General Information of DFM (ID: F23306)
Name
Tetracaine 1% cream
Company
Burn Solution Foundations
Active Pharmaceutical Ingredient (API) Tetracaine API Info click to show the detail info of this API
Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E09FSQ DIG Info Diazolidinyl urea Antimicrobial preservative
E0JW9W DIG Info Eucalyptol Flavoring agent
E09ZWX DIG Info Lauric diethanolamide Surfactant ...
E0V6QI DIG Info methylparaben Antimicrobial preservative
E0M1JK DIG Info Propylene glycol Antimicrobial preservative ...
E0X6QO DIG Info Propylparaben sodium Antimicrobial preservative
E0F9TP DIG Info Sodium lauryl sulfate Emulsifying agent ...
E06VNY DIG Info Stearic acid Emulsifying agent ...
E0EZ1L DIG Info Trolamine Alkalizing agent ...
E0H2SC DIG Info Water Solvent
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      G-protein coupled receptor (GPCR)
            DBT Name: Serotonin receptor 3A (5HT3A) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Eucalyptol
                    Biological Activity IC50 = 257039.58 nM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID 5HT3A_HUMAN
            DBT Name: Adenosine receptor A3 (AA3R) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Stearic acid
                    Biological Activity IC50 = 10 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID AA3R_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Sodium lauryl sulfate
                    Biological Activity IC50 = 15 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID AA3R_HUMAN
            DBT Name: Muscarinic receptor M1 (ACM1) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Sodium lauryl sulfate
                    Biological Activity IC50 = 29 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ACM1_HUMAN
            DBT Name: Serotonin receptor 1A (5HT1A) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Sodium lauryl sulfate
                    Biological Activity IC50 = 15 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID 5HT1A_HUMAN
            DBT Name: Alpha-1A adrenoceptor (ADA1A) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Sodium lauryl sulfate
                    Biological Activity IC50 = 15 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ADA1A_HUMAN
            DBT Name: Dopamine D3 receptor (DRD3) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Sodium lauryl sulfate
                    Biological Activity IC50 = 18 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID DRD3_HUMAN
            DBT Name: Thromboxane A2 receptor (TBXA2R) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Sodium lauryl sulfate
                    Biological Activity IC50 > 10 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID TA2R_HUMAN
      Oxidoreductase (ORase)
            DBT Name: Prostaglandin G/H synthase 1 (COX-1) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Stearic acid
                    Biological Activity IC50 > 500000 nM (tested by experiment) [3]
                    Tested Species Bos taurus (Bovine)
                    UniProt ID PGH1_BOVIN
            DBT Name: Prostaglandin G/H synthase 2 (COX-2) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Stearic acid
                    Biological Activity IC50 > 500000 nM (tested by experiment) [3]
                    Tested Species Ovis aries (Sheep)
                    UniProt ID PGH2_SHEEP
            DBT Name: Albendazole monooxygenase (CYP3A4) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Propylene glycol
                    Biological Activity Inhibition ratio < 20 % (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
      Transferase (TFase)
            DBT Name: Choline acetylase (CHAT) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Trolamine
                    Biological Activity IC50 < 200000 nM (estimated based on the structural similarity with CHEMBL1135 ) [5]
                    Structural Similarity Tanimoto coefficient = 0.896551724
                    Tested Species Rattus norvegicus (Rat)
                    UniProt ID CLAT_RAT
      Hydrolase (HDase)
            DBT Name: Soluble epoxide hydrolase (EPHX2) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Sodium lauryl sulfate
                    Biological Activity IC50 = 5500 nM (tested by experiment) [6]
                    Tested Species Homo sapiens (Human)
                    UniProt ID HYES_HUMAN
            DBT Name: Phosphodiesterase 3A (PDE3A) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Stearic acid
                    Biological Activity IC50 = 3.1 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PDE3A_HUMAN
            DBT Name: Phosphodiesterase 4D (PDE4D) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Stearic acid
