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GLASS

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GPCR

Name	Metabotropic glutamate receptor 8
Species	Homo sapiens (Human)
Gene	GRM8
Synonym	mGluR8b mGluR8 mGlu8 receptor Gprc1h glutamate receptor GLUR8 [ Show all ]
Disease	N/A
Length	908
Amino acid sequence	MVCEGKRSASCPCFFLLTAKFYWILTMMQRTHSQEYAHSIRVDGDIILGGLFPVHAKGERGVPCGELKKEKGIHRLEAMLYAIDQINKDPDLLSNITLGVRILDTCSRDTYALEQSLTFVQALIEKDASDVKCANGDPPIFTKPDKISGVIGAAASSVSIMVANILRLFKIPQISYASTAPELSDNTRYDFFSRVVPPDSYQAQAMVDIVTALGWNYVSTLASEGNYGESGVEAFTQISREIGGVCIAQSQKIPREPRPGEFEKIIKRLLETPNARAVIMFANEDDIRRILEAAKKLNQSGHFLWIGSDSWGSKIAPVYQQEEIAEGAVTILPKRASIDGFDRYFRSRTLANNRRNVWFAEFWEENFGCKLGSHGKRNSHIKKCTGLERIARDSSYEQEGKVQFVIDAVYSMAYALHNMHKDLCPGYIGLCPRMSTIDGKELLGYIRAVNFNGSAGTPVTFNENGDAPGRYDIFQYQITNKSTEYKVIGHWTNQLHLKVEDMQWAHREHTHPASVCSLPCKPGERKKTVKGVPCCWHCERCEGYNYQVDELSCELCPLDQRPNMNRTGCQLIPIIKLEWHSPWAVVPVFVAILGIIATTFVIVTFVRYNDTPIVRASGRELSYVLLTGIFLCYSITFLMIAAPDTIICSFRRVFLGLGMCFSYAALLTKTNRIHRIFEQGKKSVTAPKFISPASQLVITFSLISVQLLGVFVWFVVDPPHIIIDYGEQRTLDPEKARGVLKCDISDLSLICSLGYSILLMVTCTVYAIKTRGVPETFNEAKPIGFTMYTTCIIWLAFIPIFFGTAQSAEKMYIQTTTLTVSMSLSASVSLGMLYMPKVYIIIFHPEQNVQKRKRSFKAVVTAATMQSKLIQKGNDRPNGEVKSELCESLETNTSSTKTTYISYSNHSI
UniProt	O00222
Protein Data Bank	6bsz, 6bt5, 6e5v
GPCR-HGmod model	N/A
3D structure model	This structure is from PDB ID 6bsz.
BioLiP	BL0432251,BL0432252, BL0403876,BL0403877, BL0403874,BL0403875
Therapeutic Target Database	N/A
ChEMBL	CHEMBL3228
IUPHAR	296
DrugBank	BE0000835

Ligand

Name	MTEP
Molecular formula	C11H8N2S
IUPAC name	2-methyl-4-(2-pyridin-3-ylethynyl)-1,3-thiazole
Molecular weight	200.259
Hydrogen bond acceptor	3
Hydrogen bond donor	0
XlogP	2.3
Synonyms	BDBM50122758 GTPL3336 3-[(2-methyl-4-thiazolyl)ethynyl]pyridine CTK1B8867 mGluR5 Antagonist, MTEP 2-methyl-4-(pyridin-3-ylethynyl)thiazole 329205-68-7 ACN-027361 DTXSID30430775 SCHEMBL187254 3-(2-Methyl-thiazol-4-ylethynyl)-pyridine IN1238 3-[2-(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine D00JLE 3-((2-Methyl-1,3-thiazol-4-yl)ethynyl)pyridine API0006876 FCH3417361 ZINC1489321 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine CHEMBL292065 KB-274670 3-[2-(2-Methylthiazol-4-yl)ethynyl]pyridine D09YDQ Pyridine, 3-[(2-methyl-4-thiazolyl)ethynyl]- 3-(2-(2-methylthiazol-4-yl)ethynyl)pyridine [ Show all ]
Inchi Key	NRBNGHCYDWUVLC-UHFFFAOYSA-N
Inchi ID	InChI=1S/C11H8N2S/c1-9-13-11(8-14-9)5-4-10-3-2-6-12-7-10/h2-3,6-8H,1H3
PubChem CID	9794218
ChEMBL	CHEMBL292065
IUPHAR	3336
BindingDB	50122758
DrugBank	N/A
Structure SDF download
Lipinski's druglikeness	This ligand satisfies Lipinski's rule of five.

Experimental Data

Parameter	Value	Reference	Database source
Inhibition	>50.0 %	PMID20382541	ChEMBL

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