Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET01KCZ)
Name
Glutamate receptor mGLU3 (mGluR3)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Metabotropic glutamate receptor 3; GPRC1C; Group III metabotropic glutamate receptor; mGLUR3; mGluR3
Family G-protein coupled receptor (GPCR)  >>  G-protein coupled glutamate receptor (GPCR-C)
Organism
Homo sapiens (Human)
Gene Name GRM3 Gene ID
2913
UniProt ID GRM3_HUMAN (click to find more protein-related data of this DBT)
TTD ID T02719 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MKMLTRLQVLTLALFSKGFLLSLGDHNFLRREIKIEGDLVLGGLFPINEKGTGTEECGRI
NEDRGIQRLEAMLFAIDEINKDDYLLPGVKLGVHILDTCSRDTYALEQSLEFVRASLTKV
DEAEYMCPDGSYAIQENIPLLIAGVIGGSYSSVSIQVANLLRLFQIPQISYASTSAKLSD
KSRYDYFARTVPPDFYQAKAMAEILRFFNWTYVSTVASEGDYGETGIEAFEQEARLRNIC
IATAEKVGRSNIRKSYDSVIRELLQKPNARVVVLFMRSDDSRELIAAASRANASFTWVAS
DGWGAQESIIKGSEHVAYGAITLELASQPVRQFDRYFQSLNPYNNHRNPWFRDFWEQKFQ
CSLQNKRNHRRVCDKHLAIDSSNYEQESKIMFVVNAVYAMAHALHKMQRTLCPNTTKLCD
AMKILDGKKLYKDYLLKINFTAPFNPNKDADSIVKFDTFGDGMGRYNVFNFQNVGGKYSY
LKVGHWAETLSLDVNSIHWSRNSVPTSQCSDPCAPNEMKNMQPGDVCCWICIPCEPYEYL
ADEFTCMDCGSGQWPTADLTGCYDLPEDYIRWEDAWAIGPVTIACLGFMCTCMVVTVFIK
HNNTPLVKASGRELCYILLFGVGLSYCMTFFFIAKPSPVICALRRLGLGSSFAICYSALL
TKTNCIARIFDGVKNGAQRPKFISPSSQVFICLGLILVQIVMVSVWLILEAPGTRRYTLA
EKRETVILKCNVKDSSMLISLTYDVILVILCTVYAFKTRKCPENFNEAKFIGFTMYTTCI
IWLAFLPIFYVTSSDYRVQTTTMCISVSLSGFVVLGCLFAPKVHIILFQPQKNVVTHRLH
LNRFSVSGTGTTYSQSSASTYVPTVCNGREVLDSTTSSL
Function
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. G-protein coupled receptor for glutamate.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Glutamic acid hydrochloride Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Acidulant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki = 57.54 nM (estimated based on the structural similarity with CHEMBL575060 ) [1]
                   Structural Similarity Tanimoto coefficient = 1
                   Tested Species Homo sapiens (Human)
                   UniProt ID GRM3_HUMAN
          DIG Name: Monosodium glutamate Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Buffering agent; Flavoring agent
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 60 nM (estimated based on the structural similarity with CHEMBL575060 ) [1]
                   Structural Similarity Tanimoto coefficient = 0.979166667
                   Tested Species Homo sapiens (Human)
                   UniProt ID GRM3_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 57.54 nM (estimated based on the structural similarity with CHEMBL575060 ) [2]
                   Structural Similarity Tanimoto coefficient = 0.979166667
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID GRM3_RAT
References
1 A highly selective agonist for the metabotropic glutamate receptor mGluR2. Med Chem Comm. (2011) 2:1120-1124.
2 New 4-Functionalized Glutamate Analogues Are Selective Agonists at Metabotropic Glutamate Receptor Subtype 2 or Selective Agonists at Metabotropic Glutamate Receptor Group III. J Med Chem. 2016 Feb 11; 59(3):914-24.

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