General Information of the Protein
Protein ID
PT02444
Protein Name
Metabotropic glutamate receptor 1
Gene Name
GRM1
Secondarily
Gene Name
Gprc1a
Mglur1
Sequence
MVRLLLIFFPMIFLEMSILPRMPDRKVLLAGASSQRSVARMDGDVIIGALFSVHHQPPAEKVPERKCGEIREQYGIQRVEAMFHTLDKINADPVLLPNITLGSEIRDSCWHSSVALEQSIEFIRDSLISIRDEKDGLNRCLPDGQTLPPGRTKKPIAGVIGPGSSSVAIQVQNLLQLFDIPQIAYSATSIDLSDKTLYKYFLRVVPSDTLQARAMLDIVKRYNWTYVSAVHTEGNYGESGMDAFKELAAQEGLCIAHSDKIYSNAGEKSFDRLLRKLRERLPKARVVVCFCEGMTVRGLLSAMRRLGVVGEFSLIGSDGWADRDEVIEGYEVEANGGITIKLQSPEVRSFDDYFLKLRLDTNTRNPWFPEFWQHRFQCRLPGHLLENPNFKKVCTGNESLEENYVQDSKMGFVINAIYAMAHGLQNMHHALCPGHVGLCDAMKPIDGRKLLDFLIKSSFVGVSGEEVWFDEKGDAPGRYDIMNLQYTEANRYDYVHVGTWHEGVLNIDDYKIQMNKSGMVRSVCSEPCLKGQIKVIRKGEVSCCWICTACKENEFVQDEFTCRACDLGWWPNAELTGCEPIPVRYLEWSDIESIIAIAFSCLGILVTLFVTLIFVLYRDTPVVKSSSRELCYIILAGIFLGYVCPFTLIAKPTTTSCYLQRLLVGLSSAMCYSALVTKTNRIARILAGSKKKICTRKPRFMSAWAQVIIASILISVQLTLVVTLIIMEPPMPILSYPSIKEVYLICNTSNLGVVAPVGYNGLLIMSCTYYAFKTRNVPANFNEAKYIAFTMYTTCIIWLAFVPIYFGSNYKIITTCFAVSLSVTVALGCMFTPKMYIIIAKPERNVRSAFTTSDVVRMHVGDGKLPCRSNTFLNIFRRKKPGAGNANSNGKSVSWSEPGGRQAPKGQHVWQRLSVHVKTNETACNQTAVIKPLTKSYQGSGKSLTFSDASTKTLYNVEEEDNTPSAHFSPPSSPSMVVHRRGPPVATTPPLPPHLTAEETPLFLADSVIPKGLPPPLPQQQPQQPPPQQPPQQPKSLMDQLQGVVTNFGSGIPDFHAVLAGPGTPGNSLRSLYPPPPPPQHLQMLPLHLSTFQEESISPPGEDIDDDSERFKLLQEFVYEREGNTEEDELEEEEDLPTASKLTPEDSPALTPPSPFRDSVASGSSVPSSPVSESVLCTPPNVTYASVILRDYKQSSSTL
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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. May participate in the central action of glutamate in the CNS, such as long-term potentiation in the hippocampus and long-term depression in the cerebellum (PubMed:10945991, PubMed:1438218, PubMed:1656524, PubMed:1847995). May function in the light response in the retina (By similarity).
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Uniprot ID
P23385
Ensembl ID
ENSG00000152822
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
Compound ID Compound Name Compound Formula
CP0205005
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 = 1 nM
   TI
   LI
   LO
   TS
CP0170781
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 = 5 nM
   TI
   LI
   LO
   TS
CP0446341
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 = 21 nM
   TI
   LI
   LO
   TS
CP0505322
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 = 33 nM
   TI
   LI
   LO
   TS
CP0141727
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 = 52 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 = 10000 nM
CP0040798
(2S)-2-amino-3-(3,5-dioxo-1,2,4-oxadiazolidin-2-yl)propanoic acid
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C5H7N3O5
 1
1 EC50 = 16400 nM
CP0205005
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 = 10 nM
CP0141727
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 = 52 nM
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT05866 Metabotropic glutamate receptor 1 Mus musculus, Mouse
50% Identity
Protein ID Protein Name Protein Organism
PT01994 Metabotropic glutamate receptor 1 Homo sapiens, Human