General Information of the Protein
Protein ID
PT03263
Protein Name
Metabotropic glutamate receptor 3
Gene Name
GRM3
Secondarily
Gene Name
Gprc1c
Mglur3
Sequence
MKMLTRLQILMLALFSKGFLLSLGDHNFMRREIKIEGDLVLGGLFPINEKGTGTEECGRINEDRGIQRLEAMLFAIDEINKDNYLLPGVKLGVHILDTCSRDTYALEQSLEFVRASLTKVDEAEYMCPDGSYAIQENIPLLIAGVIGGSYSSVSIQVANLLRLFQIPQISYASTSAKLSDKSRYDYFARTVPPDFYQAKAMAEILRFFNWTYVSTVASEGDYGETGIEAFEQEARLRNICIATAEKVGRSNIRKSYDSVIRELLQKPNARVVVLFMRSDDSRELIAAANRVNASFTWVASDGWGAQESIVKGSEHVAYGAITLELASHPVRQFDRYFQSLNPYNNHRNPWFRDFWEQKFQCSLQNKRNHRQVCDKHLAIDSSNYEQESKIMFVVNAVYAMAHALHKMQRTLCPNTTKLCDAMKILDGKKLYKEYLLKINFTAPFNPNKGADSIVKFDTFGDGMGRYNVFNLQQTGGKYSYLKVGHWAETLSLDVDSIHWSRNSVPTSQCSDPCAPNEMKNMQPGDVCCWICIPCEPYEYLVDEFTCMDCGPGQWPTADLSGCYNLPEDYIKWEDAWAIGPVTIACLGFLCTCIVITVFIKHNNTPLVKASGRELCYILLFGVSLSYCMTFFFIAKPSPVICALRRLGLGTSFAICYSALLTKTNCIARIFDGVKNGAQRPKFISPSSQVFICLGLILVQIVMVSVWLILETPGTRRYTLPEKRETVILKCNVKDSSMLISLTYDVVLVILCTVYAFKTRKCPENFNEAKFIGFTMYTTCIIWLAFLPIFYVTSSDYRVQTTTMCISVSLSGFVVLGCLFAPKVHIVLFQPQKNVVTHRLHLNRFSVSGTATTYSQSSASTYVPTVCNGREVLDSTTSSL
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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
P31422
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: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0140442
(+)-2-Amino-3-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C8H10FNO4
 2
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
Ki = 65.9 nM
   TI
   LI
   LO
   TS
CP0374563
(+)-2-Amino-6-fluoro-4-oxo-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C8H8FNO5
 2
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
Ki = 3.62 nM
   TI
   LI
   LO
   TS
CP0409272
(+)-2-Amino-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C8H10FNO4
 2
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
Ki = 41.7 nM
   TI
   LI
   LO
   TS
CP0211752
(1R,2R,3R,5R,6R)-2-Amino-3-(3,4-dichloro-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C15H14Cl2FNO5
 3
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
IC50 = 24 nM
   TI
   LI
   LO
   TS
3
Ki = 4.46 nM
   TI
   LI
   LO
   TS
CP0377729
(1S,2S)-2-((S)-1-amino-1-carboxy-2-(9H-xanthen-9-yl)ethyl)cyclopropanecarboxylic acid
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C20H19NO5
 3
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
IC50 = 14.2 nM
   TI
   LI
   LO
   TS
3
Ki = 3.04 nM
   TI
   LI
   LO
   TS
CP0232347
7-ethoxy-4-(3-(2-methylpyridin-4-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C24H20F3N3O2
 1
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0338876
7-ethoxy-4-(3-(pyridin-4-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C23H18F3N3O2
 1
1
IC50 = 6 nM
   TI
   LI
   LO
   TS
CP0202837
4-(3-(2,6-dimethylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C24H20F3N3O
 1
1
IC50 < 10 nM
   TI
   LI
   LO
   TS
CP0053384
7-methyl-4-(3-(2-methylpyridin-4-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C23H18F3N3O
 1
1
IC50 = 14 nM
   TI
   LI
   LO
   TS
CP0484073
8-(4-fluorophenyl)-4-(3-imidazol-1-ylphenyl)-1,3-dihydro-1,5-benzodiazepin-2-one
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C24H17FN4O
 1
1
IC50 = 17 nM
   TI
   LI
   LO
   TS
CP0295954
4-(3-(2-methylpyridin-4-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C22H16F3N3O
 1
1
IC50 = 17 nM
   TI
   LI
   LO
   TS
CP0237670
4-(3-(pyridin-4-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C21H14F3N3O
 1
1
IC50 = 29 nM
   TI
   LI
   LO
   TS
CP0231490
7,8-dichloro-4-(3-(2-methylpyridin-4-yl)phenyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C21H15Cl2N3O
 1
1
IC50 = 30 nM
   TI
   LI
   LO
   TS
CP0059417
8-(2-fluorophenyl)-4-(3-imidazol-1-ylphenyl)-1,3-dihydro-1,5-benzodiazepin-2-one
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C24H17FN4O
 1
1
IC50 = 33 nM
   TI
   LI
   LO
   TS
CP0162027
4-(3-(1H-1,2,3-triazol-1-yl)phenyl)-8-(2-fluorophenyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C23H16FN5O
 2
1
IC50 = 33 nM
   TI
   LI
   LO
   TS
2
IC50 = 42 nM
   TI
   LI
   LO
   TS
CP0205609
8-(2-fluorophenyl)-7-hydroxy-4-(3-imidazol-1-ylphenyl)-1,3-dihydro-1,5-benzodiazepin-2-one
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C24H17FN4O2
 1
1
IC50 = 122 nM
   TI
   LI
   LO
   TS
CP0392388
(1R,2R,3R,5R,6R)-2-Amino-3-(3,4-difluoro-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C15H14F3NO5
 1
1
Ki = 3 nM
   TI
   LI
   LO
   TS
CP0391913
(1R,2R,3R,5R,6R)-2-Amino-3-benzhydryloxy-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C21H20FNO5
 1
1
Ki = 3.93 nM
   TI
   LI
   LO
   TS
CP0399772
2-[1-Amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-cyclopropanecarboxylic acid
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C20H19NO5
 1
1
Ki = 4.11 nM
   TI
   LI
   LO
   TS
CP0406578
(1R,2R,3R,5R,6R)-2-Amino-3-(4-chloro-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C15H15ClFNO5
 1
1
Ki = 4.77 nM
   TI
   LI
   LO
   TS
CP0499045
(1R,2R,3R,5R,6R)-2-Amino-6-fluoro-3-(naphthalen-2-ylmethoxy)-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C19H18FNO5
 1
1
Ki = 5.43 nM
   TI
   LI
   LO
   TS
CP0491988
(1R,2R,3R,5R,6R)-2-Amino-3-benzyloxy-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C15H16FNO5
 1
1
Ki = 15.9 nM
   TI
   LI
   LO
   TS
CP0076675
(1S,2S,5R,6S)-2-Amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C8H11NO4
 1
1
Ki = 53.5 nM
   TI
   LI
   LO
   TS
CP0497432
(1R,2R,3R,5R,6R)-2-Amino-6-fluoro-3-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C8H10FNO5
 1
1
Ki = 67.1 nM
   TI
   LI
   LO
   TS
CP0491986
(1R,2R,3R,5R,6R)-2-Amino-6-fluoro-3-methoxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C9H12FNO5
 1
1
Ki = 88.1 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0002355
(2S)-2-aminopentanedioic acid
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C5H9NO4
 1
1 EC50 = 3400 nM
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT01312 Metabotropic glutamate receptor 3 Homo sapiens, Human