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GPCR

Name	Metabotropic glutamate receptor 4
Species	Homo sapiens (Human)
Gene	GRM4
Synonym	mGluR4 mGlu4 receptor GPRC1D glutamate receptor
Disease	Anxiety disorder Neurological disease
Length	912
Amino acid sequence	MPGKRGLGWWWARLPLCLLLSLYGPWMPSSLGKPKGHPHMNSIRIDGDITLGGLFPVHGRGSEGKPCGELKKEKGIHRLEAMLFALDRINNDPDLLPNITLGARILDTCSRDTHALEQSLTFVQALIEKDGTEVRCGSGGPPIITKPERVVGVIGASGSSVSIMVANILRLFKIPQISYASTAPDLSDNSRYDFFSRVVPSDTYQAQAMVDIVRALKWNYVSTVASEGSYGESGVEAFIQKSREDGGVCIAQSVKIPREPKAGEFDKIIRRLLETSNARAVIIFANEDDIRRVLEAARRANQTGHFFWMGSDSWGSKIAPVLHLEEVAEGAVTILPKRMSVRGFDRYFSSRTLDNNRRNIWFAEFWEDNFHCKLSRHALKKGSHVKKCTNRERIGQDSAYEQEGKVQFVIDAVYAMGHALHAMHRDLCPGRVGLCPRMDPVDGTQLLKYIRNVNFSGIAGNPVTFNENGDAPGRYDIYQYQLRNDSAEYKVIGSWTDHLHLRIERMHWPGSGQQLPRSICSLPCQPGERKKTVKGMPCCWHCEPCTGYQYQVDRYTCKTCPYDMRPTENRTGCRPIPIIKLEWGSPWAVLPLFLAVVGIAATLFVVITFVRYNDTPIVKASGRELSYVLLAGIFLCYATTFLMIAEPDLGTCSLRRIFLGLGMSISYAALLTKTNRIYRIFEQGKRSVSAPRFISPASQLAITFSLISLQLLGICVWFVVDPSHSVVDFQDQRTLDPRFARGVLKCDISDLSLICLLGYSMLLMVTCTVYAIKTRGVPETFNEAKPIGFTMYTTCIVWLAFIPIFFGTSQSADKLYIQTTTLTVSVSLSASVSLGMLYMPKVYIILFHPEQNVPKRKRSLKAVVTAATMSNKFTQKGNFRPNGEAKSELCENLEAPALATKQTYVTYTNHAI
UniProt	Q14833
Protein Data Bank	N/A
GPCR-HGmod model	N/A
3D structure model	No available structures or models
BioLiP	N/A
Therapeutic Target Database	T99402
ChEMBL	CHEMBL2736
IUPHAR	292
DrugBank	BE0000833

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	CHEMBL33567 GTPL1410 L-(+)-2-Amino-4-phosphonobutyric acid, optical purity optical purity: >=95% (HPLC, Marfey's reagent) M01257 NCI30079 Tocris-0103 B6200 D0H7UP J-014961 L-2-amino-4-phosphonobutiric acid NCGC00013365 NSC-30079 [3H]AP4 (2S)-2-amino-4-phosphonobutanoic acid 23052-81-5 BN0084 CCG-37553 FCH919870 L-(+)-2-Amino-4-phosphono-butanoic acid L-APB NCGC00024468-01 SR-01000597692 (S)-2-amino-4-phosphonobutanoic acid ACM23052815 CS-0020419 GTPL1412 L-1-amino-4-phosphonobutanoic acid MFCD00083244 NCIStruc1_000162 UNII-H8B59H10OK component DDOQBQRIEWHWBT-VKHMYHEASA-N 2-Amino-3-(3,5-dioxo-[1,2,4]oxadiazolidin-2-yl)-propionic acid B6202 Butanoic acid,2-amino-4-phosphono-,(2S)- D0PN6Z l(+)-2-amino-4-phosphonobutanoic acid L-AP-4 NCGC00013365-02 S-2-amino-4-phosphonobutyrate (2S)-2-amino-4-phosphonobutanoic acid. FT-0689296 L-(+)-2-Amino-4-phosphonobutyric acid LS-46098 NCGC00024468-02 SR-01000597692-1 AKOS006239562 D08PBE HY-100781A L-150 MolPort-002-514-399 NCIStruc2_000128 ZINC2033983 2-Amino-4-phosphono-butyric acid(S-AP4) BDBM50007548 C-55169 E7P L(+)-2-Amino-4-phosphonobutanoic acid (L-AP4) NCGC00013365-03 SCHEMBL1969235 (S)-2-Amino-4-phosphono-butyric acid AC1L456H [ 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	1412, 1410
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	200.0 nM	PMID7738999	BindingDB,ChEMBL
EC50	320.0 nM	PMID9473604	IUPHAR
EC50	500.0 nM	PMID10888329	BindingDB,ChEMBL
EC50	690.0 nM	PMID17602546	BindingDB,ChEMBL
Ki	160.0 nM	PMID19042134	BindingDB,ChEMBL
Ki	470.0 nM	PMID12109902	BindingDB,ChEMBL
Ki	910.0 nM	PMID10893301	BindingDB,ChEMBL
Ratio	0.58 -	PMID12109902	ChEMBL

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