General Information of the Protein
Protein ID
PT01312
Protein Name
Metabotropic glutamate receptor 3
Gene Name
GRM3
Secondarily
Gene Name
GPRC1C
MGLUR3
Sequence
MKMLTRLQVLTLALFSKGFLLSLGDHNFLRREIKIEGDLVLGGLFPINEKGTGTEECGRINEDRGIQRLEAMLFAIDEINKDDYLLPGVKLGVHILDTCSRDTYALEQSLEFVRASLTKVDEAEYMCPDGSYAIQENIPLLIAGVIGGSYSSVSIQVANLLRLFQIPQISYASTSAKLSDKSRYDYFARTVPPDFYQAKAMAEILRFFNWTYVSTVASEGDYGETGIEAFEQEARLRNICIATAEKVGRSNIRKSYDSVIRELLQKPNARVVVLFMRSDDSRELIAAASRANASFTWVASDGWGAQESIIKGSEHVAYGAITLELASQPVRQFDRYFQSLNPYNNHRNPWFRDFWEQKFQCSLQNKRNHRRVCDKHLAIDSSNYEQESKIMFVVNAVYAMAHALHKMQRTLCPNTTKLCDAMKILDGKKLYKDYLLKINFTAPFNPNKDADSIVKFDTFGDGMGRYNVFNFQNVGGKYSYLKVGHWAETLSLDVNSIHWSRNSVPTSQCSDPCAPNEMKNMQPGDVCCWICIPCEPYEYLADEFTCMDCGSGQWPTADLTGCYDLPEDYIRWEDAWAIGPVTIACLGFMCTCMVVTVFIKHNNTPLVKASGRELCYILLFGVGLSYCMTFFFIAKPSPVICALRRLGLGSSFAICYSALLTKTNCIARIFDGVKNGAQRPKFISPSSQVFICLGLILVQIVMVSVWLILEAPGTRRYTLAEKRETVILKCNVKDSSMLISLTYDVILVILCTVYAFKTRKCPENFNEAKFIGFTMYTTCIIWLAFLPIFYVTSSDYRVQTTTMCISVSLSGFVVLGCLFAPKVHIILFQPQKNVVTHRLHLNRFSVSGTGTTYSQSSASTYVPTVCNGREVLDSTTSSL
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Organism
Homo sapiens, Human
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
Primary ID:
Q14832

Secondarily ID:
Q2PNZ6
Q75MV4
Q75N17
Q86YG6
Q8TBH9
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HGNC ID
HGNC:4595
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: CL000460 , Flp-In-T-REx-293
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0458064
 Compound Info 
3-(cyclopropylmethyl)-7-[[4-(2,4-difluorophenyl)piperidin-1-yl]methyl]-8-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine
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C23H23F5N4
  1
1
EC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0544956
 Compound Info 
7-[[4-(2-chloro-4-fluorophenyl)piperazin-1-yl]methyl]-3-(cyclopropylmethyl)-8-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine
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C22H22ClF4N5
  1
1
EC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0544958
 Compound Info 
3-(cyclopropylmethyl)-7-[[4-(2-fluorophenyl)piperazin-1-yl]methyl]-8-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine
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C22H23F4N5
  1
1
EC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0544959
 Compound Info 
3-(cyclopropylmethyl)-8-[[4-(2,4-difluorophenyl)piperazin-1-yl]methyl]-6-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine
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C22H22F5N5
  1
1
EC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0568919
 Compound Info 
7-[[4-(4-chloro-2-fluorophenyl)piperazin-1-yl]methyl]-3-(cyclopropylmethyl)-8-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine
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C22H22ClF4N5
  1
1
EC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0568137
 Compound Info 
[1-(cyclopropylmethyl)-4-(trifluoromethyl)pyrazolo[3,4-b]pyridin-5-yl]-[4-(2,4-difluorophenyl)piperazin-1-yl]methanone
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C22H20F5N5O
  1
1
EC50 > 1000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0046845
 Compound Info 
3-(cyclopropylmethyl)-7-[[4-(2,4-difluorophenyl)piperazin-1-yl]methyl]-8-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine
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C22H22F5N5
  1
1
EC50 > 8000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000125 , MCB3901
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0432878
 Compound Info 
(1S,2S,4S,5R,6R)-2-amino-4-hydroxybicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C8H11NO5
  1
1 IC50 = 6.3 nM
CP0445963
 Compound Info 
(1S,2S,4R,5R,6R)-2-amino-4-hydroxybicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C8H11NO5
  1
1 IC50 = 11.2 nM
CP0076675
 Compound Info 
(1S,2S,5R,6S)-2-Amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C8H11NO4
  2
1 IC50 = 27.9 nM
2 Ki = 125.6 nM
CP0211752
 Compound Info 
(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
  1
1 Ki = 4.5 nM
Clinical Information about the Protein
Target 1 ( Metabotropic glutamate receptor 3 (mGluR3) )
Target Type Clinical trial Target
Disease 3 Target-related Diseases  3
1 Schizophrenia [ICD-11: 6A20]
2 Major depressive disorder [ICD-11: 6A70.3]
3 Anxiety disorder [ICD-11: 6B00-6B0Z]
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 LY404039
 Drug Info 
Phase 3
Schizophrenia
2 BCI-632
 Drug Info 
Phase 1
Major depressive disorder
Discontinued Drug(s) 2 Discontinued Drugs  2
1 LY-544344
 Drug Info 
Discontinued in Phase 3
Anxiety disorder
2 LY354740
 Drug Info 
Discontinued in Phase 2
Anxiety disorder
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT03263 Metabotropic glutamate receptor 3 Rattus norvegicus, Rat
 Protein Info