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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	201943-63-7
Molecular formula	C20H19NO5
IUPAC name	(1S,2S)-2-[(1S)-1-amino-1-carboxy-2-(9H-xanthen-9-yl)ethyl]cyclopropane-1-carboxylic acid
Molecular weight	353.374
Hydrogen bond acceptor	6
Hydrogen bond donor	3
XlogP	-0.2
Synonyms	HMS3267B15 LY341495 /LY-341495 W-5248 (1S,2S)-2-[(S)-1-Amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-cyclopropanecarboxylic acid 3794AH BDBM50062522 LY 341495 RL02516 (S)-2-[(S)-1-Amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-cyclopropanecarboxylic acid ABP000453 LY-341495 SR-01000597370 (1S,2S)-2-[(1S)-1-amino-1-carboxy-2-(9H-xanthen-9-yl)ethyl]cyclopropane-1-carboxylic acid 2-[1-Amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-cyclopropanecarboxylic acid(LY341495) BC638757 GTPL1378 HY-70059 MolPort-023-276-045 Z99 (1S,2S)-2-[1-Amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-cyclopropanecarboxylic acid BRD-K69763916-001-01-7 LY 341495;LY-341495 SB17024 (1S,2S)-2-((S)-1-amino-1-carboxy-2-(9H-xanthen-9-yl)ethyl)cyclopropane-1-carboxylic acid 2(S)-Amino-2-[2(S)-carboxy-1(S)-cyclopropyl]-3-(9H-xanthen-9-yl)propionic acid AKOS024456466 CHEMBL432038 GTPL1399 LY341495 SR-01000597370-1 (1S,2S)-2-[(1S)-1-amino-1-carboxy-2-(9H-xanthen-9-yl)ethyl]cyclopropanecarboxylic acid BCP9000885 J-501015 NCGC00025041-02 ZINC3826602 (2S)-2-AMINO-2-[(1S,2S)-2-CARBOXYCYCLOPROP-1-YL]-3-(XANTH-9-YL) PROPANOIC ACID 618093-20-2 CHEBI:93224 LY-341,495 SCHEMBL481153 (1S,2S)-2-((S)-1-amino-1-carboxy-2-(9H-xanthen-9-yl)ethyl)cyclopropanecarboxylic acid 2-[(1s,2s)-2-Carboxycyclopropyl]-3-(9h-Xanthen-9-Yl)-D-Alanine API0006790 CS-0343 [ Show all ]
Inchi Key	VLZBRVJVCCNPRJ-KPHUOKFYSA-N
Inchi ID	InChI=1S/C20H19NO5/c21-20(19(24)25,15-9-13(15)18(22)23)10-14-11-5-1-3-7-16(11)26-17-8-4-2-6-12(14)17/h1-8,13-15H,9-10,21H2,(H,22,23)(H,24,25)/t13-,15-,20-/m0/s1
PubChem CID	9819927
ChEMBL	CHEMBL432038
IUPHAR	N/A
BindingDB	50062522
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	10.0 nM	PMID9464367	BindingDB,ChEMBL
IC50	14.0 nM	PMID22318160	BindingDB,ChEMBL
Ki	14.0 nM	PMID10893301	BindingDB,ChEMBL

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