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GLASS

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GPCR

Name	Metabotropic glutamate receptor 8
Species	Homo sapiens (Human)
Gene	GRM8
Synonym	mGluR8b mGluR8 mGlu8 receptor Gprc1h glutamate receptor GLUR8 [ Show all ]
Disease	N/A
Length	908
Amino acid sequence	MVCEGKRSASCPCFFLLTAKFYWILTMMQRTHSQEYAHSIRVDGDIILGGLFPVHAKGERGVPCGELKKEKGIHRLEAMLYAIDQINKDPDLLSNITLGVRILDTCSRDTYALEQSLTFVQALIEKDASDVKCANGDPPIFTKPDKISGVIGAAASSVSIMVANILRLFKIPQISYASTAPELSDNTRYDFFSRVVPPDSYQAQAMVDIVTALGWNYVSTLASEGNYGESGVEAFTQISREIGGVCIAQSQKIPREPRPGEFEKIIKRLLETPNARAVIMFANEDDIRRILEAAKKLNQSGHFLWIGSDSWGSKIAPVYQQEEIAEGAVTILPKRASIDGFDRYFRSRTLANNRRNVWFAEFWEENFGCKLGSHGKRNSHIKKCTGLERIARDSSYEQEGKVQFVIDAVYSMAYALHNMHKDLCPGYIGLCPRMSTIDGKELLGYIRAVNFNGSAGTPVTFNENGDAPGRYDIFQYQITNKSTEYKVIGHWTNQLHLKVEDMQWAHREHTHPASVCSLPCKPGERKKTVKGVPCCWHCERCEGYNYQVDELSCELCPLDQRPNMNRTGCQLIPIIKLEWHSPWAVVPVFVAILGIIATTFVIVTFVRYNDTPIVRASGRELSYVLLTGIFLCYSITFLMIAAPDTIICSFRRVFLGLGMCFSYAALLTKTNRIHRIFEQGKKSVTAPKFISPASQLVITFSLISVQLLGVFVWFVVDPPHIIIDYGEQRTLDPEKARGVLKCDISDLSLICSLGYSILLMVTCTVYAIKTRGVPETFNEAKPIGFTMYTTCIIWLAFIPIFFGTAQSAEKMYIQTTTLTVSMSLSASVSLGMLYMPKVYIIIFHPEQNVQKRKRSFKAVVTAATMQSKLIQKGNDRPNGEVKSELCESLETNTSSTKTTYISYSNHSI
UniProt	O00222
Protein Data Bank	6bsz, 6bt5, 6e5v
GPCR-HGmod model	N/A
3D structure model	This structure is from PDB ID 6bsz.
BioLiP	BL0432251,BL0432252, BL0403876,BL0403877, BL0403874,BL0403875
Therapeutic Target Database	N/A
ChEMBL	CHEMBL3228
IUPHAR	296
DrugBank	BE0000835

Ligand

Name	(RS)-PPG
Molecular formula	C8H10NO5P
IUPAC name	2-amino-2-(4-phosphonophenyl)acetic acid
Molecular weight	231.144
Hydrogen bond acceptor	6
Hydrogen bond donor	4
XlogP	-3.7
Synonyms	(RS)PPG Amino-(4-phosphono-phenyl)-acetic acid D09AQK SCHEMBL9150881 (R,S)-4-phosphonophenylglycine 2-amino-2-(4-phosphonophenyl)acetic acid BN0429 J-004376 V2034 (RS)-4-Phosphonophenylglycine AC1ND7MS CHEMBL277475 NCGC00025051-02 120667-15-4 Amino-(4-phosphono-phenyl)-acetic acid(RS-PPG) GTPL1406 SR-01000597406 (R,S)-4-PPG C8H10NO5P L000025 AKOS015911887 CTK8F0597 RT-015313 BDBM50004881 I14-37803 SR-01000597406-1 (RS) PPG 667P154 MolPort-003-983-668 [ Show all ]
Inchi Key	JRQRKFDFHAPMGQ-UHFFFAOYSA-N
Inchi ID	InChI=1S/C8H10NO5P/c9-7(8(10)11)5-1-3-6(4-2-5)15(12,13)14/h1-4,7H,9H2,(H,10,11)(H2,12,13,14)
PubChem CID	4545574
ChEMBL	CHEMBL277475
IUPHAR	1406
BindingDB	50004881
DrugBank	N/A
Structure SDF download
Lipinski's druglikeness	This ligand satisfies Lipinski's rule of five.

Experimental Data

Parameter	Value	Reference	Database source
EC50	199.526 nM	PMID10336568, PMID10866390, PMID11166323	IUPHAR
Ki	210.0 nM	PMID10893301	BindingDB,ChEMBL

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