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GPCR

Name	Metabotropic glutamate receptor 2
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 Psychiatric disorder Schizophrenia Alzheimer disease; Major depressive 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

Ligand

Name	SCHEMBL11235794
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 SDF download
Lipinski's druglikeness	Partition coefficient log P of this ligand is not available.

Experimental Data

Parameter	Value	Reference	Database source
Activity	4000.0 nM	PMID12166935	ChEMBL
EC50	290.0 nM	PMID9572889	ChEMBL
EC50	1767.0 nM	PMID26313429	BindingDB,ChEMBL
EC50	1800.0 nM	MedChemComm, (2011) 2:11:1120, PMID26814576	BindingDB,ChEMBL
EC50	1820.0 nM	PMID26814576	BindingDB
EC50	1827.0 nM	PMID26313429	BindingDB,ChEMBL
EC50	2351.0 nM	PMID26313429	BindingDB,ChEMBL
EC50	2575.0 nM	PMID26313429	BindingDB,ChEMBL
EC50	3981.07 - 19952.6 nM	PMID10443583	IUPHAR
EC50	4700.0 nM	PMID7738999	BindingDB,ChEMBL
EC50	7400.0 nM	PMID11720869	BindingDB,ChEMBL
EC50	8500.0 nM	PMID8759641	BindingDB,ChEMBL
EC50	11800.0 nM	PMID7738999	BindingDB
EC50	12589.2 nM	PMID21232953	ChEMBL
EC50	13080.0 nM	PMID26814576	BindingDB
EC50	16090.0 nM	PMID26814576	BindingDB
EC50	26000.0 nM	PMID16213710, PMID17350267	BindingDB,ChEMBL
Emax	88.0 %	PMID26313429	ChEMBL
Emax	91.0 %	PMID26313429	ChEMBL
Emax	93.0 %	PMID26313429	ChEMBL
Emax	94.0 %	PMID26313429	ChEMBL
Ki	<10000.0 nM	PMID8863838	BindingDB
Ki	1100.0 nM	PMID9463480	BindingDB
Ki	1200.0 nM	PMID12109902	ChEMBL
Ki	1258.93 nM	PMID12649361	BindingDB
Ki	1819.7 nM	MedChemComm, (2011) 2:11:1120	ChEMBL
Ki	4000.0 nM	PMID9131252	BindingDB
Ki	4400.0 nM	PMID9696422	BindingDB
Ki	6400.0 nM	PMID19042134	BindingDB,ChEMBL
Ki	11000.0 nM	PMID17725337	BindingDB,ChEMBL
Ki	12000.0 nM	PMID10893301	BindingDB,ChEMBL
Ki	12589.3 nM	PMID10530814	IUPHAR
Ratio	5.9 -	PMID12109902	ChEMBL