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Name | Metabotropic glutamate receptor 2 |
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Species | Homo sapiens (Human) |
Gene | GRM2 |
Synonym | mGluR2 mGlu2 receptor metabotropic glutamate receptor 2 GPRC1B glutamate receptor |
Disease | Central nervous system disease Anxiety disorder Bipolar disorder Major depressive disorder Mood disorder [ Show all ] |
Length | 872 |
Amino acid sequence | MGSLLALLALLLLWGAVAEGPAKKVLTLEGDLVLGGLFPVHQKGGPAEDCGPVNEHRGIQRLEAMLFALDRINRDPHLLPGVRLGAHILDSCSKDTHALEQALDFVRASLSRGADGSRHICPDGSYATHGDAPTAITGVIGGSYSDVSIQVANLLRLFQIPQISYASTSAKLSDKSRYDYFARTVPPDFFQAKAMAEILRFFNWTYVSTVASEGDYGETGIEAFELEARARNICVATSEKVGRAMSRAAFEGVVRALLQKPSARVAVLFTRSEDARELLAASQRLNASFTWVASDGWGALESVVAGSEGAAEGAITIELASYPISDFASYFQSLDPWNNSRNPWFREFWEQRFRCSFRQRDCAAHSLRAVPFEQESKIMFVVNAVYAMAHALHNMHRALCPNTTRLCDAMRPVNGRRLYKDFVLNVKFDAPFRPADTHNEVRFDRFGDGIGRYNIFTYLRAGSGRYRYQKVGYWAEGLTLDTSLIPWASPSAGPLPASRCSEPCLQNEVKSVQPGEVCCWLCIPCQPYEYRLDEFTCADCGLGYWPNASLTGCFELPQEYIRWGDAWAVGPVTIACLGALATLFVLGVFVRHNATPVVKASGRELCYILLGGVFLCYCMTFIFIAKPSTAVCTLRRLGLGTAFSVCYSALLTKTNRIARIFGGAREGAQRPRFISPASQVAICLALISGQLLIVVAWLVVEAPGTGKETAPERREVVTLRCNHRDASMLGSLAYNVLLIALCTLYAFKTRKCPENFNEAKFIGFTMYTTCIIWLAFLPIFYVTSSDYRVQTTTMCVSVSLSGSVVLGCLFAPKLHIILFQPQKNVVSHRAPTSRFGSAAARASSSLGQGSGSQFVPTVCNGREVVDSTTSSL |
UniProt | Q14416 |
Protein Data Bank | 5cnj, 5kzn, 5kzq, 5cni, 4xas, 4xaq |
GPCR-HGmod model | N/A |
3D structure model | This structure is from PDB ID 5cnj. |
BioLiP | BL0365442, BL0324559,BL0324560, BL0324557,BL0324558, BL0306697,BL0306698, BL0306695,BL0306696, BL0365443 |
Therapeutic Target Database | T62820 |
ChEMBL | CHEMBL5137 |
IUPHAR | 290 |
DrugBank | N/A |
Name | MGS-0028 |
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Molecular formula | C8H8FNO5 |
IUPAC name | (1R,2S,5S,6S)-2-amino-6-fluoro-4-oxobicyclo[3.1.0]hexane-2,6-dicarboxylic acid |
Molecular weight | 217.152 |
Hydrogen bond acceptor | 7 |
Hydrogen bond donor | 3 |
XlogP | -4.2 |
Synonyms | MGS 0028 (+)-2-Amino-6-fluoro-4-oxo-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid 321963-33-1 SCHEMBL2454643 (-)-2-Amino-6-fluoro-4-oxo-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid [ Show all ] |
Inchi Key | KFAGJPNFERWZJA-JKBXLQNXSA-N |
Inchi ID | InChI=1S/C8H8FNO5/c9-8(6(14)15)3-2(11)1-7(10,4(3)8)5(12)13/h3-4H,1,10H2,(H,12,13)(H,14,15)/t3-,4-,7+,8-/m1/s1 |
PubChem CID | 9837317 |
ChEMBL | CHEMBL121053 |
IUPHAR | 1395 |
BindingDB | 50094843 |
DrugBank | N/A |
Structure | |
Lipinski's druglikeness | This ligand satisfies Lipinski's rule of five. |
Parameter | Value | Reference | Database source |
---|---|---|---|
Activity | 0.57 nM | PMID12166935 | ChEMBL |
EC50 | <100000.0 nM | PMID11123999 | BindingDB |
EC50 | 0.57 nM | PMID11123999, PMID22318160 | BindingDB,ChEMBL |
EC50 | 1.26 nM | PMID11123999 | BindingDB |
EC50 | 94.7 nM | PMID11123999 | BindingDB |
Ki | 3.3 nM | PMID11123999 | BindingDB |
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