General Information of the Protein
Protein ID
PT01247
Protein Name
Metabotropic glutamate receptor 5
Gene Name
GRM5
Secondarily
Gene Name
Gprc1e
Mglur5
Sequence
MVLLLILSVLLLKEDVRGSAQSSERRVVAHMPGDIIIGALFSVHHQPTVDKVHERKCGAVREQYGIQRVEAMLHTLERINSDPTLLPNITLGCEIRDSCWHSAVALEQSIEFIRDSLISSEEEEGLVRCVDGSSSFRSKKPIVGVIGPGSSSVAIQVQNLLQLFNIPQIAYSATSMDLSDKTLFKYFMRVVPSDAQQARAMVDIVKRYNWTYVSAVHTEGNYGESGMEAFKDMSAKEGICIAHSYKIYSNAGEQSFDKLLKKLRSHLPKARVVACFCEGMTVRGLLMAMRRLGLAGEFLLLGSDGWADRYDVTDGYQREAVGGITIKLQSPDVKWFDDYYLKLRPETNLRNPWFQEFWQHRFQCRLEGFAQENSKYNKTCNSSLTLRTHHVQDSKMGFVINAIYSMAYGLHNMQMSLCPGYAGLCDAMKPIDGRKLLDSLMKTNFTGVSGDMILFDENGDSPGRYEIMNFKEMGKDYFDYINVGSWDNGELKMDDDEVWSKKNNIIRSVCSEPCEKGQIKVIRKGEVSCCWTCTPCKENEYVFDEYTCKACQLGSWPTDDLTGCDLIPVQYLRWGDPEPIAAVVFACLGLLATLFVTVIFIIYRDTPVVKSSSRELCYIILAGICLGYLCTFCLIAKPKQIYCYLQRIGIGLSPAMSYSALVTKTNRIARILAGSKKKICTKKPRFMSACAQLVIAFILICIQLGIIVALFIMEPPDIMHDYPSIREVYLICNTTNLGVVTPLGYNGLLILSCTFYAFKTRNVPANFNEAKYIAFTMYTTCIIWLAFVPIYFGSNYKIITMCFSVSLSATVALGCMFVPKVYIILAKPERNVRSAFTTSTVVRMHVGDGKSSSAASRSSSLVNLWKRRGSSGETLRYKDRRLAQHKSEIECFTPKGSMGNGGRATMSSSNGKSVTWAQNEKSTRGQHLWQRLSVHINKKENPNQTAVIKPFPKSTENRGPGAAAGGGSGPGVAGAGNAGCTATGGPEPPDAGPKALYDVAEAEESFPAAARPRSPSPISTLSHLAGSAGRTDDDAPSLHSETAARSSSSQGSLMEQISSVVTRFTANISELNSMMLSTAATPGPPGTPICSSYLIPKEIQLPTTMTTFAEIQPLPAIEVTGGAQGATGVSPAQETPTGAESAPGKPDLEELVALTPPSPFRDSVDSGSTTPNSPVSESALCIPSSPKYDTLIIRDYTQSSSSL
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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 activates a phosphatidylinositol-calcium second messenger system and generates a calcium-activated chloride current. Plays an important role in the regulation of synaptic plasticity and the modulation of the neural network activity.
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Uniprot ID
P31424
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: CL000094 , 1321N1
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0170781
 Compound Info 
9-Dimethylamino-3-(4-ethyl-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one
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C19H18N4OS
  1
1
IC50 = 1330 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0141727
 Compound Info 
3-(4-Ethyl-phenyl)-9-[methyl-(2-pyridin-2-yl-ethyl)-amino]-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one
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C25H23N5OS
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0205005
 Compound Info 
3-azepan-1-yl-9-dimethylamino-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one
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C17H21N5OS
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0446341
 Compound Info 
9-dimethylamino-3-(3-fluoro-4-methyl-phenyl)-3H-pyrido[4',3':4,5]thieno[3,2-d]pyrimidin-4-one
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C18H15FN4OS
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0505322
 Compound Info 
3-azepan-1-yl-9-(dimethylnitroryl)pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4(3H)-one
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C17H21N5O2S
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000011 , CHO
 Cell Line Info 
Cell Line ID: CL000026 , CHO-K1
 Cell Line Info 
Cell Line ID: CL000025 , HEK-293T
 Cell Line Info 
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000050 , HEK293-A
 Cell Line Info 
Cell Line ID: CL000031 , MDCK
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0088840
 Compound Info 
3-Cyano-N-(2,5-diphenyl-2H-pyrazol-3-yl)-benzamide
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C23H16N4O
  1
1 EC50 = 20 nM
CP0159187
 Compound Info 
N-(2,5-diphenylpyrazol-3-yl)-4-(trifluoromethyl)benzamide
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C23H16F3N3O
  1
1 EC50 = 20 nM
CP0358813
 Compound Info 
4-butoxy-N-(2,4-difluorophenyl)benzamide
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C17H17F2NO2
  1
1 EC50 = 33 nM
CP0159176
 Compound Info 
N-(2,5-diphenylpyrazol-3-yl)-4-methylbenzamide
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C23H19N3O
  1
1 EC50 = 40 nM
CP0049482
 Compound Info 
N-(2,5-diphenylpyrazol-3-yl)benzamide
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C22H17N3O
  1
1 EC50 = 300 nM
CP0002355
 Compound Info 
(2S)-2-aminopentanedioic acid
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C5H9NO4
  1
1 EC50 = 4400 nM
CP0296509
 Compound Info 
3-(6-Methyl-pyridin-2-ylethynyl)-benzonitrile
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C15H10N2
  1
1 IC50 = 5 nM
CP0182748
 Compound Info 
6-[5-(3-cyano-5-fluorophenyl)-1,2,4-oxadiazol-3-yl]pyridine-3-carbonitrile
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C15H6FN5O
  1
1 IC50 = 14.5 nM
CP0191235
 Compound Info 
2-Methyl-6-(phenylethynyl)pyridine
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C14H11N
  3
1 IC50 = 36 nM
2 Ki = 4.7 nM
3 Ki = 13 nM
CP0413752
 Compound Info 
6-bromo-N-(3-chlorophenyl)quinazolin-4-amine
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C14H9BrClN3
  1
1 Ki = 116 nM
CP0230190
 Compound Info 
N-(3-bromophenyl)-6-chloroquinazolin-4-amine
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C14H9BrClN3
  1
1 Ki = 249 nM
CP0360490
 Compound Info 
N-(3-bromophenyl)-6-fluoroquinazolin-4-amine
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C14H9BrFN3
  1
1 Ki = 736 nM
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT00854 Metabotropic glutamate receptor 5 Homo sapiens, Human
 Protein Info 
PT06161 Metabotropic glutamate receptor 5 Mus musculus, Mouse
 Protein Info