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GLASS

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GPCR

Name	Metabotropic glutamate receptor 3
Species	Rattus norvegicus (Rat)
Gene	Grm3
Synonym	mGluR3 mGlu3 receptor GPRC1C glutamate receptor
Disease	N/A for non-human GPCRs
Length	879
Amino acid sequence	MKMLTRLQILMLALFSKGFLLSLGDHNFMRREIKIEGDLVLGGLFPINEKGTGTEECGRINEDRGIQRLEAMLFAIDEINKDNYLLPGVKLGVHILDTCSRDTYALEQSLEFVRASLTKVDEAEYMCPDGSYAIQENIPLLIAGVIGGSYSSVSIQVANLLRLFQIPQISYASTSAKLSDKSRYDYFARTVPPDFYQAKAMAEILRFFNWTYVSTVASEGDYGETGIEAFEQEARLRNICIATAEKVGRSNIRKSYDSVIRELLQKPNARVVVLFMRSDDSRELIAAANRVNASFTWVASDGWGAQESIVKGSEHVAYGAITLELASHPVRQFDRYFQSLNPYNNHRNPWFRDFWEQKFQCSLQNKRNHRQVCDKHLAIDSSNYEQESKIMFVVNAVYAMAHALHKMQRTLCPNTTKLCDAMKILDGKKLYKEYLLKINFTAPFNPNKGADSIVKFDTFGDGMGRYNVFNLQQTGGKYSYLKVGHWAETLSLDVDSIHWSRNSVPTSQCSDPCAPNEMKNMQPGDVCCWICIPCEPYEYLVDEFTCMDCGPGQWPTADLSGCYNLPEDYIKWEDAWAIGPVTIACLGFLCTCIVITVFIKHNNTPLVKASGRELCYILLFGVSLSYCMTFFFIAKPSPVICALRRLGLGTSFAICYSALLTKTNCIARIFDGVKNGAQRPKFISPSSQVFICLGLILVQIVMVSVWLILETPGTRRYTLPEKRETVILKCNVKDSSMLISLTYDVVLVILCTVYAFKTRKCPENFNEAKFIGFTMYTTCIIWLAFLPIFYVTSSDYRVQTTTMCISVSLSGFVVLGCLFAPKVHIVLFQPQKNVVTHRLHLNRFSVSGTATTYSQSSASTYVPTVCNGREVLDSTTSSL
UniProt	P31422
Protein Data Bank	2e4u, 2e4v, 2e4w, 2e4x, 2e4y
GPCR-HGmod model	N/A
3D structure model	This structure is from PDB ID 2e4u.
BioLiP	BL0086116,BL0086117, BL0086120,BL0086121, BL0086118,BL0086119, BL0086114,BL0086115, BL0086112,BL0086113
Therapeutic Target Database	N/A
ChEMBL	CHEMBL3067
IUPHAR	291
DrugBank	N/A

Ligand

Name	CHEMBL3288680
Molecular formula	C26H18N4O
IUPAC name	8-isoquinolin-7-yl-4-methyl-2-phenylpyrazolo[1,5-a]quinazolin-5-one
Molecular weight	402.457
Hydrogen bond acceptor	3
Hydrogen bond donor	0
XlogP	4.8
Synonyms	BDBM50017665
Inchi Key	DUOKBXVNMNQTRT-UHFFFAOYSA-N
Inchi ID	InChI=1S/C26H18N4O/c1-29-25-15-23(18-5-3-2-4-6-18)28-30(25)24-14-20(9-10-22(24)26(29)31)19-8-7-17-11-12-27-16-21(17)13-19/h2-16H,1H3
PubChem CID	90643976
ChEMBL	CHEMBL3288680
IUPHAR	N/A
BindingDB	50017665
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	4510.0 nM	PMID24794112	BindingDB,ChEMBL

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