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GLASS

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GPCR

Name	Metabotropic glutamate receptor 4
Species	Rattus norvegicus (Rat)
Gene	Grm4
Synonym	glutamate receptor GPRC1D mGlu4 receptor mGluR4
Disease	N/A for non-human GPCRs
Length	912
Amino acid sequence	MSGKGGWAWWWARLPLCLLLSLYAPWVPSSLGKPKGHPHMNSIRIDGDITLGGLFPVHGRGSEGKACGELKKEKGIHRLEAMLFALDRINNDPDLLPNITLGARILDTCSRDTHALEQSLTFVQALIEKDGTEVRCGSGGPPIITKPERVVGVIGASGSSVSIMVANILRLFKIPQISYASTAPDLSDNSRYDFFSRVVPSDTYQAQAMVDIVRALKWNYVSTLASEGSYGESGVEAFIQKSRENGGVCIAQSVKIPREPKTGEFDKIIKRLLETSNARGIIIFANEDDIRRVLEAARRANQTGHFFWMGSDSWGSKSAPVLRLEEVAEGAVTILPKRMSVRGFDRYFSSRTLDNNRRNIWFAEFWEDNFHCKLSRHALKKGSHIKKCTNRERIGQDSAYEQEGKVQFVIDAVYAMGHALHAMHRDLCPGRVGLCPRMDPVDGTQLLKYIRNVNFSGIAGNPVTFNENGDAPGRYDIYQYQLRNGSAEYKVIGSWTDHLHLRIERMQWPGSGQQLPRSICSLPCQPGERKKTVKGMACCWHCEPCTGYQYQVDRYTCKTCPYDMRPTENRTSCQPIPIVKLEWDSPWAVLPLFLAVVGIAATLFVVVTFVRYNDTPIVKASGRELSYVLLAGIFLCYATTFLMIAEPDLGTCSLRRIFLGLGMSISYAALLTKTNRIYRIFEQGKRSVSAPRFISPASQLAITFILISLQLLGICVWFVVDPSHSVVDFQDQRTLDPRFARGVLKCDISDLSLICLLGYSMLLMVTCTVYAIKTRGVPETFNEAKPIGFTMYTTCIVWLAFIPIFFGTSQSADKLYIQTTTLTVSVSLSASVSLGMLYMPKVYIILFHPEQNVPKRKRSLKAVVTAATMSNKFTQKGNFRPNGEAKSELCENLETPALATKQTYVTYTNHAI
UniProt	P31423
Protein Data Bank	N/A
GPCR-HGmod model	N/A
3D structure model	No available structures or models
BioLiP	N/A
Therapeutic Target Database	N/A
ChEMBL	CHEMBL2787
IUPHAR	292
DrugBank	N/A

Ligand

Name	CHEMBL3357574
Molecular formula	C20H11ClFN3O3
IUPAC name	N-[3-chloro-4-(4-fluoro-1,3-dioxoisoindol-2-yl)phenyl]pyridine-2-carboxamide
Molecular weight	395.774
Hydrogen bond acceptor	5
Hydrogen bond donor	1
XlogP	3.3
Synonyms	SCHEMBL1975043 BDBM50031312 N-[3-Chloro-4-(4-fluoro-1,3-dioxo-1,3-dihydro-2H-isoindole-2-yl)phenyl]-2-pyridinecarboxamide
Inchi Key	HDLABPAQQVOWQC-UHFFFAOYSA-N
Inchi ID	InChI=1S/C20H11ClFN3O3/c21-13-10-11(24-18(26)15-6-1-2-9-23-15)7-8-16(13)25-19(27)12-4-3-5-14(22)17(12)20(25)28/h1-10H,(H,24,26)
PubChem CID	45110133
ChEMBL	CHEMBL3357574
IUPHAR	N/A
BindingDB	50031312
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	5.1 nM	PMID25330258	BindingDB,ChEMBL
IC50	5.129 nM	PMID25330258	ChEMBL
Inhibition	99.4 %	PMID25330258	ChEMBL

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