| Tchem | Metabotropic glutamate receptor 2 |
L-glutamate is the major excitatory neurotransmitter in the central nervous system and activates both ionotropic and metabotropic glutamate receptors. Glutamatergic neurotransmission is involved in most aspects of normal brain function and can be perturbed in many neuropathologic conditions. The metabotropic glutamate receptors are a family of G protein-coupled receptors, that have been divided into 3 groups on the basis of sequence homology, putative signal transduction mechanisms, and pharmacologic properties. Group I includes GRM1 and GRM5 and these receptors have been shown to activate phospholipase C. Group II includes GRM2 and GRM3 while Group III includes GRM4, GRM6, GRM7 and GRM8. Group II and III receptors are linked to the inhibition of the cyclic AMP cascade but differ in their agonist selectivities. Several transcript variants encoding different isoforms have been found for this gene. [provided by RefSeq, Mar 2017]
Comments
Property Summary
| Ligand Count | 129 |
| NCBI Gene PubMed Count | 39 |
| PubMed Score | 612.27 |
| PubTator Score | 35.42 |
| Disease | Target Count | Z-score | Confidence |
|---|---|---|---|
| Schizophrenia | 1160 | 6.347 | 3.2 |
| Amphetamine-Related Disorders | 74 | 0.0 | 0.0 |
| Epilepsy, Temporal Lobe | 23 | 0.0 | 0.0 |
| Psychoses, Substance-Induced | 17 | 0.0 | 0.0 |
| Disease | Target Count |
|---|---|
| Alcoholic Intoxication, Chronic | 289 |
| Mood Disorders | 184 |
| addicted to cocaine | 4 |
| Disease | Target Count | P-value |
|---|---|---|
| glioblastoma | 5792 | 4.5e-10 |
| ependymoma | 4679 | 9.6e-09 |
| Astrocytoma, Pilocytic | 3081 | 2.2e-07 |
| pediatric high grade glioma | 1064 | 2.5e-07 |
| atypical teratoid / rhabdoid tumor | 5112 | 1.2e-05 |
| primitive neuroectodermal tumor | 3035 | 3.0e-03 |
| Disease | Target Count | Z-score | Confidence |
|---|---|---|---|
| Cocaine Dependence | 51 | 4.119 | 2.1 |
| Epilepsy | 792 | 3.844 | 1.9 |
| Major Depressive Disorder | 301 | 3.406 | 1.7 |
| Parkinson's disease | 392 | 3.374 | 1.7 |
| Toxic encephalopathy | 141 | 3.001 | 1.5 |
| Disease | log2 FC | p |
|---|---|---|
| Astrocytoma, Pilocytic | -1.400 | 2.2e-07 |
| atypical teratoid / rhabdoid tumor | -1.500 | 1.2e-05 |
| ependymoma | -1.100 | 9.6e-09 |
| glioblastoma | -1.100 | 4.5e-10 |
| pediatric high grade glioma | -1.300 | 2.5e-07 |
| primitive neuroectodermal tumor | -1.200 | 3.0e-03 |
CHEMBL593745
pEC50 7.00
CHEMBL608103
pEC50 7.00
CHEMBL604993
pEC50 7.00
CHEMBL322465
pEC50 7.00
CHEMBL3616850
pKi 7.02
CHEMBL364324
pEC50 7.03
CHEMBL3616852
pEC50 7.06
CHEMBL323541
pEC50 7.06
CHEMBL3765537
pEC50 7.07
CHEMBL325140
pKi 7.07
CHEMBL8759
pKi 7.07
CHEMBL3616849
pKi 7.07
CHEMBL1094763
pEC50 7.09
CHEMBL3764024
pEC50 7.09
CHEMBL3764820
pEC50 7.10
CHEMBL593744
pEC50 7.10
CHEMBL605836
pEC50 7.10
CHEMBL1774231
pEC50 7.12
CHEMBL3616859
pEC50 7.13
CHEMBL105065
pEC50 7.14
MGSLLALLALLLLWGAVAEGPAKKVLTLEGDLVLGGLFPVHQKGGPAEDCGPVNEHRGIQRLEAMLFALD 1 - 70 RINRDPHLLPGVRLGAHILDSCSKDTHALEQALDFVRASLSRGADGSRHICPDGSYATHGDAPTAITGVI 71 - 140 GGSYSDVSIQVANLLRLFQIPQISYASTSAKLSDKSRYDYFARTVPPDFFQAKAMAEILRFFNWTYVSTV 141 - 210 ASEGDYGETGIEAFELEARARNICVATSEKVGRAMSRAAFEGVVRALLQKPSARVAVLFTRSEDARELLA 211 - 280 ASQRLNASFTWVASDGWGALESVVAGSEGAAEGAITIELASYPISDFASYFQSLDPWNNSRNPWFREFWE 281 - 350 QRFRCSFRQRDCAAHSLRAVPFEQESKIMFVVNAVYAMAHALHNMHRALCPNTTRLCDAMRPVNGRRLYK 351 - 420 DFVLNVKFDAPFRPADTHNEVRFDRFGDGIGRYNIFTYLRAGSGRYRYQKVGYWAEGLTLDTSLIPWASP 421 - 490 SAGPLPASRCSEPCLQNEVKSVQPGEVCCWLCIPCQPYEYRLDEFTCADCGLGYWPNASLTGCFELPQEY 491 - 560 IRWGDAWAVGPVTIACLGALATLFVLGVFVRHNATPVVKASGRELCYILLGGVFLCYCMTFIFIAKPSTA 561 - 630 VCTLRRLGLGTAFSVCYSALLTKTNRIARIFGGAREGAQRPRFISPASQVAICLALISGQLLIVVAWLVV 631 - 700 EAPGTGKETAPERREVVTLRCNHRDASMLGSLAYNVLLIALCTLYAFKTRKCPENFNEAKFIGFTMYTTC 701 - 770 IIWLAFLPIFYVTSSDYRVQTTTMCVSVSLSGSVVLGCLFAPKLHIILFQPQKNVVSHRAPTSRFGSAAA 771 - 840 RASSSLGQGSGSQFVPTVCNGREVVDSTTSSL 841 - 872 //
