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GLASS

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GPCR

Name	Metabotropic glutamate receptor 1
Species	Rattus norvegicus (Rat)
Gene	Grm1
Synonym	mGluR1 SCAR13 mGlu1 receptor metabotropic glutamate receptor 1 wobl GPRC1A glutamate receptor, metabotropic 1 glutamate receptor [ Show all ]
Disease	N/A for non-human GPCRs
Length	1199
Amino acid sequence	MVRLLLIFFPMIFLEMSILPRMPDRKVLLAGASSQRSVARMDGDVIIGALFSVHHQPPAEKVPERKCGEIREQYGIQRVEAMFHTLDKINADPVLLPNITLGSEIRDSCWHSSVALEQSIEFIRDSLISIRDEKDGLNRCLPDGQTLPPGRTKKPIAGVIGPGSSSVAIQVQNLLQLFDIPQIAYSATSIDLSDKTLYKYFLRVVPSDTLQARAMLDIVKRYNWTYVSAVHTEGNYGESGMDAFKELAAQEGLCIAHSDKIYSNAGEKSFDRLLRKLRERLPKARVVVCFCEGMTVRGLLSAMRRLGVVGEFSLIGSDGWADRDEVIEGYEVEANGGITIKLQSPEVRSFDDYFLKLRLDTNTRNPWFPEFWQHRFQCRLPGHLLENPNFKKVCTGNESLEENYVQDSKMGFVINAIYAMAHGLQNMHHALCPGHVGLCDAMKPIDGRKLLDFLIKSSFVGVSGEEVWFDEKGDAPGRYDIMNLQYTEANRYDYVHVGTWHEGVLNIDDYKIQMNKSGMVRSVCSEPCLKGQIKVIRKGEVSCCWICTACKENEFVQDEFTCRACDLGWWPNAELTGCEPIPVRYLEWSDIESIIAIAFSCLGILVTLFVTLIFVLYRDTPVVKSSSRELCYIILAGIFLGYVCPFTLIAKPTTTSCYLQRLLVGLSSAMCYSALVTKTNRIARILAGSKKKICTRKPRFMSAWAQVIIASILISVQLTLVVTLIIMEPPMPILSYPSIKEVYLICNTSNLGVVAPVGYNGLLIMSCTYYAFKTRNVPANFNEAKYIAFTMYTTCIIWLAFVPIYFGSNYKIITTCFAVSLSVTVALGCMFTPKMYIIIAKPERNVRSAFTTSDVVRMHVGDGKLPCRSNTFLNIFRRKKPGAGNANSNGKSVSWSEPGGRQAPKGQHVWQRLSVHVKTNETACNQTAVIKPLTKSYQGSGKSLTFSDASTKTLYNVEEEDNTPSAHFSPPSSPSMVVHRRGPPVATTPPLPPHLTAEETPLFLADSVIPKGLPPPLPQQQPQQPPPQQPPQQPKSLMDQLQGVVTNFGSGIPDFHAVLAGPGTPGNSLRSLYPPPPPPQHLQMLPLHLSTFQEESISPPGEDIDDDSERFKLLQEFVYEREGNTEEDELEEEEDLPTASKLTPEDSPALTPPSPFRDSVASGSSVPSSPVSESVLCTPPNVTYASVILRDYKQSSSTL
UniProt	P23385
Protein Data Bank	1iss, 1isr, 1ewk
GPCR-HGmod model	N/A
3D structure model	This structure is from PDB ID 1iss.
BioLiP	BL0023849, BL0023850,BL0023851, BL0011887,BL0011889, BL0011888,BL0011890
Therapeutic Target Database	N/A
ChEMBL	CHEMBL4477
IUPHAR	289
DrugBank	N/A

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	C-52964 CTK4J6551 GTPL1372 LP01039 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 CCG-205116 DB02999 KB-60323 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 FT-0604435 L-Quisqualic acid 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 C08296 D06DUE HMS2233G05 LS-175398 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 CHEBI:8734 EU-0101039 L(+)-alpha-Amino-3,5-dioxo-1,2,4-oxadiazolidine-2-propanoic acid 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 CHEMBL279956 GTPL1370 Lopac0_001039 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 C5H7N3O5 D0W6JO HMS3263O19 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 CHEMBL168279 FCH4012693 L-210 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 [ 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	200.0 nM	PMID7738999	ChEMBL
EC50	700.0 nM	PMID7738999	BindingDB,ChEMBL
EC50	750.0 nM	PMID7738999	BindingDB,ChEMBL
EC50	2500.0 nM	PMID7738999	BindingDB,ChEMBL
EC50	16400.0 nM	PMID7738999	BindingDB,ChEMBL
EC50 ratio	0.02 -	PMID10229625	ChEMBL
Kd	19.9526 - 31.6228 nM	PMID12695537, PMID12509432	IUPHAR
Ki	10.0 nM	PMID12109902	BindingDB,ChEMBL
Ki	10.0 - 31.6228 nM	PMID12695537, PMID11080213	IUPHAR

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