General Information of the Protein
Protein ID
PT04980
Protein Name
Metabotropic glutamate receptor 8
Gene Name
GRM8
Secondarily
Gene Name
Gprc1h
Mglur8
Sequence
MVCEGKRLASCPCFFLLTAKFYWILTMMQRTHSQEYAHSIRVDGDIILGGLFPVHAKGERGVPCGELKKEKGIHRLEAMLYAIDQINKDPDLLSNITLGVRILDTCSRDTYALEQSLTFVQALIEKDASDVKCANGDPPIFTKPDKISGVIGAAASSVSIMVANILRLFKIPQISYASTAPELSDNTRYDFFSRVVPPDSYQAQAMVDIVTALGWNYVSTLASEGNYGESGVEAFTQISREIGGVCIAQSQKIPREPRPGEFEKIIKRLLETPNARAVIMFANEDDIRRILEAAKKLNQSGHFLWIGSDSWGSKIAPVYQQEEIAEGAVTILPKRASIDGFDRYFRSRTLANNRRNVWFAEFWEENFGCKLGSHGKRNSHIKKCTGLERIARDSSYEQEGKVQFVIDAVYSMAYALHNMHKERCPGYIGLCPRMVTIDGKELLGYIRAVNFNGSAGTPVTFNENGDAPGRYDIFQYQINNKSTEYKIIGHWTNQLHLKVEDMQWANREHTHPASVCSLPCKPGERKKTVKGVPCCWHCERCEGYNYQVDELSCELCPLDQRPNINRTGCQRIPIIKLEWHSPWAVVPVFIAILGIIATTFVIVTFVRYNDTPIVRASGRELSYVLLTGIFLCYSITFLMIAAPDTIICSFRRIFLGLGMCFSYAALLTKTNRIHRIFEQGKKSVTAPKFISPASQLVITFSLISVQLLGVFVWFVVDPPHTIIDYGEQRTLDPENARGVLKCDISDLSLICSLGYSILLMVTCTVYAIKTRGVPETFNEAKPIGFTMYTTCIIWLAFIPIFFGTAQSAEKMYIQTTTLTVSMSLSASVSLGMLYMPKVYIIIFHPEQNVQKRKRSFKAVVTAATMQSKLIQKGNDRPNGEVKSELCESLETNTSSTKTTYISYSNHSI
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Organism
Rattus norvegicus, Rat
Protein Classification
Membrane receptor
>
Family C G protein-coupled receptor
>
Small molecule receptor (family C GPCR)
>
Neurotransmitter receptor (family C GPCR)
>
Metabotropic glutamate receptor
Function
G-protein coupled receptor for glutamate. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Signaling inhibits adenylate cyclase activity.
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Uniprot ID
P70579
Ensembl ID
ENSG00000179603
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0063510
(S)-2-Amino-4-phosphono-butyric acid
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C4H10NO5P
 3
1
EC50 = 70 nM
   TI
   LI
   LO
   TS
2
EC50 = 240 nM
   TI
   LI
   LO
   TS
3
EC50 = 300 nM
   TI
   LI
   LO
   TS
CP0392926
N-[3-chloro-4-(5-chloropyridin-2-yl)oxyphenyl]pyridine-2-carboxamide
   Show/Hide
C17H11Cl2N3O2
 1
1
EC50 = 125 nM
   TI
   LI
   LO
   TS
CP0106027
D-AP4
   Show/Hide
C4H10NO5P
 1
1
EC50 = 290 nM
   TI
   LI
   LO
   TS
CP0058507
(1R,2R)-1-[(2S)-2-amino-2-carboxyethyl]cyclopropane-1,2-dicarboxylic acid
   Show/Hide
C8H11NO6
 1
1
EC50 = 680 nM
   TI
   LI
   LO
   TS
CP0288101
methyl 4-[3-[2-(4-acetamidophenyl)sulfanylacetyl]-2,5-dimethylpyrrol-1-yl]benzoate
   Show/Hide
C24H24N2O4S
 1
1
EC50 = 900 nM
   TI
   LI
   LO
   TS
CP0374296
(3S)-2-[((3-Amino-3-carboxy)propyl)(hydroxy)phosphinyl]ethanoic Acid
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C6H12NO6P
 2
1
EC50 = 910 nM
   TI
   LI
   LO
   TS
2
EC50 = 2700 nM
   TI
   LI
   LO
   TS
CP0120365
5-methyl-N-(4-methylpyrimidin-2-yl)-4-(1H-pyrazol-4-yl)-1,3-thiazol-2-amine
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C12H12N6S
 1
1
EC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0406804
US9212196, Derivative 26
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C13H18NO7PS
 1
1
EC50 = 1230 nM
   TI
   LI
   LO
   TS
CP0475231
US9212196, Derivative 24
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C13H17N2O10P
 1
1
EC50 = 1590 nM
   TI
   LI
   LO
   TS
CP0853331
(3S)-3-[((3-Amino-3-carboxy)propyl)(hydroxy)phosphinyl]-2-(hydroxymethyl)ethanoic Acid
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C6H12NO7P
 1
1
EC50 = 2900 nM
   TI
   LI
   LO
   TS
CP0374295
(3S)-2-[(((3-Amino-3-carboxy)propyl)(hydroxy)phosphinyl)-methyl]butan-1,4-dioic Acid
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C9H16NO8P
 2
1
EC50 = 3500 nM
   TI
   LI
   LO
   TS
2
EC50 = 38000 nM
   TI
   LI
   LO
   TS
CP0418091
US9212196, Derivative 5
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C14H19N2O11P
 1
1
EC50 = 3720 nM
   TI
   LI
   LO
   TS
CP0907064
(3S)-3-[((3-Amino-3-carboxy)propyl)(hydroxy)phosphinyl]propenoic acid
