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GLASS

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GPCR

Name	Metabotropic glutamate receptor 3
Species	Homo sapiens (Human)
Gene	GRM3
Synonym	GPRC1C mGluR3 mGlu3 receptor glutamate receptor
Disease	Alzheimer disease; Major depressive disorder Anxiety disorder Schizophrenia
Length	879
Amino acid sequence	MKMLTRLQVLTLALFSKGFLLSLGDHNFLRREIKIEGDLVLGGLFPINEKGTGTEECGRINEDRGIQRLEAMLFAIDEINKDDYLLPGVKLGVHILDTCSRDTYALEQSLEFVRASLTKVDEAEYMCPDGSYAIQENIPLLIAGVIGGSYSSVSIQVANLLRLFQIPQISYASTSAKLSDKSRYDYFARTVPPDFYQAKAMAEILRFFNWTYVSTVASEGDYGETGIEAFEQEARLRNICIATAEKVGRSNIRKSYDSVIRELLQKPNARVVVLFMRSDDSRELIAAASRANASFTWVASDGWGAQESIIKGSEHVAYGAITLELASQPVRQFDRYFQSLNPYNNHRNPWFRDFWEQKFQCSLQNKRNHRRVCDKHLAIDSSNYEQESKIMFVVNAVYAMAHALHKMQRTLCPNTTKLCDAMKILDGKKLYKDYLLKINFTAPFNPNKDADSIVKFDTFGDGMGRYNVFNFQNVGGKYSYLKVGHWAETLSLDVNSIHWSRNSVPTSQCSDPCAPNEMKNMQPGDVCCWICIPCEPYEYLADEFTCMDCGSGQWPTADLTGCYDLPEDYIRWEDAWAIGPVTIACLGFMCTCMVVTVFIKHNNTPLVKASGRELCYILLFGVGLSYCMTFFFIAKPSPVICALRRLGLGSSFAICYSALLTKTNCIARIFDGVKNGAQRPKFISPSSQVFICLGLILVQIVMVSVWLILEAPGTRRYTLAEKRETVILKCNVKDSSMLISLTYDVILVILCTVYAFKTRKCPENFNEAKFIGFTMYTTCIIWLAFLPIFYVTSSDYRVQTTTMCISVSLSGFVVLGCLFAPKVHIILFQPQKNVVTHRLHLNRFSVSGTGTTYSQSSASTYVPTVCNGREVLDSTTSSL
UniProt	Q14832
Protein Data Bank	3sm9, 6b7h, 4xar, 5cnk, 5cnm
GPCR-HGmod model	N/A
3D structure model	This structure is from PDB ID 3sm9.
BioLiP	BL0324562, BL0307715, BL0204618, BL0324563, BL0412294, BL0412295, BL0324561
Therapeutic Target Database	T02719
ChEMBL	CHEMBL2888
IUPHAR	291
DrugBank	N/A

Ligand

Name	LY307452
Molecular formula	C21H25NO4
IUPAC name	(2S,4S)-2-amino-4-(4,4-diphenylbutyl)pentanedioic acid
Molecular weight	355.434
Hydrogen bond acceptor	5
Hydrogen bond donor	3
XlogP	1.4
Synonyms	(2S,4S)-2-amino-4-(4,4-diphenylbutyl)pentanedioic acid GTPL3350 AC1O44IF LY-307452 (2s,4s)-2-amino-4-(4,4-di-phenylbut-1-yl)-pentane-1,5-dioic acid CHEMBL39338 PDSP2_000256 2-Amino-4-(4,4-diphenyl-butyl)-pentanedioic acid LY 307452 BDBM50049748 (2S,4S)-2-Amino-4-(4,4-diphenyl-butyl)-pentanedioic acid D0OV2V SCHEMBL4257120 LY-307,452 PDSP1_000257 [ Show all ]
Inchi Key	DWLOVDOPFJPWNE-HKUYNNGSSA-N
Inchi ID	InChI=1S/C21H25NO4/c22-19(21(25)26)14-17(20(23)24)12-7-13-18(15-8-3-1-4-9-15)16-10-5-2-6-11-16/h1-6,8-11,17-19H,7,12-14,22H2,(H,23,24)(H,25,26)/t17-,19-/m0/s1
PubChem CID	6324634
ChEMBL	CHEMBL39338
IUPHAR	N/A
BindingDB	50049748
DrugBank	N/A
Structure SDF download
Lipinski's druglikeness	This ligand satisfies Lipinski's rule of five.

Experimental Data

Parameter	Value	Reference	Database source
IC50	30000.0 nM	PMID9873471, PMID9871538	BindingDB,ChEMBL
Ki	30000.0 nM	PMID10893301	BindingDB,ChEMBL

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