Details of the Drug Formulation (DFM)

General Information of DFM (ID: F23618)
Name
Amcinonide 0.1% ointment
Company
Astellas
Active Pharmaceutical Ingredient (API) Amcinonide 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
E0NY1O DIG Info Benzyl alcohol Antimicrobial preservative ...
E0QV6C DIG Info Butylhydroxyanisole Antimicrobial preservative ...
E0F6AN DIG Info Kyselina citronova Acidulant ...
E0U9NK DIG Info Propyl gallate Antimicrobial preservative ...
E0M1JK DIG Info Propylene glycol Antimicrobial preservative ...
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      G-protein coupled receptor (GPCR)
            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 Butylhydroxyanisole
                    Biological Activity IC50 = 19 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ACM1_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 Butylhydroxyanisole
                    Biological Activity IC50 = 19 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ADA1A_HUMAN
      Oxidoreductase (ORase)
            DBT Name: N1-methyl adenine demethylase (FTO) 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 Kyselina citronova
                    Biological Activity IC50 = 300000 nM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID FTO_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Propyl gallate
                    Biological Activity Ki = 3 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID FTO_HUMAN
            DBT Name: Arachidonate 5-lipoxygenase (ALOX5) 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 Propyl gallate
                    Biological Activity Ki = 0.43 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID LOX5_HUMAN
            DBT Name: Indoleamine 2,3-dioxygenase 1 (IDO1) 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 Benzyl alcohol
                    Biological Activity IC50 = 1400 nM (estimated based on the structural similarity with CHEMBL3763371 ) [3]
                    Structural Similarity Tanimoto coefficient = 0.848101266
                    Tested Species Homo sapiens (Human)
                    UniProt ID I23O1_HUMAN
            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 (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Propyl gallate
                    Biological Activity IC50 = 7.2 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PGH2_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Butylhydroxyanisole
                    Biological Activity IC50 = 2.6 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PGH2_HUMAN
            DBT Name: RNA demethylase ALKBH5 (ALKB5) 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 Kyselina citronova
                    Biological Activity IC50 = 488000 nM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ALKB5_HUMAN
            DBT Name: Lysine-specific demethylase 4C (KDM4C) 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 Propyl gallate
                    Biological Activity Ki = 39 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID KDM4C_HUMAN
            DBT Name: Tyrosine 3-monooxygenase (TH) 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 Propyl gallate
                    Biological Activity Ki = 1.9 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID TY3H_HUMAN
            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) [5]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
      Cation-dependent O-methyltransferase
            DBT Name: Catechol O-methyltransferase (COMT) 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 Propyl gallate
                    Biological Activity Ki = 0.015 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID COMT_HUMAN
      Hydrolase (HDase)
            DBT Name: Phosphodiesterase 4D (PDE4D) 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 Propyl gallate
                    Biological Activity IC50 = 26 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PDE4D_HUMAN
      Potential-driven transporter (PDT)
            DBT Name: Solute carrier SLCO2B1 (OATPB) 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 Propyl gallate
                    Biological Activity Inhibition ratio = 29.6 % (tested by experiment) [6]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
      Nuclear receptor (NR)
            DBT Name: Factor HNF-4-alpha (HNF4A) 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 Kyselina citronova
                    Biological Activity IC50 = 39869 nM (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID HNF4A_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 Butylhydroxyanisole
                    Biological Activity IC50 = 29 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PRGR_HUMAN
      Other protein families (OPF)
            DBT Name: Anthrax toxin receptor 2 (CMG-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 Propyl gallate
                    Biological Activity IC50 > 300000 nM (tested by experiment) [8]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ANTR2_HUMAN
            DBT Name: Perilipin-1 (PLIN1) 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 Kyselina citronova
                    Biological Activity IC50 = 3708 nM (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PLIN1_HUMAN
References
1 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
2 Structural basis for inhibition of the fat mass and obesity associated protein (FTO). J Med Chem. 2013 May 9; 56(9):3680-8.
3 O-alkylhydroxylamines as rationally-designed mechanism-based inhibitors of indoleamine 2,3-dioxygenase-1. Eur J Med Chem. 2016 Jan 27; 108:564-576.
4 Repair of methyl lesions in RNA by oxidative demethylation. Med Chem Comm. (2014) 5:1797-1803.
5 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
6 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.
7 PubChem BioAssay data set.
8 1,2,3,4,6-Penta-O-galloyl--D-glucopyranose inhibits angiogenesis via inhibition of capillary morphogenesis gene 2. J Med Chem. 2013 Mar 14; 56(5):1940-5.

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