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GLASS

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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	CHEMBL1830707
Molecular formula	C14H13N5S
IUPAC name	N-pyridin-2-yl-5-thia-3,11,12-triazatricyclo[8.3.0.02,6]trideca-1(10),2(6),3,12-tetraen-4-amine
Molecular weight	283.353
Hydrogen bond acceptor	5
Hydrogen bond donor	2
XlogP	2.8
Synonyms	AKOS024458120 MolPort-023-277-166 SCHEMBL369389 D00NCL BDBM50353290 N-(pyridin-2-yl)-5-thia-3,11,12-triazatricyclo[8.3.0.0^{2,6}]trideca-1(13),2(6),3,10-tetraen-4-amine 1314140-00-5 compound 22a TC-N 22A GTPL6231 NCGC00371008-01 4,5,6,8-Tetrahydro-N-2-pyridinylpyrazolo[3',4':6,7]cyclohepta[1,2]thiazol-2-amine compound 22a [PMID: 21688779] ZINC72118775 [ Show all ]
Inchi Key	DBISXWCOHGUFSF-UHFFFAOYSA-N
Inchi ID	InChI=1S/C14H13N5S/c1-2-7-15-12(6-1)17-14-18-13-9-8-16-19-10(9)4-3-5-11(13)20-14/h1-2,6-8H,3-5H2,(H,16,19)(H,15,17,18)
PubChem CID	46836562
ChEMBL	CHEMBL1830707
IUPHAR	6231
BindingDB	50353290
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	9.0 nM	PMID21688779	BindingDB,IUPHAR,ChEMBL
Emax	120.0 %	PMID21688779	ChEMBL

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