General Information of DFM (ID: F02778)
Name
Buprenorphine 8 mg tablet
Company
Actavis Pharma
Active Pharmaceutical Ingredient (API) Buprenorphine API Info click to show the detail info of this API
Opiate dependence ICD-11: 6C43 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E0F6AN DIG Info Kyselina citronova Acidulant ...
E00DHW DIG Info Lactose monohydrate Binding agent ...
E01UTP DIG Info Magnesium stearate lubricant
E0Q6DQ DIG Info Mannitol Diluent ...
E0NY5F DIG Info Sodium citrate dihydrate Alkalizing agent ...
E0L0MR DIG Info Sunset yellow FCF Colorant
E0FU1S DIG Info Vinylpyrrolidone Binding agent ...
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      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 for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Kyselina citronova
                    Biological Activity IC50 = 300000 nM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID FTO_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) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ALKB5_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 Magnesium stearate
                    Biological Activity Protein expression downregulation (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_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 (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Sunset yellow FCF
                    Biological Activity Inhibition ratio = 54.5 % (tested by experiment) [4]
                    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 Sunset yellow FCF
                    Biological Activity Ki = 68.4 uM (tested by experiment) [4]
                    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 Sunset yellow FCF
                    Biological Activity Ki = 74 uM (tested by experiment) [5]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
      Transmembrane channel/porin (TC/P)
            DBT Name: Glycine receptor alpha-1 (GLRA1) 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 Mannitol
                    Biological Activity EC50 = 12589.25 nM (estimated based on the structural similarity with CHEMBL604608 ) [6]
                    Structural Similarity Tanimoto coefficient = 0.804878049
                    Tested Species Homo sapiens (Human)
                    UniProt ID GLRA1_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
      Other protein families (OPF)
            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
            DBT Name: Thrombopoietin receptor (MPL) 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 Sunset yellow FCF
                    Biological Activity EC50 = 3000 nM (estimated based on the structural similarity with CHEMBL122867 ) [8]
                    Structural Similarity Tanimoto coefficient = 0.93081761
                    Tested Species Homo sapiens (Human)
                    UniProt ID TPOR_HUMAN
References
1 Structural basis for inhibition of the fat mass and obesity associated protein (FTO). J Med Chem. 2013 May 9; 56(9):3680-8.
2 Repair of methyl lesions in RNA by oxidative demethylation. Med Chem Comm. (2014) 5:1797-1803.
3 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
4 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.
5 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
6 Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. Bioorg Med Chem Lett. 2017 Jun 1; 27(11):2239-2258.
7 PubChem BioAssay data set.
8 Hydrazinonaphthalene and azonaphthalene thrombopoietin mimics are nonpeptidyl promoters of megakaryocytopoiesis. J Med Chem. 2001 Oct 25; 44(22):3730-45.

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