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GLASS

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GPCR

Name	Metabotropic glutamate receptor 8
Species	Rattus norvegicus (Rat)
Gene	Grm8
Synonym	GLUR8 glutamate receptor Gprc1h mGlu8 receptor mGluR8 mGluR8b [ Show all ]
Disease	N/A for non-human GPCRs
Length	908
Amino acid sequence	MVCEGKRLASCPCFFLLTAKFYWILTMMQRTHSQEYAHSIRVDGDIILGGLFPVHAKGERGVPCGELKKEKGIHRLEAMLYAIDQINKDPDLLSNITLGVRILDTCSRDTYALEQSLTFVQALIEKDASDVKCANGDPPIFTKPDKISGVIGAAASSVSIMVANILRLFKIPQISYASTAPELSDNTRYDFFSRVVPPDSYQAQAMVDIVTALGWNYVSTLASEGNYGESGVEAFTQISREIGGVCIAQSQKIPREPRPGEFEKIIKRLLETPNARAVIMFANEDDIRRILEAAKKLNQSGHFLWIGSDSWGSKIAPVYQQEEIAEGAVTILPKRASIDGFDRYFRSRTLANNRRNVWFAEFWEENFGCKLGSHGKRNSHIKKCTGLERIARDSSYEQEGKVQFVIDAVYSMAYALHNMHKERCPGYIGLCPRMVTIDGKELLGYIRAVNFNGSAGTPVTFNENGDAPGRYDIFQYQINNKSTEYKIIGHWTNQLHLKVEDMQWANREHTHPASVCSLPCKPGERKKTVKGVPCCWHCERCEGYNYQVDELSCELCPLDQRPNINRTGCQRIPIIKLEWHSPWAVVPVFIAILGIIATTFVIVTFVRYNDTPIVRASGRELSYVLLTGIFLCYSITFLMIAAPDTIICSFRRIFLGLGMCFSYAALLTKTNRIHRIFEQGKKSVTAPKFISPASQLVITFSLISVQLLGVFVWFVVDPPHTIIDYGEQRTLDPENARGVLKCDISDLSLICSLGYSILLMVTCTVYAIKTRGVPETFNEAKPIGFTMYTTCIIWLAFIPIFFGTAQSAEKMYIQTTTLTVSMSLSASVSLGMLYMPKVYIIIFHPEQNVQKRKRSFKAVVTAATMQSKLIQKGNDRPNGEVKSELCESLETNTSSTKTTYISYSNHSI
UniProt	P70579
Protein Data Bank	N/A
GPCR-HGmod model	N/A
3D structure model	No available structures or models
BioLiP	N/A
Therapeutic Target Database	N/A
ChEMBL	CHEMBL2718
IUPHAR	296
DrugBank	N/A

Ligand

Name	L-AP4
Molecular formula	C4H10NO5P
IUPAC name	(2S)-2-amino-4-phosphonobutanoic acid
Molecular weight	183.1
Hydrogen bond acceptor	6
Hydrogen bond donor	4
XlogP	-5.5
Synonyms	(2S)-2-amino-4-phosphonobutanoic acid 23052-81-5 BN0084 D0H7UP J-014961 L-2-amino-4-phosphonobutiric acid NCGC00013365 NSC-30079 [3H]AP4 (S)-2-amino-4-phosphonobutanoic acid ACM23052815 CCG-37553 FCH919870 L-(+)-2-Amino-4-phosphono-butanoic acid L-APB NCGC00024468-01 SR-01000597692 2-Amino-3-(3,5-dioxo-[1,2,4]oxadiazolidin-2-yl)-propionic acid B6202 CS-0020419 GTPL1412 L-1-amino-4-phosphonobutanoic acid MFCD00083244 NCIStruc1_000162 UNII-H8B59H10OK component DDOQBQRIEWHWBT-VKHMYHEASA-N (2S)-2-amino-4-phosphonobutanoic acid. Butanoic acid,2-amino-4-phosphono-,(2S)- D0PN6Z l(+)-2-amino-4-phosphonobutanoic acid L-AP-4 NCGC00013365-02 S-2-amino-4-phosphonobutyrate AKOS006239562 FT-0689296 L-(+)-2-Amino-4-phosphonobutyric acid LS-46098 NCGC00024468-02 SR-01000597692-1 2-Amino-4-phosphono-butyric acid(S-AP4) BDBM50007548 D08PBE HY-100781A L-150 MolPort-002-514-399 NCIStruc2_000128 ZINC2033983 (S)-2-Amino-4-phosphono-butyric acid AC1L456H C-55169 E7P L(+)-2-Amino-4-phosphonobutanoic acid (L-AP4) NCGC00013365-03 SCHEMBL1969235 B6200 CHEMBL33567 GTPL1410 L-(+)-2-Amino-4-phosphonobutyric acid, optical purity optical purity: >=95% (HPLC, Marfey's reagent) M01257 NCI30079 Tocris-0103 [ Show all ]
Inchi Key	DDOQBQRIEWHWBT-VKHMYHEASA-N
Inchi ID	InChI=1S/C4H10NO5P/c5-3(4(6)7)1-2-11(8,9)10/h3H,1-2,5H2,(H,6,7)(H2,8,9,10)/t3-/m0/s1
PubChem CID	179394
ChEMBL	CHEMBL33567
IUPHAR	1410, 1412
BindingDB	50007548
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	60.0 nM	PMID14711315	BindingDB,ChEMBL
EC50	70.0 nM	PMID26814576	BindingDB,ChEMBL
EC50	110.0 nM	PMID25958247	BindingDB,ChEMBL
EC50	128.0 nM	PMID17722902	BindingDB,ChEMBL
EC50	240.0 nM	PMID20218620	BindingDB,ChEMBL
EC50	300.0 nM	PMID20218620	BindingDB,ChEMBL
EC50	630.957 nM	PMID9016353	IUPHAR
Ki	1900.0 nM	PMID17350267, PMID16213710	BindingDB,ChEMBL
Ki	2700.0 nM	PMID11114395	BindingDB

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