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C7H12NO6P
 2
1
EC50 = 5100 nM
   TI
   LI
   LO
   TS
2
EC50 = 7200 nM
   TI
   LI
   LO
   TS
CP0096656
(1R,2S)-4-aminocyclopentane-1,2,4-tricarboxylic acid
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C8H11NO6
 1
1
EC50 = 5100 nM
   TI
   LI
   LO
   TS
CP0377002
(S)-3-amino-3-carboxypropyl-2'-carboxyethyl phosphinic acid
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C7H14NO6P
 2
1
EC50 = 6600 nM
   TI
   LI
   LO
   TS
2
EC50 = 7800 nM
   TI
   LI
   LO
   TS
CP0464832
US9212196, Derivative 21
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C14H17F3NO8P
 1
1
EC50 = 6860 nM
   TI
   LI
   LO
   TS
CP0418088
US9212196, Derivative 23
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C14H18NO10P
 1
1
EC50 = 7400 nM
   TI
   LI
   LO
   TS
CP0400028
(3S)-3-[((3-Amino-3-carboxy)propyl)(hydroxy)phosphinyl]-2-chloropropanoic Acid
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C7H13ClNO6P
 2
1
EC50 = 8100 nM
   TI
   LI
   LO
   TS
2
EC50 = 8300 nM
   TI
   LI
   LO
   TS
CP0418095
US9212196, Derivative 34
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C14H19FNO8P
 1
1
EC50 = 9170 nM
   TI
   LI
   LO
   TS
CP0482641
3-(4-methoxyphenyl)-2,5-dimethyl-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine
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C16H14F3N3O
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0402516
US9212196, Derivative 6
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C14H19FNO9P
 1
1
EC50 = 10300 nM
   TI
   LI
   LO
   TS
CP0413237
US9212196, Derivative 25
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C13H17N2O9PS
 1
1
EC50 = 11500 nM
   TI
   LI
   LO
   TS
CP0002355
(2S)-2-aminopentanedioic acid
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C5H9NO4
 1
1
EC50 = 14010 nM
   TI
   LI
   LO
   TS
CP0418093
US9212196, Derivative 18
   Show/Hide
C15H20NO11P
 1
1
EC50 = 14100 nM
   TI
   LI
   LO
   TS
CP0418089
US9212196, Derivative 29
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C14H20NO8P
 1
1
EC50 = 14300 nM
   TI
   LI
   LO
   TS
CP0374294
(3S)-4-[((3-Amino-3-carboxy)propyl)(hydroxy)phosphinyl]-butanoic Acid
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C8H16NO6P
 2
1
EC50 = 18000 nM
   TI
   LI
   LO
   TS
2
EC50 = 19000 nM
   TI
   LI
   LO
   TS
CP0418086
US9212196, Derivative 3
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C14H20NO9P
 1
1
EC50 = 18400 nM
   TI
   LI
   LO
   TS
CP0845512
(+/-)-3-amino-3-carboxypropyl-2'-carboxyethyl phosphinic acid
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C7H14NO6P
 1
1
EC50 = 20000 nM
   TI
   LI
   LO
   TS
CP0066050
(1S,2S)-1-[(2S)-2-amino-2-carboxyethyl]cyclopropane-1,2-dicarboxylic acid
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C8H11NO6
 1
1
EC50 = 20790 nM
   TI
   LI
   LO
   TS
CP0418097
US9212196, Derivative 10
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C15H22NO8P
 1
1
EC50 = 21900 nM
   TI
   LI
   LO
   TS
CP0406806
US9212196, Derivative 19
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C15H22NO9P
 1
1
EC50 = 25000 nM
   TI
   LI
   LO
   TS
CP0493272
US9212196, Derivative 4
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C15H22NO10P
 1
1
EC50 = 27200 nM
   TI
   LI
   LO
   TS
CP0418098
US9212196, Derivative 28
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C13H16F2NO8P
 1
1
EC50 = 27500 nM
   TI
   LI
   LO
   TS
CP0418087
US9212196, Derivative 13
   Show/Hide
C13H20NO7P
 1
1
EC50 = 28000 nM
   TI
   LI
   LO
   TS
CP0561457
US9212196, Derivative 8
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C14H19INO9P
 1
1
EC50 = 28000 nM
   TI
   LI
   LO
   TS
CP0442807
US9212196, Derivative 2
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C13H18NO8P
 1
1
EC50 = 29200 nM
