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GLASS

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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	Dcg-IV
Molecular formula	C7H9NO6
IUPAC name	(1R,2R)-3-[(S)-amino(carboxy)methyl]cyclopropane-1,2-dicarboxylic acid
Molecular weight	203.15
Hydrogen bond acceptor	7
Hydrogen bond donor	4
XlogP	-4.3
Synonyms	1,2-Cyclopropanedicarboxylicacid, 3-[(S)-aminocarboxymethyl]-, (1R,2R)- AKOS030230932 D0Y1WV 147782-19-2 BDBM50034503 DCGIV (1r,2r)-3-[(S)-Amino(Carboxy)methyl]cyclopropane-1,2-Dicarboxylic Acid CS-0021174 SCHEMBL658075 1,2-Cyclopropanedicarboxylicacid,3-[(S)-aminocarboxymethyl]-,(1R,2R)- API0015797 DCG IV (1R,2R)-3-((S)-Amino-carboxy-methyl)-cyclopropane-1,2-dicarboxylic acid 2CG GTPL1377 (2S,2''R,3''R)-2-(2'',3'')-dicarboxycyclopropylglycine AC1NSJRH CTK0H7426 ZINC3995770 B5039 (1R,2R)-3-[(1S)-1-amino-2-hydroxy-2-oxoethyl]cyclopropane-1,2-dicarboxylic acid 3-(Amino-carboxy-methyl)-cyclopropane-1,2-dicarboxylic acid CHEMBL284193 MATPZHBYOVDBLI-JJYYJPOSSA-N [ Show all ]
Inchi Key	MATPZHBYOVDBLI-JJYYJPOSSA-N
Inchi ID	InChI=1S/C7H9NO6/c8-4(7(13)14)1-2(5(9)10)3(1)6(11)12/h1-4H,8H2,(H,9,10)(H,11,12)(H,13,14)/t2-,3-,4+/m1/s1
PubChem CID	5310979
ChEMBL	CHEMBL284193
IUPHAR	1377
BindingDB	50034503
DrugBank	N/A
Structure SDF download
Lipinski's druglikeness	This ligand satisfies Lipinski's rule of five.

Experimental Data

Parameter	Value	Reference	Database source
Activity	300.0 nM	PMID12166935	ChEMBL
EC50	45.0 nM	PMID20218620	BindingDB
EC50	300.0 nM	PMID7738999, PMID14711315	BindingDB
EC50	350.0 nM	PMID26814576	BindingDB
Ki	0.368 nM	PMID9832156	BindingDB
Ki	60.0 nM	PMID9463480	BindingDB
Ki	110.0 nM	PMID12109902	BindingDB,ChEMBL
Ki	300.0 nM	PMID9131252	BindingDB
Ki	316.228 nM	PMID10530814	IUPHAR
Ratio	0.35 -	PMID12109902	ChEMBL

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