 ILRFFNWTYV 207 STVASEGDYG217 ETGIEAFELE227 ARARNICVAT237 SEKVGRAMSR247 AAFEGVVRAL 257 LQKPSARVAV267 LFTRSEDARE277 LLAASQRLNA287 SFTWVASDGW297 GALESVVAGS 307 EGAAEGAITI317 ELASYPISDF327 ASYFQSLDPW337 NNSRNPWFRE347 FWEQRFRCSF 357 RQRDCAAHSL367 RAVPFEQESK377 IMFVVNAVYA387 MAHALHNMHR397 ALCPNTTRLC 407 DAMRPVNGRR417 LYKDFVLNVK427 FDAPFRPADT437 HNEVRFDRFG447 DGIGRYNIFT 457 YLRAGSGRYR467 YQKVGYWAEG477 LTLDTSLIPW487 ASPSAGPLPA497 SRCSEPCLQN 507 EVKSVQPGEV517 CCWLCIPCQP527 YEYRLDEFTC537 ADCGLGYWPN547 ASLTGCFELP 557 QEYIRWGDAW567 AVGPVTIACL577 GALATLFVLG587 VFVRHNATPV597 VKAAGRELCY 607 ILLGGVFLCY617 CMTFIFIAKP627 STAVCTLRRL637 GLGTAFSVCY647 SALLTKTNRI 657 ARIFGGAREG667 AQRPRFISPA677 SQVAICLALI687 SGQLLIVVAW697 LVVEAPGTGK 707 ETAPERREVV717 TLRCNHRDAS727 MLGSLAYNVL737 LIALCTLYAF747 KTRKCPENFN 757 EAKFIGFTMY767 TTCIIWLAFL777 PIFYVTSSDY787 RVQTTTMCVS797 VSLSGSVVLG 807 CLFAPKLHI
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| Ligand Name: [3H]LY341495 | Ligand Info | |||||
| Structure Description | CryoEM Structure of Full-Length mGlu2 in Inactive-State Bound to Antagonist LY341495 | PDB:7MTQ | ||||
| Method | Electron microscopy | Resolution | 3.65 Å | Mutation | No | [56] |
| PDB Sequence |
KVLTLEGDLV
33 LGGLFPVHQK43 PAEDCGPVNE55 HRGIQRLEAM65 LFALDRINRD75 PHLLPGVRLG 85 AHILDSCSKD95 THALEQALDF105 VRASLPTAIT137 GVIGGSYSDV147 SIQVANLLRL 157 FQIPQISYAS167 TSAKLSDKSR177 YDYFARTVPP187 DFFQAKAMAE197 ILRFFNWTYV 207 STVASEGDYG217 ETGIEAFELE227 ARARNICVAT237 SEKVGRAMSR247 AAFEGVVRAL 257 LQKPSARVAV267 LFTRSEDARE277 LLAASQRLNA287 SFTWVASDGW297 GALESVVAGS 307 EGAAEGAITI317 ELASYPISDF327 ASYFQSLDPW337 NNSRNPWFRE347 FWEQRFRCSF 357 RQRDCAAHSL367 RAVPFEQESK377 IMFVVNAVYA387 MAHALHNMHR397 ALCPNTTRLC 407 DAMRPVNGRR417 LYKDFVLNVK427 FDAPFRPADT437 HNEVRFDRFG447 DGIGRYNIFT 457 YLRAGSGRYR467 YQKVGYWAEG477 LTLDTSLIPW487 ASAGPLPASR499 CSEPCLQNEV 509 KSVQEVCCWL521 CIPCQYELDE534 FTCADCGLGW545 PNLTGCFELP557 QEYIRWDAWA 568 VGPVTIACLG578 ALATLFVLGV588 FVRHNATPVV598 KASGRELCYI608 LLGGVFLCYC 618 MTFIFIAKPS628 TAVCTLRRLG638 LGTAFSVCYS648 ALLTKTNRIA658 RSPASQVAIC 683 LALISGQLLI693 VVAWLVVEAP703 GTETAPERRE715 VVTLRCNHRD725 ASMLGSLAYN 735 VLLILCTLYA746 FKTRKCPENF756 NEAKFIGFTM766 YTTCIIWLAF776 LPIFYVTSSD 786 YRVQTTTMCV796 SVSLSGSVVL806 GCLFAPKLHI816 IL
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Tissue Distribution
Human Pathway Affiliation
Biological Network Descriptors
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There is no similarity protein (E value < 0.005) for this target
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
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| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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| Phospholipase D signaling pathway | hsa04072 | Affiliated Target |
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| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
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| Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
| Glutamatergic synapse | hsa04724 | Affiliated Target |
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| Class: Organismal Systems => Nervous system | Pathway Hierarchy | ||
| Degree | 1 | Degree centrality | 1.07E-04 | Betweenness centrality | 0.00E+00 |
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| Closeness centrality | 1.56E-01 | Radiality | 1.22E+01 | Clustering coefficient | 0.00E+00 |
| Neighborhood connectivity | 2.00E+00 | Topological coefficient | 1.00E+00 | Eccentricity | 13 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
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| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 3 KEGG Pathways | + | ||||
| 1 | Neuroactive ligand-receptor interaction | |||||
| 2 | Glutamatergic synapse | |||||
| 3 | Cocaine addiction | |||||
| Panther Pathway | [+] 4 Panther Pathways | + | ||||
| 1 | Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway | |||||
| 2 | Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway | |||||
| 3 | Ionotropic glutamate receptor pathway | |||||