                    Biological Activity IC50 = 6.7 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PDE4D_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Sodium lauryl sulfate
                    Biological Activity IC50 = 23 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PDE4D_HUMAN
      Lyase/isomerase/ligase (L/I/G)
            DBT Name: Carbonic anhydrase I (CA1) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG methylparaben
                    Biological Activity Ki = 2600 nM (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH1_HUMAN
            DBT Name: Carbonic anhydrase II (CA2) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG methylparaben
                    Biological Activity Ki = 3400 nM (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH2_HUMAN
            DBT Name: Carbonic anhydrase IX (CA9) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG methylparaben
                    Biological Activity Ki = 5500 nM (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH9_HUMAN
            DBT Name: Carbonic anhydrase VII (CA7) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG methylparaben
                    Biological Activity Ki = 780 nM (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH7_HUMAN
            DBT Name: Carbonic anhydrase XII (CA12) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG methylparaben
                    Biological Activity Ki = 820 nM (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH12_HUMAN
            DBT Name: Carbonic anhydrase XIV (CA14) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG methylparaben
                    Biological Activity Ki = 4100 nM (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH14_HUMAN
      Potential-driven transporter (PDT)
            DBT Name: Solute carrier SLCO1B1 (OATP-C) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Sodium lauryl sulfate
                    Biological Activity Ki = 2.9 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO1B1_HUMAN
            DBT Name: Solute carrier SLCO2B1 (OATPB) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Sodium lauryl sulfate
                    Biological Activity Inhibition ratio = 88.6 % (tested by experiment) [8]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Sodium lauryl sulfate
                    Biological Activity Ki = 1.98 uM (tested by experiment) [8]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
               Experiment (3) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Sodium lauryl sulfate
                    Biological Activity Ki = 2.8 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
      Transmembrane channel/porin (TC/P)
            DBT Name: Vanilloid receptor 1 (TrpV1) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Lauric diethanolamide
                    Biological Activity EC50 = 600 nM (estimated based on the structural similarity with CHEMBL206425 ) [9]
                    Structural Similarity Tanimoto coefficient = 0.927272727
                    Tested Species Homo sapiens (Human)
                    UniProt ID TRPV1_HUMAN
      Nuclear receptor (NR)
            DBT Name: Androgen receptor (AR) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG methylparaben
                    Biological Activity IC50 > 426579.52 nM (tested by experiment) [10]
                    Tested Species Rattus norvegicus (Rat)
                    UniProt ID ANDR_RAT
            DBT Name: Estrogen receptor alpha (ESR1) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Propylparaben sodium
                    Biological Activity EC50 = 38200 nM (estimated based on the structural similarity with CHEMBL15841 ) [11]
                    Structural Similarity Tanimoto coefficient = 0.946428571
                    Tested Species Homo sapiens (Human)
                    UniProt ID ESR1_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Stearic acid
                    Biological Activity IC50 = 16 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ESR1_HUMAN
            DBT Name: PPAR-alpha (PPARA) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Stearic acid
                    Biological Activity IC50 = 1100 nM (tested by experiment) [12]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PPARA_HUMAN
            DBT Name: PPAR-delta (PPARD) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Stearic acid
                    Biological Activity IC50 = 6000 nM (tested by experiment) [12]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PPARD_HUMAN
            DBT Name: PPAR-gamma (PPARG) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Stearic acid
                    Biological Activity IC50 = 30000 nM (tested by experiment) [12]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PPARG_HUMAN
