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Name | Metabotropic glutamate receptor 1 |
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Species | Homo sapiens (Human) |
Gene | GRM1 |
Synonym | SCAR13 MGLUR1 mGlu1 receptor metabotropic glutamate receptor 1 GPRC1A [ Show all ] |
Disease | Alzheimer disease; Huntington's disease Neurological disease Neuropathic pain Schizophrenia Pain |
Length | 1194 |
Amino acid sequence | MVGLLLFFFPAIFLEVSLLPRSPGRKVLLAGASSQRSVARMDGDVIIGALFSVHHQPPAEKVPERKCGEIREQYGIQRVEAMFHTLDKINADPVLLPNITLGSEIRDSCWHSSVALEQSIEFIRDSLISIRDEKDGINRCLPDGQSLPPGRTKKPIAGVIGPGSSSVAIQVQNLLQLFDIPQIAYSATSIDLSDKTLYKYFLRVVPSDTLQARAMLDIVKRYNWTYVSAVHTEGNYGESGMDAFKELAAQEGLCIAHSDKIYSNAGEKSFDRLLRKLRERLPKARVVVCFCEGMTVRGLLSAMRRLGVVGEFSLIGSDGWADRDEVIEGYEVEANGGITIKLQSPEVRSFDDYFLKLRLDTNTRNPWFPEFWQHRFQCRLPGHLLENPNFKRICTGNESLEENYVQDSKMGFVINAIYAMAHGLQNMHHALCPGHVGLCDAMKPIDGSKLLDFLIKSSFIGVSGEEVWFDEKGDAPGRYDIMNLQYTEANRYDYVHVGTWHEGVLNIDDYKIQMNKSGVVRSVCSEPCLKGQIKVIRKGEVSCCWICTACKENEYVQDEFTCKACDLGWWPNADLTGCEPIPVRYLEWSNIESIIAIAFSCLGILVTLFVTLIFVLYRDTPVVKSSSRELCYIILAGIFLGYVCPFTLIAKPTTTSCYLQRLLVGLSSAMCYSALVTKTNRIARILAGSKKKICTRKPRFMSAWAQVIIASILISVQLTLVVTLIIMEPPMPILSYPSIKEVYLICNTSNLGVVAPLGYNGLLIMSCTYYAFKTRNVPANFNEAKYIAFTMYTTCIIWLAFVPIYFGSNYKIITTCFAVSLSVTVALGCMFTPKMYIIIAKPERNVRSAFTTSDVVRMHVGDGKLPCRSNTFLNIFRRKKAGAGNANSNGKSVSWSEPGGGQVPKGQHMWHRLSVHVKTNETACNQTAVIKPLTKSYQGSGKSLTFSDTSTKTLYNVEEEEDAQPIRFSPPGSPSMVVHRRVPSAATTPPLPSHLTAEETPLFLAEPALPKGLPPPLQQQQQPPPQQKSLMDQLQGVVSNFSTAIPDFHAVLAGPGGPGNGLRSLYPPPPPPQHLQMLPLQLSTFGEELVSPPADDDDDSERFKLLQEYVYEHEREGNTEEDELEEEEEDLQAASKLTPDDSPALTPPSPFRDSVASGSSVPSSPVSESVLCTPPNVSYASVILRDYKQSSSTL |
UniProt | Q13255 |
Protein Data Bank | 4or2, 3ks9 |
GPCR-HGmod model | N/A |
3D structure model | This structure is from PDB ID 4or2. |
BioLiP | BL0271871,BL0271876, BL0271872,BL0271873,BL0271874,, BL0174211,BL0174213, BL0174210,BL0174212 |
Therapeutic Target Database | T27137 |
ChEMBL | CHEMBL3772 |
IUPHAR | 289 |
DrugBank | BE0000824 |
Name | SCHEMBL11235794 |
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Molecular formula | C5H9NO4 |
IUPAC name | (2S)-2-amino-5-hydroxy-5-oxopentanoate;hydron |
Molecular weight | 147.13 |
Hydrogen bond acceptor | 5 |
Hydrogen bond donor | 3 |
XlogP | None |
Synonyms | N/A |
Inchi Key | WHUUTDBJXJRKMK-VKHMYHEASA-N |
Inchi ID | InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 |
PubChem CID | 88747398 |
ChEMBL | CHEMBL575060 |
IUPHAR | 1369 |
BindingDB | 17657 |
DrugBank | DB00142 |
Structure | |
Lipinski's druglikeness | Partition coefficient log P of this ligand is not available. |
Parameter | Value | Reference | Database source |
---|---|---|---|
N/A | N/A | DrugBank | |
Activity | 1000.0 nM | PMID12166935 | ChEMBL |
EC50 | 1050.0 nM | PMID10673095 | BindingDB,ChEMBL |
EC50 | 1600.0 nM | MedChemComm, (2011) 2:11:1120 | ChEMBL |
EC50 | 4900.0 nM | PMID9572889 | ChEMBL |
EC50 | 10000.0 - 15848.9 nM | PMID10443583 | IUPHAR |
EC50 | 19000.0 nM | PMID8759641 | BindingDB,ChEMBL |
EC50 | 156000.0 nM | PMID7738999 | BindingDB,ChEMBL |
Ki | 250.0 nM | PMID17725337 | BindingDB,ChEMBL |
Ki | 570.0 nM | PMID19042134 | BindingDB,ChEMBL |
Ki | 1584.89 nM | MedChemComm, (2011) 2:11:1120 | ChEMBL |
Ki | 9000.0 nM | PMID9131252 | BindingDB |
Ki | 10000.0 nM | PMID10893301 | BindingDB,ChEMBL |
Ratio | 1.0 - | PMID12109902 | ChEMBL |
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