Details of the Drug Formulation (DFM)
General Information of DFM (ID: F07545) | |||||
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Name |
Estazolam 2 mg tablet
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Company |
Actavis Pharma
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Active Pharmaceutical Ingredient (API) | Estazolam | API Info click to show the detail info of this API | |||
Insomnia | ICD-11: 7A00 | Approved | |||
Drug Inactive Ingredient (DIGs) | |||||
DIG ID | DIG Info | DIG Name | DIG Functional Class | ||
E01OUP | DIG Info | Allura red AC dye | Colorant | ||
E0FH4N | DIG Info | Docusate sodium | Surfactant | ||
E00DHW | DIG Info | Lactose monohydrate | Binding agent ... | ||
E01UTP | DIG Info | Magnesium stearate | lubricant | ||
E0Y7PW | DIG Info | Sodium benzoate | Antimicrobial preservative ... | ||
E06VNY | DIG Info | Stearic acid | Emulsifying agent ... | ||
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM | ||||||
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G-protein coupled receptor (GPCR) | ||||||
DBT Name: Adenosine receptor A3 (AA3R) | 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 = 10 uM (tested by experiment) | [1] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | AA3R_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 | Allura red AC dye | |||||
Biological Activity | IC50 = 19 uM (tested by experiment) | [1] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | 5HT1A_HUMAN | |||||
DBT Name: Dopamine D1 receptor (DRD1) | 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 | Allura red AC dye | |||||
Biological Activity | IC50 = 29 uM (tested by experiment) | [1] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | DRD1_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) | [2] | ||||
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 (1) for Assessing the Biological Activity of the Studied DIG on This DBT | ||||||
Interacting DIG | Stearic acid | |||||
Biological Activity | IC50 > 500000 nM (tested by experiment) | [2] | ||||
Tested Species | Ovis aries (Sheep) | |||||
UniProt ID | PGH2_SHEEP | |||||
Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT | ||||||
Interacting DIG | Allura red AC dye | |||||
Biological Activity | IC50 = 26 uM (tested by experiment) | [1] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | PGH2_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 | Magnesium stearate | |||||
Biological Activity | Protein expression downregulation (tested by experiment) | [3] | ||||
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 | Docusate sodium | |||||
Biological Activity | IC50 = 65 uM (tested by experiment) | [4] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CP3A4_HUMAN | |||||
DBT Name: Cytochrome P450 2E1 (CYP2E1) | 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 | Docusate sodium | |||||
Biological Activity | EC50 = 141.8 uM (tested by experiment) | [4] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CP2E1_HUMAN | |||||
DBT Name: Cytochrome P450 2C9 (CYP2C9) | 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 | Docusate sodium | |||||
Biological Activity | EC50 = 203.3 uM (tested by experiment) | [4] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CP2C9_HUMAN | |||||
DBT Name: Mephenytoin 4-hydroxylase (CYP2C19) | 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 | Docusate sodium | |||||
Biological Activity | IC50 = 372 uM (tested by experiment) | [4] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CP2CJ_HUMAN | |||||
DBT Name: Debrisoquine 4-hydroxylase (CYP2D6) | 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 | Docusate sodium | |||||
Biological Activity | IC50 = 95.5 uM (tested by experiment) | [4] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CP2D6_HUMAN | |||||
DBT Name: Cytochrome P450 3A5 (CYP3A5) | 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 | Docusate sodium | |||||
Biological Activity | EC50 = 195.8 uM (tested by experiment) | [4] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CP3A5_HUMAN | |||||
Hydrolase (HDase) | ||||||
DBT Name: Acetylcholinesterase (ACHE) | 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 | Allura red AC dye | |||||
Biological Activity | IC50 > 10 uM (tested by experiment) | [1] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | ACES_HUMAN | |||||
DBT Name: Histone deacetylase (HDAC) | 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 | Docusate sodium | |||||
Biological Activity | IC50 = 9600 nM (estimated based on the structural similarity with CHEMBL271677 ) | [5] | ||||
Structural Similarity | Tanimoto coefficient = 0.824561404 | |||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | HDAC1_HUMAN ; HDAC2_HUMAN ; HDAC3_HUMAN ; HDAC4_HUMAN ; HDAC5_HUMAN ; HDAC6_HUMAN ; HDAC7_HUMAN ; HDAC8_HUMAN ; HDAC9_HUMAN | |||||
DBT Name: Protein-tyrosine phosphatase 1B (PTPN1) | 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 | Allura red AC dye | |||||
Biological Activity | IC50 = 33000 nM (tested by experiment) | [6] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | PTN1_HUMAN | |||||
Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT | ||||||
Interacting DIG | Allura red AC dye | |||||
Biological Activity | IC50 = 410000 nM (tested by experiment) | [6] | ||||
Tested Species | Saccharomyces cerevisiae (Yeast) | |||||
UniProt ID | PTP1_YEAST | |||||
DBT Name: Phosphodiesterase 3A (PDE3A) | 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 = 3.1 uM (tested by experiment) | [1] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | PDE3A_HUMAN | |||||
Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT | ||||||
Interacting DIG | Allura red AC dye | |||||
Biological Activity | IC50 = 17 uM (tested by experiment) | [1] | ||||
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 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) | [1] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | PDE4D_HUMAN | |||||
Lyase/isomerase/ligase (L/I/G) | ||||||
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 | Sodium benzoate | |||||
Biological Activity | Ki = 30000 nM (tested by experiment) | [7] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CAH2_HUMAN | |||||
DBT Name: Carbonic anhydrase IV (CA4) | 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 benzoate | |||||
Biological Activity | Ki = 74700 nM (tested by experiment) | [7] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CAH4_HUMAN | |||||
DBT Name: Cholesterol 25-hydroxylase (CYP1A2) | 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 | Docusate sodium | |||||
Biological Activity | EC50 = 147.4 uM (tested by experiment) | [4] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CP1A2_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 | Allura red AC dye | |||||
Biological Activity | Inhibition ratio = 96.52 % (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 | Allura red AC dye | |||||
Biological Activity | Ki = 2.59 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 | Allura red AC dye | |||||
Biological Activity | Ki = 4.7 uM (tested by experiment) | [1] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | SO2B1_HUMAN | |||||
Experiment (4) for Assessing the Biological Activity of the Studied DIG on This DBT | ||||||
Interacting DIG | Docusate sodium | |||||
Biological Activity | Inhibition ratio = 87.8 % (tested by experiment) | [8] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | SO2B1_HUMAN | |||||
Experiment (5) for Assessing the Biological Activity of the Studied DIG on This DBT | ||||||
Interacting DIG | Docusate sodium | |||||
Biological Activity | Ki = 2.76 uM (tested by experiment) | [8] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | SO2B1_HUMAN | |||||
Experiment (6) for Assessing the Biological Activity of the Studied DIG on This DBT | ||||||
Interacting DIG | Docusate sodium | |||||
Biological Activity | Ki = 2.3 uM (tested by experiment) | [1] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | SO2B1_HUMAN | |||||
Transmembrane channel/porin (TC/P) | ||||||
DBT Name: GABA(A) receptor alpha-1 (GABRA1) | 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 | Allura red AC dye | |||||
Biological Activity | IC50 = 22 uM (tested by experiment) | [1] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | GBRA1_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 | Allura red AC dye | |||||
Biological Activity | IC50 = 28 uM (tested by experiment) | [1] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | ANDR_HUMAN | |||||
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 | Stearic acid | |||||
Biological Activity | IC50 = 16 uM (tested by experiment) | [1] | ||||
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 | Allura red AC dye | |||||
Biological Activity | IC50 = 15 uM (tested by experiment) | [1] | ||||
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) | [9] | ||||
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) | [9] | ||||
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) | [9] | ||||
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 | Allura red AC dye | |||||
Biological Activity | IC50 = 30 uM (tested by experiment) | [1] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | PRGR_HUMAN | |||||
Other protein families (OPF) | ||||||
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 | Allura red AC dye | |||||
Biological Activity | EC50 = 300 nM (estimated based on the structural similarity with CHEMBL123373 ) | [10] | ||||
Structural Similarity | Tanimoto coefficient = 0.925714286 | |||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | TPOR_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 | Docusate sodium | |||||
Biological Activity | IC50 = 154000 nM (estimated based on the structural similarity with CHEMBL271677 ) | [5] | ||||
Structural Similarity | Tanimoto coefficient = 0.824561404 | |||||
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) | [11] | ||||
Tested Species | Homo sapiens (Human) | |||||
Cellosaurus ID | CVCL_0218 | |||||
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) | [11] | ||||
Tested Species | Homo sapiens (Human) | |||||
Cellosaurus ID | CVCL_0320 | |||||
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