| 4 | Metabotropic glutamate receptor group II pathway | |||||
| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | G alpha (i) signalling events | |||||
| 2 | Class C/3 (Metabotropic glutamate/pheromone receptors) | |||||
| WikiPathways | [+] 3 WikiPathways | + | ||||
| 1 | GPCRs, Class C Metabotropic glutamate, pheromone | |||||
| 2 | GPCR ligand binding | |||||
| 3 | GPCR downstream signaling | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | LY-2140023, a prodrug of the group II metabotropic glutamate receptor agonist LY-404039 for the potential treatment of schizophrenia. Curr Opin Investig Drugs. 2010 Jul;11(7):833-45. | |||||
| REF 2 | ClinicalTrials.gov (NCT03044249) A Study of MP-101 in Dementia-Related Psychosis and/or Agitation and Aggression. U.S. National Institutes of Health. | |||||
| REF 3 | ClinicalTrials.gov (NCT04480736) A Phase 2a, Randomized, Double-blind, Placebo-controlled Trial to Evaluate the Antiviral Activity, Safety, and Pharmacokinetics of Repeated Oral Doses of JNJ-64281802 Against Dengue Serotype 1 Infection in a Dengue Human Challenge Model in Healthy Adult Participants. U.S.National Institutes of Health. | |||||
| REF 4 | ClinicalTrials.gov (NCT00449202) Phase 2a Obesity Study of Oral Doses of Oleoyl-Estrone (MP-101). U.S. National Institutes of Health. | |||||
| REF 5 | ClinicalTrials.gov (NCT01457677) ARTDeCo Study: A Study of RO4995819 in Patients With Major Depressive Disorder And Inadequate Response to Ongoing Antidepressant Treatment in Hoffmann-La Roche. | |||||
| REF 6 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 7 | ClinicalTrials.gov (NCT01548703) A Multiple Ascending Dose Study of BCI-838 in Healthy Volunteers. U.S. National Institutes of Health. | |||||
| REF 8 | ClinicalTrials.gov (NCT01548703) A Multiple Ascending Dose Study of BCI-838 in Healthy Volunteers in BrainCells Inc. | |||||
| REF 9 | ClinicalTrials.gov (NCT01359852) A Study of [11C]JNJ-42491293, a Possible PET Ligand for the mGlu2 Receptor, in Healthy Adult Volunteers in Healthy Volunteers in Johnson & Johnson Pharmaceutical Research & Development, L.L.C. | |||||
| REF 10 | ClinicalTrials.gov (NCT01248052) A First Human Dose Study to Investigate Safety and Tolerability of LY2979165 in Healthy Volunteers in Eli Lilly and Company. | |||||
| REF 11 | ClinicalTrials.gov (NCT01487083) A Long-Term Study in Schizophrenia. U.S. National Institutes of Health. | |||||
| REF 12 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018821) | |||||
| REF 13 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800034342) | |||||
| REF 14 | 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. (Ligand id: 1393). | |||||
| REF 15 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008428) | |||||
| REF 16 | ClinicalTrials.gov (NCT01184508) A Study in Migraine Prevention. U.S. National Institutes of Health. | |||||
| REF 17 | ClinicalTrials.gov (NCT00876304) Multiple Dose Safety Study of PF-04802540 in Subjects With Schizophrenia. U.S. National Institutes of Health. | |||||
| REF 18 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 19 | Novel glutamatergic drugs for the treatment of mood disorders. Neuropsychiatr Dis Treat. 2013; 9: 1101-1112. | |||||
| REF 20 | MGlu2 receptor-mediated modulation of conditioned avoidance behavior in rats. European journal of pharmacology. 01/2014; 727(1). | |||||
| REF 21 | Synthesis, in vitro pharmacology, structure-activity relationships, and pharmacokinetics of 3-alkoxy-2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent and selective group II metabotropic glutamate receptor antagonists. J Med Chem. 2004 Aug 26;47(18):4570-87. | |||||
| REF 22 | Metabotropic glutamate receptor subtype 2 (GRM2; MGLUR2); GRM3 (MGLUR3). SciBX 3(13); doi:10.1038/scibx.2010.413. April 1 2010 | |||||
| REF 23 | Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders. Nat Rev Drug Discov. 2014 Sep;13(9):692-708. | |||||
| REF 24 | Annual Reports in Medicinal Chemistry. Volume 47, 2012, Page(78). | |||||
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