   TI
   LI
   LO
   TS
CP0391280
3-[3-[(2-cyclopentyl-1-oxo-3H-isoindol-5-yl)oxymethyl]phenyl]-4-methoxybenzoic acid
   Show/Hide
C28H27NO5
 1
1
EC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0397657
2-chloro-5-[3-(2-cyclopentyl-1-oxo-3H-isoindol-5-yl)phenyl]benzoic acid
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C26H22ClNO3
 1
1
EC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0397658
2-chloro-5-[3-[(2-cyclopropyl-3-oxo-1,2-benzothiazol-6-yl)oxymethyl]phenyl]benzoic acid
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C24H18ClNO4S
 1
1
EC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0463911
US9212196, Derivative 22
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C13H18NO9P
 1
1
EC50 = 34000 nM
   TI
   LI
   LO
   TS
CP0418096
US9212196, Derivative 35
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C14H19ClNO8P
 1
1
EC50 = 38200 nM
   TI
   LI
   LO
   TS
CP0418092
US9212196, Derivative 7
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C14H19ClNO9P
 1
1
EC50 = 44000 nM
   TI
   LI
   LO
   TS
CP0905965
(3S)-2-[((3-Amino-3-carboxy)propyl)(hydroxy)phosphinyl]-ethylphosphonate
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C6H15NO7P2
 1
1
EC50 = 48000 nM
   TI
   LI
   LO
   TS
CP0413236
US9212196, Derivative 12
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C14H20NO7P
 1
1
EC50 = 48700 nM
   TI
   LI
   LO
   TS
CP0402517
US9212196, Derivative 11
   Show/Hide
C14H18NO7P
 1
1
EC50 = 49000 nM
   TI
   LI
   LO
   TS
CP0490836
(3S)-3-[((3-Amino-3-carboxy)propyl)(hydroxy)phosphinyl]-2-methylpropanoic Acid
   Show/Hide
C8H16NO6P
 1
1
EC50 = 53000 nM
   TI
   LI
   LO
   TS
CP0418094
US9212196, Derivative 20
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C14H17F3NO9P
 1
1
EC50 = 55600 nM
   TI
   LI
   LO
   TS
CP0410794
(R)-3-amino-3-carboxypropyl-2'-carboxyethyl phosphinic acid
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C7H14NO6P
 1
1
EC50 = 58000 nM
   TI
   LI
   LO
   TS
CP0377001
(2S)-2-Amino-5-[(hydroxy)phosphinyl]pentanoic Acid
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C5H12NO4P
 1
1
EC50 = 73000 nM
   TI
   LI
   LO
   TS
CP0514300
(3S)-3-[((3-Amino-3-carboxylate)propyl)(hydroxy)phosphinate]-2-(2-hydroxyethyl)propanoate
   Show/Hide
C9H18NO7P
 1
1
EC50 = 76000 nM
   TI
   LI
   LO
   TS
CP0920930
(3S)-2-[(((3-Amino-3-carboxy)propyl)(hydroxy)phosphinyl)hydroxymethyl]cyclopropane-1-carboxylic Acid hydrochloride
   Show/Hide
C9H17ClNO7P
 1
1
EC50 = 91000 nM
   TI
   LI
   LO
   TS
CP0902261
(3S)-4-[((3-Amino-3-carboxy)propyl)(hydroxy)phosphinyl]-furanone
   Show/Hide
C8H14NO6P
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0932553
(3S)-2-[(((3-Amino-3-carboxy)propyl)(hydroxy)phosphinyl)-methyl]oxotetrahydrofuran-3-yl
   Show/Hide
C9H16NO6P
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0418090
US9212196, Derivative 33
   Show/Hide
C14H17F3NO7P
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0442808
US9212196, Derivative 30
   Show/Hide
C13H18NO7P
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0475232
US9212196, Derivative 32
   Show/Hide
C14H17F3NO8P
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0389571
6-(2,4-dimethylphenyl)-2-ethyl-6,7-dihydro-5H-1,3-benzoxazol-4-one
   Show/Hide
C17H19NO2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0416254
7-(4-fluorophenyl)-2-[[2-(trifluoromethyl)pyridin-4-yl]oxymethyl]pyrazolo[1,5-a]pyrimidine-5-carboxamide
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C20H13F4N5O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0416287
2-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]methyl]-7-(4-fluorophenyl)thieno[3,2-b]pyridine-5-carboxamide
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C21H22FN3O2S
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS