Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0EM4V)
Name
Wasabi receptor (TRPA1)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Transformation-sensitive protein p120; ANKTM1; Ankyrin-like with transmembrane domains protein 1; TRPA1; Transformation-sensitive protein p120
Family Transmembrane channel/porin (TC/P)  >>  Transient receptor potential Ca channel (TRP-CC)
Organism
Homo sapiens (Human)
Gene Name TRPA1 Gene ID
8989
UniProt ID TRPA1_HUMAN (click to find more protein-related data of this DBT)
TTD ID T84040 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MKRSLRKMWRPGEKKEPQGVVYEDVPDDTEDFKESLKVVFEGSAYGLQNFNKQKKLKRCD
DMDTFFLHYAAAEGQIELMEKITRDSSLEVLHEMDDYGNTPLHCAVEKNQIESVKFLLSR
GANPNLRNFNMMAPLHIAVQGMNNEVMKVLLEHRTIDVNLEGENGNTAVIIACTTNNSEA
LQILLKKGAKPCKSNKWGCFPIHQAAFSGSKECMEIILRFGEEHGYSRQLHINFMNNGKA
TPLHLAVQNGDLEMIKMCLDNGAQIDPVEKGRCTAIHFAATQGATEIVKLMISSYSGSVD
IVNTTDGCHETMLHRASLFDHHELADYLISVGADINKIDSEGRSPLILATASASWNIVNL
LLSKGAQVDIKDNFGRNFLHLTVQQPYGLKNLRPEFMQMQQIKELVMDEDNDGCTPLHYA
CRQGGPGSVNNLLGFNVSIHSKSKDKKSPLHFAASYGRINTCQRLLQDISDTRLLNEGDL
HGMTPLHLAAKNGHDKVVQLLLKKGALFLSDHNGWTALHHASMGGYTQTMKVILDTNLKC
TDRLDEDGNTALHFAAREGHAKAVALLLSHNADIVLNKQQASFLHLALHNKRKEVVLTII
RSKRWDECLKIFSHNSPGNKCPITEMIEYLPECMKVLLDFCMLHSTEDKSCRDYYIEYNF
KYLQCPLEFTKKTPTQDVIYEPLTALNAMVQNNRIELLNHPVCKEYLLMKWLAYGFRAHM
MNLGSYCLGLIPMTILVVNIKPGMAFNSTGIINETSDHSEILDTTNSYLIKTCMILVFLS
SIFGYCKEAGQIFQQKRNYFMDISNVLEWIIYTTGIIFVLPLFVEIPAHLQWQCGAIAVY
FYWMNFLLYLQRFENCGIFIVMLEVILKTLLRSTVVFIFLLLAFGLSFYILLNLQDPFSS
PLLSIIQTFSMMLGDINYRESFLEPYLRNELAHPVLSFAQLVSFTIFVPIVLMNLLIGLA
VGDIAEVQKHASLKRIAMQVELHTSLEKKLPLWFLRKVDQKSTIVYPNKPRSGGMLFHIF
CFLFCTGEIRQEIPNADKSLEMEILKQKYRLKDLTFLLEKQHELIKLIIQKMEIISETED
DDSHCSFQDRFKKEQMEQRNSRWNTVLRAVKAKTHHLEP
Function
Receptor-activated non-selective cation channel involved in detection of pain and possibly also in cold perception and inner ear function. Has a central role in the pain response to endogenous inflammatory mediators and to a diverse array of volatile irritants, such as mustard oil, garlic and acrolein, an irritant from tears gas and vehicule exhaust fumes. Acts also as a ionotropic cannabinoid receptor by being activated by delta(9)- tetrahydrocannabinol (THC), the psychoactive component of marijuana.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Cis-3-hexenyl acetate 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
Flavoring agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 13300 nM (estimated based on the structural similarity with CHEMBL2268549 ) [1]
                   Structural Similarity Tanimoto coefficient = 0.755555556
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID TRPA1_RAT
          DIG Name: Ethyl isovalerate 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
Flavoring agent
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 8511.38 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID TRPA1_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 61000 nM (tested by experiment) [2]
                   Tested Species Mus musculus (Mouse)
                   UniProt ID TRPA1_MOUSE
          DIG Name: Levomenthol 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
Flavoring agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 96000 nM (tested by experiment) [3]
                   Tested Species Homo sapiens (Human)
                   UniProt ID TRPA1_HUMAN
          DIG Name: Menthol 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
Flavoring agent
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 30000 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID TRPA1_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 56000 nM (tested by experiment) [4]
                   Tested Species Mus musculus (Mouse)
                   UniProt ID TRPA1_MOUSE
          DIG Name: Atomic sulfur 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
Antimicrobial preservative
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 116000 nM (estimated based on the structural similarity with CHEMBL2105487 ) [5]
                   Structural Similarity Tanimoto coefficient = 1
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID TRPA1_RAT
          DIG Name: Cinnamaldehyde 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
Flavoring agent
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 8511.38 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID TRPA1_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 61000 nM (tested by experiment) [2]
                   Tested Species Mus musculus (Mouse)
                   UniProt ID TRPA1_MOUSE
          DIG Name: Thimerosal 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
Antimicrobial preservative
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 800 nM (estimated based on the structural similarity with CHEMBL23293 ) [2]
                   Structural Similarity Tanimoto coefficient = 0.859813084
                   Tested Species Homo sapiens (Human)
                   UniProt ID TRPA1_HUMAN
          DIG Name: Thymol 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
Antioxidant; Flavoring agent; Penetration agent
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 6000 nM (tested by experiment) [6]
                   Tested Species Homo sapiens (Human)
                   UniProt ID TRPA1_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 125400 nM (tested by experiment) [6]
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID TRPA1_RAT
References
1 Effect of acyclic monoterpene alcohols and their derivatives on TRP channels. Bioorg Med Chem Lett. 2014 Dec 1; 24(23):5507-11.
2 N-Cinnamoylanthranilates as human TRPA1 modulators: Structure-activity relationships and channel binding sites. Eur J Med Chem. 2019 May 15; 170:141-156.
3 Identification of a Novel TRPM8 Agonist from Nutmeg: A Promising Cooling Compound. ACS Med Chem Lett. 2017 May 31; 8(7):715-719.
4 Transient receptor potential ankyrin 1 (TRPA1) channel as emerging target for novel analgesics and anti-inflammatory agents. J Med Chem. 2010 Jul 22; 53(14):5085-107.
5 Cytoprotective effects of hydrogen sulfide-releasing N-methyl-D-aspartate receptor antagonists are mediated by intracellular sulfane sulfur. Medchemcomm. 2014 Oct 1; 5(10):1577-1583.
6 Modulation of thermo-transient receptor potential (thermo-TRP) channels by thymol-based compounds. Bioorg Med Chem Lett. 2012 May 15; 22(10):3535-9.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhang and Dr. Mou.