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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	(2S,1'S,2'S)-2-(carboxycyclopropyl)glycine
Molecular formula	C6H9NO4
IUPAC name	(1S,2S)-2-[(S)-amino(carboxy)methyl]cyclopropane-1-carboxylic acid
Molecular weight	159.141
Hydrogen bond acceptor	5
Hydrogen bond donor	3
XlogP	-3.4
Synonyms	(1S,2S)-2-[(1S)-1-amino-2-hydroxy-2-oxoethyl]cyclopropane-1-carboxylic acid 2S,1'S,2'S)-2-(Carboxycyclopropyl)Glycine CCG-204469 HMS3261K09 LP00374 SR-01000075799 (2S,3S,4S)-CCG AC1NSJQB CHEMBL280563 L-CCG-1 NCGC00024541-03 ZINC2568218 (1S,2S)-2-((S)-Amino(carboxy)methyl)cyclopropanecarboxylic acid 2-(Amino-carboxy-methyl)-cyclopropanecarboxylic acid BDBM50034504 EU-0100374 L-CCGI NCGC00261059-01 (2S,1 inverted exclamation markaS,2 inverted exclamation markaS)-2-(Carboxycyclopropyl)glycine 3,4-Cyclopropylglutamate CCPG J-003677 MolPort-003-940-678 SR-01000075799-1 117857-93-9 AKOS006275493 Cyclopropaneacetic acid, alpha-amino-2-carboxy-, (alphaS,1S,2S)- L-Ccg-I NCGC00024541-04 (1S,2S)-2-((S)-Amino-carboxy-methyl)-cyclopropanecarboxylic acid 2-(Amino-carboxy-methyl)-cyclopropanecarboxylic acid(2S,3S,4S-CCG) C-237 GTPL1368 Lopac0_000374 SCHEMBL664330 L-2-(Carboxypropyl)glycine NCGC00024541-02 Tox21_500374 B6264 D0Z7CZ L-CCG-l NCGC00024541-05 [ Show all ]
Inchi Key	GZOVEPYOCJWRFC-HZLVTQRSSA-N
Inchi ID	InChI=1S/C6H9NO4/c7-4(6(10)11)2-1-3(2)5(8)9/h2-4H,1,7H2,(H,8,9)(H,10,11)/t2-,3-,4-/m0/s1
PubChem CID	5310956
ChEMBL	CHEMBL280563
IUPHAR	1368
BindingDB	50034504
DrugBank	N/A
Structure SDF download
Lipinski's druglikeness	This ligand satisfies Lipinski's rule of five.

Experimental Data

Parameter	Value	Reference	Database source
Activity	600.0 nM	PMID12166935	ChEMBL
Ki	39.8107 nM	PMID10530814	IUPHAR
Ki	440.0 nM	PMID10893301	BindingDB,ChEMBL
Ki	1000.0 nM	PMID9131252	BindingDB

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