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GPCR

Name	Metabotropic glutamate receptor 4
Species	Homo sapiens (Human)
Gene	GRM4
Synonym	mGluR4 mGlu4 receptor GPRC1D glutamate receptor
Disease	Anxiety disorder Neurological disease
Length	912
Amino acid sequence	MPGKRGLGWWWARLPLCLLLSLYGPWMPSSLGKPKGHPHMNSIRIDGDITLGGLFPVHGRGSEGKPCGELKKEKGIHRLEAMLFALDRINNDPDLLPNITLGARILDTCSRDTHALEQSLTFVQALIEKDGTEVRCGSGGPPIITKPERVVGVIGASGSSVSIMVANILRLFKIPQISYASTAPDLSDNSRYDFFSRVVPSDTYQAQAMVDIVRALKWNYVSTVASEGSYGESGVEAFIQKSREDGGVCIAQSVKIPREPKAGEFDKIIRRLLETSNARAVIIFANEDDIRRVLEAARRANQTGHFFWMGSDSWGSKIAPVLHLEEVAEGAVTILPKRMSVRGFDRYFSSRTLDNNRRNIWFAEFWEDNFHCKLSRHALKKGSHVKKCTNRERIGQDSAYEQEGKVQFVIDAVYAMGHALHAMHRDLCPGRVGLCPRMDPVDGTQLLKYIRNVNFSGIAGNPVTFNENGDAPGRYDIYQYQLRNDSAEYKVIGSWTDHLHLRIERMHWPGSGQQLPRSICSLPCQPGERKKTVKGMPCCWHCEPCTGYQYQVDRYTCKTCPYDMRPTENRTGCRPIPIIKLEWGSPWAVLPLFLAVVGIAATLFVVITFVRYNDTPIVKASGRELSYVLLAGIFLCYATTFLMIAEPDLGTCSLRRIFLGLGMSISYAALLTKTNRIYRIFEQGKRSVSAPRFISPASQLAITFSLISLQLLGICVWFVVDPSHSVVDFQDQRTLDPRFARGVLKCDISDLSLICLLGYSMLLMVTCTVYAIKTRGVPETFNEAKPIGFTMYTTCIVWLAFIPIFFGTSQSADKLYIQTTTLTVSVSLSASVSLGMLYMPKVYIILFHPEQNVPKRKRSLKAVVTAATMSNKFTQKGNFRPNGEAKSELCENLEAPALATKQTYVTYTNHAI
UniProt	Q14833
Protein Data Bank	N/A
GPCR-HGmod model	N/A
3D structure model	No available structures or models
BioLiP	N/A
Therapeutic Target Database	T99402
ChEMBL	CHEMBL2736
IUPHAR	292
DrugBank	BE0000833

Ligand

Name	CHEMBL541754
Molecular formula	C13H10F2N2O2
IUPAC name	N-[3-(difluoromethoxy)phenyl]pyridine-2-carboxamide
Molecular weight	264.232
Hydrogen bond acceptor	5
Hydrogen bond donor	1
XlogP	2.9
Synonyms	N-(3-(difluoromethoxy)phenyl)picolinamide VU0361741-1 BDBM50293720 cid_44189740
Inchi Key	DVMQKRGCWAAYQR-UHFFFAOYSA-N
Inchi ID	InChI=1S/C13H10F2N2O2/c14-13(15)19-10-5-3-4-9(8-10)17-12(18)11-6-1-2-7-16-11/h1-8,13H,(H,17,18)
PubChem CID	44189740
ChEMBL	CHEMBL541754
IUPHAR	N/A
BindingDB	50293720
DrugBank	N/A
Structure SDF download
Lipinski's druglikeness	This ligand satisfies Lipinski's rule of five.

Experimental Data

Parameter	Value	Reference	Database source
EC50	336.0 nM	, PubChem BioAssay data set	BindingDB,ChEMBL
EC50	340.0 nM	PMID26231155, PMID19469556	BindingDB,ChEMBL
Emax	235.0 %	PMID19469556	ChEMBL
FC	27.8 -	PMID19469556	ChEMBL
IC50	4.571 nM	PMID26231155	ChEMBL
IC50	4.6 nM	PMID26231155	BindingDB,ChEMBL

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