            DBT Name: Progesterone receptor (PGR) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Sodium lauryl sulfate
                    Biological Activity IC50 = 15 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PRGR_HUMAN
      Cell line (CELL)
            DBT Name: Lung cancer A-549 cells (A-549) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG methylparaben
                    Biological Activity IC50 > 20 ug.mL-1 (tested by experiment) [13]
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0023
            DBT Name: Colon cancer COLO 205 cells (COLO 205) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Stearic acid
                    Biological Activity IC50 > 200000 nM (tested by experiment) [14]
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0218
            DBT Name: Colon cancer HCT-116 cells (HCT-116) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Sodium lauryl sulfate
                    Biological Activity IC50 > 100000 nM (tested by experiment) [15]
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0291
            DBT Name: Hepatoblastoma HepG2 cells (HepG2) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG methylparaben
                    Biological Activity IC50 > 20 ug.mL-1 (tested by experiment) [13]
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0027
            DBT Name: Colon cancer HT-29 cells (HT-29) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Stearic acid
                    Biological Activity IC50 > 200000 nM (tested by experiment) [14]
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0320
            DBT Name: Cervical cancer KB cells (KB) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG methylparaben
                    Biological Activity IC50 > 200000 nM (tested by experiment) [16]
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0372
            DBT Name: Carcinoma MDA-MB-231 cells (MDA-MB-231) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG methylparaben
                    Biological Activity IC50 > 20 ug.mL-1 (tested by experiment) [13]
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0062
            DBT Name: Leukemia RAW264.7 cells (RAW264.7) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Sodium lauryl sulfate
                    Biological Activity IC50 > 100000 nM (tested by experiment) [15]
                    Tested Species Mus musculus (Mouse)
                    Cellosaurus ID CVCL_0493
References
1 Progress in the discovery of small molecule modulators of the Cys-loop superfamily receptors. Bioorg Med Chem Lett. 2017 Aug 1; 27(15):3207-3218.
2 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
3 Cox-2 inhibitory effects of naturally occurring and modified fatty acids. J Nat Prod. 2001 Jun; 64(6):745-9.
4 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
5 Chemistry and biological activities of N,N-dimethylaminoethyl acrylate, a choline acetyltransferase inhibitor. J Med Chem. 1976 Feb; 19(2):300-3.
6 Discovery of the First in Vivo Active Inhibitors of the Soluble Epoxide Hydrolase Phosphatase Domain. J Med Chem. 2019 Sep 26; 62(18):8443-8460.
7 Mono-/dihydroxybenzoic acid esters and phenol pyridinium derivatives as inhibitors of the mammalian carbonic anhydrase isoforms I, II, VII, IX, XII and XIV. Bioorg Med Chem. 2013 Mar 15; 21(6):1564-9.
8 Bacterial metabolism rescues the inhibition of intestinal drug absorption by food and drug additives. Proc Natl Acad Sci U S A. 2020 Jul 7;117(27):16009-16018.
9 Oxyhomologues of anandamide and related endolipids: chemoselective synthesis and biological activity. J Med Chem. 2006 Apr 6; 49(7):2333-8.
10 Impact of induced fit on ligand binding to the androgen receptor: a multidimensional QSAR study to predict endocrine-disrupting effects of environmental chemicals. J Med Chem. 2005 Sep 8; 48(18):5666-74.
11 Discovery of natural estrogen receptor modulators with structure-based virtual screening. Bioorg Med Chem Lett. 2013 Jun 1; 23(11):3329-33.
12 Molecular properties of fatty acids related to PPAR binding and metabolic diseases. Med Chem Res (2013) 22:3126-3133.
13 Bioactive Phenolic Components from the Twigs of Atalantia buxifolia. J Nat Prod. 2018 Jul 27; 81(7):1534-1539.
14 Liposomal formulation of retinoids designed for enzyme triggered release. J Med Chem. 2010 May 13; 53(9):3782-92.
15 Synthesis of amphiphilic, chalcogen-based redox modulators with in vitro cytotoxic activity against cancer cells, macrophages and microbes. Med Chem Comm. (2014) 5:25-31.
16 Synthesis and biological evaluation of 12 allenic aromatic ethers. Bioorg Med Chem Lett. 2007 May 15; 17(10):2785-8.

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