Details of the Drug Formulation (DFM)

General Information of DFM (ID: F04449)
Name
Clarithromycin 500 mg tablet
Company
Mayne Pharma
Active Pharmaceutical Ingredient (API) Clarithromycin API Info click to show the detail info of this API
Pneumocystis pneumonia ICD-11: CA40 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E09YYN DIG Info Eisenoxyd Colorant
E0M0IE DIG Info Ferric hydroxide oxide yellow Colorant
E02FBG DIG Info Ferrosoferric oxide Colorant
E0F6AN DIG Info Kyselina citronova Acidulant ...
E00DHW DIG Info Lactose monohydrate Binding agent ...
E0G3NO DIG Info Polyethylene glycol 4000 Coating agent ...
E01UTV DIG Info Silicon dioxide Anticaking agent ...
E0RS6F DIG Info Sodium stearyl fumarate lubricant
E05BSD DIG Info Titanium dioxide Coating agent ...
E08VAJ DIG Info Vanillin Flavoring 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: Aldehyde dehydrogenase 5A1 (ALDH5A1) 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 Vanillin
                    Biological Activity IC50 = 15600 nM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SSDH_HUMAN
            DBT Name: Albendazole monooxygenase (CYP3A4) 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 Polyethylene glycol 4000
                    Biological Activity Inhibition ratio < 40 % (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Silicon dioxide
                    Biological Activity Protein expression downregulation (tested by experiment) [5]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
      Transferase (TFase)
            DBT Name: GABA transaminase (ABAT) 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 Vanillin
                    Biological Activity IC50 = 17100 nM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID GABT_HUMAN
      Hydrolase (HDase)
            DBT Name: Pancreatic lipase (PTL) 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 Vanillin
                    Biological Activity IC50 = 74400 nM (tested by experiment) [6]
                    Tested Species Sus scrofa (Pig)
                    UniProt ID LIPP_PIG
      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 Vanillin
                    Biological Activity IC50 > 426579.52 nM (tested by experiment) [7]
                    Tested Species Rattus norvegicus (Rat)
                    UniProt ID ANDR_RAT
            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) [8]
                    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) [8]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PLIN1_HUMAN
      Cell line (CELL)
            DBT Name: Leukemia K562 cells (K562) 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 stearyl fumarate
                    Biological Activity IC50 = 20.2 ug.mL-1 (estimated based on the structural similarity with CHEMBL3126829 ) [9]
                    Structural Similarity Tanimoto coefficient = 0.75
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0004
            DBT Name: Breast cancer MCF7 cells (MCF7) 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 stearyl fumarate
                    Biological Activity IC50 = 60 ug.mL-1 (estimated based on the structural similarity with CHEMBL3126829 ) [9]
                    Structural Similarity Tanimoto coefficient = 0.75
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0031
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 Inhibition of GABA shunt enzymes' activity by 4-hydroxybenzaldehyde derivatives. Bioorg Med Chem Lett. 2006 Feb; 16(3):592-5.
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 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
6 Enhancement of pancreatic lipase inhibitory activity of curcumin by radiolytic transformation. Bioorg Med Chem Lett. 2011 Mar 1; 21(5):1512-4.
7 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.
8 PubChem BioAssay data set.
9 Synthesis and evaluation of (-)-Massoialactone and analogues as potential anticancer and anti-inflammatory agents. Eur J Med Chem. 2014 Apr 9; 76:291-300.

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