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GLASS

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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	QUISQUALIC ACID
Molecular formula	C5H7N3O5
IUPAC name	(2S)-2-amino-3-(3,5-dioxo-1,2,4-oxadiazolidin-2-yl)propanoic acid
Molecular weight	189.127
Hydrogen bond acceptor	6
Hydrogen bond donor	3
XlogP	-3.9
Synonyms	NCGC00024489-04 Quisqualate, L (2S)-2-amino-3-(3,5-dioxo-1,2,4-oxadiazolidin-2-yl)propanoic acid SR-01000075471-1 V0329 2or4 ACM52809071 C-52964 CTK4J6551 GTPL1372 LP01039 MLS001074741 PDSP1_000814 QUS (S)-2-amino-3-(3,5-dioxo-1,2,4-oxadiazolidin-2-yl)propanoic acid SR-01000597681-1 1mm7 809Q071 BCP13297 CCG-205116 DB02999 KB-60323 NCGC00024489-02 QC-11635 (+)-Quisqualic acid SMR000471890 1,2,4-Oxadiazolidine-2-propanoicacid, a-amino-3,5-dioxo-, (aS)- Tox21_501039 2-amino-3-(3,5-dioxo[1,2,4]oxadiazolidin-2-yl)propionic acid AC1ODZB5 beta-(3,5-Dioxo-1,2,4-oxadiazolidin-2-yl)-L-alanine FT-0604435 L-Quisqualic acid NCGC00024489-05 (2S)-2-amino-3-(3,5-dioxo-1,2,4-oxadiazolidin-2-yl)propanoic acid. SR-01000075471-5 ZINC897456 3-(3,5-Dioxo-1,2,4-oxadiazolidin-2-yl)-L-alanine AKOS024456826 C08296 D06DUE HMS2233G05 LS-175398 MolPort-003-939-212 PDSP2_000801 SCHEMBL13319908 (S)-2-AMINO-3-(3,5-DIOXO-[1,2,4]OXADIAZOLIDIN-2-YL)-PROPIONIC ACID ST50825297 1p1o 8OC22C1B99 BDBM17660 CHEBI:8734 EU-0101039 L(+)-alpha-Amino-3,5-dioxo-1,2,4-oxadiazolidine-2-propanoic acid NCGC00024489-03 Quisqualate (2S)-2-amino-3-(3,5-dioxo(1,2,4-oxadiazolidin-2-yl))propanoic acid SR-01000075471 UNII-8OC22C1B99 2jbk AC1Q6GK0 BN0434 CHEMBL279956 GTPL1370 Lopac0_001039 MFCD00069337 NCGC00261724-01 Quisqualic acid, powder (L)-(+)-?-Amino-3,5-dioxo-1,2,4-oxadiazolidine-2-propanoic acid SR-01000597681 1mm6 [3H]quisqualate 52809-07-1 ASNFTDCKZKHJSW-REOHCLBHSA-N C5H7N3O5 D0W6JO HMS3263O19 NCGC00024489-01 Q 2128 ()-Quisqualic Acid SCHEMBL136819 1,2,4-Oxadiazolidine-2-propanoic acid, alpha-amino-3,5-dioxo-, (S)- Tocris-0188 2-Amino-3-(3,5-dioxo-[1,2,4]oxadiazolidin-2-yl)-propionic acid(Quisqualic acid) AC1L23YS BDBM50164445 CHEMBL168279 FCH4012693 L-210 [ Show all ]
Inchi Key	ASNFTDCKZKHJSW-REOHCLBHSA-N
Inchi ID	InChI=1S/C5H7N3O5/c6-2(3(9)10)1-8-4(11)7-5(12)13-8/h2H,1,6H2,(H,9,10)(H,7,11,12)/t2-/m0/s1
PubChem CID	40539
ChEMBL	CHEMBL279956
IUPHAR	1372, 1370
BindingDB	17660
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	<500000.0 nM	PMID7738999	BindingDB,ChEMBL
Ki	<10000.0 nM	PMID9131252	BindingDB
Ki	112000.0 nM	PMID12109902	BindingDB,ChEMBL
Ki	1000000.0 nM	PMID10893301	BindingDB,ChEMBL
Ratio	593.0 -	PMID12109902	ChEMBL

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