Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0B2YE)
Name
Glycine receptor alpha-1 (GLRA1)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Strychnine-binding glycine receptor; GLRA1; Glycine receptor 48 kDa subunit; Glycine receptor strychnine-binding subunit; Strychnine binding subunit; Strychnine-insensitive glycine receptor
Family Transmembrane channel/porin (TC/P)  >>  Ligand-gated ion channel (LIC)
Organism
Homo sapiens (Human)
Gene Name GLRA1 Gene ID
2741
UniProt ID GLRA1_HUMAN (click to find more protein-related data of this DBT)
TTD ID T50269 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MYSFNTLRLYLWETIVFFSLAASKEAEAARSAPKPMSPSDFLDKLMGRTSGYDARIRPNF
KGPPVNVSCNIFINSFGSIAETTMDYRVNIFLRQQWNDPRLAYNEYPDDSLDLDPSMLDS
IWKPDLFFANEKGAHFHEITTDNKLLRISRNGNVLYSIRITLTLACPMDLKNFPMDVQTC
IMQLESFGYTMNDLIFEWQEQGAVQVADGLTLPQFILKEEKDLRYCTKHYNTGKFTCIEA
RFHLERQMGYYLIQMYIPSLLIVILSWISFWINMDAAPARVGLGITTVLTMTTQSSGSRA
SLPKVSYVKAIDIWMAVCLLFVFSALLEYAAVNFVSRQHKELLRFRRKRRHHKSPMLNLF
QEDEAGEGRFNFSAYGMGPACLQAKDGISVKGANNSNTTNPPPAPSKSPEEMRKLFIQRA
KKIDKISRIGFPMAFLIFNMFYWIIYKIVRREDVHNQ
Function
The glycine receptor is a neurotransmitter-gated ion channel. Binding of glycine to its receptor increases the chloride conductance and thus produces hyperpolarization (inhibition of neuronal firing).
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Aminoethanoic acid 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; Disintegrant; Lyophilization aid
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 94000 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID GLRA1_HUMAN
          DIG Name: Mannitol 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
Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 12589.25 nM (estimated based on the structural similarity with CHEMBL604608 ) [2]
                   Structural Similarity Tanimoto coefficient = 0.804878049
                   Tested Species Homo sapiens (Human)
                   UniProt ID GLRA1_HUMAN
          DIG Name: Glycine 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
Buffering agent; Disintegrant; Lyophilization aid
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 94000 nM (estimated based on the structural similarity with CHEMBL773 ) [1]
                   Structural Similarity Tanimoto coefficient = 0.964285714
                   Tested Species Homo sapiens (Human)
                   UniProt ID GLRA1_HUMAN
References
1 Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor. J Med Chem. 2007 Sep 20; 50(19):4616-29.
2 Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. Bioorg Med Chem Lett. 2017 Jun 1; 27(11):2239-2258.

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