General Information of DFM (ID: F18028)
Name	Promethazine 50 mg tablet
Company	McKesson
Active Pharmaceutical Ingredient (API)	Promethazine		API Info click to show the detail info of this API
	Allergic rhinitis		ICD-11: CA08	Approved
Drug Inactive Ingredient (DIGs)
	DIG ID	DIG Info	DIG Name	DIG Functional Class
	E06RUT	DIG Info	D&C red no. 27	Colorant
	E01VHX	DIG Info	D&C red no. 30	Colorant
	E00DHW	DIG Info	Lactose monohydrate	Binding agent ...
	E01UTP	DIG Info	Magnesium stearate	lubricant

Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
Oxidoreductase (ORase)
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)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	CP3A4_HUMAN
Transferase (TFase)
DBT Name: Arginine methyltransferase 1 (PRMT1)				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	D&C red no. 27
Biological Activity	IC50 = 1400 nM (estimated based on the structural similarity with CHEMBL376503 )					[2]
Structural Similarity	Tanimoto coefficient = 0.781914894
Tested Species	Homo sapiens (Human)
UniProt ID	ANM1_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	D&C red no. 27
Biological Activity	Inhibition ratio = 69 % (tested by experiment)					[3]
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	D&C red no. 27
Biological Activity	Ki = 1 uM (tested by experiment)					[3]
Tested Species	Homo sapiens (Human)
UniProt ID	SO2B1_HUMAN
Other protein families (OPF)
DBT Name: Heat shock factor 1 (HSF1)				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	D&C red no. 30
Biological Activity	EC50 = 9054 nM (estimated based on the structural similarity with CHEMBL1339303 )					[4]
Structural Similarity	Tanimoto coefficient = 0.776859504
Tested Species	Mus musculus (Mouse)
UniProt ID	HSF1_MOUSE
DBT Name: Nuclear factor-kappa B (NFKB)				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	D&C red no. 30
Biological Activity	EC50 = 122869 nM (estimated based on the structural similarity with CHEMBL1339303 )					[4]
Structural Similarity	Tanimoto coefficient = 0.776859504
Tested Species	Homo sapiens (Human)
UniProt ID	NFKB1_HUMAN ; NFKB2_HUMAN ; TF65_HUMAN

References
1	Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
2	Small molecule inhibitors of histone arginine methyltransferases: homology modeling, molecular docking, binding mode analysis, and biological evaluations. J Med Chem. 2007 Mar 22; 50(6):1241-53.
3	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.
4	PubChem BioAssay data set.

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